Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/523)
  • Patent number: 9884844
    Abstract: Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Grant
    Filed: December 31, 2013
    Date of Patent: February 6, 2018
    Assignee: SUNOVION PHARMACEUTICALS, INC.
    Inventors: Qun Kevin Fang, Una Campbell, Kerry L. Spear
  • Patent number: 9440924
    Abstract: The present invention relates to a novel solvate of ivabradine hydrochloride, a process of its preparation and its use for the preparation of specific polymorphic forms of ivabradine hydrochloride.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: September 13, 2016
    Assignee: SANDOZ AG
    Inventors: Josef Wieser, Ulrich Griesser, Michael Enders, Volker Kahlenberg
  • Patent number: 9045788
    Abstract: Process for the enzymatic synthesis of the compound of formula (I), (7S)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl)N-methyl methanamine: and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: June 2, 2015
    Assignee: LES LABORATOIRES SERVIER
    Inventors: Sandrine Pedragosa-Moreau, François Lefoulon, Francisco Moris Varas, Javier Gonzalez Sabin
  • 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: 9006424
    Abstract: The invention concerns a new process for the resolution of ivabradine and of intermediates of synthesis thereof.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: April 14, 2015
    Assignee: Laboratorio Chimico Internazionale S.p.A.
    Inventors: Antonio Nardi, Bruno De Angelis, Paolangelo Cerea, Jane Llorenc Rafecas, Nicolas Tesson
  • Publication number: 20150065703
    Abstract: Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: Northwestern University
    Inventors: Karl A. Scheidt, Javier Izquierdo Ferrer
  • Publication number: 20150025062
    Abstract: The present invention is directed to a method of enhancing visual function in a subject, comprising administering to the subject in need of such enhancement, a therapeutically effective amount of an inhibitor of a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the HCN channel inhibitor.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 22, 2015
    Inventor: Movses H. Karakossian
  • Patent number: 8927708
    Abstract: Process for the synthesis of the compound of formula (I): wherein R represents a para-methoxybenzyl (PMB) group or the following group: Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: January 6, 2015
    Assignee: Les Laboratoires Servier
    Inventor: Alexandre Le Flohic
  • Publication number: 20140357860
    Abstract: The present invention relates to pharmaceutical compositions with delayed release which contain ivabradine adipate as active substance. The present invention furthermore relates to processes for the preparation of this composition and certain salts of ivabradine.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 4, 2014
    Applicant: ratiopharm GmbH
    Inventors: Ramesh Matioram GIDWANI, Mayur Vilas KOLHATKAR, Dominique MEERGANS, Ralph STEFAN, Jens GEIER
  • Publication number: 20140357859
    Abstract: The invention concerns a new process for the resolution of ivabradine and of intermediates of synthesis thereof.
    Type: Application
    Filed: July 31, 2012
    Publication date: December 4, 2014
    Applicant: LOBORATORIO CHIMICO INTERNAZIONALE S.p.A.
    Inventors: Antonio Nardi, Bruno De Angelis, Paolangelo Cerea, Jane Llorenc Rafecas, Nicolas Tesson
  • Publication number: 20140349998
    Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 27, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sean P Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
  • 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
  • Publication number: 20140336179
    Abstract: The present invention relates to a novel solvate of ivabradine hydrochloride, a process of its preparation and its use for the preparation of specific polymorphic forms of ivabradine hydrochloride.
    Type: Application
    Filed: July 31, 2012
    Publication date: November 13, 2014
    Applicant: SANDOZ AG
    Inventors: Josef Wieser, Ulrich Griesser, Michael Enders, Volker Kahlenberg
  • Publication number: 20140323471
    Abstract: Stable crystalline Form II and stable crystalline Form III of ivabradine hydrochloride and processes for their preparation are disclosed.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 30, 2014
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Mukul Hariprasad Sharma, Piyush Rajendra Sharma, Jaiprakash Ajitsingh Parihar
  • Publication number: 20140315890
    Abstract: Ivabradine hydrochloride Form IV, its pharmaceutical composition, process for its preparation, and its use as therapeutically active ingredient.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 23, 2014
    Inventors: Rafel Prohens Lopez, Cristina Puigjaner Vallet, Rafael Barbas Canero, Jose Luis Del Rio Pericacho, Josep Marti Via
  • Patent number: 8859763
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Grant
    Filed: May 14, 2014
    Date of Patent: October 14, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Lucile Vaysse-Ludot, Alexandre Le Flohic, Michel Vaultier, Mathieu Pucheault, Thomas Kaminski
  • Publication number: 20140296512
    Abstract: Process for the synthesis of the compound of formula (I): wherein R represents a para-methoxybenzyl (PMB) group or the following group: Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Application
    Filed: March 24, 2014
    Publication date: October 2, 2014
    Applicant: LES LABORATOIRES SERVIER
    Inventor: Alexandre LE FLOHIC
  • Patent number: 8835627
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: March 25, 2013
    Date of Patent: September 16, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Alexandre Le Flohic, Mathieu Grandjean
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Publication number: 20140221352
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Patent number: 8796259
    Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: August 5, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Joane Litvak
  • Patent number: 8779121
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: July 15, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Maria Del Pilar Carranza, Maria Isabel Garcia Aranda, José Lorenzo Gonzalez, Frédéric Sanchez
  • Patent number: 8779123
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: July 15, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Maria Del Pilar Carranza, Maria Isabel Garcia Aranda, José Lorenzo Gonzalez, Frédéric Sanchez
  • Patent number: 8779122
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Grant
    Filed: November 6, 2013
    Date of Patent: July 15, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Maria Del Pilar Carranza, Maria Isabel Garcia Aranda, José Lorenzo Gonzalez, Frédéric Sanchez
  • Publication number: 20140171415
    Abstract: The present invention relates to an If blocker or a pharmaceutically acceptable salt thereof for the treatment and/or prevention of a canine patient suffering from heart diseases, preferably heart diseases such as dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia. Each of these diseases may or may not result in heart failure (HF) in canine patients. The invention also relates to improving the quality of life, improving the general health condition as well as a prolonging the life expectancy in canine patients suffering from heart diseases and/or heart failure due to one or more of the following etiologies dilated cardiomyopathy (DCM), mitral valve insufficiency (MI), arrthymias, preferably tachyarrthymias, preferably arterial arrhythmias, atrioventricular nodal arrhythmias and/or tachycardia.
    Type: Application
    Filed: December 11, 2013
    Publication date: June 19, 2014
    Applicant: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Saskia KLEY, Ingo LANG, Joerg Christian MEIL, Randolph SEIDLER, Michael MARKERT
  • Publication number: 20140163220
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Application
    Filed: December 3, 2013
    Publication date: June 12, 2014
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Maria Del Pilar CARRANZA, Maria Isabel GARCIA ARANDA, José Lorenzo GONZALEZ, Frédéric SANCHEZ
  • Publication number: 20140155382
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: November 22, 2013
    Publication date: June 5, 2014
    Applicant: ABBVIE INC.
    Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
  • Patent number: 8741889
    Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: John Frederick Boylan, Leopoldo Ladores Luistro, Kathryn Elizabeth Packman
  • Patent number: 8741890
    Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
  • Publication number: 20140128598
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Application
    Filed: November 6, 2013
    Publication date: May 8, 2014
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Maria Del Pilar CARRANZA, Maria Isabel GARCIA ARANDA, José Lorenzo GONZALEZ, Frédéric SANCHEZ
  • Publication number: 20140107334
    Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Application
    Filed: October 11, 2013
    Publication date: April 17, 2014
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Maria Del Pilar CARRANZA, Maria Isabel GARCIA ARANDA, José Lorenzo GONZALEZ, Frédéric SANCHEZ
  • Publication number: 20140100217
    Abstract: The present invention provides a compound comprising a general formula 1: In general formula 1, X is at least one of O and S. A is a ring bridge. Y1 is at least one of H, alkyl, fluoroalkyl, aryl and heteroaryl. Z1, Z2, Z3 are, individually or alternatively, at least one of H, carbonyl, OH, O-alkyl, O-acyl, N—R1R2 (where R1 or R2 are, individually or alternatively, at least one of H, alkyl, acyl, and sulfonyl), alkyl, acyl, fluoroalkyl, aryl, and heteroaryl. R1 is at least one of alkyl, acyl, alkoxycarbonyl, aryloxycarbonyl, and aminocarbonyl. R2 is at least one of H, alkyl, aryl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aminocarbonyl, aryloxycarbonyl, alkylsulfonyl, arylsulfonyl, aminoacyl and peptidyl. The present invention furthermore relates to the use of the compound as a pharmaceutical active compound, and to the use of the pharmaceutical active compound to treat bacterial diseases, neurodegenerative diseases and tumors.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 10, 2014
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITAET ZU KOELN
    Inventors: HANS-GUENTHER SCHMALZ, CÉDRIC MICHAEL REUTER, RONALD KUEHNE, HARTMUT OSCHKINAT, MATTHIAS MUELLER, ROBERT OPITZ
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • Publication number: 20140031334
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
  • Publication number: 20130303517
    Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 14, 2013
    Inventors: Christopher W. Boyce, Sylvia Joanna Degrado, Xiao Chen, Jun Qin, Robert D. Mazzola, JR., Younong Yu, Kevin D. McCormick, Anandan Palani, Dong Xiao, Robert George Aslanian, Jie Wu, Ashwin Umesh Rao, Phieng Siliphaivanh, Joey L. Methot, Hongjun Zhang, Elizabeth Helen Kelley, William Colby Brown, Qin Jiang, Jolicia Polivina Gauuan, Andrew J. Leyhane, Purakkattle Johny Biju, Pawan K. Dhondi, Li Dong, Salem Fevrier, Xianhai Huang, Henry M. Vaccaro
  • Patent number: 8575150
    Abstract: According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of A?42 and hence are useful in treatment of Alzheimer's disease and related conditions.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: November 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Joey Methot, Hua Zhou, Adam J. Schell, Benito Munoz, Alexey A. Rivkin, Sean P. Ahearn, Stephanie Chichetti, Rachel N. MacCoss, Sam Kattar, Matthew Christopher, Chaomin Li, Andrew Rosenau, William Colby Brown
  • Publication number: 20130281438
    Abstract: The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/or Pyk2 mediated disorder or disease.
    Type: Application
    Filed: January 7, 2012
    Publication date: October 24, 2013
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Liang Cheng, Xijie Liu, Yuandong Hu, Xinhe Xu, Zhihua Liu, Lipeng Zhang, Wei Wu, Shulong Wang, Yu Shen, Gen Li, Yin Wang, Sheng Zhao, Chonglong Li, Jia Tang, Honghao Yu
  • Publication number: 20130261081
    Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
    Type: Application
    Filed: September 12, 2011
    Publication date: October 3, 2013
    Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
  • Publication number: 20130261106
    Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 3, 2013
    Applicant: SANOFI
    Inventors: Jean-Christophe CARRY, Fabienne CHATREAUX, Stephanie DEPRETS, Olivier DUCLOS, Vincent LEROY, Sergio MALLART, Dominique MELON-MANGUER, Maria MENDEZ-PEREZ, Fabrice VERGNE
  • Publication number: 20130261298
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Application
    Filed: March 25, 2013
    Publication date: October 3, 2013
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Alexandre LE FLOHIC, Mathieu GRANDJEAN
  • Patent number: 8541405
    Abstract: Methods for the preparation of Ivabradine sulfate and form I crystal thereof. In particular, the Ivabradine sulfate and the preparation methods thereof, and the stable form I crystal of Ivabradine sulfate and the preparation methods thereof.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: September 24, 2013
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Piaoyang Sun, Yongjiang Chen, Guangliang Yu
  • Patent number: 8541404
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 24, 2013
    Assignee: ElexoPharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Patent number: 8513410
    Abstract: Process for the synthesis of ivabradine of formula (I): addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: August 20, 2013
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Luc Renaud, Nicolas Pannetier, Jean-Pierre Lecouve, Lucile Vaysse-Ludot, Solenne Moulin
  • Publication number: 20130210805
    Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
    Type: Application
    Filed: October 6, 2011
    Publication date: August 15, 2013
    Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, JR., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Johny Biju, Li Dong, Xian Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi
  • Publication number: 20130211070
    Abstract: Process for the optical resolution of the compound of formula (I): by chiral chromatography. Application in the synthesis of ivabradine, of its addition salts with a pharmaceutically acceptable acid and of their hydrates.
    Type: Application
    Filed: March 26, 2013
    Publication date: August 15, 2013
    Applicant: LES LABORATOIRES SERVIER
    Inventor: LES LABORATOIRES SERVIER
  • Patent number: 8507668
    Abstract: Process for the synthesis of ivabradine of formula (I): addition salts thereof with a pharmaceutically acceptable acid, and hydrates thereof.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: August 13, 2013
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Luc Renaud, Nicolas Pannetier, Sylvain Gaillard, Jean-Pierre Lecouve, Lucile Vaysse-Ludot
  • Publication number: 20130203974
    Abstract: A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.
    Type: Application
    Filed: December 14, 2012
    Publication date: August 8, 2013
    Inventors: Ronald Thaddeus RAINES, Eddie Leonard MYERS
  • Publication number: 20130184256
    Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 18, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR
  • Patent number: 8476426
    Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.
    Type: Grant
    Filed: February 9, 2012
    Date of Patent: July 2, 2013
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Louis Peglion, Aimee Dessinges