Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 548/154)
  • Patent number: 9833621
    Abstract: Systems, devices and methods for modulation of sirtuins by neurostimulation. In particular, sirtuins may be modulated by stimulation of the vagus nerve. Further described herein generally are methods, systems and devices, for specifically modulating sirtuins, including sub-sets (types or localized regions) of sirtuins by vagus nerve stimulation (VNS).
    Type: Grant
    Filed: December 27, 2011
    Date of Patent: December 5, 2017
    Assignee: SETPOINT MEDICAL CORPORATION
    Inventor: Jacob A. Levine
  • Patent number: 9556201
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: January 31, 2017
    Assignee: GLAXOSMITHKLINE LLC
    Inventors: Pui Yee Ng, Charles Blum, Lauren McPherson, Robert B. Perni, Chi B. Vu, Mohammed Mahmood Ahmed, Jeremy S. Disch
  • Patent number: 8957066
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 17, 2015
    Assignee: Biomarin Pharmaceutical Inc.
    Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 8916711
    Abstract: The present invention provides a compounds 7a-f to 18a-f and 19a-f to 30a-f of general formula A, useful as potential anticancer agents against human cancer cell lines.
    Type: Grant
    Filed: October 7, 2010
    Date of Patent: December 23, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmed Kamal, Dastagiri Dudekula, Surendranadha Reddy Jonnala, Vijaya Bharathi Earla
  • Patent number: 8895313
    Abstract: Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: November 25, 2014
    Assignee: Wista Laboratories Ltd.
    Inventors: Steven John Kemp, Lynda Jane Storey, John Mervyn David Storey, Janet Rickard, Charles Robert Harrington, Claude Michel Wischik, Scott Clunas, Tobias Kerst Heinrich
  • Publication number: 20140343066
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 20, 2014
    Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H.M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
  • Publication number: 20140303372
    Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 9, 2014
    Applicant: ABBVIE BHAMAS LTD.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Patent number: 8722887
    Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: May 13, 2014
    Assignee: Abbvie Bahamas, Ltd.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20130317003
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: March 15, 2013
    Publication date: November 28, 2013
    Inventor: Repligen Corporation
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Patent number: 8552215
    Abstract: Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: October 8, 2013
    Assignee: Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Isamu Shiina, Kenya Nakata
  • Patent number: 8530504
    Abstract: A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.
    Type: Grant
    Filed: October 7, 2010
    Date of Patent: September 10, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Kogyoku Shin, Taro Terauchi, Yoshinori Takahashi, Minako Hashizume, Kunitoshi Takeda, Kodo Shikata, Akira Inomata
  • Publication number: 20130158018
    Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
  • Publication number: 20130131321
    Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; a
    Type: Application
    Filed: August 3, 2011
    Publication date: May 23, 2013
    Applicant: GRAFFINITY PHARMACEUTICALS GMBH
    Inventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
  • Patent number: 8431603
    Abstract: A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: April 30, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Hisashi Shibata, Kodo Shikata, Akira Inomata, Kogyoku Shin, Taro Terauchi, Yoshinori Takahashi, Minako Hashizume, Kunitoshi Takeda
  • Publication number: 20130085157
    Abstract: This disclosure relates to compounds, compositions and methods for the treatment of various disorders. In particular, the disclosure relates to thiazolotriazole and thiazoloimidazole compounds which agonize the activity of the protein TGR5.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 4, 2013
    Inventors: Emilie D. Smith, Mark E. Fitzgerald, Rong Jiang, Robert N. Atkinson, James M. Veal, Kenneth H. Huang
  • Publication number: 20120271054
    Abstract: The present invention provides a compounds 7a-f to 18a-f and 19a-f to 30a-f of general formula A, useful as potential anticancer agents against human cancer cell lines. The present invention further provides a process for the preparation of imidazothiazole-chalcone hybrids 7a-f to 18a-f and 19a-f to 30a-f of general formula A.
    Type: Application
    Filed: October 7, 2010
    Publication date: October 25, 2012
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Ahmed Kamal, Dastagiri Dudekula, Surendranadha Reddy Jonnala, Vijaya Bharathi Earla
  • Patent number: 8252822
    Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a heteroaryl five-membered ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: August 28, 2012
    Assignee: Acea Biosciences, Inc.
    Inventors: Haoyun An, Biao Xi, Yama Abassi, Xiaobo Wang, Xiao Xu
  • Patent number: 8236964
    Abstract: The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and R1 are as described in the description and their use as medicaments, especially as orexin receptor antagonists.
    Type: Grant
    Filed: March 25, 2008
    Date of Patent: August 7, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
  • Publication number: 20120197013
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: August 2, 2012
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
  • Patent number: 8178672
    Abstract: An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.
    Type: Grant
    Filed: October 19, 2005
    Date of Patent: May 15, 2012
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre
  • Publication number: 20120114633
    Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
    Type: Application
    Filed: April 6, 2010
    Publication date: May 10, 2012
    Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
  • Patent number: 8106215
    Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: January 31, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
  • Publication number: 20120015926
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Application
    Filed: November 9, 2009
    Publication date: January 19, 2012
    Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Publication number: 20110275663
    Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.
    Type: Application
    Filed: April 16, 2009
    Publication date: November 10, 2011
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
  • Patent number: 8008290
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.
    Type: Grant
    Filed: August 9, 2010
    Date of Patent: August 30, 2011
    Assignee: Amura Therapeutics Limited
    Inventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
  • Publication number: 20110207751
    Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a thiazole ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 25, 2011
    Inventors: Long Mao, Xiaobo Wang, Xiao Xu, Li Zhao, Jia Liu
  • Publication number: 20110171739
    Abstract: Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
    Type: Application
    Filed: September 23, 2009
    Publication date: July 14, 2011
    Inventors: Steven John Kemp, Lynda Jane Storey, John Mervyn David, Janet Richard, Charles Robert Harrington, Claude Michael Wischik, Scott Clunas, Tobias Kerst Heinrich
  • Publication number: 20110150827
    Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Application
    Filed: December 17, 2010
    Publication date: June 23, 2011
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
  • Publication number: 20110124636
    Abstract: The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
    Type: Application
    Filed: December 28, 2007
    Publication date: May 26, 2011
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
  • Publication number: 20110105555
    Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT6 receptor, and more particularly to some N-imidazo[2,1-b]thiazole-5-sulfonamide derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT6 is involved.
    Type: Application
    Filed: May 8, 2009
    Publication date: May 5, 2011
    Inventors: Josep Mas Prio, Antoni Torrens Jover
  • Publication number: 20110105491
    Abstract: The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.
    Type: Application
    Filed: July 7, 2009
    Publication date: May 5, 2011
    Inventors: Hamed Aissaoui, Christoph Boss, Julien Hazemann, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen
  • Publication number: 20110092540
    Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT6; receptor, and more particularly to some N-phenyl-2,3-dihydroimidazol[2,1-b]thiazole-5-sulfonamide derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT6 is involved.
    Type: Application
    Filed: May 8, 2009
    Publication date: April 21, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Josep Mas Prio, Antoni Torrens Jover
  • Publication number: 20110086882
    Abstract: A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.
    Type: Application
    Filed: October 7, 2010
    Publication date: April 14, 2011
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Kogyoku SHIN, Taro TERAUCHI, Yoshinori TAKAHASHI, Minako HASHIZUME, Kunitoshi TAKEDA, Kodo SHIKATA, Akira INOMATA
  • Patent number: 7893069
    Abstract: Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, a method for producing them, pharmaceutical compositions containing them, and the use thereof for regularing mGluR5 receptors, or for treating or inhibiting disorders or disease states at least partially mediated by mGluR5 receptor such as pain, anxiety attacks, drug or alcohol dependency, and others.
    Type: Grant
    Filed: September 9, 2008
    Date of Patent: February 22, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Sven Kuehnert, Saskia Zemolka, Michael Haurand, Klaus Schiene
  • Publication number: 20110028423
    Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect choline acetyltransferase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a choline acetyltransferase in a reaction system in which the choline acetyltransferase contacts with a test substance, and the like.
    Type: Application
    Filed: November 21, 2008
    Publication date: February 3, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Junko Otsuki, Marc Van De Craen, Annelies Roobrouck, Guy Nys, Bert Demey
  • Publication number: 20110009385
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.
    Type: Application
    Filed: August 9, 2010
    Publication date: January 13, 2011
    Applicant: Amura Therapeutics Limited
    Inventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
  • Publication number: 20110009631
    Abstract: Compounds of the formula (II) and (IV) are provided, which may be employed as intermediates for making compounds useful in treating respiratory diseases.
    Type: Application
    Filed: July 14, 2010
    Publication date: January 13, 2011
    Applicant: Glaxo Group Limited
    Inventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Inderjit Singh Mann, Panayiotis Alexandrou Procopiou
  • Patent number: 7868001
    Abstract: A compound of Formula I: Each variable is defined in the specification. This invention relates to a method of decreasing a level of a cytokine (e.g., TNF? or interlukine such as IL-1?) in a subject with a compound of Formula I. It also relates to a method of treating a disorder mediated by an overproduction of a cytokine with such a compound.
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: January 11, 2011
    Assignee: Hutchison Medipharma Enterprises Limited
    Inventors: Wei Deng, Wei-Guo Su, Yu Cai, Jeff Duan
  • Publication number: 20110003806
    Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY 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: January 28, 2010
    Publication date: January 6, 2011
    Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
  • Publication number: 20110003807
    Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.
    Type: Application
    Filed: January 28, 2010
    Publication date: January 6, 2011
    Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Hiroshi Banno, Masaaki Hirose, Osamu Kurasawa
  • Publication number: 20100292232
    Abstract: Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs) of the formula Also disclosed are methods of making the NNRTIs, as well as compositions that include such NNRTIs and methods of their use for treating viral infections, in particular retroviral infections, such as HIV infection.
    Type: Application
    Filed: November 5, 2008
    Publication date: November 18, 2010
    Inventors: Daniel Elleder, John A.T. Young, Thomas J. Baiga, Joseph P. Noel
  • Publication number: 20100261710
    Abstract: The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.
    Type: Application
    Filed: August 21, 2008
    Publication date: October 14, 2010
    Applicant: ARQULE, INC.
    Inventors: Mark A. Ashwell, Manish Tandon, Nivedita D. Namdev, Jean-Marc Lapierre, Yanbin Liu, Hui Wu
  • Patent number: 7799795
    Abstract: Provided herein are compounds of the formula where A1, A2, A3, A4, L, Q, R1, R2, R3, R4, Rx, Ry, Rz, X, Y1, Y2, Y4 and Z are as described herein, and compositions thereof that are useful in the treatment of inflammatory and immune conditions and diseases. In particular, the invention provides aryl nitrile compounds which modulate the expression and/or function of a chemokine receptor.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: September 21, 2010
    Assignee: Amgen Inc.
    Inventors: Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Julio C. Medina, Jeffrey T. Mihalic, George R. Tonn
  • Publication number: 20100234610
    Abstract: Disclosed is a method for producing an optically active ester by highly selectively esterifying one enantiomer of a racemic carboxylic acid, while producing an optically active carboxylic acid which is the other enantiomer. An optically active ester is produced while producing an optically active carboxylic acid at the same time by reacting a racemic carboxylic acid with a specific alcohol or phenol derivative in the presence of benzoic anhydride or a derivative thereof and a catalyst such as tetramisole or benzotetramisole, thereby selectively esterifying one enantiomer of the racemic carboxylic acid.
    Type: Application
    Filed: March 4, 2009
    Publication date: September 16, 2010
    Inventors: Isamu Shiina, Kenya Nakata
  • Patent number: 7790741
    Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: September 7, 2010
    Assignee: Abbott Laboratories
    Inventors: David J. Calderwood, Kristine E. Frank, David W. Borhani, Heather M. Davis, Nathan S. Josephsohn, Barbara S. Skinner
  • Publication number: 20100210850
    Abstract: The present invention is related to the a new process for the preparation of 6-substituted-imidazo[2,1-b]thiazole-5-sulfonyl halides of formula (I), comprising gradually adding a compound of formula (II), into a heated solution of R1SO3H where R1 represents F or Cl, and R2 represents H, F, Cl, Br, S, (C1-C6)alkyl, (C1-C6)alkoxy or trifluoromethyl.
    Type: Application
    Filed: October 22, 2008
    Publication date: August 19, 2010
    Applicant: LABORATORIOS DEL DR ESTEVE S.A.
    Inventors: Josep Mas-Prio, Antonio Torrens-Jover
  • Publication number: 20100184808
    Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.
    Type: Application
    Filed: July 2, 2008
    Publication date: July 22, 2010
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen