Polycyclo Ring System Having The 1,2-diazole Ring As One Of The Cyclos Patents (Class 546/275.7)
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Publication number: 20120270905Abstract: The present invention relates to novel fluorinated 2,6-dialkyl-3,5-dicyano-4-(1H-indazol-5-yl)-1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: ApplicationFiled: October 1, 2010Publication date: October 25, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Mario Lobell, Karen Engel
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Patent number: 8293738Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.Type: GrantFiled: May 12, 2011Date of Patent: October 23, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman
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Publication number: 20120264785Abstract: The present invention relates to novel fluoro-substituted 3,5-dicyano-4-(1H-indazol-5-yl)-2,6-dimethyl-1,4-dihy-dropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: ApplicationFiled: October 1, 2010Publication date: October 18, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Martin Michels, Markus Follman, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Mario Lobell, Donald Bierer, Karen Engel, Maria Kissel
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Publication number: 20120252770Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicamentsType: ApplicationFiled: March 23, 2012Publication date: October 4, 2012Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrencher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Patent number: 8273770Abstract: 5-pyridinone substituted indazoles of the formula and methods of their use are presented.Type: GrantFiled: July 18, 2008Date of Patent: September 25, 2012Assignee: Albany Molecular Research, Inc.Inventors: Peter Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden
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Publication number: 20120238559Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: December 3, 2010Publication date: September 20, 2012Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8268868Abstract: Various 5-substituted 1-substituted indazoles are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.Type: GrantFiled: January 9, 2008Date of Patent: September 18, 2012Assignee: Albany Molecular Research, Inc.Inventors: Peter Robert Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden, May Xiaowu Jiang
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Patent number: 8268870Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, R1-R3 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: December 13, 2011Date of Patent: September 18, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun
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Patent number: 8263597Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: July 18, 2011Date of Patent: September 11, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Daniel Kuzmich, Can Mao, Alan David Swinamer, David Smith Thomson
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Publication number: 20120225909Abstract: [Objective] To provide a drug that selectively stimulates the ?3-adrenergic receptors, particularly a drug capable of preferentially stimulating the ?3-adrenergic receptors over the ?1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.Type: ApplicationFiled: September 30, 2010Publication date: September 6, 2012Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Yasuhiro Wada, Akifumi Morimoto
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Publication number: 20120214766Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.Type: ApplicationFiled: August 27, 2010Publication date: August 23, 2012Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
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Publication number: 20120214847Abstract: The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 26, 2010Publication date: August 23, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Christopher James Bungard, James J. Perkins, Jesse J. Manikowski, Pablo de Leon, Robert S. Meissner
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Publication number: 20120214846Abstract: The present invention encompasses compounds of Formula (I): or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 26, 2010Publication date: August 23, 2012Applicant: MERCK SHARP & DOHME CORPInventors: Helen J. Mitchell, William P. Dankulich, Mildred K. Kaufman, Robert S. Meissner
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Publication number: 20120214794Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: October 13, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120214807Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20120208818Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 10, 2011Publication date: August 16, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Amy M. Elder, Shomir Ghosh, Sian Griffiths, Prakash Raman, Francois Soucy, Kevin Sprott, Qing Ye
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Patent number: 8242280Abstract: The present invention provides fused ring heterocycles as kinase modulators, pharmaceutical compositions containing these modulators, and methods of using these modulators to treat diseases mediated by kinase activity.Type: GrantFiled: April 10, 2008Date of Patent: August 14, 2012Assignee: SGX Pharmaceuticals, Inc.Inventors: Chixu Chen, Brian Eastman, Andreas Gosberg, Stefan N. Gradl, Gavin Hirst, Stephanie Hopkins, Khanh Thi Tuong Nguyen, Richard Pracitto, Paul E. Sprengeler, Ruo W. Steensma
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Publication number: 20120202817Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
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Publication number: 20120196880Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: December 19, 2011Publication date: August 2, 2012Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Publication number: 20120183496Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20120172397Abstract: The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: August 30, 2010Publication date: July 5, 2012Applicant: MERCK SHARP & DOHME CORP.Inventors: Helen J. Mitchell, Danielle M. Hurzy, Robert S. Meissner
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Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Publication number: 20120148534Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: ApplicationFiled: March 16, 2010Publication date: June 14, 2012Inventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
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Patent number: 8198456Abstract: This invention provides novel dihydropyridine derivatives of the formula I having protein tyrosine kinase inhibitory activity, to process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions.Type: GrantFiled: December 13, 2007Date of Patent: June 12, 2012Assignee: Bayer Intellectual Property GmbHInventors: Marc Adler, Stefan Baeurle, Judi Bryant, Ming Chen, Yuo-Ling Chou, Paul Hrvatin, Seock-Kyu Khim, Monica Kochanny, Wheeseong Lee, Michael Mamounas, Janet Meurer Ogden, Gary Bruce Phillips, Victor Selchau, Christopher West, Bin Ye, Shendong Yuan, Martin Krueger
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Publication number: 20120130069Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.Type: ApplicationFiled: December 4, 2009Publication date: May 24, 2012Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han
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Publication number: 20120101131Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1-R5 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: January 2, 2012Publication date: April 26, 2012Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
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Publication number: 20120095053Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, R1-R3 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: ApplicationFiled: December 13, 2011Publication date: April 19, 2012Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun
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Publication number: 20120095055Abstract: The present invention encompasses compounds of Formula (I): or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: May 24, 2010Publication date: April 19, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Helen J. Mitchell, Danielle M. Hurzy, Mildred K. Kaufman
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Patent number: 8153663Abstract: This invention relates to novel indazole derivatives of formula I: wherein R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.Type: GrantFiled: September 21, 2009Date of Patent: April 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Markus Rudolph, Sven Taylor
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Publication number: 20120083511Abstract: The present invention provides crystalline (R)-(E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol useful in the treatment of cancer.Type: ApplicationFiled: September 29, 2011Publication date: April 5, 2012Applicant: ELI LILLY AND COMPANYInventor: Benjamin Alan Diseroad
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Patent number: 8143289Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 12, 2009Date of Patent: March 27, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ping Chen, Jason M. Cox, Ann E. Weber
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Patent number: 8143290Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.Type: GrantFiled: December 2, 2010Date of Patent: March 27, 2012Assignees: AstraZeneca AB, Bayer Schering Pharma AktiengesellschaftInventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
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Patent number: 8138208Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1-R5 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: July 6, 2009Date of Patent: March 20, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
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Publication number: 20120065173Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: September 2, 2011Publication date: March 15, 2012Inventors: Markus Berger, Lena Bergström, Jan Dahmén, Anders Eriksson, Balint Gabos, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Stinabritt Nilsson, Camilla Taflin, Darren McKerrecher, Hartmut Rehwinkel
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Patent number: 8114865Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer formula (I).Type: GrantFiled: December 14, 2007Date of Patent: February 14, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Marcella Nesi, Ettore Perrone, Roberto Bossi, Paolo Polucci
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Publication number: 20120035131Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: October 20, 2011Publication date: February 9, 2012Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
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Publication number: 20120028963Abstract: The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.Type: ApplicationFiled: March 18, 2010Publication date: February 2, 2012Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
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Publication number: 20120022253Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: September 29, 2011Publication date: January 26, 2012Applicant: ABBOTT LABORATORIESInventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Publication number: 20110319379Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R4, R6, X, Y and Z are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.Type: ApplicationFiled: March 4, 2010Publication date: December 29, 2011Inventors: Jeffrey W. Corbett, Angel Guzman-Perez, Jeffrey A. Pfefferkorn, Meihua Tu
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Publication number: 20110306599Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: November 24, 2010Publication date: December 15, 2011Applicant: JAPAN TOBACCO INC.Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
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Publication number: 20110306592Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
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Patent number: 8076488Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: GrantFiled: March 1, 2004Date of Patent: December 13, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, Stephen Boyer, Sharad Verma, Lila Adnane, Yuanwei Chen, Wendy Lee, Barton Phillips, Roger A. Smith, William J. Scott, Jennifer Burke, Jianqing Chen, Zhi Chen, Jianmei Fan, Karl Miranda, Brian Raudenbush, Aniko Redman, Jianxing Shao, Ning Su, Gan Wang, Lin Yi, Qingming Zhu
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Publication number: 20110301082Abstract: 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 15, 2010Publication date: December 8, 2011Inventors: Songnian Lin, Libo Xo, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20110301155Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.Type: ApplicationFiled: June 18, 2008Publication date: December 8, 2011Inventors: Tsuneo Yasuma, Shigekazu Sasaki, Osamu Ujikawa, Yasufumi Miyamoto, Stephen L. Gwaltney, Sheldon Cao, Andy Jennings
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Publication number: 20110301148Abstract: The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH2, —CH(R?)—, —NH(R?)— or a heteroatom chosen from O and S, it being understood that R? represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO2—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; orType: ApplicationFiled: June 29, 2011Publication date: December 8, 2011Applicant: SANOFIInventors: Jean-Michel ALTENBURGER, Valérie FOSSEY, Stéphane ILLIANO, Géraldine MANETTE
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Patent number: 8071628Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y 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 in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.Type: GrantFiled: September 8, 2010Date of Patent: December 6, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
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Publication number: 20110294808Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: July 18, 2011Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Daniel KUZMICH, Can MAO, Alan David SWINAMER, David Smith THOMSON
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Publication number: 20110294854Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein a, R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Applicant: ABBOTT LABORATORIESInventors: Xenia B. Searle, Ming C. Yeung, Michael R. Schrimpf
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Publication number: 20110281868Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A1, A2, A3 and L are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora and KDR.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Michaelides, James H. Holms, Douglas H. Steinman