18th week of 2010 patent applcation highlights part 61 |
Patent application number | Title | Published |
20100113420 | PYRROLOPYRIMIDINE DERIVATIVES AS JAK3 INHIBITORS - Pyrrolopyrimidine derivatives of Formula (I) that are useful as JAK3 kinase inhibitors. | 2010-05-06 |
20100113421 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein X, R | 2010-05-06 |
20100113422 | Pyrimido [4,5-D] Azepine Derivatives As 5-HT2C Agonists - The present invention provides a compound of formula (I): | 2010-05-06 |
20100113423 | Modulators of Aldehyde Dehydrogenase and Methods of Use Thereof - The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. | 2010-05-06 |
20100113424 | N-BENZYL PYRROLIDINE DERIVATIVES - The present invention relates to a compound of formula I | 2010-05-06 |
20100113425 | PYRROLOBENZODIAZEPINES - Compounds of the formula I: | 2010-05-06 |
20100113426 | Intranasal Benzodiazepine Compositions - A pharmaceutical composition for intranasal administration to a mammal. The pharmaceutical composition comprises an effective amount of a benzodiazepine or pharmaceutically acceptable salt thereof; and a nasal carrier. In some embodiments, the pharmaceutical composition when administered intranasally produces a rapid physiological response. Pharmaceutical compositions may also include at least one or more sweeteners, flavoring agents, or masking agents or combinations thereof. | 2010-05-06 |
20100113427 | COMPOSITIONS OF 5-HT3 ANTAGONISTS AND DOPAMINE D2 ANTAGONISTS FOR TREATMENT OF DOPAMINE-ASSOCIATED CHRONIC CONDITIONS - The present invention provides novel compositions comprising a combination of a 5-HT | 2010-05-06 |
20100113428 | DIAZABICYCLIC ARYL DERIVATIVES AS CHOLINERGIC RECEPTOR MODULATORS - 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 as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2010-05-06 |
20100113429 | INHIBITORS OF FTSZ AND USES THEREOF - The invention relates to inhibitors of FtsZ polymerization and uses thereof. | 2010-05-06 |
20100113430 | THIOXANTHENE DERIVATES USEFUL TO TREAT INFECTIOUS DISEASES - The present invention is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for treatment of infectious diseases. The invention furthermore relates to compositions comprising said anti-infective agents. | 2010-05-06 |
20100113431 | N-METHYL PIPERAZINE MODULATORS OF H1 RECEPTOR - The present invention relates to new N-methyl piperazine modulators of H1 receptor activity, pharmaceutical compositions thereof, and methods of use thereof. | 2010-05-06 |
20100113432 | PHENOTHIAZINE MODULATORS OF D2 RECEPTORS AND 5-HT2 RECEPTORS - The present invention relates to new phenothiazine modulators of D2 receptor activity and/or 5-HT2 receptor activity, pharmaceutical compositions thereof, and methods of use thereof. | 2010-05-06 |
20100113433 | N-Substituted Thiomorpholine Derivatives as the Inhibitors of Dipeptidyl Peptidase IV and the Pharmaceutical Uses Thereof - The present invention relates to N-Substituted thiomorpholine compounds of formula I, the possible isomers, the pharmaceutically acceptable salts, the solvates, the hydrates or the prodrugs thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV); and to a method for preparing the compounds of formula I, pharmaceutical compositions comprising the compounds of formula I and use of the compounds of formula II in medical field, particularly in the preparation of medicaments for treating and preventing diabetes (in particular type II diabetes), hyperglycemia, X syndrome, hyperinsulinemia, obesity, atherosclerosis and all kinds of diseases modulated by immune system. | 2010-05-06 |
20100113434 | CARBAMATE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 2010-05-06 |
20100113435 | INHIBITORS OF 11-BETA-HYDROXY STERIOD DEHYDROGENASE TYPE 1 - The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme. | 2010-05-06 |
20100113436 | DISPIRO TETRAOXANE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MALARIA AND/OR CANCER - A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=—C(O)NR | 2010-05-06 |
20100113437 | Active Compound Combinations Having Insecticidal and regular, utility - The novel active compound combinations comprising compounds of the formula (I) or (II) and active compounds (1) to (30) listed in the description have very good insecticidal and acaricidal properties. | 2010-05-06 |
20100113438 | CLASS OF HISTONE DEACETYLASE INHIBITORS - New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH | 2010-05-06 |
20100113439 | Antifungal agents - Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions. | 2010-05-06 |
20100113440 | PYRIMIDINE SUBSTITUTED MACROCYCLIC HCV INHIBITORS - Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient. | 2010-05-06 |
20100113441 | SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES - The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia. | 2010-05-06 |
20100113442 | TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES - The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH | 2010-05-06 |
20100113443 | LIQUID FORMULATIONS OF PHOSPHOLIPASE ENZYME INHIBITORS - The present invention relates to liquid formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA | 2010-05-06 |
20100113444 | PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example. | 2010-05-06 |
20100113445 | Chemical Compounds - The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity. | 2010-05-06 |
20100113446 | HYDANTOIN COMPOUNDS - The invention relates to the use of hydantoin compounds useful for treating or preventing autoimmune disorders. The present invention also provides compositions and uses thereof. | 2010-05-06 |
20100113447 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound. | 2010-05-06 |
20100113448 | OXAZOLIDINONE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 - Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. | 2010-05-06 |
20100113449 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): | 2010-05-06 |
20100113450 | Agent for Preventing and Alleviating Wrinkles - The present invention provides an agent for preventing and alleviating wrinkles which has excellent effects of preventing and alleviating wrinkles formed by decreased barrier function of the skin owing to aging or photo aging, that is graphic wrinkles or linear wrinkles. The agent for preventing and alleviating wrinkles consisting of one or more compounds selected from the group consisting of gamma-aminobutyric acid derivatives represented by the following formula (1) or N,N,N-trimethyl gamma-aminobutyric acid represented by the following formula (3) and salts thereof: | 2010-05-06 |
20100113451 | NOVEL PREVENTIVE AND/OR THERAPEUTIC AGENT FOR DIABETIC NEUROPATHY - The present invention relates to an agent for preventing and/or treating diabetic neuropathy comprising a 2-[(substituted-inden-7-yloxy)methyl]morpholine of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The invention is useful for providing an excellent agent for preventing and/or treating diabetic neuropathy, and particularly useful for providing an agent for preventing and/or treating diabetic motor neuropathy (such as muscle weakness disorder (such as muscle weakness disorder with inability to walk independently)), diabetic sensory neuropathy (such as paresthesia (such as vibration perception abnormality), allodynia, hypoesthesia (such as numbness of extremities or cold sensation), or pain), or diabetic autonomic neuropathy (such as stool abnormality (such as constipation or diarrhea), urination disorder, impotence, orthostatic hypotension, sudomotor dysfunction, abnormal heart rate variability, or delayed gastric emptying). Further, the invention is particularly useful for providing an agent for improving pathophysiology of diabetic neuropathy. | 2010-05-06 |
20100113452 | COMPOUNDS FOR TREATING PULMONARY HYPERTENSION - The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing pulmonary hypertension comprising small molecule heterocyclic pharmaceuticals, and more particularly, substituted pyridines and pyridazines optionally combined with at least one additional therapeutic agent. | 2010-05-06 |
20100113453 | Sublingual Formulations of D-Cycloserine and Methods of Using Same - The invention provides methods and compositions for treating anxiety-related disorders in a subject. The methods include sublingually administering D-cycloserine to a subject with the anxiety-related disorder, either alone or in combination with extinction training. | 2010-05-06 |
20100113454 | PYRROLOTRIAZINE KINASE INHIBITORS - The invention provides compounds of formula I | 2010-05-06 |
20100113455 | Method of reducing intraosseous hypertension - A method of treating bone pain caused by osteoarthritis by administering to a patient an effective amount of a composition containing a bone edema medication, such as a vasoactive medication or phosphodiesterase inhibitor, including a PDE-5 inhibitor. | 2010-05-06 |
20100113456 | THERAPEUTIC AGENT FOR CORNEAL DISEASE - A therapeutic agent for a corneal disease comprising irsogladine or a salt thereof as an active ingredient. The purpose is to find a substance capable of effectively treating/ameliorating a corneal disease which has been increased in the number of cases thereof in recent years and to provide a therapeutic agent for a corneal disease comprising the substance as an active ingredient. | 2010-05-06 |
20100113457 | NOVEL PYRIDAZINE DERIVATIVES - The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R | 2010-05-06 |
20100113458 | IMIDAZOPYRIDAZINECARBONITRILES USEFUL AS KINASE INHIBITORS - The invention provides compounds of Formula (I) | 2010-05-06 |
20100113459 | Gene Polymorphisms as Predictors of Tumor Progression and Their Use in Cancer Therapy - The invention provides compositions and methods for determining the likelihood of successful treatment with a pyrimidine based antimetabolite chemotherapy drug and a platinum based chemotherapy drug, such as 5-FU/oxaliplatin. The methods comprise determining the genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response. Patients identified as responsive are then treated with the appropriate therapy. | 2010-05-06 |
20100113460 | Organic Compounds - Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them. | 2010-05-06 |
20100113461 | SUBSTITUTED HETEROCYCLIC COMPOUNDS - The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): | 2010-05-06 |
20100113462 | SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS - The present invention relates to novel compounds of the formula I: | 2010-05-06 |
20100113463 | PTERIDINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses pteridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: | 2010-05-06 |
20100113464 | NOVEL PYRIDAZINE DERIVATIVES - The present invention relates to novel pyridazine derivatives of formula I as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R | 2010-05-06 |
20100113465 | 7-AZASPIRO[3.5]NONANE-7-CARBOXAMIDE COMPOUNDS - Provided herein are 7-azaspiro[3.5]nonane-7-carboxamide compounds and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, cancer and cancer pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease. | 2010-05-06 |
20100113466 | OXAZOLE-PYRIDAZINE-OXAZOLE ALPHA-HELIX MIMETIC - There are provided alpha helix scaffolds mimicking i, i+3/i+4, i+7 or i+11 residues having the general structure oxazole-pyridazine-piperidine or oxazole-pyridazine-oxazole. The common pyridazine heterocycle originates from substituted or unsubstituted dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate. These scaffolds are synthetic counterparts of amphiphilic alpha helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix. | 2010-05-06 |
20100113467 | Organic Compounds - The invention relates to naphthalene carboxylic acid and isoquinoline carboxylic acid amides, and related compounds of formula I | 2010-05-06 |
20100113468 | QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 2010-05-06 |
20100113470 | BCR-ABL VARIANTS - A splice variant of bcr-abl mRNA that produces BCR-ABL protein with a truncated C-terminus and its role in resistance to treatment with kinase inhibitors is disclosed. Vectors for expressing the truncated gene product are provided as well as recombinant cells that express the truncated gene product from a cDNA construct. Also provided are methods compositions and kits for detecting the BCR-ABL splice variant. Additionally, methods for screening BCR-ABL kinase domain inhibitors which rely on the recombinant cells and methods of predicting likelihood for resistance of a CML patient with a BCR/ABL translocation respond to treatment with one or more BCR-ABL kinase inhibitors are also disclosed. | 2010-05-06 |
20100113471 | 2-Aminoaryloxazole compounds as tyrosine kinase inhibitors - The present invention relates to novel compounds selected from 2-aminoaryloxazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl, FGFR3 and/or Flt-3 inhibitors. | 2010-05-06 |
20100113472 | COMPOUNDS FOR THE TREATMENT OF OSTEOPOROSIS AND CANCERS - Methods are provided for the treatment of osteoporosis and multiple myeloma, using 3-imidazoyl-pyrazolo[3,4-b]pyridine compounds. | 2010-05-06 |
20100113473 | ARYL AMIDE COMPOUND AS AN ACETYL COENZYME A CARBOXYLASE INHIBITOR - An aryl amide compound of Formula (I): | 2010-05-06 |
20100113474 | Antineoplastic Combinations of 4-Anilino-3-Cyanoquinolines and Capecitabine - A combination of a 4-anilino-3-cyanoquinoline compound (e.g. HKI-272, SKI-606, EKB-569) and a capecitabine compound in the treatment of a neoplasm is provided. Regimens, kits, and methods for treatment of neoplasm, including breast cancer including metastatic breast cancer, and lung cancer, using this combination, optionally in combination with other anti-neoplastic agents, or immune modulators are also described. | 2010-05-06 |
20100113475 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 2010-05-06 |
20100113476 | CHEMICAL LINKERS WITH SINGLE AMINO ACIDS AND CONJUGATES THEREOF - The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them. | 2010-05-06 |
20100113477 | Inhibitors of mycobacterium tuberculosis malate synthase, methods of making and uses thereof - The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided. | 2010-05-06 |
20100113478 | INDOLONE MODULATORS OF 5-HT3 RECEPTOR - The present invention relates to new indolone modulators of 5-HT3 receptor, pharmaceutical compositions thereof, and methods of use thereof. | 2010-05-06 |
20100113479 | PROCESS FOR THE PREPARATION OF TRI-SUBSTITUTED PYRIDINE AND TRI-SUBSTITUTED PYRIMIDINE DERIVATIVES USEFUL AS GDIR AGONISTS - The present invention is directed to novel processes for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. | 2010-05-06 |
20100113480 | PROCESS FOR THE PREPARATION OF TRI-SUBSTITUTED PYRIDINE AND TRI-SUBSTITUTED PYRIMIDINE DERIVATIVES USEFUL AS GDIR AGONISTS - The present invention is directed to novel processes for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. | 2010-05-06 |
20100113481 | USE OF SERUM AMYLOID A GENE IN DIAGNOSIS AND TREATMENT OF GLAUCOMA AND IDENTIFICATION OF ANTI-GLAUCOMA AGENTS - The present invention provides compositions and methods for treating glaucoma, methods for diagnosing glaucoma, and methods for identifying agents which may be useful in the treatment of glaucoma. More specifically, the present invention describes the use of agents that modulate the expression of serum amyloid A, wherein such agents are inhibitors of p38 MAPkinase. | 2010-05-06 |
20100113482 | Novel Compounds for Treating Mental Disorders, and Preparation and Uses Thereof - The present invention relates to a compound of formula (I), an optical isomer or a pharmaceutically acceptable salt thereof, its preparation and uses, wherein R is defined as herein. Such compounds can be presented as an optical isomer or a racemic mixture. The compounds can be metabolized in vivo to form a pharmacologically active substance as antagonist of neurotransmitters, and can be used for the treatment of the related mental disorders such as schizophrenia. | 2010-05-06 |
20100113483 | COMPOSITIONS OF 5-HT3 ANTAGONISTS AND DOPAMINE D2 ANTAGONISTS FOR TREATMENT OF DOPAMINE-ASSOCIATED CHRONIC CONDITIONS - The present invention provides novel compositions comprising a combination of a 5-HT | 2010-05-06 |
20100113485 | Piperidinylamino-thieno[2,3-D] Pyrimidine Compounds - The invention relates to 5-HT receptor modulators, particularly 5-HT | 2010-05-06 |
20100113486 | USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS - A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act. | 2010-05-06 |
20100113487 | PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient. | 2010-05-06 |
20100113488 | MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS - The present invention relates generally to novel macrocycles of Formula (I): | 2010-05-06 |
20100113489 | MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS - The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin- 4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: | 2010-05-06 |
20100113490 | Substituted Pyrimidine Ether Compounds and use thereof - The invention relates to substituted pyrimidine ether compounds having general formula I: | 2010-05-06 |
20100113491 | SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS - A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM. | 2010-05-06 |
20100113492 | Substituted Aminopyrimidines as Cholecystokinin-1 Receptor Modulators - Certain novel substituted aminopyrimidines are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes. | 2010-05-06 |
20100113493 | (PYRROLIDIN-2-YL)PHENYL DERIVATIVES - The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I | 2010-05-06 |
20100113494 | 13,13a-Dihydroberberine Derivatives For Use In Pharmaceutical Compositions - The present invention provides 13,13a-dihydroberberine derivatives or their physiologically acceptable salts represented by the following formula, pharmaceutical compositions comprising the same, and uses thereof. The 13,13a-dihydroberberine derivatives have an activity of promoting glucose absorption in muscle cells, and the whole animal tests show that the present compounds have effects on improving glucose-tolerance and insulin-resistance, facilitating weight loss, relieving fatty liver and the like. Thus, the present compounds can be used in treating diabetes mellitus, adiposity, fatty liver and complications thereof induced by insulin resistance. | 2010-05-06 |
20100113496 | PIPERIDINE MODULATORS OF VMAT2 - The present invention relates to new piperidine modulators of VMAT2, nicotinic acetylcholine receptors, and/or μ-opioid receptors, pharmaceutical compositions thereof, and methods of use thereof. | 2010-05-06 |
20100113497 | GABA CONJUGATES AND METHODS OF USE THEREOF - In one aspect, the present invention provides a composition of a covalent conjugate of a GABA analog with a drug. In another aspect, the present invention provides methods for treating pain and neurological disorders using the conjugates of GABA analogs. | 2010-05-06 |
20100113498 | NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES - The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors. | 2010-05-06 |
20100113499 | MEDICAMENT FOR THE TREATMENT OF ENDOMETRIOSIS - The use of a dopamine agonist in the manufacture of a medicament for the treatment or prevention of endometriosis. | 2010-05-06 |
20100113500 | ORALLY BIOAVAILABLE PRODUCTS OF (+)-3-HYDROXYMORPHINAN FOR PARKINSON'S DISEASE PREVENTION OR TREATMENT - The present invention is directed to a novel prodrug of (+)-3-hydroxymorphinan compound of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the same, and its use for preventing or treating Parkinson's disease. | 2010-05-06 |
20100113501 | Ophthalmic Composition Comprising Ascomycin - This invention relates to topical ophthalmic compositions comprising an ascomycin e.g. for the treatment of inflammatory diseases such as blepharitis. | 2010-05-06 |
20100113502 | Novel Tetrahydro-1H-Pyrido[4,3-b] Indole Derivatives as CB1 Receptor Ligands - Compounds of formulae I, or pharmaceutically acceptable salts thereof: wherein R | 2010-05-06 |
20100113503 | CYCLOALKANE[B]AZAINDOLE ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD | 2010-05-06 |
20100113504 | AMIDE COMPOUNDS AND THEIR USE AS ANTITUMOR AGENTS - The present invention relates to a compound of Formula (I), its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemate, as well as pharmaceutically acceptable salts thereof, wherein R is selected from CONHOH, CONHCH | 2010-05-06 |
20100113505 | AMINO-NAPHTHYRIDINE DERIVATIVES - The present invention relates to new compounds having an amino-naphthyridine group. In particular, the present invention relates to new compounds, its stereoisomers and pharmaceutically acceptable salts or solvates thereof having a first unit (moiety) selected from the group of a phenyl derivative, a biphenyl derivative or a diphenyl alkane derivative and at least one amino-naphthyridine group linked with the first unit via a linking group. In specific embodiments, the present invention relates to compounds having a phenyl derivative unit and three amino-naphthyridine groups bound to the phenyl derivative unit via a linking group as well as salts or solvates thereof, in particular, pharmaceutically acceptable salts or solvates thereof. Further, the present invention relates to pharmaceutical compositions comprising said compounds. The compounds are particularly useful for treating or preventing infections, like viral infections. | 2010-05-06 |
20100113506 | COMPOSITION FOR PREVENTING OR TREATING THROMBUS- OR EMBOLUS- ASSOCIATED DISEASE - Provided is a composition for the prevention or treatment of a thrombus- or embolus-associated disease, which comprises, as active ingredients to be applied in combination, at least one selected from the group consisting of clopidogrel and its pharmaceutically acceptable salts and at least one selected from the group consisting of icosapentaenoic acid as well as its pharmaceutically acceptable salts and esters. | 2010-05-06 |
20100113507 | 3-Tetrazolyl Indazoles, 3-Tetrazolyl Pyrazolopyridines, and use Thereof - The present application relates to novel 3-tetrazolylindazole and 3-tetrazolylpyrazolo[3,4-b]-pyridine derivatives, processes for their preparation, their use alone or in combination for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders. | 2010-05-06 |
20100113508 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 2010-05-06 |
20100113509 | MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR. | 2010-05-06 |
20100113510 | QUINUCLIDINOL DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS - The invention provides compounds of formula (I) wherein R | 2010-05-06 |
20100113511 | Mono Quaternary Ammonium Salts and Methods for Modulating Neuronal Nicotinic Acetylcholine Receptors - Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders. | 2010-05-06 |
20100113513 | QUINOLINE DERIVATIVES AS FUNGICIDES - Compounds of the general formula (I) wherein the substituents are as defined in claim | 2010-05-06 |
20100113514 | FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present invention relates to sodium channel inhibitors of Formula : | 2010-05-06 |
20100113515 | PTEN INHIBITOR OR MAXI-K CHANNELS OPENER - A new PTEN opener or a new opener of a large conductance Ca | 2010-05-06 |
20100113516 | QUINOLYNYLMETHYLIMIDIZOLES AS THERAPEUTIC AGENTS - Disclosed herein is a compound of the formula (I):(I). Therapeutic methods, compositions and medicaments related thereto are also disclosed. | 2010-05-06 |
20100113517 | METHOD FOR THE TREATMENT OF FABRY DISEASE USING PHARMACOLOGICAL CHAPERONES - The present invention provides a method treating a patient with Fabry disease by determining whether there is an improvement of a surrogate marker that is associated with Fabry disease following administration of a specific pharmacological chaperone of α-galactosidase A. The method includes administering an effective amount of 1-deoxygalactonojirimycn to the individual, wherein the 1-deoxygalactonojirimycin binds to alpha-galactosidase A in an amount effective to increase activity of the alpha-galactosidase A. The present invention also provides a method for monitoring and increasing a therapeutic response of a patient with Fabry disease following administration of a specific pharmacological chaperone of α-galactosidase A by evaluating the effect on the cytoplasmic staining pattern of a cell from the patient, wherein detection of a staining pattern in the cell that is similar to the staining pattern in a cell from a healthy individual indicates that the individual with Fabry disease is a responder. | 2010-05-06 |
20100113518 | METHODS OF USING ANTI-INFLAMMATORY COMPOUNDS - The invention relates to the use of 3-(2′,2′-dimethylpropanoylamino)-tetrahydropyridin-2-one for preparing a medicament intended to prevent or treat inflammatory disorders. | 2010-05-06 |
20100113519 | 1,5-Dideoxy-1,5-imino-D-glucitol Compounds - 1,5-Dideoxy-1,5-imino-D-glucitol compounds as shown in the specification. Also disclosed is a method of treating a hexosaminidase-associated disease. | 2010-05-06 |
20100113520 | KINASE KNOCKDOWN VIA ELECTROPHILICALLY ENHANCED INHIBITORS - Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same. | 2010-05-06 |
20100113521 | PHARMACEUTICAL COMPOSITIONS COMPRISING 2-METHOXY-5-(5-TRIFLUOROMETHYL-TETRAZOL-1-YL-BENZYL)-(2S-PHENYLPIPERIDIN-- 3S-YL-) - The present invention relates to pharmaceutical compositions comprising the NK1 receptor antagonist [2-Methoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-benzyl]-(2S-phenyl-piperidin-3S-yl)-amine, or a pharmaceutically acceptable salt or solvate thereof, and a sodium channel blocker, as a combined preparation for simultaneous or sequential administration and to the use of such compositions in the treatment of certain disorders, including epilepsy, mood disorders and pain. | 2010-05-06 |
20100113522 | COMPOUNDS FOR THE MODULATION OF PPARgamma ACTIVITY - Modulators of PPARγ activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity. | 2010-05-06 |
20100113523 | Tryptase Enzyme Inhibiting Aminopyridines - Disclosed herein are novel compounds and pharmaceutical compositions comprising these compounds. In some embodiments, the compounds are inhibitors of the tryptase enzyme and are useful for treating allergic rhinitis, asthma, vascular injury (e.g., restenosis and atherosclerosis), inflammatory bowel disease, arthritis, psoriasis, anaphylaxis, wounds, infections, and other allergy and inflammatory related diseases. | 2010-05-06 |