Halogen Bonded Directly To The Hetero Ring Patents (Class 540/511)
  • Patent number: 6307045
    Abstract: The present invention provides a process for producing halogenated benzene compounds. In the process, an organometallic compound represented by the general formula [I]: wherein M represents an R13Sn group, an R13Si group, an R13Ge group, an (R2CO2)Hg group, a ClHg group or an (R3O)2B group wherein each R1 independently represents a C1-C8 alkyl group, R2 represents a C1-C3 alkyl group or a C1-C3 haloalkyl group, R3 represents a hydrogen atom or a C1-C3 alkyl group, n represents an integer of from 0 to 4, m represents an integer of from 0 to 1, each A independently represents a fluorine atom, a nitro group, a cyano group, a C1-C8 alkyl group, a C1-C8 alkoxy group or a C2-C8 acyloxy group, and Q represents an organic residue, is reacted in a solvent with a halide ion represented by the general formula X−, under light irradiation conditions in the presence of a semiconductor catalyst with a photocatalytic activity.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: October 23, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Komori, Kazuhiko Nishioka
  • Patent number: 6232308
    Abstract: The present invention relates to benzazepine derivatives and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
    Type: Grant
    Filed: February 2, 2000
    Date of Patent: May 15, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Ben C. Askew
  • Patent number: 6100254
    Abstract: Disclosed herein are small molecule, non-peptidyl inhibitors of protein tyrosine kinases, and methods for their use. The instant inhibitors are based on a 1,4-benzodiazepin-2-one nucleus. Methods are provided for inhibition of specific protein tyrosine kinases, for example pp60.sup.c-src. Methods are further provided for the use of these inhibitors in situations where the inhibition of a protein tyrosine kinase is indicated, for example, in the treatment of certain diseases in mammals, including humans.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: August 8, 2000
    Assignees: Board of Regents, The University of Texas System, The Regents of the University of California
    Inventors: Raymond J. A. Budde, Jonathan A. Ellman, Victor A. Levin, Gary E. Gallick, Robert A. Newman
  • Patent number: 6015791
    Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors, including inhibitors for human neutrophil elastase. Compounds of the invention are useful in treating conditions such as adult respiratory distress syndrome, septic shock, and multiple organ failure.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: January 18, 2000
    Assignee: Cortech Inc.
    Inventors: Albert Gyorkos, Lyle W. Spruce
  • Patent number: 5580979
    Abstract: The present invention makes available novel compounds represented by the general formula ##STR1## wherein Y represents a phosphate analog. Which compounds are useful for inhibiting an interaction between a protein containing an SH2 domain and a phophotyrosine-containing polypeptide.
    Type: Grant
    Filed: March 15, 1994
    Date of Patent: December 3, 1996
    Assignee: Trustees of Tufts University
    Inventor: William W. Bachovchin
  • Patent number: 5312625
    Abstract: A therapeutically effective antipsychotic preparation comprising a fused cyclic compound for the treatment of diseases involving the serotonergic pathway having the formula (I) or salts thereof: ##STR1## wherein both of A and B are carbonyl groups, or one represents a methylene group and the other a carbonyl group, Z represents a sulfur atom, or a nitrogen atom which may be substituted, or a methylene group, R represents an aromatic or heterocylcic group, which may be substituted, X represents a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.5 lower alkyl group, a C.sub.1 -C.sub.5 lower alkoxy group, a C.sub.7 -C.sub.9 arylalkoxy group, a C.sub.1 -C.sub.5 lower acyloxy group, a C.sub.7 -C.sub.10 arylcarbonyloxy group, a hydroxy group, a nitro group or an ester group, and n is an integer of 2 to 10.
    Type: Grant
    Filed: May 11, 1993
    Date of Patent: May 17, 1994
    Assignee: Suntory Limited
    Inventors: Toshio Tatsuoka, Kayoko Nomura
  • Patent number: 4775671
    Abstract: There is presented compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. signifies one of the groups ##STR2## and the dotted line signifies the double bond present in cases (1), (2) and (4) and wherein R.sup.1 signifies a 5- or 6-membered aromatic heterocyclic group or the group --C(R.sup.6).dbd.NOR.sup.7 (B), R.sup.2 signifies hydrogen and R.sup.3 signifies hydrogen or lower alkyl or R.sup.2 and R.sup.3 together signify dimethylene, trimethylene or propenylene, R.sup.4 and R.sup.5 each signify hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl, R.sup.6 signifies hydrogen or lower alkyl and R.sup.7 signifies lower alkyl, the compound of formula I having the (S) or (R,S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.
    Type: Grant
    Filed: November 18, 1987
    Date of Patent: October 4, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Hunkeler, Emilio Kyburz