Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/371.4)
  • Publication number: 20030134848
    Abstract: There is provided heterocyclic compounds of the following formula (I): 1
    Type: Application
    Filed: November 21, 2001
    Publication date: July 17, 2003
    Inventors: Masahiro Imoto, Tatsuya Iwanami, Minako Akabane, Yoshihiro Tani
  • Patent number: 6586433
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: July 1, 2003
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6531478
    Abstract: Amino pyrazole derivatives of the formula: which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active ingredient are described. The amino pyrazole derivatives are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.
    Type: Grant
    Filed: February 22, 2001
    Date of Patent: March 11, 2003
    Inventors: Cheryl P. Kordik, Scott L. Dax, Chi Luo, Allen B. Reitz, James J. McNally, Timothy W. Lovenberg
  • Publication number: 20020156114
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I): 1
    Type: Application
    Filed: January 11, 2002
    Publication date: October 24, 2002
    Inventors: David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brain Sjogren, Francisco Xavier Talamas
  • Patent number: 6458823
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: October 1, 2002
    Assignee: Wyeth
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen
  • Patent number: 6444612
    Abstract: A method of controlling a plant disease caused by a fungus comprising applying a 5-amino-pyrazole of the formula wherein, R1, R2, R3, R4, R5 and Y are as defined in the specification.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: September 3, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Markus Heil, Thomas Bretschneider, Hans-Christian Militzer, Astrid Mauler-Machnik, Klaus Stenzel
  • Publication number: 20020095050
    Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.
    Type: Application
    Filed: June 12, 2001
    Publication date: July 18, 2002
    Inventor: Andrea Vaupel
  • Patent number: 6407238
    Abstract: Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: June 18, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: James A. Baron, Vittorio Farina, Nizar Haddad
  • Publication number: 20020058810
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Application
    Filed: November 29, 2001
    Publication date: May 16, 2002
    Applicant: Pharmacia Corporation
    Inventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffery S. Carter, Bryan H. Norman, Balekudru Devadas
  • Patent number: 6387900
    Abstract: 3-ureido-pyrazole derivatives represented by formula (I): where R, R1 and R2 are as described herein, or pharmnaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
    Type: Grant
    Filed: August 12, 1999
    Date of Patent: May 14, 2002
    Assignees: Pharmacia & Upjohn S.p.A., Pharmacia & Upjohn Co.
    Inventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce
  • Patent number: 6372774
    Abstract: N-Phenylpyrazole derivatives of the formula: wherein R1 represents optionally halogenated alkyl; R2 represents halogen, cyano, nitro, cycloalkyl, alkenyl, thiocyanato, optionally alkyl substituted sulphamoyl, optionally alkyl substituted carbamoyl, alkoxycarbonyl, alkanoyl or optionally halogenated alkyl; and R3 represents a hydrogen atom or a group N″R′″ or a variety of other groupings. These compounds possess arthropodicidal, plant nematocidal, anthelmintic and anti-protozoal properties; their preparation, compositions containing them and their use are described.
    Type: Grant
    Filed: July 16, 1999
    Date of Patent: April 16, 2002
    Assignee: Rhone-Poulenc Agriculture Ltd.
    Inventors: Leslie Roy Hatton, Ian George Buntain, David William Hawkins, Edgar William Parnell, Christopher John Pearson, David Alan Roberts
  • Patent number: 6319941
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: November 20, 2001
    Assignee: American Home Products Corporation
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen
  • Patent number: 6207829
    Abstract: A process is provided for the preparation of a compound of formulae (IA) (sidenafil) and (IB) comprising reacting a compound of formula (IIA) and (IIB) respectively in the presence of —OR, wherein R in the case of formation of compound (IA) is CH2CH3 and R in the case of formation of compound (IB) is CH2CH2CH3, where X is a leaving group:
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: March 27, 2001
    Assignee: Pfizer Inc.
    Inventors: Peter James Dunn, Philip Charles Levett
  • Patent number: 6172222
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 7, 1999
    Date of Patent: January 9, 2001
    Assignee: American Home Products Corporation
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen