The Additional Hetero Ring Is Six-membered Patents (Class 546/282.1)
  • Publication number: 20150119378
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Inventors: Srinivasa Rao Akireddy, Scott R. Breining
  • Patent number: 9006429
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: April 14, 2015
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Publication number: 20150094338
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 2, 2015
    Applicant: PFIZER INC.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Publication number: 20150065507
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 5, 2015
    Applicant: Glaxo Group Limited
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Publication number: 20150038707
    Abstract: Methods for preventing pest infestations are disclosed. In some embodiments, the methods for preventing infestations involve use of pyrethroid insecticides or the stereoisomers or salts thereof.
    Type: Application
    Filed: September 19, 2013
    Publication date: February 5, 2015
    Inventors: Kevin M. Belyk, Edward Cleator, Shen-Chun Kuo, Peter Emmanuel Maligres, Bangping Xiang, Nobuyoshi Yasuda, Jianguo Yin
  • Publication number: 20150018321
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 15, 2015
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
  • Publication number: 20150005348
    Abstract: An amide compound represented by formula (I) has an excellent pest control effect. (In the formula, Y represents a 3-7 membered saturated heterocyclic ring which contains, as ring-forming components(s), one or more atoms or groups that are selected from the group consisting of an oxygen atom and —S(O)t—, the saturated heterocyclic ring may have one to three atoms or groups selected from group D and t represents 0 or the like; x represents a C1-C8 chain hydrocarbon group having one group that is selected from group A; W represents —CR8— or the like; r represents 1 or the like; R1, R2, R3, R4, R5, R6, R7 and R8 may be the same or different and each represents a hydrogen atom or the like; and n represents 1 or the like.
    Type: Application
    Filed: February 5, 2013
    Publication date: January 1, 2015
    Inventors: Jun Ohshita, Tomotsugu Awano, Hideki Ihara
  • Publication number: 20140378305
    Abstract: Compounds of formula wherein the substituents are as defined in claim 1, and related compositions, methods of use and processes of preparation.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: SYNGENTA LIMITED
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20140371268
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases, gastrointestinal diseases and respiratory diseases.
    Type: Application
    Filed: August 31, 2012
    Publication date: December 18, 2014
    Applicant: AMAKEM NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
  • Patent number: 8906939
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: December 9, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, S.A.
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey
  • Publication number: 20140336137
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • Patent number: 8883850
    Abstract: The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Christina Ng DiMarco, Scott D. Kukuk
  • Patent number: 8865623
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: October 21, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Publication number: 20140309427
    Abstract: Certain 3,6-disubstituted and 2, 4, 5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3, 6 and 2, 4, 5 pyrans are useful in probing the effects of their binding to monoamine transporter systems and the corresponding relationships to various afflictions affecting the CNS, or as a treatment for various CNS-related disorders in which the monoamine transport and related systems are implicated.
    Type: Application
    Filed: February 6, 2014
    Publication date: October 16, 2014
    Inventor: Aloke K. DUTTA
  • Publication number: 20140288041
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: May 12, 2014
    Publication date: September 25, 2014
    Applicant: EPIZYME, INC.
    Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
  • Publication number: 20140243374
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 28, 2014
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
  • Publication number: 20140234245
    Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
    Type: Application
    Filed: November 5, 2012
    Publication date: August 21, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Patent number: 8796311
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: August 5, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey
  • Publication number: 20140213569
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: March 31, 2014
    Publication date: July 31, 2014
    Applicant: GRUNENTHAL GMBH
    Inventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER, Simon LUCAS
  • Patent number: 8765790
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: July 1, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Patent number: 8735322
    Abstract: Cyclohexanedione compounds, which are suitable for use as herbicides.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: May 27, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, John Martin Clough, Kevin Beautement, Melloney Tyte, Louisa Robinson, Stephane AndréMarie Jeanmart
  • Publication number: 20140142083
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 22, 2014
    Applicant: EPIZYME, INC.
    Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy James Nelson Wigle, Masashi Seki
  • Publication number: 20140135301
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: January 22, 2014
    Publication date: May 15, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • Patent number: 8722894
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: May 13, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
  • Patent number: 8722672
    Abstract: The present invention relates to pharmaceutical compositions of 2-Methyl-4?-trifluoromethoxy-biphenyl-3-carboxylic acid [6-(cis-2,6-dimethyl-morpholin-4-yl)-pyridin-3-yl]-amide, to the use of such compositions in therapeutic applications and to methods for manufacturing such compositions.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: May 13, 2014
    Assignee: Novartis AG
    Inventors: Andreas Fritze, Karine Corcelle, Melinda Eniko Grubesa
  • Publication number: 20140107340
    Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • Publication number: 20140107339
    Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.
    Type: Application
    Filed: September 4, 2013
    Publication date: April 17, 2014
    Applicant: Cornell University
    Inventors: Geoffrey W. Coates, John W. Kramer
  • Patent number: 8680012
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: March 25, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach
  • Publication number: 20140057926
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
  • Publication number: 20140051727
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 20, 2014
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20140045770
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the small molecule drug not attached to the water-soluble oligomer.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Jennifer RIGGS-SAUTHIER, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
  • Publication number: 20140024621
    Abstract: The invention generally relates to aminopyridines and methods of use thereof. In certain embodiments, the invention provides an aminopyridine or a pharmaceutically-acceptable salt thereof, in which the aminopyridine or the salt thereof includes a cleavable functional group that substantially prevents extra-hepatic hydrolysis.
    Type: Application
    Filed: July 23, 2012
    Publication date: January 23, 2014
    Applicant: MS THERAPEUTICS LIMITED
    Inventors: Michael J. Hudson, Alan Palmer, Richard Todd, Patrick Camilleri
  • Publication number: 20140023611
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: January 4, 2013
    Publication date: January 23, 2014
    Inventor: ARDELYX, INC.
  • Publication number: 20140010898
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 9, 2014
    Inventors: Jorgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20140005389
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.
    Type: Application
    Filed: August 30, 2013
    Publication date: January 2, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Christopher John MATHEWS, James Nicholas SCUTT, Michel MUEHLEBACH
  • Publication number: 20130324412
    Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 5, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
  • Patent number: 8598364
    Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: December 3, 2013
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
  • Publication number: 20130296561
    Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.
    Type: Application
    Filed: January 13, 2012
    Publication date: November 7, 2013
    Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
    Inventors: Karin Henderika Maria Bessembinder, Dennis Heemskerk, Ben De Lange
  • Publication number: 20130296369
    Abstract: The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 7, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Desbordes, Christophe Dubost, Pierre Genix, Shinichi Narabu, Jean-Pierre Vors
  • Publication number: 20130281366
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 24, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
  • Publication number: 20130271719
    Abstract: To provide a liquid crystal compound having a large positive value of dielectric anisotropy and a small viscosity. The compound is represented by formula (1): wherein, in formula (1), R1 is alkyl having 1 to 20 carbons or the like; ring A1 is 1,4-cyclohexylene or the like; ring A2 is 1,4-phenylene, 2-fluoro-1,4-phenylene, 2,6-difluoro-1,4-phenylene or the like; ring A3 is 1,4-cyclohexylene, 1,4-phenylene, 2-fluoro-1,4-phenylene, 2,6-difluoro-1,4-phenylene or the like; and X1 is halogen, alkyl having 1 to 10 carbons or the like, and in the alkyl, at least one of hydrogen may be replaced by halogen.
    Type: Application
    Filed: April 4, 2013
    Publication date: October 17, 2013
    Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATION
    Inventors: Takahiro KUBO, Yasuyuki GOTOH
  • Publication number: 20130253186
    Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • Patent number: 8524897
    Abstract: The invention relates to 5-cyano-3-methyl-pyridine-2-carboxylic acid [3-((3R,6R)-5-amino-3,6-dimethyl-6-trifluoromethyl-3,6-dihydro-2H-[1,4]oxazin-3-yl)-4-fluoro-phenyl]-amide in crystalline form, to its preparation, its medical use and to medicaments comprising said compound in crystalline form.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: September 3, 2013
    Assignee: Novartis AG
    Inventor: Rita Ramos
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20130225587
    Abstract: The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.
    Type: Application
    Filed: November 9, 2011
    Publication date: August 29, 2013
    Applicants: Zhejiang Beta Pharma Incorporation, Fujian Haixi Pharmaceuticals, Inc.
    Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Xiaoyan Shen, Yunyan Hu, Fenlai Tan, Yinxiang Wang
  • Publication number: 20130158034
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: June 21, 2012
    Publication date: June 20, 2013
    Applicant: Amgen Inc.
    Inventors: James BROWN, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. Horne, Matthew R. KALLER, Qingyian LIU, Holger MONENSCHEIN, Thomas T. NGUYEN, Nobuko NISHIMURA, Wenge ZHONG
  • Publication number: 20130131036
    Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Application
    Filed: October 23, 2012
    Publication date: May 23, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • Publication number: 20130131056
    Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 23, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8410088
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: April 2, 2013
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Masashi Seki, Syuji Shirotori