36th week of 2009 patent applcation highlights part 42 |
Patent application number | Title | Published |
20090221542 | Inhibition of Inflammatory Cytokine Production With Tanshinones - Provided are methods of attenuating release of a proinflammatory cytokine from a mammalian cell. Also provided are methods of inhibiting or treating an inflammatory cytokine cascade in a mammal. Further provided are methods of treating a mammal at risk for or undergoing sepsis, septicemia, and/or endotoxic shock. Additionally provided are methods of attenuating NO release from a mammalian cell. Also provided are methods of attenuating NO production in a mammal at risk for, or having, a disorder mediated by excessive NO production. | 2009-09-03 |
20090221543 | NEW CORTICOSTEROIDS - Nitrooxy derivatives of steroidal compounds of general formula | 2009-09-03 |
20090221544 | METHODS FOR THE TREATMENT OF A TRAUMATIC CENTRAL NERVOUS SYSTEM INJURY VIA A TAPERED ADMINISTRATION PROTOCOL - The present invention provides methods for the treatment or the prevention of neuronal damage in the CNS. Specifically, the methods of the invention provide for the administration of a therapeutically effective amount of a progestin or progestin metabolite following a traumatic or ischemic injury to the CNS such that, prior to termination of administration of the progestin or progestin metabolite the administration is tapered to avoid withdrawal. The drug taper employed can involve a linear taper, an exponential taper, progressively dividing administered doses by 50%, or can be determined based on the treating physician's assessment of the patient's response to therapy. The tapered administration methods of the present invention may be used in combination with any therapeutic protocol or regimen for the administration of a therapeutically effective amount of a progestin or progestin metabolite to treat a traumatic or ischemic CNS injury. | 2009-09-03 |
20090221545 | Ophthalmic Pharmaceutical Composition Containing Amphiphilic Polyaspartamide Copolymers - The present invention relates in general to the use of amphiphilic graft-type copolymers of polyaspartamide for the ophthalmic administration of drugs, such as for example steroidal and non-steroidal anti-inflammatory agents, antimicrobial agents such as aminoglycosides, macrolides, cephalosporin, tetracycline, quinolones, penicillin, beta-lactams, anti-glaucoma agents such as prostaglandins, alpha- and beta-blockers, inhibitors of carbonic anhydrase, cannabinoids, antiviral agents, diagnostic agents, anti-angiogenic agents, antioxidants. | 2009-09-03 |
20090221546 | INHIBITORS OF FACTOR XA AND OTHER SERINE PROTEASES INVOLVED IN THE COAGULATION CASCADE - Compounds useful as intermediates for synthesis of compounds of Formula (1): | 2009-09-03 |
20090221547 | Immunosuppressant Compounds and Compositions - The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. This application relates to compounds selected from Formula (Ia), (Ib), (Ic) and (Id). | 2009-09-03 |
20090221548 | MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I | 2009-09-03 |
20090221549 | ANTIHYPERTENSIVE THERAPY - A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers. | 2009-09-03 |
20090221550 | COMPOSITIONS FOR TREATMENT OF SYSTEMIC MASTOCYTOSIS - The present invention relates to the use of the combination of tyrosine phosphate inhibitors AMN107 and PKC412 for the preparation of a drug for the treatment of a mast cell-related proliferative disease. The present invention is also drawn to a combination treatment of a tyrosine phosphate inhibitor and a TK-inhibitor that is effective against a mast cell-related proliferative disease, including especially systemic mastocytosis (SM) including aggressive SM (ASM) and mast cell leukemia (MCL). | 2009-09-03 |
20090221551 | SUBSTITUTED FUSED[1,2] IMIDAZO[4,5C] RING COMPOUNDS AND METHODS - [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed. | 2009-09-03 |
20090221552 | Methods for the Treatment of ADHD and Related Disorders - The invention features methods, compositions, and kits for the treatment of attention deficit hyperactivity disorder and related behavioral disorders by administering an organic cation 3 (hOCT3) inhibitor. | 2009-09-03 |
20090221554 | METHOD OF TREATING COGNITIVE IMPAIRMENT - Disclosed is an method of treating cognitive impairment, including administering to a subject in need thereof a combination of a therapeutic agent for neurodegenerative disease and a therapeutically effective amount of a heterocyclic compound represented by the following general formula (I): | 2009-09-03 |
20090221555 | FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND c-MET INHIBITORS - The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R | 2009-09-03 |
20090221556 | HYDROXY AND ALKOXY SUBSTITUTED 1H-IMIDAZOQUINOLINES AND METHODS - 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed. | 2009-09-03 |
20090221557 | 3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 2009-09-03 |
20090221558 | METHODS OF MODULATING THE ACTIVITY OF THE MC5 RECEPTOR AND TREATMENT OF CONDITIONS RELATED TO THIS RECEPTOR - The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases. | 2009-09-03 |
20090221559 | BENZODIAZEPINES AS HCV INHIBITORS - The present invention relates to the use of benzodiazepines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to benzodiazepine compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents. | 2009-09-03 |
20090221560 | Pharmaceutical Formulation - This invention relates to a stable pharmaceutical formulation containing olanzapine. The composition comprises olanzapine or a pharmaceutically acceptable salt thereof, one or more suitable pharmaceutical excipients and a compound of formula (I) and/or a compound of formula (II): or a pharmaceutically acceptable salt thereof. | 2009-09-03 |
20090221561 | Cell Migration Modulating Compounds - The described invention relates to compounds which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis. | 2009-09-03 |
20090221563 | ORAL SUSPENSION COMPRISING MELOXICAM - The present invention relates to an oral suspension comprising meloxicam, its preparation and its use in alleviating inflammation and pain in both acute and chronic musculo-skeletal disorders. | 2009-09-03 |
20090221564 | Heterocyclic Compounds and Their Use in the Treatment of Cardiovascular Disease - Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R | 2009-09-03 |
20090221565 | NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS - A subject of the invention is the compounds of formula (I): | 2009-09-03 |
20090221566 | INHIBITORS OF PHOSPHODIESTERASE TYPE-IV - The present invention relates to oxazine derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CMS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors. | 2009-09-03 |
20090221567 | MUSCARINIC RECEPTOR AGONISTS, COMPOSITIONS, METHODS OF TREATMENT THEREOF, AND PROCESSES FOR PREPARATION THEREOF 177 - Compounds of Formula I, or pharmaceutically acceptable salts thereof: | 2009-09-03 |
20090221568 | Synthesis of Inhibitors of FtsZ - FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity. | 2009-09-03 |
20090221569 | USE OF LHRH ANTAGONISTS FOR INTERMITTENT TREATMENTS - The invention relates to methods of treatment or prophylaxis of physiological and/or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonistsuch that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration. | 2009-09-03 |
20090221570 | Uses of 2-Phenyl-Substituted Imidazotriazinone Derivatives for Treating Pulmonary Hypertension - The present invention relates to the use of PDE 5 inhibitors generally and in particular of known 2-phenyl-substituted imidazotriazinone derivatives for manufacturing medicaments for the treatment of pathological states which can be treated by raising cGMP levels in certain tissues, such as, for example, of, for example: primary pulmonary hypertension, secondary pulmonary hypertension, pulmonary arterial hypertension, portopulmonary hypertension, hepatopulmonary syndrome, pulmonary hypertension caused by medicaments (amphetamines), interstitial lung disease, pulmonary hypertension occurring with HIV, thromboembolic pulmonary hypertension, pulmonary hypertension in children and neonates, pulmonary hypertension induced by atmospheric hypoxia (altitude sickness), COPD, emphysema, chronic bronchial asthma, mucoviscidosis-related pulmonary hypertension, right heart failure, left heart failure and global failure, and which can be treated by raising cGMP levels in certain tissues, such as, for example, isolated systiolic hypertension (ISH) and hardening of blood vessels, specifically of arterial blood vessels, and combination of PDE 5 inhibitors generally and in particular of known 2-phenyl-substituted imidazotriazinone derivatives with further therapeutic agents in the said indications. | 2009-09-03 |
20090221571 | HIV INTEGRASE INHIBITORS - Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 2009-09-03 |
20090221572 | 4,5,6,7-TETRAHYDROBENZO[B]THIOPHENE DERIVATIVES AND THEIR USE AS SIGMA RECEPTOR LIGANDS - The present invention relates to compounds having pharmacological activity towards the sigma (σ) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis. | 2009-09-03 |
20090221573 | Use of Activators of Soluble Guanylate Cyclase for Promoting Wound Healing - The present invention relates to a method for promoting wound healing by administering one or more compounds identified in the claims, and to pharmaceutical compositions containing such compounds. | 2009-09-03 |
20090221574 | 5-Lipoxygenase-Activating Protein (FLAP) Inhibitors - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases. | 2009-09-03 |
20090221575 | Sulfonamide derivatives and use thereof for the modulation of metalloproteinases - The present invention is related to sulfonamide derivatives of Formula (Ia) | 2009-09-03 |
20090221576 | Pharmaceutical Use of 2-Hydroxy-3-[5-(Morpholin-4-Ylmethyl) Pyridin-2-YL]-1H-IN-Dole-5-Carbonitrile as a Free Base or Salts - New use of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile as a free base or a pharmaceutically acceptable salt thereof, in a method of prevention and/or treatment of bone-related disorders, osteoporosis, increasing bone formation or increasing bone mineral density. | 2009-09-03 |
20090221577 | COMPOUNDS HAVING MORPHOLINYL AND PIPERIDINYL GROUPS FOR USE AS GLYT1 INHIBITORS - The invention provides a compound of formula (I) or a salt or solvate thereof: | 2009-09-03 |
20090221578 | Organic Compounds - There are provided according to the invention compounds of formula (I) | 2009-09-03 |
20090221579 | Substituted Amino-Compounds and Uses Thereof - This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 2009-09-03 |
20090221580 | Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase - This invention comprises the novel compounds of formula (I) wherein R | 2009-09-03 |
20090221581 | Methods of treating pain - The invention relates to methods of treating any type of pain comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. | 2009-09-03 |
20090221582 | Piperazine Derivatives And Their Use In Therapy - Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB | 2009-09-03 |
20090221583 | NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE - The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 2009-09-03 |
20090221584 | Bisaryl-sulfonamides - Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ or PPARδ. In particular, the compounds of the invention modulate the function of PPARγ or PPARδ. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis. | 2009-09-03 |
20090221585 | NOVEL COMPOUNDS AND THEIR USE RELATED TO COMPOSITIONS FOR TREATING DISEASE - Novel compounds and their uses are disclosed herein. | 2009-09-03 |
20090221586 | OXAZOLE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: | 2009-09-03 |
20090221587 | NOVEL INSECTICIDES - Compounds of formula (I), wherein the substituents are as defined in claim ( | 2009-09-03 |
20090221588 | FUNGICIDAL COMPOSITIONS - A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of Formula (I) or a compound of Formula (II) wherein R | 2009-09-03 |
20090221589 | Use of aminoalcohol derivatives for the treatment of overactive bladder - The present invention relates to the use of new beta-agonists of general formula (Ia) or (Ib) wherein the groups R | 2009-09-03 |
20090221590 | SALT OF CD 80 ANTAGONIST - The choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide (I) has good aqueous solubility and is therefore convenient for pharmaceutical use. | 2009-09-03 |
20090221591 | Selective Inhibitors of Human Corticosteroid Synthases - The invention relates to compounds for selectively inhibiting human corticosteroid synthases CYP1 1 B1 and CYP1 1 B2, and to the production and use thereof for treating hypercortisolism, diabetes mellitus, hyperaldosteronism, cardiac insufficiency, myocardial fibrosis, depression, age-related cognitive decline and metabolic syndrome. | 2009-09-03 |
20090221592 | Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor - The dodecylsulfate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]- | 2009-09-03 |
20090221593 | TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or a salt thereof: | 2009-09-03 |
20090221594 | STABLE PHARMACEUTICAL COMPOSITIONS OF 5, 10 METHYLENETRAHYDROFOLATE - The invention provides a stable lyophilized composition of 5,10 methylenetetrahydrofolate suitable for use in the treatment of cancer and other therapies. The composition comprises 5,10-MTHF in combination with citric acid and ascorbic acid, with the ratio of citric acid to ascorbic acid from about 0.75:1 to about 2.25:1 by weight, and the ratio of total citric acid and ascorbic acid to 5,10-MTHF from about 1.4:1 to about 3.4:1 by weight. Prior to lyophilization, the solution is adjusted to an essentially neutral pH. | 2009-09-03 |
20090221595 | Crystalline form of sitagliptin - A Sitagliptin crystalline form characterized by PXRD pattern having any 5 peaks selected from the group consisting of 7.4, 11.5, 16.7, 17.7, 18.9, 24.1, 24.5, 27.0, 28.5 and 28.8±0.2 degrees 2-theta, wherein any combination of peaks selected includes the peak at 7.4±0.2 degrees two theta, processes for preparing said Sitagliptin crystalline form, and pharmaceutical compositions thereof, are provided. | 2009-09-03 |
20090221596 | Substtituted aryl oximes - The invention relates to compounds of the formula (I) | 2009-09-03 |
20090221597 | HETEROARYL DERIVATIVES AS CFTR MODULATORS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. | 2009-09-03 |
20090221598 | Use of Sanglifehrin in HCV - The present invention discloses the use of a cyclophilin-binding compound such as a sanglifehrin for the treatment and prevention of hepatitis C and related diseases such as liver fibrosis, liver cirrhosis and hepatocellular carcinoma. | 2009-09-03 |
20090221599 | PHTHALAZINONE PYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS - Objects of the present invention are the compounds of formula I | 2009-09-03 |
20090221600 | PYRIDO-PYRIDIMIDINE DERIVATIVES USEFUL AS ANTIINFLAMMATORY AGENTS - Provided are novel pyrido-pyrimidine derivatives, having the structure of Formula (I): which can be used as anti-inflammatory agents. Also provided are pharmaceutical compositions comprising one or more pyrido-pyrimidine derivatives, as well as methods of treating autoimmune diseases, inflammation or associated pathologies, including for example, sepsis, rheumatoid arthritis, inflammatory bowel disease, type-1 diabetes, asthma, chronic obstructive pulmonary disorder, organ transplant rejection and psoriasis, comprising administering such compounds or pharmaceutical compositions comprising them. | 2009-09-03 |
20090221601 | Methods of identifying and treating individuals exhibiting mutant kit protein - The invention described herein relates to methods of identifying and treating individuals with protein tyrosine kinase associated disorders that have, or may, become resistant to treatment with a kinase inhibitor such as imatinib due to a gain-of-function mutation in KIT tyrosine kinase. | 2009-09-03 |
20090221602 | PROCESSES FOR PREPARING SUBSTITUTED PYRIMIDINES - The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions. | 2009-09-03 |
20090221603 | HETEROCYCLIC AMIDE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of heterocyclic amides are disclosed of the general formula (1) where Z is N or ═CHNR | 2009-09-03 |
20090221604 | Thiazole Compounds and Their Use as PGD2 Antagonists - A compound for use as a PGD2 antagonist is of structural formula [1] in which: A represents a fully saturated or partially unsaturated monocyclic 5-7 membered ring containing one or two nitrogen atoms; B represents a direct bond, an optionally substituted methylene group, an optionally substituted nitrogen atom, oxygen, or S(O) | 2009-09-03 |
20090221605 | SUBSTITUTED PYRROLE-2, 5-DIONES AS PROTEIN KINASE C INHIBITORS - A compound of formula I | 2009-09-03 |
20090221606 | CRYSTALLINE (3-CYANO-1H-INDOL-7-YL)-[4-(4-FLUOROPHENETHYL) PIPERAZIN-1-YLIMETHANONE PHOSPHATE - The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms. | 2009-09-03 |
20090221607 | Piperazine Derivatives - Compounds of general formula (I) | 2009-09-03 |
20090221608 | PYRAZOLE COMPOUNDS - The present invention is directed to compounds of Formula (I), | 2009-09-03 |
20090221609 | Gene Predictors of Response to Metastatic Colorectal Chemotherapy - The present invention provides for the identification of genes that are expressed in tumors that are responsive to a given therapeutic regime and whose expression correlates with responsiveness to that therapeutic regime. One or more of the genes of the present invention can be used as markers to identify patients that are likely to be successfully treated by a therapeutic regime. | 2009-09-03 |
20090221610 | Compositions and Methods for Treating Cognitive Disorders - The present invention relates to the use of inhibitors or blockers of I | 2009-09-03 |
20090221611 | Fused Triazole Tachykinin Receptor Antagonists - The present invention is directed to certain fused triazole compounds which are useful as neurokinin-1 (NK-I) 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 their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. | 2009-09-03 |
20090221612 | CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 2009-09-03 |
20090221613 | Use of Adenine-Derived Compounds for the Treatment of Lupus - The invention relates to the use of adenine-derived compounds substituted in the 2- and 9-positions and, optionally, in the N(6)-position of the adenine, for the manufacture of a medicament for use in the treatment of systemic lupus erythematosus (SLE). The compounds can also be used in combination with a second compound used in the treatment of SLE. | 2009-09-03 |
20090221614 | SELECTIVE SERINE/THREONINE KINASE INHIBITORS - Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue. | 2009-09-03 |
20090221615 | COMBINATION ANTI-CANCER AGENTS - The present disclosure relates to methods of treating cancer in mammals by administration of Lucanthone and at least one anti-metabolite. Pharmaceutical compositions and kits comprising Lucanthone and at least one anti-metabolite also are disclosed. | 2009-09-03 |
20090221616 | QUINAZOLINE DERIVATIVES AS EGF AND/OR ERBB2 TYROSINE KINASE INHIBITORS - A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man. | 2009-09-03 |
20090221617 | LEAD COMPOUND OF ANTI-HYPERTENSIVE DRUG AND METHOD FOR SCREENING THE SAME - A system for screening a small molecule library with 250,000 molecules to find out a compound of an anti-hypertensive drug aiming at human Angiotensin II type IA receptor is provided. The system includes a first database having a three-dimensional structure datum of a human Angiotensin II type IA receptor, a second database having molecular data of a plurality of small molecules, and a computer acquiring the three-dimensional structure datum and the molecular data from the first database and the second database respectively, wherein the computer has a molecular docking software for calculating a free energy of the human Angiotensin II type IA receptor bound to each of the plurality of small molecules, ranks the plurality of small molecules according to the respective free energy so as to select a top small molecule in the ranking as the compound of the drug. | 2009-09-03 |
20090221618 | AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or a salt thereof: | 2009-09-03 |
20090221619 | NOVEL MATERIALS AND METHODS FOR THE PRODUCTION THEREOF - The present invention relates to, inter alia, methods for the treatment of wallboards with fungicides and the treated wallboards. In particular, the invention relates to the treatment of wallboards with synergistic combinations of an anilinopyrimidine fungicide and other fungicides. The invention also provides the treatment of building materials with synergistic mixtures containing an anilinopyrimidine fungicide. More specifically the anilinopyrimidine fungicide is cyprodinil. | 2009-09-03 |
20090221620 | GENTIC POLYMORPHISMS ASSOCIATED WITH STROKE, METHODS OF DETECTION AND USES THEREOF - The present invention provides compositions and methods based on genetic polymorphisms that are associated with vascular diseases such as stroke. In particular, the present invention relates to genetic polymorphisms that have utility for such uses as predicting disease risk or predicting an individual's response to a treatment such as statins, including groups of polymorphisms that may be used as a signature marker set for such uses, as well as nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection. | 2009-09-03 |
20090221622 | TOPOTECAN READY TO USE SOLUTIONS - Aqueous-based, ready to use topotecan-containing formulations for parenteral use having extended stability are disclosed. The formulations are surprisingly free of precipitated degradation products such as 10-hydroxycamptothecin (10-HCPT) after periods of up to 1 year or greater. | 2009-09-03 |
20090221624 | 4-AMINOQUINOLINE COMPOUNDS FOR TREATING VIRUS-RELATED CONDITIONS - This invention is directed to aminoquinoline compounds, pharmaceutical compositions of such compounds, kits comprising such compounds, and uses of such compounds for preparing medicaments and treating virus-related conditions in animals. | 2009-09-03 |
20090221625 | COSMECEUTICAL COMPOSITION - Topical compositions comprising: —a physiologically acceptable alkanediol, ether diol or diether alcohol containing up to (8) carbon atoms; —water; and—optionally an unsaturated fatty alcohol; and optionally further conventional excipients, for use as a cosmeceutical, in particular for use in the repair or maintenance of skin barrier function. They are indicated for use in e.g. moisturizing skin, nail and mucosa and, when an optional pharmaceutically active agent is present, additionally in the treatment of various skin, nail and mucosal diseases. Also disclosed are compositions suitable for topical application to infants and babies for treating dry skin, and soothing skin irritated from diaper rash and scrapes. | 2009-09-03 |
20090221626 | AEROSOL FORMULATION FOR INHALATION CONTAINING AN ANTICHOLINERGIC AGENT - The invention relates to specific aqueous aerosol formulations that are devoid of propellant, containing one or more anticholinergic agents of formula (1), in which X represents an anion, and containing at least one pharmacologically compatible organic acid and optionally additional pharmacologically compatible adjuvants and/or complexing agents. The cation of formula (1′) is contained in the preparation at a concentration of between 411 and 460.32 mg per 100 ml of medicament preparation. | 2009-09-03 |
20090221627 | Fluoro-containing derivatives of hydrogenated pyrido[4,3-b]indoles with neuroprotective and cognition enhancing properties, process for preparing, and use - Some exemplary embodiments comprise fluoro-containing derivatives of pyrido[4,3-b]indoles (and exemplary methods of making the same) that may be administered to a mammal (including a human) in an effective amount for potential use in the treatment or prophylaxis of neurological disorders including AD, mild cognitive impairment, senile and vascular dementia, HD, ALS, Parkinson's disease, AIDS-related dementia, ischaemic cerebral pathologies, neuropathic pain, ADHD (attention deficit disorder/hyperactivity syndrome), eating disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia (in particular the cognitive deficit of schizophrenia), stroke and also disorders associated with spinal trauma and/or head injury. These derivatives may also be useful for the treatment of borderline personality disorder, obesity, and for use as geroprotectors. The compounds may also be used as “pharmacological tools” for an investigation of the mechanism of protection against neurodegeneration disorders in vivo or in vitro. | 2009-09-03 |
20090221628 | Compositions and methods for treatment of prostate and breast cancer - Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents. | 2009-09-03 |
20090221629 | Method for antagonizing MIF activity - Methods of antagonizing MIF activity using ibudilast are described. Also described are methods of screening for MIF antagonists. These agents can be used for treating addictions, including drug and behavioral addictions, as well as for treating neuropathic pain. | 2009-09-03 |
20090221630 | IAP INHIBITORS - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X | 2009-09-03 |
20090221631 | IMIDAZOPYRIDINONES - The invention relates to imidazopyridinones, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. | 2009-09-03 |
20090221632 | Bicyclo-Pyrazoles and Pharmaceutical Compositions Comprising Them - Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases. | 2009-09-03 |
20090221633 | INHIBITORS OF AKT (PROTEIN KINASE B) - 4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds and methods of using these compounds. | 2009-09-03 |
20090221634 | Compositions and Methods for Disruption of BRCA2-Rad51 Interaction - Contemplated compounds disrupt interaction between BRCA2 and RAD51, likely by binding to RAD51. Based on the crucial role of the BRCA2-RAD51 complex formation in DNA repair and the role of RAD51 in the control of entry into S-phase from G1, numerous compositions and methods are presented. Among other advantageous uses, contemplated compounds may be employed as protective agents for non-neoplastic cells in chemotherapy before exposure of the cells to a chemotherapeutic drug, and/or as DNA-damage sensitizer for neoplastic cells. | 2009-09-03 |
20090221635 | QUINOLINYL AND BENZOTHIAZOLYL MODULATORS - Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ. In particular, the compounds of the invention modulate the function of PPARγ. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis. | 2009-09-03 |
20090221636 | ARGATROBAN FORMULATIONS AND METHODS FOR MAKING AND USING SAME - Formulations comprising argatroban and methods of making and using the formulations are provided. In an embodiment, the formulation comprises a solution having an argatroban concentration ranging from greater than about 10 to about 500 mg/mL. The solution can comprise an aqueous solution. The solution can be packaged in a sealed container that may either be aseptically-filled or subjected to sterilization to reduce the microbiological burden of the formulation. The solution can further be diluted and administered to persons needing same. | 2009-09-03 |
20090221637 | SOLID-STATE SALT ARGATROBAN FORMULATIONS AND METHODS FOR PRODUCING AND USING THE SAME - Argatroban formulations and methods of making and using the formulations are provided. In an embodiment, the present disclosure provides a solid-state salt formulation of argatroban. Upon reconstitution, the solid-state argatroban forms a solution that can be essentially free of particles and suitable for administration. The solid-state argatroban can be in a crystalline and/or amorphous form. The solid-state argatroban can be packaged in a sealed container that may be aseptically-filled to reduce the microbiological burden of the formulation. The solid-state argatroban can be reconstituted with a solution and administered to persons needing same. | 2009-09-03 |
20090221638 | CRYSTALLINE FORM OF A BIPHENYL COMPOUND - The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5 -yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder. | 2009-09-03 |
20090221639 | Heterocyclic GPCR Agonists - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of diabetes. | 2009-09-03 |
20090221640 | Novel Crystal Modifications - Novel crystal modifications of (5S)-5-[4-(5-chloro-pyridin-2-yloxy)-piperidine-1-sulfonylmethyl]-5-methyl-imidazolidine-2,4-dione are disclosed together with processes for preparing such modifications, pharmaceutical compositions comprising such a modification, and the use of such a modification in therapy. | 2009-09-03 |
20090221641 | Diaza-spiro--nonane derivatives as neurokinin (nk1) antagonists - This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonist ic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nocicept ion, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim | 2009-09-03 |
20090221642 | MUSCARINIC RECEPTOR AGONISTS, COMPOSITIONS, METHODS OF TREATMENT THEREOF, AND PROCESSES FOR PREPARATION THEREOF-176 - Compounds of Formula 1, or pharmaceutically acceptable salts thereof: | 2009-09-03 |
20090221643 | 4-PHENYL-3-(2-PROPYLSULFONYLAMINO) TETRAHYDROFURAN DERIVATIVES WHICH POTENTIATE GLUTAMATE RECEPTORS AND ARE USEFUL IN THE TREATMENT OF SCHIZOPHRENIA - Compounds of formula (I), salts and solvates thereof are provided: | 2009-09-03 |
20090221644 | Gpcr Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. | 2009-09-03 |
20090221645 | Dihydroimidazothiazole Derivatives - Compounds of formula (I) or pharmaceutically acceptable salts thereof, exhibit 5-HT | 2009-09-03 |