The Spiro Includes The Six-membered Hetero Ring Patents (Class 546/16)
  • Patent number: 10259812
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2 and R3 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: April 16, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Patent number: 10093672
    Abstract: A process for making certain spiroheterocyclic pyrrolidine dione derivatives.
    Type: Grant
    Filed: April 20, 2018
    Date of Patent: October 9, 2018
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Edouard Godineau, Tomas Smejkal, Sophie Pelletier, Michel Muehlebach, Régis Jean Georges Mondiere, Helmars Smits, Jochen Weckesser, Alan James Robinson
  • Patent number: 9969734
    Abstract: A process for making certain spiroheterocyclic pyrrolidine dione derivatives.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: May 15, 2018
    Assignee: Syngenta Participations AG
    Inventors: Edouard Godineau, Tomas Smejkal, Sophie Pelletier, Michel Muehlebach, Regis Jean Georges Mondiere, Helmars Smits, Jochen Weckesser, Alan James Robinson
  • Patent number: 9951084
    Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (1) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: April 24, 2018
    Assignees: Abb Vie B.V., Abb Vie, Inc.
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Maria J. P. van Dongen, Nicolas J.-L. D. Leflemme, Adrian Hobson
  • Patent number: 9834541
    Abstract: The invention provides novel substituted 2-aminopyridine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
    Type: Grant
    Filed: October 2, 2013
    Date of Patent: December 5, 2017
    Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, MERCK PATENT GMBH
    Inventors: Kai Schiemann, Frank Stieber, Julian Blagg, Aurelie Mallinger, Dennis Waalboer, Christian Rink, Simon Ross Crumpler
  • Patent number: 9822116
    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: Grant
    Filed: February 1, 2016
    Date of Patent: November 21, 2017
    Assignee: 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: 9809542
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the spiroheterocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular spiroheterocyclically substituted tetramic acid derivatives through the addition of ammonium or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or fungicides and/or for preventing unwanted vegetation.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: November 7, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Reiner Fischer, Arnd Voerste, Isolde Häuser-Hahn, Stefan Lehr, Elmar Gatzweiler, Ulrich Görgens, Ines Heinemann
  • Patent number: 9802935
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2 and R3 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: October 31, 2017
    Assignee: Heptares Therapeutics Limited
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Patent number: 9750745
    Abstract: The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
    Type: Grant
    Filed: February 15, 2017
    Date of Patent: September 5, 2017
    Assignee: REMYND NV
    Inventors: Gerard Griffioen, Bart De Taeye, Katrien Princen, Koen De Witte, Emilie Blanche, Hasane Ratni, Mark Rogers-Evans
  • Patent number: 9617264
    Abstract: The present invention relates to a compound of formula (I) or a stereoisomer, enantiomer, racemic, or tautomer thereof, Formula (I), wherein R1, R3, R4, L1, L2, L3, L4, and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: April 11, 2017
    Assignee: REMYND NV
    Inventors: Gerard Griffioen, Bart De Taeye, Katrien Princen, Koen De Witte, Emilie Blanche, Hasane Ratni, Mark Rogers-Evans
  • Patent number: 9593129
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Grant
    Filed: January 27, 2016
    Date of Patent: March 14, 2017
    Assignee: Amgen, Inc.
    Inventors: Michael D. Bartberger, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Duquette, John Eksterowicz, Benjamin Fisher, Brian M. Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael W. Gribble, Jr., Darin J. Gustin, Julie A. Heath, Xin Huang, XianYun Jiao, Michael G. Johnson, Frank Kayser, David John Kopecky, SuJen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan D. Low, Brian S. Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin L. McMinn, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yosup Rew, Philip M. Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • Patent number: 9493486
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: November 15, 2016
    Assignee: Hoffmann-La Roches Inc.
    Inventors: Daniel Hunziker, Patrizio Mattei, Harald Mauser, Marco Prunotto, Christoph Ullmer
  • Patent number: 9403839
    Abstract: The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: August 2, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Vijayalaksmi Arumugam, Michael Paul Deninno, Bryan A. Frieman, Edward Adam Kallel, Mark Thomas Miller, Johnny Uy, Jinglan Zhou
  • Patent number: 9249144
    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: Grant
    Filed: October 1, 2013
    Date of Patent: February 2, 2016
    Assignee: 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: 9067892
    Abstract: A compound of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: June 30, 2015
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Michel Muehlebach, Thomas Pitterna, Jerome Yves Cassayre, Andrew Edmunds, Camilla Corsi, Myriem El Qacemi, Roger Graham Hall, Andre Jeanguenat, Andre Stoller, Christopher Richard Godfrey, Jurgen Harry Schaetzer, Olivier Loiseleur, Peter Maienfisch, Neil Brian Carter
  • Patent number: 9061016
    Abstract: A liquid composition that is an aqueous solution of a compound of formula (I), wherein the aqueous solution has a pH from about 3.0 to about 5.0. The liquid composition may be used in the treatment of a disorder selected from hyperproliferative diseases, autoimmune diseases and heart diseases.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: June 23, 2015
    Assignee: APREA AB
    Inventors: Styrbjorn Bystrom, Charlotta Liljebris, Ninus Caram-Lelham
  • Publication number: 20150148363
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) for the treatment of diabetes, metabolic syndrome and obesity.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 28, 2015
    Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
  • Patent number: 9034891
    Abstract: There are provided certain bicyclic heterocyclic compounds that act as M1 muscarinic receptor modulators. Compositions containing these compounds and their use are also disclosed.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: May 19, 2015
    Assignee: ISRAEL INSTITUTE FOR BIOLOGICAL RESEARCH
    Inventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
  • Patent number: 9023760
    Abstract: A compound of the formula (1) wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: May 5, 2015
    Assignee: Syngenta Participations AG
    Inventors: Michel Muehlebach, Jürgen Harry Schaetzer
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150105548
    Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.
    Type: Application
    Filed: May 25, 2012
    Publication date: April 16, 2015
    Inventors: Allan Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
  • Patent number: 9005578
    Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.
    Type: Grant
    Filed: May 28, 2013
    Date of Patent: April 14, 2015
    Assignees: Fluoropharma, Inc., The General Hospital Corporation
    Inventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
  • Patent number: 9006260
    Abstract: The present invention relates to certain spirocyclic compounds that are inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 (11?HSD1), compositions containing the same, and methods of using the same for the treatment of diabetes, obesity and other diseases.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 14, 2015
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Colin Zhang
  • Patent number: 9006442
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Lupin Limited
    Inventors: Sanjeev Anant Kulkarni, Sachin Madan, Nirmal Kumar Jana, Prashant Vitthalrao Tale, Narasimha Murthy Cheemala, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Chaitanya Prabhakar Kulkarni, Sapana Suresh Patel, Amolsing Dattu Patil, Seema Prabhakar Zade, Rohan Mahadev Shinde, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150099734
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20150080393
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Publication number: 20150065477
    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.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 5, 2015
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • 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: 8927715
    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 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: August 24, 2007
    Date of Patent: January 6, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Salvacion Cacatian, Wei He, Robert Simpson, Zhenrong Xu, Wei Zhao
  • Publication number: 20150005304
    Abstract: The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: January 15, 2013
    Publication date: January 1, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Vijayalaksmi Arumugam, Michael Paul Deninno, Bryan A. Frieman, Edward Adam Kallel, Mark Thomas Miller, Johnny Uy, Jinglan Zhou
  • Patent number: 8921551
    Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: December 30, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Nobuyuki Ae, Yuji Fujiwara
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Publication number: 20140371199
    Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
    Type: Application
    Filed: April 1, 2013
    Publication date: December 18, 2014
    Applicant: Agency for Science, Technology and Research
    Inventors: Kassoum Nacro, Athisayamani Jeyaraj Duraiswamy, Lohitha Rao
  • Publication number: 20140371455
    Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Beth Adams Norton
  • Patent number: 8907098
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the meanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: December 9, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Frank Stieber, Dirk Wienke
  • Publication number: 20140350015
    Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 27, 2014
    Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
  • Publication number: 20140350005
    Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.
    Type: Application
    Filed: February 19, 2014
    Publication date: November 27, 2014
    Inventors: GARY W. LUEHR, ARATHI SUNDARAM, PRIYADARSHINI JAISHANKAR, PHILIP W. PAYNE, PASCAL DRUZGALA
  • Patent number: 8895750
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: November 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Michael J. Burke, Darren Disalvo, Wang Mao, John Westbrook
  • Publication number: 20140343277
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Application
    Filed: June 25, 2014
    Publication date: November 20, 2014
    Inventors: Shinichi TAIRA, Kunio OSHIMA, Takashi OSHIYAMA, Yasuhiro MENJO, Yasuo KOGA, Hokuto YAMABE, Sunao NAKAYAMA, Kenji TSUJIMAE, Toshiyuki ONOGAWA, Kuninori TAI, Motohiro ITOTANI
  • Patent number: 8889702
    Abstract: The invention relates to a compound of the general formula (I) in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, NR8R9 group; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-member heterocyclic compound; the compound being in the form of a base or acid addition salt. The invention also relates to the therapeutic use thereof.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: November 18, 2014
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
  • Publication number: 20140336158
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Publication number: 20140329986
    Abstract: The Michael reaction is employed, for example, to condense methyl acrylate with diethyl malonate to prepare the corresponding tetra-ester. Subsequent reaction with primary amines followed by thermal condensation results in spiroimides. A similar series of reaction steps can be performed starting with malonamides.
    Type: Application
    Filed: May 1, 2013
    Publication date: November 6, 2014
    Inventor: Robert Bernard Login
  • Patent number: 8877743
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: November 4, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Publication number: 20140323468
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: April 28, 2014
    Publication date: October 30, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael BALESTRA, Jennifer BURKE, Zhidong CHEN, Derek COGAN, Lee FADER, Xin GUO, Bryan MCKIBBEN, Daniel Richard MARSHALL, Peter Allen NEMOTO, Hui YU
  • Publication number: 20140323470
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
  • Patent number: 8871210
    Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: October 28, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaya Kokubo, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
  • Publication number: 20140315876
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 12, 2014
    Publication date: October 23, 2014
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Publication number: 20140315912
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).
    Type: Application
    Filed: July 18, 2011
    Publication date: October 23, 2014
    Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson