The Additional Hetero Ring Is Five-membered Having Ring Nitrogen Patents (Class 514/254.01)
  • Publication number: 20090281116
    Abstract: The invention relates to compounds having the formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R9 and A-R9 are as defined herein. Also disclosed are the preparative methods for the compounds of formula (I) and their use in therapy.
    Type: Application
    Filed: May 14, 2009
    Publication date: November 12, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
  • Publication number: 20090253684
    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 diseases such as, for example, COPD.
    Type: Application
    Filed: December 2, 2008
    Publication date: October 8, 2009
    Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 7598250
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.
    Type: Grant
    Filed: August 4, 2004
    Date of Patent: October 6, 2009
    Assignee: Schering Corporation
    Inventors: Jared N. Cumming, Ying Huang, Guoqing Li, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Jianping Pan, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie
  • Patent number: 7595320
    Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.
    Type: Grant
    Filed: August 29, 2007
    Date of Patent: September 29, 2009
    Assignee: Aventis Pharma S.A.
    Inventors: Claude Barberis, Jean-Christophe Carry, Gilles Doerflinger, Dominique Barbalat-Damour, Francois Clerc, Herve Minoux
  • Publication number: 20090239866
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Application
    Filed: July 28, 2006
    Publication date: September 24, 2009
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Jeffrey Michael Axten, Jesus R. Medina
  • Publication number: 20090215765
    Abstract: Neuroprotective compounds for treating optic neuropathies and screening methods for identifying neuroprotective compounds.
    Type: Application
    Filed: April 24, 2006
    Publication date: August 27, 2009
    Applicant: The Johns Hopkins University
    Inventors: John Barnwell Kerrison, Donald J. Zack
  • Publication number: 20090215795
    Abstract: A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.
    Type: Application
    Filed: July 17, 2008
    Publication date: August 27, 2009
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musha, Motoji Kogushi, Tsutomu Kawata, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
  • Publication number: 20090192136
    Abstract: A compound of formula wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
    Type: Application
    Filed: July 22, 2008
    Publication date: July 30, 2009
    Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
  • Publication number: 20090186867
    Abstract: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 27, 2009
    Publication date: July 23, 2009
    Inventors: Alan David Borthwick, Richard Jonathan Hatley, Deirdre Mary Bernadette Hickey, John Liddle, David George Hubert Livermore, Andrew McMurtrie Mason, Neil Derek Miller, Fabrizio Nerozzi, Steven Leslie Sollis, Anna Katrin Szardenings, Paul Graham Wyatt
  • Patent number: 7560546
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: July 14, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
  • Publication number: 20090176799
    Abstract: Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity with regard to inhibition of other classes of PDEs. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein.
    Type: Application
    Filed: December 1, 2008
    Publication date: July 9, 2009
    Inventors: Liu Ruiping, Mike De Vivo, Hans-Jurgen Ernst Hess, Allen Hopper, Erik Kreuster, Ashok Tehim
  • Publication number: 20090156571
    Abstract: The present invention discloses novel compounds of Formula I: possessing 11 ?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 ?-HSD type 1 activity.
    Type: Application
    Filed: April 19, 2007
    Publication date: June 18, 2009
    Inventors: Thomas Daniel Aicher, Zhaogen Chen, Ronald Jay Hinklin, Gary Alan Hite, Alexei Pavlovych Krasutsky, Renhua Li, Jefferson Ray McCowan, Ashraf Saeed, Nancy June Snyder, James Lee Toth, Owen Brendan Wallace, Leonard Larry Winneroski, Jr., Yanping Xu, Jeremy Schulenburg York
  • Patent number: 7528136
    Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, R4, R5, X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: May 5, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bo Han, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
  • Patent number: 7524848
    Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: April 28, 2009
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
  • Patent number: 7524844
    Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: April 28, 2009
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Abraham Thomas, Balasubramanian Gopalan, V.S. Prasada Rao Lingam, Daisy Manish Shah
  • Publication number: 20090105256
    Abstract: Prodrugs of ion channeling modulating compounds, including, for example, prodrugs of the ion channel modulating compound of the following formula: are described herein, as well as methods of making and using such prodrugs and pharmaceutical compositions containing such prodrugs.
    Type: Application
    Filed: March 31, 2005
    Publication date: April 23, 2009
    Applicant: Cardiome Pharma Corp.
    Inventors: Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Adewale Eniale, Bertrand M.C. Plouvier
  • Publication number: 20090099182
    Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.
    Type: Application
    Filed: April 24, 2007
    Publication date: April 16, 2009
    Inventors: Renhua Li, Thomas Edward Mabry, Owen Brendan Wallace, Leonard Larry Winneroski, JR., Yanping Xu
  • Publication number: 20090087405
    Abstract: The invention relates to a method of treating immunologic diseases or pathological conditions involving an immunologic component using certain Lck inhibitors already known as kinase inhibitors for therapy in oncology, optionally in combination with one or more other drugs selected from NSAIDs, steroids, DMARDs, immunsuppressives, biologic response modifiers and antinfectives, pharmaceutical compositions comprising said Lck inhibitors together with said other drugs, and the use of the Lck inhibitors for the manufacture of a pharmaceutical composition for the treatment of immunologic diseases or pathological conditions involving an immunologic component.
    Type: Application
    Filed: December 12, 2008
    Publication date: April 2, 2009
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Gerald Juergen ROTH, Armin HECKEL, Rainer WALTER, Frank HILBERG, Rudolf HAUPTMANN, Martin Friedrich STEFANIC, Florian COLBATZKY, Steffen ERNST
  • Publication number: 20090076020
    Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
    Type: Application
    Filed: August 21, 2008
    Publication date: March 19, 2009
    Applicant: ASTRAZENECA AB
    Inventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
  • Publication number: 20090069326
    Abstract: The present invention discloses novel compounds of Formula I: (I) possessing 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11?-HSD type 1 activity.
    Type: Application
    Filed: April 23, 2007
    Publication date: March 12, 2009
    Inventors: John Gordon Allen, Alexei Pavlovych Krasutsky, Owen Brendan Wallace, Yanping Xu, Jeremy Schulenburg York
  • Publication number: 20090069324
    Abstract: Compounds that bind to Bfl-1 as well as conjugates of such compounds are provided. Various embodiments additionally provide methods of using such compounds to identify additional anti-apoptotic Bfl-1 binding compounds. Methods of using such compounds to increase apoptosis in a cell are also provided.
    Type: Application
    Filed: May 30, 2008
    Publication date: March 12, 2009
    Applicant: The Burnham Institute
    Inventors: John C. Reed, Dayong Zhai, Shinichi Kitada, Eduard Sergienko
  • Patent number: 7482346
    Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
    Type: Grant
    Filed: August 22, 2006
    Date of Patent: January 27, 2009
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
  • Patent number: 7482335
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: January 27, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney, Douglas G. Batt, John V. Duncia, Daniel S. Gardner, Soo S. Ko, Anurag S. Srivastava, Michael G. Yang
  • Publication number: 20090023708
    Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
    Type: Application
    Filed: October 25, 2006
    Publication date: January 22, 2009
    Applicant: UCB PHARMA, S.A.
    Inventors: Sylvain Celanire, Luc Quere, Frederic Denonne, Laurent Provins
  • Patent number: 7468437
    Abstract: The present invention is directed to certain phenyl pyrrolidine ether compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, depression, and anxiety.
    Type: Grant
    Filed: September 24, 2004
    Date of Patent: December 23, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. DeVita, Peter Lin, Sander G. Mills, Jonathan R. Young
  • Patent number: 7468371
    Abstract: Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: December 23, 2008
    Assignee: Abbott Laboratories Inc.
    Inventors: Lee D. Arnold, Jürgen Dinges, Richard W. Dixon, Stevan W. Djuric, Anna M. Ericsson, Kimba Fischer, Alan F. Gasiecki, Vijaya J. Gracias, James H. Holms, Makoto Takeshita, Michael R. Michaelides, Melanie A. Muckey, Paul Rafferty, Douglas H. Steinman, Carol K. Wada, Zhiren Xia, Irini Akritopoulou-Zanze, Henry Q. Zhang
  • Publication number: 20080306086
    Abstract: The present invention relates to a compound of formula I wherein R2 R3, R4, R5, X, n, and o are as defined herein and to a pharmaceutically acceptable acid addition salt thereof which are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: May 30, 2008
    Publication date: December 11, 2008
    Inventors: Bo Han, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
  • Publication number: 20080306085
    Abstract: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Application
    Filed: August 20, 2008
    Publication date: December 11, 2008
    Inventors: Richard Apodaca, Nicholas I. Carruthers, Curt A. Dvorak, Dale A. Rudolph, Chandravadan R. Shah, Wei Xiao
  • Publication number: 20080287419
    Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
    Type: Application
    Filed: May 15, 2008
    Publication date: November 20, 2008
    Applicant: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
  • Publication number: 20080275043
    Abstract: The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
    Type: Application
    Filed: October 26, 2005
    Publication date: November 6, 2008
    Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace, John Gordon Allen, Zhaogen Chen, Thomas Edward Mabry, Jefferson Ray McCowan, Nancy June Snyder, Leonard Larry Winneroski
  • Publication number: 20080275021
    Abstract: The invention relates to pyrrolidine derivatives of formula wherein R1, R2, R3, n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
    Type: Application
    Filed: April 14, 2008
    Publication date: November 6, 2008
    Inventors: Caterina Bissantz, Torsten Hoffmann, Philippe Jablonski, Henner Knust, Mathias Nettekoven, Hasane Ratni, Xihan Wu
  • Publication number: 20080275027
    Abstract: The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.
    Type: Application
    Filed: July 17, 2006
    Publication date: November 6, 2008
    Inventors: Rachael Ann Ancliff, Mark James Bamford, Simon Teanby Hodgson, Christopher Allan Parr, Panayiotic Alexandrou Procopiou, David Matthew Wilson, Michael Woodrow
  • Publication number: 20080254040
    Abstract: The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
    Type: Application
    Filed: June 17, 2008
    Publication date: October 16, 2008
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Martin Friedrich STEFANIC, Frank HILBERG, Gerd MUNZERT, Flavio SOLCA, Anke BAUM, Jacobus C.A. van MEEL
  • Patent number: 7432264
    Abstract: Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.
    Type: Grant
    Filed: August 9, 2004
    Date of Patent: October 7, 2008
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Elizabeth Anne Jefferson, Eric E. Swayze, Punit P. Seth, Dale E. Robinson, Jr.
  • Publication number: 20080242676
    Abstract: Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
    Type: Application
    Filed: June 11, 2008
    Publication date: October 2, 2008
    Applicant: Lupin Limited
    Inventors: Sudershan Kumar Arora, Neelima Sinha, Sanjay Jain, Ram Shankar Upadhayaya, Gourhari Jana, Shankar Ajay, Rakesh Kumar Sinha
  • Publication number: 20080241077
    Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+ exchange is of therapeutic benefit.
    Type: Application
    Filed: June 6, 2008
    Publication date: October 2, 2008
    Inventors: Christian Eickmeier, Peter Sieger, Werner Rall, Volkmar Koerner, Rolf Herter
  • Publication number: 20080234273
    Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
    Type: Application
    Filed: June 3, 2006
    Publication date: September 25, 2008
    Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
  • Patent number: 7419980
    Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Grant
    Filed: October 12, 2004
    Date of Patent: September 2, 2008
    Assignee: Wyeth
    Inventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
  • Publication number: 20080206137
    Abstract: The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography.
    Type: Application
    Filed: January 11, 2006
    Publication date: August 28, 2008
    Inventors: Christopher John Helal, Gunnar Antoni, Bengt Langstrom, Jia Zhi Sheng, Susan Beth Jaynes-Sobolov, Timothy John McCarthy
  • Patent number: 7414047
    Abstract: Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: August 19, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Richard L. Apodaca, Jill A. Jablonowski, Kiev S. Ly, Chandravadan R. Shah, Devin M. Swanson, Wei Xiao
  • Publication number: 20080194581
    Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds including the intermediates therefor and their therapeutic use.
    Type: Application
    Filed: April 14, 2008
    Publication date: August 14, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Francis BARTH, Christian CONGY, Laurent HORTALA, Murielle RINALDI-CARMONA
  • Publication number: 20080176854
    Abstract: The present invention relates to nitro-substituted phenyl-piperazine compounds of general formula I, a process for their preparation, medicaments comprising said nitro-substituted phenyl-piperazine compounds as well as the use of said nitro-substituted phenylpiperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
    Type: Application
    Filed: December 29, 2005
    Publication date: July 24, 2008
    Applicant: Laboratorios Del Dr. Esteve S.A
    Inventors: Andrea Aschenbrenner, Juergen Kraus, Stefan Tasler, Andreas Wuzik, Jordi-Ramon Quintana-Ruiz
  • Patent number: 7396834
    Abstract: Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Grant
    Filed: November 5, 2003
    Date of Patent: July 8, 2008
    Assignee: AstraZeneca AB
    Inventors: William Brown, Andrew Griffin, Niklas Plobeck, Christopher Walpole
  • Publication number: 20080153821
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; A: —CH2— or —S—, B: CH or N, R1: H, a lower alkyl group, etc., X: a single bonding arm, —CO—, -Alk-CO—, —COCH2—, -Alk-O—, —O—CH2—, —SO2—, —S—, —COO—, —CON(R3)—, -Alk-CON(R3)—, —CON(R3)CH2—, —NHCH2—, etc., R3: hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R2: (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is —CO—, then B is N, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 7, 2007
    Publication date: June 26, 2008
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Patent number: 7390799
    Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: June 24, 2008
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
  • Publication number: 20080139575
    Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
    Type: Application
    Filed: July 31, 2007
    Publication date: June 12, 2008
    Inventors: Pu-Ping Lu, Xiangping Qian, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans
  • Patent number: 7381727
    Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds and their therapeutic use.
    Type: Grant
    Filed: January 22, 2007
    Date of Patent: June 3, 2008
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
  • Publication number: 20080113968
    Abstract: A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.
    Type: Application
    Filed: April 10, 2007
    Publication date: May 15, 2008
    Applicant: Novo Nordisk A/S
    Inventors: Florencio Zaragoza Dorwald, Knud Erik Andersen, Jan Lindy Sorensen
  • Patent number: 7358239
    Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is
    Type: Grant
    Filed: March 14, 2005
    Date of Patent: April 15, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
  • Patent number: 7358253
    Abstract: Provided are compounds of formula (I) which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts, graft versus host diseases, atherosclerosis, vascular occlusion due to vascular injury such as angioplasty, restenosis, obesity, syndrome X, impaired glucose tolerance, polycystic ovary syndrome, hypertension, heart failure, chronic obstructive pulmonary disease, CNS diseases such as Alzheimer disease or amyotrophic lateral sclerosis, cancer, infectious diseases such as AIDS, septic shock or adult respiratory distress syndrome, ischemia/reperfusion injury e.g. myocardial infarction, stroke, gut ischemia, renal failure or hemorrhage shock, or traumatic shock, e.g. traumatic brain injury. The compounds of formula I are also useful in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory disease or disorders or autoimmune diseases e.g.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: April 15, 2008
    Assignee: Novartis AG
    Inventors: Jean-Pierre Evenou, Peter Von Matt, Jürgen Wagner, Gerhard Zenke