Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Additional Six-membered Nitrogen Hetero Ring Patents (Class 514/253.13)
  • Patent number: 6458793
    Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and more accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).
    Type: Grant
    Filed: January 28, 2000
    Date of Patent: October 1, 2002
    Assignee: Zeneca Limited
    Inventors: Peter Warner, Roger James, Thorsten Nowak
  • Patent number: 6455528
    Abstract: The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: September 24, 2002
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Hiroshi Morimoto, Masao Hisadome
  • Patent number: 6451803
    Abstract: This invention relates to the use of a compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined in the disclosure, for treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: September 17, 2002
    Assignee: Pfizer INC
    Inventor: Harry R. Howard
  • Publication number: 20020123499
    Abstract: One aspect of the present invention relates to piperidine-piperazine compounds. A second aspect of the present invention relates to the use of the piperidine-piperazine compounds as ligands for various mammalian cellular receptors or transporters or both, including dopamine, serotonin or norepinephrine receptors or transporters, any combination of them, or all of them. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.
    Type: Application
    Filed: March 1, 2002
    Publication date: September 5, 2002
    Inventors: Paul E. Persons, Heike Radeke
  • Patent number: 6432960
    Abstract: A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: August 13, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sing-Yuen Sit, Graham S. Poindexter
  • Patent number: 6432956
    Abstract: Certain azapirone compounds and their pharmaceutically acceptable salts are useful in the treatment of sleep apneas.
    Type: Grant
    Filed: May 3, 1991
    Date of Patent: August 13, 2002
    Inventors: William C. Dement, Mark R. Rosekind, Jeffrey L. Schwimmer
  • Publication number: 20020099046
    Abstract: This invention relates to pharmaceutical combinations of atorvastatin or a pharmaceutically acceptable salt thereof and antihypertensive agents, kits containing such combinations and methods of using such combinations to treat subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and to treat subjects presenting with symptoms of cardiac risk, including humans. This invention also relates to additive and synergistic combinations of atorvastatin or a pharmaceutically acceptable salt thereof and antihypertensive agents whereby those synergistic combinations are useful in treating subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and those subjects presenting with symptoms of cardiac risk, including humans.
    Type: Application
    Filed: October 23, 2001
    Publication date: July 25, 2002
    Applicant: Pfizer Inc.
    Inventor: Robert Andrew Donald Scott
  • 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
  • Patent number: 6391881
    Abstract: A series of antagonists of NPY have been synthesized and are comprised of thiourea linked piperazine and piperidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where Z is NR7R8 or and X is CH or N. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: May 21, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventor: Sing-Yuen Sit
  • Publication number: 20020042421
    Abstract: This invention provides a compound of the formula (I): 1
    Type: Application
    Filed: September 27, 2001
    Publication date: April 11, 2002
    Inventors: Yoshiyuki Okumura, Mitsuhiro Kawamura, Makato Kawai, Noriaki Murase, Takafumi Ikeda
  • Publication number: 20020019384
    Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1.
    Type: Application
    Filed: May 10, 2001
    Publication date: February 14, 2002
    Inventors: Graham S. Poindexter, Marc Bruce, Sing-Yuen Sit, Scott W. Martin
  • Publication number: 20020019393
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Application
    Filed: December 21, 2000
    Publication date: February 14, 2002
    Inventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
  • Publication number: 20020013296
    Abstract: Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided.
    Type: Application
    Filed: March 13, 2001
    Publication date: January 31, 2002
    Inventors: Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, Deqi Guo
  • Publication number: 20020002167
    Abstract: A dihydropyridine compound of the formula: 1
    Type: Application
    Filed: April 23, 2001
    Publication date: January 3, 2002
    Applicant: AJINOMOTO CO., INC.
    Inventors: Seiji Niwa, Seiji Ohno, Akira Takahara, Morikazu Kito
  • Publication number: 20010049370
    Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I.
    Type: Application
    Filed: April 24, 2001
    Publication date: December 6, 2001
    Inventor: Sing-Yuen Sit
  • Patent number: 6326371
    Abstract: The present invention relates to a method for treating a patient suffering from a mental disorder, comprising administering to the patient an effective 5-HT1A agonistic and 5-HT2 antagonistic amount of a compound having the formula (I): or a pharmacologically active salt thereof.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: December 4, 2001
    Assignee: Pharmacia Aktiebolag
    Inventors: Lisbeth Abramo, Torbjörn Lundstedt, Curt Nordvi, Knut Gunnar Olsson, Martin Brodszki
  • Publication number: 20010047003
    Abstract: A series of antagonists of NPY have been synthesized and are comprised of thiourea linked piperazine and piperidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1.
    Type: Application
    Filed: April 24, 2001
    Publication date: November 29, 2001
    Inventor: Sing-Yuen Sit
  • Publication number: 20010047002
    Abstract: A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I).
    Type: Application
    Filed: April 24, 2001
    Publication date: November 29, 2001
    Inventors: Sing-Yuen Sit, Graham S. Poindexter
  • Patent number: 6323207
    Abstract: Novel benzoylguanidine derivatives of general formula I useful for the treatment or reduction of tissue damage due to ischaemia.
    Type: Grant
    Filed: September 15, 1999
    Date of Patent: November 27, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Christian Eickmeier, Erich Buerger, Stefan Matthias Blech, Otto Roos
  • Patent number: 6323229
    Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: November 27, 2001
    Assignee: Pfizer INC
    Inventor: Harry R. Howard
  • Patent number: 6316445
    Abstract: The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.
    Type: Grant
    Filed: May 6, 1999
    Date of Patent: November 13, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Timothy P. Burkholder, George D. Maynard, Elizabeth M. Kudlacz
  • Patent number: 6306860
    Abstract: Anti-viral agents of formula (1) have been identified. Their preparation method is described. These 2,5-pyridinedicarboxylic acid derivatives or their pharmaceutically acceptable salts are useful in countering the proliferation of viruses such as hepatitis B virus and human immunodeficiency virus.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: October 23, 2001
    Assignee: Dong Wha Pharm. Inc. Co., Ltd.
    Inventors: Sung Joon Yoon, Sang Wook Lee, Hyeong Su Sim, Yong Kyun Park, Wang Yong Yang, Jong Woo Kim, Jae Jin Han, Je In Yoon, Sang Jin Park, Hee Jeoung Park, Dong Hyuk Sin, Hwan Bong Chang
  • Patent number: 6281214
    Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R1, R2, R3, R4, and R5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: August 28, 2001
    Assignee: Eisai Co., Ltd
    Inventors: Kozo Akasaka, Masahiro Yonaga, Akiharu Kajiwara, Kunizo Higurashi, Kohshi Ueno, Satoshi Nagato, Makoto Komatsu, Noritaka Kitazawa, Masataka Ueno, Yoshiharu Yamanishi, Yoshimasa Machida, Yuki Komatsu, Naoyuki Shimomura, Norio Minami, Toshikazu Shimizu, Atsushi Nagaoka
  • Publication number: 20010014682
    Abstract: This invention relates to a compound of the formula (I): 1
    Type: Application
    Filed: April 23, 2001
    Publication date: August 16, 2001
    Applicant: SmithKline Beecham Corporation
    Inventors: Dirk A. Heerding, James Martin Samanen
  • Patent number: 6211242
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by the general formula (I): wherein R1 is aryl optionally substituted with lower alkyl, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., R4 is aryl, etc., X is CH or N, and Y is CH or N, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: April 3, 2001
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Keiji Hemmi, Hirokazu Tanaka
  • Patent number: 6197772
    Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: March 6, 2001
    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: 6194413
    Abstract: The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: February 27, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Pradip Kumar Bhatnagar, Dirk Andries Heerding