Having -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Nitrogen By Nonionic Bonding Patents (Class 548/139)
  • Publication number: 20150087646
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts 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: June 10, 2013
    Publication date: March 26, 2015
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20140369961
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
  • Publication number: 20140323722
    Abstract: A compound represented by formula: its pharmaceutically acceptable salt, or a solvate thereof. Ring B is substituted or unsubstituted nitrogen-containing hetero ring, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R2 and R3 taken together may form oxo, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R6 and R7 taken together with the adjacent carbon atom to which they are attached may form a substituted or unsubstituted ring, and n is an integer of 0 to 3.
    Type: Application
    Filed: April 29, 2014
    Publication date: October 30, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji MASUDA, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
  • Patent number: 8865744
    Abstract: Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
  • Patent number: 8859596
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: October 14, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Teodozyj Kolasa, Tongmei Li, Sridhar Peddi, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Derek W. Nelson
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Patent number: 8835469
    Abstract: The present invention relates to substituted benzamide derivatives of the Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: September 16, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Rajendra Kharul, Mukul R. Jain, Pankaj R. Patel
  • Publication number: 20140194421
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: November 15, 2013
    Publication date: July 10, 2014
    Applicant: CALITHERA BIOSCIENCES, INC.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Patent number: 8765968
    Abstract: A polymer comprises a polymeric chain represented by formula (I) or (II). In formula (I), a, b, c, d, and n are integers, a from 0 to 3, b from 1 to 5, c from 1 to 3, d from 1 to 5, and n from 2 to 5000; R1 and R2 are side chains; R3 and R4 are each independently H or a side chain; and when a is 0, R3 and R4 are side chains. In formula (II), a, b, c, d, e, and n are integers, a from 1 to 3, b and c being independently 0 or 1, d and e being independently 1 or 2, and n from 2 to 5000; R1 and R2 are side chains except —COOalkyl; and X1, X2 and X3 are independently O, S, or Se. Semiconductors and devices comprising the polymer are also provided.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: July 1, 2014
    Assignee: Agency for Science, Technology and Research
    Inventors: Zhikuan Chen, Jun Li, Beng Ong, Samarendra P. Singh, Hoi Kai Ivy Wong, Kok Haw Ong
  • Patent number: 8754053
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: June 17, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Patent number: 8735430
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: May 27, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki
  • Publication number: 20140142081
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Application
    Filed: November 21, 2013
    Publication date: May 22, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Publication number: 20140142146
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Application
    Filed: November 21, 2013
    Publication date: May 22, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
  • Publication number: 20140135331
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 15, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Patent number: 8629157
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain (I).
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khor, Doris Riether, Lifen Wu, Renee M. Zindell
  • Patent number: 8604016
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: December 10, 2013
    Assignee: Calithera Biosciences Inc.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Publication number: 20130317032
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 16, 2013
    Publication date: November 28, 2013
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Publication number: 20130274256
    Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
    Type: Application
    Filed: October 11, 2012
    Publication date: October 17, 2013
    Applicant: SEQUOIA SCIENCES, INC.
    Inventor: Sequoia Sciences, Inc.
  • Patent number: 8546391
    Abstract: The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.
    Type: Grant
    Filed: January 27, 2010
    Date of Patent: October 1, 2013
    Assignee: Sanofi
    Inventors: Eykmar Fett, Patrick Mougenot, Claudie Namane, Eric Nicolai, Christophe Philippo
  • Patent number: 8541453
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: September 24, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • Patent number: 8518979
    Abstract: Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: August 27, 2013
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Meir Bialer, Boris Yagen, Neta Pessah
  • Publication number: 20130184315
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Publication number: 20130157998
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: November 19, 2012
    Publication date: June 20, 2013
    Applicant: CALITHERA BIOSCIENCES INC.
    Inventor: Calithera Biosciences Inc.
  • Publication number: 20130116240
    Abstract: 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: Application
    Filed: September 26, 2012
    Publication date: May 9, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventor: Japan Tobacco Inc.
  • Publication number: 20130030022
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • Publication number: 20130023528
    Abstract: Compounds for inhibiting hypoxia inducible factor (HIF) prolyl-4-hydroxylases (PHDs) having the general formula (1). Methods of using these and related compounds for treating a patient having a condition that would benefit from inhibiting HIF PHD are also described herein.
    Type: Application
    Filed: February 17, 2011
    Publication date: January 24, 2013
    Applicant: CORNELL UNIVERSITY
    Inventors: Rajiv R. Ratan, Irina Gazaryan, Natalya Smirnova
  • Patent number: 8349871
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: January 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
  • Publication number: 20120321563
    Abstract: The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.
    Type: Application
    Filed: May 9, 2012
    Publication date: December 20, 2012
    Inventors: Kevin Groves, Bagna Bao
  • Publication number: 20120316124
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Patent number: 8329735
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: December 11, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Monika Ermann, Doris Riether, Renee M. Zindell
  • Patent number: 8318782
    Abstract: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(?W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(?Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: November 27, 2012
    Assignees: Kyowa Hakko Kirin Co., Ltd., Fujifilm Corporation
    Inventors: Kazuhiko Kato, Yushi Kitamura
  • Patent number: 8314247
    Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: November 20, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
  • Publication number: 20120253040
    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.
    Type: Application
    Filed: December 14, 2010
    Publication date: October 4, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
  • Patent number: 8236822
    Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: August 7, 2012
    Assignee: Abbott Laboratories
    Inventors: Xueqing Wang, Michael J. Dart, Bo Liu
  • Publication number: 20120189579
    Abstract: The present invention concerns a substituted pyrrolidinone of the following formula I or a salt, solvate, tautomer, isotope, enantiomer, diastereoisomer or racemic mixture thereof: (I), for the treatment of hepatitis C.
    Type: Application
    Filed: July 9, 2010
    Publication date: July 26, 2012
    Applicant: VIVALIS
    Inventors: Amaya Berecibar, Philippe Guedat, Isabelle Valarche, Céline Mohamed-Arab, Christophe Matt
  • Publication number: 20120184544
    Abstract: The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.
    Type: Application
    Filed: July 22, 2010
    Publication date: July 19, 2012
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Rajendra Kharul, Makul R. Jain, Pankaj R. Patel
  • Publication number: 20120101103
    Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.
    Type: Application
    Filed: December 18, 2009
    Publication date: April 26, 2012
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
  • Publication number: 20120083440
    Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.
    Type: Application
    Filed: October 5, 2011
    Publication date: April 5, 2012
    Inventors: William M. Pierce, JR., K. Grant Taylor, Leonard C. Waite, Kevyn Merten
  • Publication number: 20120040984
    Abstract: The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.
    Type: Application
    Filed: January 27, 2010
    Publication date: February 16, 2012
    Applicant: SANOFI
    Inventors: Eykmar Fett, Patrick Mougenot, Claudie Namane, Eric Nicolai, Christophe Philippo
  • Patent number: 8106046
    Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: January 31, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Bingwei Vera Yang
  • Publication number: 20120015929
    Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.
    Type: Application
    Filed: September 26, 2011
    Publication date: January 19, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
  • Publication number: 20110306637
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: May 20, 2011
    Publication date: December 15, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • Publication number: 20110306599
    Abstract: 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: Application
    Filed: November 24, 2010
    Publication date: December 15, 2011
    Applicant: JAPAN TOBACCO INC.
    Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
  • Patent number: 8067447
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: November 29, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: James E. Sheppeck, John L. Gilmore, T. G. Murali Dhar, Hai-Yun Xiao
  • Publication number: 20110288083
    Abstract: The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK.
    Type: Application
    Filed: May 19, 2011
    Publication date: November 24, 2011
    Applicant: NEW YORK UNIVERSITY
    Inventors: Timothy CARDOZO, Hong WANG, David Ron
  • Patent number: 8058293
    Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: November 15, 2011
    Assignee: Abbott Laboratories
    Inventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
  • Publication number: 20110275827
    Abstract: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(?W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(?Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
    Type: Application
    Filed: July 22, 2011
    Publication date: November 10, 2011
    Applicants: FUJIFILM CORPORATION, KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Kazuhiko KATO, Yushi KITAMURA
  • Patent number: 8048899
    Abstract: are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: November 1, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Markus Ostermeier, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
  • Patent number: 7968577
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: June 28, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar