The Additional Hetero Ring Is Six-membered Patents (Class 546/282.1)
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Publication number: 20150119378Abstract: 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: ApplicationFiled: October 24, 2014Publication date: April 30, 2015Inventors: Srinivasa Rao Akireddy, Scott R. Breining
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Patent number: 9006429Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.Type: GrantFiled: August 30, 2013Date of Patent: April 14, 2015Assignee: Syngenta Crop Protection, LLCInventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach
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Publication number: 20150099696Abstract: 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: ApplicationFiled: June 26, 2012Publication date: April 9, 2015Applicant: Cadila Healthcare LimitedInventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
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Publication number: 20150094338Abstract: 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: ApplicationFiled: December 5, 2014Publication date: April 2, 2015Applicant: PFIZER INC.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20150065507Abstract: 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: ApplicationFiled: April 25, 2013Publication date: March 5, 2015Applicant: Glaxo Group LimitedInventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
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Publication number: 20150038707Abstract: 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: ApplicationFiled: September 19, 2013Publication date: February 5, 2015Inventors: Kevin M. Belyk, Edward Cleator, Shen-Chun Kuo, Peter Emmanuel Maligres, Bangping Xiang, Nobuyoshi Yasuda, Jianguo Yin
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Publication number: 20150018321Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: September 25, 2014Publication date: January 15, 2015Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
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Publication number: 20150005348Abstract: 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: ApplicationFiled: February 5, 2013Publication date: January 1, 2015Inventors: Jun Ohshita, Tomotsugu Awano, Hideki Ihara
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Publication number: 20140378305Abstract: Compounds of formula wherein the substituents are as defined in claim 1, and related compositions, methods of use and processes of preparation.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: SYNGENTA LIMITEDInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20140371268Abstract: 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: ApplicationFiled: August 31, 2012Publication date: December 18, 2014Applicant: AMAKEM NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Patent number: 8906939Abstract: 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: GrantFiled: March 7, 2008Date of Patent: December 9, 2014Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, S.A.Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey
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Publication number: 20140336137Abstract: 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: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
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Patent number: 8883850Abstract: 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: GrantFiled: May 23, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Christina Ng DiMarco, Scott D. Kukuk
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Patent number: 8865623Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: GrantFiled: January 6, 2010Date of Patent: October 21, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20140309427Abstract: 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: ApplicationFiled: February 6, 2014Publication date: October 16, 2014Inventor: Aloke K. DUTTA
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Publication number: 20140288041Abstract: 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: ApplicationFiled: May 12, 2014Publication date: September 25, 2014Applicant: 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
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Publication number: 20140243374Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.Type: ApplicationFiled: October 4, 2012Publication date: August 28, 2014Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
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Publication number: 20140234245Abstract: 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: ApplicationFiled: November 5, 2012Publication date: August 21, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Cédric Poinsard
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Patent number: 8796311Abstract: 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: GrantFiled: March 7, 2008Date of Patent: August 5, 2014Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, SAInventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey
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Publication number: 20140213569Abstract: 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: ApplicationFiled: March 31, 2014Publication date: July 31, 2014Applicant: GRUNENTHAL GMBHInventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER, Simon LUCAS
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Patent number: 8765790Abstract: 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: GrantFiled: July 3, 2013Date of Patent: July 1, 2014Assignee: H. Lundbeck A/SInventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
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Patent number: 8735322Abstract: Cyclohexanedione compounds, which are suitable for use as herbicides.Type: GrantFiled: September 23, 2009Date of Patent: May 27, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, John Martin Clough, Kevin Beautement, Melloney Tyte, Louisa Robinson, Stephane AndréMarie Jeanmart
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Publication number: 20140142083Abstract: 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: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: 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
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Publication number: 20140135301Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 22, 2014Publication date: May 15, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
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Patent number: 8722894Abstract: 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: GrantFiled: September 12, 2008Date of Patent: May 13, 2014Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma SAInventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
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Patent number: 8722672Abstract: 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: GrantFiled: July 20, 2010Date of Patent: May 13, 2014Assignee: Novartis AGInventors: Andreas Fritze, Karine Corcelle, Melinda Eniko Grubesa
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Publication number: 20140107340Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptorType: ApplicationFiled: October 10, 2013Publication date: April 17, 2014Applicant: H. Lundbeck A/SInventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
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Publication number: 20140107339Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.Type: ApplicationFiled: September 4, 2013Publication date: April 17, 2014Applicant: Cornell UniversityInventors: Geoffrey W. Coates, John W. Kramer
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4-phenyl-pyrane-3,5-diones,4-phenyl-thiopyrane-3,6-diones and cyclohexanetriones as novel herbicides
Patent number: 8680012Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.Type: GrantFiled: December 12, 2007Date of Patent: March 25, 2014Assignee: Syngenta Crop Protection LLCInventors: Christopher John Mathews, James Nicholas Scutt, Michel Muehlebach -
Publication number: 20140057926Abstract: 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: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
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Publication number: 20140051727Abstract: 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: ApplicationFiled: December 8, 2011Publication date: February 20, 2014Applicant: Lycera CorporationInventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
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Publication number: 20140045770Abstract: 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: ApplicationFiled: October 16, 2013Publication date: February 13, 2014Applicant: NEKTAR THERAPEUTICSInventors: Jennifer RIGGS-SAUTHIER, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
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Publication number: 20140023611Abstract: 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: ApplicationFiled: January 4, 2013Publication date: January 23, 2014Inventor: ARDELYX, INC.
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Publication number: 20140024621Abstract: 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: ApplicationFiled: July 23, 2012Publication date: January 23, 2014Applicant: MS THERAPEUTICS LIMITEDInventors: Michael J. Hudson, Alan Palmer, Richard Todd, Patrick Camilleri
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Publication number: 20140010898Abstract: 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: ApplicationFiled: July 3, 2013Publication date: January 9, 2014Inventors: Jorgen Eskildsen, Anette Graven Sams, Ask Püschl
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Publication number: 20140005389Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.Type: ApplicationFiled: August 30, 2013Publication date: January 2, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John MATHEWS, James Nicholas SCUTT, Michel MUEHLEBACH
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Publication number: 20130324412Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.Type: ApplicationFiled: August 8, 2013Publication date: December 5, 2013Applicant: DOW AGROSCIENCES LLCInventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
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Patent number: 8598364Abstract: 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: GrantFiled: March 12, 2008Date of Patent: December 3, 2013Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
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Publication number: 20130296369Abstract: 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: ApplicationFiled: November 11, 2011Publication date: November 7, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Desbordes, Christophe Dubost, Pierre Genix, Shinichi Narabu, Jean-Pierre Vors
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Publication number: 20130296561Abstract: 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: ApplicationFiled: January 13, 2012Publication date: November 7, 2013Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.Inventors: Karin Henderika Maria Bessembinder, Dennis Heemskerk, Ben De Lange
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Publication number: 20130281366Abstract: 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: ApplicationFiled: December 26, 2011Publication date: October 24, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
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Publication number: 20130271719Abstract: 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: ApplicationFiled: April 4, 2013Publication date: October 17, 2013Applicants: JNC PETROCHEMICAL CORPORATION, JNC CORPORATIONInventors: Takahiro KUBO, Yasuyuki GOTOH
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Publication number: 20130253186Abstract: 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: ApplicationFiled: May 10, 2013Publication date: September 26, 2013Applicant: 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
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Patent number: 8524897Abstract: 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: GrantFiled: January 10, 2012Date of Patent: September 3, 2013Assignee: Novartis AGInventor: Rita Ramos
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Publication number: 20130225587Abstract: 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: ApplicationFiled: November 9, 2011Publication date: August 29, 2013Applicants: 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
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Publication number: 20130225619Abstract: 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: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Publication number: 20130158034Abstract: 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: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: 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
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Publication number: 20130131056Abstract: 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: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130131036Abstract: 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: ApplicationFiled: October 23, 2012Publication date: May 23, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Patent number: 8410088Abstract: 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: GrantFiled: April 13, 2012Date of Patent: April 2, 2013Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Masashi Seki, Syuji Shirotori