The Additional Hetero Ring Is A Five-membered Nitrogen Hetero Ring Patents (Class 514/252.05)
  • Publication number: 20030114459
    Abstract: The use of compounds that are antagonists of the pain enhancing effects of E-type prostaglandins for the treatment or prevention of neuropathic pain are described. The use of a compound that is an antagonist of the pain enhancing effects of E-type prostaglandins in the production of a medicament for use in the treatment or prevention of neuropathic pain, and a method of treating or preventing neuropathic pain by administration of an effective amount of an antagonist of the pain enhancing effects of E-type prostaglandins to a warm blooded animal such as man are also described.
    Type: Application
    Filed: January 31, 2003
    Publication date: June 19, 2003
    Inventors: John S. Shaw, William Bastain
  • Publication number: 20030114418
    Abstract: A method of treating, preventing, or inhibiting pain, inflammation or inflammation-associated disorder in a subject in need of such treatment or prevention provides for treating the subject with glucosamine and a cyclooxygenase-2 selective inhibitor or prodrug thereof, wherein the amount of glucosamine and the amount of a cyclooxygenase-2 selective inhibitor or prodrug thereof together constitute a pain or inflammation suppressing treatment or prevention effective amount of the composition. Compositions and pharmaceutical compositions that contain glucosamine and a cyclooxygenase-2 selective inhibitor are also disclosed.
    Type: Application
    Filed: August 9, 2002
    Publication date: June 19, 2003
    Applicant: Pharmacia Corporation
    Inventors: Steven P. Pulaski, Susan Kundel
  • Publication number: 20030114452
    Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
    Type: Application
    Filed: May 17, 2002
    Publication date: June 19, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Ralph F. Hall
  • Publication number: 20030114456
    Abstract: Novel heterocyclic compounds of formula I and the salts, solvates and prodrugs thereof, wherein the meanings of the various substituents are as disclosed in the description. Said compounds are useful as anti-inflammatories.
    Type: Application
    Filed: October 25, 2002
    Publication date: June 19, 2003
    Inventors: Carmen Almansa Rosales, Concepcion Gonzalez Gonzalez, MaCarmen Torres Barreda
  • Patent number: 6579879
    Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: June 17, 2003
    Assignee: Pfizer Inc
    Inventor: Banavara L. Mylari
  • Publication number: 20030105105
    Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II: 1
    Type: Application
    Filed: June 26, 2002
    Publication date: June 5, 2003
    Inventor: Donald J.P. Pinto
  • Patent number: 6569860
    Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: May 27, 2003
    Assignee: Roćhe Palo Alto LLC
    Inventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
  • Publication number: 20030092714
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: February 8, 2002
    Publication date: May 15, 2003
    Inventors: Jingrong Cao, Jeremy Green, Michael Hale, Francois Maltais, Judy Straub, Qing Tang, Alex Aronov
  • Publication number: 20030092678
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: May 15, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030083332
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: May 1, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030078236
    Abstract: According to the invention there is provided a compound the formula I; 1
    Type: Application
    Filed: August 29, 2002
    Publication date: April 24, 2003
    Applicant: Allergan, Inc.
    Inventors: Robert M. Burk, Sophie Beauchemin
  • Publication number: 20030078265
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: April 24, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030069243
    Abstract: Novel 1,4,5 substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
    Type: Application
    Filed: July 19, 2002
    Publication date: April 10, 2003
    Applicant: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Ralph F. Hall
  • Publication number: 20030069210
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: April 10, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030069241
    Abstract: This invention relates to 1-diphenylmethyl-pyrazole derivatives of formula (I): 1
    Type: Application
    Filed: July 23, 2002
    Publication date: April 10, 2003
    Inventors: Stanton F. Mchardy, Michael G. Vetelino
  • Publication number: 20030069250
    Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian Factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: April 1, 2002
    Publication date: April 10, 2003
    Inventors: Bing-Yan Zhu, Penglie Zhang, Erick A. Goldman, Zhaozhong Jon Jia, Shawn Bauer, Wenrong Huang, John Woolfrey, Robert M. Scarborough
  • Publication number: 20030060452
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: March 27, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030060471
    Abstract: The invention provides a novel pest control agent having a high systemic activity and a high safety with reduced adverse influences on the environment neighboring the place to which the agent is applied, and a process for producing the same.
    Type: Application
    Filed: December 28, 2001
    Publication date: March 27, 2003
    Applicant: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Shuko Okui, Nobuo Kyomura, Toshiki Fukuchi, Ken Tanaka, Manabu Katsurada, Kazuya Okano, Naoko Sumitani, Akiko Miyauchi, Akiko Yabe
  • Publication number: 20030040516
    Abstract: aP2 inhibiting compounds are provided having the formula 1
    Type: Application
    Filed: July 12, 2002
    Publication date: February 27, 2003
    Inventors: Richard Sulsky, Jeffrey A. Robl
  • Patent number: 6521656
    Abstract: Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A1 antagonist.
    Type: Grant
    Filed: January 4, 2001
    Date of Patent: February 18, 2003
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Satoru Kaneko, Kazuhiko Nomura, Yutaka Kohno, Hiroshi Kodama, Tokuaki Kajiho
  • Publication number: 20030027826
    Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CERP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
    Type: Application
    Filed: December 12, 2001
    Publication date: February 6, 2003
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20030027794
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: February 6, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030027798
    Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.
    Type: Application
    Filed: September 21, 2001
    Publication date: February 6, 2003
    Inventors: Pascal Druzgala, Peter G. Milner, Jurg R. Pfister
  • Patent number: 6506755
    Abstract: 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I in which the symbols R1, R2, A, A1 and A2 have the significance given in the description as medicaments for the treatment of cancer diseases.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: January 14, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter-Gunar Friebe, Hans-Willi Krell, Sabine Woelle, Hans-Peter Wolff
  • Publication number: 20030004137
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: January 2, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030004164
    Abstract: This invention describes novel pyrazole compounds of formula III: 1
    Type: Application
    Filed: December 20, 2001
    Publication date: January 2, 2003
    Inventors: David Bebbington, Jean-Damien Charrier
  • Publication number: 20020193375
    Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, 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 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: Application
    Filed: June 27, 2002
    Publication date: December 19, 2002
    Applicant: ZENECA LIMITED
    Inventors: Peter Warner, Roger James, Thorsten Nowak
  • Publication number: 20020183365
    Abstract: Provided is a method of treating or ameliorating certain fibrotic diseases or other indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I:
    Type: Application
    Filed: December 31, 2001
    Publication date: December 5, 2002
    Inventors: Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
  • Publication number: 20020183323
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: December 5, 2002
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20020183317
    Abstract: Provided is a method of treating or ameliorating a number of indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I or IA, 1
    Type: Application
    Filed: December 31, 2001
    Publication date: December 5, 2002
    Inventors: Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
  • Publication number: 20020177586
    Abstract: Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I: 1
    Type: Application
    Filed: December 31, 2001
    Publication date: November 28, 2002
    Inventors: John J. Egan, Dilip Wagle, Sara Vasan, Martin Gall, Stanley Bell, Edmond J. LaVoie
  • Patent number: 6486156
    Abstract: This invention relates to compounds of formula (1), wherein substituents are defined in the description, that inhibit farnesylation of mutant ras gene products tough inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation of ras.
    Type: Grant
    Filed: September 21, 2001
    Date of Patent: November 26, 2002
    Assignee: Astrazeneca AB
    Inventors: Jean-Claude Arnould, Annie Antoinette Christiane Olivier
  • Publication number: 20020165236
    Abstract: Treatment of Protozoan Infections with new diphenylurea derivatives.
    Type: Application
    Filed: December 12, 2001
    Publication date: November 7, 2002
    Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Stefano Pegoraro, Jurgen Kraus, Rolf Krauss, Hans Leban, Wael Saeb, Kristina Wolf
  • Publication number: 20020165235
    Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: 1
    Type: Application
    Filed: March 1, 2002
    Publication date: November 7, 2002
    Inventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
  • Publication number: 20020165218
    Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.
    Type: Application
    Filed: August 28, 2001
    Publication date: November 7, 2002
    Inventors: James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G Schiro, Hongmei Huang, Michael Evans, Yongxin Han
  • Publication number: 20020160993
    Abstract: Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising administering an intraocular pressure decreasing or accommodation improving amount of a compound of the formula I: 1
    Type: Application
    Filed: December 31, 2001
    Publication date: October 31, 2002
    Inventors: John J. Egan, Dilip Wagle, Sara Vasan, Martin Gall, Stanley Bell, Edmond Joseph LaVoie
  • Publication number: 20020156080
    Abstract: Provided is a method of treating, ameliorating or preventing certain fibrotic diseases or other indications in an animal, including a human, comprising administering an intraocular pressure decreasing or accommodation improving amount of (A) a compound of formula (I):
    Type: Application
    Filed: December 31, 2001
    Publication date: October 24, 2002
    Inventors: Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
  • Publication number: 20020156082
    Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
    Type: Application
    Filed: February 21, 2002
    Publication date: October 24, 2002
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
  • Patent number: 6469003
    Abstract: A pyridazinone derivative represented by formula (I): a pharmaceutically acceptable salt thereof, or a derivative thereof, or a pharmaceutical composition comprising as an active ingredient the derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: October 22, 2002
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Makoto Gotoh, Koji Umimoto, Masanobu Onishi, Akiyuki Satoh, Yoshitami Oshita, Masashi Nagamine
  • Publication number: 20020143017
    Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.
    Type: Application
    Filed: March 21, 2002
    Publication date: October 3, 2002
    Inventor: Banavara L. Mylari
  • Publication number: 20020132812
    Abstract: Compounds of formula (I) which are optionally substituted 2-(&ohgr;,&ohgr;-diarylalkyl)-4,5-dihydro-1H-imidazoles and 2-(&ohgr;,&ohgr;-diarylalkyl)-1,4,5,6-tetrahydropyrimidines and salts thereof with inorganic and organic acids have interesting pharmacological properties. Thus, the compounds are useful in the treatment of type 2 diabetes.
    Type: Application
    Filed: November 9, 2001
    Publication date: September 19, 2002
    Inventors: Henrik Sune Andersen, Palle Jakobsen, Peter Madsen
  • Publication number: 20020123496
    Abstract: This invention relates to pyridazine derivatives represented by the formula (1): 1
    Type: Application
    Filed: November 30, 2001
    Publication date: September 5, 2002
    Applicant: Kowa Co., Ltd.
    Inventors: Masao Ohkuchi, Yoshinori Kyotani, Hiromichi Shigyo, Tomoyuki Koshi, Takahiro Kitamura, Tadaaki Ohgiya, Takayuki Matsuda, Yukiyoshi Yamazaki, Natsuyo Kumai, Kyoko Kotaki, Hideo Yoshizaki, Yuriko Habata
  • Publication number: 20020119970
    Abstract: Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, 1
    Type: Application
    Filed: December 31, 2001
    Publication date: August 29, 2002
    Inventors: Dilip Wagle, Martin Gall, Stanley C. Bell, Edmond J. LaVoie
  • Publication number: 20020115669
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: August 29, 2001
    Publication date: August 22, 2002
    Inventors: Paul E. Wiedeman, Steven W. Djuric, Marina Pilushchev, Richard J. Sciotti, David J. Madar, Hana Kopecka
  • Publication number: 20020107252
    Abstract: The invention relates to heteroaromatic carboxamides of formula (I), 1
    Type: Application
    Filed: February 5, 2002
    Publication date: August 8, 2002
    Inventors: Andrew Baxter, Stephen Brough, Alan Faull, Craig Johnstone, Thomas McInally
  • Patent number: 6423842
    Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: July 23, 2002
    Assignee: UCB, S.A.
    Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
  • 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: 6417189
    Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: July 9, 2002
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
  • Publication number: 20020086862
    Abstract: The invention provides certain 1,2,4-triazole-3-thione compounds, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 10, 2001
    Publication date: July 4, 2002
    Applicant: AstraZeneca AB
    Inventors: Andrew Baxter, Colin Bennion, Peter Cage, Nicholas Kindon, Michael Mortimore, Bryan Roberts
  • Patent number: 6410539
    Abstract: The present invention relates to a compound of Formula (1) wherein Ar1 represent (A) or (B) or (C); R1 is hydrogen, C1-4alkyl or C1-4alkanoyl; R12 and R13 are independently hydrogen or C1-4alkyl; Ar2 is phenyl or heteroaryl; p is 0 or 1; Ar3 is of formula (I) wherein W, X, Y and Z are independently CH or N, provided that at least two of W, X, Y and Z are CH and R2 and —(CH2)nR3 are attached to ring carbon atoms; R2 is a group of Formula (II) or R2 represents a lactone of Formula (III) the group of Formula (II) or (III) having L or D configuration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3 is phenyl or heteroaryl; provided that: when n is 0, Ar3 is substituted by R2 in the 4-position and —(CH2)nR3 in the 3- or 5-position; and when n is 1 or 2, Ar3 is substituted by R2 in the 3- or 5-position and —(CH2)nR3 in the 4-position; and R5-R9, m and n are as defined in the specification; or a pharmaceutically-acceptable salt, prodrug or solvate thereof.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: June 25, 2002
    Assignees: Astrazenca UK Limited, Zeneca Pharma SA
    Inventor: Jean-Claude Arnould