25th week of 2010 patent applcation highlights part 63 |
Patent application number | Title | Published |
20100160296 | USE OF IMIPRAMINE BLUE AND ANALOGS THEREOF IN TREATING CANCERS - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, and parasitic infections. The compounds are triphenyl methane analogs of imipramine blue and analogs thereof, as defined herein. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases. | 2010-06-24 |
20100160297 | COMPOUNDS FOR PIM KINASE INHIBITION AND FOR TREATING MALIGNANCY - The present invention relates to the compounds of formula I as well as to their use as PIM kinase inhibitors and, thereby, their use for treating oncological diseases, particularly of the hematopoietic system, the liver and the prostate gland. | 2010-06-24 |
20100160298 | METHOD OF TREATING OCULAR ALLERGY - The topical use of 5,6,7-trihydroxyheptanoic acid and analogs alone or in combination with histamine antagonists and/or mast cell stabilizers is disclosed for the treatment of ocular allergy. | 2010-06-24 |
20100160299 | DENDRIMER CONJUGATES - The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. | 2010-06-24 |
20100160300 | Method of Treating Depression - Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K | 2010-06-24 |
20100160301 | MICROANGIOPATHY TREATMENT AND PREVENTION - The present invention relates to the use of selective factor Xa inhibitors, in particular of oxazolidinones of the formula (I) | 2010-06-24 |
20100160302 | NOVEL DIPEPTIDYL PEPTIDASE IV INHIBITORS AND PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined. The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia. | 2010-06-24 |
20100160303 | CARBAZOLE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, | 2010-06-24 |
20100160304 | AROMATIC SULFONE COMPOUND AS ALDOSTERONE RECEPTOR MODULATOR - The present invention provides a compound represented by the following formula (I): | 2010-06-24 |
20100160305 | 3, 4, 5 - Substituted Piperidine Compounds - 3,4,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. | 2010-06-24 |
20100160306 | Acylated Piperidine Derivatives as Melanocortin-4 Receptor Agonists - Certain novel 4 alkyl substituted N acylated piperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. | 2010-06-24 |
20100160307 | METHOD FOR CONTROLLING PARTICULAR INSECT PESTS BY APPLYING ANTHRANILAMIDE COMPOUNDS - This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof | 2010-06-24 |
20100160308 | Thiazolyl-Benzimidazoles - The invention is directed to compounds of formula (1) | 2010-06-24 |
20100160309 | INHIBITORS OF JANUS KINASES AND/OR 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1 - The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer. | 2010-06-24 |
20100160310 | 2,4 (4,6) PYRIMIDINE DERIVATIVES - The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z | 2010-06-24 |
20100160311 | Fungicidal Azolopyrimidines, Process for Their Preparation and Their Use For Controlling Harmful Fungi, and Also Compositions Comprising Them - The present invention relates to azolopyrimidines of the formula I | 2010-06-24 |
20100160312 | Substituted Pyridone Compounds and Methods of Use - The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I | 2010-06-24 |
20100160313 | DISCOVERY OF NOVEL ANTICANCER COMPOUNDS BASED ON CONFORMATIONAL SAMPLING OF QUINOXALINHYDRAZIDE PHARMACOPHORE - The present invention relates in general to anti-cancer drug design. More specifically, the invention provides methods of mapping and screening for anti-cancer agents using pharmacophore models. The invention demonstrates that, conformational sampling of a small lead molecule, followed by representative pharmacophore model development, is an efficient approach for rational design of novel anticancer agents with similar or better potency than the original lead but with different physicochemical properties. | 2010-06-24 |
20100160314 | Small Molecule Inhibitors of Toll-Like Receptor 9 - Small molecule compounds and compositions containing said compounds useful for inhibiting signaling by certain Toll-like receptors (TLRs), particularly TLR9, are provided. The compounds and compositions can be used to inhibit immune responses, including unwanted immune responses in particular. Compounds, compositions, and methods are provided to treat a variety of conditions involving unwanted immune responses, including for example autoimmune disease, inflammation, transplant rejection, and sepsis. | 2010-06-24 |
20100160315 | NOVEL 2, 3-DIAMINO-QUINAZOLINONE DERIVATIVES AND THEIR MEDICAL USE - This invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the 2,3-diamino-quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2,3-diamino-quinazolinone derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of K | 2010-06-24 |
20100160316 | QUINAZOLINES USEFUL AS MODULATORS OF ION CHANNELS - The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2010-06-24 |
20100160317 | 2-(2-OXOINDOLINE-3-YLIDENE)METHYL-5-(2-HYDROXY-3-MORPHOLIN-4-YL-PROPYL)-6,- 7-DIHYDRO-1H-PYRROL[3,2-C]PYRIDINE-4(5H)-ONE COMPOUNDS AND USE AS PROTEIN KINASE INHIBITORS - Pyrrolo[3,2-c]pyridine-4-one-2-indolinone compounds, especially 2-(2-oxoindoline-3-ylidene)methyl-5-(2-hydroxy-3-morpholin-4-yl-propyl)-6,7-dihydro-1H-pyrrol[3,2-c]pyridine-4(5H)-one compounds. Their preparation and pharmaceutical composition, and pharmaceutical use as protein kinase inhibitors. | 2010-06-24 |
20100160318 | 3-Pyrrolo[b]Cyclohexylene-2-Dihydroindolinone Derivatives and Uses Thereof - 3-pyrrolo[b]cyclohexylene-2-dihydro-indolinone derivatives of formula (I) or their pharmaceutically acceptable salts and uses thereof. The intermediates of formula (II) for preparing the above compounds. The bioassay shows that the above compounds and their pharmaceutically acceptable salts can modulate the activity of protein kinases (PKs), inhibit the activity of tyrosine kinases (PTKs) and inhibit many kinds of tumor cells as well as. | 2010-06-24 |
20100160319 | HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES - The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I) | 2010-06-24 |
20100160320 | C5aR ANTAGONISTS - Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors. | 2010-06-24 |
20100160321 | IMIDAZOLINONE AND HYDANTOINE DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of Formula (I) wherein R | 2010-06-24 |
20100160322 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 2010-06-24 |
20100160323 | 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. | 2010-06-24 |
20100160324 | PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES - The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R | 2010-06-24 |
20100160325 | 4-(3-AMINOPYRAZOLE) PYRIMIDINE DERIVATIVES FOR USE AS TYROSINE KINASE INHIBITORS IN THE TREATMENT OF CANCER - This invention relates to novel compounds having the formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer. | 2010-06-24 |
20100160326 | PEST CONTROL AGENT CONTAINING NOVEL PYRIDYL-METHANAMINE DERIVATIVE OR SALT THEREOF - A novel pesticide is provided. The present invention provides a pesticide containing, as an active ingredient, a pyridyl-methanamine derivative represented by the formula (I) or its salt: | 2010-06-24 |
20100160327 | Modified Malonate Derivatives - The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the modified malonate derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the modified malonate derivatives in vivo. | 2010-06-24 |
20100160328 | NEW COMPOUNDS USEFUL FOR DPP-IV ENZYME INHIBITION - The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX). | 2010-06-24 |
20100160329 | USE OF CONDENSED PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES - The invention relates to the use of a compound of the formula (I), or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for use in modulating an immune or inflammatory response: wherein: Z=O or S; n=1-3; R | 2010-06-24 |
20100160330 | NOVEL BICYCLIC HETEROCYCLES USEFUL AS SELECTIVE ANDROGEN RECEPTOR MODULATORS - The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. | 2010-06-24 |
20100160331 | NOVEL CARBAMOYLOXY ARYLALKAN ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE COMPOUND AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING THE COMPOUND - There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof. | 2010-06-24 |
20100160332 | a2-Adrenoceptor Ligands - The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into α and β subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel compounds which are ligands of the alpha2-adrenoceptor (α | 2010-06-24 |
20100160333 | NOVEL 3,9-DIAZABICYCLO[3.3.1]NONANE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - 3,9-diazabicyclo[3.3.1]nonane derivatives, useful as monoamine neurotransmitter re-uptake inhibitors. Also, use of these compounds in a method for therapy and in pharmaceutical compositions comprising the compounds. The 3,9-diazabicyclo[3.3.1]nonane derivatives have the formula | 2010-06-24 |
20100160334 | TRICYCLIC ANILIDE SPIROLACTAM CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I: I (where A | 2010-06-24 |
20100160335 | PYRIDAZINONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT - It is to provide a novel pyridazinone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: | 2010-06-24 |
20100160336 | Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors - The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: | 2010-06-24 |
20100160337 | SULFAMIDES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 2010-06-24 |
20100160338 | BENZENESULFONAMIDE MODULATORS OF ALPHA-1A ADRENERGIC RECEPTORS - The present invention relates to new benzenesulfonamide modulators of alpha-1A adrenergic receptors, pharmaceutical compositions thereof, and methods of use thereof. | 2010-06-24 |
20100160339 | TREATING PANCREATITIS - This document provides methods and materials related to treating pancreatitis. For example, methods and materials relating to the use of a tyrosine kinase inhibitor to pancreatitis are provided. | 2010-06-24 |
20100160340 | PROTEIN KINASE INHIBITORS - The present invention provides a compound of formula (I): | 2010-06-24 |
20100160341 | HETEROARYL, HETEROCYCLIC AND ARYL 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. | 2010-06-24 |
20100160342 | Compositions of Topical Ocular Solutions to Deliver Effective Concentrations of Active Agent to the Posterior Segment of the Eye - The present invention relates to development of efficacious pharmaceutical compositions comprising an active agent, such as the free base or hydrochloride salt of tandospirone, for topical delivery to the eye for the treatment of retinal disorders. | 2010-06-24 |
20100160343 | HETEROARYL, HETEROCYCLIC AND ARYL 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. | 2010-06-24 |
20100160344 | NOVEL COMPOUNDS - This invention relates to imidazopyrimidine substituted piperidine derivatives and their use as pharmaceuticals. | 2010-06-24 |
20100160345 | NOVEL COMPOUNDS - This invention relates to imidazopyrazine substituted piperidine derivatives and their use as pharmaceuticals. | 2010-06-24 |
20100160346 | NEUROLOGICALLY ACTIVE COMPOUNDS - The present invention relates to neurologically-active compounds, processes for their preparation and their use as pharmaceutical or veterinary agents, in particular for the treatment of neurological conditions, more specifically neurodegenerative conditions such as Alzheimer's disease. | 2010-06-24 |
20100160347 | PYRIDO[1,2-a]PYRIMIDIN-4-ONE INHIBITORS OF MAST CELL DEGRANULATION - The present invention relates to new pyrido[1,2-a]pyrimidin-4-one inhibitors of mast cell degranulation, pharmaceutical compositions thereof, and methods of use thereof. | 2010-06-24 |
20100160348 | MATERIALS AND METHODS FOR DETECTING AND TREATING PERITONEAL OVARIAN TUMOR DISSEMINATION INVOLVING TISSUE TRANSGLUTAMINASE - Tissue transglutaminase-2 (TG2) is involved in Ca | 2010-06-24 |
20100160349 | TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS - This invention concerns a compound of formula | 2010-06-24 |
20100160350 | PYRAZOLOPYRIMIDINONE KINASE INHIBITOR - The present invention provides a novel pyrazolo[3,4-d]pyrimidin-4-one, specifically a derivative of 1-(pyridine-4-yl)-pyrazolo[3,4-d]pyrimidin-4-one. This compound is a kinase inhibitor that shows unexpected anti-proliferative activity against cells, including against tumor cells, and anti-tumor activity in xenograft tumor models. The compound or a suitable salt or prodrug thereof is useful for the treatment of individuals suffering from a cancer or another proliferative disorder or disease. | 2010-06-24 |
20100160351 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING HYPERURICEMIA AND RELATED DISORDERS - Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II: | 2010-06-24 |
20100160352 | ADENINE DERIVATIVES - Novel adenine derivatives of the formula (I), in which R | 2010-06-24 |
20100160353 | PHARMACEUTICAL COMPOSITION AND BEVERAGE COMPOSITION COMPRISING L-ARGININE - A pharmaceutical composition and a beverage composition comprising the following three components (A), (B) and (C): (A) L-arginine or a salt thereof; (B) caffeine or a salt thereof; and (C) at least one substance selected from the group consisting of vitamin C or a derivative thereof, vitamin E or a derivative thereof and folic acid or a derivative thereof. The compositions show an effect of L-arginine even at a low L-arginine content, and therefore can be suitably used for the prevention, amelioration and/or treatment of at least one disease selected from the group consisting of arteriosclerosis, angiectasia, hyperlipemia, climacteric disorder, diabetes, angina pectoris, hypertension, erectile dysfunction, thrombosis, immunodeficiency, dementia, gestosis, respiratory failure and hemorrhoid, in the form of a pharmaceutical preparation or a beverage. | 2010-06-24 |
20100160354 | NOVEL COMPOUNDS - The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): | 2010-06-24 |
20100160355 | Anti-Viral Compounds - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection. | 2010-06-24 |
20100160356 | NOVEL CYCLOBUTYL COMPOUNDS AS KINASE INHIBITORS - The invention relates to compounds of the formula I, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the formation or course of which protein kinases are involved. | 2010-06-24 |
20100160357 | Heterobicyclic sphingosine 1-phosphate analogs - Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors. | 2010-06-24 |
20100160358 | Pyridylsulfonamidyl-Pyrimidines for the Prevention of Blood Vessel Graft Failure - The present invention relates to the use of a compound of formula (I), wherein R | 2010-06-24 |
20100160359 | Modulators of Metabolism and the Treatment of Disorders Related Thereto - The present invention relates to 4-[5-methyl-6-(2-methyl-pyridin-3-yloxy)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity. | 2010-06-24 |
20100160360 | JNK MODULATORS - Compounds of formula I modulate JNK: | 2010-06-24 |
20100160361 | TREATMENT OF MAJOR ADVERSE CARDIAC EVENTS AND ACUTE CORONARY SYNDROME USING SECRETORY PHOSPHOLIPASE A2 (SPLA2) INHIBITOR OR SPLA2 INHIBITOR COMBINATION THERAPIES - Administration of sPLA | 2010-06-24 |
20100160362 | SPIRO (FURO [3, 2-C] PYRIDINE-3-3' -INDOL) -2' (1'H)-ONE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF SODIUM-CHANNEL MEDIATED DISEASES, SUCH AS PAIN - This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X, R | 2010-06-24 |
20100160363 | EXTENDED-RELEASE PHARMACEUTICAL FORMULATIONS - The present invention provides matrix-forming, sustained-release pharmaceutical formulations comprising four primary components: i) an effective amount of at least one drug substance; ii) at least one pharmaceutically acceptable, water-swellable, pH independent polymer; iii) at least one pharmaceutically-acceptable, anionic, pH dependent polymer; and (iv) a pharmaceutically-acceptable polymer selected from the group consisting of a) at least one pharmaceutically-acceptable cationic polymer; and b) at least one pharmaceutically acceptable hydrocolloid. The present formulations can be used with compounds having a wide range of solubilities as well as compounds characterized as having hydrophobic or hydrophilic characteristics. | 2010-06-24 |
20100160364 | REMEDY OR PREVENTIVE FOR INTEGRATION DYSFUNCTION SYNDROME - A composition includes a therapeutic or prophylactic agent for schizophrenia, which therapeutic or prophylactic agent can treat especially positive symptoms of schizophrenia and does not cause impaired information processing related to cognitive deficiencies or the like which is a symptom of schizophrenia. The therapeutic or prophylactic agent for schizophrenia includes as an effective ingredient a compound having a specific morphinan skeleton or a pharmaceutically acceptable acid addition salt thereof. | 2010-06-24 |
20100160365 | TREATMENT OF NON-HODGKIN'S LYMPHOMAS WITH MULTI-ARM POLYMERIC CONJUGATES OF 7-ETHYL-10-HYDROXYCAMPTOTHECIN - The present invention relates to methods of treatment of non-Hodgkin's lymphomas. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to patients in need thereof. | 2010-06-24 |
20100160366 | TREATMENT METHOD - Methods of treating and/or preventing a cardiovascular disease in a human suffering from an allergic and/or inflammatory condition or cardiovascular disease by administrating an effective amount of loratadine, in combination with an effective amount of montelukast, for such treating and/or preventing are disclosed. | 2010-06-24 |
20100160367 | PHARMACEUTICAL COMPOSITIONS CONTAINING PYRROLOQUINOLINE QUINONE AND NEPHROPROTECTANT FOR TREATING ISCHEMIA REPERFUSION INJURIES - The invention includes compositions comprising substantially purified pyrroloquinoline quinone, that are useful in methods for the treatment and prevention of cardiac injury caused by hypoxia or ischemia. The invention also includes methods for the treatment and prevention of cardiac injury comprising contacting a composition of the invention with a human patient. | 2010-06-24 |
20100160368 | Methods of Treating Dermatological Disorders and Inducing Interferon Biosynthesis With Shorter Durations of Imiquimod Therapy - Pharmaceutical Formulations and Methods for the Topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namely, viral infections, such as Type I or Type II Herpes simplex infections and genital and perianal warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis to achieve an antiviral effect, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”). | 2010-06-24 |
20100160369 | S1P1 Agonists and Methods of Making And Using - The invention is directed to Compounds of Formula I: | 2010-06-24 |
20100160370 | METHOD OF TREATMENT AND PHARMACEUTICAL COMPOSITIONS - The present invention relates to methods, uses, and compositions comprising the caspase inhibitor (R)-N-((2S,3S)-2-(fluoromethyl)-2-hydroxy-5-oxo-tetrahydrofuran-3-yl)-5-isopropyl-3-(isoquinolin-1-yl)-4,5-dihydroisoxazole-5-carboxamide, or a pharmaceutically acceptable salt thereof. | 2010-06-24 |
20100160371 | INHIBITION OF P38 KINASE ACTIVITY BY ARYL UREAS - This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy. | 2010-06-24 |
20100160372 | TREATMENT OF PROTEINOPATHIES USING A FARNESYL TRANSFERASE INHIBITOR - Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA antagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant. | 2010-06-24 |
20100160373 | DIHYDROPYRIDONE AMIDES AS P2X7 MODULATORS - Compounds of the formula I: | 2010-06-24 |
20100160374 | N-(2-Hydroxyethyl)-N-Methyl-4-(Quinolin-8-yl(1-(Thiazol-4-ylmethyl)Piperid- in-4-ylidene)Methyl)Benzamide - N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, pharmaceutically acceptable salts thereof, and/or mixtures thereof, as well as, pharmaceutical compositions thereof, methods of treatment therewith, and processes of making N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide and intermediates thereof. | 2010-06-24 |
20100160375 | METHODS AND COMPOSITIONS FOR TREATING INFECTIONS COMPRISING A LOCAL ANESTHETIC - The present invention is directed to a drug depot useful for reducing, preventing or treating an infection in a patient in need of such treatment. The drug depot includes a polymer and a therapeutically effective amount of a local anesthetic or pharmaceutically acceptable salt thereof. The drug depot is administered at a site to reduce, prevent or treat an infection. The drug depot is capable of releasing (i) a bolus dose of the local anesthetic or pharmaceutically acceptable salt thereof at the site and (ii) a sustained release dose of an effective amount of the local anesthetic or pharmaceutically acceptable salt thereof over a period of at least 4 days at the site. | 2010-06-24 |
20100160376 | NICOTINE-ALTERNATIVE COMPOSITIONS AND METHODS OF PRODUCING SUCH COMPOSITIONS - A method for producing a consumable nicotine-alternative composition includes measuring a quantity of a cigarette nicotine-alternative alkaloid and/or a larger quantity of lobeline. The quantities of cigarette nicotine-alternative alkaloid and/or lobeline are diluted into one or more successive intermediate solutions, a last of which constitutes a final solution. The final solution is apportioned so that each portion contains a precise quantity of cigarette nicotine-alternative alkaloid and/or lobeline appropriate for consumption in a single use by a single person. Each portion is introduced into a separate single-serving dispenser. | 2010-06-24 |
20100160377 | DERIVATIVES OF PYRAZOLE 3,5-CARBOXYLATES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS - The invention relates to derivatives of pyrazole 3,5-carboxylates, of general formula (I): | 2010-06-24 |
20100160378 | COMPOSITIONS FOR DRUG ADMINISTRATION - The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject, as well as compositions and methods for providing migraine pain relief. The compositions include at least one alkyl glycoside and at least one therapeutic agent, such as a 5-HT receptor agonist, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms. | 2010-06-24 |
20100160379 | HETEROCYCLES SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING THEREOF - An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: | 2010-06-24 |
20100160380 | Therapeutic Salt Compositions and Methods - Therapeutic salt compositions and methods are disclosed herein. | 2010-06-24 |
20100160381 | RAF Inhibitors for the Treatment of Thyroid Cancer - The invention relates to the use of an Raf inhibitor for the manufacture of pharmaceutical compositions for the treatment of thyroid cancer, more specifically papillary thyroid cancer (PTC); the use of a Raf inhibitor in the treatment of thyroid cancer, more specifically PTC; a method of treating warm-blooded animals including mammals, especially humans, suffering from thyroid cancer, more specifically PTC, by administering to a said animal in need of such treatment a dose effective against said disease of an Raf inhibitor. The invention also relates to the use of a Raf inhibitor in combination with a platin compound for the treatment of thyroid cancer, more specifically papillary thyroid cancer. | 2010-06-24 |
20100160382 | ANTI-ACID PHARMACEUTICAL COMPOSITION IN POWDER FORM AND PROCESS FOR MAKING IT - An anti-acid pharmaceutical composition for the rapid and prolonged neutralization of gastric acidity with mucosa-protecting activity in powder form to prepare, by dispersion in water, a pharmaceutical solution or suspension for oral use characterized in that the composition includes sodium alginate; an anti-acid soluble agent or a combination of anti-acids; an inhibitor of proton pump; diluent and sweetening agents, wherein a) at least 30% of sodium alginate present in the formulation along with the total of the inhibitor of proton pump are homogeneously distributed over the surface of the total soluble anti-acid agent [or] of the combination of anti-acids of the composition; and b) the rest, about 70%, of sodium alginate present in the formulation contains a percentage of humidity of less than 2%. | 2010-06-24 |
20100160383 | PYRAZOLE CARBOXAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND ITS PREPARATION - A compound of formula (I) or pharmaceutically acceptable salts and/or solvates or hydrates thereof. A process for preparing the compound, a pharmaceutical composition comprising the compound and an application for resisting cannabinoid CB1 receptor are provided. | 2010-06-24 |
20100160384 | DIHYDROPYRIDONE AMIDES AS P2X7 MODULATORS - Compounds of the formula I: | 2010-06-24 |
20100160385 | FUNGICIDAL TRIPHENYL-SUBSTITUTED PYRIDONES - Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, | 2010-06-24 |
20100160386 | 4-PHENOXY-NICOTINE ACID DERIVATIVES AND USE THEREOF AS PPAR-MODULATORS - The present invention relates to novel 4-phenoxy-6-phenyl- and 4-phenoxy-6-pyridylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis and heart failure. | 2010-06-24 |
20100160387 | DIHYDROPYRIDONE AMIDES AS P2X7 MODULATORS - Compounds of the formula I: | 2010-06-24 |
20100160388 | DIHYDROPYRIDONE UREAS AS P2X7 MODULATORS - Compounds of the formula I: | 2010-06-24 |
20100160389 | DIHYDROPYRIDONE AMIDESAS P2X7 MODULATORS - Compounds of the formula I: | 2010-06-24 |
20100160390 | 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. | 2010-06-24 |
20100160391 | Substituted Aminopyridines as Fluorescent Reporters for Amide Hydrolases - The present invention provides conjugates comprising a substituted aminopyridine covalently attached to an organic molecule via an amide bond. Such conjugates find utility as substrates for amide hydrolases, where the substituted aminopyridine acts as a fluorescent reporter of amide hydrolase activity. As a result, the conjugates described herein can advantageously be used in assays to detect amide hydrolase activity based upon measuring the fluorescence of a substituted aminopyridine that is released after amide hydrolysis. The conjugates of the present invention are also particularly useful in screening assays, which enable the identification of inhibitory molecules for amide hydrolases and other enzymes. The identified amide hydrolase inhibitors can be used in the treatment of a variety of diseases and disorders associated with aberrant amide hydrolase activity. | 2010-06-24 |
20100160392 | HISTONE DEACETYLASE INHIBITORS - The present invention provides histone deacetylase inhibitors of general formula (I), a process for the preparation of such compounds and uses of the compounds in medicine, especially in the treatment of cancers: in which R | 2010-06-24 |
20100160393 | CRYSTAL FORM OF EPOTHILONE B AND USE IN PHARMACEUTICAL COMPOSITIONS - The invention relates to new crystal forms of epothilone B. | 2010-06-24 |
20100160394 | USE OF 4-[(4- THIAZOLYL)PHENOXY]ALKOXY-BENZAMIDINE DERIVATIVES FOR THE PROPHYLAXIS AND TREATMENT OF OSTEOPOROSIS - This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prophylaxis and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isoproply-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1 as a pharmaceutical composition for the prophylaxis and treatment of osteoporosis. | 2010-06-24 |
20100160395 | CYCLOPROPYL COMPOUNDS - A compound of the formula: | 2010-06-24 |