Benzothiazoles (including Hydrogenated) Patents (Class 544/135)
  • Patent number: 10927106
    Abstract: The present invention relates to compounds of Formula (I), which are DYRK1A and/or DYRK1B inhibitors, and their use in the treatment of neurodegenerative disorders such as Alzheimer's disease (AD) and Parkinson's disease (PD), metabolic disorders such as Metabolic Syndrome or diabetes mellitus, and cancer.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: February 23, 2021
    Assignee: PHARMASUM THERAPEUTICS AS
    Inventors: John Sigurd Svendsen, Wenche Stensen, Roderick Alan Porter
  • Patent number: 9169240
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicament.
    Type: Grant
    Filed: September 5, 2013
    Date of Patent: October 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: George O. Tora, Heather Finlay, Carol Hui Hu, Ji Jiang, James A. Johnson, Soong-Hoon Kim, John Lloyd, Brandon Parkhurst, Zulan Pi, Jennifer X. Qiao, Tammy C. Wang
  • Patent number: 9000154
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: October 17, 2011
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Martin Kirrane, Daniel Richard Marshall, Robert Sibley, Roger John Snow, Fariba Soleymanzadeh, Ronald John Sorcek
  • Patent number: 8987314
    Abstract: The present invention provides compounds of Formula (I): 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: Grant
    Filed: July 18, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
  • Publication number: 20150065490
    Abstract: Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Applicant: NOVARTIS AG
    Inventors: Bernard CUENOUD, Robin Alec FAIRHURST, Roger John TAYLOR, David BEATTIE
  • Patent number: 8952058
    Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: February 10, 2015
    Assignee: Ambit Biosciences Corporation
    Inventors: Michael J. Hadd, Michael D. Hocker, Mark W. Holladay, Gang Liu, Martin W. Rowbottom, Shimin Xu
  • Patent number: 8952005
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Layton, Michael J. Kelly, III
  • Publication number: 20150011528
    Abstract: Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.
    Type: Application
    Filed: September 21, 2012
    Publication date: January 8, 2015
    Applicant: YUHAN CORPORATION
    Inventors: Youn Hur, Dong-Hyun Kim, Eun-Kyung Kim, Jin-Hwi Park, Jae-Eun Joo, Ho-Woong Kang, Se-Woong Oh, Dong-Kyun Kim, Kyoung-Kyu Ahn
  • Publication number: 20140329800
    Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 6, 2014
    Inventors: Daxin Gao, Heping Yang, Yajun Yu
  • Publication number: 20140323722
    Abstract: A compound represented by formula: its pharmaceutically acceptable salt, or a solvate thereof. Ring B is substituted or unsubstituted nitrogen-containing hetero ring, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R2 and R3 taken together may form oxo, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl or substituted or unsubstituted alkyloxy, R6 and R7 taken together with the adjacent carbon atom to which they are attached may form a substituted or unsubstituted ring, and n is an integer of 0 to 3.
    Type: Application
    Filed: April 29, 2014
    Publication date: October 30, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji MASUDA, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
  • Patent number: 8871944
    Abstract: An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: October 28, 2014
    Assignee: Gifu University
    Inventor: Toshiaki Murai
  • Publication number: 20140288302
    Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 25, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
  • Publication number: 20140275224
    Abstract: Compounds and methods are provided for enhancing or boosting the transfection rate or efficiency of mammalian cells by foreign DNA, such as bacterial plasmid DNA. Compounds, including natural products and inventive synthetic compounds can increase the effectiveness of uptake and incorporation of foreign DNA by mammalian cells, such as human cells, by suppression of DNA cytosine deamination, which is believed to be a mechanism by which these cells eliminate foreign DNA. Inhibition of the cytosine deaminase enzymes by compounds as described herein serves to provide more effective transfection of eukaryotic cells by plasmids including engineered gene sequences. Transfection can be used to study cellular processes, or to cure genetic diseases in human patients. The inventive materials and methods increase the efficiency and effectiveness of such transfection techniques.
    Type: Application
    Filed: November 3, 2011
    Publication date: September 18, 2014
    Applicant: Regents of the University of Minnesota
    Inventors: Reuben S. Harris, Daniel A. Harki, Angela L. Perkins-Harki, Michael A. Carpenter, Ming Li
  • Publication number: 20140235629
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 26, 2012
    Publication date: August 21, 2014
    Inventors: Michael D. Bartberger, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Duquette, John Eksterowicz, Brian M. Fox, Jiasheng Fu, Ana Gonzalez Buenrostro, Felix Gonzalez Lopez De Turiso, Darin J. Gustin, Julie A. Heath, Michael G. Johnson, Frank Kayser, David John Kopecky, Yihong Li, Zhihong Li, Zhihua Ma, Joel Micintosh, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yosup Rew, Philip M. Roveto, Michael J. Schmitt, Daqing Sun, Xiaodong Wang, Malgorzata Wanska, Christine Weathers, Xuelei Yan
  • Publication number: 20140227320
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 14, 2014
    Inventors: Shawn P. Iadonato, Kristin Bedard, Myra Wang Imanaka, Kerry W. Fowler
  • Patent number: 8796268
    Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Patent number: 8772285
    Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: July 8, 2014
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Florencio Zaragoza Dorwald, Inge Thoger Christensen
  • Patent number: 8680090
    Abstract: The present invention provides compounds of Formula (I): 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: Grant
    Filed: July 8, 2013
    Date of Patent: March 25, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
  • Publication number: 20140045829
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly
  • Publication number: 20140045811
    Abstract: The present invention provides compounds of Formula (I): 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: July 18, 2013
    Publication date: February 13, 2014
    Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
  • Publication number: 20140011799
    Abstract: The present invention provides compounds of Formula (I): 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: July 8, 2013
    Publication date: January 9, 2014
    Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
  • Patent number: 8580968
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: November 12, 2013
    Assignee: AbbVie Inc.
    Inventors: Lawrence A. Black, Marlon D. Cowart, Gregory A. Gfesser, Brian D. Wakefield, Robert J. Altenbach, Huaqing Liu, Chen Zhao, Gin C. Hsieh
  • Publication number: 20130245008
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 19, 2013
    Applicant: SANOFI
    Inventor: Alain Pellet
  • Publication number: 20130203730
    Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 8, 2013
    Applicant: AstraZeneca AB
    Inventor: AstraZeneca AB
  • Publication number: 20130183753
    Abstract: The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cells.
    Type: Application
    Filed: February 26, 2013
    Publication date: July 18, 2013
    Applicant: KYOTO UNIVERSITY
    Inventor: Kyoto University
  • Patent number: 8481532
    Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Publication number: 20130096113
    Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: October 12, 2012
    Publication date: April 18, 2013
    Applicant: Ambit Biosciences Corporation
    Inventor: Ambit Biosciences Corporation
  • Publication number: 20130085143
    Abstract: Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.
    Type: Application
    Filed: November 28, 2012
    Publication date: April 4, 2013
    Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE LORRAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S), UNIVERSITAT DE BARCELONA, ORESTE PICCOLO STUDIO DI CONSULENZA SCIENTIFICA
    Inventors: Universite D'aix-Marseille, Universite De Lorraine, Oreste Piccolo Studio Di Consulenza Scientifica, Universitat De Barcelona, Centre National De La Recherche Scientifique (C.
  • Patent number: 8399465
    Abstract: Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A4 hydrolase (LTA4H) modulators and for the treatment of diseases, disorders and conditions mediated by LTA4H.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: March 19, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Genesis Bacani, Christa C. Chrovian, Wendy Eccles, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Virginia M. Tanis, John J. M. Wiener
  • Publication number: 20130035332
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: April 25, 2011
    Publication date: February 7, 2013
    Inventors: Mark E. Layton, Michael J. Kelly
  • Publication number: 20130018039
    Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.
    Type: Application
    Filed: March 31, 2011
    Publication date: January 17, 2013
    Inventors: Vera Q. Bodmer, Linda N. Casillas, Michael P. DeMartino, Philip A. Harris, Bryan W. King, Ami Lakdawala Shah, Lara Kathryn Leister, Joshi M. Ramanjulu, Joseph J. Romano, Gren Z. Wang, Matthew A. Wilson, David Duff Wisnoski
  • Patent number: 8350048
    Abstract: The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: January 8, 2013
    Assignee: Janssen R&D Ireland
    Inventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
  • Publication number: 20130005966
    Abstract: Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-fe][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert-Butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-&][1,3]benzo-thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers.
    Type: Application
    Filed: November 4, 2010
    Publication date: January 3, 2013
    Applicant: Ambit Biosciences Corp.
    Inventors: Timothy David Gross, Rathan Prasad Achampeta, Janakiram Citineni
  • Publication number: 20120270868
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: October 17, 2011
    Publication date: October 25, 2012
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thomas Martin KIRRANE, Daniel Richard MARSHALL, Robert SIBLEY, Roger John SNOW, Fariba SOLEYMANZADEH, Ronald John SORCEK
  • Publication number: 20120252801
    Abstract: The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
    Type: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Dorothée Bardiot, Bruno Cammue, Patrick Chaltin, Arnaud Marchand, Karin Thevissen
  • Publication number: 20120253040
    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.
    Type: Application
    Filed: December 14, 2010
    Publication date: October 4, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
  • Publication number: 20120238545
    Abstract: This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 20, 2012
    Applicant: MERCK SERONO SA
    Inventors: Pascale Gaillard, Isabelle Jeanclaude-Etter, Vincent Pomel, Eric Sebille, Seenisamy Jeyaprakashnarayanan, Mathilde Muzerelle
  • Patent number: 8247412
    Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, Y and G have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: August 21, 2012
    Assignee: Galapagos Sasu
    Inventors: Pierre Deprez, Hélène Jary, Taoues Temal
  • Publication number: 20120178752
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: June 29, 2011
    Publication date: July 12, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: John David GINN, Daniel Richard MARSHALL, Robert SIBLEY, Ronald John SORCEK, Erick Richard Roush YOUNG, Yunlong ZHANG
  • Publication number: 20120165322
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: June 29, 2011
    Publication date: June 28, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Patent number: 8203001
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: June 19, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
  • Patent number: 8188078
    Abstract: The disclosure relates to compounds of formula (I): wherein A, W, R, R5, and R6 are as defined in the disclosure, or a salt thereof, and to their use as drugs, in particular as c-Met inhibitors.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: May 29, 2012
    Assignee: Sanofi-Aventis
    Inventors: Conception Nemecek, Sylvie Wentzler
  • Publication number: 20120129811
    Abstract: This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventors: Aihua WANG, Yan Zhang, Kristi Anne Leonard, Michael Hawkins, Brett Andrew Tounge, Umar S.M. Maharoof, Joseph Kent Barbay
  • Publication number: 20120115845
    Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.
    Type: Application
    Filed: November 7, 2011
    Publication date: May 10, 2012
    Inventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
  • Patent number: 8173649
    Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: May 8, 2012
    Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma Limited
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
  • Patent number: 8163932
    Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.
    Type: Grant
    Filed: February 8, 2010
    Date of Patent: April 24, 2012
    Assignee: Alinea Pharmaceuticals, Inc.
    Inventors: Michael Lee Jones, David Gunn, John Howard Jones, Michael C. Van Zandt
  • Patent number: 8153813
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: April 10, 2012
    Assignee: Abbott Laboratories
    Inventors: Lawrence A. Black, Marlon D. Cowart, Gregory A. Gfesser, Brian D. Wakefield, Robert J. Altenbach, Huaqing Liu, Chen Zhao, Gin C. Hsieh
  • Publication number: 20120035360
    Abstract: Provided are a method for dual-color imaging of sodium/calcium activities using a two-photon fluorescent probe and a method for preparing the two-photon fluorescent probe. The disclosed two-photon fluorescent probe for detecting calcium ions near the cell membrane reacts with calcium cations to exhibit strong two-photon fluorescence and may be selectively and easily loaded into the cell membrane by forming a complex with a calcium ion. Further, it allows imaging of the distribution of calcium cations in a living cell or tissue since it can selectively detect calcium ions in the living cell or tissue at a depth of 100 to 200 ?m for more than 60 minutes. In addition, by staining the living cell or tissue with two probes of different fluorescent colors, the calcium and sodium activities can be imaged simultaneously at different channels.
    Type: Application
    Filed: October 27, 2010
    Publication date: February 9, 2012
    Inventor: Hwan Myung Kim
  • Patent number: 8110571
    Abstract: This invention relates to benzimidazole and benzothiazole compounds of formula (I) to methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.
    Type: Grant
    Filed: March 25, 2008
    Date of Patent: February 7, 2012
    Assignee: Aventis Pharma S.A.
    Inventors: Conception Nemecek, Francois Clerc
  • Publication number: 20110263593
    Abstract: The disclosure concerns imidazo[1,2-a]pyrimidine derivatives of formula (I) and isomers and pharmaceutically acceptable salts thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.
    Type: Application
    Filed: January 17, 2011
    Publication date: October 27, 2011
    Applicant: sanofi-aventis
    Inventors: Eric Bacque, Dominique Damour, Conception Nemecek, Patrick Nemecek, Laurent Schio, Sylvie Wentzler