Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Five Membered Hetero Ring (e.g., Pyrrole Carbonyl Halides, Pyrrole Carboxaldehyde, Etc.) Patents (Class 548/530)
  • Patent number: 10577318
    Abstract: The present invention is directed to novel intermediates of the formula E: which are useful in the synthesis of agonists of g-protein coupled receptor 43 for treating and/or preventing metabolic diseases.
    Type: Grant
    Filed: June 18, 2019
    Date of Patent: March 3, 2020
    Assignee: Epics Therapeutics
    Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
  • Patent number: 10513490
    Abstract: The invention relates to a method for producing compounds of formula (Ia), in particular to a method for producing N-[4-(cyclopropylcarbamoyl)phenylsulfonyl]-2-methoxybenzamide.
    Type: Grant
    Filed: April 4, 2016
    Date of Patent: December 24, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Taraneh Farida, Michael Esser, Hubertus Stakemeier
  • Patent number: 10358416
    Abstract: The present invention is directed to a process for the preparation of aryl-carbonyl-pyrrolidine carboxylic acid derivative compounds which are useful in treating metabolic diseases, said process consisting of coupling a pyrrolidine ester compound with an aryl carboxylic acid derivative, followed by alkaline or acidic treatment, hydrogenolysis or treatment with a fluoride of the obtained intermediate, to afford novel aryl-carbonyl-pyrrolidine carboxylic acid derivative compounds.
    Type: Grant
    Filed: June 20, 2018
    Date of Patent: July 23, 2019
    Assignee: Epics Therapeutics
    Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
  • Patent number: 10017468
    Abstract: The present invention is directed to a process for the preparation of aryl-pyrrolidine carboxylic acid derivative compounds which are useful in treating metabolic diseases, said process consisting of coupling an aryl-pyrrolidine compound with an aryl carboxylic acid compound followed by alkaline or acidic treatment, hydrogenolysis or treatment with a fluoride of the ester intermediate to afford novel aryl-pyrrolidine carboxylic acid derivative compounds.
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: July 10, 2018
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
  • Publication number: 20140301948
    Abstract: The compounds and the synthesis of [F-18]-labeled L-glutamic acid, [F-18]-labeled L-glutamate, their derivatives as set forth in formula (I) and their uses are described.
    Type: Application
    Filed: January 13, 2014
    Publication date: October 9, 2014
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Ludger DINKELBORG, Matthias FRIEBE, Nikolaevna Raisa KRASIKOWA, Yuri BELOKON, Fedorovna Olga KUZNETSOVA, Keith GRAHAM, Lutz LEHMANN, Mathias BERNDT
  • Patent number: 8785475
    Abstract: Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: July 22, 2014
    Assignee: Cornerstone Pharmaceuticals, Inc.
    Inventors: Paul Bingham, Tom Kwok, Zuzana Zachar
  • Patent number: 8759365
    Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: June 24, 2014
    Assignee: Novartis AG
    Inventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori
  • Patent number: 8747809
    Abstract: The present invention is directed single diasteromers of 4-fluoroglutamine having a diastereomeric excess of at least 80%. Methods of preparing the single diastereomers are also described, as well as methods of using the single diastereomers of radiolabeled 4-fluoroglutamine as imaging agent is also described.
    Type: Grant
    Filed: August 13, 2010
    Date of Patent: June 10, 2014
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Hank F. Kung, Craig B. Thompson, Wenchao Qu, Karl Ploessl
  • Patent number: 8748430
    Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: June 10, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Patent number: 8680102
    Abstract: The subject of the invention is compounds of formula (I): in which R1-R10 are as defined within, the method of preparation and therapeutic application as cannabinoid CB1 receptor antagonists.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: March 25, 2014
    Assignee: Sanofi
    Inventors: Francis Barth, Daniel Bichon, Murielle Rinaldi-Carmona, Christian Congy
  • Patent number: 8673911
    Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: March 18, 2014
    Assignee: MethylGene Inc.
    Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
  • Patent number: 8664255
    Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: March 4, 2014
    Assignee: The Texas A&M University System
    Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
  • Publication number: 20140056880
    Abstract: The present invention provides triazole compounds of Formula I: as further described herein. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, and a method of treating a disorder mediated, at least in part, by KSP in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of a compound of Formula I.
    Type: Application
    Filed: August 28, 2013
    Publication date: February 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Tinya Abrams, Paul Barsanti, Yu Ding, David Duhl, Wooseok Han, Cheng Hu, Yue Pan
  • Patent number: 8642634
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: February 4, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Robert James Pasteris, Mary Ann Hanagan
  • Publication number: 20140031549
    Abstract: This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.
    Type: Application
    Filed: October 1, 2013
    Publication date: January 30, 2014
    Applicant: OPKO Health, Inc.
    Inventors: George G. Wu, Gerald Werne, Xiaoyong Fu, Robert K. Orr, Frank Xing Chen, Jian Cui, Victoria M. Sprague, Fucheng Zhang, Ji Xie, Liansheng Zeng, Louis Peter Castellanos, Yuyin Chen, Marc Poirier, Ingrid Mergelsberg
  • Patent number: 8609659
    Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: December 17, 2013
    Assignee: Neuroscienze Pharmaness S.C.A.R.L.
    Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Gabriele Murineddu, Luca Pani, Gerard Aime Pinna
  • Patent number: 8551364
    Abstract: A process for inhibiting polymerization of an aromatic vinyl compound during the stage of producing, purifying, storing or transporting the aromatic vinyl compound which not only inhibits an initial polymerization but also inhibits polymerization efficiently over a long period of time and which is excellent in handleability. The process involves the step of adding a nitrogenous aromatic compound in combination with a sulfonic acid compound to the aromatic vinyl compound during the production, purification, storage of transportation thereof.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: October 8, 2013
    Assignee: Hakuto Co., Ltd.
    Inventors: Junichi Nakajima, Seiji Tanizaki
  • Patent number: 8512879
    Abstract: A polymer useful in an optoelectronic device comprises structural unit of formula I: wherein R1 is, independently at each occurrence, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; a is, independently at each occurrence, an integer ranging from 0-4; Ar1 is aryl or heteroaryl; Ar2 is fluorene; R2 is alkylene, substituted alkylene, oxaalkylene, CO, or CO2; R3, R4 and R5 are independently hydrogen, alkyl, alkoxy, alkylaryl, aryl, arylalkyl, heteroaryl, substituted alkyl; substituted alkoxy, substituted alkylaryl, substituted aryl, substituted arylalkyl, or substituted heteroaryl; and L is derived from phenylpyridine, tolylpyridine, benzothienylpyridine, phenylisoquinoline, dibenzoquinozaline, fluorenylpyridine, ketopyrrole, 2-(1-naphthyl)benzoxazole)), 2-phenylbenzoxazole, 2 phenylbenzothiazole, coumarin, thienylpyridine, phenylpyridine, benzothienylpyridine, 3 methoxy-2-phenylpyridine, thienylpyridine, phenylimine, vinylpyridine, pyridylnaphthalene, pyridylpyrro
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: August 20, 2013
    Assignee: General Electric Company
    Inventors: Qing Ye, Jie Lu, Kelly Scott Chichak
  • Patent number: 8497263
    Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: July 30, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
  • Publication number: 20130137018
    Abstract: The invention provides a dye compound having a partial structure represented by the following formula (5): wherein in formula (5), Dye represents a dye structure; G1 represents NR or an oxygen atom; G2 represents a monovalent substituent group having an ?Es? value as a steric parameter of 1.5 or more; p represents an integer from 1 to 8; when p is 2 or greater, the two or more structures represented by p may be the same or different from each other; and R represents a hydrogen atom or a monovalent substituent group.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: FUJIFILM CORPORATION
    Inventor: FUJIFILM CORPORATION
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8399504
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: March 19, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
  • Patent number: 8383666
    Abstract: The subject of the invention is Compound of Formula (I): in which R1-R8 and R10 are defined within, its method of preparation, and its therapeutic application.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: February 26, 2013
    Assignee: Sanofi
    Inventors: Francis Barth, Audrey Jeanjean, Murielle Rinaldi-Carmona, Christian Congy
  • Patent number: 8372982
    Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: February 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
  • Patent number: 8354444
    Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, R5, R6 and R7 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: January 15, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Jing Zhang, Zhuming Zhang
  • Patent number: 8349215
    Abstract: The invention relates to the use of salts of compound of the formula (1) and amines of the formula (2), where R1 means C8- to C30-Alkyl or C8- to C30-Alkenyl, R2 means hydrogen or a group of the formula -(A-O)x—H, R3, R4 mean hydrogen, C1- to C4-Alkyl or a group of the formula -(A-O)x—H, A means C2- to C4-Alkylene, and x means a number from 1 to 10, as water-soluble or water-dispersible corrosion inhibitors.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: January 8, 2013
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Dirk Leinweber, Alexander Roesch, Michael Feustel
  • Patent number: 8344161
    Abstract: The invention relates to a novel process for the preparation of (3S,4S)- or (3R,4R)-1-benzyl-4-(halogen-aryl)-pyrrolidine-3-carboxylic acids of formula I or salts thereof, wherein X and Y are each independently hydrogen or a halogen atom, with the proviso that at least one of X or Y is a halogen atom. The compounds of formula I are useful as starting materials or intermediates for the preparation of pharmaceutically active compounds, especially for compounds, which are useful for the treatment of central nervous system disorders.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: January 1, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fabienne Hoffmann-Emery, Kurt Puentener, Hasane Ratni
  • Patent number: 8338620
    Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, the invention relates to a process for the manufacture of a compound of the formula I, or a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.
    Type: Grant
    Filed: April 1, 2008
    Date of Patent: December 25, 2012
    Assignee: Novartis AG
    Inventor: Gottfried Sedelmeier
  • Patent number: 8304561
    Abstract: A method of making a metalloporphyrin is carried out by reacting (i) a linear tetrapyrrole, said linear tetrapyrrole having a 19-acyl group and a 1-protecting group, with (ii) a metal salt under basic conditions to produce the metalloporphyrin. Products produced by such methods and intermediates useful for carrying out such methods are also described.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: November 6, 2012
    Assignee: North Carolina State University
    Inventors: Jonathan S. Lindsey, Dilek Dogutan Kiper
  • Patent number: 8293770
    Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: October 23, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angelique Patiny-Adam, Hasane Ratni, Claus Riemer
  • Patent number: 8273901
    Abstract: Disclosed is a process of forming a pyrrole compound. The process comprises contacting an ?-carbonyl oxime compound 1 and an ?,?-unsaturated aldehyde 2 R1 and R2 in compound 1 are independently selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. R3 in aldehyde 2 is selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. The ?-carbonyl oxime compound 1 an the ?,?-unsaturated aldehyde 2 are contacted in a suitable solvent in the presence of a secondary amine.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: September 25, 2012
    Assignee: Nanyang Technical University
    Inventors: Guofu Zhong, Bin Tan, Zugui Shi, Pei Juan Chua
  • Patent number: 8252923
    Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: August 28, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
  • Patent number: 8226966
    Abstract: The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3 and B represents an aromatic, 6-membered, fused, (hetero)aryl; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: July 24, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Philippe Desbordes, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
  • Patent number: 8207220
    Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: June 26, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Patent number: 8203003
    Abstract: Novel 4-fluoropyrrolidine-2-carbonyl fluoride compounds as useful fluorinated intermediates are disclosed. Their preparative methods are also disclosed. Useful applications of the 4-fluoropyrrolidine-2-carbonyl fluorides are shown.
    Type: Grant
    Filed: January 8, 2010
    Date of Patent: June 19, 2012
    Assignee: UBE Industries, Ltd.
    Inventors: Teruo Umemoto, Rajendra P. Singh
  • Publication number: 20120142930
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Application
    Filed: December 21, 2011
    Publication date: June 7, 2012
    Inventors: Josep CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
  • Patent number: 8178533
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: May 15, 2012
    Assignee: UCB Pharma, S.A.
    Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
  • Patent number: 8115016
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: February 14, 2012
    Assignee: Novartis AG
    Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar M Waykole
  • Patent number: 8093379
    Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: January 10, 2012
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Adel Moussa, Benjamin Alexander Mayes, Elodie Rosinovsky, Alistair Stewart
  • Patent number: 8076330
    Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: December 13, 2011
    Assignee: Amgen Inc.
    Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochgürtel, Fritz-Frieder Frickel, Arthur G. Taveras, Christoph Steeneck
  • Patent number: 8071787
    Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 6, 2011
    Assignee: National Health Research Institutes
    Inventors: Weir-Tong Jiaang, Xin Chen
  • Patent number: 8063045
    Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
    Type: Grant
    Filed: February 1, 2010
    Date of Patent: November 22, 2011
    Assignee: Sanofi-Aventis
    Inventors: Peter Aranyi, Laszlo Balazs, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Karoly Kanai, Zoltan Kapui, Edit Susan, Tibor Szabo, Lajos T. Nagy, Katalin Urban-Szabo, Marton Varga
  • Patent number: 8063075
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R?, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
  • Patent number: 8053465
    Abstract: Summary Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. Solving Means The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: November 8, 2011
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Kohei Ohata, Kazuya Yokota, Koji Murakami, Toshiyuki Matsui
  • Patent number: 8048907
    Abstract: The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: November 1, 2011
    Assignee: Glaxo Group Limited
    Inventors: Laura J Chambers, Robert Gleave, Stefan Senger, Daryl Simon Walter
  • Patent number: 8039507
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt or a prodrug thereof; wherein Y, A, X, R and D are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: October 18, 2011
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Patent number: 7982053
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: July 19, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Michael Axten, Jesus R. Medina
  • Patent number: 7977372
    Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: July 12, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
  • Patent number: 7968542
    Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: June 28, 2011
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Katsuaki Miyaji, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
  • Patent number: 7968591
    Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: June 28, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies