Polycyclo Ring System Having The 1,3-diazole Ring As One Of The Cyclos Patents (Class 546/273.1)
  • Patent number: 11639355
    Abstract: Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: May 2, 2023
    Assignees: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD., SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD., MEDSHINE DISCOVERY INC.
    Inventors: Kevin X Chen, Xiaobing Yan, Jianglei Huang, Yuekun Nie, Guoping Hu, Jian Li, Shuhui Chen, Jiaqiang Dong, Tie-Lin Wang
  • Patent number: 9290503
    Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
    Type: Grant
    Filed: January 15, 2014
    Date of Patent: March 22, 2016
    Assignee: CHEMBRIDGE CORPORATION
    Inventor: Vlad Edward Gregor
  • Patent number: 9029399
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: May 12, 2015
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Saumitra Sengupta
  • Patent number: 8969341
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: March 3, 2015
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20140374706
    Abstract: Disclosed are a compound for an organic optoelectric device, an organic optoelectric device including the same and a display device including the organic optoelectric device, wherein the compound for an organic optoelectric device is represented by the following Chemical Formula 1, In the above Chemical Formula 1, R1 to R7, X, L1 and L2 are the same as described in the detailed description.
    Type: Application
    Filed: November 20, 2013
    Publication date: December 25, 2014
    Inventors: Jin-Seok HONG, Dong-Min KANG, Eun-Sun YU, Soo-Young JEONG, Ji-Hun SHIN, Dong-Kyu RYU, Han-ill LEE, Yu-Na JANG
  • Publication number: 20140357673
    Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
    Type: Application
    Filed: July 31, 2014
    Publication date: December 4, 2014
    Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey William Perry, Roderick Joseph Sorenson, Mary Xuan Dziem O'Riordan, Yafei Jin
  • Publication number: 20140350010
    Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: November 28, 2012
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Patent number: 8835463
    Abstract: The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: September 16, 2014
    Assignees: Allergan, Inc., Exonhit Therapeutics SA
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
  • Patent number: 8815906
    Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: August 26, 2014
    Assignee: Chembridge Corporation
    Inventors: Yahua Liu, Alexey Vyacheslavovich Anikin, Charles Chamchoumis Mikel, Douglas Eric McGrath, Goverdhan Reddy Vavilala, Jason Conrad Pickens, Aleksander Kadushkin, Luyong Jiang, Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong Zhu, Alexander Chucholowski, Zheng Yan, Alisher Khasanov, Christina Gregor
  • Publication number: 20140155602
    Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: November 20, 2013
    Publication date: June 5, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20140051689
    Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.
    Type: Application
    Filed: October 24, 2013
    Publication date: February 20, 2014
    Applicant: Biota Scientific Management Pty Ltd.
    Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
  • Publication number: 20140011212
    Abstract: The present invention relates to trifunctional crosslinking reagents carrying (i) a ligand-reactive group for conjugation to a ligand of interest having at least one binding site on a target glycoprotein receptor, (ii) an optionally protected aromatic hydrazine group for the capturing of oxidized receptor-glycopeptides and (iii) an affinity group for the detection, isolation and purification of captured glycopeptides, their methods of production, as well as their use in methods for detecting, identifying and characterizing interactions between ligands and their corresponding glycoprotein target receptors on living cells and in biological fluids.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 9, 2014
    Applicant: ETH ZURICH
    Inventors: Andreas Frei, Bernd Wollscheid, Ock-Youm Jeon, Erick Carreira
  • Publication number: 20140011798
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: January 24, 2013
    Publication date: January 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
  • Patent number: 8598217
    Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: December 3, 2013
    Assignees: Astex Therapeutics Ltd., Novartis AG
    Inventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
  • Patent number: 8575360
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: November 5, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rene Marc Lemieux, Steven Richard Brunette, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Bryan McKibben, Craig Andrew Miller, Antonio J. M. Barbosa
  • Patent number: 8552205
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Patent number: 8541595
    Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: September 24, 2013
    Assignee: Merch Sharp & Dohme Corp.
    Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
  • Patent number: 8519149
    Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: August 27, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
  • Patent number: 8497288
    Abstract: The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease and non-alcoholic steatohepatitis.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: July 30, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch
  • Publication number: 20130190290
    Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: January 23, 2013
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventor: BAYER INTELLECTUAL PROPERTY GmbH
  • Patent number: 8481750
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: July 9, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jennifer A. Kowalski, Matt Aaron Tschantz
  • Patent number: 8461181
    Abstract: A fused heterocyclic compound of formula (1): wherein, A1 and A2 represent a nitrogen atom or the like, R1, R2, R3 and R4 represent a halogen atom or the like, R2 and R3 represent a halogen atom or the like, R5 represents a C1-C6 chain hydrocarbon group optionally substituted with one or more halogen atoms, or the like, R6 and R7 represent a C1-C4 chain hydrocarbon group substituted with one or more halogen atoms, or the like, and n represents 0 or 1, has an excellent noxious arthropod controlling effect.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: June 11, 2013
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Masaki Takahashi, Mitsuhiko Iwakoshi, Hiroshi Ikegami
  • Patent number: 8415484
    Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: April 9, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M. Jones, Daniel J. Buzard, Andrew M. Kawasaki, Sun Hee Kim, Lars Thoresen, Juerg Lehmann, Xiuwen Zhu
  • Publication number: 20130065893
    Abstract: The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 29, 2010
    Publication date: March 14, 2013
    Applicant: NOVARTIS AG
    Inventors: Robert Sun, Lauren G. Monovich, Sylvie Chamoin, John Westbrook
  • Publication number: 20130053376
    Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
    Type: Application
    Filed: March 18, 2009
    Publication date: February 28, 2013
    Inventors: Yahua Liu, Alexey Vyacheslavovich Anikin, Charles Chamchoumis Mikel, Douglas Eric McGrath, Goverdhan Reddy Vavilala, Jason Conrad Pickens, Aleksander Kadushkin, Luyong Jiang, Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong Zhu, Alexander Chucholowski, Zheng Yan, Alisher Khasanov, Christina Gregor
  • Publication number: 20130023568
    Abstract: The present invention relates to benzimidazole derivatives and their pharmaceutical compositions and uses, specifically to benzimidazole derivatives of Formula (I), or their stereoisomer, pharmaceutically acceptable salt or solvates thereof, in which R1, R2, R3, R4, R5 and n have the definitions in the description; the present invention further relates to a pharmaceutical composition containing the compounds, methods for preparing the compounds, and use of the compounds for manufacturing of a medicament for prophylaxis and/or treatment of peptic ulcer, ulcer hemorrhage and diseases associated with gastric acid.
    Type: Application
    Filed: January 31, 2011
    Publication date: January 24, 2013
    Inventors: Zhenhua Huang, Guanglian Zhou
  • Publication number: 20130018052
    Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 17, 2013
    Applicant: SK CHEMICALS CO., LTD.
    Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
  • Publication number: 20120289549
    Abstract: The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease and non-alcoholic steatohepatitis.
    Type: Application
    Filed: May 2, 2012
    Publication date: November 15, 2012
    Inventors: Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch
  • Patent number: 8288376
    Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: October 16, 2012
    Assignee: Sanofi
    Inventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
  • Patent number: 8273764
    Abstract: A fused heterocyclic compound of formula (1): wherein, A1 and A2 represent a nitrogen atom or the like, R1, R2, R3 and R4 represent a halogen atom or the like, R2 and R3 represent a halogen atom or the like, R5 represents a C1-C6 chain hydrocarbon group optionally substituted with one or more halogen atoms, or the like, R6 and R7 represent a C1-C4 chain hydrocarbon group substituted with one or more halogen atoms, or the like, and n represents 0 or 1, has an excellent noxious arthropod controlling effect.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: September 25, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masaki Takahashi, Mitsuhiko Iwakoshi, Hiroshi Ikegami
  • Patent number: 8227485
    Abstract: The invention relates to novel benzimidazole and imidazopyridine derivatives having general formula (I), which have a good affinity with certain sub-types of melanocortin receptors, particularly MC4 receptors. Said derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said products.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: July 24, 2012
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Lydie Poitout, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
  • Publication number: 20120178779
    Abstract: A fused heterocyclic compound of formula (1): wherein, A1 and A2 represent a nitrogen atom or the like, R1, R2, R3 and R4 represent a halogen atom or the like, R2 and R3 represent a halogen atom or the like, R5 represents a C1-C6 chain hydrocarbon group optionally substituted with one or more halogen atoms, or the like, R6 and R7 represent a C1-C4 chain hydrocarbon group substituted with one or more halogen atoms, or the like, and n represents 0 or 1, has an excellent noxious arthropod controlling effect.
    Type: Application
    Filed: March 9, 2012
    Publication date: July 12, 2012
    Inventors: Masaki TAKAHASHI, Mitsuhiko IWAKOSHI, Hiroshi IKEGAMI
  • Publication number: 20120178734
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Application
    Filed: May 28, 2010
    Publication date: July 12, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Jennifer A. Kowalski, Matt Aaron Tschantz
  • Publication number: 20120157403
    Abstract: 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: Application
    Filed: February 24, 2012
    Publication date: June 21, 2012
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
  • Publication number: 20120157497
    Abstract: The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.
    Type: Application
    Filed: March 1, 2012
    Publication date: June 21, 2012
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
  • Publication number: 20120108583
    Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Application
    Filed: October 28, 2011
    Publication date: May 3, 2012
    Applicant: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
  • Patent number: 8148363
    Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: April 3, 2012
    Assignee: Schering Corporation
    Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
  • Patent number: 8143248
    Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: March 27, 2012
    Assignee: Sanofi-Aventis
    Inventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
  • Publication number: 20120065233
    Abstract: The present disclosure relates to the field of tyrosine kinase enzyme inhibition, in particular anaplastic lymphoma kinase (ALK) inhibition using novel small molecules. Provided are compounds capable to modulate ALK activity, compositions that comprise the compounds, and methods of using the compounds for the treatment or prevention of diseases or conditions that are characterized by ALK activity or expression.
    Type: Application
    Filed: September 13, 2011
    Publication date: March 15, 2012
    Inventors: Vlad Edward GREGOR, Nelson Levy
  • Publication number: 20120065210
    Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R1?, R2, R2?, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.
    Type: Application
    Filed: September 7, 2011
    Publication date: March 15, 2012
    Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Patent number: 8101637
    Abstract: The present invention relates to novel compounds of formula (I) wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors-subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: January 24, 2012
    Assignee: Addex Pharma SA
    Inventors: Anne-Sophie Bessis, Christelle Bolea, Béatrice Bonnet, Mark Epping-Jordan, Nicholas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
  • Publication number: 20120015975
    Abstract: A fused heterocyclic compound of formula (1): wherein, A1 and A2 represent a nitrogen atom or the like, R1, R2, R3 and R4 represent a halogen atom or the like, R2 and R3 represent a halogen atom or the like, R5 represents a C1-C6 chain hydrocarbon group optionally substituted with one or more halogen atoms, or the like, R6 and R7 represent a C1-C4 chain hydrocarbon group substituted with one or more halogen atoms, or the like, and n represents 0 or 1, has an excellent noxious arthropod controlling effect.
    Type: Application
    Filed: April 20, 2010
    Publication date: January 19, 2012
    Inventors: Masaki Takahashi, Mitsuhiko Iwakoshi, Hiroshi Ikegami
  • Patent number: 8063225
    Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.
    Type: Grant
    Filed: August 10, 2007
    Date of Patent: November 22, 2011
    Assignee: Chembridge Corporation
    Inventors: Vlad E. Gregor, Yahua Liu, Alexey Anikin, Danny Peter Claude McGee, Charles Mikel, Douglas Eric McGrath, Goverdhan Reddy Vavilala, Jason C. Pickens, Alexander Kadushkin, Luyong Jiang, Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong Zhu, Alexander Chucholowski, Thomas Webb, Vidyasagar Reddy Gantla, Zheng Yan
  • Publication number: 20110224188
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Application
    Filed: November 20, 2008
    Publication date: September 15, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Antonio Jose del Moral Barbosa, Joerg Martin Benzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan Mckibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Publication number: 20110212941
    Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
    Type: Application
    Filed: November 3, 2009
    Publication date: September 1, 2011
    Inventors: Peter J. Manley, Kausik K. Nanda, B. Wesley Trotter
  • Publication number: 20110207719
    Abstract: A series of novel anthra[1,2-d]imidazole-6,11-dione derivatives, and the preparation method and application of said derivatives, wherein said application includes a pharmaceutical composition containing said derivatives for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 25, 2011
    Inventor: Hsu-Shan HUANG
  • Patent number: 7943649
    Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: May 17, 2011
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Tom Wu
  • Publication number: 20110111514
    Abstract: A process for synthesis of a labelling reagent, a process for the labelling of a biological molecule, a labelled biological molecule obtained by the process, a process for labelling and fragmentation of a single or double strand nucleic acid, a labelled nucleic acid capable of being obtained by the process, a kit for detection of a target nucleic acid containing a labelled nucleic acid, a solid support onto which is attached a reagent and a process for capture of nucleic acids.
    Type: Application
    Filed: July 28, 2009
    Publication date: May 12, 2011
    Applicants: BIOMERIEUX, UNIVERSITE DE STRASBOURG, CNRS
    Inventors: Alain Laurent, Ali Laayoun, Mitsuhara Kotera
  • Publication number: 20110065682
    Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
    Type: Application
    Filed: May 18, 2009
    Publication date: March 17, 2011
    Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu,, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick,, Liyuan Wang, Xiaobang Gao
  • Publication number: 20100317660
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
    Type: Application
    Filed: August 2, 2010
    Publication date: December 16, 2010
    Inventors: Oivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. Mackinnon