Patents Examined by M. S. H. Gabilan
  • Patent number: 5147885
    Abstract: N-amino hexahydrocyclopenta imidazole-2(1H)-one derivatives useful for treating or preventing thrombo-embolic disorders and ocular diseases characterized by increased ocular pressure.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: September 15, 1992
    Assignee: Burroughs Wellcome Co.
    Inventors: Heather Giles, Alan D. Robertson, Michael G. Kelly, Leff, Paul
  • Patent number: 5145501
    Abstract: A composition comprising(a) a 3-isothiazolone compound of the formula ##STR1## wherein R and R.sup.1 are independently selected from hydrogen, halogen or R is a (C.sub.1 -C.sub.4) alkyl group and R.sup.1 is a halogen or R and R.sup.1 may be joined to form an unsaturated 5- or 6-membered carbocyclic ring; Y is hydrogen, a (C.sub.1 -C.sub.18) alkyl group, an unsubstituted or halo-substituted alkenyl or alkynyl of 2 to 8 carbon atoms, a cycloalkyl or substituted cycloalkyl of 3 to 12 carbon atoms, an aralkyl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aralkyl of up to 10 carbon atoms, or an aryl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aryl group of up to 10 carbon atoms; and(b) an amount of a metal bromate salt sufficient to stabilize said composition;wherein said composition if free of metal nitrate salt is disclosed. Methods of use of the above compositions are also disclosed.
    Type: Grant
    Filed: November 12, 1991
    Date of Patent: September 8, 1992
    Assignee: Rohm and Haas Company
    Inventors: Edward S. Lashen, Ramesh B. Petigara
  • Patent number: 5140046
    Abstract: Novel phenylene derivatives shown by the general formula ##STR1## where A represents a hydrogen atom, a phenyl group or a phenoxy group, n represents an integer of 3 to 10, R.sub.1 represents a hydrogen atom or a lower alkoxy group, X.sub.1 represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CONH--, B represents ##STR2## wherein R.sub.2 represents a hydrogen atom, a halogen atom, a nitro group, etc.), ##STR3## (wherein R.sub.3 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group), X.sub.2 represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, etc. and D represents a carboxy group, a lower alkoxycarbonyl group or ##STR4## which are useful as drugs, particularly SRS-A(slow reacting substance of anaphylaxis) antagonist, i.e. they are useful as prophylaxis and treatment for various allergic diseases (e.g. bronchial asthma, allergic rhinitis, urticaria) or, ischemic heart diseases, inflammation, etc. induced by SRS-A.
    Type: Grant
    Filed: August 13, 1990
    Date of Patent: August 18, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Toshiyasu Mase, Kiyoshi Murase, Hiromu Hara, Kenichi Tomioka
  • Patent number: 5138061
    Abstract: Thioacylating reagents are provided for the introduction of thioamide bonds into growing peptides represented by the structure: ##STR1## where the substituents are disclosed herein. Intermediate precursors for preparing these thioacylating reagents are also provided. A process for preparing the thioacylating reagents and the intermediate precursors is further provided.
    Type: Grant
    Filed: August 4, 1989
    Date of Patent: August 11, 1992
    Assignee: BioChem Pharma Inc.
    Inventors: Bernard Belleau, deceased, Denis Brillon, Gilles Sauve, Boulos Zacharie
  • Patent number: 5137899
    Abstract: An improved process for preparing a 3-isothiazolone of the formula ##STR1## wherein R and R.sup.1 are independently selected from hydrogen, halogen or R is a (C.sub.1 -C.sub.4) alkyl group and R.sup.1 is a halogen; Y is hydrogen, a (C.sub.1 -C.sub.18) alkyl group, an unsubstituted or halo-substituted (C.sub.2 -C.sub.8) alkenyl or alkynyl, a cycloalkyl or substituted (C.sub.3 -C.sub.12) cycloalkyl, an aralkyl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aralkyl of to 10 carbon atoms, or an aryl or halo-, (C.sub.1 -C.sub.4) alkyl-, or (C.sub.1 -C.sub.4) alkoxy-substituted aryl aryl group of up to 10 carbon atoms; comprising(a) reacting a disulfide ester with an amine to generate a disulfide amide;(b) contacting the disulfide amide with a halogenating agent in order to cyclize the amide to form the isothiazolone.HX;(c) neutralizing the isothiazolone.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: August 11, 1992
    Assignee: Rohm and Haas Company
    Inventors: Ramesh B. Petigara, Edward S. Lashen
  • Patent number: 5135914
    Abstract: Novel substituted derivatives of 3-amino-2-hydroxypropionic acid are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as renin inhibitors and thus useful in controlling hypertension, hyperaldosteronism and congestive heart failure as well as diagnostic agents.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: August 4, 1992
    Assignee: Warner-Lambert Company
    Inventors: Harriet W. Hamilton, William C. Patt
  • Patent number: 5132448
    Abstract: .alpha.-Chloro phosphorus ylides of the formula I ##STR1## where the Ar radicals are identical or different aryl groups, and E is a substituent which stabilizes the ylide (I), are prepared by reacting a phosphonium salt of the formula II ##STR2## where Hal is chlorine, bromine or iodine, with a chlorinating agent, using bleaching powder as chlorinating agent.
    Type: Grant
    Filed: September 11, 1990
    Date of Patent: July 21, 1992
    Assignee: BASF Aktiengesellschaft
    Inventor: Bernd Schaeffer
  • Patent number: 5132428
    Abstract: A process for enantioselectively alkylating, at the asterisked carbon atom, a single enantiomer of a glycine derivative having the general formula ZCOCH(R)NY wherein Z is a moiety derived from a chiral sultam, R is hydrogen or C.sub.1 to C.sub.10 alkyl and Y is one or more groups rendering the nitrogen atom unreactive towards alkylating agents comprises:(i) reacting the glycine derivative with an enolising agent to produce the corresponding enolate of the glycine derivative, and(ii) thereafter reacting the enolate of the glycine derivative with an alkylating agent of formula R.sup.1 X to generate a single enantiomer of a product of formula ZCOC(R)(R.sup.1)NY where R.sup.1 is selected from C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.20 aralkyl, C.sub.2 to C.sub.10 alkenyl or substituted derivatives thereof and X is Cl, Br or I. The product of the process can be treated with first acid and then base to generate the enantiomerically pure alpha-amino acid of formula HO.sub.2 CC(R)(R.sup.1)NH.sub.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: July 21, 1992
    Assignee: BP Chemicals Limited
    Inventor: Wolfgang W. R. E. J. von Oppolzer
  • Patent number: 5130443
    Abstract: A process for the preparation of anilide couplers which comprises the reaction of an acid, an aromatic hydroxy compound, and an oxyhalide; isolating and purifying the aromatic ester formed; and subsequently reacting said ester with an aniline in the presence of a solvent.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: July 14, 1992
    Assignee: Xerox Corporation
    Inventors: Kock-Yee Law, Ihor W. Tarnawskyj, F. Courtney Bailey
  • Patent number: 5128364
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: March 28, 1991
    Date of Patent: July 7, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Pierre Hamel
  • Patent number: 5126362
    Abstract: An oxime derivative represented by the general formula [1]: ##STR1## wherein A, B, Y and W represent each a specified group, and an optically active isomer thereof and a fungicide for agricultural and horticultural use for containing said derivative or an optically active isomer thereof as an active ingredient are disclosed.
    Type: Grant
    Filed: September 25, 1989
    Date of Patent: June 30, 1992
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Hideo Suzuki, Takeshi Mita, Toshiaki Takeyama, Masami Hanaue, Masao Nishikubo, Kazuhiro Yamagishi
  • Patent number: 5126435
    Abstract: A process for the preparation of azo dyes of formula ##STR1## wherein K is the radical of a coupling component of the benzene or naphthalene series or of the heterocyclic series, and the hydroxy group is attached to K adjacent to the azo group, X is hydrogen or nitro and M is an alkali metal ion or an ammonium ion, which process comprises coupling a diazo component of formula ##STR2## in the presence of a zinc salt and in an inert gas atmosphere, to a coupling component of formula ##STR3## in which formula (2) and (3) above K and X are as defined for formula (1). The process makes it possible to obtain the azo dyes in high yield.
    Type: Grant
    Filed: October 11, 1990
    Date of Patent: June 30, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans P. Joswig, Werner Huber
  • Patent number: 5126459
    Abstract: A process for preparing a 5-arylhydantoin having the formula (II): ##STR1## which comprises: reacting methyl 2-hydroxy-2-methoxyacetate, urea and an aryl compound having the formula (I): ##STR2## in the presence of an acid. According to the process, the 5-arylhydantoin which is a very effective intermediate for preparing D-arylglycines can be easily prepared from inexpensive raw materials in a high purity.
    Type: Grant
    Filed: September 3, 1991
    Date of Patent: June 30, 1992
    Assignee: Kanegafuchi Kagaku Kogyo Kabushiki Kaisha
    Inventors: Masahiko Yamada, Satomi Takahashi
  • Patent number: 5126326
    Abstract: Disclosed herein are peptide derivatives which inhibit the activities of human immunodeficiency virus (HIV) protease and renin. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is a derived amino acid based on an O.sup.4 -(carboxymethyl)-tyrosyl residue, R.sup.2 and are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CHR.sup.18 --C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or one and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives are useful as agents for combatting HIV infections and for treating renin-associated hypertension and congestive heart failure.
    Type: Grant
    Filed: June 6, 1989
    Date of Patent: June 30, 1992
    Assignee: Bio-Mega, Inc.
    Inventors: Paul C. Anderson, Yvan Guindon, Christiane Yoakim
  • Patent number: 5126363
    Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.
    Type: Grant
    Filed: January 23, 1991
    Date of Patent: June 30, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Peter H. Andersen, Louis B. Hansen, Peter Faarup, John B. Hansen
  • Patent number: 5120740
    Abstract: Prodrugs for the treatment of kidney tumors are disclosed. The prodrugs are conjugates that can require the cooperation of multiple enzymes in the kidney to release 6-mercaptopurine or 6-thioguanin, or can selectively release 6-thioguanine. Methods for use of these prodrugs are also disclosed.
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: June 9, 1992
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Adnan A. Elfarra
  • Patent number: 5120854
    Abstract: There are provided novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl-2-imidazolin-5-one compounds, novel intermediates and methods for the preparation of said compounds, and a method for controlling a variety of annual and perennial plant species utilizing novel benzenesulfonyl carboxamide compounds and novel intermediate benzenesulfonyl 2-imidazolin-5-one compounds.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: June 9, 1992
    Assignee: American Cyanamid Company
    Inventors: Sergio I. Alvarado, Alvin D. Crews, Jr., Peter J. Wepplo, Robert F. Doehner, Jr., Thomas E. Brady, David M. Gange, Desiree L. Little
  • Patent number: 5117006
    Abstract: A DC-88A derivative represented by general formula: ##STR1## wherein ##STR2## represents ##STR3## has an excellent antitumor activity and is useful as an anti-tumor agent.
    Type: Grant
    Filed: May 15, 1991
    Date of Patent: May 26, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiromitsu Saito, Masaji Kasai, Makoto Morimoto, Eiji Kobayashi, Yoichi Uosaki, Yutaka Kanda, Hiroshi Sano
  • Patent number: 5115337
    Abstract: A nonlinear optical material comprising a compound represented by formula (I) ##STR1## wherein Z.sup.1, Z.sup.2, R.sup.1, X and n are as defined before, or a compound represented by formula (II) ##STR2## wherein Z.sup.11 and Z.sup.12 are as defined before. The compounds of formulae (I) and (II) exhibits high transmittance to blue light and high nonlinear optical effects.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: May 19, 1992
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Masaki Okazaki, Tadao Shishido, Seiiti Kubodera
  • Patent number: 5110934
    Abstract: Bisphenols having a pendent imide moiety, of formula (I) ##STR1## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from hydrogen, fluorine, chlorine, bromine, alkyl of 1 to 6 carbon atoms, aryl of 6 to 10 carbon atoms, alkoxy of 1 to 6 carbon atoms and aryloxy of 6 to 10 carbon atoms; R.sub.5 is selected from fluorine, chlorine, bromine and alkyl of 1 to 6 carbon atoms, and m is 0, 1, 2, 3 or 4; and R.sub.7 is alkyl of 1 to 18 carbon atoms, aryl of 6 to 10 carbon atoms, unsubstituted or substituted one or more times by a substituent selected from fluorine, chlorine, trifluoromethyl, alkyl of 1 to 6 carbon atoms, and phenyl, or heteroaryl; are useful in producing poly(imidoarylether ketone)s and poly(imidoarylether sulfone)s which are amorphous and are soluble in readily available solvents, while displaying high glass transition temperatures and good thermo-oxidative stability.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: May 5, 1992
    Inventors: Allan S. Hay, Marko Strukelj