Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/298)
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Publication number: 20140057926Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
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Publication number: 20140058104Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.Type: ApplicationFiled: October 29, 2013Publication date: February 27, 2014Applicant: ZERIA PHARMACEUTICAL CO., LTD.Inventors: Masaaki NAGASAWA, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
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Publication number: 20140051697Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.Type: ApplicationFiled: October 23, 2013Publication date: February 20, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Helen Anderson
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Patent number: 8648099Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: GrantFiled: September 11, 2012Date of Patent: February 11, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
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Publication number: 20140031370Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Patent number: 8637553Abstract: A compound of Formula (I): salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by raf, VEGFR, PDGFR, p38 and flt-3.Type: GrantFiled: July 22, 2004Date of Patent: January 28, 2014Assignee: Bayer Healthcare LLCInventors: Stephen Boyer, Jacques Dumas, Bernd Riedl, Scott Wilhelm
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Publication number: 20140024639Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.Type: ApplicationFiled: July 19, 2013Publication date: January 23, 2014Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
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Patent number: 8629166Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: GrantFiled: September 11, 2012Date of Patent: January 14, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Uwe Grether, Stephan Roever
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Patent number: 8618306Abstract: Disclosed are an intermediate compound of N-(1,1,1-trideuterated methyl)phthalimide, and its use in the preparation of deuterated diphenylurea derivative.Type: GrantFiled: March 17, 2011Date of Patent: December 31, 2013Assignee: Suzhou Zelgen Biopharmaceutical Co., Ltd.Inventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
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Patent number: 8598210Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: November 20, 2012Date of Patent: December 3, 2013Assignee: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
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Publication number: 20130317000Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: ApplicationFiled: May 21, 2013Publication date: November 28, 2013Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INCInventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
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Publication number: 20130296380Abstract: A compound of Formula (I), salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by multiple kinases, such as raf, VEGFR, PDGFR, FLT-3, and c-Kit.Type: ApplicationFiled: January 5, 2012Publication date: November 7, 2013Applicant: Beta Pharma Canada Inc.Inventors: Zhaoyin Wang, Chunrong Yu
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Publication number: 20130274478Abstract: The present invention provides amorphous and crystalline forms of acid addition salts of sorafenib, pharmaceutical compositions comprising them, and their use for the treatment of cancer. The present invention also provides processes for the preparation of acid addition salts of sorafenib.Type: ApplicationFiled: June 7, 2013Publication date: October 17, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Jagdev Singh JARYAL, Swargam SATHYANARAYANA, Rajesh Kumar THAPER, Mohan PRASAD
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Publication number: 20130267699Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.Type: ApplicationFiled: March 12, 2013Publication date: October 10, 2013Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
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Publication number: 20130245076Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: April 9, 2013Publication date: September 19, 2013Applicants: Akebia Therapeutics Inc., Aerpio Therapeutics Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Publication number: 20130203816Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: November 20, 2012Publication date: August 8, 2013Applicant: Akebia Therapeutics Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
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Publication number: 20130203757Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: November 16, 2012Publication date: August 8, 2013Applicants: THE GENERAL HOSPITAL CORPORATION, CANTHERA THERAPEUTICS INC.Inventors: Canthera Therapeutics Inc., The General Hospital Corporation
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Publication number: 20130158076Abstract: The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: MERCK PATENT GMBHInventor: Merck Patent GmbH
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Patent number: 8455654Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 18, 2011Date of Patent: June 4, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Patent number: 8450347Abstract: The invention relates to a method of controlling feelings of pain in infants or diseased or elderly persons using a complete nutrition or a nutritional supplement. The method comprises administering increased levels of folic acid, vitamin B6 and vitamin B12 or their functional equivalents.Type: GrantFiled: February 19, 2008Date of Patent: May 28, 2013Assignee: N.V. NutriciaInventors: Robert Johan Joseph Hageman, Jacob Geert Bindels
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Publication number: 20130131122Abstract: A compound of Formula (I): salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by raf, VEGFR, PDGFR, p38 and flt-3.Type: ApplicationFiled: November 5, 2012Publication date: May 23, 2013Applicant: BAYER HEALTHCARE LLCInventor: Bayer Healthcare LLC
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Patent number: 8445687Abstract: There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A) wherein R? is selected from the group consisting of hydrogen, —C(O)OA, —C(O)CX3, —C(O)NH2, —C(O)—NHOH or There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2-trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.Type: GrantFiled: September 10, 2008Date of Patent: May 21, 2013Assignee: Cipla LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ghagare, Sandip Chikhalikar
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Patent number: 8431710Abstract: A process for the manufacture of a cyclic compound of formula (I) which comprises (a) adding an acid halide of formula R1—C(O)—X, to a vinyl ether of formula (II): CH2?CH—OR2, to produce an addition product, and (b) reacting the addition product with a compound of formula (III): Y-A-Z; wherein R1 is a halogenated alkyl group; wherein X is fluorine, chlorine, or bromine; wherein R2 is an alkyl group, an aralkyl group, or an aryl group; wherein Z and Y designate independently carbon or a heteroatom; and wherein A is a linking group between Z and Y comprising 0, 1, 2 or 3 atoms in the cycle.Type: GrantFiled: September 25, 2009Date of Patent: April 30, 2013Assignee: Solvay SAInventor: Max Braun
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Patent number: 8410082Abstract: This invention relates to novel diaryl urea compounds, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of multiple kinases.Type: GrantFiled: May 20, 2010Date of Patent: April 2, 2013Assignee: Concert Pharmaceuticals, Inc.Inventors: Julie F. Liu, Roger D. Tung, Scott L. Harbeson
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Publication number: 20130065876Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
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Publication number: 20130060043Abstract: A fluoro-substituted deuterated diphenylurea compound, especially 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-2-(N-(methyl-d3))picolinamide, preparing method and use for treating or preventing tumor and relative diseases thereof.Type: ApplicationFiled: March 17, 2011Publication date: March 7, 2013Applicant: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTDInventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
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Publication number: 20130060044Abstract: Disclosed are an intermediate compound of N-(1,1,1-trideuterated methyl)phthalimide, and its use in the preparation of deuterated diphenylurea derivative.Type: ApplicationFiled: March 17, 2011Publication date: March 7, 2013Applicant: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.Inventors: Weidong Feng, Xiaoyong Gao, Xiaojun Dai
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Publication number: 20130053565Abstract: Described herein are methods for synthesizing substituted 3-piperidone compounds. Notably, substituted 3-piperidones can also be prepared in enantiopure form. The methods may allow for preparation of highly substituted piperidine cores. Also disclosed are 3-piperidone compounds and pharmaceutical compositions comprising the compounds.Type: ApplicationFiled: August 29, 2012Publication date: February 28, 2013Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATIONInventors: Janis Louie, Puneet Kumar
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Publication number: 20130040997Abstract: Provided are a novel pyridine carboxylic acid based compound used as a P2X1 and P2X3 receptor antagonist, a production method for the same and a composition comprising the same. The compound according to the present invention is a powerful antagonist of P2X1 and P2X3 receptors, and hence can be used as a drug for treating or preventing diseases involving neurological pain or chronic inflammatory diseases which are diseases caused by P2X1 and P2X3 receptor activity.Type: ApplicationFiled: December 20, 2010Publication date: February 14, 2013Applicant: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Yong-Chul Kim, Kwan-Young Jung, Joong Heui Cho
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Patent number: 8367666Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.Type: GrantFiled: February 28, 2012Date of Patent: February 5, 2013Assignee: Shionogi & Co., Ltd.Inventors: Takashi Sasatani, Yoshiharu Hiramatsu, Susumu Mitsumori
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Patent number: 8349832Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: GrantFiled: September 2, 2010Date of Patent: January 8, 2013Assignees: Canthera Therapeutics, The Massachusetts General Hospital CorporationInventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova
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Patent number: 8334307Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.Type: GrantFiled: October 7, 2011Date of Patent: December 18, 2012Assignee: Biotheryx Inc.Inventors: Frank Mercurio, Kyle W. H. Chan
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Publication number: 20120309977Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]aminolacetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.Type: ApplicationFiled: June 5, 2012Publication date: December 6, 2012Applicant: Akebia Therapeutics Inc.Inventors: Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
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Patent number: 8323671Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: August 20, 2010Date of Patent: December 4, 2012Assignee: Akebia Therapeutics Inc.Inventors: Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Richard Masaru Kawamoto
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Publication number: 20120302519Abstract: Disclosed herein are substituted fluoromethanes; pharmaceutical compositions comprising a therapeutically effective amount of the same; processes for preparing these fluoromethanes; and methods of using the same in alleviating infection and parasitism. Also disclosed are methods for identifying substituted fluoromethanes for modulating the activity of receptors and enzymes that bind and/or modify phosphate containing ligands and substrates.Type: ApplicationFiled: February 3, 2011Publication date: November 29, 2012Applicant: MEH ASSOCIATES, INC.Inventor: Mark E. Hediger
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Publication number: 20120258924Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.Type: ApplicationFiled: June 20, 2012Publication date: October 11, 2012Applicant: INTERMUNE, INC.Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
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Patent number: 8283366Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection, acquired immune deficiency syndrome (AIDS), AIDS-related complex (ARC), hepatitis C, and other diseases and conditions caused or mediated by HIV infection.Type: GrantFiled: January 11, 2011Date of Patent: October 9, 2012Assignee: Ambrilia Biopharma, Inc.Inventors: Brent Richard Stranix, Guy Milot, Jean-Emmanuel Bouchard
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Patent number: 8278336Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: GrantFiled: November 21, 2008Date of Patent: October 2, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Patent number: 8273774Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: GrantFiled: May 26, 2009Date of Patent: September 25, 2012Assignee: AstraZeneca ABInventors: Glen Andrews, Rhona Jane Cox, Christopher De Savi, Premji Meghani, Hitesh Jayantilal Sanganee, Daniel Jon Warner
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Publication number: 20120237474Abstract: This invention relates to novel diaryl urea compounds, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an inhibitor of multiple kinases.Type: ApplicationFiled: May 20, 2010Publication date: September 20, 2012Applicant: CONCERT PHARMACEUTICALS INC.Inventors: Julie F. Liu, Roger D. Tung, Scott L. Harbeson
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Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20120232277Abstract: The present invention discloses processes for the preparation and isolation of [1,2,4]oxadiazo-3-yl derivatives of carboxylic acids. The derivatives are useful in the treatment of inflammatory diseases and conditions.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Applicant: ABBOTT LABORATORIESInventors: Kirill A. Lukin, Vimal Kishore, Thomas D. Gordon
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Publication number: 20120225891Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: March 22, 2012Publication date: September 6, 2012Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Publication number: 20120213758Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: DeCODE Genetics enfInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO, Timothy HAGEN
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Patent number: 8236798Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: April 27, 2010Date of Patent: August 7, 2012Assignees: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20120190699Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: December 14, 2011Publication date: July 26, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Steven Durrant, Sharn Ramaya, Juan-Miguel Jimenez, Alistair Rutherford
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Patent number: 8227491Abstract: The present invention relates to a compound of formula I, in all its isomeric forms and pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: GrantFiled: September 3, 2010Date of Patent: July 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Stephan Roever, Matthew Wright
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Patent number: 8217061Abstract: Provided are sorafenib hemi-tosylate, polymorphs thereof, polymorphs of sorafenib tosylate, preparation thereof and pharmaceutical compositions thereof.Type: GrantFiled: January 19, 2009Date of Patent: July 10, 2012Assignee: Sicor Inc.Inventors: Ale{hacek over (s)} Gavenda, Alexandr Jegorov, Pierluigi Rossetto, Peter Lindsay MacDonald, Augusto Canavesi
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Publication number: 20120157455Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: June 17, 2011Publication date: June 21, 2012Applicant: CANTHERA THERAPEUTICS, INC.Inventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova, Sam Lee