1,2-diazines Which Contain An Additional Hetero Ring Patents (Class 544/238)
  • Patent number: 8604038
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Patent number: 8604040
    Abstract: Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y1, Y2, Y3, L1, L2, RG, and R1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer CropScience AG
    Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Nicola Rahn, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Patent number: 8604036
    Abstract: Compounds of the formula (I), in which R1, R2, R3, W and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: December 10, 2013
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Patent number: 8604016
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: December 10, 2013
    Assignee: Calithera Biosciences Inc.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Publication number: 20130324544
    Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Application
    Filed: November 25, 2011
    Publication date: December 5, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
  • Publication number: 20130324529
    Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.
    Type: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
  • Publication number: 20130323203
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: August 2, 2013
    Publication date: December 5, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
  • Patent number: 8598175
    Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: December 3, 2013
    Assignees: Sanofi, Mitsubishi Tanabe Pharma Corporation
    Inventors: Nathalie Chereze, Thierry Gallet, Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
  • Patent number: 8598176
    Abstract: A pyridazine compound of the formula: has an excellent plant disease controlling effect.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: December 3, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Akio Manabe
  • Patent number: 8592591
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: November 26, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Swen Hölder, Armin Zülch, Thomas Bär, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
  • Patent number: 8592383
    Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: November 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
  • Publication number: 20130310361
    Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or analplastic lymphoma kinase (ALK).
    Type: Application
    Filed: July 23, 2013
    Publication date: November 21, 2013
    Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
  • Publication number: 20130310379
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 21, 2011
    Publication date: November 21, 2013
    Applicant: CONSTELLATION PHARMACEUTICALS
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
  • Publication number: 20130310364
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Publication number: 20130310393
    Abstract: Disclosed are heteroaryl compounds of Formula (I), (I), or pharmaceutically acceptable salts thereof, wherein Z is CH or N; W is CR3 or N; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: September 23, 2011
    Publication date: November 21, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Audris Huang
  • Publication number: 20130310357
    Abstract: Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: May 26, 2011
    Publication date: November 21, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventor: Gang Liu
  • Publication number: 20130310375
    Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 21, 2013
    Applicant: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • Publication number: 20130310342
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.
    Type: Application
    Filed: October 24, 2012
    Publication date: November 21, 2013
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
  • Patent number: 8586588
    Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds and/or their pharmaceutically acceptable salts may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: November 19, 2013
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
  • Publication number: 20130303510
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
  • Publication number: 20130303509
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
  • Patent number: 8580790
    Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: November 12, 2013
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Patent number: 8580781
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: November 12, 2013
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • 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
  • Patent number: 8580791
    Abstract: Novel acid addition salts of 6-{2-[1-(6-methyl-3-pyridazinyl)-4-piperidinyl]ethoxy}-3-ethoxy-1,2-benzisoxazole of following formula are disclosed, particularly a crystalline form of a bis-dihydrogenphosphate salt: Such compounds have particular advantages with regard to treatment of picornaviruses. Related pharmaceutical compositions and methods of treating a picornavirus infection are also disclosed.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: November 12, 2013
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Jane Ryan, Margaret Anne Butt
  • Publication number: 20130296320
    Abstract: Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, particularly, cancer. The present invention provides a compound represented by the following general formula (I) or a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are the same or different and each represent C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are the same or different and each represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.; R4 represents a hydrogen atom, —CO—R6, —N(R7)(R8) etc.
    Type: Application
    Filed: January 6, 2012
    Publication date: November 7, 2013
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
  • Publication number: 20130296310
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
    Type: Application
    Filed: July 1, 2013
    Publication date: November 7, 2013
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Publication number: 20130296333
    Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).
    Type: Application
    Filed: July 9, 2013
    Publication date: November 7, 2013
    Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
  • Publication number: 20130296332
    Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
    Type: Application
    Filed: July 1, 2013
    Publication date: November 7, 2013
    Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
  • Patent number: 8575360
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: November 5, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rene Marc Lemieux, Steven Richard Brunette, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Bryan McKibben, Craig Andrew Miller, Antonio J. M. Barbosa
  • Patent number: 8575163
    Abstract: Pyrrolopyridinylpyrimidin-2-ylamine derivatives of the formula (I), in which R1-R6 and R1 have the meanings indicated in claim 1, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: November 5, 2013
    Assignee: Merck Patent GmbH
    Inventors: Margarita Wucherer-Plietker, Christina Esdar, Brian Hodous
  • Patent number: 8575167
    Abstract: The present invention aims to provide a novel SCD inhibitor. The present invention relate to SCD inhibitor comprising A compound represented by the formula (I) wherein R is an optionally substituted cyclic group or an optionally substituted carbamoyl group, provided that R is not an optionally substituted 7-pyrido[2,3-d]pyrimidyl group; ring A is an optionally further substituted pyridazine ring; R1, R2, R3, R4, R11, R12, R13 and R14 are each independently a hydrogen atom or a substituent, or R1 and R11 in combination, R2 and R12 in combination, R3 and R13 in combination, or R4 and R14 in combination optionally form an oxo group, or R2 and R4 in combination optionally form a bond or an alkylene cross-linkage; m and n are each independently an integer of 0 to 2; ring B is an optionally substituted ring, provided that the two atoms constituting ring B, which are adjacent to the spiro carbon atom, are not oxygen atoms at the same time, or a salt thereof, or a prodrug thereof.
    Type: Grant
    Filed: February 5, 2008
    Date of Patent: November 5, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Kenichi Miyata, Osamu Kubo
  • Publication number: 20130289013
    Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.
    Type: Application
    Filed: June 24, 2013
    Publication date: October 31, 2013
    Inventors: Qun Kevin FANG, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
  • Patent number: 8569487
    Abstract: A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections. Methods of making and formulating compound (1) are provided.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: October 29, 2013
    Assignees: Gilead Sciences, Inc., K.U. Leuven Research & Development
    Inventors: Steven S. Bondy, Terrence C. Dahl, David A. Oare, Reza Oliyai, Winston C. Tse, Vahid Zia
  • Patent number: 8569488
    Abstract: A crystalline compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating crystalline compound (1) are provided.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: October 29, 2013
    Assignees: Gilead Sciences, Inc., K.U. Leuven Research & Development
    Inventors: Eric D. Dowdy, Kenneth M. Kent, Norma J. Tom, Vahid Zia
  • Publication number: 20130281433
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Publication number: 20130281690
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 24, 2013
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20130281428
    Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.
    Type: Application
    Filed: January 30, 2013
    Publication date: October 24, 2013
    Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
  • Publication number: 20130274468
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 17, 2013
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20130274469
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 17, 2013
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Patent number: 8557819
    Abstract: The invention relates to compounds having general formula (I), wherein R is as defined herein. The invention also relates to acid addition salt, a hydrate or a solvate of compounds of formula (I). The invention further relates to the method of preparing said compounds and to the use of same in therapeutics.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: October 15, 2013
    Assignee: Sanofi
    Inventors: Frederic Galli, Odile Leclerc, Alistair Lochead, Julien Vache
  • Patent number: 8557813
    Abstract: Compounds of the formula I in which R1, R2, R3, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: October 15, 2013
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Publication number: 20130267521
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 10, 2013
    Applicants: Intellikine LLC, Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
  • Publication number: 20130267519
    Abstract: This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
    Type: Application
    Filed: April 3, 2013
    Publication date: October 10, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Shawn David Erickson, Patrizio Mattei, Hans Richter
  • Publication number: 20130267529
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 10, 2013
    Inventors: Michael Patrick Dillon, Nancy Elizabeth Krauss
  • Patent number: 8551984
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: October 8, 2013
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou
  • Patent number: 8552205
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Antonio Jose del Moral Barbosa, Jr., Joerg Martin Bentzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan McKibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
  • Publication number: 20130261129
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: March 29, 2013
    Publication date: October 3, 2013
    Applicant: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Wei, Lijuan Jane Wang
  • Publication number: 20130261299
    Abstract: The present invention relates to compounds of formula I: in which L, W, X, Y, Z, m, p, R1, R2, R3, R4 and R7 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.
    Type: Application
    Filed: May 30, 2013
    Publication date: October 3, 2013
    Applicant: Novartis AG
    Inventors: Feng He, Stefan Peukert, Karen Marie Miller-Moslin, Naeem Yusuff, Zhuoliang Chen, Bharat Lagu
  • Publication number: 20130261103
    Abstract: Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: August 31, 2011
    Publication date: October 3, 2013
    Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.
    Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young