| 35th week of 2010 patent applcation highlights part 41 |
| Patent application number | Title | Published |
|---|
| 20100222302 | Novel Antibacterial Compounds - The invention relates to novel chimeric antibiotics of formula I | 2010-09-02 |
| 20100222303 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins as well as their prodrugs are disclosed. Such reverse-turn mimetic structures and prodrugs have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds and prodrugs for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 2010-09-02 |
| 20100222304 | Methods of Treating Neuropathic Pain by Modulation of Glycogenolysis or Glycolysis - Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain as well as methods for preparing medicaments used in the treatment of mammalian pain. Preferably, methods of the invention comprise the modulation of glycogeno lysis or glycolysis pathways for the treatment of mammalian pain. | 2010-09-02 |
| 20100222305 | COMPLEXES OF PHOSPHATE DERIVATIVES - There is provided a composition comprising the reaction product of: a) one or more phosphate derivatives of one or more hydroxylated actives; and b) one or more complexing agents selected from the group consisting of amphoteric surfactants, cationic surfactants, amino acids having nitrogen functional groups and proteins rich in these amino acids. | 2010-09-02 |
| 20100222306 | Class of Gamma Delta T Cells Activators and Use Thereof - The present invention relates to a new class of compounds having γδ T cells activating properties referred to herein as angelyl or tiglyl phosphoesters, compositions comprising any of these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds. | 2010-09-02 |
| 20100222307 | VITAMIN D AND VITAMIN D ANALOGS OR DERIVATIVES AS NEW ANTI-HYPERTENSIVE AGENTS - Methods and compositions to suppress renin expression and blood pressure in mammals are disclosed. Vitamin D and its analogues and derivatives, including Gemini compounds, are negative regulators of renin synthesis and blood pressure. Renin expression and plasma angiotensin II production were increased several fold in vitamin D receptor (VDR) null mice, leading to hypertension, cardiac hypertrophy and increased water intake. Vitamin D or its analogue-mediated regulation of renin expression and blood pressure is independent of calcium metabolism. Vitamin D analogues or derivatives are novel preventive or therapeutic anti-hypertension agents. Assays to identify novel vitamin D analogues or derivatives as anti-hypertensive agents are disclosed. | 2010-09-02 |
| 20100222308 | OPHTHALMIC, OTIC OR NASAL PHARMACEUTICAL COMPOSITION AND THE USE THEREOF - The invention provides an ophthalmic, otic or nasal pharmaceutical composition, comprising levofloxacin or the pharmaceutical acceptable salts thereof and loteprednol etabonate, wherein the weight ratio of loteprednol etabonate to levofloxacin is 1:0.2-5. The use of ophthalmic, otic or nasal pharmaceutical composition of the invention in preparation of the medication for treatment of conjunctivitis, keratitis, blepharitis, dacrycystitis, hordeolum, corneal ulcer and ocular infection accompanied with ophthalmitis and even inflammation of the surrounding tissues, to prevent increase of bacterial infection risks and the tissue inflammation of the infected area after the ophthalmic surgeries or ocular injuries, to treat or alleviate the bacterial infection in combination with the tissue inflammation of the infected area, or to treat tympanitis, otitis externa and infective rhinitis. | 2010-09-02 |
| 20100222309 | SKIN PROPERTY-IMPROVING THERAPEUTIC AGENT COMPRISING A MORPHINAN DERIVATIVE OR ANY OF ITS PHARMACOLOGICALLY PERMISSIBLE ACID ADDITION SALTS AS AN ACTIVE INGREDIENT - A skin property-improving therapeutic agent includes a compound having a specific morphinan skeleton typified by a compound 1 represented by the following formula (II) or any of its pharmacologically permissible acid addition salts as an active ingredient: | 2010-09-02 |
| 20100222310 | BENZODIAZEPINE COMPOSITIONS FOR TREATING EPIDERMAL HYPERPLASIA AND RELATED DISORDERS - The present invention provides, for example, pharmaceutical compositions comprising a benzodiazepine compound and an agent selected from the group consisting of a topical steroid, a keratolytic agent, a topical retinoid, a coal tar, and a vitamin D-3 analog. The pharmaceutical compositions are useful for treating medical disorders, such as epidermal hyperplasia | 2010-09-02 |
| 20100222311 | SOLID FORMULATIONS OF CRYSTALLINE COMPOUNDS - Described herein are formulations of active pharmaceutical ingredients, where the active pharmaceutical ingredients or drugs are included in a solid suspension with one or more solid additives. The formulations described herein are useful for formulating any drug or active pharmaceutical ingredient, including those that have limited solubility in organic and/or aqueous solvent systems. | 2010-09-02 |
| 20100222312 | DELAYED-RELEASE GLUCOCORTICOID TREATMENT OF ASTHMA - The present invention refers to the treatment of asthma by administering a delayed-release dosage form of a glucocorticoid to a subject in need thereof. | 2010-09-02 |
| 20100222313 | PHARMACEUTICAL COMPOSITIONS-4 - The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16α-bromo-3β-hydroxy-5α-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations. | 2010-09-02 |
| 20100222314 | Aqueous-based Pharmaceutical Composition - An aqueous pharmaceutical composition which is capable of being sprayed into the nasal cavity of an individual and which comprises: (A) a pharmaceutically effective amount of solid particles of medicament which is effective in treating a bodily condition by virtue of its being present on the mucosal surfaces of the nasal cavity; and (B) a suspending agent in an amount effective to maintain said particles dispersed uniformly in the composition and to impart to the composition the following thixotropic properties: (i) the viscosity of the position in unsheared form is relatively high, with the composition being in gel-like form; (ii) as the composition is subjected to shear (shaken) in preparation for spraying, the viscosity of the composition becomes relatively low and such that the composition in the form of a mist flows readily into the nasal passages for deposit on the mucosal surfaces of the nasal cavity; and (D) in deposited form on the mucosal surfaces, the viscosity of the composition is relatively high and such that it resists being cleared from the mucosal surfaces by the inherent mucocillary forces which are present in the nasal cavity, a method of use of the composition and a method for preparation of the composition, including in preferred form the use of anti-inflammatory steroid, for example, triamcinolone acetonide, and an odorless form of the composition. | 2010-09-02 |
| 20100222315 | Patient populations and treatment methods - The invention provides 17α-ethynylandrost-5-ene-3β, 7β, 17β-triol for use in methods to treat, e.g., hyperglycemia or diabetes patients having a body mass index of at least about 31 (≧30.5, ≧31 or ≧32), wherein the patients are not concurrently treated with metformin and optionally another antidiabetic agent. In these methods, the patient will generally have a fasting insulin level of at least 4 μU/mL or another characteristic as described herein. | 2010-09-02 |
| 20100222316 | INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action. | 2010-09-02 |
| 20100222317 | Azetidine Derivatives as GlyT1 Inhibitors - The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof, as GIyT1 inhibitors for treating neurological and psychiatric disorders. | 2010-09-02 |
| 20100222318 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 2010-09-02 |
| 20100222319 | NICOTINAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to compounds of formula (I): | 2010-09-02 |
| 20100222320 | TRIAZOLE DERIVATIVES FOR TREATING ALZHEIMER'S DISEASE AND RELATED CONDITIONS - Compounds of formula I: Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain, in particular Alzheimer's disease. | 2010-09-02 |
| 20100222321 | Inhibitors of akt activtiy - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 2010-09-02 |
| 20100222322 | Non-Nucleoside Reverse Transcriptase Inhibitors - Indole compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein R | 2010-09-02 |
| 20100222323 | IMIDAZOPYRAZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. 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 provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 2010-09-02 |
| 20100222324 | Substituted Indole Compounds - Substituted indole compounds corresponding to the formula I: | 2010-09-02 |
| 20100222325 | Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: | 2010-09-02 |
| 20100222326 | New Heterocyclic Derivatives Useful For The Treatment of CNS Disorders - The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 2010-09-02 |
| 20100222327 | Methods of Preparing Pharmaceutical Compositions Comprising Eslicarbazepine Acetate and Methods of Use - The present disclosure relates to the treatment of various diseases and conditions with eslicarbazepine acetate. The present disclosure also relates to the use of eslicarbazepine acetate in a method for reducing or decreasing epileptic seizures in a patient. The present disclosure also relates to a method for increasing the exposure to eslicarbazepine in a patient. The present disclosure also relates to a method of preparing a pharmaceutical composition comprising eslicarbazepine acetate. | 2010-09-02 |
| 20100222328 | 2-CYCLOPROPYL-THIAZOLE DERIVATIVES - The invention relates to selected 2-cyclopropyl-thiazole derivatives of the formula (I) wherein B, Y and R1 are as described in the description; to salts and especially pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists. | 2010-09-02 |
| 20100222329 | 2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF - A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia. | 2010-09-02 |
| 20100222330 | New Compounds - The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system. | 2010-09-02 |
| 20100222331 | NEW COMPOUNDS - The present invention encompasses compounds of general Formula (1) wherein R | 2010-09-02 |
| 20100222332 | PYRAZOLO-PYRAZINES DERIVATIVES USED AS G PROTEIN INHIBITORS - The invention relates to pyrazolo-pyrazines derivatives of the general formula (I) in which the radicals Z, R | 2010-09-02 |
| 20100222333 | EXCIPIENT PRESERVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISED THEREOF - Topically applicable pharmaceutical compositions contain at least one pharmaceutically active agent and an effective antimicrobial amount of a preservative excipient mixture and devoid of such amount of known preservative(s) as would otherwise itself impart an effective antimicrobial action thereto. | 2010-09-02 |
| 20100222334 | Pharmaceutical Formulation of Valsartan - The present invention relates to a pharmaceutical composition in a form of suspension for oral administration comprising valsartan or its pharmaceutically acceptable salts and at least one or two or more of the components selected from glycerol or syrup or the mixture thereof, a preservative, a buffer system and a suspending/stabilizing agent. The present invention further relates to the therapeutic uses of the pharmaceutical composition. | 2010-09-02 |
| 20100222335 | Process For The Preparation Of N,N'-Disubstituted Oxabispidines - There is provided a process for the preparation of a sulfonic acid salt of formula I, or a solvate thereof, which process comprises hydrogenating a sulfonic acid salt of formula II, or a solvate thereof; in the presence of a solvent system consisting essentially of water, a C | 2010-09-02 |
| 20100222336 | SINGLE ENANTIOMER BETA-AGONISTS, METHODS FOR THE PRODUCTION THEREOF AND THE USE THEREOF AS MEDICATION - The present invention relates to single enantiomer compounds of formula (1), where the moieties n, A, R | 2010-09-02 |
| 20100222337 | FUNGICIDAL COMPOSITION CONTAINING CARBOXYLIC ACID AMIDE DERIVATIVE - Conventional fungicidal compositions have had practical problems such that either a preventive effect or a curative effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired. The present invention provides a fungicidal composition containing a carboxylic acid amide derivative of the formula (I) or a salt thereof, as an active ingredient: wherein A is phenyl which may be substituted, benzodioxolanyl which may be substituted, or benzodioxanyl which may be substituted; B is 2- or 3-pyridyl which may be substituted; each of R | 2010-09-02 |
| 20100222338 | BETA-SECRETASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I | 2010-09-02 |
| 20100222339 | Thiazole pyrazolopyrimidines CRF1 receptor antagonists - The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome. | 2010-09-02 |
| 20100222340 | SUBSTITUTED PYRIDO [1,2-a] ISOQUINOLINE DERIVATIVES - The present invention relates to compounds of formula (I) | 2010-09-02 |
| 20100222341 | PIPERIDINE AND PIPERAZINE DERIVATIVES - Compounds of the formula (I), in which R | 2010-09-02 |
| 20100222342 | PYRROLOPYRAZOLE, POTENT KINASE INHIBITORS - Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4. | 2010-09-02 |
| 20100222343 | PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY - The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase. | 2010-09-02 |
| 20100222344 | 4-ANILINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS - A quinazoline derivative of the Formula (I): | 2010-09-02 |
| 20100222346 | 4-BENZYLAMINOQUINOLINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors. | 2010-09-02 |
| 20100222347 | PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA, COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT - Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1); | 2010-09-02 |
| 20100222348 | QUINOLINONE DERIVATIVES AS PARP INHIBITORS - Compounds of formula (I): | 2010-09-02 |
| 20100222349 | QUINOLINE DERIVATIVES USED TO TREAT INFLAMMATORY AND ALLERGIC DISEASES - The present invention relates to compounds of formula (I) | 2010-09-02 |
| 20100222350 | PHENYL, PYRIDINE, QUINOLINE, ISOQUINOLINE, NAPHTHYRIDINE AND PYRAZINE DERIVATIVES - This invention is concerned with compounds of the formula | 2010-09-02 |
| 20100222351 | METHODS OF CONTROLLING INSECTS - The invention relates to a method of controlling insects in the family Nitidulidae using the compound 4,5-di-hydro-6-methyl-4-(3-pyridylmethyleneamino)-1,2,4-triazin-3(2H)-one and also encompasses the use of compositions comprising 4,5-dihydro-6-methyl-4-(3-pyridylmethyleneamino)-1,2,4-triazin-3(2H)-one for controlling Nitidulidae, in particular pollen beetles as well as the preparation of said compound and/or compositions for use in controlling Nitidulidae. In particular, the invention relates to the use of 4,5-dihydro-6-methyl-4-(3-pyridylmethyleneamino)-1,2,4-triazin-3(2H)-one and/or compositions comprising this compound in controlling such insects in crops of useful plants, in particular flowering crops and/or flowering ornamental plants. | 2010-09-02 |
| 20100222352 | Compounds and Methods for the Treatment of Viruses and Cancer - The present invention relates to compounds according to the formula I: Where R | 2010-09-02 |
| 20100222353 | AMINOPHTHALAZINE DERIVATIVE COMPOUNDS - The invention pertains to new aminophthalazine compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE-10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom. | 2010-09-02 |
| 20100222354 | AMPA Receptor Antagonists and Aldose Reductase Inhibitors for Neuropathic Pain - The invention provides methods for treating and/or preventing neuropathic pain by administering to patients therapeutically effective amounts of AMPA receptor antagonists and aldose reductase inhibitors. The neuropathic pain may be diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and aldose reductase inhibitors. The AMPA receptor antagonists may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The aldose reductase inhibitor may be, for example, ranirestat. | 2010-09-02 |
| 20100222355 | QUINOLIZIDINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to spiropiperidine compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 2010-09-02 |
| 20100222356 | Furazano '3, 4-B! Pyrazines and Their Use as Anti-Tumor Agents - The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas. | 2010-09-02 |
| 20100222357 | INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES - The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: | 2010-09-02 |
| 20100222358 | OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES - Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein. | 2010-09-02 |
| 20100222359 | COMPOSITIONS, SYNTHESIS, AND METHODS OF UTILIZING QUINAZOLINEDIONE DERIVATIVES - The present invention provides quinazolinedione derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, depression and dementia. | 2010-09-02 |
| 20100222360 | Treatment of Malignant Peripheral Nerve Sheath Tumors - The present invention pertains to a combination comprising (a) at least one c-Jun N-terminal kinase (JNK) inhibitor and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide or a pyrimidylaminobenzamide of formula I | 2010-09-02 |
| 20100222361 | 2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF - A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia. | 2010-09-02 |
| 20100222362 | N-OXIDES OF N-PHENYL-2-PYRAMIDINE-AMINE DERIVATIVES - The invention relates to N-phenyl-2-pyrimidine-amine derivatives derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans. | 2010-09-02 |
| 20100222363 | Bicyclic Derivatives as P38 Inhibitors - New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors. | 2010-09-02 |
| 20100222364 | PHARMACEUTICAL COMPOSITION FOR TREATING HAIR LOSS AND BENIGN PROSTATIC HYPERPLASIA - Disclosed is the use of 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid or its pharmaceutically acceptable salt for the prevention of hair loss; for hair regrowth, hair toning and hair growth; and for the treatment of female hirsutism and benign prostatic hyperplasia. | 2010-09-02 |
| 20100222365 | SUBSTITUTED TRIAZOLE DERIVIATIVES AS OXYTOCIN ANTAGONISTS - The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.). | 2010-09-02 |
| 20100222366 | PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed. | 2010-09-02 |
| 20100222367 | PYRAZINE KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions. | 2010-09-02 |
| 20100222368 | N-(Heteroaryl)-1-heteroarylalkyl-1H-indole-2-carboxamide derivatives, preparation and therapeutic use thereof - The invention concerns compounds of general formula (I), wherein n, X | 2010-09-02 |
| 20100222369 | TREATMENT FOR DRY EYE CONDITIONS - The present invention provides a method for treating dry eye condition in an individual comprising administrating to said individual an amount of A | 2010-09-02 |
| 20100222370 | Methods of Treating Cancer - The invention relates to the treatment of cancer using an inhibitor of 5′-methylthioadenosine phosphorylase (MTAP). The invention particularly relates to the treatment of prostate cancer and head and neck cancer. | 2010-09-02 |
| 20100222371 | PREVENTION OF SURGICAL ADHESIONS - The present invention relates to methods for treatment (particularly the prevention or suppression) of formation or reformation of adhesions, particularly in the peritoneal or pelvic cavities resulting from wound, surgery, infection, inflammation or trauma. The invention provides methods useful for inhibiting, suppressing or ameliorating adhesion formation in mammals, including humans wherein an individual is administered a compound selected from the group consisting of sunitinib malate, axitinib, semaxanib, sorafenib, ZD1839, and erlotinib. The invention applies to human and veterinary applications. The inventive method has been shown to be especially effective in preventing adhesion formation in the peritoneum following surgery. | 2010-09-02 |
| 20100222372 | THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE COMPRISING URACIL DERIVATIVE AS ACTIVE INGREDIENT - To provide a therapeutic agent for inflammatory bowel disease. | 2010-09-02 |
| 20100222373 | Crystalline Form of Bis [(E)-7-[4-(4-fluoro-phenyl)-6-isopropyl-2-[methyl(methyl-sulfonyl)amino] pyrimidin-5-yl] (3R,5S)-3,5-dihydroxyhept-6-enoic acid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described. | 2010-09-02 |
| 20100222374 | SPIROCYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF THEIR USE - Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions. | 2010-09-02 |
| 20100222375 | Pharmaceutical Composition Comprising Trospium Chloride for Once-A-Day Administration - A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C | 2010-09-02 |
| 20100222376 | CHELERYTHRINE, ANALOGS THEREOF AND THEIR USE IN THE TREATMENT OF BIPOLAR DISORDER AND OTHER COGNITIVE DISORDERS - The present invention relates to the use of chelerythrine and chelerythrine analogs in pharmaceutical compositions for the treatment of prefrontal cortical cognitive disorders, including bipolar disorder, among others. | 2010-09-02 |
| 20100222377 | BIS-QUATERNARY AMMONIUM CYCLOPHANE COMPOUNDS THAT INTERACT WITH NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS - Provided are bis-quaternary ammonium cyclophane 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. | 2010-09-02 |
| 20100222378 | 2-HETEROARYLCARBOXYLIC ACID AMIDES - The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. | 2010-09-02 |
| 20100222379 | NOVEL HISTONE DEACETYLASE INHIBITORS - Provided herein are novel, stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds can inhibit HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as WO 2009/047615 A2 malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, etc. | 2010-09-02 |
| 20100222380 | Modified Chalcone Compounds as Antimitotic Agents - Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN-COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients. | 2010-09-02 |
| 20100222381 | Cyclopentathiophene/cyclohexathiophene DNA methyltransferase inhibitors - Compounds represented by Formula (I): | 2010-09-02 |
| 20100222382 | Esters of Compounds in the Leptomycin Family - Esters of compounds in the leptomycin family, having a structure according to formula I | 2010-09-02 |
| 20100222383 | Iminosugars and methods of treating viral diseases - Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars. | 2010-09-02 |
| 20100222384 | Iminosugars and methods of treating arenaviral infections - Provided are methods of treating a disease or condition caused by or associated with a virus belonging to the Arenaviridae family using iminosugars, such as DNJ derivatives. | 2010-09-02 |
| 20100222385 | SELECTIVE ABLATION OF PAIN-SENSING NEURONS BY ADMINISTRATION OF A VANILLOID RECEPTOR AGONIST - The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons. | 2010-09-02 |
| 20100222386 | SUBSTITUTED PIPERIDINES - A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. | 2010-09-02 |
| 20100222387 | 3-Fluoro-Piperidine T-Type Calcium Channel Antagonists - The present invention is directed to 3-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved. | 2010-09-02 |
| 20100222388 | Enhanced Migraine Treatments Based on Ghrelin Mimetics - The present invention relates to method of enhancing the absorption of migraine medications and thereby treating migraines by co-administering to a subject in need thereof an effective amount of a ghrelin mimetic or pharmaceutically acceptable salt, hydrate or solvate thereof and at least one migraine medication selected from a serotonin 5-HT | 2010-09-02 |
| 20100222389 | NOVEL MICROBIOCIDES - Compounds of the formula (I), in which the substituents are as defined in claim | 2010-09-02 |
| 20100222390 | Methods and Compositions for the Intravenous Administration of Compounds Related to Proton Pump Inhibitors - Disclosed herein are liquid compositions comprising a therapeutically effective concentration of a prodrug of a sulfonyl-containing proton pump inhibitor, wherein said compositions have a pH of from 3 to 7.3. Solid compositions related thereto are also disclosed. Methods of delivering a proton pump related thereto are also disclosed. Compositions comprising a second therapeutically active agent are also disclosed herein. | 2010-09-02 |
| 20100222391 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent. | 2010-09-02 |
| 20100222392 | INSECTICIDAL COMPOUNDS - A compound of formula (I) wherein A | 2010-09-02 |
| 20100222393 | MUSCARINIC RECEPTOR ANTAGONISTS - Compounds of Formula (I), wherein represents a single bond when G is —OH and double bond when G is —O; R | 2010-09-02 |
| 20100222394 | METHOD FOR PRODUCING PYRAZOL-3-YL-BENZAMIDE DERIVATIVE - The present invention provides a more efficient industrial method for producing a pyrazol-3-yl-benzamide derivative expressed by a formula useful as medicine: | 2010-09-02 |
| 20100222395 | COMPOUNDS CAPABLE OF ACTIVATING CHOLINERGIC RECEPTORS - Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine. | 2010-09-02 |
| 20100222396 | 4-ARYL-BUTANE-1,3-DIAMIDES - The invention relates to compound of the formula I | 2010-09-02 |
| 20100222397 | Use of Succinate Dehydrogenase Inhibitors For Controlling Powdery Mildew Primary Infections - The present invention relates to the use of succinate dehydrogenase Inhibitors for controlling powdery mildew primary infections in crops and to a method for controlling those primary infections. | 2010-09-02 |
| 20100222398 | NOVEL 1,2,3-TRIAZOLE DERIVATIVES USEFUL AS MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. 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. | 2010-09-02 |
| 20100222399 | Thiazolidinedione Analogues For The Treatment Of Hypertension - The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases. Formula (I), wherein: each of R | 2010-09-02 |
| 20100222400 | F1F0-ATPase Inhibitors and Related Methods - The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders. | 2010-09-02 |
| 20100222401 | COMPOSITIONS AND METHODS FOR TREATING PATHOLOGIC ANGIOGENESIS AND VASCULAR PERMEABILITY - Compounds, compositions and methods for inhibiting vascular permeability and pathologic angiogenesis by modulating a signaling pathway delineated herein are described. Moreover, methods for producing and screening compounds and compositions capable of modulating the signaling pathway described herein, inhibiting vascular permeability, and inhibiting pathologic angiogenesis are also provided. | 2010-09-02 |
| 20100222402 | METHOD OF MANUFACTURING 4'-[[4-METHYL-6-(1-METHYL-1H-BENZIMIDAZOL-2-YL)-2-PROPYL-1H-BENZIMIDAZOL-- 1YL]METHYL]BIPHENYL-2-CARBOXYLIC ACID (TELMISARTAN) - A carboxylic acid of the general formula R | 2010-09-02 |
