Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 540/500)
  • Patent number: 9914732
    Abstract: The present invention relates to diazabicyclo[4.3.1]decane derivatives, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said diazabicyclo[4.3.1]decane derivatives can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
    Type: Grant
    Filed: January 26, 2015
    Date of Patent: March 13, 2018
    Assignee: Max-Planck-Gesellschaft zur Forderung der Wissensc haften e.V.
    Inventors: Yansong Wang, Felix Hausch, Matthias Bischoff, Sebastian Pomplun
  • Patent number: 9371322
    Abstract: The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza-amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
    Type: Grant
    Filed: July 24, 2013
    Date of Patent: June 21, 2016
    Assignee: Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
    Inventors: Yansong Wang, Felix Hausch
  • Publication number: 20150141411
    Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Frederik Jan Rita Rombouts, Andres Avelino Trabanco-Suarez, Henricus Jacobus Maria Gijsen, Gregor James Macdonald, Francois Paul Bischoff, Sergio-Alvar Alonso-de-Diego, Adriana Ingrid Velter, Yves Emiel Maria Van Roosbroeck
  • 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
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Patent number: 8975219
    Abstract: A fabric cleaning composition comprising from 1% to 20% by weight of the fabric cleaning composition of an oxygen-based bleaching source and a hueing agent, and wherein the neat composition has a pH between 2.5 and 5.5, and a method of using said fabric cleaning composition.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: March 10, 2015
    Assignee: The Procter & Gamble Company
    Inventors: Margherita Scartozzi, Luca Sarcinelli, Sophie Anne Marguerite Goellner, Enza Ceccobelli, Leo Gagliardi
  • Publication number: 20140255344
    Abstract: The present invention discloses compounds of Formulae I and II, wherein the variables in Formulae I and II are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formulae I and II in the treatment of HCV infection.
    Type: Application
    Filed: October 8, 2012
    Publication date: September 11, 2014
    Applicant: Hiffmann-La Roche Inc.
    Inventors: John A. Brinkmann, Hongju Li, Ramakanth Sarabu, Sung-Sau So
  • Patent number: 8785431
    Abstract: The present invention relates to diester prodrugs of cilazaprilate which undergo enzymatic cleavage to release the active metabolite cilazaprilate that is used for the treatment of hypertension and congestive heart failure. Furthermore the diester prodrugs of cilazaprilate possess all the properties necessary to be topically administered, preferably via transdermal therapeutic systems.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: July 22, 2014
    Assignee: Hexal AG
    Inventors: Günther Bernhardt, Miriam Ertel, Armin Buschauer, Jörg Nink
  • Patent number: 8629137
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: October 2, 2012
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
  • Publication number: 20130345123
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1-C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.
    Type: Application
    Filed: March 13, 2012
    Publication date: December 26, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Chongqing Sun, William R. Ewing, Scott A. Bolton, Zhengxiang Gu, Yanting Huang, Natesan Murugesan, Yeheng Zhu
  • Patent number: 8551987
    Abstract: The invention relates to the novel salts AB of the base A with a physiologically acceptable acid B which is selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, fumaric acid and salicylic acid and the polymorphic compounds, the corresponding solvates and hydrates thereof.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kathrin Pachur, Uwe Joerg Ries, Ulrike Werthmann, Sonja Sproll
  • Patent number: 8507477
    Abstract: Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 receptors are involved.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: August 13, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Michael R. Wood, Ian M. Bell, June J. Kim, Harold G. Selnick, Craig A. Stump
  • Publication number: 20130150342
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: February 17, 2011
    Publication date: June 13, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas Brain, Young Shin Cho, John William Giraldes, Bharat Lagu, Julian Roy Levell, Michael J. Luzzio, Lawrence Blas Perez, Yaping Wang, Fan Yang
  • Publication number: 20130029975
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Application
    Filed: October 2, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: BOEHRINGER INGELHEIM INTERNATIONAL GM
  • Publication number: 20120328565
    Abstract: The present invention discloses compounds of Formula I wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the treatment of HCV infection.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: John A. Brinkman, Andrew F. Donnell, Robert Francis Kester, Yimin Qian, Ramakanth Sarabu, Sung-Sau So
  • Patent number: 8329771
    Abstract: The object of the present invention is to provide a photobase generator capable of efficiently generating amines (tertiary amines and amidine) high in catalytic activity by sensing light with a wavelength of from 350 to 500 nm (especially, from 400 to 500 nm). The present invention is a photobase generator characterized in being represented by general formula (1) or (2). Y+ is a quaternary ammonio group of general formula (3) to (5), and X? is a counter anion selected from among a borate anion, a phenolate anion, and a carboxylate anion.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: December 11, 2012
    Assignee: San-Apro Limited
    Inventors: Atsushi Shiraishi, Hideki Kimura
  • Patent number: 8288531
    Abstract: A process for preparing compounds of the formula (I) in which R1 and R2 are as defined in the description.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: October 16, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Juergen Schnaubelt, Thomas Fachinger, Michael Konrad, Thomas Krueger, Joern Merten, Carsten Reichel, Svenja Renner, Rolf Schmid, Emanuel Stehle, Bianca Werner
  • Publication number: 20120238749
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
    Type: Application
    Filed: October 12, 2011
    Publication date: September 20, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
  • Publication number: 20120230951
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 13, 2012
    Inventors: Muzaffar Alam, Steven Joseph Berthel, John A. Brinkman, Ronald Charles Hawley, Hongju Li, Wylie Solang Palmer, Sherrie Pietranico-Cole, Ramakanth Sarabu, Mark Smith, Sung-Sau So, Lin Yi, Yansheng Zhai, Qiang Zhang, Shu-Hai Zhao
  • Patent number: 8222402
    Abstract: A process for preparing compounds of the formula (I) in which R1.1, R1.2, R1.3 and R2 are as defined in the description.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: July 17, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kathrin Pachur, Stefan Goepper, Guenther Huchler, Michael Konrad, Kathrin Maier, Werner Rall, Uwe Joerg Ries, Andreas Zopf
  • Publication number: 20120165319
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.
    Type: Application
    Filed: November 10, 2011
    Publication date: June 28, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M.C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L.C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
  • Patent number: 8163737
    Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: April 24, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Corey Anderson, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Sanghee Yoo, Daniele Bergeron, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar, Elaine Krueger, John Maxwell, Arnaud Le Tiran, Yusheng Liao
  • Publication number: 20120088755
    Abstract: The present invention relates to the new compounds of general formula I wherein A, U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers thereof, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
    Type: Application
    Filed: December 17, 2009
    Publication date: April 12, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dirk Gottschling, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
  • Publication number: 20120058994
    Abstract: The invention relates to the novel salts AB of the base A with a physiologically acceptable acid B which is selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, fumaric acid and silcylic acid and the polymorphic compounds, the corresponding solvates and hydrates thereof.
    Type: Application
    Filed: September 25, 2008
    Publication date: March 8, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Kathrin Pachur, Uwe Joerg Ries, Ulrike Werthmann, Sonja Sproll
  • Publication number: 20120028965
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: October 13, 2010
    Publication date: February 2, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
  • Publication number: 20110281845
    Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.
    Type: Application
    Filed: June 15, 2011
    Publication date: November 17, 2011
    Applicant: NOVARTIS AG
    Inventors: Zhuoliang CHEN, Mark G. PALERMO, Sushil K. SHARMA, Troy SMITH, Christopher S. STRAUB, Run-Ming D. WANG, Yaping WANG, Leigh ZAWEL
  • Patent number: 8044043
    Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: October 25, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventor: Guanglin Luo
  • Patent number: 8039460
    Abstract: Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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: October 12, 2005
    Date of Patent: October 18, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Diem N. Nguyen, Zhengwu J. Deng, Theresa M. Williams, Joseph P. Vacca, Craig M. Potteiger, Harold G. Selnick
  • Patent number: 7985747
    Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: July 26, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Alexander Dreyer, Kirsten Arndt, Gerhard Schaenzle, Henri Doods, Marco Santagostino, Fabio Paleari
  • Patent number: 7947678
    Abstract: Compounds of formula I: (where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the 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: July 25, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Theresa M. Williams
  • Publication number: 20110087021
    Abstract: A process for preparing compounds of the formula (I) in which R1 and R2 are as defined in the description.
    Type: Application
    Filed: August 12, 2008
    Publication date: April 14, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Juergen Schnaubelt, Thomas Fachinger, Michael Konrad, Thomas Krueger, Joern Merten, Carsten Reichel, Svenja Renner, Rolf Schmid, Emanuel Stehle, Bianca Werner
  • Publication number: 20110082294
    Abstract: The invention is concerned with novel bicyclic compounds of formula (I), wherein A, L, E, F, G, R1, R2, R3, R4, R5, R6, R7, V, W and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
    Type: Application
    Filed: September 29, 2010
    Publication date: April 7, 2011
    Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei
  • Publication number: 20110071286
    Abstract: A process for preparing compounds of the formula (I) in which R1.1, R1.2, R1.3 and R2 are as defined in the description.
    Type: Application
    Filed: August 12, 2008
    Publication date: March 24, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Kathrin Pachur, Stefan Goepper, Guenther Huchler, Michael Konrad, Kathrin Maier, Werner Rall, Uwe Joerg Ries, Andreas Zopf
  • Publication number: 20110059954
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Application
    Filed: October 16, 2008
    Publication date: March 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
  • Publication number: 20110059018
    Abstract: The present invention relates to molecular probes of the formula (I) L1-R1-L-A-X??(I) as defined herein that allow for the observation of the catalytic activity of a selected caspase, cathepsin, MMP and carboxypeptidase in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.
    Type: Application
    Filed: August 20, 2010
    Publication date: March 10, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Karl-Ulrich WENDT, Maik KINDERMANN, Catherine MINIEJEW, Anja GLOBISCH
  • Publication number: 20110034444
    Abstract: The present invention relates to the CGRP antagonists of general formula I wherein R1, R2, R3 and R4 are as defined in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Application
    Filed: October 19, 2010
    Publication date: February 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Dirk STENKAMP, Kirsten ARNDT, Henri DOODS
  • Publication number: 20100324028
    Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: November 21, 2008
    Publication date: December 23, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
  • Publication number: 20100303728
    Abstract: The present invention relates to molecular probes of formula (I) {L1-R1-L}n-A-CO—NH—R2-L2??(I) as defined herein that allow for the observation of the catalytic activity of a selected caspase in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.
    Type: Application
    Filed: January 28, 2010
    Publication date: December 2, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Karl-Ulrich WENDT, Maik KINDERMANN, Catherine MINIEJEW
  • Patent number: 7838517
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: May 15, 2009
    Date of Patent: November 23, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
  • Publication number: 20100249114
    Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: February 25, 2010
    Publication date: September 30, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Alexander DREYER, Kirsten ARNDT, Henri DOODS, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Fabio PALEARI
  • Publication number: 20100247519
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Application
    Filed: June 7, 2010
    Publication date: September 30, 2010
    Applicant: Schering Corporation
    Inventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
  • Publication number: 20100234361
    Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: February 17, 2010
    Publication date: September 16, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Alexander DREYER, Kirsten ARNDT, Gerhard SCHAENZLE, Henri Doods, Marco SANTAGOSTINO, Fabio PALEARI
  • Publication number: 20100190688
    Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.
    Type: Application
    Filed: July 12, 2005
    Publication date: July 29, 2010
    Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
  • Patent number: 7763606
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: July 27, 2010
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
  • Publication number: 20100152439
    Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
    Type: Application
    Filed: February 23, 2010
    Publication date: June 17, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Guenther HUCHLER, Werner RALL, Uwe RIES
  • Publication number: 20100144716
    Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: February 18, 2010
    Publication date: June 10, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Marco SANTAGOSTINO, Fabio PALEARI, Gerhard SCHAENZLE, Kirsten ARNDT, Henri DOODS
  • Patent number: 7700589
    Abstract: CGRP antagonists of the formula of which the following are exemplary: (1) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(1-methyl-piperidin-4-yl)-piperazin-1-yl]-2-oxo-ethyl}-amide, (2) 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylic acid-{(R)-1-(3,4-diethyl-benzyl)-2-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-2-oxo-ethyl}-amide.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: April 20, 2010
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Klaus Rudolf, Stephan Georg Mueller, Dirk Stenkamp, Philipp Lustenberger, Alexander Dreyer, Eckhart Bauer, Marcus Schindler, Kirsten Arndt, Henri Doods
  • Patent number: 7696196
    Abstract: The present invention relates to the CGRP antagonists of general formula wherein A, X, D, E, G, M, Q and R1 to R3 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: August 5, 2008
    Date of Patent: April 13, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Alexander Dreyer, Kirsten Arndt, Gerhard Schaenzle, Henri Doods, Marco Santagostino, Fabio Paleari
  • Patent number: 7696346
    Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
    Type: Grant
    Filed: August 17, 2007
    Date of Patent: April 13, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenther Huchler, Werner Rall, Uwe Ries