Chalcogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 546/278.4)
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Patent number: 10570091Abstract: The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.Type: GrantFiled: June 29, 2016Date of Patent: February 25, 2020Assignee: Takeda Pharmaceutical Company LimitedInventors: Takashi Ouchi, Giho Goh, Sunmi Kim, Jinsoon Choi, Hunsoo Park
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Patent number: 10370357Abstract: An object of the present invention is to provide a production method of an intermediate used in the production method of a sulfonylpyrrole compound useful as a pharmaceutical product. The present invention relates to a method of producing sulfonylpyrrole compound (VI) by reacting a pyridine-3-sulfonic acid compound with phosphorus pentachloride in a solvent of chlorobenzene or trifluoromethylbenzene to give a pyridine-3-sulfonyl chloride compound, reacting the compound without isolation with compound (III) to give compound (IV), and subjecting the compound (IV) to a reductive amination reaction. wherein R2 is a hydrocarbon group etc. and R3 and R4 are each a hydrogen atom etc., wherein R2 is an optionally substituted pyridin-3-yl group, and the other symbols are as defined above, wherein R5 is an alkyl group and the other symbols are as defined above.Type: GrantFiled: February 19, 2018Date of Patent: August 6, 2019Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: Keisuke Majima
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Patent number: 9932322Abstract: An object of the present invention is to provide a production method of an intermediate used in the production method of a sulfonylpyrrole compound useful as a pharmaceutical product. The present invention relates to a method of producing sulfonylpyrrole compound (VI) by reacting a pyridine-3-sulfonic acid compound with phosphorus pentachloride in a solvent of chlorobenzene or trifluoromethylbenzene to give a pyridine-3-sulfonyl chloride compound, reacting the compound without isolation with compound (III) to give compound (IV), and subjecting the compound (IV) to a reductive amination reaction. wherein R2 is a hydrocarbon group etc. and R3 and R4 are each a hydrogen atom etc., wherein R1 is an optionally substituted pyridin-3-yl group, and the other symbols are as defined above, wherein R5 is an alkyl group and the other symbols are as defined above.Type: GrantFiled: September 15, 2016Date of Patent: April 3, 2018Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: Keisuke Majima
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Patent number: 9732037Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.Type: GrantFiled: August 15, 2016Date of Patent: August 15, 2017Assignee: Northwestern UniversityInventors: Richard B. Silverman, Qing Jing
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Patent number: 9556141Abstract: The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carboxylate compound of the formula (I-A) comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined in the description and the claims, with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a carbonylation by reacting it with a reagent selected from the group consisting carbon dioxide or a carbon dioxide equivalent, to obtain a compound of formula (I-A); and it relates to further conversions to yield a N-substituted 1H-pyrazole-5-carbonyl chloride compound of the formula (I)Type: GrantFiled: November 20, 2012Date of Patent: January 31, 2017Assignee: BASF SEInventors: Maximilian Dochnahl, Karsten Koerber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch
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Patent number: 9416106Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.Type: GrantFiled: August 31, 2015Date of Patent: August 16, 2016Assignee: Northwestern UniversityInventors: Richard B. Silverman, Qing Jing
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Chiral synthesis of pyrrolidine core compounds en route to neuronal nitric oxide synthase inhibitors
Patent number: 9212161Abstract: A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.Type: GrantFiled: April 14, 2014Date of Patent: December 15, 2015Assignee: Northwestern UniversityInventors: Richard B. Silverman, Fengtian Xue -
Patent number: 9120750Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.Type: GrantFiled: March 6, 2014Date of Patent: September 1, 2015Assignee: Northwestern UniversityInventors: Richard B. Silverman, Qing Jing
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Publication number: 20150126485Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 9, 2013Publication date: May 7, 2015Applicant: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Publication number: 20150126490Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.Type: ApplicationFiled: October 29, 2014Publication date: May 7, 2015Applicant: Novartis AGInventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
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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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Publication number: 20150119384Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor 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 can be used for the treatment of schizophrenia or cognitive disorders.Type: ApplicationFiled: January 6, 2015Publication date: April 30, 2015Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9018206Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: September 12, 2012Date of Patent: April 28, 2015Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150099786Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150065500Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 11, 2014Publication date: March 5, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
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Patent number: 8969338Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: GrantFiled: September 27, 2012Date of Patent: March 3, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 8957213Abstract: The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined herein or 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 can be used for the treatment of schizophrenia or cognitive disorders.Type: GrantFiled: April 23, 2012Date of Patent: February 17, 2015Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150031627Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 25, 2014Publication date: January 29, 2015Applicant: AGIOS PHARMACEUTICALS, INCInventors: Rene M. Lemieux, Janeta Popovici-Muller, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
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Publication number: 20150018341Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
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Patent number: 8927730Abstract: Compounds and related compositions and methods as can be used to selectively inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.Type: GrantFiled: September 30, 2011Date of Patent: January 6, 2015Assignee: Northwestern UniversityInventors: Richard B. Silverman, Fengtlan Xue
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Patent number: 8927534Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.Type: GrantFiled: January 31, 2007Date of Patent: January 6, 2015Assignee: Shire Orphan Therapies GmbHInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Patent number: 8921567Abstract: The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carbonylchloride compound of the formula (I) in which R1 is hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, C1-C4-fluoroalkoxy-C1-C4-alkyl, phenyl and the like; each R2 is independently selected from halogen, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, phenyl and the like; r is 0, 1, 2, 3 or 4; comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined above, with a base selected from lithium-organic base having a carbon or nitrogen bound lithium or with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a chlorocarbonylation by reacting it with a reagent selected from the group cType: GrantFiled: August 10, 2012Date of Patent: December 30, 2014Assignee: BASF SEInventors: Karsten Körber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch, Markus Kordes
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Publication number: 20140357612Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: May 29, 2014Publication date: December 4, 2014Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Betsy Burton
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Publication number: 20140343086Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Applicant: NOVARTIS AGInventors: Stephanie Kay DODD, Pascal FURET, Robert Martin GROTZFELD, Wolfgang JAHNKE, Darryl Brynley JONES, Paul William MANLEY, Andreas MARZINZIK, Xavier Francois Andre PELLE, Bahaa SALEM, Joseph SCHOEPFER
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Publication number: 20140343070Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug theType: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Publication number: 20140343083Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.Type: ApplicationFiled: May 12, 2014Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8889715Abstract: The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption.Type: GrantFiled: November 2, 2012Date of Patent: November 18, 2014Assignee: Alcobra Ltd.Inventors: Rina Yamin, Dalia Megiddo
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Publication number: 20140336168Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: May 10, 2013Publication date: November 13, 2014Inventor: AbbVie Inc.
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Publication number: 20140303378Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.Type: ApplicationFiled: June 12, 2014Publication date: October 9, 2014Inventors: Tomomi IKEMOTO, Hideya MIZUFUNE, Toshiaki NAGATA, Misayo SERA, Naohiro FUKUDA, Takeshi YAMASAKI
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Patent number: 8853412Abstract: The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: GrantFiled: October 8, 2013Date of Patent: October 7, 2014Assignee: SanofiInventors: Lothar Schwink, Martin Bossart, Heiner Glombik, Matthias Gossel, Dieter Kadereit, Thomas Klabunde, Thomas Maier, Siegfried Stengelin
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Publication number: 20140275087Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: March 17, 2014Publication date: September 18, 2014Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
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Patent number: 8835466Abstract: Novel pyroglutamic acid derivatives (I), wherein R1 is —OH, —ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group which hydrolyzes under acidic conditions or phtalamide; X is a pharmaceutically acceptable anion; and Y is a N-containing group; either in the form of their isolated optically active stereoisomers or in the form of mixtures thereof, are useful compounds for enhancing an immuneresponse in a subject and/or for treating tumors, bacterial, fungal or viral infections, or autoimmune diseases.Type: GrantFiled: April 20, 2007Date of Patent: September 16, 2014Assignee: Prodimed, S.A.Inventors: Julio Álvarez Builla Gómez, José Luis Novella Robisco, Ma Paz Matía Martín, Sonia Serna Pereda
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Patent number: 8835640Abstract: Described are novel nicotine derivatives represented by general formulas (I) and (III), and salts thereof, and herbicide & pharmaceutical compositions containing the same as the active ingredient. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose. The compounds and salts thereof can be useful as an anti-microbial and anti-fungal agents and also for the treatment of blood pressure, skeletal muscle, attention deficit disorder, mental disorders, schizophrenia, Alzheimer disease, Parkinson's disease and depression. Also described is the preparation of the nicotine derivatives having formula (I) and (III).Type: GrantFiled: May 14, 2014Date of Patent: September 16, 2014Inventor: Paresh T. Gandhi
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Publication number: 20140256016Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Northwestern UniversityInventors: Richard B. Silverman, Qing Jing
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Patent number: 8829187Abstract: Diastereomeric pyrrolidine compounds and methods of preparation, as can be used en route to the preparation of a range of nitric oxide synthase inhibitors.Type: GrantFiled: March 4, 2013Date of Patent: September 9, 2014Assignee: Northwestern UniversityInventors: Richard B. Silverman, Fengtian Xue
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Patent number: 8822694Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.Type: GrantFiled: February 24, 2010Date of Patent: September 2, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Tomomi Ikemoto, Misayo Sera, Naohiro Fukuda
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Patent number: 8822503Abstract: A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.Type: GrantFiled: April 6, 2011Date of Patent: September 2, 2014Assignees: Taisho Pharmaceutical Co., Ltd, Nissan Chemical Industries, Ltd.Inventors: Takanori Kawaguchi, Kengo Watatani, Keiko Fusegi, Masahiro Bohno, Hajime Asanuma, Shoichi Kuroda, Yudai Imai, Tomomichi Chonan, Nagaaki Sato, Shigeru Tokita, Shigetada Sasako, Takumi Okada, Keishi Hayashi, Shin Itoh, Noriko Saito, Rui Jibiki, Seishi Ishiyama, Hirofumi Ota
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Patent number: 8822505Abstract: The invention relates to a compound of formula (I) wherein A1, A2 and R1 to R8 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: February 6, 2013Date of Patent: September 2, 2014Assignee: Genentech, Inc.Inventors: Lilli Anselm, David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Beat Spinnler
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Publication number: 20140235608Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 26, 2012Publication date: August 21, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: John Lloyd, Jeniffer X. Qiao, Heather Finlay, James Neels, Zulan Pi, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140235673Abstract: The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 24, 2012Publication date: August 21, 2014Inventors: Zulan Pi, John Llyod, Jennifer X. Qiao, Tammy C. Wang, George O. Tora
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Chiral Synthesis of Pyrrolidine Core Compounds en route to Neuronal Nitric Oxide Synthase Inhibitors
Publication number: 20140228578Abstract: A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.Type: ApplicationFiled: April 14, 2014Publication date: August 14, 2014Applicant: Northwestern UniversityInventors: Richard B. Silverman, Fengtian Xue -
Patent number: 8802665Abstract: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: February 14, 2013Date of Patent: August 12, 2014Assignee: Genentech, Inc.Inventors: David Banner, Wolfgang Haap, Thomas Luebbers, Jens-Uwe Peters
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Publication number: 20140213568Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 22, 2014Publication date: July 31, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8778977Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: GrantFiled: July 2, 2007Date of Patent: July 15, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Patent number: 8765739Abstract: Compounds of formula [I]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salts or solvates thereof.Type: GrantFiled: May 14, 2010Date of Patent: July 1, 2014Assignee: Japan Tobacco Inc.Inventors: Kazutaka Ikegashira, Taku Ikenogami, Naoki Ogawa, Tatsuya Matsumoto, Takahiro Oka, Takuya Matsuo, Takayuki Yamasaki
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Patent number: 8754228Abstract: Described are novel nicotine derivatives represented by general formulas (I) and (III), and salts thereof, and herbicide & pharmaceutical compositions containing the same as the active ingredient. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose. The compounds and salts thereof can be useful as an anti-microbial and anti-fungal agents and also for the treatment of blood pressure, skeletal muscle, attention deficit disorder, mental disorders, schizophrenia, Alzheimer disease, Parkinson's disease and depression. Also described is the preparation of the nicotine derivatives having formula (I) and (III).Type: GrantFiled: November 7, 2012Date of Patent: June 17, 2014Inventor: Paresh T. Gandhi
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Patent number: 8754226Abstract: 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: GrantFiled: May 13, 2011Date of Patent: June 17, 2014Assignee: Array BioPharma Inc.Inventors: 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, David A. Mareska, Steven Armen Boyd
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Publication number: 20140163234Abstract: The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carbonylchloride compound of the formula (I) in which R1 is hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, C1-C4-fluoroalkoxy-C1-C4-alkyl, phenyl and the like; each R2 is independently selected from halogen, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, phenyl and the like; r is 0, 1, 2, 3 or 4; comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined above, with a base selected from lithium-organic base having a carbon or nitrogen bound lithium or with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a chlorocarbonylation by reacting it with a reagent selected from the group cType: ApplicationFiled: August 10, 2012Publication date: June 12, 2014Applicant: BASF SEInventors: Karsten Körber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch, Markus Kordes
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Publication number: 20140142082Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: PHENEX PHARMACEUTICALS AGInventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Patent number: 8729063Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: December 20, 2012Date of Patent: May 20, 2014Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han