Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 514/369)
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Publication number: 20120225909Abstract: [Objective] To provide a drug that selectively stimulates the ?3-adrenergic receptors, particularly a drug capable of preferentially stimulating the ?3-adrenergic receptors over the ?1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.Type: ApplicationFiled: September 30, 2010Publication date: September 6, 2012Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Yasuhiro Wada, Akifumi Morimoto
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Publication number: 20120219613Abstract: Provided herein are a series of arylmethylidene rhodanine derivatives having broad-spectrum antiviral activity against enveloped viruses, including but not limited to filoviruses, poxviruses, arenaviruses, bunyaviruses, paramyxoviruses, flaviviruses, influenza A, and HIV-1. The compounds act via a novel mechanism to disrupt viral membranes and inhibit viral attachment, fusion, and/or entry into host cells. The membrane disrupting activity of the compounds is selective for viral membranes relative to other biological membranes, making the compounds non-toxic to cells and host subjects.Type: ApplicationFiled: June 18, 2009Publication date: August 30, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Benhur Lee, Michael E. Jung, Michael C. Wolf, Tinghu Zhang
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Patent number: 8252940Abstract: A method for inhibiting Gram-negative bacterial pathogenesis, a method of screening for compounds that inhibit type III secretion in Gram-negative bacteria, and compounds that inhibit type III secretion in Gram-negative bacteria.Type: GrantFiled: August 16, 2010Date of Patent: August 28, 2012Assignee: University of WashingtonInventors: Heather B. Felise, Samuel I. Miller, Toni Kline
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Publication number: 20120207703Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, and pharmaceutical compositions and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: February 9, 2012Publication date: August 16, 2012Applicant: IDENIX PHARMACEUTICALS, INC.Inventors: Christophe Claude PARSY, Francois-Rene ALEXANDRE, Thierry CONVARD, Dominique SURLERAUX
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Publication number: 20120202687Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: February 6, 2012Publication date: August 9, 2012Inventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
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Publication number: 20120202814Abstract: The present invention relates to the medical use of the compound of formula 1, 2, 3 or 4:Type: ApplicationFiled: October 4, 2010Publication date: August 9, 2012Applicants: UNIVERSITÀ DEGLI STUDI DI SIENA, CONSIGLIO NAZIONALE DELLE RICERCHEInventors: Marco Radi, Maurizio Botta, Federico Falchi, Giovanni Maga, Fausto Baldanti, Stefania Paolucci
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Patent number: 8236834Abstract: It is an object of the present invention to provide the crystalline form of a thiazolidinedione compound, which is effective as a pharmaceutical ingredient for manufacturing a peroxisome proliferator-activated receptor (PPAR) activator and an anticancer pharmaceutical composition. The present invention relates to a crystalline form of a hydrate of 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione dihydrochloride represented by the following formula (I).Type: GrantFiled: February 8, 2008Date of Patent: August 7, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Hisaki Kajino, Yutaka Ikeuchi, Eiji Numagami
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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Publication number: 20120196838Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.Type: ApplicationFiled: January 25, 2012Publication date: August 2, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
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Publication number: 20120196864Abstract: A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-? modulator, and is useful as a prophylactic or therapeutic agent for cancer.Type: ApplicationFiled: August 4, 2010Publication date: August 2, 2012Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
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Publication number: 20120189579Abstract: The present invention concerns a substituted pyrrolidinone of the following formula I or a salt, solvate, tautomer, isotope, enantiomer, diastereoisomer or racemic mixture thereof: (I), for the treatment of hepatitis C.Type: ApplicationFiled: July 9, 2010Publication date: July 26, 2012Applicant: VIVALISInventors: Amaya Berecibar, Philippe Guedat, Isabelle Valarche, Céline Mohamed-Arab, Christophe Matt
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Patent number: 8222285Abstract: Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R1 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R2 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R5 is as defined herein; Z is O, S, S(O), S(O)2, or NR5a; X is S, O, N, NR3, or CR3; Y is NCR4 or NR4; R3, R4, and R5 are as defined herein; R8 is aryl, heteroaryl, —PO(OR9)(OR10), —PO(OR9)R10 or —P(O)(R9)R10 (wherein R9 and R10 are as defined herein)/R6 and R7 are independently H, halogen, or alkyl; m is 0 or 1; and n is 0 to 3, or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: GrantFiled: June 11, 2008Date of Patent: July 17, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Sean Chen, Peter T. W. Cheng, Rebecca A. Smirk
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Publication number: 20120178782Abstract: Synergistic pharmaceutical compositions and the methods for preventing and treating proliferative diseases such as cancer and psoriasis. The compositions comprise synergistic combinations of: (i) an acyl-CoA-synthetase enzyme inhibitor (AcsI4), (ii) a compound having an inhibiting effect on enzymes with cyclooxygenase activity (COX); and (iii) a compound selected from a 5-lypoxygenase enzyme (LOX-5) inhibitor and a leukotriene receptor antagonist.Type: ApplicationFiled: September 10, 2010Publication date: July 12, 2012Inventor: Ernesto Jorge Podesta
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Publication number: 20120178749Abstract: The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.Type: ApplicationFiled: February 21, 2012Publication date: July 12, 2012Inventors: Michael Roth, Beatriz Fontoura, Shuguang Wei, Neal Satterly
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Publication number: 20120165375Abstract: This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.Type: ApplicationFiled: March 8, 2012Publication date: June 28, 2012Applicant: Novo Nordisk A/SInventors: Anthony Murray, Jasper Lau, Per Vedsø, Lise Brown Christiansen
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Publication number: 20120165335Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.Type: ApplicationFiled: June 23, 2011Publication date: June 28, 2012Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Publication number: 20120164120Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.Type: ApplicationFiled: December 23, 2011Publication date: June 28, 2012Applicant: FOOD INDUSTRY RESEARCH AND DEVELOPMENT INSTITUTEInventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
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Patent number: 8206949Abstract: A method is described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of an inhibitor of Pmt-mediated O-linked glycosylation and/or in the presence of one or more ?-1,2-mannosidases.Type: GrantFiled: November 10, 2006Date of Patent: June 26, 2012Assignee: GlycoFi, Inc.Inventors: Piotr Bobrowicz, W. James Cook, Warren Kett
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Patent number: 8202861Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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.Type: GrantFiled: August 9, 2004Date of Patent: June 19, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus E Gonzales, III, Andreas P Termin, Esther Martinborough, Nicole Zimmerman
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Publication number: 20120149710Abstract: Bacterial infections, including Methicillin resistant Staphylococcus aureus (MRSA) infections are a major health problem that has created a pressing need for new antibiotics. Pyridazinone, rhodanine, and pyrazolethione compounds effective inhibit the enzymatic activity of sortase A (srtA) found in gram positive bacteria are disclosed. A structure activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC50 values in the sub-micromolar range. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Many of these molecules also inhibit the sortase enzyme from B. anthracis suggesting that they may be generalized sortase inhibitors. The novel compounds, compositions, uses, formulations, medicaments, articles of manufacture provide improved materials, uses, and treatments useful in combating infectious disorders.Type: ApplicationFiled: August 23, 2010Publication date: June 14, 2012Inventors: Michael E. Jung, Robert T. Clubb, Sung Wook Yi, Nutee Suree, Jeremy Justin Clemens
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Patent number: 8193224Abstract: The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect.Type: GrantFiled: September 30, 2005Date of Patent: June 5, 2012Assignees: Fujifilm CorporationInventors: Masataka Ihara, Kiyosei Takasu, Khanitha Pudhom, Hiroshi Kitaguchi, Masayuki Kawakami, Kozo Sato
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Publication number: 20120136034Abstract: Compounds of formula I and their metabolites are potent mediators of an inflammatory response: (I) where a, b, c, d, e, f, V, W, X, Y, Ra, Ra?, Rb, Rb?, Rc, and Rc? are defined herein. In particular, the compounds of the invention are candidate therapeutics for treating inflammatory conditions.Type: ApplicationFiled: August 2, 2010Publication date: May 31, 2012Applicant: University of Pittsburgh -Of the Commonwealth SystInventors: Bruce A. Freeman, Francisco J. Schopfer
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Publication number: 20120136033Abstract: Disclosed are a new class of non-lipid small molecule inhibitors which interfere with the interaction between PIP3 and pleckstrin homology domains. These molecules target a broad range of PIP3-dependent signaling events in vitro and exert significant anti-tumor activity in vivo. The small molecule inhibitors of the invention can be used alone or together with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) or other cancer medicament to treat cancer. Small molecule inhibitors of the invention act synergistically in combination with TRAIL in treating cancer. Pharmaceutical compositions and methods for treating cancer are provided.Type: ApplicationFiled: May 17, 2010Publication date: May 31, 2012Applicants: President and Fellows of Harvard College, Tufts UniversityInventors: Alexei Degterev, Mikhail Reibarkh, Gerhard Wagner, Junying Yuan
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Publication number: 20120135929Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, a compound disclosed herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 20, 2010Publication date: May 31, 2012Applicant: Ardea Biosciences Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet, Karen Watson
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Patent number: 8188080Abstract: Disclosed herein are Vaccinia H1-related (VHR) protein tyrosine phosphatase (PTP) inhibitors that provide a method for treating cancer.Type: GrantFiled: October 17, 2008Date of Patent: May 29, 2012Assignee: Sanford-Burnham Medical Research InstituteInventors: Tomas Mustelin, Lutz Tautz
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Patent number: 8188126Abstract: The invention provides methods of treating a memory deficiency in a subject in need of such treatment, where the methods comprise administering to a subject an effective amount of a compound of formula (1): wherein: R1 is hydrogen, fluorine or a methoxyl group, R1 being in position 2, 3, 4 or 5 of the aromatic carbocycle; R2 is hydrogen or a methyl group; R3 is hydrogen, a methyl group or an ethyl group; and their pharmaceutically acceptable acid addition salt as well as the isomers and the tautomers thereof. The memory deficiency may be correlated with a memory deficiency induced by scopolamine.Type: GrantFiled: May 24, 2010Date of Patent: May 29, 2012Assignee: Pierre Fabre MedicamentInventors: Bernard Vacher, Bernard Bonnaud, Marc Marien, Peter Pauwels
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Publication number: 20120129896Abstract: The present invention relates to thiazolidinedione analogues that are useful for treating hypertension, diabetes, and inflammatory diseases.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Applicant: Metabolic Solutions Development CompanyInventors: Gerard R. Colca, Robert C. Gadwood, Tim Parker
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Publication number: 20120129847Abstract: Disclosed are methods for the treatment of diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (wet form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like.Type: ApplicationFiled: October 5, 2011Publication date: May 24, 2012Inventors: Kevin Gene Peters, Robert Shalwitz
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Publication number: 20120129893Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: January 12, 2012Publication date: May 24, 2012Inventors: Jacques DUMAS, Uday Khire, Timothy B. Lowinger, Holger Paulsen, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, Holia Hatoum-Mokdad, Jeffrey Johnson, Wendy Lee, Aniko Redman, Robert Sibley, Joel Renick
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Patent number: 8183213Abstract: Combination therapy comprising RXR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.Type: GrantFiled: October 24, 2007Date of Patent: May 22, 2012Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Jacqueline C. Bussolari, Xiaoli Chen, Bruce R. Conway, Keith T. Demarest, Hamish N. M. Ross, Rafael Severino
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Publication number: 20120122939Abstract: A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.Type: ApplicationFiled: January 19, 2012Publication date: May 17, 2012Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20120122877Abstract: The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in S. aureus. The compositions also have the ability to inhibit growth of S. aureus and as such are useful as antibiotic compounds.Type: ApplicationFiled: July 1, 2010Publication date: May 17, 2012Applicant: TRUSTEES OF DARTMOUTH COLLEGEInventors: Ambrose Cheung, Zhibiao Fu
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Publication number: 20120122780Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 20, 2010Publication date: May 17, 2012Applicant: Ardea Biosciences Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet
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Publication number: 20120122907Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X1, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 14, 2010Publication date: May 17, 2012Inventor: Christelle Boléa
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Publication number: 20120115916Abstract: The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: ApplicationFiled: June 11, 2010Publication date: May 10, 2012Applicant: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20120114765Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.Type: ApplicationFiled: March 31, 2010Publication date: May 10, 2012Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
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Publication number: 20120115912Abstract: A method of treating a PPAR? and/or RXR related disease or disorder in a subject includes adminstering to the subject an RXR agonist alone or in combination with a PPAR? agonist.Type: ApplicationFiled: July 12, 2010Publication date: May 10, 2012Inventors: Gary E. Landreth, Paige E. Cramer
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Publication number: 20120108591Abstract: A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol
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Publication number: 20120108571Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: January 10, 2012Publication date: May 3, 2012Inventors: Michael Gaul, Lily Lee Searle, Dionisios Rentzeperis
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Patent number: 8168231Abstract: Antimicrobial compositions useful for preserving wood, and comprising a variety of antimicrobial compounds.Type: GrantFiled: November 9, 2007Date of Patent: May 1, 2012Assignee: Rohm and Haas CompanyInventors: John William Ashmore, Kiran Pareek
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Publication number: 20120101067Abstract: Described herein are methods for improving engraftment of hematopoietic cells in an individual following hematopoietic progenitor cell transplantation (e.g., via bone marrow or cord blood transplantation). Methods for increasing hematopoietic progenitor cell proliferation in individuals with bone marrow aplasia are also described. The methods involve administering an agent that inhibits adipogenesis, adipocyte growth, adipocyte differentiation and/or adipocyte proliferation.Type: ApplicationFiled: April 15, 2010Publication date: April 26, 2012Applicant: CHILDREN'S MEDICAL CENTER CORPORATIONInventors: Olaia Naveiras, George Daley, Pamela L. Wenzel
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Publication number: 20120093878Abstract: The present invention relates to pharmaceutical compositions that include a combination of a biguanide present in an extended-release form and a thiazolidinedione present in an immediate-release form. The present invention further relates to the processes for preparing such compositions.Type: ApplicationFiled: July 29, 2011Publication date: April 19, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Romi Barat SINGH, Kalaiselvan RAMARAJU, Sandeep Kumar VATS, Balaram MONDAL
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Publication number: 20120093748Abstract: Topical compositions are provided that have 0.5% or more of at least one personal care or pharmaceutical acid, and lightly- to moderately-crosslinked PVP, which is an effective thickener in the low pH systems. In preferred embodiments, the acid is a hydroxy acid and the composition used for personal care, or prescriptive or non-prescriptive medication indications for use on the skin, hair, scalp, foot, or lips. Also provided is the use of the topical compositions to deliver the acid(s) to the skin, hair, scalp, foot, or lips. Especially preferred is a use to reduce irritation and stinging compared to an equivalent compositions not having lightly- to moderately-crosslinked PVP.Type: ApplicationFiled: March 11, 2010Publication date: April 19, 2012Applicant: ISP INVESTMENTS INC.Inventors: Hani Fares, Chris Barrett, Tracey Ross, Anthony Luschen
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Publication number: 20120088783Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: September 26, 2011Publication date: April 12, 2012Applicant: Ampere Life Sciences, Inc.Inventors: Bing WANG, Gail Walkinshaw, Donald R. James
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Publication number: 20120088759Abstract: The present invention relates to thiazolidin-4-one and [1,3]-thiazinan-4-one compounds of formula (I) wherein X, Y, R3 and R4 are as described in the description, or pharmaceutically acceptable salts thereof, for the prevention or treatment of diseases related to the orexin system. The present invention also relates to novel thiazolidin-4-one compounds of formula (II) and their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (II), and especially their use as orexin receptor antagonists.Type: ApplicationFiled: May 11, 2010Publication date: April 12, 2012Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, John Gatfield, Romain Siegrist, Thierry Sifferlen, Jodi T. Williams
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COMPOUND HAVING DETRUSOR MUSCLE-CONTRACTING ACTIVITY AND URETHRAL SPHINCTER MUSCLE-RELAXING ACTIVITY
Publication number: 20120088805Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.Type: ApplicationFiled: June 9, 2010Publication date: April 12, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Hidekazu Matsuta, Hiroki Okada -
Patent number: 8148541Abstract: Disclosed herein are rhodanine derivatives, a method for the preparation thereof, and a pharmaceutical composition containing the same. The rhodanine derivatives have inhibitory activity against protein phosphatases (PPase) such as PTP1B, Prl-3, LAR, CD45, Cdc25A, Cdc25B, Cdc25C, Yop, PP1 and VHR, and can be applied for the prevention and treatment of PPase-caused diseases, including autoimmune diseases, diabetes, impaired glucose intolerance, insulin resistance, obesity, cancers, etc. when the inhibitory activity thereof is modulated.Type: GrantFiled: December 8, 2006Date of Patent: April 3, 2012Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Seong Eon Ryu, Seung Jun Kim, Dae Gwin Jeong, Sang Hyeup Lee, Suk Kyeong Jung, Hwan Mook Kim, Song Kyu Park, Ki Ho Lee, Chang Woo Lee, Joong-Kwon Choi, Jin Hee Ahn
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Publication number: 20120077804Abstract: The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.Type: ApplicationFiled: July 24, 2008Publication date: March 29, 2012Applicant: The Regents of the University of CaliforniaInventor: Shou-Wei Ding
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Patent number: RE43615Abstract: A method for controlling yeast-to-filamentous growth transition in fungi comprising contacting a fungal cell with an anti-fungal small molecule in an amount effective to reduce or inhibit the yeast-to-filamentous growth transition, wherein the anti-fungal small molecule is 5-(p-Bromobenzylidine)-?-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid or an analog thereof. A method for treating fungal infections comprising contacting one or more fungal cells with an anti-fungal small molecule in an amount effective to control the fungal infection, wherein the anti-fungal small molecule is 5-(p-Bromobenzylidine)-?-isopropyl-4-oxo-2-thioxo-3-thiozolidineactic acid or an analog thereof.Type: GrantFiled: January 25, 2012Date of Patent: August 28, 2012Assignee: Montana State University—BillingsInventors: Kurt A. Toenjes, David K. Butler