Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/231)
  • Muscarinic receptor agonists
    Patent number: 6911477
    Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.
    Type: Grant
    Filed: February 28, 2003
    Date of Patent: June 28, 2005
    Assignee: Pfizer Inc.
    Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane R. Liston
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6906066
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 19, 2003
    Date of Patent: June 14, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker, Paul S. Watson, Jeffrey G. Varnes, Wenqing Yao
  • Propenecarboxylic acid amidoxime derivatives, a process for the preparation thereof, and pharmaceutical compositions containing the same
    Patent number: 6887872
    Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
    Type: Grant
    Filed: March 13, 2001
    Date of Patent: May 3, 2005
    Assignee: N-Gene Research Laboratiories Inc.
    Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040259914
    Abstract: The present application describes modulators of chemokine receptor activity of formula (I): 1
    Type: Application
    Filed: June 10, 2004
    Publication date: December 23, 2004
    Inventors: Soo S. Ko, George V. Delucca
  • VLA-4 inhibitor compounds
    Publication number: 20040229858
    Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed.
    Type: Application
    Filed: February 26, 2004
    Publication date: November 18, 2004
    Applicants: Daiichi Pharmaceutical Co., LTD., Pharmacopeia Drug Discovery, Inc.
    Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Shin Iimura, Yoshiyuki Yoneda
  • Heterocyclic ureas, their preparation and their use as vanilloid receptor antagonists
    Publication number: 20040171639
    Abstract: The invention relates to compounds of formula (I) having Vanilloid Receptor (VR1) antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.
    Type: Application
    Filed: March 31, 2004
    Publication date: September 2, 2004
    Inventors: Harshad Kantilal Rami, Mervyn Thompson, Paul Adrian Wyman
  • Diphenylurea compounds
    Patent number: 6784183
    Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: August 31, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
  • Pharmaceutically active compounds and methods of use
    Patent number: 6756389
    Abstract: The present invention relates to certain imine-substituted heterocyclic compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: June 29, 2004
    Assignee: Cambridge Neuroscience, Inc.
    Inventors: Graham J. Durant, Michael Maillard, Jun Qing Guo
  • MCH antagonists for the treatment of obesity
    Publication number: 20040122017
    Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Application
    Filed: December 3, 2002
    Publication date: June 24, 2004
    Applicant: Schering Corporation
    Inventors: John W. Clader, Anandan Palani, Ruo Xu, Mark D. McBriar, Jing Su, Haiqun Tang
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040058960
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: June 19, 2003
    Publication date: March 25, 2004
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker
  • Urea derivative and adhesive-molecule inhibitor containing the same as active ingredient
    Publication number: 20040039040
    Abstract: Disclosed are novel urea derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases.
    Type: Application
    Filed: March 14, 2003
    Publication date: February 26, 2004
    Inventors: Toshiya Takahashi, Takeshi Ishigaki, Miyuki Funahashi, Koji Taniguchi, Masayuki Kaneko, Mie Kainoh, Hiroyuki Meguro
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040034063
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: February 6, 2003
    Publication date: February 19, 2004
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040006107
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: October 24, 2002
    Publication date: January 8, 2004
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker, Ui Tae Kim
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20040002515
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: October 24, 2002
    Publication date: January 1, 2004
    Inventors: Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker
  • Amidine derivatives, their preparation and application as medicines and pharmaceutical compositions containing same
    Patent number: 6653312
    Abstract: Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: November 25, 2003
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
  • N-(4-carbamimidoyl-phenyl)-glycine derivatives
    Patent number: 6642386
    Abstract: The invention is concerned with water soluble N-(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I) wherein R1 to R4 and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: November 4, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Katrin Groebke Zbinden, Ulrike Obst
  • Piperidine amides as modulators of chemokine receptor activity
    Patent number: 6638950
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 20, 2001
    Date of Patent: October 28, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
  • Monoacyl-substituted guanidines, a process for their preparation, their use as a medicament or diagnostic aid, and pharmaceutical compositions containing them
    Patent number: 6632840
    Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) is
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: October 14, 2003
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
  • omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
    Publication number: 20030181442
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: November 27, 2001
    Publication date: September 25, 2003
    Applicant: BAYER CORPORATION
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
  • N-(4-CARBAMIMIDOYL-PHENYL)-GLYCINE DERIVATIVES
    Publication number: 20030166683
    Abstract: The invention is concerned with water soluble N—(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I) 1
    Type: Application
    Filed: January 24, 2003
    Publication date: September 4, 2003
    Inventors: Leo Alig, Katrin Groebke Zbinden, Ulrike Obst
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6605623
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: August 12, 2003
    Assignee: Bristol-Myers Squibb Pharma Co.
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • 2-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
    Publication number: 20030144273
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: June 26, 2002
    Publication date: July 31, 2003
    Inventors: Paul S. Watson, Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20030114489
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: June 26, 2002
    Publication date: June 19, 2003
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, Dean A. Wacker
  • VLA-4 inhibitor compounds
    Publication number: 20030078249
    Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed.
    Type: Application
    Filed: December 28, 2001
    Publication date: April 24, 2003
    Applicant: Daiichi Pharmaceutical Co., LTD.
    Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Shin Iimura, Yoshiyuki Yoneda
  • PHARMACEUTICALLY ACTIVE COMPOUNDS AND METHODS OF USE
    Publication number: 20030069274
    Abstract: The present invention relates to certain imine-substituted heterocyclic compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
    Type: Application
    Filed: August 9, 1996
    Publication date: April 10, 2003
    Inventors: GRAHAM J. DURANT, MICHAEL MAILLARD, JUN QING GUO
  • N-substituted-N?-substituted urea derivatives and the use thereof as TNF-&agr; production inhibitory agents
    Patent number: 6534499
    Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.
    Type: Grant
    Filed: October 4, 2001
    Date of Patent: March 18, 2003
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
  • Compounds and compositions as protease inhibitors
    Patent number: 6525036
    Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.
    Type: Grant
    Filed: January 5, 2001
    Date of Patent: February 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6525069
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: February 25, 2003
    Assignee: Bristol-Myers Squibb Pharma Co.
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
  • N-ureidoheterocycloalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20030032654
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: June 29, 2001
    Publication date: February 13, 2003
    Inventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Publication number: 20030013741
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: October 23, 2001
    Publication date: January 16, 2003
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, Daniel S. Gardner
  • Unsaturated hydroximic acid derivatives as per abstract inhibitors
    Patent number: 6500823
    Abstract: The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical compositions. The novel compounds possess valuable pharmaceutical effects, so they can be used in the treatment of states connected with energy deficiency of the cell caused by PARP inhibition, in diabetes complications, in oxygen deficient status of the heart and brain, in neurodegenerative diseases, in the treatment of autoimmune and/or viral diseases. In formula (I).
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: December 31, 2002
    Assignee: N-Gene Research Laboratories, Inc.
    Inventors: Péter Literáti Nagy, Kálmán Takács, Balázs Sümegi
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6486180
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: November 26, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • Substituted urea neuropeptide Y Y5 receptor antagonists
    Publication number: 20020165223
    Abstract: Compounds represented by structural formula I 1
    Type: Application
    Filed: September 12, 2001
    Publication date: November 7, 2002
    Inventors: William J. Greenlee, Ying Huang, Joseph M. Kelly, Stuart W. McCombie, Andrew W. Stamford, Yusheng Wu
  • 3-substituted piperidines comprising urea functionality, and methods of use thereof
    Patent number: 6476050
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: November 5, 2002
    Assignee: Sepracor, Inc.
    Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
  • Cyclic amine modulators of chemokine receptor activity
    Patent number: 6476054
    Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, m and n 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-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: November 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates, Dooseop Kim, Shankaran Kothandaraman, Liping Wang
  • Piperidine amides as modulators of chemo kine receptor activity
    Publication number: 20020156102
    Abstract: The present application describes modulators of CCR3 of formula (I): 1
    Type: Application
    Filed: June 20, 2001
    Publication date: October 24, 2002
    Inventors: John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
  • Novel guanidinobenzamides
    Publication number: 20020137939
    Abstract: Compounds of formula IA and IB are new 1
    Type: Application
    Filed: August 31, 2001
    Publication date: September 26, 2002
    Inventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, Zhi-Jie Ni, David Duhl, Effie Tozzo, Kirk Johnson, David C. Myles
  • Adhesion receptor antagonists
    Patent number: 6455529
    Abstract: Compounds of the formula I in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treatment of thromboses, osteoporoses, oncoses, stroke, myocardial infarct, ischemias, inflammations, arteriosclerosis and osteolytic disorders.
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: September 24, 2002
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Joachim Gante, Hörst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
  • Compounds and methods for treatment of asthma, allergy and inflammatory disorders
    Patent number: 6451801
    Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl peperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferable asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: September 17, 2002
    Assignee: UCB, S.A.
    Inventors: Ralph Scannell, Pierre Chatelain, Anna Toy-Palmer, Edmond Differding, James Ellis, Marie-Agnes Lassoie, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, Timothy Lewis
  • N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
    Patent number: 6444686
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: September 3, 2002
    Assignee: Brsitol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, III, Dean A. Wacker
  • Diacyl-substituted guanidines, a process for their preparation, their use as medicine or diagnostic aid, and medicine containing them
    Patent number: 6436999
    Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.
    Type: Grant
    Filed: April 18, 1997
    Date of Patent: August 20, 2002
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
  • Amidino compounds useful as nitric oxide synthase inhibitors
    Publication number: 20020111493
    Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
    Type: Application
    Filed: March 23, 2001
    Publication date: August 15, 2002
    Inventors: Ronald Keith Webber, Alok K. Awasthi, Arija A. Bergmanis, Richard C. Durley, Kam F. Fok, Scott S. Ganser, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Brian S. Hickory, Pamela T. Manning, Michael Mao, Alan E. Moormann, Barnett S. Pitzele, Michelle A. Promo, Richard R. Schartman, Jeffrey A. Scholten, Jeffrey S. Snyder, Mihaly V. Toth, Mahima Trivedi, Sofya Tsymbalov, Foe Siong Tjoeng
  • Novel muscarinic receptor agonists
    Publication number: 20020103194
    Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism
    Type: Application
    Filed: February 15, 2000
    Publication date: August 1, 2002
    Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane Liston
  • Azo amino acids derivatives
    Publication number: 20020103190
    Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
    Type: Application
    Filed: January 3, 2002
    Publication date: August 1, 2002
    Inventors: David Lauffer, Michael Mullican
  • Pyridazin-3-one derivatives, their use, and intermediates for their production
    Patent number: 6348628
    Abstract: Novel hydrazones of formula [2] having the following structural formula are provided, which are useful intermediates to form active ingredients of herbicides, wherein R3 is hydrogen, alkyl, haloalkyl, or alkoxy alkyl; and Q is [Q-1], [Q-2], [Q-3], [Q-4] or [Q-5] as defined herein.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: February 19, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tadashi Katayama, Shinichi Kawamura, Yuzuru Sanemitsu, Yoko Mine
  • Piperididinyl and N-amidinopiperidinyl derivatives
    Publication number: 20020016339
    Abstract: This invention is directed to a compound of fornula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amnount of thrombin.
    Type: Application
    Filed: August 6, 2001
    Publication date: February 7, 2002
    Inventors: Scott I. Klein, Kevin R. Guertin
  • 3-substituted piperidines comprising urea functionality, and methods of use thereof
    Publication number: 20010056090
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.
    Type: Application
    Filed: February 23, 2001
    Publication date: December 27, 2001
    Inventors: Brian M. Aquila, Gregory D. Cuny, James R. Hauske, Liming Shao, Xinhe Wu
  • Cyclic amine derivatives- CCR-3 receptor antagonists
    Patent number: 6323223
    Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: November 27, 2001
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
  • Amino acid derivatives and their use as thrombin inhibitors
    Patent number: 6255301
    Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: July 3, 2001
    Assignee: AstraZeneca AB
    Inventors: David Gustafsson, Jan-Erik Nyström
  • Substituted phenylamidines
    Patent number: 6242466
    Abstract: Phenylamidines of the formula (I) wherein: R6 is a C5-12-alkyloxycarbonyl group, and R7 is a hydrogen atom, or a C1-8-alkyl, C4-7-cycloalkyl, phenyl-C1-4-alkyl, or R8—CO—OCHR9— group, wherein R8 is a C1-4-alkyl, C1-4-alkoxy, C3-7-cycloalkyl, or C4-7-cycloalkoxy group, and R9 is a hydrogen atom or a C1-4-alkyl group, or a tautomer or pharmaceutically acceptable salt thereof. These compounds inhibit cell aggregation and are useful for the treatment or prevention of thrombosis, inflammation, bone degradation, tumors and tumor metastasis.
    Type: Grant
    Filed: July 14, 1999
    Date of Patent: June 5, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Brian Guth, Hans-Dieter Schubert