Spiro Patents (Class 546/15)
  • Patent number: 10576064
    Abstract: The present invention relates to compounds of formula (I) wherein the groups R1 to R3, R7, U, V, W, X, Y, n and q are as defined herein, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases and synthetic intermediates.
    Type: Grant
    Filed: July 2, 2015
    Date of Patent: March 3, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Weinstabl, Andreas Gollner, Juergen Ramharter, Tobias Wunberg
  • Patent number: 10556882
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Grant
    Filed: July 10, 2019
    Date of Patent: February 11, 2020
    Assignees: Aragon Pharmaceuticals, Inc., Sloan-Kettering Institute For Cancer Research
    Inventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
  • Patent number: 10526310
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3,4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Grant
    Filed: April 15, 2019
    Date of Patent: January 7, 2020
    Assignees: Aragon Pharmaceuticals Inc., Sloan Kettering Institute for Cancer Research
    Inventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
  • Patent number: 10513504
    Abstract: The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1).
    Type: Grant
    Filed: March 6, 2019
    Date of Patent: December 24, 2019
    Assignee: Apotex Inc.
    Inventors: Prabhudas Bodhuri, Alfredo Paul Ceccarelli, Michael R. Emmett, Avedis Karadeolian, Fabio E. S. Souza, Gamini Weeratunga, Boris Gorin
  • Patent number: 10406139
    Abstract: The invention provides derivatives of cyclopamine having the following formula:
    Type: Grant
    Filed: March 27, 2018
    Date of Patent: September 10, 2019
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Andre B. Charette, Martin R. Tremblay
  • Patent number: 10385039
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: August 20, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • Patent number: 10351706
    Abstract: The invention relates to a near-infrared fluorescent dye and use thereof, and particularly relates to compounds represented by following Formulae A, B and C, wherein each group in the Formulae is described in the specification. Further provided are a dye composition comprising the compound represented by Formula A or Formula B, and a preparation method of the compound represented by Formula A or Formula B. The compound has a maximum absorption wavelength of 880 nm, considerably exceeding maximum absorption wavelengths of the majority of small-molecule near-infrared fluorescent dyes in the prior art. Moreover, the structure thereof does not aggregate even if the concentration thereof is excessively high, thereby having considerably high chemical stability and light stability.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: July 16, 2019
    Assignee: East China University of Science and Technology
    Inventors: Youjun Yang, Xinran Li, Zuhai Lei, Yi Li
  • Patent number: 10308630
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Grant
    Filed: May 9, 2018
    Date of Patent: June 4, 2019
    Assignees: Sloan-Kettering Institute for Cancer Research, Aragon Pharmaceuticals, Inc.
    Inventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
  • Patent number: 10239876
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein L and R1 to R5 are as described herein, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: March 26, 2019
    Assignee: Hoffman La-Roche Inc.
    Inventors: Bernd Buettelmann, Buelent Kocer, Bernd Kuhn, Marco Prunotto, Hans Richter, Martin Ritter, Markus Rudolph, Alexander Lee Satz
  • Patent number: 10196380
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: February 22, 2018
    Date of Patent: February 5, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • Patent number: 10106541
    Abstract: The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: October 23, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyoshi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch, Teresa Andreani
  • Patent number: 10030028
    Abstract: The present disclosure provides a method for efficiently producing and providing compounds having a spirooxindole skeleton, for example compounds having a spirooxindole skeleton and having antitumor activity that inhibit the interaction between Mdm2 protein and p53 protein, or intermediates thereof, using an asymmetric catalyst. Compounds having optically active tricyclic dispiroindole skeletons are obtained through catalytic asymmetric 1,3-dipolar cycloaddition reactions using ketimine as a reaction substrate and using a chiral ligand and a Lewis acid.
    Type: Grant
    Filed: September 3, 2014
    Date of Patent: July 24, 2018
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Motoshi Yamauchi, Keiji Nakayama
  • Patent number: 10005790
    Abstract: The present invention relates to compounds of formula I and a process for the synthesis: The invention further relates to a process for the synthesis of 3-carboxamide substituted morphinans where a 3-cyano substituted 6-oxo substituted morphinan is reacted with a 1,3-diol.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: June 26, 2018
    Assignee: Alkermes Pharma Ireland Limited
    Inventor: Scott Duncan
  • Patent number: 9994545
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: June 12, 2018
    Assignees: Aragon Pharmaceuticals, Inc., Sloan-Kettering Institute For Cancer Research
    Inventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
  • Patent number: 9951083
    Abstract: The invention provides derivatives of cyclopamine having the following formula:
    Type: Grant
    Filed: October 10, 2016
    Date of Patent: April 24, 2018
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Andre B. Charette, Martin R. Tremblay
  • Patent number: 9926297
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: March 27, 2018
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • Patent number: 9884871
    Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: February 6, 2018
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shoko Yoshida, Yuuichi Sugimoto
  • Patent number: 9850246
    Abstract: The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine.
    Type: Grant
    Filed: September 15, 2015
    Date of Patent: December 26, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyoshi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch, Teresa Andreani
  • Patent number: 9765074
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: September 19, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Fa-Xiang Ding, Shuzhi Dong, Dipshikha Biswas, Haifeng Tang, Jinlong Jiang, Cangming Yang, Xin Gu
  • Patent number: 9745315
    Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4'S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: August 29, 2017
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shoko Yoshida, Yuuichi Sugimoto
  • Patent number: 9725469
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: August 8, 2017
    Assignee: Amgen, Inc.
    Inventors: Ryan White, Oleg Epstein, Jason B. Human, Xiao Mei Zheng, Yuan Cheng, Kelvin Sham, Qingyian Liu, Ning Chen
  • Patent number: 9718831
    Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: August 1, 2017
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shoko Yoshida, Yuuichi Sugimoto
  • Patent number: 9718830
    Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)-N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: August 1, 2017
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shoko Yoshida, Yuuichi Sugimoto
  • Patent number: 9714252
    Abstract: The present disclosure provides cyclic sulfonamides of Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3a, R3b, and n are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. For example, compounds of the present disclosure are useful for treating pain.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: July 25, 2017
    Assignee: Purdue Pharma L.P.
    Inventor: Mark Andrew Youngman
  • Patent number: 9688655
    Abstract: Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: June 27, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Cyril Ben Haim, Andras Horvath, Johan Erwin Edmond
  • Patent number: 9676761
    Abstract: The present invention relates to difluoroethyl-oxazole substituted bridged spiro[2.4] heptane derivatives of formula (I), wherein the substituents at the piperidine ring are in trans-arrangement, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: June 13, 2017
    Assignee: ACTELION PHARMACEUTICALS, LTD.
    Inventors: Olivier Corminboeuf, Sylvaine Cren, Davide Pozzi
  • Patent number: 9650336
    Abstract: Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: May 16, 2017
    Assignee: ASTRAZENECA AB
    Inventors: Anna Minidis, Fredrik Rahm, Jenny Viklund
  • Patent number: 9540386
    Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)-N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
    Type: Grant
    Filed: May 2, 2016
    Date of Patent: January 10, 2017
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shoko Yoshida, Yuuichi Sugimoto
  • Patent number: 9499557
    Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: November 22, 2016
    Assignee: Rhodes Technologies
    Inventors: Joshua Robert Giguere, Keith Edward McCarthy, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
  • Patent number: 9481664
    Abstract: Described herein are compounds that are androgen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such androgen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon androgen receptors.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: November 1, 2016
    Assignee: Aragon Pharmaceuticals, Inc.
    Inventors: Nicholas D. Smith, Celine Bonnefous, Jackaline D. Julien
  • Patent number: 9481663
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Grant
    Filed: June 4, 2013
    Date of Patent: November 1, 2016
    Assignees: Aragon Pharmaceuticals, Inc., Sloan-Kettering Institute For Cancer Research
    Inventors: Anna Dilhas, Mark R Herbert, Ouathek Ouerfelli, Nicholas D Smith
  • Patent number: 9376436
    Abstract: The invention relates to spiro derivatives of formula (I), to the use of said derivatives in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: June 28, 2016
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: David R. Witty, David T. MacPherson, Gerard M. P. Giblin, Steven J. Stanway, Antonio K. K. Vong
  • Patent number: 9359368
    Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N—[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro [cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
    Type: Grant
    Filed: September 5, 2013
    Date of Patent: June 7, 2016
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shoko Yoshida, Yuuichi Sugimoto
  • Patent number: 9309255
    Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: April 12, 2016
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Nobuyuki Ae, Yuji Fujiwara
  • Patent number: 9303032
    Abstract: The invention relates to spiro derivative of formula (I), to the use of said derivative in treating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivative and processes for its preparation.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: April 5, 2016
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: David R. Witty, David T. MacPherson, Gerard M. P. Giblin, Steven J. Stanway
  • Patent number: 9296750
    Abstract: The present invention is directed to spirolactam analogs which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: March 29, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
  • Patent number: 9249158
    Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: February 2, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
  • Patent number: 9227972
    Abstract: The present invention is directed to aliphatic spirolactam derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical\compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: January 5, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair, Helen Mitchell
  • Patent number: 9174989
    Abstract: The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are CGRP receptor antagonists, useful for the treatment of migraine. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of Formulae B (after salt break) and C with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: November 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Chen, Carmela Molinaro, W. Peter Wuelfing, Nobuyoshi Yasuda, Jianguo Yin, Yong-Li Zhong, Joseph Lynch, Teresa Andreani
  • Patent number: 9079950
    Abstract: A composition comprising a hepatitis C virus (HCV) Envelope 2 (E2) polypeptide including a receptor binding variant, wherein the polypeptide is modified to comprise: (i) a cysteine mutated or disrupted at 2, 3, or 4 cysteines selected from C452, C486, C569, and C597; and wherein the polypeptide forms substantially fewer multimers by intermolecular disulfide bonding relative to the HCV E2 polypeptide without cysteine modification, and substantially retains CD81 binding; and various uses thereof.
    Type: Grant
    Filed: August 4, 2011
    Date of Patent: July 14, 2015
    Assignee: The Macfarlane Burnet Institute for Medical Research and Public Health Ltd
    Inventors: Heidi Drummer, Kathleen McCaffrey, Pantelis Poumbourios
  • Patent number: 9064633
    Abstract: A method for preparing a spiro quaternary ammonium system and electrolytes containing spiro quaternary ammonium cations, comprising a synthesizing step wherein a spiro ammonium system is formed in a medium that can serve as both the reaction solvent and as an electrolyte solvent.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: June 23, 2015
    Assignee: HONEYWELL INTERNATIONAL INC.
    Inventors: Alfred Siggel, Frank Nerenz, Thirumalai Palanisamy, Andrew Poss, Sonja Demel
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20150141406
    Abstract: The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 31, 2013
    Publication date: May 21, 2015
    Inventors: Hiroshi Nara, Masaki Daini, Akira Kaieda, Taku Kamei, Toshihiro Imaeda, Fumiaki Kikuchi
  • Publication number: 20150133481
    Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 14, 2015
    Applicant: Aragon Pharmaceuticals, Inc.and Sloan -Kettering Institute for Cancer Research
    Inventors: Anna Dilhas, Mark R. Herbert, Ouathek Ouerfelli, Nichola D. Smith
  • Publication number: 20150133400
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Publication number: 20150115241
    Abstract: The disclosure relates to xanthene derivatives, and electronic devices including xanthene derivatives. The electronic devices may includes an electron transporting layer or an electron injecting layer, and the electron transporting layer or the electron injecting layer may include one of the xanthene derivative.
    Type: Application
    Filed: March 28, 2013
    Publication date: April 30, 2015
    Inventors: Mike Zoellner, Jens Wutke, Omrane Fadhel, Ulrich Denker
  • Publication number: 20150118258
    Abstract: The present invention relates to fluorinated bridged spiro[2.4]heptane derivatives of formula (I), wherein n and R1 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: May 15, 2013
    Publication date: April 30, 2015
    Inventors: Olivier Corminboeuf, Davide Pozzi
  • Publication number: 20150111910
    Abstract: Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
    Type: Application
    Filed: May 22, 2013
    Publication date: April 23, 2015
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Agostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
  • Publication number: 20150111882
    Abstract: The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 23, 2015
    Applicant: Ares Trading S.A.
    Inventors: Anna Quattropani, Dominique Swinnen
  • Publication number: 20150111914
    Abstract: The present invention is directed to spirolactam analogues which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: May 3, 2013
    Publication date: April 23, 2015
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair