Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
  • Publication number: 20130143880
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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, such as schizophrenia.
    Type: Application
    Filed: August 5, 2011
    Publication date: June 6, 2013
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Publication number: 20130137865
    Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.
    Type: Application
    Filed: August 11, 2011
    Publication date: May 30, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto, Hideaki Amada, Hiroki Urabe, Rie Nishikawa, Shuhei Kashiwa ASHIWA
  • Publication number: 20130137661
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Application
    Filed: November 19, 2010
    Publication date: May 30, 2013
    Applicant: SK CHEMICALS CO. LTD.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Publication number: 20130131091
    Abstract: The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. wherein Het represents pyridyl; X represents an oxygen atom; R1, R2, R3, R7, R10a, R10b, R11, and R12 represent a hydrogen atom; R4, R5, and R6 represent a hydrogen atom, hydroxyl, optionally substituted C1-18 alkylcarbonyloxy, optionally substituted C1-18 alkylsulfonyloxy, optionally substituted arylcarbonyloxy, C1-6 alkyloxy-C1-6 alkyloxy, C1-6 alkyloxy-C1-6 alkyloxy-C1-6 alkyloxy; R8 represents a hydrogen atom; and R13a, R13b, and R13c represent methyl.
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Inventors: Kimihiko Goto, Ryo Horikoshi, Kazuhiko Oyama, Yoshimasa Fukuda, Nozomu Nakanishi, Masato Tani, Nobuto Minowa, Masaaki Mitomi, Satoshi Omura, Toshiaki Sunazuka, Hiroshi Tomoda
  • Publication number: 20130123230
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 16, 2013
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Publication number: 20130123284
    Abstract: Provided herein are compounds useful for kinase inhibition.
    Type: Application
    Filed: March 24, 2011
    Publication date: May 16, 2013
    Applicant: AMITECH THERAPEUTIC SOLUTIONS INC
    Inventors: Lee Daniel Arnold, Eric A. Murphy
  • Publication number: 20130090339
    Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.
    Type: Application
    Filed: June 17, 2011
    Publication date: April 11, 2013
    Applicants: THE UAB RESEARCH FOUNDATION, FUZIANS BIOMEDICALS, INC.
    Inventors: Guoxin Wang, Ming Luo, Zhen Yang
  • Patent number: 8415351
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: April 9, 2013
    Assignee: Abbott Laboratories
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Patent number: 8410123
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: April 2, 2013
    Assignee: AstraZeneca AB
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Publication number: 20130079518
    Abstract: The present invention relates to a method of making pyrimidines of formula (III) wherein X1, X2, R1 and R2 have the meanings as defined herein.
    Type: Application
    Filed: November 16, 2012
    Publication date: March 28, 2013
    Inventors: Guenter LINZ, Gerd KRAEMER, Adil DURAN
  • Publication number: 20130078256
    Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: November 20, 2012
    Publication date: March 28, 2013
    Applicant: Korea Research Institute of Chemical Technology
    Inventor: Korea Research Institute of Chemical Technology
  • Patent number: 8404840
    Abstract: The present invention relates to improved processes for the preparation of endolthelin receptor antagonists darusentan and ambrisentan, their salts and intermediates. Processes for the preparation of darusentan and ambrisentan comprise reacting benzophenone with a compound of Formula-3 to provide a compound of Formula-4, which on in-situ treatment with methanol and a suitable acid provides a compound of Formula-5; hydrolyzing the compound of Formula-5 to provide a compound of Formula-6; resolving the compound of Formula-6 to provide a compound of Formula-7; esterifying the compound of Formula-7 to provide a compound of Formula-8; reacting the compound of Formula-8 with a compound of Formula-9 to provide a compound of Formula-10; hydrolyzing the compound of Formula-10 to provide darusentan or ambrisentan; and purifiying darusentan or ambrisentan to provide darusentan or ambrisentan having purity greater than 99.00% by HPLC.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: March 26, 2013
    Assignee: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Chakilam Nagaraju, Achampeta Kodanda Ramprasad
  • Patent number: 8404859
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: March 26, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
  • Publication number: 20130072486
    Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: March 16, 2012
    Publication date: March 21, 2013
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
  • Publication number: 20130059849
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: May 5, 2011
    Publication date: March 7, 2013
    Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
  • Patent number: 8372973
    Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: February 12, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz
  • Patent number: 8362247
    Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: January 29, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara A. Miskowski, Janet L. Ralbovsky, Mark J. Schulz
  • Publication number: 20130023542
    Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.
    Type: Application
    Filed: September 25, 2012
    Publication date: January 24, 2013
    Applicant: Aerpio Therapeutics Inc.
    Inventor: Aerpio Therapeutics Inc.
  • Publication number: 20130023538
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 24, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
  • Patent number: 8354535
    Abstract: The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical composition for use, e.g., in treatment of airway disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: January 15, 2013
    Assignee: Nycomed GmbH
    Inventors: Ulrich Kautz, Matthias Webel, Christian Scheufler, Rolf-Peter Hummel
  • Publication number: 20130012490
    Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Patent number: 8349859
    Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: January 8, 2013
    Assignee: Hutchison Medipharma Enterprises Limited
    Inventors: Wei-Guo Su, Hong Jia, Weihan Zhang, Yumin Cui, Xiaoqiang Yan, Yongxin Ren, Jifeng Duan, Yang Sai
  • Publication number: 20120289700
    Abstract: Provided is a cyclic amine compound, represented by the following formula (I) that has superior acaricidal activity, has superior properties and safety, and which can be synthesized industrially advantageously, a salt thereof and an acaricide: (wherein, Cy1 and Cy2 respectively and independently represent, for example, an aryl group, R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b and R5a respectively and independently represent, for example, a hydrogen atom, R1a and R2a or R3a and R4a may together form, for example, an ethylene group, R10, R11, R20 and R21 respectively and independently represent, for example, an alkyl group, R10 or R11 may respectively or mutually, or together with an atom that bonds on Cy1, form a ring, R20 or R21 on Cy2 may respectively or mutually, or with an atom that bonds on Cy2, form a ring, m represents an integer of 0 to 5, n represents an integer of 0 to 5, p represents an integer of 0 to 5, and r represents an integer of 0 to 5).
    Type: Application
    Filed: December 17, 2010
    Publication date: November 15, 2012
    Inventors: Isami Hamamoto, Keiji Koizumi, Makio Yano, Masahiro Kawaguchi, Hazumi Nomura, Tetsuya Haruyama
  • Patent number: 8309543
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: November 13, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
  • Patent number: 8278316
    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 2, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Saleem Ahmad
  • Publication number: 20120238569
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
    Type: Application
    Filed: February 17, 2012
    Publication date: September 20, 2012
    Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
  • Patent number: 8269002
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: September 18, 2012
    Assignee: AstraZeneca AB
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Publication number: 20120232103
    Abstract: The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.
    Type: Application
    Filed: March 14, 2012
    Publication date: September 13, 2012
    Inventors: Masakazu FUKUSHIMA, Shozo Yamada, Ryo Oyama
  • Patent number: 8252797
    Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: August 28, 2012
    Assignee: Advinus Therapeutics Pvt. Ltd.
    Inventors: Venkata Palle, Sujay Basu, Yogesh Waman, Vidya Ramdas, Dinesh Barawkar, Meena Patel, Anil Panmand
  • Publication number: 20120213733
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: April 3, 2012
    Publication date: August 23, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Patent number: 8242129
    Abstract: A compound having Formula I or II (Formula I) or (Formula II), or a pharmaceutically acceptable salt thereof, wherein X, Z, R1, R2, R11 and R12 are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: August 14, 2012
    Assignee: Exelixis, Inc.
    Inventors: Amy L. Tsuhako, Naing Aay, S. David Brown, Wai Ki Vicky Chan, Hongwang Du, Ping Huang, Brian Kane, Patrick Kearney, Moon Hwan Kim, Elena S. Koltun, Michael Pack, Wei Xu, Peiwen Zhou
  • Patent number: 8236951
    Abstract: There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of the enzyme myeloperoxidase (MPO) is beneficial. Certain novel compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof are disclosed, together with processes for their preparation. The compounds of formulae (Ia) and (Ib) are MPO inhibitors and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders.
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: August 7, 2012
    Assignee: AstraZeneca AB
    Inventors: Sverker Hanson, Gunnar Nordvall, Anna-Karin Tiden
  • Publication number: 20120190684
    Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.
    Type: Application
    Filed: July 22, 2011
    Publication date: July 26, 2012
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
  • Publication number: 20120184521
    Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
    Type: Application
    Filed: September 24, 2010
    Publication date: July 19, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Eiji Kawaminami, Tatsuhisa Takahashi, Takatoshi Kanayama, Yuta Fukuda, Hiroyuki Kaizawa, Yutaka Kondoh, Ryushi Seo, Kazuyuki Kuramoto, Kazuhiko Take, Kazuyuki Sakamoto
  • Publication number: 20120172378
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
    Type: Application
    Filed: December 2, 2011
    Publication date: July 5, 2012
    Inventors: Deirdre Mary Bernadette HICKEY, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Publication number: 20120157487
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: December 9, 2011
    Publication date: June 21, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20120157431
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 21, 2012
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Patent number: 8202861
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 9, 2004
    Date of Patent: June 19, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jesus E Gonzales, III, Andreas P Termin, Esther Martinborough, Nicole Zimmerman
  • Publication number: 20120149677
    Abstract: The present invention is directed to ether benzotriazole 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: August 16, 2010
    Publication date: June 14, 2012
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
  • Publication number: 20120142711
    Abstract: The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: June 21, 2010
    Publication date: June 7, 2012
    Applicant: KTB TUMORFORSCHUNGSGESELLSCHAFT MBH
    Inventors: André Warnecke, Ivonne Müller
  • Patent number: 8188104
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: May 29, 2012
    Assignee: Abbott Laboratories
    Inventors: Charles A. Flengte, Douglas K. Hutchinson, David A. Betebenner, David A. DeGoey, Pamela L. Donner, Warren M. Kati, Allan C. Krueger, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, Christopher E. Motter, John K. Pratt, John T. Randolph, Todd W. Rockway, Kent D. Stewart, Rolf Wagner, Shuang Chen, Yi Gao, Xiaochun Lou, Geoff G. Z. Zhang
  • Patent number: 8178549
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
    Type: Grant
    Filed: October 1, 2008
    Date of Patent: May 15, 2012
    Assignee: Glaxo Group Limited
    Inventors: Barbara Bertani, Francesca Cardullo, Paolo Dambruoso, Paola Marzorati, Fabrizio Micheli, Alessandra Pasquarello, Catia Seri, Giovanna Tedesco
  • Publication number: 20120100104
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 25, 2010
    Publication date: April 26, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Todd W. Rockway, David A. Betebenner, David A. DeGoey, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Dachun Liu, Kenton L. Longenecker, John K. Pratt, Kent D. Stewart, Rolf Wagner, Clarence J. Maring
  • Patent number: 8163750
    Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R2?, L, Het, p and p? are as defined herein, compositions containing them, and their use as medicinal products.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: April 24, 2012
    Assignee: Sanofi-Aventis
    Inventors: Fabienne Thompson, Patrick Mailliet, Jean-Marie Ruxer, Helene Goulaouic, Francois Vallee, Herve Minoux, Fabienne Pilorge, Luc Bertin, Stephane Hourcade, Maria Mendez-Perez, Peter Hamley
  • Publication number: 20120082646
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 25, 2010
    Publication date: April 5, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Publication number: 20120077975
    Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.
    Type: Application
    Filed: December 1, 2011
    Publication date: March 29, 2012
    Inventors: Jeffrey Lyle Gray, Kande K. D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
  • Publication number: 20120071475
    Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 26, 2010
    Publication date: March 22, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Daisuke Taniyama, Yasunori Mitsuoka, Kayoko Hata
  • Publication number: 20120040950
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: December 21, 2010
    Publication date: February 16, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, JR., Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Suganthini S. Nanthakumar, Jingrong Cao, Upul Keerthi Bandarage, Anne-Laure Grillot
  • Publication number: 20120035157
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.
    Type: Application
    Filed: October 14, 2011
    Publication date: February 9, 2012
    Applicant: AstraZeneca AB
    Inventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
  • Publication number: 20120028997
    Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
    Type: Application
    Filed: December 16, 2010
    Publication date: February 2, 2012
    Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz