32nd week of 2009 patent applcation highlights part 44 |
Patent application number | Title | Published |
20090197862 | 2-AMINOPYRIDINE KINASE INHIBITORS - 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition. | 2009-08-06 |
20090197863 | BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) - A compound having the structure set forth in Formula (I) or Formula (II): | 2009-08-06 |
20090197864 | Furo- and Thieno [3,2-c] Pyridines - Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET. | 2009-08-06 |
20090197865 | THERAPEUTIC METHODS, COMPOSITIONS AND COMPOUNDS - In one embodiment the invention provides a method of combating cyanide poisoning, which comprises administering to a subject a compound capable of releasing 3-mercapto-pyruvate in vivo. In other embodiments the invention also provides pharmaceutical compositions comprising a compound capable of releasing 3-mercaptopyruvate in vivo, as well as novel compounds that are capable of releasing 3-mercaptopyruvate in vivo. | 2009-08-06 |
20090197866 | PYRAZOLYLBENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM AND USE THEREOF - The disclosure relates to compounds of formula (I): | 2009-08-06 |
20090197867 | ENANTIOMERICALLY ENRICHED IMIDAZOAZEPINONE COMPOUNDS - The present invention provides an enantiomerically pure compound of Formula I: | 2009-08-06 |
20090197868 | 5ht2c receptor modulator compositions and methods of use - The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity. | 2009-08-06 |
20090197869 | AZEPINE INHIBITORS OF JANUS KINASES - The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 2009-08-06 |
20090197870 | Pharmaceutical Compositions - Compounds for use in compositions and methods for modulating the activity of nuclear receptors are provided. In particular, compounds for use in compositions and methods for modulating the estrogen related receptors are provided. In one embodiment, the compounds provided herein are ERR modulators. In another embodiment, the compounds provided herein are agonists, partial agonists, antagonists, or inverse agonists of ERR or ERR?. In certain embodiments, the compounds of the invention, as described above in the Summary of the Invention, are compounds of formula (I). | 2009-08-06 |
20090197871 | Dual Pharmacophores - PDE4-Muscarinic Antagonistics - The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis. | 2009-08-06 |
20090197872 | NOVEL 1,4-DIAZA-BICYCLO[3.2.2]NONYL PYRIMIDINYL DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. | 2009-08-06 |
20090197873 | COMPOSITIONS COMPRISING ALPRAZOLAM FOR TREATING PRIMARY INSOMNIA AND INSOMNIA ASSOCIATE WITH ANXIETY STATES AND PROCESS FOR PREPARING THEM - Disclosed is a composition comprising alprazolam for treating primary insomnia and insomnia associated with anxiety states and the corresponding use and method comprising the administration of alprazolam sublingual tablets having a disintegration time lower than 30 seconds and having the alprazolam preferably in non-crystalline or partially crystalline form according to the X-ray diffraction crystallography expanded for the position delta 9-12.5 (2 theta), to a patient suffering from said disorder. There is also disclosed a method for preparing a composition according to the invention, where the alprazolam is solved in a pharmaceutical acceptable solvent and a binder, preferably polyvinylpyrrolidone, is incorporated to the solution. A pre-made mixture of part of the cross-linked carboxymethyl-cellulose and the rest of the ingredients of the composition is impregnated with the solution and is dried and grinded, and is added to the rest of the cross-linked carboxymethyl-cellulose and the flavoring additives, being then mixed and compressed. | 2009-08-06 |
20090197874 | SOLID FORMS CONTAINING MELOXICAM WITH IMPROVED BUCCAL TASTE AND PROCESS FOR THEIR PREPARATION - A solid dosage form of meloxicam containing an acid and sugars or polyalcohols or a mixture thereof. | 2009-08-06 |
20090197875 | ARYL-ISOXAZOLO-4-YL-OXADIAZOLE DERIVATIVES - The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula | 2009-08-06 |
20090197876 | INDOLINONE DERIVATIVES SUBSTITUTED IN THE 6 POSITION, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula | 2009-08-06 |
20090197877 | Antibacterial Compositions - Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C | 2009-08-06 |
20090197878 | SUBSTITUTED BENZO[d][1,3]OXAZIN-2(4H)-ONES AND RELATED DERIVATIVES AND THEIR USES FOR MODULATING THE PROGESTERONE RECEPTOR - Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R | 2009-08-06 |
20090197879 | VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS - Compounds having the general structure | 2009-08-06 |
20090197880 | ANTI-VIRAL COMPOUNDS, COMPOSITIONS, AND METHODS OF USE - Disclosed are compounds of Formula (I), pharmaceutically acceptable salts and solvates thereof, compositions thereof, and methods for their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses. | 2009-08-06 |
20090197881 | Azaindole Derivative Having PGD2 Receptor Antagonistic Activity - The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases. | 2009-08-06 |
20090197882 | INDAZOLE DERIVATIVES FOR THE TREATMENT OF HSP90-INDUCED DISEASES - Novel indazole derivatives of the formula (I), in which R | 2009-08-06 |
20090197883 | Diphenyl Substituted Cycloalkanes, Compositions Containing Such Compounds and Methods Of Use - The instant invention provides compounds of Formula (I) which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents. | 2009-08-06 |
20090197884 | Compounds Useful as Antagonists of CCR2 - The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions. | 2009-08-06 |
20090197885 | COMPOSITIONS AND TREATMENTS USING PYRIDAZINE COMPOUNDS AND CHOLINESTERASE INHIBITORS - The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications. | 2009-08-06 |
20090197886 | HEXAHYDRO-CYCLOHEPTAPYRAZOLE CANNABINOID MODULATORS - This invention is directed to a hexahydro-cycloheptapyrazole cannabinoid modulator compound of formula (I): | 2009-08-06 |
20090197887 | PIPERAZINYLPIPERIDINE DERIVATIVES AS CHEMOKINE RECEPTOR ANTAGONISTS - The present invention relates to compounds of Formula I: | 2009-08-06 |
20090197888 | FLUORINATED TRIPEPTIDE HCV SERINE PROTEASE INHIBITORS - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: | 2009-08-06 |
20090197889 | SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. | 2009-08-06 |
20090197890 | PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - A method of treating an SCD-mediated disease or condition in a mammal, preferably a human, includes administering to a mammal a compound of formula (I): | 2009-08-06 |
20090197891 | Use of (4-Alkylpiperazinyl)(phenyl) methanones in the treatment of alzheimer's disease - The invention provides a therapeutic method for treating at least one symptom of Alzheimer's disease in a mammal, such as a human, wherein the toxicity of a pathogen of β amyloid peptide mammalian cells is implicated and inhibition of the subsequently-induced pathological pathways is desired comprising administering to a mammal in need of such therapy, an effective amount of a benzoylpiperazine derivative, including pharmaceutically acceptable salts thereof. | 2009-08-06 |
20090197893 | Methods of Identifying and Treating Individuals Exhibiting Complex Karyotypes - The invention described herein relates to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that harbor complex karyotypes. The present invention also related to mutant BCR-ABL kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant BCR-ABL kinase proteins. | 2009-08-06 |
20090197894 | NICOTINAMIDE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): | 2009-08-06 |
20090197895 | OXAZOLE-PYRROLE-PIPERAZINE ALPHA-HELIX MIMETIC - Amphiphilic α-helix mimetics are provided. These compounds are constructed using an oxazole-pyrrole-piperazine (OPP) scaffold. The amphiphilic α-helix mimetics are also employable for making libraries and for treating diseases or conditions effected by the inhibition or disruption of interactions with the alpha helix of a protein. | 2009-08-06 |
20090197896 | Methods and compositions for increasing solubility of azole drug compounds that are poorly soluble in water - The combination of any two of a polyol, a polyol ether, and a low carbon organic alcohol provides a synergistic effect on the solubility of azole compounds, such as metronidazole, in aqueous fluid. | 2009-08-06 |
20090197897 | Novel Oxadiazole Derivatives and Their Use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R | 2009-08-06 |
20090197898 | SELECTIVE SUBTYPE ALPHA 2 ADRENERGIC AGENTS AND METHODS FOR USE THEREOF - The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors. | 2009-08-06 |
20090197899 | 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 3′,5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5. | 2009-08-06 |
20090197900 | METHODS OF TREATING HEART FAILURE AND RENAL DYSFUNCTION IN INDIVIDUALS WITH AN ADENOSINE A1 RECEPTOR ANTAGONIST - Provided herein are methods of improving, maintaining and restoring renal function, treating heart failure, treating subjects with acute fluid overload, and slowing or reversing an existing or developing renal impairment in subjects with BNP levels of at least 400 pg/mL and/or NT-proBNP levels of at least about 1500 pg/mL by administering a therapeutically effective amount of an AA | 2009-08-06 |
20090197901 | VARIOLIN DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS - Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X | 2009-08-06 |
20090197902 | Use of Pyrimidine Compounds in the Preparation of Parasiticides - The invention relates to the use of compounds of the general formula (I), wherein R | 2009-08-06 |
20090197903 | PROCESS FOR PREPARING SPRAY DRIED FORMULATION OF TMC125 - This invention relates to a process for producing a spray-dried powder comprising microcrystalline cellulose in a solid dispersion of the anti-HIV compound etravirine (TMC125) in a water-soluble polymer. | 2009-08-06 |
20090197904 | Sulphamides for Treatment of Cancer - Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer. | 2009-08-06 |
20090197906 | REVERSION OF MALIGNANT PHENOTYPE WITH 9-HYDROXY ELLIPTICINE DERIVATIVES - The invention relates to the use of 9-hydroxy ellipticine derivatives for the treatment of cancer. 9-hydroxy ellipticine derivatives may prove particularly useful for the treatment of metastatic cancers or cancers escaping conventional cytotoxic chemotherapies. | 2009-08-06 |
20090197907 | NOVEL CRYSTALLINE FORM OF RUPATADINE FREE BASE - The present invention relates to a novel crystalline form of rupatadine free base, process for its preparation and to a pharmaceutical composition containing it. In accordance with the present invention rupatadine is suspended in n-hexane, n-heptane, cyclohexane, diethyl ether or diisopropyl ether, stirred for at least 1 hour, filtered the solid and dried to give crystalline rupatadine form-B. The isolation of novel rupatadine free base as crystalline form-B may be useful as a purification of rupatadine or a salt thereof. | 2009-08-06 |
20090197908 | Benzocycloheptapyridines as inhibitors of the receptor tyrosine kinase met - The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 2009-08-06 |
20090197909 | Bis-Heterocyclic Imidazolyl Compounds - The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R | 2009-08-06 |
20090197910 | NOVEL VIRAL REPLICATION INHIBITORS - The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one benzimidazole conjugates derivative having the general formula (I). The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections. | 2009-08-06 |
20090197911 | LONIDAMINE ANALOGUES AND TREATMENT OF POLYCYSTIC KIDNEY DISEASE - Lonidamine derivatives can be useful in methods of treating, inhibiting, and/or preventing polycystic kidney disease (PKD). Accordingly, lonidamine derivatives can be administered in a therapeutically effective amount for inhibiting, and/or preventing polycystic kidney disease (PKD) in the subject. This can include administering a therapeutically effective amount of the lonidamine derivatives for inhibiting CFTR and/or Hsp90 or biological pathway thereof. Also, the method can include administering the lonidamine derivatives in a therapeutically effective amount for inhibiting ErbB2, Src, Raf-1, B-Raf, MEK, Cdk4, NKCC1, or combinations thereof. For example, the therapeutically effective amount of the lonidamine derivatives can be configured so as to provide a concentration in or adjacent to a kidney cell of about 0.25 uM or more or less. | 2009-08-06 |
20090197912 | Sulfonamide Derivatives for the Treatment of Diseases - The invention relates to compounds of formula (1) | 2009-08-06 |
20090197913 | SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR - The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′: | 2009-08-06 |
20090197914 | Piperidine Derivatives, Their Process for Preparation, Their Use as Therapeutic Agents and Pharmaceutical Compositions Containing Them - The present invention provides a compound of a formula (I) wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state. | 2009-08-06 |
20090197915 | SIGMA RECEPTOR COMPOUNDS - The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals. | 2009-08-06 |
20090197916 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS FOR TREATMENT OF METABOLIC SYNDROME AND RELATED DISORDERS - Compounds, compositions, and methods for inhibiting the onset of metabolic syndrome and treating related disorders in a subject in need of such therapy are disclosed. | 2009-08-06 |
20090197917 | USE OF RIMONABANT FOR THE PREPARATION OF MEDICAMENTS USEFUL IN THE PREVENTION AND TREATMENT OF TYPE 2 DIABETES - The invention relates to the use of rimonabant, either alone or combined with another active ingredient, for the preparation of medicaments useful in the prevention and treatment of type 2 diabetes or non-insulin-dependent diabetes and/or its complications. | 2009-08-06 |
20090197918 | PESTICIDE BENZYLOXY- AND PHENETYL-SUBSTITUTED PHENYL-AMIDINE DERIVATIVES - The present invention relates to benzyloxy- and phenethyl-substituted phenyl-amidine derivatives of formula (I) wherein 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 insects, notably of plants, using these compounds or compositions. | 2009-08-06 |
20090197919 | Novel Method for Preparation of Ammonium Salts of Esomeprazole - The present invention relates to a process for the preparation of quartenary ammoniumsalts of esomeprazole. Further, the present invention also relates to the use quartenary ammoniumsalts of esomeprazole for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the quartenary ammoniumsalts of esomeprazole, as such. | 2009-08-06 |
20090197920 | METHODS AND COMPOSITIONS FOR MODULATING CALCIUM CHANNELS - The present invention relates to methods and compositions for modulating calcium channels. In particular, the present invention provides methods and compositions for modulating (e.g., disrupting) Cav1.3a calcium channels for research and therapeutic methods (e.g., treating dopaminergic diseases and conditions). | 2009-08-06 |
20090197921 | USE OF NICOTINE, ANALOGUES, THEREOF, PRECURSORS THEREOF OR DERIVATIVES THEROF IN THE TREATMENT OF VARIOUS PATHOLOGICAL PROCESSES CAPABLE OF IMPROVEMENT WITH a-MSH ADMINISTERED IN PROPHYLACTIC OR THERAPEUTIC FORM - This invention protects the use of nicotine, analogues thereof precursors thereof or its derivates for treatment of inflammatory, infectious, candidal or degenerative (of the joints and/or of the central nervous system, of kidneys, the lungs, liver), depression, obesity, bone disease and the like, which can be improved by means of intensification of the actions of α-MSH, given the fact that this hormone are extraordinary properties: e.g., it has an antipyretic potency 20,000 times as great as acetaminophen, its antimicrobian potency, is comparable to gentamycine, it is the best anticandidiasic known; it inhibits apoptosis of various stem cells, and significantly modulates the immune reactions, and therefore the use of agents that affect its release may have significant therapeutic potential. This patent protects the use of nicotine, analogues thereof, precursors thereof or its derivates for the purpose of increasing and/or reducing the bioavailability of α-MSH in blood and/or central or peripheral tissues to accentuate or diminish the effect of the α-MSH by means of changes in its concentration or its effect on the corresponding receptors of any cell, tissue or organ in the body, administrated for therapeutic and/or prophylactic purposes in the short medium and/or long term. | 2009-08-06 |
20090197922 | COMPOSITIONS AND METHODS FOR TREATING PULMONARY HYPERTENSION - Compositions and methods of the invention are related to treating pulmonary hypertension using a Raf kinase inhibitor, such as sorafenib. IQ a particular aspect, pulmonary hypertension is pulmonary arterial hypertension. | 2009-08-06 |
20090197923 | METHOD OF PROVIDING PIRFENIDONE THERAPY TO A PATIENT - The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse events associated with the administration of pirfenidone. The invention also discloses a starter pack that may be used in conjunction with the dose escalation scheme. | 2009-08-06 |
20090197924 | 2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R | 2009-08-06 |
20090197925 | O-CYCLOPROPYL-CARBOXANILIDES AND THEIR USE - A compound of formula (I): | 2009-08-06 |
20090197926 | BENZIMIDAZOLES AND THEIR USE FOR THE TREATMENT OF DIABETES - Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, | 2009-08-06 |
20090197927 | JASMONATE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF - The present invention relates to novel jasmonate derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers. | 2009-08-06 |
20090197928 | Novel Receptor Antagonists and Their Methods of Use - The present invention relates to novel isoxazole derivatives of formula (I) which bind to the P2X7 receptor and are capable of interfering with the effects of ATP at the P2X7 receptor: | 2009-08-06 |
20090197929 | Azolylmethyloxiranes, Their Use for Controlling Phytopathogenic Fungi and Agents Containing Said Compounds - The present invention relates to azolylmethyloxiranes of the general formula I | 2009-08-06 |
20090197930 | Eyedrops - It is intended to provide eyedrops which have an ocular tension-lowering effect and a hypotensive effect based on novel function mechanisms. The above-described eyedrops contain a muscle relaxant as the active ingredient and dantrolene sodium is preferably usable as the muscle relaxant employed as the active ingredient. The eyedrops lower the ocular tension via the relaxation of the extraocular muscle tension and lower the blood pressure via the relaxation of the sympathetic nerve tension, thereby exhibiting the ocular tension-lowering effect and the hypotensive effect. | 2009-08-06 |
20090197931 | IMIDAZOLINYLMETHY ARYL SULFONAMIDE - This invention relates to an alpha-1 A receptor partial agonist, which is represented by Formula I: | 2009-08-06 |
20090197932 | IMIDAZOLINYLMETHYL ARYL SULFONAMIDE - This invention relates to an alpha-1A receptor partial agonist, which is represented by Formula I: | 2009-08-06 |
20090197933 | IMIDAZOLINYLMETHYL ARYL SULFONAMIDE - This invention relates to an alpha-1 A receptor partial agonist, which is represented by Formula I: | 2009-08-06 |
20090197934 | IMIDAZOLINYLMETHYL ARYL SULFONAMIDE - This invention relates to an alpha-1A receptor partial agonist, which is represented by Formula I: | 2009-08-06 |
20090197935 | PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 2009-08-06 |
20090197936 | SALTS OF N-HYDROXY-3-[4-[[[2-(2-METHYL-1H-INDOL-3-YL)ETHYL]AMINO]METHYL]PH- ENYL]-2E-2-PROPENAMIDE - Salts of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide are prepared and characterized. | 2009-08-06 |
20090197937 | MARINE ACTINOMYCETE TAXON FOR DRUG AND FERMENTATION PRODUCT DISCOVERY - The invention is the discovery of an actinomycete genus, given the name | 2009-08-06 |
20090197938 | Polyphenol Type Compounds, Compositions Containing Same and Use Thereof for Preventing or Treating Diseases Involving Abnormal Cell Proliferation - The invention concerns compounds of formula (I), wherein —X | 2009-08-06 |
20090197939 | METHODS OF TREATING SKIN WITH AROMATIC SKIN-ACTIVE INGREDIENTS - A method for treating skin, reducing oxidative damage to a skin cell, reducing lipoxygenase (LO) activity in a skin cell, reducing cyclooxygenase (COX) activity in a skin cell, reducing tumor necrosis factor alpha (TNF-α) in a skin cell, or reduction matrix metalloproteinase enzyme activity in a skin cell comprising contacting skin or a skin cell with an aromatic skin-active ingredient. | 2009-08-06 |
20090197940 | CHONDROPSIN-CLASS ANTITUMOR V-ATPase INHIBITOR COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF - A composition comprising a substantially purified compound of the formula: | 2009-08-06 |
20090197941 | Pharmaceutical Compositons for the Treatment of Chronic Obstructive Pulmonary Disease - The invention relates to the use of a combination of cannabinoids for the treatment of Chronic Obstructive Pulmonary Disease (COPD). Preferably the combination of cannabinoids are cannabidiol (CBD) and delta-9-tetrahydrocannabinol (THC). More preferably the cannabinoids are in a predefined ratio by weight of approximately 1:1 of CBD to THC. | 2009-08-06 |
20090197942 | Method For Producing Polyphenol-Rich Composition - An object of the present invention is to provide a method for producing polyphenol-containing compositions and purifying polyphenols safely and simply. By contacting a polyphenol-containing solution to a specific polysaccharide to support polyphenols with the polysaccharide, a polyphenol-containing composition usable as an additive for foods and drinks can be obtained. In addition, polyphenol can be purified by contacting polysaccharide-supported polyphenols with solvent to elute polyphenols into the solvent and then powderizing the polyphenols after removing the solvent. | 2009-08-06 |
20090197943 | Flavonoid Dimers and Methods of Making and Using Such - Multidrug resistance (MDR) is a major problem in cancer chemotherapy. The best characterized resistance mechanism is the one mediated by the over-expression of drug efflux transporters, permeability-glycoprotein (P-gp), which pump a variety of anticancer drugs out of the cells, resulting in lowered intracellular drug accumulation. A series of flavonoid dimers are developed in this invention, which are linked together by linker groups of various lengths. These flavonoid dimers are found to be efficient P-gp modulators that increase cytotoxicity of anticancer drugs in vitro and dramatically enhance their intracellular drug accumulation. It is found that the flavonoid dimers of this invention is also useful in reducing drug resistance in treating parasitic diseases. | 2009-08-06 |
20090197944 | AGENT FOR IMPROVING MUSCLE FORCE - Provision of an agent for improving muscle force and for improving exercise effect. An agent for improving muscle force containing a catechin as an effective ingredient. | 2009-08-06 |
20090197945 | Method for Generating Reference Controls for Pharmacogenomic Testing - Reference controls for use with pharmacogenomic testing, and methods for their identification, preparation, and use, are disclosed. The reference controls can confirm that pharmacogenomic testing correctly identifies individuals that do or do not have the mutation of interest, in both clinical trial and patient treatment settings. The reference controls can be selected to include one or more mutations to be identified, and prescreened to confirm that they bind to one or more of the primers used in the pharmacogenomic testing. The reference controls are human genomic DNA that includes certain identified polymorphisms (mutations) of interest, ideally derived from individuals, pre-selected and optionally properly consented, which have one or more of the polymorphism(s) of interest. The reference controls can be prepared by targeted pre-screening of human patients, by examining the genotype or genetic profile of the patients, isolating cells with the desired mutation, optionally immortalizing the cells, and obtaining DNA from the cells. The prescreening of prospective donors can be targeted based on any of a number of factors, such as genes of interest, mutations within the genes of interest, and membership in a specific ethnic or disease state population. The genomic DNA can be pre-screened for its ability to be detected, using a standard pharmacogenomic test, as including a specific mutation. Examples of mutations of interest include those present in a Phase I or Phase II metabolic enzyme such as CYP2D6, CYP2C19, CYP2C9, CYP2C8, and CYP3A5, CYP3A4, CYP2A6, CYP2B6, UGT1A1, DPD, ERCC1, MDR1, ADH2, NAT1 and NAT2 or any other metabolic or disease gene. | 2009-08-06 |
20090197947 | MEDICAMENTS AND METHODS FOR LOWERING PLASMA LIPID LEVELS AND SCREENING DRUGS - The invention relates to compositions, medicaments, methods for treating individuals with high plasma lipid levels, and methods for screening drug candidates useful in, for example, the treatment of hypercholesterolemia. Specifically, the invention relates to the discovery that MTP inhibition leads to increased accumulation in cellular free-cholesterol and is useful in the development of compositions, medicaments, methods of treatment and drug screening methods to treat high plasma lipid levels. | 2009-08-06 |
20090197948 | Skin External Preparation - The present invention is to provide a skin external preparation with good moisture retention, a rough skin improving effect, and an improved feeling in use. A skin external preparation comprising a polyoxyalkylene glycol/polyethylene glycol copolymer alkyl ether derivative represented by the below-described general formula (I): | 2009-08-06 |
20090197949 | ANTITUMOR METHODS AND COMPOSITIONS COMPRISING SESQUITERPENE DERIVATIVES - The present invention relates to novel antitumor compositions, the use of sesquiterpene derivatives as antitumor agents and to methods of treatment thereof. More precisely, The present invention relates to an antitumor composition comprising a therapeutically effective quantity of at least one sesquiterpene derivative in association with a pharmaceutically acceptable carrier. | 2009-08-06 |
20090197950 | Substituted Fullerenes and Their Use as Inhibitors of Cell Death - This patent discloses the use of water-soluble substituted fullerenes as inhibitors of cell death. The substituted fullerenes comprise a fullerene core (Cn) and at least one of: (i) from 1 to 6 (>CX | 2009-08-06 |
20090197951 | Substituted Fullerene Formulations and Their Use in Ameliorating Oxidative Stress Diseases or Inhibiting Cell Death - This patent discloses a composition comprising a substituted fullerene, wherein the substituted fullerene comprises a fullerene core (Cn), wherein n is an even integer greater than or equal to 60, and at least one substituent group bonded to at least one carbon atom of the fullerene core, and at least one adjuvant, wherein the adjuvant is an absorption enhancer or bioavailability enhancer. It also discloses methods of using such compositions to ameliorate oxidative stress diseases or inhibit cell death. | 2009-08-06 |
20090197952 | Glyceride Esters for the Treatment of Diseases Associated with Reduced Neuronal Metabolism of Glucose - Provided are alternative sources of ketone bodies for reducing or eliminating symptoms of Parkinson's disease, amyotrophic lateral sclerosis (ALS, also called Lou Gehrig's disease), Alzheimer's disease, Huntington's disease, epilepsy and other diseases or disorders characterized by impaired glucose metabolism. The alternative sources of ketone bodies include mono-, di- and triglyceride esters of acetoacetate and mixtures thereof, and/or mono-, di- and triglyceride esters of 3-hydroxybutyrate and mixtures thereof. These glyceride esters can be administered orally as a dietary supplement or in a nutritional composition. | 2009-08-06 |
20090197953 | Pharmaceutical composition for the specific treatment of acute myeloid leukemia - The present invention provides the use of all-trans retinoic acid for the production of a pharmaceutical composition for the treatment of acute myeloid leukemia, which use is characterized in that the patients are selected from the group of non-M3 acute myeloid leukemia patients according to a physiologic concentration, e.g. a level of MN1 below a certain critical level analysed in total blood cells, preferably analysed in bone marrow cells. The critical level of MN1 can be determined according to known methods, e.g. by specific determination of the presence of MN1, e.g. using specific anti-MN1 antibody, e.g. in an ELISA or in another immuno specific assay. Preferably, the level of MN1 is determined at its transcription level, e.g. as the concentration of mRNA encoding MN1. | 2009-08-06 |
20090197954 | Linoleic acid preparations for the topical treatment of male and female pattern androgenetic alopecia, age-related alopecia, and keratosis pilaris - A preparation for the topical application of linoleic acid to treat male and female androgenetic alopecia, age-related alopecia, and keratosis pilaris contains between about 0.1% and about 10%, preferably between about 1% and about 5%, and specifically about 2% linoleic acid by volume in its carrier vehicle. This acts to correct the local linoleic acid deficiency that exists in the follicles in these conditions and provides linoleic acid to suppress growth of Propionibacterium acnes with resultant reduction in its porphyrin production which in turn reduces microinflammation and altered keratinization that damages follicles and eliminates functioning follicles in alopecia and causes follicle plugging in keratosis pilaris. | 2009-08-06 |
20090197955 | METHODS OF IMPROVING DHA DEPOSITION AND RELATED FUNCTION AND/OR DEVELOPMENT - The present invention provides for improved deposition of DHA in human or animal tissues by incorporating healthy lipids containing stearidonic acid into humans or animal through prolonged food or feed, as well as through supplements, and therapeutics. Improved deposition of DHA through consumptions of edible compositions comprising stearidonic acid can be used to improve numerous indicators of health and development, including indicators of heart health, neurological function and development, and the Omega-3 Index in tissues. | 2009-08-06 |
20090197956 | TREATMENT OF ACUTE OTITIS MEDIA WITH XYLITOL AND N-ACETYLCYSTEINE - The present invention relates to the discovery that the treatment of Acute Otis Media (AOM) can be accomplished by a synergistic combination of xylitol and N-acetylcysteine. The treatment with this combination shows that symptoms of AOM can be decreased and or treated to a greater degree than know with xylitol alone. The present invention includes both pharmaceutical compositions and methods of treatment. | 2009-08-06 |
20090197957 | Methods and compositions for the treatment of pain - The present invention relates generally to the area of pain management and more particularly, to a method of analgesia and agents useful for same. More particularly, the present invention relates to a method of analgesia utilising a compound of formula (I). The method of the present invention is useful, inter alia, in the therapeutic or prophylactic treatment of pain, including acute pain, chronic non-malignant pain and chronic malignant pain. Also provided are compounds for use in the method of the invention. | 2009-08-06 |
20090197958 | Sustained Release Particulate Oral Dosage Forms of (R) Baclofen and Methods of Treatment - Sustained release particulate oral dosage forms of (R)-baclofen prodrugs and methods of treating a disease comprising orally administering such dosage forms are disclosed. | 2009-08-06 |
20090197959 | N,N-DISUBSTITUTED AMINOALKYLBIPHENYL ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD | 2009-08-06 |
20090197960 | Method of Inhibiting Polyneuropathic Pain with 3-(2-Dimethylaminomethylcyclohexyl) Phenol - A method of using 3-(2-dimethylaminomethylcyclohexyl)phenol or a pharmaceutically acceptable salt thereof as an active pharmaceutical ingredient for treating or inhibiting polyneuropathic pain, in particular in diabetic polyneuropathy. | 2009-08-06 |
20090197961 | Diclofenac Formulations and Methods of Use - Methods and formulations are provided for treating migraine and other acute pain episodes using diclofenac, and formulations of diclofenac that provide both rapid and sustained relief from acute pain. Methods and formulations are also provided for treating symptoms that often accompany migraine and acute pain such as photophobia, phonophobia, nausea and vomiting. | 2009-08-06 |
20090197962 | SUBSTITUTED CYCLOPENTANES HAVING PROSTAGLANDIN ACTIVITY - Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein. | 2009-08-06 |
20090197963 | Method and compositions for suppressing appetite or treating obesity - The present invention provides a method for reducing the appetite in a mammal by contacting the mammal with an amount of a noxious smelling agent effective in reducing appetite or by contacting the mammal with an agent effective in inhibiting the effect of another agent in stimulating appetite. Also, the present invention provides a method for treating obesity in a mammal by contacting the mammal with an amount of a noxious smelling agent effective in reducing appetite or with an agent effective in inhibiting the effect of another agent in stimulating appetite. Similarly, the present invention provides compositions and kits for both reducing appetite and treating obesity. In some instances, an isonitrile or an isocyanide is present in the composition or kit. | 2009-08-06 |
20090197964 | Methods and compositions for treatment for coronary and arterial aneurysmal subarachnoid hemorrhage - Methods and compositions for treating a complication associated with aneurysmal subarachnoid hemorrhage (SAH), the method comprising administering an effective amount of a nitric oxide precursor to a subject in need thereof. Methods and compositions for treating vasospasm, the method comprising administering an effective amount of a nitric oxide precursor to a subject in need thereof. | 2009-08-06 |