1,3-oxazoles (including Hydrogenated) Patents (Class 514/374)
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Patent number: 8268873Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: August 7, 2008Date of Patent: September 18, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Stamos, Martin Trudeau, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Jeffrey O. Saunders
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Patent number: 8268874Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to anti-cancer compounds, synthesis thereof, and methods of using same. Disclosed herein are various heterocyclic compounds and methods of using the novel anti-cancer compounds to inhibit the growth of a cancer cell, for instance a leukemia, non-small cell lung, central nervous system (CNS), skin, ovarian, renal, prostate, breast, or colon cancer cell. Other embodiments include methods of treating cancer in a subject, such as using the disclosed heterocyclic anti-cancer agents.Type: GrantFiled: March 3, 2009Date of Patent: September 18, 2012Assignee: University of Notre Dame du LacInventors: Marvin J. Miller, Garrett C. Moraski, Jonathan Stefely
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Patent number: 8263629Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: May 27, 2010Date of Patent: September 11, 2012Assignee: Novartis AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20120225883Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: May 14, 2012Publication date: September 6, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
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Patent number: 8252788Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 13, 2009Date of Patent: August 28, 2012Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Patent number: 8252823Abstract: A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of ?-cat oxazole and thiazole compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cancer, and others.Type: GrantFiled: January 28, 2009Date of Patent: August 28, 2012Assignee: New York UniversityInventors: Ramanuj Dasgupta, Foster Gonsalves
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Publication number: 20120214814Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: ApplicationFiled: January 23, 2012Publication date: August 23, 2012Inventors: Eric Anderson, Xin Jiang, Melean Visnick
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Publication number: 20120214802Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: ApplicationFiled: October 9, 2009Publication date: August 23, 2012Inventors: Geoffrey M. Bilcer, Thippeswamy Devasamudram, Sudha V. Ankala, John C. Lilly, Chunfeng Liu, Hui Lei, Arun K. Ghosh, Makoto Inoue
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Publication number: 20120214854Abstract: Heteroaryl compounds, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or disorders mediated by Diacylglycerol acyltransferase (DGAT) enzyme, particularly DGAT-1 is described.Type: ApplicationFiled: November 1, 2010Publication date: August 23, 2012Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma, Kishorkumar Shivajirao Kadam, Shivaji Sadashiv Kandre
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Publication number: 20120214804Abstract: The present invention relates to a pharmaceutical composition comprising a compound of formula (1), (2) or (3) as defined in the specification for the prevention or treatment of diseases associated with oxidative stress, mitochondria dysfunction, hypoxic injury, necrosis and/or ischemic reperfusion injury, and a cosmetic composition comprising an indole compound having an antioxidant effect.Type: ApplicationFiled: October 25, 2010Publication date: August 23, 2012Inventors: Soon Ha Kim, Hyoung Jin Kim, Heui Sul Park, Seon Yeong Gu, Hyo Shin Kwak, Du Hee Park, Hyo Soo Kim, Hyun Jai Cho, Ji Hyun Kim, Ju Young Kim, Kwang Min Park
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Patent number: 8247401Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: GrantFiled: October 29, 2008Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
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Patent number: 8247432Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs).Type: GrantFiled: May 19, 2011Date of Patent: August 21, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Publication number: 20120208852Abstract: The present application relates to new, heterocyclyl-substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: August 24, 2010Publication date: August 16, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Chantal Fürstner, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
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Publication number: 20120207769Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: April 26, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Patent number: 8242153Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: GrantFiled: September 14, 2009Date of Patent: August 14, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Publication number: 20120202852Abstract: The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: October 25, 2010Publication date: August 9, 2012Inventors: James Barrow, Kelly-Ann Schlegel, Yoheng Shu, Zhi-Qiang Yang
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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: 20120202856Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 2, 2012Publication date: August 9, 2012Inventors: Mark R. PLAYER, Raul CALVO, Jinsheng CHEN, Carl ILLIG, Sanath MEEGALLA, Daniel PARKS, William PARSONS
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Patent number: 8236836Abstract: The invention concerns a composition containing at least an oxazolin, optionally combined with at least a compound such as a metalloprotease inhibitor, a PKC inhibitor, an anti-inflammatory agent, a soothing agent, an immunosuppressor, an ion chelating agent, an alkanolamide, an oxazolidinone and a carbamic acid derivative. The invention also concerns the use of such a composition as medicine, in particular for preventing or treating skin pathologies of allergic and/or inflammatory and/or irritative origin or resulting from a danger signal. The invention further concerns a method for cosmetic treatment of sensitive, irritated, intolerant, allergy-prone, ageing skin and/or mucosa exhibiting skin barrier disorder, or exhibiting non-pathological immunologic imbalance, which consists in applying such composition on the skin and/or mucosa.Type: GrantFiled: December 27, 2002Date of Patent: August 7, 2012Assignee: Laboratoires ExpanscienceInventors: Philippe Msika, Nathalie Piccardi, Antoine Piccirilli
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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: 20120196824Abstract: The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.Type: ApplicationFiled: October 8, 2010Publication date: August 2, 2012Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Tomofumi Setsuta, Maki Seki, Hiroshi Iwasaki, Minoru Tanaka
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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: 20120196862Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Wael SAEB, Carine CHEVRIER
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Publication number: 20120195857Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 4, 2011Publication date: August 2, 2012Inventors: Makonen Belema, Pothukanuri Srinivasu, John A. Bender, Omar D. Lopez, Qi Chen, Richard A. Rampulla, Samayamunthula Venkata Satya Arun Kumar Gupta, Nicholas A. Meanwell
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Patent number: 8232302Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: October 27, 2010Date of Patent: July 31, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark Thomas Miller, Sara S. Hadida Ruah, Peter Diederik Jan Grootenhuis, Matthew Hamilton
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Publication number: 20120190700Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.Type: ApplicationFiled: January 17, 2012Publication date: July 26, 2012Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
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Publication number: 20120184436Abstract: A synergistic antimicrobial composition. The composition contains at least two components. The first component is ortho-phenylphenol or its alkali metal or ammonium salts. The second component is 4,4-dimethyloxazolidine (DMOZ).Type: ApplicationFiled: September 15, 2010Publication date: July 19, 2012Inventor: Bei Yin
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Publication number: 20120184518Abstract: Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.Type: ApplicationFiled: January 20, 2012Publication date: July 19, 2012Applicant: PROBIODRUG AGInventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
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Patent number: 8222277Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.Type: GrantFiled: December 28, 2010Date of Patent: July 17, 2012Assignee: NiCox S.A.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Patent number: 8222425Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: July 19, 2011Date of Patent: July 17, 2012Assignee: Novartis AGInventors: Shawn D. Britt, Lech Andrzej Ciszewski, Jiping Fu, Subramanian Karur, Yugang Liu, Peichao Lu, David Thomas Parker, Mahavir Prashad, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng
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Patent number: 8221737Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Patent number: 8222243Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: GrantFiled: August 26, 2008Date of Patent: July 17, 2012Assignee: Dart NeuroScience (Cayman) LtdInventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20120171133Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that modulate dynein expression in the skin. Also provided are methods for screening for substances which modulate dynein expression levels and the methods of using active agents identified by the screening protocol in the treatment of skin.Type: ApplicationFiled: November 29, 2011Publication date: July 5, 2012Applicant: AVON PRODUCTS, INC.Inventors: Qian ZHENG, John W. LYGA, Russell J. WYBORSKI
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Patent number: 8211932Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: September 10, 2010Date of Patent: July 3, 2012Assignee: Novartis AGInventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
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Publication number: 20120165276Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: May 6, 2008Publication date: June 28, 2012Applicant: Mpex Pharmaceuticals, Inc.Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
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Patent number: 8207183Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: GrantFiled: July 8, 2011Date of Patent: June 26, 2012Assignee: Novartis AGInventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanling Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
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Publication number: 20120157448Abstract: The invention provides novel tricyclic compounds of Formula I? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.Type: ApplicationFiled: November 22, 2011Publication date: June 21, 2012Inventors: Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Andrew T. Metcalf, Brad Newhouse, Tony P. Tang, Allen A. Thomas, Michael Siu, Malcolm Huestis, Matthew Volgraf
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Patent number: 8202999Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: January 6, 2006Date of Patent: June 19, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
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Patent number: 8202875Abstract: The present invention relates to the use of selective insecticidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one compound of the formula (I) in which CKE, W, X, Y and Z are as defined in the description, and (b) at least one crop plant compatibility-improving compound, from the group of compounds mentioned in the description, for controlling insects and/or arachnids, and to a method for controlling insects and/or arachnids using the compositions.Type: GrantFiled: July 18, 2005Date of Patent: June 19, 2012Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Udo Reckmann, Christopher Hugh Rosinger, Erich Sanwald, Christian Arnold
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Publication number: 20120142689Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Applicant: THERAVANCE, INC.Inventors: Eric L. STANGELAND, Lori Jean VAN ORDEN, Daisuke Roland SAITO
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Publication number: 20120142732Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 10, 2011Publication date: June 7, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Courtney A. Cullis, Krista E. Granger, Jianping Guo, Masaaki Hirose, Gang Li, Miho Mizutani, Tricia J. Vos
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Publication number: 20120141483Abstract: The present invention provides indane acetic acids and their derivatives and methods for the treatment and/or prevention of psoriasis and/or Alzheimer's diseases using the same.Type: ApplicationFiled: June 3, 2010Publication date: June 7, 2012Inventor: Mary Katherine Delmedico
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Publication number: 20120136027Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R* have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in the treatment or prophylaxis of HCV.Type: ApplicationFiled: August 6, 2010Publication date: May 31, 2012Inventors: David Mc Gowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8188127Abstract: Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one.Type: GrantFiled: July 8, 2008Date of Patent: May 29, 2012Assignee: Rohm and Haas CompanyInventors: Richard Levy, Beverly Jean El A'mma, Beat Heer, Kiran Pareek
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Patent number: 8188301Abstract: The present invention relates to the use of compounds which increase extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically to the use of 3-disubstituted phenyl-1-pyrrolidinols for the treatment of central nervous system disorders.Type: GrantFiled: June 4, 2008Date of Patent: May 29, 2012Assignee: NSAB, Filial af NeuroSearch Sweden AB, SverigeInventors: Clas Sonesson, Lars Swanson, Fredrik Pettersson, Nicholas Waters, Susanna Waters
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Publication number: 20120129861Abstract: A biocidal composition comprising 2,2-dibromomalonamide and an aldehyde-based biocidal compound, and its use for the control of microorganisms in aqueous and water-containing systems.Type: ApplicationFiled: September 27, 2010Publication date: May 24, 2012Inventors: Bei Yin, Freddie L. Singleton
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Publication number: 20120129830Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3, provided that m+n?7 and that o+p?7; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.Type: ApplicationFiled: May 11, 2010Publication date: May 24, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20120129886Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: November 10, 2011Publication date: May 24, 2012Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
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Publication number: 20120128657Abstract: Disclosed herein are macrocyclic compounds that are effective to inhibit cell migration. In one embodiment, the compounds have the structure: or any pharmaceutically acceptable salt or solvate thereof, wherein: m is 0 or 1; R1, R2 and R3 independently are H, aralkyl, acyl, lower alkyl or silyl; X is —C(O)N(R4)— or —C(S)N(R4)—; —C(O)—; —C(S)—; Y is —OC(O)—; —OC(O)N(R5)—; —N(R5)C(O)—; or —OC(O)O—; G comprises a saturated or unsaturated aliphatic chain having from 2 to about 10 atoms in the chain, the chain optionally including 1, 2, or 3 heteroatoms; the chain optionally being substituted with 1, 2 or 3 substituents independently selected from lower alkyl, —OR6, epoxy, aziridinyl, cyclopropyl, —NR7R8 and halo; R4, R5, R6, R7 and R8 independently are selected from H, lower alkyl and acyl. Also disclosed are methods for making and using compounds as well as pharmaceutical compositions including one or more of the disclosed macrocycles.Type: ApplicationFiled: February 7, 2008Publication date: May 24, 2012Inventors: Carole A. Bewley, Belhu B. Metaferia, Xin-Yu Huang
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Patent number: 8183383Abstract: PTP1B inhibitors with the following structure (formula I). Experiments indicate that these inhibitors can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B). They can be used as insulin sensitisers. They can be used to prevent, delay or treat diseases which are related to insulin antagonism mediated by PTP1B, especially diabetes type II and obesity. The invention also provides methods for preparing these inhibitors.Type: GrantFiled: February 26, 2008Date of Patent: May 22, 2012Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jia Li, Yi Wei, Wei Zhang, Jingya Li, Lei Shi