24th week of 2010 patent applcation highlights part 56 |
Patent application number | Title | Published |
20100152185 | DIPHENYL SUBSTITUTED CYCLOALKANES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. | 2010-06-17 |
20100152186 | TRIAZOLYL PYRIDYL BENZENESULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists. | 2010-06-17 |
20100152187 | AMINOTHIAZOLE DERIVATIVES AS HUMAN STEAROYL-COA DESATURASE INHIBITORS - Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R | 2010-06-17 |
20100152188 | Novel Heterocyclic Compounds - The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I). | 2010-06-17 |
20100152189 | NOVEL POLYMORPHOUS FORM AND THE AMORPHOUS FORM OF 5-CHLORO-N-({ (5S)-2-OXO-3[4-(3-OXO-4-MORPHOLINYL(-PHENYL]-1,3-OXAZOLIDINE-5-YL}-METHYL- )-2-THIOPHENE CARBOXAMIDE - The present invention relates to a novel polymorphic form and the amorphous form of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophene-carboxamide, processes for their preparation, medicaments comprising these forms, and their use in the control of diseases. | 2010-06-17 |
20100152190 | Substituted Pyrrolidine-2-Carboxamides - There are provided compounds of the formula | 2010-06-17 |
20100152191 | CYCLOPROPYL PYRROLIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 orexin receptors are involved. | 2010-06-17 |
20100152192 | FUSED IMIDAZOLE CARBOXAMIDES AS TRPV3 MODULATORS - The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. | 2010-06-17 |
20100152193 | PYRIDAZINONES - The present invention is concerned with novel pyridazinones of formula (I) | 2010-06-17 |
20100152194 | ANTHRANILAMIDE ARTHROPODICIDE TREATMENT - This invention pertains to methods for protecting a propagule or a plant grown therefrom from invertebrate pests comprising contacting the propagule or the locus of the propagule with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof | 2010-06-17 |
20100152195 | 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: | 2010-06-17 |
20100152196 | Novel Fused Pyrrolocarbazoles - The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles. | 2010-06-17 |
20100152197 | (4-TERT-BUTYLPIPERAZIN-2-YL)(PIPERAZIN-1-YL)METHANONE-N-CARBOXAMIDE DERIVATIVES - The present invention relates to compounds of formula (I) | 2010-06-17 |
20100152198 | USE OF C-SRC INHIBITORS IN COMBINATION WITH A PYRIMIDYLAMINOBENZAMIDE COMPOUND FOR THE TREATMENT OF LEUKEMIA - The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl]benzamide. | 2010-06-17 |
20100152200 | ALPHAVIRUS INHIBITORS AND USES THEREOF - The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of alphaviruses. | 2010-06-17 |
20100152201 | Oligomer-Antihistamine Conjugates - The invention provides antihistamine drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the antihistamine drug not attached to the water-soluble oligomer. | 2010-06-17 |
20100152202 | Tissue Factor Promoter Polymorphisms - The invention provides compositions and methods for determining the likelihood of successful treatment with a pyrimidine based antimetabolite chemotherapy drug such as 5-fluorouracil or in combination with a platinum based chemotherapy drug, such as 5-fluorouracil/oxaliplatin. The methods comprise determining the genomic polymorphism present in a predetermined region of a gene of interest and correlating the polymorphism to the predictive response. Patients identified as responsive are then treated with the appropriate therapy. | 2010-06-17 |
20100152203 | THIADIAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2010-06-17 |
20100152204 | TREATMENT FOR SPINAL MUSCULAR ATROPHY - A method of treating spinal muscular atrophy. The method includes administering an effective amount of composition including a sodium-proton exchanger inhibitor and a pharmaceutically acceptable carrier or salt, to a subject with spinal muscular atrophy to ameliorate a symptom of spinal muscular atrophy. | 2010-06-17 |
20100152205 | CXCR2 INHIBITORS - The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease. | 2010-06-17 |
20100152206 | Bicyclic Dihydropyrimidines and Uses Thereof - The present invention provides compounds having formula (I): (I) and pharmaceutically acceptable derivatives thereof; as described generally and in subclasses herein, which compounds are useful as kinesin inhibitors (e.g., Eg5 inhibitors), and thus are useful, for example, for the treatment of proliferative disorders e.g., cancer. The invention additionally provides methods for preparing compounds of the invention, compositions comprising them, and methods for the use thereof in the treatment of various disorders where Eg5 is involved. In certain embodiments, the present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily. | 2010-06-17 |
20100152207 | GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R | 2010-06-17 |
20100152208 | BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis. Formula (I). | 2010-06-17 |
20100152209 | Compounds for Modulating TRPV3 Function - The present application relates to compounds and methods for treating pain and other conditions related to TRPV3. | 2010-06-17 |
20100152210 | PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 2010-06-17 |
20100152211 | INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo. | 2010-06-17 |
20100152212 | PREQ1 RIBOSWITCHES AND METHODS AND COMPOSITIONS FOR USE OF AND WITH PREQ1 RIBOSWITCHES - The preQ1 riboswitch is a target for antibiotics and other small molecule therapies. The preQ1riboswitch and portions thereof can be used to regulate the expression or function of RNA molecules and other elements and molecules. The preQ1 riboswitch and portions thereof can be used in a variety of other methods to, for example, identify or detect compounds. Compounds can be used to stimulate, active, inhibit and/or inactivate the preQ1 riboswitch. The preQ1 riboswitch and portions thereof, both alone and in combination with other nucleic acids, can be used in a variety of constructs and RNA molecules and can be encoded by nucleic acids. | 2010-06-17 |
20100152213 | COMPOUND THAT IS A DUAL INHIBITOR OF ENZYMES PDE7 AND/OR PDE4, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The invention relates to a series of dual inhibitors of enzymes PDE7 and PDE4, having formula (I) and to the use thereof in the production of pharmaceutical compositions for the treatment of inflammatory and/or autoimmune processes. | 2010-06-17 |
20100152214 | NOVEL PYRIMIDINECARBOXAMIDE DERIVATIVES - This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections. | 2010-06-17 |
20100152215 | METHODS OF IDENTIFYING ACTIVATORS OF LYN KINASE - The present invention relates to methods of identifying activators of lyn kinase by preincubating a test compound in the presence of lyn kinase; adding ATP and substrate to the lyn kinase and test compound; incubating the test compound, lyn kinase, ATP, and substrate; and measuring phosphorylation level of the substrate, whereby an increase in the phosphorylation of the substrate indicates that the test compound is an activator of lyn kinase. | 2010-06-17 |
20100152216 | MONOCYCLIC ANILIDE SPIROLACTAM CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I: | 2010-06-17 |
20100152217 | METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years. | 2010-06-17 |
20100152218 | COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY - The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful. | 2010-06-17 |
20100152219 | PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES - Compounds of formula (I): and their use in the inhibition of Trk activity are described. | 2010-06-17 |
20100152220 | INDENE DERIVATIVES AS PHARMACEUTICAL AGENTS - Compounds of formula (Ia): | 2010-06-17 |
20100152221 | PHARMACEUTICAL COMPOSITION - Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided. Methods for treating pain using such compositions is also demonstrated. | 2010-06-17 |
20100152222 | Medicinal Compositions Comprising Buprenorphine And Nalmefene - An analgesic composition, in parenteral unit dosage form or in a unit dosage form suitable for delivery via the dermis or mucosa, comprises buprenorphine and an amount nalmefene such that the ratio by weight of buprenorphine to nalmefene delivered to or reaching the plasma of a patient is in the range 22.6:1 to 40:1. The analgesic action of the buprenorphine is potentiated by the low dose of nalmefene. Also provided are a method of treatment of pain and the use of nalmefene and buprenorphine for the manufacture of a medicament. | 2010-06-17 |
20100152223 | CRYSTAL FORM OF CABERGOLINE - The present invention relates to a cabergoline crystal form L, its preparation from halogenated aromatic solvents and aliphatic hydrocarbons and to pharmaceutical compositions containing the new form. | 2010-06-17 |
20100152224 | SCOPINE MODULATORS OF MUSCARINIC ACETYLCHOLINE RECEPTOR - The present invention relates to new scopine modulators of muscarinic acetylcholine receptors, pharmaceutical compositions thereof, and methods of use thereof. | 2010-06-17 |
20100152225 | HYDROGENATED PYRIDO [4,3-B] INDOLES SUCH AS DIMEBON FOR TREATING CANINE COGNITIVE DYSFUNCTION SYNDROME - The invention provides method for treating Cognitive Dysfunction Syndrome (CCDS), slowing the onset and/or development and/or progression of CCDS or preventing the development of CCDS in canines, such as dogs, using hydrogenated pyrido[4,3-b]indoles, including dimebon. | 2010-06-17 |
20100152226 | SUSTAINED RELEASE IMPLANT FOR GRANISETRON - The main goals of the invention are to develop the long-term release of Granisetron injection implant composition with biodegradable polymer and to develop relative processing. Granisetron is mixed with different biodegradable polymers, and then hot melt extrusion technique with different diameter, temperature, rate of extrusion and holding time is applied to make implant. In vitro dissolution of the Granisetron injection implant composition shows the component continued release of the drug for over 7 days. | 2010-06-17 |
20100152227 | Methods for Enhancing Stability of Polyorthoesters and Their Formulations - Disclosed herein are methods of enhancing the stability of a sustained pharmaceutical composition comprising an active agent and a polymer and methods of preparing such pharmaceutical compositions with enhanced stability. | 2010-06-17 |
20100152228 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR RELIEVING PAIN AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS - Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like. | 2010-06-17 |
20100152229 | Process for the Synthesis of Moxifloxacin Hydrochloride - A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II): | 2010-06-17 |
20100152230 | HYDROXY SUBSTITUTED 1H-IMIDAZOPYRIDINES AND METHODS - Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy 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. | 2010-06-17 |
20100152231 | Compositions Useful For Treating Irritable Bowel Syndrome - The present invention relates to a method of treating irritable bowel syndrome with constipation (IBS-c) or irritable bowel syndrome with alternating constipation and diarrhea (IBS-a) in a subject in need of treatment. The method comprises administering to said subject a therapeutically effective amount of a thieno[3,2-b]pyridine compound of Structural Formula I or a pharmaceutically acceptable salt or N-oxide derivative thereof. | 2010-06-17 |
20100152232 | 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF - The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C | 2010-06-17 |
20100152233 | 3-SUBSTITUTED-2(ARYLALKYL)-1-AZABICYCLOALKANES AND METHODS OF USE THEREOF - The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C | 2010-06-17 |
20100152234 | Substituted 4-(1,2,3,4-tetrahydroisoquinolin-2-yl)-4-oxobutyric acid amide as KCNQ2/3 modulators - The invention relates to substituted tetrahydroisoquinolinyl-4-oxobutyric acid amides, methods for the preparation thereof, medicinal products containing these compounds and the use of these compounds for the preparation of medicinal products. | 2010-06-17 |
20100152235 | OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (S1P) - The present invention relates to a novel oxadiazole derivative having pharmacological activity, processes for its preparation, pharmaceutical compositions containing it and its use in the treatment of various disorders. | 2010-06-17 |
20100152236 | Cyclic amine compound - A compound represented by the formula (I) | 2010-06-17 |
20100152237 | BIS-PYRINDINO CONTAINING COMPOUNDS FOR THE USE IN THE TREATMENT OF CNS PATHOLOGIES - N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter. | 2010-06-17 |
20100152238 | NOVEL QUINONOID DERIVATIVES OF CANNABINOIDS AND THEIR USE IN THE TREATMENT OF MALIGNANCIES - Novel cannabinoid-derived quinone derivatives (quinonoid derivatives) having a substituted hydroxyl group, pharmaceutical compositions comprising same and uses thereof as anti-proliferative agents, are provided. | 2010-06-17 |
20100152239 | Method to Improve Survival in Sepsis - This invention relates to the use of an α7nAChR-agonist such as GTS to control systemic inflammation during resuscitation following severe trauma such blood loss because of severe hemorrhage. | 2010-06-17 |
20100152240 | PYRROLINE-2-ONE DERIVATIVES AGAINST CELL RELEASING TUMOR NECROSIS FACTOR, PREPARATION METHODS AND USES THEREOF - Compounds represented by Formula (I) or Formula (II), their pharmaceutically acceptable salts or hydrates | 2010-06-17 |
20100152241 | INHIBITORS OF STORE OPERATED CALCIUM RELEASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 2010-06-17 |
20100152242 | Transdermal Electrotransport Delivery Device Including an Antimicrobial Compatible Reservoir Composition - A transdermal electrotransport drug delivery device having an anode, a cathode and a source of electrical power electrically connected to the anode and the cathode. At least one of the anode and the cathode includes an electrode and a reservoir comprised of a housing composed of a polymeric material and an aqueous medium in contact with the housing. The aqueous medium includes (i) a drug or an electrolyte salt or a mixture thereof, (ii) propylene glycol, and (iii) an antimicrobial agent in an amount sufficient to inhibit microbial growth in the aqueous medium. The propylene glycol prevents the antimicrobial agent from being adsorbed by other materials used in the construction of the delivery device. A process for preparing a transdermal electrotransport drug delivery device is also provided. | 2010-06-17 |
20100152243 | Treatment of renal cell carcinoma - Methods are provided of treating renal cancer by administration of certain 3,3′,4,4′-tetrahydroxy-2,2′-bipyridine-N,N′-dioxide compounds, especially 3,3′,4,4′-tetrahydroxy-2,2′-bipyridine-N,N′-dioxide (Orellanine), using particular administration protocols and dosing regimens, as well as pharmaceutical compositions suitable for use in the treatment methods that are provided. | 2010-06-17 |
20100152244 | SELF-EMULSIFYING FORMULATION OF TIPRANAVIR FOR ORAL ADMINISTRATION - A self-emulsifying formulation of tipranavir for oral administration. | 2010-06-17 |
20100152245 | INSECTICIDAL N-SUBSTITUTED (6-HALOOALKYLPYRIDIN-3-YL)-ALKYL SULFOXIMINES - N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects. | 2010-06-17 |
20100152246 | 5-Oxoisoxazoles as inhibitors of lipases and phospholipases - The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances. | 2010-06-17 |
20100152247 | MEDICAMENT FOR TREATING SCHIZOPHRENIA COMPRISING CILOSTAZOL - The invention relates to a medicament for preventing and/or treating schizophrenia which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof. | 2010-06-17 |
20100152248 | ISCHEMIC DISORDER OR DISEASE INHIBITORS - The invention relates to the use of at least on inhibitor selected from the group consisting of raf-, protein kinase C(PKC)-, MEK1/2-, or ERK1/2-inhibitors, for the manufacturing of a medicament to be administrated from 1 up to 12 hours after initiation of an ischemic disease. | 2010-06-17 |
20100152249 | COMPOSITONS AND METHOD FOR TREATMENT OF MOOD AND COGNITIVE IMPAIRMENTS - Compositions, manufacture, and methods for diagnosis and treatment of subjects exhibiting mood disorders and/or being at risk of cognitive impairment. | 2010-06-17 |
20100152250 | CAPSULE FORMULATION OF PIRFENIDONE AND PHARMACEUTICALLY ACCEPTABLE EXCIPIENTS - A capsule formulation of pirfenidone is provided that includes pharmaceutically acceptable excipients. In one embodiment, this capsule formulation is capable of sustaining desirable pharmacokinetic responses in a patient. Further provided are methods of treating fibrotic conditions and other cytokine-mediated disorders by administering pirfenidone capsules of such formulation to a patient in need. | 2010-06-17 |
20100152251 | PYRIDINE, QUINOLINE, AND ISOQUINOLINE N-OXIDES AS KINASE INHIBITORS - This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders. | 2010-06-17 |
20100152252 | Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments - The present invention relates to heterocyclyl-substituted-ethylamino-phenyl compounds of general formula (I), wherein K-L-M-N, Z and R | 2010-06-17 |
20100152253 | NON-STEROIDAL BRASSINOSTEROID MIMETIC - The present invention relates to non-steroidal mimetics of brassinosteroids. More specifically, it relates to non-steroidal monocyclic compounds, capable of rescuing the brassinosteroid receptor null mutation bri1-116. Preferably, said compounds are low molecular weight, monocyclic halogenated compound. | 2010-06-17 |
20100152254 | ALPHA-HALO- AND ALPHA-ALKYL-CYCLOPROPYLCARBOXY COMPOUNDS AND USES THEREOF - Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided. | 2010-06-17 |
20100152255 | Organic Compounds - Compounds of the formula | 2010-06-17 |
20100152256 | (2R)-2-[(4-sulfonyl) aminophenyl] propanamides and pharmaceutical compositions containing them - The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma. | 2010-06-17 |
20100152257 | ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS - Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases. | 2010-06-17 |
20100152258 | ANGIOTENSIN II RECEPTOR ANTAGONISTS - A compound having the structure (Formula I), wherein Y is —Y | 2010-06-17 |
20100152259 | ANGIOTENSIN II RECEPTOR ANTAGONISTS - A compound having the structure (Formula I), wherein R an angiotensin receptor antagonist active group, Y is Y | 2010-06-17 |
20100152260 | CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES - The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders. | 2010-06-17 |
20100152261 | NOVEL NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - A nitrogen-containing heterocyclic derivative represented by the following general formula (I), or a hydrate or solvate thereof, which has a selective antagonistic action on the muscarinic M | 2010-06-17 |
20100152262 | BUCCAL, POLAR AND NON-POLAR SPRAY CONTAINING ONDANSETRON - Buccal aerosol sprays or capsules using polar and non-polar solvents have now been developed which provide ondansetron for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, ondansetron, and optional flavoring agent; formulation II: aqueous polar solvent, ondansetron, optionally flavoring agent, and propellant; formulation III: non-polar solvent, ondansetron, and optional flavoring agent; formulation IV: non-polar solvent, ondansetron, optional flavoring agent, and propellant; formulation V: a mixture of a polar solvent and a non-polar solvent, ondansetron, and optional flavoring agent; formulation VI: a mixture of a polar solvent and a non-polar solvent, ondansetron, optional flavoring agent, and propellant. | 2010-06-17 |
20100152263 | THERAPY FOR THE TREATMENT OF DISEASE - Disclosed herein are pharmaceutical compositions comprising oxybutynin or tolterodine, or a free base thereof or a pharmaceutically acceptable salt thereof, and pilocarpine, or a free base thereof or a pharmaceutically acceptable salt thereof. Also disclosed are methods of treating a patient suffering from overactive bladder comprising administering to the patient the above pharmaceutical composition. | 2010-06-17 |
20100152264 | 3- TO 7-MEMBERED 1,3-DIAZA-4-OXO-HETEROCYCLIC DERIVATIVES CAPABLE OF RELEASING ACTIVE ALDEHYDES OR KETONES - The present invention provides 3- to 7-membered 1,3-diaza-4-oxo-heterocyclic derivatives, such as imidazolidinone O derivatives, capable of releasing in a controlled manner a biologically active aldehyde or ketone in the surrounding. The invention also relates to the use of these compounds as perfuming or flavoring ingredients, as well as to the perfuming compositions and consumer articles containing such derivatives. It also provides a process for preparing said derivatives of the invention | 2010-06-17 |
20100152265 | INDAZOLE DERIVATIVES - Compounds represented by the Formula (A-1) and the Formula (1) or salt thereof are provided. The compounds represented by the Formula (A-1) and the Formula (1) or salt thereof have a β3 adrenergic receptor agonist activity, and therefore are useful as an agent for the prevention and treatment of diabetes, obesity, hyperlipidemia, depression, biliary stone, a disorder derived from hyperactivity of biliary tract, a disorder derived from hyperactivity of digestive tract, interstitial cystitis, overactive bladder, urinary incontinence or a disorder derived from decreased tear secretion, etc. | 2010-06-17 |
20100152266 | Iodopyrazolyl Carboxanilides - This invention relates to novel intermediates used in the preparation of iodopyrazolylcarboxanilides of the formula (I) | 2010-06-17 |
20100152267 | NOVEL RIFAMYCIN 3,4-(3-SUBSTITUTED AMINOMETHYL) FUSED PYRROLO DERIVATIVES - The present invention is directed to novel 3,4-(3′-substituted aminomethyl) fused pyrrolo rifamyacin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes. | 2010-06-17 |
20100152268 | STABLE ATORVASTATIN FORMULATIONS - The present invention provides novel alternative pharmaceutical compositions comprising amorphous atorvastatin or a pharmaceutically acceptable salt thereof and a controlled amount of one or more additional compounds selected from the group consisting of compounds of formula I (formed by ring opening of the epoxide of Formula II to form a diketo dihydroxy derivative), II (diketo epoxide derivative), III (di-epoxide derivative formed by ring closure of the heptanoic acid chain to form a cyclohexanoate substituent), IV (2-oxo derivative with the isopropyl group rearranged to the 3-position) and V (phenantrene derivative of the 2-oxo derivative), together with one or more suitable pharmaceutical excipients, which compositions have improved stability. | 2010-06-17 |
20100152269 | MODIFIED-RELEASE FORMULATIONS OF AZABICYCLO DERIVATIVES - The present invention discloses modified-release oral dosage forms of an azabicyclo derivative or its pharmaceutically acceptable salts, solvates, esters, enantiomers, diastereomers, N-oxides and polymorphs; and processes for the preparation thereof. The modified release formulation comprises an azabicyclo derivative, at least one rate-controlling polymer and at least one pharmaceutically acceptable excipient which provides therapeutically effective plasma levels of the active ingredient for a period of up to 24 hours. | 2010-06-17 |
20100152270 | PESTICIDE COMPOSITION COMPRISING A STRIGOLACTONE DERIVATIVE AND A FUNGICIDE COMPOUND - A composition comprising at least a strigolactone derivative (a) of general formula: | 2010-06-17 |
20100152271 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and OR | 2010-06-17 |
20100152272 | FUNCTIONALIZED DRUGS AND POLYMERS THEREFROM - Compounds selected from: | 2010-06-17 |
20100152273 | LOW-VISCOUS ANTHRACYCLINE FORMULATION - The present invention relates to formulations comprising an anthracycline compound and an aromatic or heterocyclic compound. | 2010-06-17 |
20100152274 | CRYSTALLINE FORMS OF ATORVASTATIN 4-(NITROOXY) BUTYL ESTER - The present invention relates to two crystalline forms designated as form A and form B, of (βR,δR)-2(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbon-yl]-1H-pyrrole-1-heptanoic acid 4-(nitrooxy)butyl ester (atorvastatin 4-(nitrooxy)butyl ester), represented by the formula (I), The invention also relates to processes for the preparation of the forms A and B, to pharmaceutical compositions comprising the two forms, and to their use for treating and/or preventing acute coronary syndromes, stroke, neurodegenerative disorders, such as Alzheimer's and Parkinson's disease as well as autoimmune diseases, such as multiple sclerosis. | 2010-06-17 |
20100152275 | Drug or Supplement Combination with Conjugated Linoleic Acid for Fat Loss in Mammals - Food, feed or drug combinations with conjugated linoleic acid are described that cause enhanced fat loss in mammals more efficiently than any of the individual components of the combination. Food, feed, or drugs that activate AMP activated protein kinase, agonists of nuclear receptors that bind RXR in adipocytes, or statin inhibitors were found to be more effective for fat loss when combined with conjugated linoleic acid. | 2010-06-17 |
20100152276 | DEUTERATED AMINOCYCLOHEXYL ETHER COMPOUNDS AND PROCESSES FOR PREPARING SAME - This invention is directed to deuterated aminocyclohexyl ether compounds and processes for preparing same and methods of using same. | 2010-06-17 |
20100152277 | DIACYLGLYCEROL ACYLTRANSFERASE ASSAY - The present invention generally provides a method of measuring the biological activity of diacylglycerol acyltransferase (DGAT). Specifically, the present invention provides a method for rapid, mass screening of compounds which are able to modulate the biological activity of DGAT. More specifically, the present invention provides an assay system for measuring DGAT activity based on the use of particular micelles with the FlashPlate™ technology. | 2010-06-17 |
20100152278 | RNA Interference Mediated Inhibition of Cyclic Nucleotide Type 4 Phosphodiesterase (PDE4B) Gene Expression Using Short Interfering Nucleic Acid (siNA) - The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-1, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-1, MMP -2, MMP-3, MMP-9 and MMP-12. Specifically, the invention relates to double stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA), and multifunctional siNA molecules capable of mediating RNA interference (RNAi) against cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression, including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. The present invention also relates to small nucleic acid molecules, such as siNA, siRNA, antisense and others that can inhibit the function of endogenous RNA molecules or RNAi pathway components (RNAi inhibitors), such as endogenous micro-RNA (miRNA) (e.g., miRNA inhibitors) or endogenous short interfering RNA (siRNA), (e.g., siRNA inhibitors) or that can inhibit the function of RISC (e.g., RISC inhibitors), to modulate PDE4B gene expression by interfering with the regulatory function of such endogenous RNAs or proteins associated with such endogenous RNAs (e.g., RISC) including cocktails of such small nucleic acid molecules and lipid nanoparticle (LNP) formulations of such small nucleic acid molecules. Such small nucleic acid molecules are useful, for example, in providing compositions to prevent, inhibit, or reduce inflammatory, respiratory, and autoimmune diseases, traits, and conditions, and/or other disease states associated with PDE4B gene expression or activity in a subject or organism. | 2010-06-17 |
20100152279 | RNAi Inhibition of Serum Amyloid A For Treatment of Glaucoma - RNA interference is provided for inhibition of serum amyloid A mRNA expression in glaucomas involving SAA expression. | 2010-06-17 |
20100152280 | MODULATION OF SID-1 EXPRESSION - Compounds, compositions and methods are provided for modulating the expression of SID-1. The compositions comprise oligonucleotides, targeted to nucleic acid encoding SID-1. Methods of using these compounds for modulation of SID-1 expression and for diagnosis and treatment of diseases and conditions associated with expression of SID-1 are provided. | 2010-06-17 |
20100152281 | METHODS OF TREATING SYSTEMIC LUPUS ERYTHEMATOSUS IN INDIVIDUALS HAVING SIGNIFICANTLY IMPAIRED RENAL FUNCTION - The invention provides methods treating lupus nephritis based in individuals with significantly impaired renal function, and methods of selecting individuals for treatment based on significantly impaired renal function. The treatment entails administration of a conjugate comprising a non-immunogenic valency platform molecule and at least two double stranded DNA epitopes, such as DNA molecules, which bind to anti-DNA antibodies from the patient. The invention also provides methods of identifying individuals suitable for treatment for lupus, based on assessing renal function to identify those individuals with significant impairment of renal function. | 2010-06-17 |
20100152282 | USE OF DOUBLE STRANDED RNA HAIRPIN DUPLEXES IN GENE SILENCING - A DNA polynucleotide is described herein having a modified sequence of a target gene, wherein any one type of nucleotide in the target gene sequence has been chemically modified to another type of nucleotide; and a complementary sequence of the unmodified target gene; wherein either one of the modified sequence or the complementary sequence is in a reverse orientation to the other sequence; and wherein the RNA sequence transcribed from the DNA polynucleotide forms a duplex between the modified sequence and the complementary sequence so that a long double stranded RNA (IdsRNA) duplex forms between the modified and complementary sequences with base pair mismatches where the nucleotides have been modified, the IdsRNA duplex being capable of inhibiting expression of the target gene. RNA polynucleotides and IdsRNA duplexes transcribed by the DNA polynucleotide are also described, as is a method for producing the IdsRNA duplexes. These IdsRNA duplexes can be used in gene silencing. | 2010-06-17 |
20100152283 | TETRAHYDROCANNABINOL MODULATORS OF CANNABINOID RECEPTORS - The present invention relates to new tetrahydrocannabinol modulators of cannabinoid receptors, pharmaceutical compositions thereof, and methods of use thereof. | 2010-06-17 |
20100152284 | PREVENTION AND REVERSAL OF CHEMOTHERAPY-INDUCED PERIPHERAL NEUROPATHY - Provided herein are methods for treating or preventing neuropathy, neuropathy-related conditions, wherein the neuropathy or neuropathy-related conditions are induced by, or otherwise associated with, treatment of the subject with at least one chemotherapeutic agent, the methods comprising administering an effective amount of an isoflavonoid compound of formula (I). Also provided are methods for the treatment of nerve damage. Also provided are uses of isoflavonoid compounds of formula (I) in the treatment of neuropathy, neuropathy-related conditions and nerve damage. | 2010-06-17 |
20100152285 | Flavononol Renin Inhibitor Compounds and Methods of Use Thereof - The present disclosure relates in part to methods of treating or preventing renin mediated conditions comprising administering to a subject in need thereof a flavononol compound represented by formula I: | 2010-06-17 |