Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/316)
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Publication number: 20120148690Abstract: A novel skin barrier function recovery acceleration method and accelerator are provided. The present invention provides a skin barrier function recovery accelerator that comprises a TRPA1 agonist capable of activating TRPA1 in epidermal cells.Type: ApplicationFiled: December 10, 2010Publication date: June 14, 2012Inventors: Mitsuhiro Denda, Moe Tsutsumi, Sumiko Denda
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Patent number: 8198273Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.Type: GrantFiled: May 4, 2010Date of Patent: June 12, 2012Assignee: Plexxikon Inc.Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
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Patent number: 8198267Abstract: The invention relates to novel substituted oxazolidinones, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.Type: GrantFiled: June 13, 2008Date of Patent: June 12, 2012Assignee: Bayer Intellectual Property GmbHInventors: Swen Allerheiligen, Marcus Bauser, Hartmut Schirok, Michael Härter, Stephan Siegel, Ulrich Rester, Christoph Gerdes, Stefan Heitmeier, Georges Von Degenfeld, Anja Buchmüller, Elke Dittrich-Wengenroth, Uwe Saatman, Julia Strassburger, Mark Jean Gnoth, Dieter Lang
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Publication number: 20120135977Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.Type: ApplicationFiled: September 28, 2011Publication date: May 31, 2012Inventors: Douglas C. Beshore, Vadim Dudkin, Robert M. Garbaccio, Adam W. Johnson, Scott D. Kuduk, Jason W. Skudlarek, Cheng Wang, Mark E. Fraley
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Publication number: 20120130058Abstract: Method of synthesizing a compound of formula (I), wherein R1, R2 are, independently, chloro or fluoro, and wherein R3 is H, alkyl, aralkyl or is an alkylether or alkylthioether comprising the steps of firstly reducing a diazeny compound of formula (II) non-catalytically or with a catalytic amount of an homogenous organic, non-metal catalyst to the corresponding hydrazo compound of formula (III) and in a second step catalytically hydrogenating said hydrazo compound in with a heterogeneous Ni-catalyst to the compound of formula (I).Type: ApplicationFiled: January 5, 2012Publication date: May 24, 2012Inventors: Wilhelm Quittmann, Wei Zhu, Feng Ye, Rongmin Chen
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Publication number: 20120122891Abstract: 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 R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Richard Lowe, Willy Moree, Nicole Smith, Warren Wade, Liren Zhao, Yun-Fei Zhu, Martin Rowbottom, Neil Ashweek
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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: 20120122860Abstract: Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer.Type: ApplicationFiled: May 4, 2010Publication date: May 17, 2012Inventors: Gary Conard Visor, Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Guoxian Wu
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Patent number: 8178540Abstract: The present invention relates to novel pyrimidylmethyl-sulfonamide compounds and to their N-oxides, their agriculturally acceptable salts and their veterinarily acceptable salts and also to agricultural compositions comprising at least one such compound as active component, and also to their use for controlling harmful fungi. The present invention also relates to a method for controlling arthropod pests.Type: GrantFiled: November 21, 2007Date of Patent: May 15, 2012Assignee: BASF SEInventors: Jan Klaas Lohmann, Wassilios Grammenos, Michael Puhl, Jochen Dietz, Bernd Müller, Joachim Rheinheimer, Jens Renner, Marianna Vrettou, Sarah Ulmschneider, Thomas Grote
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Publication number: 20120115894Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: February 22, 2010Publication date: May 10, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Ping Liu, Robert J. DeVita, Linus S. Lin, Marc D. Chioda, Terence G Hamill, Wenping Li
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Publication number: 20120108576Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: November 30, 2011Publication date: May 3, 2012Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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Publication number: 20120108616Abstract: The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors.Type: ApplicationFiled: January 5, 2012Publication date: May 3, 2012Inventors: David Grierson, Abdellah Benjahad, Alain Moussy, Martine Croisy
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Publication number: 20120108529Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.Type: ApplicationFiled: May 14, 2010Publication date: May 3, 2012Inventors: Robert R. Webb, II, Mitchell W. Mutz, Kenneth J. Barr
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Publication number: 20120101274Abstract: The present invention is directed to a process for preparing [1S-[1?,2?,3?(1S*,2R*),5?]]-3-[7-[2-(3,4-difluorophenyl)-cyclopropylamino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol and to intermediates useful in the process.Type: ApplicationFiled: September 8, 2009Publication date: April 26, 2012Applicant: ASTRAZENECA ABInventors: Martin Hans Bohlin, Helena Hellström, Peter W. Johansson, Ulf G. Larsson, Mikaela Recknagel, Rhony Aufdenblatten, Andreas Weiss, Ursula Weiss
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Publication number: 20120101078Abstract: Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.Type: ApplicationFiled: March 19, 2010Publication date: April 26, 2012Applicant: H. Lundbrck A/SInventors: Bin Chen, James Ford Burns, Dario Doller
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Publication number: 20120094968Abstract: The present application relates to novel sulfonamidw- or sulfoximine-substituted 1,4-diaryldihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: March 30, 2010Publication date: April 19, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Dirk Schneider
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Patent number: 8158787Abstract: A process for producing a trichloropyrimidine compound represented by the formula (2): wherein R represents a hydrogen atom etc., comprising reacting a dihydroxypyrimidine compound represented by the formula (1): wherein R represents the same meaning as above, with sulfuryl chloride and at least one chlorinating agent selected from the group consisting of hydrogen chloride, thionyl chloride, phosgene, phosphorus oxychloride, phosphorus pentachloride and phosphorus trichloride in the presence of an organic base.Type: GrantFiled: March 26, 2008Date of Patent: April 17, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Koichi Nakazawa, Tomonori Yoshiyama, Kouji Yoshikawa
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Patent number: 8153644Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 1, 2008Date of Patent: April 10, 2012Assignee: Madrigal Pharmaceuticals, Inc.Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Aopstle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
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Publication number: 20120083490Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Applicant: ABBOTT LABORATORIESInventors: Larry L. Klein, Hui-Ju Chen, Ming C. Yeung, Charles A. Flentge, John T. Randolph, Peggy P. Huang, Douglas K. Hutchinson, Dale J. Kempf
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Publication number: 20120083474Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: June 4, 2010Publication date: April 5, 2012Inventors: Didier Jean-Claude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Wei Xiao, Bryan Branstetter, Guy J. Breitenbucher
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Patent number: 8148380Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: GrantFiled: July 23, 2008Date of Patent: April 3, 2012Assignee: Crestone, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20120053180Abstract: This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.Type: ApplicationFiled: March 17, 2011Publication date: March 1, 2012Applicant: CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.Inventors: Sang Uk Kang, Min Jeong Kim, Byung Nam Kang, Wei Tan, Albert Charles Gyorkos, Suk Young Cho
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Publication number: 20120053150Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.Type: ApplicationFiled: April 22, 2010Publication date: March 1, 2012Inventors: David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
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Publication number: 20120053346Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: August 30, 2011Publication date: March 1, 2012Inventor: Hubert Maehr
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Patent number: 8124628Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: April 6, 2007Date of Patent: February 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Patent number: 8119635Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: August 19, 2009Date of Patent: February 21, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120040991Abstract: Disclosed are 3-azabicyclo[4.1.0]heptane derivatives of formula (I) and their use as orexin receptor antagonists.Type: ApplicationFiled: April 23, 2010Publication date: February 16, 2012Applicant: Glaxo Group LimitedInventors: David Amantini, Romano Di Fabio, Massimo Gianotti, Francesca Pavone, Francesco Ferroni
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Publication number: 20120041009Abstract: A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent.Type: ApplicationFiled: March 11, 2010Publication date: February 16, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Hajime Mizuno
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Patent number: 8114996Abstract: Method of synthesizing a compound of formula (I), wherein R1, R2 are, independently, chloro or fluoro, and wherein R3 is H, alkyl, aralkyl or is an alkylether or alkylthioether comprising the steps of firstly reducing a diazeny compound of formula (II) non-catalytically or with a catalytic amount of an homogenous organic, non-metal catalyst to the corresponding hydrazo compound of formula (III) and in a second step catalytically hydrogenating said hydrazo compound in with a heterogeneous Ni-catalyst to the compound of formula (I).Type: GrantFiled: September 28, 2010Date of Patent: February 14, 2012Assignee: Lonza AGInventors: Wilhelm Quittmann, Wei Zhu, Feng Ye, Rongmin Chen
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Publication number: 20120035171Abstract: The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: April 15, 2010Publication date: February 9, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gordon Saxty, Valerio Berdini, Eddy Jean Edgard Freyne, Alexandra Papanikos, Pascal Benderitter, Werner Constant Johan Embrechts, Berthold Wroblowski, Rhalid Akkari
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Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
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Publication number: 20120028920Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20120022074Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: ApplicationFiled: October 4, 2011Publication date: January 26, 2012Inventors: Dominik FEUERBACH, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
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Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Patent number: 8101625Abstract: A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.Type: GrantFiled: October 23, 2006Date of Patent: January 24, 2012Assignee: Exelixis, Inc.Inventors: Kenneth D. Rice, Neel Kumar Anand, Arlyn Arcalas, Charles M. Blazey, Joerg Bussenius, Wai Ki Vicky Chan, Hongwang Du, Sergey Epshteyn, Mohamed Abdulkader Ibrahim, Patrick Kearney, Abigail R. Kennedy, Moon Hwan Kim, Jean-Claire Limun Manalo, Csaba J. Peto, Tsze H. Tsang, Amy Lew Tsuhako, Peiwen Zhou, Elena S. Koltun
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Publication number: 20120015966Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
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Publication number: 20120010192Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Publication number: 20120004243Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: April 5, 2011Publication date: January 5, 2012Applicant: AstraZeneca ABInventors: Dearg Sutherland Brown, John Graham Cumming, Ian Alun Nash
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Publication number: 20110319438Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: September 7, 2011Publication date: December 29, 2011Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
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Publication number: 20110312976Abstract: The present invention relates to a compound represented by formula (I): (wherein R, R2, R3 and R4 each independently represent a hydrogen or halogen atom; R5 and R6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 9, 2010Publication date: December 22, 2011Applicant: MSD K.K.Inventors: Keisuke Arakawa, Teruyuki Nishimura, Yuichi Sugimoto, Hiroyuki Takahashi, Tadashi Shimamura
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Publication number: 20110306624Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: February 3, 2010Publication date: December 15, 2011Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20110301347Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: August 15, 2011Publication date: December 8, 2011Inventors: Markus BERGER, Jan Dahmen, Hartmut Rehwinkel, Stefan Jaroch, Heike Schäcke
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Publication number: 20110301160Abstract: In general, the present invention relates to compounds capable of inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.Type: ApplicationFiled: December 3, 2010Publication date: December 8, 2011Applicant: ARQULE, INC.Inventors: Mark A. ASHWELL, Syed ALI, Jifeng LIU, Yanbin LIU, Peter LOHSE, Belew MEKONNEN, Robert SELLIAH, Manish TANDON, Woj WRONA, Valery ANTONENKO
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Publication number: 20110294839Abstract: The present invention provides a novel cyclohexane solvate form of lopinavir, and a process for its preparation thereof. The present invention also provides a novel desolvated crystalline form of lopinavir, process for its preparation and to pharmaceutical composition containing it. Thus, for example, lopinavir cyclohexane solvate was heated at 100° C. for 10 hours to give lopinavir desolvated crystalline form H1.Type: ApplicationFiled: February 6, 2009Publication date: December 1, 2011Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Publication number: 20110294809Abstract: The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11?-hydroxysteroid dehydrogenose type 1 (11?HSD1).Type: ApplicationFiled: October 27, 2009Publication date: December 1, 2011Applicant: SANOFI-AVENTISInventors: Alain Jean Braun, Olivier Crespin, Eric Nicolai, Cecile Pascal, Olivier Venier
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Publication number: 20110288054Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: Schering CorporationInventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K.C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Patent number: 8058433Abstract: New crystalline forms of lopinavir are disclosed.Type: GrantFiled: October 2, 2006Date of Patent: November 15, 2011Assignee: Abbott LaboratoriesInventors: Daniel A. Dickman, Sanjay Chemburkar, James J. Fort, Rodger F. Henry, David Lechuga-Ballesteros, Yuping Niu, William Porter
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Publication number: 20110275812Abstract: In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof. The compound, 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile “ETHER” of formula (A) wherein n is either 0 or 1 and HA is an acid.Type: ApplicationFiled: July 27, 2010Publication date: November 10, 2011Inventors: Irena Krizmanic, Jasna Dogan, Marina Marinkovic, Maja Sepelj
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Publication number: 20110269960Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Naoya ONO, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato