Five-membered Hetero Ring Consisting Of One Nitrogen And Four Carbons Patents (Class 544/372)
The five-membered hetero ring is one of the cyclos in a bicyclo ring system (Class 544/373)
  • Phosphodiesterase 4 inhibitors
    Publication number: 20030139406
    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.
    Type: Application
    Filed: October 16, 2002
    Publication date: July 24, 2003
    Applicant: MEMORY PHARMACEUTICALS CORP.
    Inventors: Ruiping Liu, Mike De Vivo, Hans-Jurgen Ernst Hess, Allen Hopper, Erik Kreuster, Ashok Tehim
  • Novel compounds
    Publication number: 20030134840
    Abstract: The invention provides compounds of general formula 1
    Type: Application
    Filed: January 9, 2003
    Publication date: July 17, 2003
    Applicant: AstraZeneca AB, a Sweden corporation
    Inventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas Mclnally, Bryan Roberts, Stephen Thom
  • &bgr;2-adrenergic receptor agonists
    Patent number: 6593497
    Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: February 14, 2000
    Date of Patent: July 15, 2003
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Edmund J. Moran
  • Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia
    Patent number: 6593474
    Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: July 15, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Linda Mulcahy, Xiaobing Li, Allen Reitz, Cynthia Maryanoff, Frank Villani
  • Compounds and compositions as protease inhibitors
    Patent number: 6593327
    Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: July 15, 2003
    Assignee: Axys Pharmaceuticals, Inc.
    Inventors: Clifford M. Bryant, James T. Palmer, Robert M. Rydzewski, Eduardo L. Setti, Zong-Qiang Tian, Shankar Venkatraman, Dan-Xiong Wang
  • Amino lactam sulfonamides as inhibitors of A-beta protein production
    Publication number: 20030130251
    Abstract: This invention relates to novel lactams having the Formula (I): 1
    Type: Application
    Filed: November 4, 2002
    Publication date: July 10, 2003
    Inventors: Lorin A. Thompson, Amy Qi Han
  • Sulfonamide compounds with pharmaceutical activity
    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
  • Serotonin 5-HT1A and dopamin D2 receptor ligands
    Publication number: 20030120070
    Abstract: The present invention relates to a series of 4-phenylpiperazines of formula (I) 1
    Type: Application
    Filed: December 30, 2002
    Publication date: June 26, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Jens Kristian Perregaard, Ejner Kund Moltzen
  • Useful aroyl aminoacyl pyrrole compounds
    Patent number: 6573267
    Abstract: This invention is directed to aroyl aminoacyl pyrroles pharmaceutically useful as agents and modulators for the treatment of central nervous system disorders and a method for the treatment of central nervous system disorders including, but not limited to, use of the compounds of the present invention as anticonvulsant agents and modulators, antiepileptic agents and modulators, neuroprotective agents and modulators, muscle relaxant agents and modulators and as agents and modulators for the treatment of neuropathic pain.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: June 3, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: John R. Carson, Philip M. Pitis
  • Substituted phenylamidines medicaments containing said compounds and method for production thereof
    Publication number: 20030096824
    Abstract: The present invention relates to phenylamidines of general formula 1
    Type: Application
    Filed: October 21, 2002
    Publication date: May 22, 2003
    Inventors: Frank Himmelsbach, Brian Guth
  • Cyclic and bicyclic diamino histamine-3 receptor antagonists
    Patent number: 6559140
    Abstract: Compounds of formula (I) compounds of formula (II) compounds of formula (III) and compounds of formula (IV) or pharmaceutically acceptable salts thereof are useful as H3 receptor antagonists. Processes to make the compounds and methods of treatment using the compounds are also disclosed.
    Type: Grant
    Filed: March 5, 2001
    Date of Patent: May 6, 2003
    Assignee: Abbott Laboratories
    Inventors: Youssef L. Bennani, Lawrence A. Black, Wesley J. Dwight, Ramin Faghih, Robert G. Gentles, Huaqing Liu, Kathleen M. Phelan, Anil Vasudevan, Henry Q. Zhang
  • Optically active 3-[(2-piperazinylphenyl)methyl]-1-[4-(trifluoromethyl)phenyl]-2-pyrrolidinone compounds as 5-HT1D receptor selective antagonists
    Publication number: 20030083337
    Abstract: The present invention relates to optically active 3-[(2-piperazinylphenyl)methyl]-1-[4(trifluoromethylphenyl]-2-pyrrolidinones and pharmaceutically acceptable salts thereof, to processes for their preparation, to isotopically-labeled analogs thereof, to pharmaceutical compositions comprising them and to their medicinal use as selective antagonists of the 5-HT1D rector. The compounds of the invention are useful in treating depression, obsessive-compulsive disorder (OCD) and diseases, disorders or conditions for which a 5-HT1D receptor selective antagonist is therapeutically indicated.
    Type: Application
    Filed: August 9, 2002
    Publication date: May 1, 2003
    Inventors: Harry R. Howard, Stephane Caron, Mavis D. Adam
  • Piperazine derivatives and their use as anti-inflammatory agents
    Patent number: 6555537
    Abstract: This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: April 29, 2003
    Assignee: Schering Aktiengesellschaft
    Inventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
  • Mediators of hedgehog signaling pathways, compositions and uses related thereto
    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
  • Benzamide derivatives and their use as ApoB-100 secretion inhibitors
    Patent number: 6552022
    Abstract: The invention relates to therapeutic benzamide compounds of formula (I) wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present invention also provides pharmaceutical compositions, processes for the preparation of compounds of formula (I) and their use in the treatment of conditions mediated by ApoB-100 regulation.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: April 22, 2003
    Assignee: SmithKline Beecham Corporation
    Inventor: Alain Claude-Marie Daugan
  • CXCR3 antagonists
    Publication number: 20030069234
    Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
    Type: Application
    Filed: June 6, 2002
    Publication date: April 10, 2003
    Inventors: Julio C. Medina, Michael G. Johnson, An-Rong Li, Jiwen Liu, Alan Xi Huang, Liusheng Zhu, Andrew P. Marcus
  • Urotensin-II receptor antagonists
    Patent number: 6544992
    Abstract: The present invention relates to pyrrolyl and pyridyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of urotensin II.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: April 8, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dashyant Dhanak, Steven David Knight, Jian Jin, Richard McCulloch Keenan
  • Substituted alkyl piperazine derivatives
    Publication number: 20030064994
    Abstract: Novel compounds of the general formula: 1
    Type: Application
    Filed: September 13, 2002
    Publication date: April 3, 2003
    Applicant: CV Therapeutics, Inc.
    Inventors: Vaibhav Varkhedkar, Venkata P. Palle, Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn
  • &bgr;2-adrenergic receptor agonists
    Patent number: 6541669
    Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: April 1, 2003
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, Seok-Ki Choi
  • Heterocyclic carboxamides
    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
  • Piperazine derivatives inhibiting human immunodeficiency virus replication
    Patent number: 6531476
    Abstract: The invention concerns the use of a piperazine derivative of formula (I) wherein: A and B=C═O, C═S or CR7R8 with R7=H, methyl, cyano, cyanomethyl, CO2CH3 or (C═O)CH3 and R8=H or phenyl; R1 to R6=H, OH, or C1-C5 alkoxy; X represents: either C═O, O(C═O), O(C═S), O(SO2), NH(C═O), NH(C═S), NH(SO2), S(C═O) or S(C═S), then Y=NR9R10, CR9R10R11 in which R9, R10 and R11=H, C1-C5 alkyl, C2-C5 alkenyl, or C2-C5 alkynyl or Y=nitrogenous heterocycle comprising 5 to 10 atoms; or X represents O, S, O(C═O)O, NH(C═O)O, or S(C═O)O, then Y=CR9R10R11 with R9, R10, R11 as above; or one of its pharmaceutically acceptable salts for preparing a medicine inhibiting HIV. The invention is useful for treating HIV infection.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: March 11, 2003
    Assignees: Universite Paris 7 - Denis Diderot, Commissariat a l'Energie Atomique
    Inventors: Francoise Heymans, Nathalie Dereuddre-Bosquet, Jean-Jacques Godfroid, Aazdine Lamouri, Pascal Clayette, Marc Martin
  • Naphthostyrils
    Patent number: 6531598
    Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: March 11, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk
  • Arylpiperazines having activity at the serotonin 1A receptor
    Publication number: 20030027831
    Abstract: A series of aryl piperazine compounds of the formula: 1
    Type: Application
    Filed: December 18, 2001
    Publication date: February 6, 2003
    Inventor: Yao-Chang Xu
  • Aminoalkoxy carbazoles for the treatment of cns diseases
    Patent number: 6514968
    Abstract: The present invention provides aminoalkoxy carbazole derivatives, and more specifically, provides compounds of formula (I) wherein R1, R2, R3, R4, R8 and R9 are described herein. These compounds are 5-HT ligands, and are useful for treating diseases wherein modulation of 5-HT activity is desired.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: February 4, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventor: Ruth Elizabeth TenBrink
  • Pyrrole derivatives useful for farnesyl transferase inhibitors and their preparations
    Patent number: 6511978
    Abstract: The present invention relates to a novel pyrrole derivative which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof; to a process for preparation of said compound; and to a pharmaceutical composition such as anti-cancer composition, etc. comprising said compound as an active ingredient together with pharmaceutically acceptable carrier.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: January 28, 2003
    Assignee: LG Life Sciences, Ltd.
    Inventors: Jong-Sung Koh, Hyun-Il Lee, You-Seung Shin, Hak-Joong Kim, Jin-Ho Lee, Jong-Hyun Kim, Hyun-Ho Chung, Shin-Wu Jeong, Tae-Saeng Choi, Jung-Kwon Yoo, Chung-Mi Kim, Kwi-Hwa Kim, Sun-Hwa Lee, Sang-Kyun Lee
  • Piperazine compounds and medicinal use thereof
    Publication number: 20030018034
    Abstract: The present invention relates to a piperazine compound of the formula 1
    Type: Application
    Filed: August 1, 2002
    Publication date: January 23, 2003
    Applicant: Mitsubishi Pharma Corporation
    Inventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Hiroshi Morimoto, Masao Hisadome
  • 4-amino-1-aryl-1,5-dihydropyrrol-2-ones and process for making
    Patent number: 6500821
    Abstract: The invention relates to 1,5-dihydropyrrol-2-ones of Formula 1 which contain an aryl radical in the 1-position and a secondary amine radical in the 4-position, to a process for making and for a process to treat various forms of epilepsies and of states of anxiety and tension.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: December 31, 2002
    Assignee: Arzneimittelwerk Dresden GmbH
    Inventors: Thomas Arnold, Klaus Unverferth, Hans-Joachim Lankau, Angelika Rostock, Christine Tober, Chris Rundfeldt, Reni Bartsch
  • Arylglycinamide derivatives, method of producing said derivatives and pharmaceutical compositions containing these compounds
    Patent number: 6498162
    Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: December 24, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
  • 1-azatricyclic-4-benzylpiperazines
    Publication number: 20020193364
    Abstract: Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
    Type: Application
    Filed: May 7, 2002
    Publication date: December 19, 2002
    Applicant: Neurogen Corporation
    Inventors: Xiaoyan Zhang, Kevin Hodgetts, Stanislaw Rachwal, Daniel Rosewater, Andrew Thurkauf
  • Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
    Patent number: 6492421
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: July 30, 1998
    Date of Patent: December 10, 2002
    Assignees: Athena Neurosciences, Inc., American Home Products Corp.
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Louis John Lombardo, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen, Reinhardt Bernhard Baudy, Susan Ashwell
  • Amidoalkyl-piperidine and amidoalkyl-piperazine derivatives useful for the treatment of nervous system disorders
    Publication number: 20020183316
    Abstract: Novel amidoalkyl-piperidine and amidoalkyl-piperazine derivatives of the general formula 1
    Type: Application
    Filed: October 22, 2001
    Publication date: December 5, 2002
    Inventors: Kevin Pan, Michael H. Parker, Allen B. Reitz, Steven J. Coats, Cheryl P. Kordik, Chi Luo
  • 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
    Patent number: 6489354
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: December 3, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
  • Tricyclic sulfonamides and their derivatives as inhibitors of matrix metalloproteinases
    Publication number: 20020169164
    Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
    Type: Application
    Filed: March 27, 2002
    Publication date: November 14, 2002
    Applicant: Warner-Lambert Company
    Inventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
  • Benzamidine derivatives and their use as anti-coagulants
    Patent number: 6479485
    Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: August 7, 2001
    Date of Patent: November 12, 2002
    Assignee: Berlex Laboratories, Inc.
    Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
  • Novel heterocycles useful in the treatment of benign prostatic hyperplasia
    Publication number: 20020165219
    Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I 1
    Type: Application
    Filed: November 26, 2001
    Publication date: November 7, 2002
    Inventors: Richard H. Hutchings, Haripada Khatuya, Gee-Hong Kuo, Xiaobing Li, William V. Murray, Catherine Prouty, Frank Villani, Nelson C.F. Yim, Cynthia Maryanoff
  • Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
    Publication number: 20020156075
    Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula 1
    Type: Application
    Filed: March 27, 2002
    Publication date: October 24, 2002
    Applicant: Wyeth (formerly American Home Products Corporation)
    Inventors: Wayne E. Childers, Michael G. Kelly, Yvette L. Palmer, Edward J. Podlesny
  • Tyrosine derivatives
    Patent number: 6469047
    Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: October 22, 2002
    Assignee: Genentech, Inc.
    Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
  • Benzyl(idene)-lactam derivatives, their preparation and their use as selective (ant)agonists of 5-HT1A- and/or 5-HT1D receptors
    Patent number: 6462048
    Abstract: The present invention relates to lactam derivatives of the formula wherein R1, R2, R3, A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to processes and intermediates for their preparation, and to their medicinal use as selective agonists and antagonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1D receptors. These compounds are useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: October 8, 2002
    Assignee: Pfizer Inc.
    Inventor: Harry R. Howard
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 6458787
    Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: May 2, 2001
    Date of Patent: October 1, 2002
    Assignee: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlacter
  • 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
    Publication number: 20020137931
    Abstract: Compounds of formula I 1
    Type: Application
    Filed: January 11, 2002
    Publication date: September 26, 2002
    Inventors: Yousseff L. Bennani, Ramin Faghih, Wesley J. Dwight, Anil Vasudevan, Scott E. Conner
  • Benzoylguanidine salt and hydrates thereof
    Publication number: 20020137753
    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: January 25, 2002
    Publication date: September 26, 2002
    Inventors: Christian Eickmeier, Peter Sieger, Werner Rall, Volkmar Koerner, Rolf Herter
  • Alpha-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
    Publication number: 20020128434
    Abstract: Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a &bgr;-dicarbonyl enol ether leaving group.
    Type: Application
    Filed: September 14, 2001
    Publication date: September 12, 2002
    Inventors: Mary P. Zimmerman, Robert E. Smith, Mark Becker
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 6444671
    Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: September 3, 2002
    Assignee: ICOS Corporation
    Inventor: John J. Gaudino
  • Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications
    Publication number: 20020111340
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: November 16, 2001
    Publication date: August 15, 2002
    Inventors: Youssef Bennani, Ramin Faghih
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 6423710
    Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: July 23, 2002
    Assignee: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
  • Pyrrolidine modulators of CCR5 chemokine receptor activity
    Publication number: 20020094989
    Abstract: Pyrrolidine compounds of Formula I: 1
    Type: Application
    Filed: October 10, 2001
    Publication date: July 18, 2002
    Inventors: Jeffrey J. Hale, Christopher L. Lynch, Charles G. Caldwell, Christopher A. Willoughby, Dooseop Kim, Dong-Ming Shen, Sander G. Mills, Kevin T. Chapman, Liya Chen, Amy Gentry, Malcolm MacCoss, Zenon D. Konteatis
  • 1-(4-arylpiperazin-1-yl)-&ohgr;-[N-(&agr;&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers
    Patent number: 6420366
    Abstract: Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.
    Type: Grant
    Filed: May 24, 2000
    Date of Patent: July 16, 2002
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Nitya Anand, Neelima Sinha, Sanjay Jain, Anita Mehta, Jang Bahadur Gupta
  • 1-(4-arylpiperazin-1-yl)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers
    Patent number: 6420559
    Abstract: Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.
    Type: Grant
    Filed: May 24, 2000
    Date of Patent: July 16, 2002
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Nitya Anand, Neelima Sinha, Sanjay Jain, Anita Mehta, Anil Kumar Saxena
  • Hetero-substituted cyclic amine metalloprotease inhibitors
    Patent number: 6417219
    Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: July 9, 2002
    Assignee: The Proctor & Gamble Company
    Inventors: Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
  • 1-(4-arylpiperazin-1-y1)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers
    Patent number: 6410735
    Abstract: Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.
    Type: Grant
    Filed: May 24, 2000
    Date of Patent: June 25, 2002
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Nitya Anand, Neelima Sinha, Sanjay Jain, Anita Mehta, Anil Kumar Saxena