Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/260.1)
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Patent number: 8541421Abstract: The present invention provides, in part, substituted thieno[2,3-d]pyrimidines and methods of contacting compositions with such compounds to enhance the sweet taste of said compositions.Type: GrantFiled: March 18, 2011Date of Patent: September 24, 2013Assignee: Senomyx Inc.Inventors: Catherine Tachdjian, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
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Patent number: 8530652Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.Type: GrantFiled: October 6, 2011Date of Patent: September 10, 2013Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.Inventors: Junhu Zhang, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
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Patent number: 8530483Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.Type: GrantFiled: May 28, 2009Date of Patent: September 10, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg, Eric Hostetler
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Patent number: 8524719Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: GrantFiled: August 21, 2012Date of Patent: September 3, 2013Assignee: The Trustees of the University of PennsylvaniaInventor: Robert P. Ricciardi
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Patent number: 8524712Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: GrantFiled: March 24, 2008Date of Patent: September 3, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Chi-Wan Lee, Teresa Przewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20130225609Abstract: The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.Type: ApplicationFiled: April 1, 2011Publication date: August 29, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Peter Nickolaus
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Patent number: 8507502Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: November 9, 2009Date of Patent: August 13, 2013Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
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Patent number: 8507503Abstract: The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: GrantFiled: March 23, 2010Date of Patent: August 13, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: Sukeerthi Kumar, Abraham Thomas, Nayan Taterao Waghmare, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
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Patent number: 8507491Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: GrantFiled: August 24, 2009Date of Patent: August 13, 2013Assignee: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Patent number: 8501750Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.Type: GrantFiled: May 20, 2008Date of Patent: August 6, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
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Publication number: 20130196988Abstract: The present invention relates to dihydrothienopyrimidines, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.Type: ApplicationFiled: July 27, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kia GERLACH, Niklas HEINE, Scott HOBSON, Christoph HOENKE, Alexander WEBER
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Publication number: 20130190297Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.Type: ApplicationFiled: May 20, 2011Publication date: July 25, 2013Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&DInventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
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Publication number: 20130183269Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: January 7, 2013Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8486952Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: July 28, 2010Date of Patent: July 16, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Patent number: 8486953Abstract: The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: GrantFiled: August 24, 2009Date of Patent: July 16, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Austen, Phillip Black, Wesley Blackaby, John Danilewicz, Ian Linney, Kay Schreiter, Martin Schneider
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Publication number: 20130178460Abstract: The present invention relates to the use of novel compounds of Formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: January 10, 2013Publication date: July 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130178462Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: March 5, 2013Publication date: July 11, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8470850Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: GrantFiled: May 6, 2010Date of Patent: June 25, 2013Assignee: MethylGene Inc.Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
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Publication number: 20130158051Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2, R3, R4, X and Y are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.Type: ApplicationFiled: January 12, 2011Publication date: June 20, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
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Patent number: 8466163Abstract: The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.Type: GrantFiled: December 11, 2007Date of Patent: June 18, 2013Assignee: Bionomics LimitedInventors: Bernard Luke Flynn, Jason Hugh Chaplin, Dharam Paul, Damian Wojciech Grobelny, Brian Kelly
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Publication number: 20130137685Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2 and R3 are defined as stated in the claims. The compounds of formula (I) are suitable, for example, for wound healing.Type: ApplicationFiled: January 12, 2011Publication date: May 30, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
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Patent number: 8445491Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: GrantFiled: May 27, 2009Date of Patent: May 21, 2013Assignee: The Board of Regents of the University of Texas SystemInventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
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Publication number: 20130123241Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: ApplicationFiled: May 10, 2011Publication date: May 16, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Publication number: 20130123279Abstract: Crystals are obtained by heating an aqueous suspension of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid. Novel crystals are obtained by adjusting the heating temperature and/or duration.Type: ApplicationFiled: May 31, 2011Publication date: May 16, 2013Applicant: ASKA PHARMACEUTICAL CO., LTD.Inventors: Hiroyuki Hayashi, Takayoshi Nakagawa, Koichi Miyazaki
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Publication number: 20130123231Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.Type: ApplicationFiled: November 9, 2012Publication date: May 16, 2013Applicant: Nimbus Apollo, Inc.Inventor: Nimbus Apollo, Inc.
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Patent number: 8440654Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: May 14, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20130109698Abstract: The present invention includes a method of inhibiting, suppressing or preventing retroviral infection in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds of the invention.Type: ApplicationFiled: April 25, 2011Publication date: May 2, 2013Inventor: Simon Cocklin
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Publication number: 20130102621Abstract: The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic ? cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and the compound represented by the following formula (1): wherein one of A and B represents a nitrogen atom and the other represents a nitrogen atom or CR10, X represents an oxygen atom, a sulfur atom or —(CH2)n-N(R12)—, Y represents an oxygen atom, a sulfur atom or —N(R13)—, and R1 to R9 each represent a hydrogen atom or another substituent, or a salt thereof, or a solvate of the compound or the salt.Type: ApplicationFiled: June 24, 2011Publication date: April 25, 2013Applicant: KOWA CO., LTD.Inventors: Toshiharu Morimoto, Tomoaki Koshizawa, Gen Watanabe, Tadaaki Ohgiya, Nao Yamasaki, Noriyuki Inoue
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Publication number: 20130102600Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Publication number: 20130102595Abstract: The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.Type: ApplicationFiled: October 15, 2012Publication date: April 25, 2013Inventor: Curis, Inc.
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Publication number: 20130102601Abstract: The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Patent number: 8426427Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA is halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; ring B is aryl or heteroaryl; RB is halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl, etc.; E1 and E2 are oxygen atom, etc.; Q is hydrogen atom, alkyl, alkylsulfonyl, acyl, etc.; X is -(alkylene)-Z, —CO—Y, —SO2—Y, etc. (in which Y is Z or amino, etc.; Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: GrantFiled: April 16, 2008Date of Patent: April 23, 2013Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kohsuke Ohno, Noboru Kamada
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Publication number: 20130096141Abstract: Compounds of structural formula I: are GPR119 agonists and are useful for the treatment, control or prevention of disorders responsive to agonism of GPR119, such as metabolic-related disorders such as type I diabetes, type II diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia or syndrome X. The compounds are also reported as being useful for controlling weight gain, controlling food intake, and inducing satiety in mammals.Type: ApplicationFiled: June 14, 2011Publication date: April 18, 2013Inventors: Bernard R. Neustadt, Hong Liu
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Publication number: 20130090336Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: December 5, 2012Publication date: April 11, 2013Applicant: YM BIOSCIENCES AUSTRALIA PTY LTDInventor: YM Biosciences Australia Pty Ltd
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N3-HETEROARYL SUBSTITUTED TRIAZOLES AND N5-HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20130090330Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: October 4, 2012Publication date: April 11, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC. -
Publication number: 20130079359Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.Type: ApplicationFiled: August 23, 2012Publication date: March 28, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pascale A.J. POUZET, Peter NICKOLAUS, Ulrike WERTHMANN, Rogelio Perez FRUTOS, Bing-Shiou YANG, Soojin KIM, Jason Alan MULDER, Nitinchandra D. PATEL, Chris Hugh SENANAYAKE, Thomas Gabriel TAMPONE, Xudong WEI
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Publication number: 20130079357Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2, R3, R4 and X are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.Type: ApplicationFiled: January 12, 2011Publication date: March 28, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
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Publication number: 20130079358Abstract: The present invention relates to oxazolopyrimidine compounds of the formula I, in which A, R1, R2, R3 and X are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 12, 2011Publication date: March 28, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Katrin Hiss
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Publication number: 20130072502Abstract: Heterocyclic carboxylic acid derivatives comprising a 2,5-substituted oxazolopyrimidine ring as Edg-1 receptor agonists The present invention relates to oxazolopyrimidine compounds of the formula I, in which A, R1, R2, R3, X and Y are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 12, 2011Publication date: March 21, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Katrin Hiss
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Publication number: 20130072482Abstract: The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.Type: ApplicationFiled: May 26, 2011Publication date: March 21, 2013Inventors: Beom-Seok Yang, Yong-Zu Kim, Tae-Kyo Park, Sung-Ho Woo, Hyang-Sook Lee, Sun-Young Kim, Jong-Un Cho, Hong-Bum Lee
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Publication number: 20130072501Abstract: The invention relates to oxazolopyrimidine compounds of formula I, where A, R1 and R2 are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.Type: ApplicationFiled: January 14, 2011Publication date: March 21, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Katrin Hiss
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
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Publication number: 20130065914Abstract: The present invention relates to novel thienopyhmidine compounds of general formula (I), pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: ApplicationFiled: February 25, 2011Publication date: March 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Armin Heckel, Frank Himmelsbach, Thorsten Lehmann-Lintz, Norbert Redemann, Achim Sauer, Leo Thomas, Phillip Black, Wesley Blackaby, John Danilewicz, Ian Linney, Matthias Austen, Martin Schneider, Kay Schreiter
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Publication number: 20130058980Abstract: Compounds that modulate, for example, that inhibit, syk kinase, and, optionally other kinases. The compounds can be used to treat a variety of disorders, including inflammatory disorders and autoimmune disorders.Type: ApplicationFiled: November 2, 2010Publication date: March 7, 2013Inventors: Ketan Desai, Renee Desai
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Publication number: 20130059867Abstract: An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 342-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.Type: ApplicationFiled: February 9, 2011Publication date: March 7, 2013Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Kazumichi Jo, Hideki Takeuchi
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Publication number: 20130059866Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.Type: ApplicationFiled: February 23, 2012Publication date: March 7, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Horst Dollinger, Rogelio Perez Frutos, Soojin Kim, Jason Alan Mulder, Peter Nickolaus, Nitinchandra D. Patel, Pascale Pouzet, Chris Hugh Senanayake, Thomas Gabriel Tampone, Xudong Wei, Ulrike Werthmann, Bing-Shiou Yang
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Publication number: 20130053370Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.Type: ApplicationFiled: January 31, 2011Publication date: February 28, 2013Applicants: HANMI SCIENCE CO., LTD., CATHOLIC UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Jung Beom Son, Seung Hyun Jung, Wha ll Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
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Patent number: 8377944Abstract: This invention provides thienopyrimidine derivatives of the formula, wherein R1 stands for hydrogen atom, an alkyl group or the like; R2 stands for a hydrogen atom, an alkyl or amino group or the like, R3 stands for an alkyl, alkenyl or alkylthio group or the like or a group Y—X—; or R2 and R3 may together form tetramethylene group; X standing for a direct bond or linking group such as CH2, CH(OH), S, O, NH; Y standing for a substituted or unsubstituted aromatic carbocyclic, aromatic heterocylic, cycloalkyl or saturated heterocyclic group or the like; Z stands for S or O, and n is 0 or an integer of 1 to 4, or salts thereof, which exhibit an inhibitory effect on PDE9, and are therefore useful for prevention or treatment of overactive bladder syndrome, pollakiuria, urinary incontinence, dysuria associated with prostatic hyperplasia, urolithiasis, Alzheimer's disease, chronic obstructive pulmonary disease, myocardial infarction, thrombosis, diabetes and the like.Type: GrantFiled: August 14, 2012Date of Patent: February 19, 2013Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Kotaro Gotanda, Atsushi Shinbo, Youichi Nakano, Hideo Kobayashi, Makoto Okada, Akira Asagarasu
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Publication number: 20130040957Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof, and their uses in the treatment, prevention and modulation of various diseases including chronic liver diseases, liver cirrhosis, liver fibrosis, hepatocellular carcinoma, liver cancer, renal cell carcinoma, kidney cancer, colorectal cancer, brain cancer, breast cancer, blood cancer, lung cancer, thyroid cancer, ovarian cancer, pancreas cancer, prostate cancer, stomach cancer, testicular cancer, uterus cancer, intestinal cancer, skin cancer, and other forms of cancer, carcinoid tumors, teratocarcinoma, tumor progression, metastasis and fibrosis in the neuroendocrine neoplasia, fibrotic processes as well as a disease state modulated directly or indirectly with 5-HT receptors, 5-HT1, 5-HT1A, 5-HT2 receptors, 5-HT2A and 5-HT2B receptors, dopamine receptors and multiple kinase pathways.Type: ApplicationFiled: October 12, 2012Publication date: February 14, 2013Inventor: Daljit Singh Dhanoa
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Publication number: 20130035347Abstract: The present invention relates to novel aromatic bicyclic derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the CXCR4 receptor.Type: ApplicationFiled: August 2, 2012Publication date: February 7, 2013Inventors: Vidyasagar Vuligonda, Richard L. Beard, Thong Vu, John E. Donello, Gerard Rodrigues, Veena Viswanath, Michael E. Garst