Patents Examined by M. S. H. Gabilan
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Patent number: 5147885Abstract: 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: GrantFiled: May 23, 1991Date of Patent: September 15, 1992Assignee: Burroughs Wellcome Co.Inventors: Heather Giles, Alan D. Robertson, Michael G. Kelly, Leff, Paul
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Patent number: 5145501Abstract: 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: GrantFiled: November 12, 1991Date of Patent: September 8, 1992Assignee: Rohm and Haas CompanyInventors: Edward S. Lashen, Ramesh B. Petigara
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Patent number: 5140046Abstract: 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: GrantFiled: August 13, 1990Date of Patent: August 18, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Kiyoshi Murase, Hiromu Hara, Kenichi Tomioka
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Patent number: 5137899Abstract: 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: GrantFiled: October 30, 1991Date of Patent: August 11, 1992Assignee: Rohm and Haas CompanyInventors: Ramesh B. Petigara, Edward S. Lashen
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Patent number: 5138061Abstract: 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: GrantFiled: August 4, 1989Date of Patent: August 11, 1992Assignee: BioChem Pharma Inc.Inventors: Bernard Belleau, deceased, Denis Brillon, Gilles Sauve, Boulos Zacharie
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Patent number: 5135914Abstract: 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: GrantFiled: May 23, 1988Date of Patent: August 4, 1992Assignee: Warner-Lambert CompanyInventors: Harriet W. Hamilton, William C. Patt
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Patent number: 5132448Abstract: .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: GrantFiled: September 11, 1990Date of Patent: July 21, 1992Assignee: BASF AktiengesellschaftInventor: Bernd Schaeffer
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Patent number: 5132428Abstract: 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: GrantFiled: November 5, 1990Date of Patent: July 21, 1992Assignee: BP Chemicals LimitedInventor: Wolfgang W. R. E. J. von Oppolzer
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Patent number: 5130443Abstract: 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: GrantFiled: April 29, 1991Date of Patent: July 14, 1992Assignee: Xerox CorporationInventors: Kock-Yee Law, Ihor W. Tarnawskyj, F. Courtney Bailey
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Patent number: 5128364Abstract: 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: GrantFiled: March 28, 1991Date of Patent: July 7, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Yves Girard, Pierre Hamel
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Patent number: 5126326Abstract: 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: GrantFiled: June 6, 1989Date of Patent: June 30, 1992Assignee: Bio-Mega, Inc.Inventors: Paul C. Anderson, Yvan Guindon, Christiane Yoakim
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Patent number: 5126363Abstract: 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: GrantFiled: January 23, 1991Date of Patent: June 30, 1992Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Peter H. Andersen, Louis B. Hansen, Peter Faarup, John B. Hansen
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Patent number: 5126435Abstract: 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: GrantFiled: October 11, 1990Date of Patent: June 30, 1992Assignee: Ciba-Geigy CorporationInventors: Hans P. Joswig, Werner Huber
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Patent number: 5126459Abstract: 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: GrantFiled: September 3, 1991Date of Patent: June 30, 1992Assignee: Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Masahiko Yamada, Satomi Takahashi
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Patent number: 5126362Abstract: 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: GrantFiled: September 25, 1989Date of Patent: June 30, 1992Assignee: Nissan Chemical Industries, Ltd.Inventors: Hideo Suzuki, Takeshi Mita, Toshiaki Takeyama, Masami Hanaue, Masao Nishikubo, Kazuhiro Yamagishi
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Patent number: 5120854Abstract: 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: GrantFiled: November 13, 1990Date of Patent: June 9, 1992Assignee: American Cyanamid CompanyInventors: Sergio I. Alvarado, Alvin D. Crews, Jr., Peter J. Wepplo, Robert F. Doehner, Jr., Thomas E. Brady, David M. Gange, Desiree L. Little
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Patent number: 5120740Abstract: 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: GrantFiled: June 25, 1990Date of Patent: June 9, 1992Assignee: Wisconsin Alumni Research FoundationInventor: Adnan A. Elfarra
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Patent number: 5117006Abstract: 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: GrantFiled: May 15, 1991Date of Patent: May 26, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiromitsu Saito, Masaji Kasai, Makoto Morimoto, Eiji Kobayashi, Yoichi Uosaki, Yutaka Kanda, Hiroshi Sano
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Patent number: 5115337Abstract: 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: GrantFiled: October 16, 1990Date of Patent: May 19, 1992Assignee: Fuji Photo Film Co., Ltd.Inventors: Masaki Okazaki, Tadao Shishido, Seiiti Kubodera
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Patent number: 5110797Abstract: Peptide compounds of formula (I): ##STR1## wherein A is hydrogen or an amino-protecting group; X is a member selected from the group consisting of Gly, Glu, Tyr, Asp, Phe, Ile, Ala, Pro, Leu, Hyp, Val, His, Arg, Ser, Thr, Pyr, Trp, 5-HTP, Cys, Met, .tau.-Glu, .beta.-Asp; Y is a (CH.sub.2).sub.3-6 or (CH.sub.2).sub.3-6 having an hydroxy group; R is an hydroxy group or an oxygen atom with a carboxy-protecting group; are useful as neurotropic agents.Type: GrantFiled: April 29, 1988Date of Patent: May 5, 1992Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kazuharu Ienaga, Kunihiko Higashiura