Five-membered Nitrogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/253.09)
  • Publication number: 20040082566
    Abstract: The present invention relates to pyrrolidine sulfonamides, pharmaceutical compositions containing them and their use as urotensin II antagonists.
    Type: Application
    Filed: September 26, 2003
    Publication date: April 29, 2004
    Inventors: Dashyant Dhanak, Steven D Knight, Jian Jin, Ralph A Rivera, Anthony Sapienza
  • Publication number: 20040077640
    Abstract: The invention concerns novel sodium channel modulators derived from 2-piperidylimidazoles. The inventive compounds correspond to the general formula (I), wherein: R1 represents a hydrogen atom or an —X—Y—R4 radical wherein —X—Y represents a bond, a —CO—, —CO—O——CO—NH— or —CS—NH— radical and R4 represents an alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl radical, said radicals being optionally substituted; R2 represents in particular an alkyl, cycloalkyl, cycloalkylalkyl or aryl radical optionally substituted; and R3 represents a hydrogen atom or an alkyl, cycloalkyl, cycloalkylalkyl, or aryl radical optionally substituted.
    Type: Application
    Filed: June 11, 2003
    Publication date: April 22, 2004
    Inventors: Dennis Bigg, Jacques Pommier, Anne-Marie Liberatore
  • Patent number: 6723742
    Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.
    Type: Grant
    Filed: May 29, 2003
    Date of Patent: April 20, 2004
    Assignee: Novartis AG.
    Inventors: René Lattmann, Pierre Acklin
  • Patent number: 6723723
    Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, of formula (I) wherein: A is an optionally substituted 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 ring heteroatoms selected from oxygen, nitrogen and sulphur atoms; which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to phaautical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: April 20, 2004
    Assignee: AstraZeneca
    Inventor: Peter W. R. Caulkett
  • Publication number: 20040072838
    Abstract: The present invention provides a compound of formula (1) wherein R1-R5, R25, R26, Y and X2 are defined as in claim 1. The compounds activate human peroxisome proliferator activated receptors (hPPARs) and arc useful for the treatment of associated disorders such as cardiovascular disease and hypercholesteremia.
    Type: Application
    Filed: October 31, 2003
    Publication date: April 15, 2004
    Inventors: Pierette Banker, Rodolfo Cadilla, Millard Hurst Lambert lll, Stephen William Rafferty, Daniel David Sternbach, Marcos Luis Sznaidman
  • Publication number: 20040067961
    Abstract: The use of CCR5 antagonists of the formula 1
    Type: Application
    Filed: September 23, 2003
    Publication date: April 8, 2004
    Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
  • Publication number: 20040063721
    Abstract: The present invention relates to a method for treating thermoregulatory disorders by administering compounds and compositions of compounds which by modulating 5HT levels activate the 5HT2a receptor. The invention also relates to therapy using 5HT1a antagonists and SRIs in combination and pharmaceutical compositions and products containing it. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the claims.
    Type: Application
    Filed: August 14, 2003
    Publication date: April 1, 2004
    Applicant: Wyeth
    Inventors: Darlene Coleman Deecher, Istvan Jozsef Merchenthaler, Liza Leventhal, Kimberly Jean Sipe, Lawrence Thomas O'Connor, Terrance Andree
  • Publication number: 20040053914
    Abstract: A compound of formula 1
    Type: Application
    Filed: May 2, 2003
    Publication date: March 18, 2004
    Inventors: Parviz Gharagozloo, Khondaker Islam, Donald J. Kyle, Qun Sun, Laykea Tafesse, John William Frank Whitehead, Ji Yang, Xiaoming Zhou
  • Publication number: 20040044007
    Abstract: The present invention relates to methods of treating psychiatric or neurologic disorders, in particular psychoses, by administration of a compound formula of (I) 1
    Type: Application
    Filed: June 17, 2003
    Publication date: March 4, 2004
    Applicant: H. Lundbeck A/S
    Inventors: Jan Kehler, Benny Bang-Andersen
  • Publication number: 20040044203
    Abstract: The present invention provides compounds of formula I 1
    Type: Application
    Filed: October 2, 2002
    Publication date: March 4, 2004
    Inventors: Mark D. Wittman, Neelakantan Balasubramanian, Upender Velaparthi, Kurt Zimmermann, Mark G. Saulnier, Peiying Liu, Xiaopeng Sang, David B. Frennesson, Karen M. Stoffan, James G. Tarrant, Anne Marinier, Stephan Roy
  • Patent number: 6699864
    Abstract: The present invention provides compounds of the formula: wherein R1-R8, X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT1A receptor.
    Type: Grant
    Filed: June 20, 2002
    Date of Patent: March 2, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Christian Krog-Jensen, Mario Rottländer, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
  • Publication number: 20040024023
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: July 17, 2003
    Publication date: February 5, 2004
    Applicant: Wyeth
    Inventors: Ronald Charles Bernotas, Steven Edward Lenicek
  • Patent number: 6686370
    Abstract: Disclosed are compounds of the formula (I) wherein A, R1, R2, R3, R4 and X1 are as disclosed herein. The compounds have affinity for the ORL1 receptor and are useful in the treatment of chronic and acute pain.
    Type: Grant
    Filed: December 6, 2000
    Date of Patent: February 3, 2004
    Assignee: Euro-Celtique S.A.
    Inventors: Donald Kyle, R. Richard Goehring
  • Publication number: 20030236282
    Abstract: The present invention relates to substituted piperidines of general formula 1
    Type: Application
    Filed: March 13, 2003
    Publication date: December 25, 2003
    Applicant: Boehringer ingelheim Pharma GmbH & Co.
    Inventors: Rudolf Hurnaus, Klaus Rudolf, Stephan Georg Mueller, Dirk Stenkamp, Philipp Lustenberger, Alexander Dreyer, Kai Gerlach, Marcus Schindler, Kirsten Arndt, Eckhart Bauer
  • Publication number: 20030232814
    Abstract: Compounds of the general formula (I): 1
    Type: Application
    Filed: May 16, 2003
    Publication date: December 18, 2003
    Inventors: Bjorn M. Nilsson, Erik Ringberg
  • Publication number: 20030232807
    Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.
    Type: Application
    Filed: October 4, 2002
    Publication date: December 18, 2003
    Inventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
  • Publication number: 20030207892
    Abstract: The invention relates to novel N-substituted indole-3-glyoxylamides, to processes for their preparation and to their pharmaceutical use. The compounds have antiasthmatic, antiallergic and immuno-suppressant/immunomodulating actions.
    Type: Application
    Filed: April 1, 2003
    Publication date: November 6, 2003
    Inventors: Guillaume Lebaut, Cecilia Menciu, Bernhard Kutscher, Peter Emig, Stefan Szelenyi, Kay Brune
  • Patent number: 6638935
    Abstract: The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: October 28, 2003
    Assignee: Zentaris AG
    Inventors: Peter Emig, Eckhard Günther, Bernhard Kutscher, Bernd Nickel, Jürgen Schmidt, Anita Storch
  • Patent number: 6635646
    Abstract: Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interferon-alfa, e.g., pegylated interferon alfa-2b, in association with a therapeutically effective amount of a CCR5 antagonist or preferably further in association with a therapeutically effective amount of at least one of ribavirin, IL-2, IL-12, pentafuside alone or in combination with a therapeutically effective amount of an anti-HIV-1 drug therapy, e.g., HAART are disclosed.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: October 21, 2003
    Assignee: Schering Corporation
    Inventor: Mark A. Laughlin
  • Patent number: 6635640
    Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: October 21, 2003
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
  • Publication number: 20030195356
    Abstract: 4-Aryl-1-(indanmethyl, dibydrobenzofuramethyl or dihydrobenzotbiophenemethyl) piperidine, -tetrabydropyridine or -piperazine compounds of general formula (I) 1
    Type: Application
    Filed: April 14, 2000
    Publication date: October 16, 2003
    Inventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
  • Patent number: 6632828
    Abstract: Compounds of the formula I or a pharmaceutically acceptable salt, solvate or N-oxide thereof, wherein X is ═CH— or ═N—; Y is H, halogen, trihaloalkyl, alkyl, alkenyl, cycloalkyl, cycloalkyl, SH, —S-alkyl, or —CN. R is alkyl, —CF3, cycloalkyl, heterocycloalkyl, heterocycloalkyl-alkyl, heteroarylalky or adamantyl, or optionally substituted phenyl, phenoxyalkyl, phenylthioalkyl, pyridyl, thienyl, thiazolyl, pyrazinyl, 1,2,5,6-tetrahydropyridine or  wherein R10 and R11 are hydrogen, alkyl or together form a cycloalkyl, are disclosed, as well as pharmaceutical compositions and methods of using said compounds in the treatment of eating disorders and diabetes.
    Type: Grant
    Filed: July 23, 2002
    Date of Patent: October 14, 2003
    Assignee: Schering Corporation
    Inventors: Andrew W. Stamford, Craig D. Boyle, Ying Huang
  • Publication number: 20030176445
    Abstract: This invention provides a compound of the formula (I): 1
    Type: Application
    Filed: February 13, 2003
    Publication date: September 18, 2003
    Applicant: Pfizer Inc.
    Inventors: Yoshiyuki Okumura, Mitsuhiro Kawamura, Makato Kawai, Noriaki Murase, Takafumi Ikeda
  • Publication number: 20030166649
    Abstract: This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: 1
    Type: Application
    Filed: November 22, 2002
    Publication date: September 4, 2003
    Applicant: Wyeth
    Inventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
  • Publication number: 20030166633
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1, R2 and R3 represent various functional groups, and one of X1 and X2 is N and the other is NR10; and their use as pharmaceuticals.
    Type: Application
    Filed: October 29, 2002
    Publication date: September 4, 2003
    Inventors: Laramie Mary Gaster, Michael Stewart Hadley, John David Harling, Frank Peter Harrington, Jag Paul Heer, Thomas Daniel Heightman, Andrew Hele Payne
  • Publication number: 20030162790
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: September 6, 2002
    Publication date: August 28, 2003
    Inventors: Marlon D. Cowart, Pramila A. Bhatia, Jerome F. Daanen, Andrew O. Stewart, Meena V. Patel, Teodozyj Kolasa, Jorge D. Brioni, Jeffrey Rohde, Kenneth M. Engstrom
  • Publication number: 20030158208
    Abstract: The present invention provides a method of treating or preventing a novelty-seeking disorder such as pathological gambling, attention deficit disorder with hyperactivity disorder, substance addiction, drug addiction, alcohol addiction and sex addiction. using a compound which is a dopamine D4 receptor ligand, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 10, 2003
    Publication date: August 21, 2003
    Applicant: Pfizer Inc.
    Inventors: Stevin H. Zorn, Mark A. Sanner, Antor F. Fliri, Patricia A. Seymour
  • Patent number: 6602874
    Abstract: A compound of the formula wherein X, Y, Z, R2 and R3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1, agonist or antagonist is indicated.
    Type: Grant
    Filed: May 22, 2001
    Date of Patent: August 5, 2003
    Assignee: Pfizer Inc.
    Inventor: Harry R. Howard
  • Publication number: 20030144309
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: May 16, 2002
    Publication date: July 31, 2003
    Inventor: Young Choon-Moon
  • Patent number: 6596750
    Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.
    Type: Grant
    Filed: September 23, 2002
    Date of Patent: July 22, 2003
    Assignee: Novartis AG
    Inventors: René Lattmann, Pierre Acklin
  • Patent number: 6596745
    Abstract: Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: July 22, 2003
    Assignee: Alteon, Inc.
    Inventor: Martin Gall
  • Publication number: 20030130275
    Abstract: The invention relates to novel sulphonamide compounds having 5-HT7 antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
    Type: Application
    Filed: November 27, 2002
    Publication date: July 10, 2003
    Applicant: SmithKline Beecham p.l.c.
    Inventor: Peter John Lovell
  • Patent number: 6586418
    Abstract: This invention relates generally to heteroaryl-phenyl substituted compounds that are inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: July 1, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Donald J. P. Pinto, Mimi L Quan
  • Publication number: 20030114465
    Abstract: Compounds of the formula I 1
    Type: Application
    Filed: July 23, 2002
    Publication date: June 19, 2003
    Inventors: Andrew W. Stamford, Craig D. Boyle, Ying Huang
  • Patent number: 6573262
    Abstract: The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: June 3, 2003
    Assignee: Bristol-Myers Sqibb Company
    Inventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
  • Publication number: 20030087912
    Abstract: In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more of diseases associated with the CCR5 receptor.
    Type: Application
    Filed: March 27, 2002
    Publication date: May 8, 2003
    Applicant: SCHERING CORPORATION
    Inventors: John W. Clader, Sue-Ing Y. Lin, Stuart W. McCombie, Pradeep B. Pushpavanam, Susan Vice
  • Patent number: 6555542
    Abstract: Sulfonamide lactams of the following formula wherein X, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R7 and R8 are as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.
    Type: Grant
    Filed: January 29, 2002
    Date of Patent: April 29, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen P. O'Connor, Michael Lawrence, Yan Shi, Philip D. Stein
  • Patent number: 6552016
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: April 22, 2003
    Assignee: Curis, Inc.
    Inventors: Anthony David Baxter, Edward Andrew Boyd, Oivin M. Guicherit, Stephen Price, Lee Rubin
  • Publication number: 20030069240
    Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
    Type: Application
    Filed: February 13, 2002
    Publication date: April 10, 2003
    Inventors: J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei
  • Publication number: 20030069252
    Abstract: The use of CCR5 antagonists of the formula 1
    Type: Application
    Filed: January 30, 2002
    Publication date: April 10, 2003
    Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
  • Publication number: 20030069245
    Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
    Type: Application
    Filed: December 19, 2001
    Publication date: April 10, 2003
    Inventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
  • Patent number: 6537995
    Abstract: A method is provided for treating or preventing a disorder or condition selected from hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant personality disorder, premature ejaculation, eating disorders, obesity, cluster headache, migraine, pain, obsessive-compulsive disorder, panic disorder, endocrine disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, premenstrual syndrome, fibromyalgia syndrome, stress incontinence, chronic paroxysmal hemicrania and headache in a mammal, comprising administering to a mammal in need of such treatment or prevention an amount of a compound of the formula (I) or the pharmaceutically acceptable salt thereof; wherein X, Y, Z, R2 and R3 are as defined herein.
    Type: Grant
    Filed: May 22, 2001
    Date of Patent: March 25, 2003
    Assignee: Pfizer Inc.
    Inventor: Harry R. Howard
  • Publication number: 20030050311
    Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
    Type: Application
    Filed: September 3, 2002
    Publication date: March 13, 2003
    Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
  • Patent number: 6521623
    Abstract: A compound of formula (I) wherein: R1 is C1-C6-alkyl substituted by a group selected from OH, C1-C6-alkoxy, —OCONHC1-C6-alkyl, —OCONHC1-C6-alkyl, —NHSO2C1-C6-alkyl, and —NHCOC1-C6-alkyl, or R1 is C1-C6-alkyl substituted by a saturated or unsaturated 5- or 6-membered heterocycle containing one or two heteroatoms selected from the group consisting of nitrogen and oxygen, the heterocycle optionally substituted by a group selected from C1-C4-alkyl, halogen, and benzyl; R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each of these groups optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated 5-
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: February 18, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Enzo Cereda, Luciano Maiocchi, Alessandro Brambilla, Ettore Giraldo, Eugenia Monferini, Giovanni Battista Schiavi
  • Patent number: 6521621
    Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R2 is Ar2, Ar2C1-6alkyl, Het1 or Het1C1-6alkyl; R3 is hydrogen or C1-6alkyl; L is hydrogen; Ar3; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar1, Ar2 and Ar3 are each phenyl or substituted phenyl; Het1 and Het2 are each monocyclic or a bicyclic heterocycles; as substanc
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: February 18, 2003
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
  • Patent number: 6518273
    Abstract: The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: February 11, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Kevin Tyler Chapman, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Steven Michael Hutchins, Duncan Edward Shaw, Christopher Alan Willoughby
  • Patent number: 6514975
    Abstract: This invention relates to tetrazoles and their pharmaceutically acceptable salts which are selective agonists for the delta opioid receptor, particularly useful in the treatment of inflammatory diseases such as arthritis, psoriasis, asthma, inflammatory bowel disease, disorders or respiratory function, gastrointestinal disorders such as functional bowel disease and functional GI disorders, of formula (I) wherein R1 is H, C2-C6 alkanoyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (C3-C7 cycloalkyl)-(C1-C4 alkyl), (C1-C4 alkoxy)-(C1-C4 alkyl), carboxy-(C1-C4 alkyl), aryl-(C1-C4 alkyl) or heteroaryl-(C1-C4 alkyl); R2 and R3 are each independently H or C1-C4 alkyl; R4 is selected from (i) H, (ii) a group of the formula R6—(CH2)m—Z—(CH2)n—, where m is 0, 1, 2 or 3, n is 1, 2 or 3, Z is a direct link or O, and R6 is —CO2H or —CO2(C1-C4 alkyl), and (iii) a group of formula (a) where R7 is H or C1-C4 alkyl; and R5 is hydroxy, C1-C4 alkoxy or &mda
    Type: Grant
    Filed: August 11, 1999
    Date of Patent: February 4, 2003
    Assignee: Pfizer Inc
    Inventor: Graham N. Maw
  • Patent number: 6514969
    Abstract: Compounds of general formula (I) wherein: A is —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—, —CH2—CO—, —CH2—CH2—CO—, or —CH═CH—CO—; Het is piperidinyl, piperazinyl, or dihydrobenzimidazolonyl; R1 is hydrogen or halogen; R2 is hydrogen, C1-C4-alkyl, CF3, or a phenyl group optionally substituted by halogen, C1-C4-alkyl, or C1-C4-alkyloxy; and R3 is hydrogen, C1-C4-alkyl, HO—C1-C4-alkyl, or C2-C4-alkenyl; or a group selected from phenyl, benzyl, and phenylethyl, each optionally substituted by halogen, CF3, C1-C4-alkyl, or C1-C4-alkyloxy; or a heterocycle selected from among morpholine, piperidine, piperazine, and dihydrobenzimidazolone, the heterocycle either linked directly or via a C1-C4-alkylene bridge, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of
    Type: Grant
    Filed: July 24, 2001
    Date of Patent: February 4, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Hans Briem, Klaus Mendla, Helmut Michael Romig, Katja Fechteler, Klaus Fuchs
  • Patent number: 6509340
    Abstract: Amide and urea derivatives of the formula I R1—(CH2)n—(Y)q—(Z)r—CO—NH—R2  (I) in which R1, n, Y, q, Z, r and R2 have the meanings indicated in Claim 1, are potent 5-HT1B/1D antagonists and exhibit 5-HT reuptake-inhibiting actions and are suitable for the treatment and prophylaxis of anxiety states, depressions, schizophrenia, compulsive ideas, tardive dyskinesias, learning disorders, age-dependent memory disorders, for positively affecting obsessive-compulsive behaviour (OCD), and also for the treatment and for the control of the sequelae of cerebral infarcts such as stroke and cerebral ischaemias.
    Type: Grant
    Filed: October 3, 2001
    Date of Patent: January 21, 2003
    Assignee: Merck Patentgesellschaft
    Inventors: Christoph Van Amsterdam, Hartmut Greiner, Henning Boettcher, Gerd Bartoszyk, Juergen Harting, Lisa Matzen, Wilfried Rautenberg
  • Publication number: 20030008878
    Abstract: The present invention relates to the use of compounds of formula (I) 1
    Type: Application
    Filed: June 5, 2001
    Publication date: January 9, 2003
    Inventors: Marlon D. Cowart, Pramila A. Bhatia, Jerome F. Daanen, Andrew O. Stewart, Meena V. Patel, Teodozyj Kolasa, Jorge D. Brioni