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NOLVADEX D :
Nolvadex D tablets contain the active ingredient tamoxifen citrate, which is a type of medicine known as an 'anti-oestrogen'. (NB. Tamoxifen is also available without a brand name, ie as the generic medicine.) Tamoxifen is mainly used to treat women with breast cancers that respond to the female sex hormone, oestrogen.
Most breast cancers are sensitive to oestrogen, and their growth is increased in the presence of this hormone. Oestrogen binds to oestrogen receptors on the breast cancer cells and causes changes within the cells that result in faster growth of the cancer. Breast cancers that are sensitive to oestrogen are called oestrogen receptor positive cancers.
Tamoxifen works by blocking the oestrogen receptors, thereby blocking the effect of oestrogen on the cancer. This starves the breast cancer cells and stops them from growing.
Tamoxifen helps prevent breast cancer from spreading to other areas of the body and also reduces risk of developing cancer in the other breast.
Tamoxifen is also used in the treatment of female infertility that is caused by problems with ovulation. Again, it acts by blocking oestrogen receptors, this time in a part of the brain called the hypothalamus. The effect of this is an increase in the levels of the hormones that control the development and release of an egg. These hormones are released from the pituitary gland and are known as follicle stimulating hormone (FSH) and luteinising hormone (LH). FSH stimulates the ovaries and LH causes the release of an egg from the ovaries (ovulation).
In the normal menstrual cycle, oestrogen acts on receptors in the hypothalamus after ovulation. This causes the pituitary gland to stop releasing FSH and LH. As tamoxifen blocks the oestrogen receptors in the hypothalamus, it prevents this action of oestrogen. FSH and LH levels therefore increase, which increases the chances of egg development and ovulation.
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Complex drug delivery composition and method for treating cancerThe present invention relates to compositions and methods for producing a complex drug delivery system which specifically targets cancer cells, has an increase in cellular uptake, is cytotoxic, and suppresses antiapoptotic cellular defenses....
Compositions and methods for treating vascular permeability
The present invention provides methods and composition for the treatment and diagnosis of disorders associated with excessive vascular permeability and edema....
Human immunosuppressive protein
A method for purifying an immunosuppressant protein (HISP) has the steps of obtaining supernatant from hNT cells; exposing the supernatant to preparative polyacrylamide gel electrophoresis to produce 20 isoelectric fractions, including active isoelectric fraction #10; placing the active isoelectric fraction on a Blue Sepharose column to bind albumin; and collecting...
Peptides having affinity for body surfaces
Peptides having affinity for a body surface are provided. The peptides comprise a body surface-binding peptide block and at least one charged, terminal peptide block. These peptides have enhanced affinity for body surfaces and deposit more rapidly onto body surfaces than peptides lacking the charged terminal groups. The peptides are...
Lowering serum lipids
The present invention relates to a method for lowering serum lipids, eg. triglycerides and/or cholesterol in a subject comprising administering a GLP-1 agonist to said subject....
Methods and pharmaceutical compositions for healing wounds
A pharmaceutical composition and method for inducing or accelerating a healing process of a skin wound are described. The pharmaceutical composition contains, as an active ingredient, a therapeutically effective amount of at least one agent for modulating PKC production and/or activation, and a pharmaceutically acceptable carrier. The method is effected...
Modified amino acid for the inhibition of platelet aggregation
A method of inhibiting blood platelet aggregation in a mammal is provided. The method comprises the administration of a platelet aggregation inhibiting amount of a modified amino acid or pharmaceutically acceptable salt thereof....
Pharmaceutical compositions containing insulin and insulinotropic peptide
Pharmaceutical composition for parenteral administration comprising insulin peptide an insulinotropic peptide and a ligand for the Hisb10 anion site....
Glycosylation of peptides via o-linked glycosylation sequences
The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries...
Methods for promoting hair growth
This disclosure reveals that cyclic corticotrophin releasing factor (CRF) antagonist peptides (such as astressin B, its functional fragments, and their derivatives) induce hair growth and prevent hair loss in vivo. This important discovery enables, for instance, methods of promoting hair growth, and methods of treating hair loss (such as the...
Novel peptides for use in the treatment of obesity
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the...
recombinant protein having an anti-cancer effect, its encoding gene and uses thereof
The present invention discloses a recombinant protein having an anti-cancer effect, its encoding gene and uses thereof. The recombinant protein having an anti-cancer effect provided by the present invention is one selected from the group consisting of: 1) a protein having the amino acid sequence of SEQ ID No:2 shown...
Chimeric proteins with phosphatidylserine binding domains
Chimeric proteins comprising soluble Tissue Factor (sTF) and another subunit (e.g., annexin V) are described. The proteins promote blood clotting and/or inhibit cancer by targeting sTF to specific receptors such as phosphatidylserine (PS) on activated cells. These chimeric proteins are useful in treating patients with excessive bleeding due to inborn...
Compositions and methods for treatment of cancer or neurodegenerative disease with peptide based microtubule stabilizers or inhibitors
Small molecular weight molecules are provided including, but not limited to, peptides, peptide analogs and peptide mimetics that can interact with microtubules to promote their assembly or prevent their disassembly and can interrupt mitosis, prevent cell division, and trigger apoptosis. methods for the prevention or treatment of neoplastic disease in...
Compositions comprising igbpma and uses thereof
The present invention relates generally to methods and materials for treating conditions associated with IgE activation in humans and animals, and to agents capable of modulating the activation. The agents of the invention comprise or are related to IGBPMA polypeptides from ticks....
Fusion protein comprising fk506 binding protein and method of making and using the same
Disclosed is a fusion protein containing a FK506 binding protein and a cell-transducing domain. Also, disclosed is a method of making the fusion protein and use of the fusion protein in a pharmaceutical or cosmetic composition. The cell-transducing domain is, for example, a PEP-1....
Inhibitor of tgf-beta activation reaction
The present invention aims to provide a substance(s), especially a peptide(s) capable of inhibiting the TGF-? activation reaction. The present invention provides a peptide consisting of 11 to 50 amino acid residues, which comprises an amino acid sequence Gln-Ile-Leu-Ser-X1-X2-X3-X4-Ala-Ser-Pro (SEQ ID NO: 1) wherein each of X1 to X4 independently...
Methods for bone treatment by modulating an arachidonic acid metabolic or signaling pathway
Methods for promoting osteogenesis to accelerate or enhance bone fracture healing, treat bone defects, and enhance bone formation are disclosed. The methods modulate an arachidonic acid metabolic or signaling pathway in general, and, in particular, utilize 5-lipoxygenase inhibitors. These molecules can be delivered alone or in combination with one or...
Methods of treatment and prevention of metabolic bone diseases and disorders
The present invention provides compostions and methods useful for treating and preventing metabolic bone diseases and disorders by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing metabolic bone diseases and disorders such as, for example osteoporosis, osteopenia and osteopenia related diseases and abnormal bone marrow....
Novel fsh glycosylation variant d3n
FSH mutant with increased glycosylation and longer half-life is described. The use of this FSH mutant for inducing folliculogenesis in human patients is also described....
Nucleic acid and corresponding protein entitled 161p5c5 useful in treatment and detection of cancer
A novel gene (designated 161P5C5) and its encoded protein, and variants thereof, are described wherein 161P5C5 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table 1. Consequently, 161P5C5 provides a diagnostic, prognostic, prophylactic and/or therapeutic target for cancer. The 161P5C5 gene...
Protective complement proteins and age-related macular degenration
Methods for identifying a subject at risk for developing AMD are disclosed. The methods include identifying specific protective or risk polymorphisms or genotypes from the subject's genetic material. Therapeutic compositions and methods are also provided for delaying the progression or onset of the development of AMD in a subject, including...
Treatment of non-alcoholic steatotic hepatitis (nash)
The present invention relates to a method for treating nonalcoholic steatotic hepatitis (NASH) in a subject by administering an effective amount of a lipoprotein lipase (LPL) therapeutic to the subject. The LPL therapeutic is advantageously a S447X protein or a derivative or variant thereof, or a nucleic acid encoding such...
Therapeutic peptides derived from urokinase plasminogen activator receptor
The present invention relates to a chemotactically active epitope derivable from the urokinase receptor, a mutated peptide that acts as an inhibitor of chemotaxis, and their therapeutic use....
Compounds and methods for inhibiting apoptosis
The invention provides compounds, compositions, and methods for inhibiting apoptosis and for the treatment of conditions related thereto....
Novel use of peptide compounds for treating muscle pain
The present invention is directed to the use of a class of peptide compounds for treating non-inflammatory musculoskeletal pain or/and non-inflammatory osteoarthritic pain....
Anti-hypercholesterolemic biaryl azetidinone compounds
and the pharmaceutically acceptable salts thereof, wherein R12 is an alkyl, alkeny or alkynyl group mono- or poly-substituted with ?OH, ?COOH or a combination of ?OH and ?COOH, and R9 contains an alkyl, alkeny or alkynyl group substituted with a heterocyclic ring, amino or sulfonyl. The compounds are useful for...
Biologically active compounds with anti-angiogenic properties
A method for inhibiting angiogenesis in a subject comprising administering to the subject at least one compound of General Formula (I), wherein the ring or any chiral center(s) may be of any configuration; Z is sulphur, oxygen, CH2, C(O), C(O)HN, NH, NRA or hydrogen, in the case where Z is...
Composition containing ginsenoside f1 and egcg for preventing skin damage
The present invention relates to a skin-care composition containing ginsenoside F1 and EGCG. More particularly, the present invention relates to an inhibitor of UV-induced apoptosis in epidermal cells showing an excellent skin-care effect by the synergistic interaction of the said ginsenoside F1 and EGCG even at low concentrations, and to...
Anti-cancer activity of androsace umbellata merr. extract and contained triterpene saponin
The present invention relates to an Androsace umbellata Merr. extract having anticancer activity and a triterpene saponin compound isolated therefrom, more particularly to an Androsace umbellata (Lour.) Merr. extract, triterpene saponin compounds isolated therefrom, saxifragifolin B and saxifragifolin D, which inhibit the growth of cancer cells and induce apoptosis of...
Meloxicam for the treatment of respiratory diseases in pigs
A method of treating or preventing a respiratory disease in a pig, the method comprising administering to the pig in need thereof an effective amount of meloxicam or a pharmaceutically acceptable salt thereof....
Amorphous telithromycin compound
The present invention relates to stable amorphous 3-De[(2,6-dideoxy-3-C-methyl-3-O-methyl-?-L-ribohexopyranosyl)oxy]-11,12-dideoxy-6-O-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl]imino]]erythromycin (telithromycin), methods for the preparation thereof, the use of stable amorphous telithromycin in the treatment of bacterial infections and to pharmaceutical compositions comprising stable amorphous telithromycin....
Fluorinated pyrrolo[2,3-d]pyrimidine nucleosides for the treatment of rna-dependent rna viral infection
The present invention provides fluorinated pyrrolo[2,3,d]pyrimidine nucleoside compounds which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B...
2', 3'-dideoxynucleoside analogues for the treatment or prevention of flaviviridae infections
A method for the treatment or prevention of Flaviviridae infections, in particular, hepatitis C virus infection, in a host, and in particular, a human, is provided that includes administering an effective amount of a ?-L- or ?-D-2?,3?-dideoxynucleoside or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable...
Compositions and their uses directed to ptpru
Disclosed herein are compounds, compositions and methods for modulating the expression of PTPRU in a cell, tissue or animal. Also provided are methods of active target segment validation. Also provided are uses of disclosed compounds and compositions in the manufacture of a medicament for treatment of diseases and disorders. Also...
Methods and compositions for the diagnosis and treatment of ewing's sarcoma
The present invention relates to methods and compositions for the detection and treatment of Ewing's sarcoma. In particular, the methods of detection relate to measuring in Ewing's sarcoma cells the expression of the NKX2.2 gene, as well as targets genes downstream of NKX2.2. The compositions and method of treatment for...
Methods and kits for linking polymorphic sequences to expanded repeat mutations
Methods and kits are provided for determining which single nucleotide polymorphism (?SNP?) variant of an allele of a heterozygous patient is on the same mRNA transcript as a disease-causing mutation that is at a remote region of the gene's mRNA comprising a) an allele-specific reverse transcription reaction using an allele-specific...
Pit-1 and vascular calcification
The present invention relates to methods and compositions comprising small interfering RNAs (siRNAs) to identify nucleotides encoding proteins involved in the co-transport of inorganic phosphate in vascular tissues. Specifically, it relates to the identification of Pit-1 and Pit-2 as key proteins involved in vascular calcification, the deposition of calcium phosphate,...
Structures of active guide rna molecules and method of selection
The present invention relates to methods and compositions for modulating RNA silencing efficiency by providing selective RISC (RNA-induced silencing complex) formation. The present invention also relates to methods for identifying nucleic acids and/or determining their structures....
Synergic combinations comprising a quinoline compound and other hiv infection therapeutic agents
The invention relates to a combination comprising a quinoline compound or its sail, according to general formula (I) and at least one HIV infection therapeutic agent selected from the group consisting of entry inhibitors, reverse-transcriptase inhibitors, strand-transfer inhibitors, protease inhibitors, and maturation inhibitors. Said combination has therapeutic synergy in the...
Methods and compositions for treating flaviviruses, pestiviruses and hepacivirus
A method and composition for treating a host infected with flavivirus, pestivirus or hepacivirus comprising administering an effective flavivirus, pestivirus or hepacivirus treatment amount of a described base-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided....
Oral dosage forms of gemcitabine derivatives
The present invention relates to oral dosage forms of certain long chain saturated and monounsaturated fatty acid derivatives of 2?,2?-difluorodeoxycytidine (Gemcitabine). In particular, the present invention relates to the use of the said gemcitabine derivatives or a pharmaceutical acceptable salt thereof for preparing an oral dosage form ameliorating compliance in...
Composition containing fermentable polysaccharides
The present invention relates to a composition to a nutritional composition comprising 0.1 to 15 gram fermentable e partially hydrolysed gum having a degree of polymerisation between 10 and 300 per 100 gram dry weight of the composition and 0.1 to 15 gram fermentable, indigestible polysaccharide other than a hydrolysed...
Compositions for reducing, ameliorating, treating, or preventing condition of dry eye and methods of making and using same
Compositions for relief, treatment, or prevention of a condition of dry eye comprise alginate, at least a polyol, and a pharmaceutically acceptable carrier, wherein the compositions have pH in the range from about 5 to about 7.5. In some embodiment, the compositions can further include a chelating agent, a buffering...
Preventing or reducing oxidative stress or oxidative cell injury
A water-soluble cellulose derivative is useful for preventing or reducing oxidative stress or oxidative cell injury in tissues of an animal and in particular for regulating Stearoyl-CoA Desaturase-1 gene expression and/or ATPF1 gene expression in non-adipose tissues of the animal....
Process for the production of intermediates for the preparation of tricyclic benzimidazoles
The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
The invention relates to a process for the synthesis of compounds of...
Fibroblast activation protein inhibitor compounds and methods
Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro,...
Cgrp receptor antagonists
(where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache....
Method of creating crystalline substances
Process for preparing a cocrystal of an active substance and a cocrystal former, the process involving precipitating the active substance and the cocrystal former together from solution or suspension, in the presence of a supercritical or near-critical fluid, in particular using a GAS, SAS, SEDS or SAS-EM process. The invention...
Gemini vitamin d3 compounds and methods of use thereof
The invention provides Gemini vitamin D3 compounds, methods for using the compounds to treat vitamin D3 associated states and pharmaceutical compositions containing the compounds....
Use of vitamin d compounds to treat endometriosis
The use of vitamin D compounds in the treatment or prevention of endometriosis, methods for the treatment or prevention of endometriosis by administering a vitamin D compound, and compounds for use therein....
Method of female contraception and a kit for use therein
The invention is concerned with a method of contraception in a female mammal of childbearing capability. The method has two alternating phases?a preservation phase and a shedding phase?and has at least two sequences of (a) a preservation phase of 3-12 months involving continuous oral administration to the female of dosage...
Compositions for the treatment of inflammatory disorders
The invention features methods and compositions for the treatment of immunoinflammatory disorders....
Methods, compositions, and kits for the treatment of pain
The invention features methods, compositions, and kits for the treatment of pain....
Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic ?addition-elimination? substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs...
Water-in-oil type emulsified composition
Water-in-oil type emulsified compositions with a high silicone oil content which are excellent in emulsification stability and whose sticky feeling has been improved may be obtained by incorporating a specific (A) N-long chain acyl neutral amino acid ester, (B) a silicone oil, and (C) water therein....
Method of treating or sepsis
Provided is a method of treating trauma or sepsis comprising: administering an effective amount of one or both of a SOC channel-selective inhibitor or a SphK inhibitor to an animal at risk of inflammation-mediated organ damage from trauma or sepsis....
Combination therapy with parp inhibitors
The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ)....
Beta-lactamyl phenylalanine, cysteine, and serine vasopressin antagonists
Substituted 2-(azetidin-2-on-1-yl)alkoxyalkylalkanoic acids and 2-(azetidin-2-on-1-yl)arylalkylalkanoic acids, and analogs and derivatives thereof are described. Methods for using the described compounds, and pharmaceutical compositions thereof, to treat disease states responsive to antagonism of one or more vasopressin receptors are also described....
Pyrazole or triazole compounds and their use for the manufacture of a medicament for treating somatic mutation-related diseases
The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a...
5-phenyl-4-methyl-thiazol-2-yl-amine derivatives as inhibitors of phosphatidylin ositol 3 kinase enzymes (pi13) for treatment of inflammatory diseases
in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described....
Azetidines
wherein Ar, R1, X, and Z are as defined herein, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids, to intermediates useful in their synthesis, and to compositions containing them.
The invention relates to EP2 antagonist azetidines of formula (I)...
Benzamide derivatives and their use as glucokinase activating agents
Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from ?C(O)NR4R5, ?SO2NR4R5, ?S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl,...
Biaryl substituted pyrazinones as sodium channel blockers
Biaryl substituted pyrazinone compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by,...
Fused phenyl amido heterocyclic compounds
Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase,...
Novel oxadiazole compounds
Novel oxadiazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions as agonists or antagonists of the S1P family of G protein-coupled receptors for treating diseases associated with modulation of S1P family receptor activity, in particular by affording a beneficial immunosuppressive effect are disclosed....
Phenoxy benzamide compounds with utility in the treatment of type 2 diabetes and obesity
wherein: R1 is methoxymethyl; R2 is selected from ?C(O)NR4R5, ?SO2NR4R5, ?S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano;...
Pyridine derivatives and their use as cb2 receptor modulators
and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.
The present invention relates to novel pyridine derivatives such as compounds of the formula (I):...
Methods and compositions for treating chronic lymphocytic leukemia
Novel method of treating chronic lymphocytic leukemia by the administering of HSP90 inhibitors, particularly ansamycins, more particularly I 7-allylamino-I 7-demethoxygetdanarnycin (17-AAG)....
Substituted heterocyclic derivatives and their pharmaceutical use and compositions
Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents....
Staurosporine derivatives for use in alveolar rhabdomyosarcoma
This invention relates to staurosporine derivatives are effective when used in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a disease associated with a PAX/FKHR translocation including a PAX3/FKHR translocation and a PAX7/FKHR translocation, more especially a solid tumor disease such as...
Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication
a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one...
Novel substituted diazabicyclo derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
This invention relates to novel substituted diazabicyclo derivatives useful as monoamine neurotransmitter re-uptake inhibitors....
Muscarinic receptor antagonists
This present invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed...
Methods for treating anxiety related disorders
The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. In one treatment method, methods of, and compositions for, modulating the expression of certain GABAA receptor subunits are used to...
Mixed solvate of olanzapine, method for preparing it and method for preparing form i of olanzapine therefrom
Said mixed solvate is a solvate of olanzapine/water/tetrahydrofuran in the proportion 1:1:1/2 (I). The method for preparing said solvate comprises treating a crude anhydrous olanzapine with a mixture of tetrahydrofuran/water. The method for preparing Form I of olanzapine includes desolvating the mixed solvate of formula I, by means of drying,...
Substituted ureas
Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders....
Selected cgrp-antagonists, processes for preparing them and their use as pharmaceutical compositions
The invention relates to CGRP-antagonists of general formula (I), wherein R1, R2, R3, R4 and R5 are defined in claim 1, to the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures salts and salt hydrates thereof, in particular to 10 salts thereof, which are physiologically compatible with acids or inorganic or organic...
Antibiotics derivatives
only one or two of Y1, Y2, Y3 and Y4 can represent N at the same time.
if A represents O or S, then W represents ?CH2?; and
if Z-B represents NCH2CH2, NCOCH2, NCH2CO or NCH2CH(OH),...
Hydroxylamine compounds and methods of their use
The present disclosure provides compounds that include hydroxylamines of formula I or II, pharmaceutical compositions, and methods for their use. The methods utilize hydroxylamine compounds and/or their pharmaceutical compositions for the treatment of angiogenesis, hepatitis, complement-mediated pathologies, drusen-mediated pathologies, macular degeneration and certain other ophthalmic conditions, inflammation, arthritis, and related...
Inhibitors of akt activity
The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration (if the compounds of the...
Anti-cancer agents and uses thereof
and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring...
Compounds
Tricyclic nitrogen containing compounds and their use as antibacterials....
Dihydro[1,4]oxazino[2,3,4-hi]indazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor....
Substituted-dihydro[1,4]oxazino[2,3,4-hi]indazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor....
5-amino-4-hydroxy-7-(1h-indolmethyl)-8-methylnonamide derivatives as renin inhibitors for the treatment of hypertension
The application relates to novel alkanamides of the general formula (I) where X is ?CH2? or >CH?OH; (A) R1 is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R2 is C1-C6-alkyl or C3-C6-cydoalkyl; R3 are each independently H, C1-C6-alkyl, C1-6-alkoxycarbonyl...
Aerosol formulation for inhalation
The present invention relates to a propellant-free aerosol formulation which contains one or more compounds of general formula 1....
Dipyrrole compounds, compositions, and methods for treating cancer or viral diseases
The present invention relates to novel Dipyrrole Compounds, compositions comprising a Dipyrrole Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Dipyrrole Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or...
Spiro-piperidine derivatives
wherein R1 to R5, R5?, X, Y and A are as defined in the specification.
In particular, the present invention is concerned with compounds of the general formula (I)
The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as...
Bicyclic pyrimidine derivatives as calcium channel blockers
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an...
Inhibitors of akt activity
The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention....
Apoptosis inhibitors
The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can...
Inhibitors of checkpoint kinases
The instant invention provides for compounds which comprise substituted quinolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer....
N-substituted pyridinone or pyrimidinone compounds useful as soluble epoxide hydrolase inhibitors
Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same....
Pharmaceutical composition for preventing and treating metabolic bone diseases containing alpha-arylmethoxyacrylate derivatives
The present invention relates to a use of a specific alpha-arylmethoxyacrylate derivative, or its pharmacologically acceptable salt or solvate for preventing and treating metabolic bone diseases....
Urea antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity....
Imidazolyl-pyrimidine compounds for use in the treatment of proliferative disorders
which possess cell-cycle inhibitory activity are described.
Compounds of formula (I):...
Triazolophthalazines
in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.
The compounds of formula (I)...
Naphthyl(ethyl) acetamides
This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual...
Cinnoline compounds as inhibitors of phosphodiesterase type iv (pde4)
There are provided according to the invention novel compounds of formula (I)...
New phenylalanine derivatives
wherein R1 is a methyl group and R2 is a methoxy group.
Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning ?4 integrin in which ?4 integrin-depending...
Phthalazinone derivatives
RD is an optionally substituted C5-20 aryl group, bound to D by a carbon-carbon bond.
where Q is O or S; and
where Q is O or S; and
where Y1 is selected from CH and N and Y2 is selected from CH and N;
where Y1 is selected from CH and N, Y2...
Novel diazabicycylic aryl derivatives and their medical use
This invention relates to novel diazabicyclic aryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse...
Tetrahydrotriazolopyrazine derivatives and uses thereof
This invention relates to novel substituted tetrahydrotriazolopyrazines and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an enzyme inhibitor...
Intravenous formulations of pde inhibitors
The invention relates to a novel pharmaceutical dosage form of PDE 5 inhibitors for intravenous administration and the use thereof for the treatment of diseases....
Pyridazine derivatives and their use as therapeutic agents
where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein.
Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need...
Nitrogen-containing heterocyclyl ketones and methods of use
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention...
Pyridazin-3(2h)-one derivatives and their use as pde4 inhibitors
The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of...
Insecticidal n-substituted (heteroaryl)alkyl sulfilimines
N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects....
Quinoline and quinazoline derivatives having affinity for 5ht1-type receptors
wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description.
Disclosed are methods for use of compounds of formula (I) in combination with other active substances in the treatment of CNS disorders such as depression or anxiety....
Plasminogen activator inhibitor-1 inhibitors
Inhibitors of plasminogen activator inhibitor-1 (PAI-I) are provided, which may also act as anti cancer agents, of formulae (I-V)....
Amorphous aripiprazole and process for the preparation thereof
Morphologically stabilized amorphous aripiprazole and process for preparing the same....
Intermittent dosing regimen for overweight and obese subjects
The present invention concerns an intermittent dosing regimen for the treatment of obesity or the reduction of body weight wherein a pharmaceutical composition containing an apoB secretion/MTP inhibitor is administered to a subject in need thereof for a period of time, then withheld for a period of time, and again...
1-benzylindole-2-carboxamide derivatives
The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence....
Pyridine and pyrimidine derivatives as mglur2 antagonists
wherein A, B, Q, X, Y, R1, and R2 are as defined herein; pharmaceutical compositions containing them; a process for their manufacture; and methods for treating CNS disorders with the same.
The present invention relates to compounds of formula (I)...
Amines as small molecule inhibitors
The present invention relates to compounds that are useful as inhibitors of protein arginine methyltransferase that have a formula selected from Formula (I), Formula (II) and Formula (III), as well as racemic mixtures, diastereomers, enantiomers and tautomers thereof and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof as...
Phosphodiesterase inhibitors
The present invention relates to purine derivatives, which can be used as selective phosphodiesterase (PDE) type IV inhibitors. Compounds disclosed herein can be useful in the treatment of asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic...
3-(dihydro-1h-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide derivatives and methods of use
This invention relates to novel 3-(dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of cyclic guanosine...
Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with a cyclic amino group as crf antagonists
has a high affinity for CRF receptors and/or ? receptors, and is effective against diseases in which CRF is considered to be involved.
[SOLUTION] A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following a [I]
[PROBLEM TO BE SOLVED] An object of the present invention is...
Antifungal wallboards and building materials and methods for the production thereof
The present invention relates to, inter alia, methods for the treatment of wallboards and the treated wallboards. In particular, the invention relates to the treatment of wallboards with a fungicidally effective amount of a strobilurin or strobilurin-type fungicide. In a particular embodiment the fungicide is azoxystrobin. The invention also provides...
Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
wherein the Compound I is present in one or more polymorphic forms. Also provided are novel methods for the preparation of the polymorphs of Compound I, and kits and articles of manufacture of the compositions, and methods of using the compositions to treat various diseases.
Compositions comprising the succinate salt of...
Pyrimidinone compounds and preparation and use thereof
Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for preventing and treating cardiovascular and cerebrovascular disorders, senile dementia, diabetes mellitus, osteoporosis and tumors, and enhancing immune functions in a subject, and...
Compositions and methods for treating vascular, autoimmune, and inflammatory diseases
The disclosure provides methods and compositions for the treatment of vascular, autoimmune and inflammatory diseases using a combination of an inosine monophosphate dehydrogenase (IMPDH) inhibitor and a HMG CoA reductase inhibitor....
Benzimidazolyl compounds
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I...
Method of preparing porphyrin derivatives, porphyrin derivatives, uses thereof and pharmaceutical compositions
Method of preparing a porphyrin derivative starting from a meso-substituted porphyrin compound. According to the invention, the meso-substituted porphyrin compound used is a meso-(2?-cyanovinyl)-substituted porphyrin compound, wherein said meso-(2?-cyanovinyl)-substituted porphyrin compound, in a form in which its porphyrin ring is complexed with a bivalent metal ion is converted, in the...
Process to prepare camptothecin derivatives
A process is provided for the preparation of camptothecin derivatives, such as irinotecan, in a one-pot operation....
Morphinan compounds
This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor...
Ligand conjugates of vinca alkaloids, analogs, and derivatives
Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations in a patient. The compounds described herein include conjugates of cytotoxic drugs and vitamin receptor binding ligands. The conjugates also include a linker that is formed from one or more spacer linkers, heteroatom linkers, and releasable linkers....
Screening method
The present invention provides a medicament for preventing/treating cancer, comprising a tacrine compound, or a compound promoting the binding between the tacrine compound and a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1....
Combination of organic compounds
The invention relates to a pharmaceutical combinations comprising an AT1 receptor blocker or pharmaceutically acceptable salts thereof and a mTOR inhibiting agent, e.g. rapamycin or a rapamycin derivative, optionally in the presence of a pharmaceutically acceptable carrier....
Rapamycin derivative or an impdh inhibitor for treating polycystic kidney disease
A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5?-monophosphate dehydrogenase inhibitor or a rapamycin derivative....
8-phenoxy-gamma carboline derivatives
Compounds of Formula I and corresponding pharmaceutical compositions are disclosed....
Methods and packages to enhance safety when using imiquimod to treat children diagnosed with skin disorders
Pharmaceutical packages and methods for enhancing the safety of imiquimod when used to treat children affected by skin disorders are disclosed. More particularly, the safety profile of imiquimod use is enhanced by providing information to the children, guardians of the children, including parents and health care professionals, that systemic absorption...
Tetrahydro-beta-carbolin-sulfonamide derivatives as 5-ht6 ligands
The present invention relates to new tetrahydro-?-carbolin-sulfonamide derivatives of general formula (I), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemates or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or corresponding physiologically...
Crystalline forms of an hiv integrase inhibitor
Crystalline forms of a hexahydro-diazocinonaphthyridine trione compound are disclosed. The compound and its crystalline forms thereof are HIV integrase inhibitors useful for the prophylaxis or treatment of HIV infection or for the prophylaxis, treatment or delay in the onset or progression of AIDS....
Imidazo[1,2-a]pyridine derivatives for the treatment of silent gastro-esophageal reflux
The present invention relates to a new method of treatment of sleep disturbance due to silent gastro-esophageal reflux. In particular, the present invention relates to the use of certain imidazo (1,2-a)pyridines derivatives (I) in said treatment....
Anti-insomnia compositions and methods
Compositions of zolpidem, and methods for their manufacture and use for treating insomnia. The compositions are formulated as oral sprays for transmucosal absorption of zolpidem. The methods of treatment in some cases involve night-time dosing administration to achieve therapeutic zolpidem blood levels within 20 minutes or less, tapering off to...
Azaindole-derivatives as factor xa inhibitors
wherein R0, R1, R2, R3, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They...
Modulators of amyloid beta
wherein hetaryl I, hetaryl II, and R1 are as described herein. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease.
The invention relates to...
Oxopyridyl quinoline amides as nk3 receptor modulators
Compounds of Formula I wherein R1, A, R2, R3, R4, R5, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same....
Hydantoin derivatives useful as metalloproteinase inhibitors
Formula (I) wherein R1 is a (2-4C)alkyl and is substituted by two or more fluorine groups and R2 is methyl or ethyl, or a pharmaceutically acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by metalloproteinase...
Salt il
The invention provides N-{2-[((2S)-3-{[1-(4-chlorobenzyl)piperidin-4-yl]amino}-2-hydroxy-2-methyl-propyl)oxy]-4-hydroxyphenyl}acetamide furoate or a solvate thereof, pharmaceutical compositions containing the salt or solvate and use of the salt or solvate in therapy....
Agents used for the treatment of seeds
The present invention relates to inter alia the use of known compounds for the treatment of seed....
Pyridine derivatives as connabinoid receptor modulators
and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.
The present invention relates to novel pyridine derivatives such as compounds of the formula (I):...
Method of improving wakefulness
The present invention relates to the use of certain imidazolylalkyl-pyridines as wakefulness compounds....
Methods and compositions for screening and treatment of disorders of blood glucose regulation
In one aspect, the invention provides a method of screening and, optionally, treatment of an individual suffering from an insulin resistance disorder by screening an individual in need of treatment for an insulin resistance disorder for one or more genetic variations indicating a predisposition to a response to an insulin...
Heteroarylsulfonyl stilbenes as 5-ht2a antagonists
Compounds of formula I: are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various 10 CNS disorders....
Heterocyclic inhibitors of mek and methods of use thereof
Disclosed are MEK inhibitors useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds....
Topically applicable pharmaceutical preparation
A topical pharmaceutical preparation for administering a slightly soluble PDE4 inhibitor is described. A surprisingly good systemic bioavailability is observed with this dosage form....
Cyclic n-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for the therapeutic use thereof
wherein the various R1-R9 substituents are defined herein. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and...
New amino-alkyl-amide derivatives as ccr3 receptor ligands
The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology,...
Waterbased bit/tmad formulations
Aqueous formulations having a pH of >10 of 1,2-benzoisothiazolin-3-one (BIT) and/or its alkali metal salts and tetramethylolacetylenediurea (TMAD) are outstandingly suitable for protecting industrial materials and products from infection and destruction by microorganisms....
Novel thiazolidin-4-one derivatives
The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents....
New amino-alkyl-amide derivatives as ccr3 receptor ligands
The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.
as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology,...
Novel antibiotics comprising bis(1-aryl-5-tetrazolyl)methane derivatives
The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds, the bis(1-aryl-5-tetrazolyl)methanes, which are especially useful for combating infections with gram-positive bacteria and especially MRSA....
Novel tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of g-protein coupled receptors (gpcps)
The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in...
Hydroisoindoline tachykinin receptor antagonists
The present invention is directed to certain hydroisoindoline compounds of formula I which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and...
Substituted acylhydroxamic acids and method of reducing tnfalpha levels
Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF? and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate....
Methods of using [3.2.0] heterocyclic compounds and analogs thereof for treating infectious diseases
Disclosed are methods of treating infectious diseases comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent....
Deuterium-enriched atorvastatin
The present application describes deuterium-enriched atorvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same....
Deuterium-enriched atorvastatin
The present application describes deuterium-enriched atorvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same....
Novel compounds
The invention provides a compound of formula (I), pharmaceutical compositions thereof, and methods of treatment using the same....
Iminosugar treatment of tumors
where R and R? are each alkyl groups, R? is hydrogen or an alkyl group and X3, X4 and X5 are each independently selected from the group consisting of hydrogen, benzyl, t-butyldimethylsiloxy radical and triphenylmethyl. Accordingly, compounds of formula (I) can be used for treatment of tumors including melanoma. Also...
Laulimalide analogues as therapeutic agents
Laulimalide analogues useful as microtubule stabilizing agents, and in the treatment of abnormal cell proliferation, are disclosed. Methods of making the compounds, as well as methods of using such compounds in treating abnormal cell proliferation diseases are also described....
Spiro compounds for treatment of inflammatory disorders
wherein Y, Z and R1-R12 are defined herein.
Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof:...
Methods of preventing the serotonin syndrome and compositions for use thereof
The present invention is directed at methods for preventing or minimizing the intensity of the serotonin syndrome in humans and lower animals which comprises administering proserotonergic agents and serotonin surge protectors. The present invention is also directed to pharmaceutical compositions comprising proserotonergic agents and serotonin surge protectors useful for carrying...
Composition comprising the alcohol compound isolated from the extract of cucurbitaceae family plant having anti-adipogenic and anti-obesity activity
The present invention is related to an alcohol compound isolated from the extract of Cucurbitaceae family plant having anti-adipogenic and anti-obesity activity, and a composition comprising the same. The compound showed potent reducing activity of body weight, decreasing effect on the blood triglyceride and cholesterol level, activating activity of PPAR...
Process for preparation of mycophenolate mofetil and other esters of mycophenolic acid
Provided are processes for the preparation of mycophenolate mofetil and other esters of mycophenolic acid....
Insect repellent compositions
An insect repellent composition containing 3,8-p-menthane-diol and benzylbenzoate as active compounds is described. Typically, the active compounds are each present in the composition in an amount which is less than an amount of the compound required to be effective as an insect repellent by itself. The composition may additionally include...
Methods and compositions of derivatives of probucol for the treatment of diabetes
This present invention provides methods and pharmaceutical compositions for the treatment or prophylaxis of diabetes and related disorders, comprising the administration of an effective amount of a monoester of probucol, particularly the monosuccinic acid ester, or a pharmaceutically acceptable salt or derivative thereof....
Treatment and prevention of bone loss using resolvins
The present invention provides new methods for inducing or promoting bone growth and/or for reducing or preventing bone deterioration in a mammal subject. The inventive methods generally comprise administering to the subject an effective amount of a resolvin. In particular, the inventive methods may be useful for treating or preventing...
Tranexamic acid formulations
Disclosed are oral tranexamic acid formulations and methods of treatment therewith....
Glucagon receptor antagonists, preparation and therapeutic uses
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using...
Methods of treating rett syndrome
The present embodiments relate to methods for the treatment of Rett Syndrome. More specifically, the present embodiments relate to pivagabine for use in the treatment of Rett Syndrome. Some embodiments relate to treatment of a patient with Rett Syndrome. Other embodiments relate to treatment of the indications of Rett Syndrome....
Transdermal delivery of beneficial substances effected by a hostile biophysical environment
The present invention generally relates to the transdermal delivery of substances and, in some embodiments, to the transdermal delivery of beneficial substances by a hostile biophysical environment. In one aspect, various methods for the transdermal delivery of beneficial substances are disclosed. By creating a hostile biophysical environment, beneficial substances may...
Methods and compositions using certain phenolic derivatives for the treatment of diabetes
This present invention provides methods and pharmaceutical compositions for the treatment or prophylaxis of diabetes and related disorders, comprising the administration of an effective amount of a compound including an optionally substituted phenyl ring linked to an aromatic or alkyl group by a spacer, wherein the spacer includes two groups...
Treprostinil treatment for interstitial lung disease and asthma
The present invention describes methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of interstitial lung disease or asthma, or a condition, such as pulmonary fibrosis, associated with interstitial lung disease or a condition associated with asthma. The invention also relates...
Methods of inhibiting angiogenesis and treating angiogenesis-associated diseases
The invention provides methods of inhibiting angiogenesis in an individual by administering a composition (such as protein containing composition) comprising colchicine or thiocolchicine dimer. The composition is in an amount that is effective in inhibiting angiogenesis but is in some embodiments insufficient to induce significant cytotoxicity in the individual. The...
Use of (n'-methyl) benzoylurea compound
wherein R1 represents a hydrogen atom, a C1-C6 alkyl group optionally substituted with a halogen atom, or the like, R2 represents a halogen atom, or the like, and R3 represents a halogen atom, a C1-C4 alkyl group optionally substituted with a halogen atom, a C1-C4 alkoxy group optionally substituted with...
Hydroxybenzamide derivatives, the method for preparing thereof and the cosmetic composition containing the same
Disclosed is a hydroxybenzamide derivative represented by the following Formula. A method for preparing the same and a cosmetic composition comprising the same are also disclosed. More particularly, the hydroxybenzamide derivative is obtained by reacting a hydroxybenzoic acid having a protecting group introduced thereto with a hydroxyphenyl amine to form...
Carboxamido opioid compounds
This invention is directed to carboxamido opioid compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder....
Substituted naphthalenes
Disclosed herein are substituted naphthalene-based melatonin (MT) receptor modulators and/or 5-HT receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof....
Pesticide bi-phenyl-amidine derivatives
The present invention relates to bi-phenyl-amidine derivatives of formula (I) in which the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging...
Treatment of cns disorders with trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine
Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful....
Ascophyllum compositions and methods
The invention provides extracts of brown seaweed of the genus Ascophyllum that have valuable pharmacological properties. In particular, compositions of the invention are useful for e.g.: inhibiting alpha-glucosidase activity; preventing or treating conditions mediated by alpha-glucosidase activity; reducing blood glucose levels; preventing or treating diabetes; modulating glucose uptake in adipocytes;...
Extracts of latex of calotropis procera and to a method of preparation thereof
The invention relates to aqueous suspension of dried latex (DL) of Calotropis procera and to a method of preparation for the prevention/treatment of cancer. The DL suspension when administered orally in the X-myc mice?a transgenic mouse model of hepatocellular carcinoma (HCC), was effective in protecting the animals from the atypical...
Use of carophyllenes in the manufacture of medicaments and treatment of bodily conditions of inflammation and inflammatory pain
The invention concerns the use of caryophyllenes related to medicaments and to the treatment of bodily conditions of inflammation and inflammatory pain....
Novel pharmaceutical or cosmetic carriers containing cyclic acetals
The use of a cyclic acetal obtained by reacting an aliphatic aldehyde having 2 to 4 carbon atoms with a polyol having 3 to 6 carbon atoms and at least three hydroxy functions, including two on vicinal carbons or carbons having one carbon atom therebetween, as a pharmaceutical or cosmetic...
Bifunctional derivatives of polyethylene glycol, their preparation and use
The patent describes homo- or hetero-bifunctional derivatives of polyethylene glycol (PEG) obtained by selectively modifying the hydroxyl end groups of commercial PEGs of different molecular weights with reactive bifunctional molecules. The synthesis process comprises steps involving sequential derivatization of PEG terminal hydroxyl groups with a bifunctional compound, purification of the...
Process for making pharmaceutical compositions with a transient plasticizer
A process for making a solid oral dosage form that has a therapeutic compound (e.g., a poorly soluble and/or poorly compactible therapeutic compound) and a polymer. The process is accomplished by the use of an extruder. A transient plasticizer, e.g., a liquefied gas such as supercritical carbon dioxide, is added...
Hydrophobic polysaccharide derivatives
Novel cross-linked gels comprised of alkoxyetheramides grafted to polysaccharides that have superior viscosity properties have been made. By controlling the chain length of the alkoxyetheramides and the hydrophobic nature of the gel, these materials are ideal for many uses such as in hydraulic fracturing of oil-bearing geological formations, in the...
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