Halogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/409)
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Patent number: 10519117Abstract: The purpose of the present invention is to provide a method for producing 6-bromo-3-hydroxy-2-pyrazinecarboxamide in which the content ratio of impurities is reduced. This production method includes a step of obtaining 6-bromo-3-hydroxy-2-pyrazinecarboxamide crystal having diffraction angles expressed in degrees 2? of 5.5, 20.1, 23.7, 26.7, 27.5, and 28.1° and/or diffraction angles expressed in degrees 2? of 7.1, 21.4, 25.2, 25.7, 27.1, and 28.8° in powder X-ray diffraction.Type: GrantFiled: March 5, 2019Date of Patent: December 31, 2019Assignee: FUJIFILM Toyama Chemical Co., Ltd.Inventors: Tetsuro Uchida, Sayuri Uehara, Takayoshi Tsuzuki, Yusuke Okubo, Yuta Kobayashi, Yu Koseki
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Patent number: 10266501Abstract: The purpose of the present invention is to provide a method for producing 6-bromo-3-hydroxy-2-pyrazinecarboxamide in which the content ratio of impurities is reduced. This production method includes a step of obtaining 6-bromo-3-hydroxy-2-pyrazinecarboxamide crystal having diffraction angles expressed in degrees 2? of 5.5, 20.1, 23.7, 26.7, 27.5, and 28.1° and/or diffraction angles expressed in degrees 2? of 7.1, 21.4, 25.2, 25.7, 27.1, and 28.8° in powder X-ray diffraction.Type: GrantFiled: June 8, 2016Date of Patent: April 23, 2019Assignee: FUJIFILM Toyama Chemical Co., Ltd.Inventors: Tetsuro Uchida, Sayuri Uehara, Takayoshi Tsuzuki, Yusuke Okubo, Yuta Kobayashi, Yu Koseki
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Patent number: 9193692Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof. Furthermore, provided herein are compounds having the following formulas (IV), (V), (VII) and (VIII): wherein R, R2, R3, R4, Hal and Hal2 are as defined herein, for preparation of the Heteroaryl Compounds.Type: GrantFiled: October 31, 2014Date of Patent: November 24, 2015Assignee: Signal Pharmaceuticals, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella I. Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Jan Elsner
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Publication number: 20150051397Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Inventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella I. Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Jan Elsner
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Publication number: 20140287916Abstract: A compound of formula (I), wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, an unsubstituted aromatic 6-membered heterocycle; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.Type: ApplicationFiled: October 31, 2012Publication date: September 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch
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Patent number: 8841309Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.Type: GrantFiled: September 23, 2013Date of Patent: September 23, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dieter Hamprecht, Armin Heckel, Joerg Kley
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Publication number: 20140275536Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.Type: ApplicationFiled: December 22, 2010Publication date: September 18, 2014Applicant: Galderma Research & DevelopmentInventor: Cédric Poinsard
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Patent number: 8835636Abstract: A method for producing a hydroxypyrazine derivative represented by formula (I) (wherein R1 represents a halogen atom), the method including reacting a pyrazine derivative represented by formula (III) (wherein R2 represents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group or a carboxyl group, M represents a cation capable of forming a salt, and n represents a number corresponding with the valence of M) with a halogenating agent. According to the present invention, a hydroxypyrazine derivative that functions as a production intermediate for the dichloropyrazine derivative can be produced efficiently at low cost.Type: GrantFiled: September 25, 2013Date of Patent: September 16, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Tamio Hara, Naoki Norimatsu, Hiroaki Kurushima, Takuya Kano
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Publication number: 20140213598Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.Type: ApplicationFiled: June 15, 2012Publication date: July 31, 2014Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATIONInventors: Changling Liu, Guang Huang, Jie Lan, Shulin Hao, Zhinian Li, Huichao Li, Aiying Guan, Airu Jiang, Ying Xu
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Publication number: 20140120538Abstract: Coelenterazine analogues with different luminescence properties from conventional ones and coelenteramide analogues with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogues modified at the 8-position of coelenterazine and coelenteramide analogues modified at the 2- or 3-position of coelenteramide.Type: ApplicationFiled: December 3, 2013Publication date: May 1, 2014Applicants: National University Corporation Tokyo Medical and Dental University, JNC CorporationInventors: SATOSHI INOUYE, YUIKO SAHARA, TAKAMITSU HOSOYA
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Patent number: 8697705Abstract: The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.Type: GrantFiled: May 22, 2013Date of Patent: April 15, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Robert Francis Kester, Lucja Orzechowski
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Publication number: 20140080770Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 17, 2013Publication date: March 20, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
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Patent number: 8586741Abstract: A method for producing a hydroxypyrazine derivative represented by formula (I) (wherein R1 represents a halogen atom), the method including reacting a pyrazine derivative represented by formula (III) (wherein R2 represents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group or a carboxyl group, M represents a cation capable of forming a salt, and n represents a number corresponding with the valence of M) with a halogenating agent. Also, a method for producing a dichloropyrazine derivative represented by formula (II) (wherein R21 represents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group, a carboxyl group, or a group formed as a result of a change in the functional group of R2 during chlorination), the method including reacting the hydroxypyrazine derivative (I) with a chlorinating agent.Type: GrantFiled: January 14, 2010Date of Patent: November 19, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Tamio Hara, Naoki Norimatsu, Hiroaki Kurushima, Takuya Kano
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Publication number: 20130289271Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: ApplicationFiled: June 26, 2013Publication date: October 31, 2013Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella I. Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Elizabeth Fultz, Rama Narla, Sabita Sankar, Jan Elsner
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Publication number: 20130261306Abstract: A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.Type: ApplicationFiled: May 23, 2013Publication date: October 3, 2013Applicant: OSI Pharmaceuticals, LLCInventors: Yunyu Mao, Kristen Michelle Mulvihill, Josef A. Rechka, Paula A. Tavares-Greco
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Patent number: 8513415Abstract: A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.Type: GrantFiled: April 19, 2010Date of Patent: August 20, 2013Assignee: OSI Pharmaceuticals, LLCInventors: Yunyu Mao, Josef A. Rechka, Paula A. Tavares-Greco
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Publication number: 20130184292Abstract: The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I or II: wherein the variables are as defined herein.Type: ApplicationFiled: September 28, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, John Studley, Francoise Yvonne Theodora Marie Pierard, Steven John Durrant, Benjamin Joseph Littler, Robert Michael Hughes, David Andrew Siesel, Paul Angell, Armando Urbina, Yi Shi
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Publication number: 20130158009Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: ApplicationFiled: May 13, 2011Publication date: June 20, 2013Inventors: Thomas Daniel Aicher, Josef Roland Bencsik, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt, Ajay Singh, Timothy M. Turner, Steven Armen Boyd
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Publication number: 20130137660Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: YM Biosciences Australia Pty LtdInventor: YM Biosciences Australia Pty Ltd
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Patent number: 8324218Abstract: The present application provides sodium channel blockers exemplified by the following structure: The compounds of the invention useful for treating chronic bronchitis, cystic fibrosis, sinusitis, vaginal dryness, dry eye, Sjogren's disease, distal intestinal obstruction syndrome, dry skin, esophagitis, dry mouth (xerostomia), nasal dehydration, ventilator-induced pneumonia, asthma, primary ciliary dyskinesia, otitis media, chronic obstructive pulmonary disease, emphysema, pneumonia, constipation, and chronic diverticulitis, for example.Type: GrantFiled: June 11, 2007Date of Patent: December 4, 2012Assignee: Parion Sciences, Inc.Inventor: Michael Ross Johnson
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Publication number: 20120283271Abstract: The present invention relates to compounds of the formula I, as well as pharmaceutically-acceptable salts thereof, pharmaceutical compositions containing said compounds and methods of using said compounds in the treatment or prophylaxis of diseases and disorders. The compounds and compositions disclosed herein are glucokinase activators useful for the treatment or prophylaxis of metabolic diseases and disorders, for example diabetes mellitus, including type II diabetes mellitus.Type: ApplicationFiled: April 25, 2012Publication date: November 8, 2012Inventors: Steven Joseph Berthel, Robert Francis Kester, Lucja Orzechowski
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Patent number: 8293729Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: GrantFiled: June 23, 2010Date of Patent: October 23, 2012Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
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Publication number: 20120208820Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: January 31, 2012Publication date: August 16, 2012Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120178681Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: HAROLD B. WOOD, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang
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Publication number: 20120149718Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker
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Patent number: 8168789Abstract: Disclosed is an organic amine salt of 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile, which is excellent in crystallinity and useful as a production intermediate for 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.Type: GrantFiled: September 25, 2008Date of Patent: May 1, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Tamotsu Takamatsu, Kenji Yonezawa
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Patent number: 8124607Abstract: Polyaromatic sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.Type: GrantFiled: February 26, 2009Date of Patent: February 28, 2012Assignee: Parion Sciences, Inc.Inventor: Michael Ross Johnson
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Patent number: 8119635Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: August 19, 2009Date of Patent: February 21, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120041202Abstract: A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.Type: ApplicationFiled: April 19, 2010Publication date: February 16, 2012Inventors: Yunyu Mao, Kristen Michelle Mulvihill, Josef A. Rechka, Paula A. Tavares-Greco
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Publication number: 20110306493Abstract: The invention relates to sulfoximinamid compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the sulfoximinamid compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such sulfoximine compounds. The sulfoximinamid compounds of the present invention are defined by the following formula I: wherein Q, Het, R1, R2, R3, R4 and n are defined as in the description.Type: ApplicationFiled: June 19, 2009Publication date: December 15, 2011Applicant: BASF SEInventors: Ralph Paulini, Delphine Breuninger, Wolfgang Von Deyn, Henricus Maria Martinus Bastiaans, Carsten Beyer, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Faraneh Oloumi
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Publication number: 20110288296Abstract: The application relates to a reagent of the general formula R1R2N—ZnY LiY??(I) wherein R1, R2 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 is other than H; Y is selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; Halon, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx; wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, orType: ApplicationFiled: February 11, 2010Publication date: November 24, 2011Inventors: Paul Knochel, Marc Mosrin
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Publication number: 20110275817Abstract: A method for producing a hydroxypyrazine derivative represented by formula (I) (wherein R1 represents a halogen atom), the method including reacting a pyrazine derivative represented by formula (III) (wherein R2 represents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group or a carboxyl group, M represents a cation capable of forming a salt, and n represents a number corresponding with the valence of M) with a halogenating agent. Also, a method for producing a dichloropyrazine derivative represented by formula (II) (wherein R21 represents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group, a carboxyl group, or a group formed as a result of a change in the functional group of R2 during chlorination), the method including reacting the hydroxypyrazine derivative (I) with a chlorinating agent.Type: ApplicationFiled: January 14, 2010Publication date: November 10, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Tamio Hara, Naoki Norimatsu, Hiroaki Kurushima, Takuya Kano
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Publication number: 20110218208Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: ApplicationFiled: June 23, 2009Publication date: September 8, 2011Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Patent number: 7994167Abstract: The present invention relates to pentafluorosulphanyl-substituted compounds, methods for their production, medicaments containing such compounds and the use of such compounds for producing medicaments.Type: GrantFiled: May 17, 2006Date of Patent: August 9, 2011Assignee: Gruenenthal GmbHInventors: Robert Frank, Bernd Sundermann, Hans Schick
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Patent number: 7960391Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: May 2, 2006Date of Patent: June 14, 2011Assignee: Bayer Cropscience AGInventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippes Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Patent number: 7872017Abstract: The invention relates to fused bicycloheterocycle substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 15, 2007Date of Patent: January 18, 2011Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li, Christopher L. Lynch, Murali Gopalakrishnan
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Publication number: 20110009418Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: ApplicationFiled: July 29, 2010Publication date: January 13, 2011Applicant: Purdue Pharma L.P.Inventor: Qun Sun
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Publication number: 20100267945Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Publication number: 20100249049Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 7, 2010Publication date: September 30, 2010Inventors: Hiroshi MIYAZAKI, Junko TSUBAKIMOTO, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAL, Tetsuya YANAGIDA, Yataka HISADA
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Patent number: 7803804Abstract: Disclosed herein are substituted pyrazine compounds and tautomers, stereoisomers, solvates, or pharmaceutically acceptable salts thereof for the treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition, including compounds of formula I:Type: GrantFiled: December 20, 2006Date of Patent: September 28, 2010Assignee: Novartis AGInventors: Stephen Paul Collingwood, Nichola Smith
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Publication number: 20100144759Abstract: The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I) wherein R1-R5 are as defined in the specification; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapyType: ApplicationFiled: December 8, 2009Publication date: June 10, 2010Applicant: AstraZeneca ABInventors: David CHESHIRE, Nicholas Kindon, Antonio Mete, Bryan Roberts
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Publication number: 20100130739Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: ASUBIO PHARMA CO., LTD.Inventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Patent number: 7691858Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as uveitis, retinopathies or macular degeneration, macular edema or other vitreoretinal diseases, inflammatory diseases such as autoimmune diseases, vascular leakage syndrome, edema, or diseases involving leukocyte activation, transplant rejection, respiratory diseases such as asthma, adult or acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease, and the like.Type: GrantFiled: April 25, 2007Date of Patent: April 6, 2010Assignee: TargeGen, Inc.Inventors: John Doukas, Chi Ching Mak, Elena Dneprovskaia, Glenn Noronha
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Publication number: 20100056534Abstract: Pesticide compositions and their use in controlling pests are provided.Type: ApplicationFiled: August 25, 2009Publication date: March 4, 2010Applicant: DOW AGROSCIENCES LLCInventors: Benjamin M. Nugent, Zoltan L. Benko, James M. Renga, Michael R. Loso, Timothy P. Martin
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Patent number: 7652010Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: October 14, 2005Date of Patent: January 26, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
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Patent number: 7615635Abstract: Novel N-formyl hydroxylamine compounds and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed.Type: GrantFiled: May 22, 2006Date of Patent: November 10, 2009Assignees: Novartis AG, Vicuron Pharmaceuticals, Inc.Inventors: Kathryn Rene Bracken, Simon Bushell, Karl Dean, Charles Francavilla, Rakesh K. Jain, Kwangho Lee, Mohindra Seepersaud, Lei Shu, Arathi Sundaram, Zhengyu Yuan
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Patent number: 7608618Abstract: Compounds of the formula wherein: Y? is O or S, W? is optionally substituted, Z? is selected from the group consisting of wherein Q? is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.Type: GrantFiled: April 27, 2005Date of Patent: October 27, 2009Assignee: Icos CorporationInventors: Edward A. Kesicki, John Joseph Gaudino, Adam Wade Cook, Scott Douglas Cowen, Laurence Edward Burgess
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20090093490Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: May 2, 2006Publication date: April 9, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippes Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Publication number: 20090088425Abstract: The present invention relates to compounds of formula I wherein A, n, R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: September 15, 2008Publication date: April 2, 2009Inventors: Jacques Bailly, Cornelia Hertel, Daniel Hunziker, Christian Lerner, Ulrike Obst Sander, Jens-Uwe Peters, Philippe Pflieger, Tanja Schulz-Gasch