Chalcogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 546/278.4)
  • Patent number: 10570091
    Abstract: 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: Grant
    Filed: June 29, 2016
    Date of Patent: February 25, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takashi Ouchi, Giho Goh, Sunmi Kim, Jinsoon Choi, Hunsoo Park
  • Patent number: 10370357
    Abstract: 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: Grant
    Filed: February 19, 2018
    Date of Patent: August 6, 2019
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventor: Keisuke Majima
  • Patent number: 9932322
    Abstract: 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: Grant
    Filed: September 15, 2016
    Date of Patent: April 3, 2018
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventor: Keisuke Majima
  • Patent number: 9732037
    Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: August 15, 2017
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Qing Jing
  • Patent number: 9556141
    Abstract: 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: Grant
    Filed: November 20, 2012
    Date of Patent: January 31, 2017
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Karsten Koerber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch
  • Patent number: 9416106
    Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: August 16, 2016
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Qing Jing
  • Patent number: 9212161
    Abstract: A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: December 15, 2015
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Fengtian Xue
  • Patent number: 9120750
    Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: September 1, 2015
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Qing Jing
  • Publication number: 20150126485
    Abstract: 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: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150126490
    Abstract: 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: Application
    Filed: October 29, 2014
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: 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
  • Publication number: 20150119378
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Inventors: Srinivasa Rao Akireddy, Scott R. Breining
  • Publication number: 20150119384
    Abstract: 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: Application
    Filed: January 6, 2015
    Publication date: April 30, 2015
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Patent number: 9018206
    Abstract: 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: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150099786
    Abstract: 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: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150065500
    Abstract: 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: Application
    Filed: September 11, 2014
    Publication date: March 5, 2015
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
  • Patent number: 8969338
    Abstract: 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: Grant
    Filed: September 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 8957213
    Abstract: 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: Grant
    Filed: April 23, 2012
    Date of Patent: February 17, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Publication number: 20150031627
    Abstract: 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: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
  • Publication number: 20150018341
    Abstract: 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: Application
    Filed: December 28, 2012
    Publication date: January 15, 2015
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • Patent number: 8927534
    Abstract: 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: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Patent number: 8927730
    Abstract: 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: Grant
    Filed: September 30, 2011
    Date of Patent: January 6, 2015
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Fengtlan Xue
  • Patent number: 8921567
    Abstract: 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 c
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 30, 2014
    Assignee: BASF SE
    Inventors: Karsten Körber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch, Markus Kordes
  • Publication number: 20140357612
    Abstract: 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: Application
    Filed: May 29, 2014
    Publication date: December 4, 2014
    Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Betsy Burton
  • Publication number: 20140343086
    Abstract: 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: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: NOVARTIS AG
    Inventors: 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
  • Publication number: 20140343070
    Abstract: 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 the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20140343083
    Abstract: 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: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8889715
    Abstract: 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: Grant
    Filed: November 2, 2012
    Date of Patent: November 18, 2014
    Assignee: Alcobra Ltd.
    Inventors: Rina Yamin, Dalia Megiddo
  • Publication number: 20140336168
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 13, 2014
    Inventor: AbbVie Inc.
  • Publication number: 20140303378
    Abstract: 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: Application
    Filed: June 12, 2014
    Publication date: October 9, 2014
    Inventors: Tomomi IKEMOTO, Hideya MIZUFUNE, Toshiaki NAGATA, Misayo SERA, Naohiro FUKUDA, Takeshi YAMASAKI
  • Patent number: 8853412
    Abstract: 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: Grant
    Filed: October 8, 2013
    Date of Patent: October 7, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Martin Bossart, Heiner Glombik, Matthias Gossel, Dieter Kadereit, Thomas Klabunde, Thomas Maier, Siegfried Stengelin
  • Publication number: 20140275087
    Abstract: 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: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: 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
  • Patent number: 8835466
    Abstract: 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: Grant
    Filed: April 20, 2007
    Date of Patent: September 16, 2014
    Assignee: Prodimed, S.A.
    Inventors: Julio Álvarez Builla Gómez, José Luis Novella Robisco, Ma Paz Matía Martín, Sonia Serna Pereda
  • Patent number: 8835640
    Abstract: 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: Grant
    Filed: May 14, 2014
    Date of Patent: September 16, 2014
    Inventor: Paresh T. Gandhi
  • Publication number: 20140256016
    Abstract: Aminopyridine compounds, as can be used in conjunction with methods for modulation of nitric oxide synthase activity.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 11, 2014
    Applicant: Northwestern University
    Inventors: Richard B. Silverman, Qing Jing
  • Patent number: 8829187
    Abstract: 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: Grant
    Filed: March 4, 2013
    Date of Patent: September 9, 2014
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Fengtian Xue
  • Patent number: 8822505
    Abstract: 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: Grant
    Filed: February 6, 2013
    Date of Patent: September 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Lilli Anselm, David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Beat Spinnler
  • Patent number: 8822503
    Abstract: 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: Grant
    Filed: April 6, 2011
    Date of Patent: September 2, 2014
    Assignees: 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
  • Patent number: 8822694
    Abstract: 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: Grant
    Filed: February 24, 2010
    Date of Patent: September 2, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tomomi Ikemoto, Misayo Sera, Naohiro Fukuda
  • Publication number: 20140235608
    Abstract: 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: Application
    Filed: September 26, 2012
    Publication date: August 21, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: John Lloyd, Jeniffer X. Qiao, Heather Finlay, James Neels, Zulan Pi, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20140235673
    Abstract: 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: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Inventors: Zulan Pi, John Llyod, Jennifer X. Qiao, Tammy C. Wang, George O. Tora
  • Publication number: 20140228578
    Abstract: A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 14, 2014
    Applicant: Northwestern University
    Inventors: Richard B. Silverman, Fengtian Xue
  • Patent number: 8802665
    Abstract: 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: Grant
    Filed: February 14, 2013
    Date of Patent: August 12, 2014
    Assignee: Genentech, Inc.
    Inventors: David Banner, Wolfgang Haap, Thomas Luebbers, Jens-Uwe Peters
  • Publication number: 20140213568
    Abstract: 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: Application
    Filed: January 22, 2014
    Publication date: July 31, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: 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
  • Patent number: 8765739
    Abstract: Compounds of formula [I]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salts or solvates thereof.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Japan Tobacco Inc.
    Inventors: Kazutaka Ikegashira, Taku Ikenogami, Naoki Ogawa, Tatsuya Matsumoto, Takahiro Oka, Takuya Matsuo, Takayuki Yamasaki
  • Patent number: 8754226
    Abstract: 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: Grant
    Filed: May 13, 2011
    Date of Patent: June 17, 2014
    Assignee: 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
  • Patent number: 8754228
    Abstract: 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: Grant
    Filed: November 7, 2012
    Date of Patent: June 17, 2014
    Inventor: Paresh T. Gandhi
  • Publication number: 20140163234
    Abstract: 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 c
    Type: Application
    Filed: August 10, 2012
    Publication date: June 12, 2014
    Applicant: BASF SE
    Inventors: Karsten Körber, Prashant Deshmukh, Florian Kaiser, Michael Rack, Timo Frassetto, Gemma Veitch, Markus Kordes
  • Publication number: 20140142082
    Abstract: 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: Application
    Filed: April 13, 2012
    Publication date: May 22, 2014
    Applicant: PHENEX PHARMACEUTICALS AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8729063
    Abstract: 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: Grant
    Filed: December 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han