The Additional Hetero Ring Is Five-membered Patents (Class 546/283.4)
  • Patent number: 6350766
    Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel such as encephalopathies caused by the ischemia in the acute phase after the onset of cerebral infarction, cerebral hemorrhage or the like, Alzheimer's disease, etc.
    Type: Grant
    Filed: October 25, 1999
    Date of Patent: February 26, 2002
    Assignee: Ajinomoto Co., Inc.
    Inventors: Hisayuki Uneyama, Seiji Niwa, Tomoyuki Onishi
  • Publication number: 20020022729
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: July 30, 2001
    Publication date: February 21, 2002
    Inventors: Akiyoshi Kawai, Makoto Kawai
  • Patent number: 6262083
    Abstract: The present invention relates to novel genipin derivatives which have an excellent liver protection activity with little cytotoxicity, and these compounds are so stable in vivo that they do not induce any side effects.
    Type: Grant
    Filed: May 5, 2000
    Date of Patent: July 17, 2001
    Assignee: Choongwae Pharma Corporation
    Inventors: Sung-Hwan Moon, Hea-Jin Choi, Su-Jin Lee, Jea-Uk Chung, Jong-Ryul Ha, Kyoung-June Lee, Se-Woong Oh, Kwang-Won Jeong
  • Patent number: 6262082
    Abstract: Compounds of the formula wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; A is heteroaryl.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: July 17, 2001
    Inventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
  • Patent number: 6262088
    Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.
    Type: Grant
    Filed: November 19, 1998
    Date of Patent: July 17, 2001
    Assignee: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Patent number: 6258822
    Abstract: Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
    Type: Grant
    Filed: August 6, 1998
    Date of Patent: July 10, 2001
    Assignee: Abbott Laboratories
    Inventors: Andrew G. Geyer, William J. McClellan, Todd W. Rockway, Kent D. Stewart, Moshe Weitzberg, Michael D. Wendt
  • Patent number: 6255340
    Abstract: A pesticidal composition comprising prallethrin and a neonicotinoid compound given in the following formula (1), (2) or (3), as an active ingredient wherein, A represents a 6-chloro-3-pyridyl, 2-chloro-5-thiazolyl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 5-methyltetrahydrofuran-3-yl, 3-pyridyl, 6-bromo-3-pyridyl, 3-cyanophenyl, 2-methyl-5-thiazolyl, 2-phenyl-5-thiazolyl or 2-bromo-5-thiazolyl group; R1 represents a hydrogen atom, methyl, ethyl, formyl or acetyl group; R2 represents a methyl, amino, methylamino, N,N-dimethylamino, ethylamino, N,N-diethylamino, N-methyl-N-ethylamino, 1-pyrrolidinyl, (6-chloro-3-pyridyl) methylamino or N-methyl-N-(6-chloro-3-pyridyl)methylamino group; R3 represents a methyl, ethyl, propyl, propenyl or propynyl group; X represents a nitrogen atom or CH group; Y represents a cyano, nitro or trifluoroacetyl group; Z represents a NH group or sulfur atom; D represents an oxygen atom or —N(CH3)— group; m represents 0 or 1; and n represents 2 or 3, has
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: July 3, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Izumi Fujimoto
  • Patent number: 6245774
    Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D):  wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12
    Type: Grant
    Filed: June 20, 1995
    Date of Patent: June 12, 2001
    Assignee: Celltech Therapeutics Limited
    Inventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
  • Patent number: 6235758
    Abstract: A compound of formula (I) or a salt thereof: wherein: P1 is pyridiyl; P2 is phenyl; A is a bond or a chain of 1 to 5 atoms optionally substituted by C1-6 alkyl; R1 and R2 groups are each independently hydrogen, C1-6alkyl optionally substituted by NR12R13, C2-6alkenyl, C2-6alkynyl, cyano, halogen, CF3, NR12R13, CHO, OCF3, COR14, CH2OR14 or OR14 where R12, R13 and R14 are independently hydrogen or C1-6alkyl; n and m are independently 0, 1 or 2; R3 is hydrogen or C1-6 alkyl; R4 is a group of formula (i): in which: R6 and R7 are independently hydrogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C1-6alkylthio, C1-6alkoxy or halogen.
    Type: Grant
    Filed: July 23, 1999
    Date of Patent: May 22, 2001
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies, David Malcolm Duckworth, Ian Thomson Forbes, Graham Elgin Jones
  • Patent number: 6211203
    Abstract: Compounds of formula I wherein R1 is 1-2C-alkoxy optionally substituted by flourine, R2 is methyl, 1-methylethyl, 3-7C-cycloalkyl or 3-7Ccycloalkylmethyl and Ar is a pyridyl which is optionally di-halo substituted.
    Type: Grant
    Filed: February 5, 1999
    Date of Patent: April 3, 2001
    Assignee: Byk Gulden Lomberg Chemische Fabrik GmbH
    Inventor: Hermann Amschler
  • Patent number: 6197750
    Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: March 6, 2001
    Assignee: Idun Pharmaceuticals, Inc.
    Inventors: Donald S. Karanewsky, Robert J. Ternansky
  • Patent number: 6194581
    Abstract: In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: February 27, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Nicholas D. Cosford, Jean-Michel Vernier