The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/510)
  • Patent number: 4740519
    Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein Z is O or S, ##STR5## wherein R.sub.5 is lower alkyl or ##STR6## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: April 26, 1988
    Assignee: Centre International de Recherches Dermatologiques C.I.R.D.
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 4729986
    Abstract: Substituted silylmethyl 1,2,4-triazoles and imidazoles also having selected substituents on the heterocyclic ring, agriculturally useful compositions comprising such compounds and the use of such compounds as fungicides.
    Type: Grant
    Filed: March 18, 1987
    Date of Patent: March 8, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Richard E. Olson
  • Patent number: 4675405
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is --O--, --S--, ##STR3## when n=0, or W is ##STR4## when n=1, and the dotted line represents an optional double bond; Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR5## n is 0-1; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is loweralkyl, perfluoroloweralkyl or perfluorophenyl, with the proviso that when X=N, W=O or S and n=0, R.sup.3 is other than loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.
    Type: Grant
    Filed: January 27, 1986
    Date of Patent: June 23, 1987
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Dennis M. Kubrak, Anthony F. Kreft, III
  • Patent number: 4661511
    Abstract: Pharmaceutical compositions are provided containing a 2-(hydroxyphenyl)-indole or a 2-(C.sub.2 -C.sub.6 -alkanoxyloxyphenyl) indole and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 27, 1984
    Date of Patent: April 28, 1987
    Assignee: Degussa Aktiengesellschaft
    Inventors: Erwin von Angerer, Helmut Schonenberger
  • Patent number: 4647666
    Abstract: Functionally substituted arenes selected from the group consisting of p-tolylacetic acid, N-methylbenzamide, benzamide and acetanilide which are thallated provide an organothallium salt which undergoes subsequent palladium promoted olefination to provide oxygen and/or nitrogen heterocycles such as ethers lactones, isoquinolones, indoles and isocarbostyrils.
    Type: Grant
    Filed: July 15, 1985
    Date of Patent: March 3, 1987
    Assignee: Iowa State University Research Foundation, Inc.
    Inventor: Richard C. Larock
  • Patent number: 4634716
    Abstract: Compounds of the formula: ##STR1## where R.sup.3 is ##STR2## where n is 1-3 and the R.sup.a 's and R.sup.b 's are independently hydrogen or loweralkyl; and pharmaceutically acceptable salts thereof; are inhibitors or angiotensin I converting enzyme useful as antihypertensive agents.
    Type: Grant
    Filed: May 16, 1983
    Date of Patent: January 6, 1987
    Assignee: Merck & Co., Inc.
    Inventors: William H. Parsons, David Taub
  • Patent number: 4581457
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## W is ##STR3## Y is ##STR4## n is 0-8; R.sup.1 is hydrogen, loweralkyl, loweralkoxy, lower alkanoyl, halo, trifluoromethyl, cyano or nitro;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and in antithrombotic therapy.
    Type: Grant
    Filed: September 21, 1984
    Date of Patent: April 8, 1986
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Dennis M. Kubrak
  • Patent number: 4510158
    Abstract: 4-(1-R'-2-phenyl-1H-indol-3-yl)-3-cyclohexene-1-carboxylic acids, 4-(1'R'-2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids, 4-(1-R'-2-phenyl-1H-indol-3-yl)benzoic acids, the corresponding cyclohexene- and cyclohexane-1,1-dicarboxylic acids, and lower-alkyl esters thereof, wherein R' is hydrogen or lower-alkyl, are prepared by reacting a 1-R'-2-phenyl-1H-indole with a cyclohexanone-4-carboxylic acid or -4,4-dicarboxylic acid, followed as desired by a hydrogenation or aromatization process. The compounds which are free carboxylic acids or salts thereof are useful as complement inhibitors. The corresponding esters are useful as intermediates.
    Type: Grant
    Filed: March 5, 1984
    Date of Patent: April 9, 1985
    Assignee: Sterling Drug Inc.
    Inventor: Denis M. Bailey
  • Patent number: 4500341
    Abstract: Phenoxycarboxylic acid amide compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 are individually selected from hydrogen and methyl,R.sup.3 is hydrogen or alkyl with from 1 to 5 carbon atomsR.sup.4 is optionally substituted alkoxycarbonylalkyl, aminocarbonylalkyl or dialkylaminocarbonylalkyl, phenyl, or substituted phenyl wherein the substituent is at least one of the group consisting of alkyl, alkoxy or alkylthio of from 1 to 4 carbon atoms, carbalkoxy of from 2 to 4 carbon atoms, halogen, and nitro; orR.sup.3 and R.sup.
    Type: Grant
    Filed: October 21, 1981
    Date of Patent: February 19, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz Forster, Ludwig Eue, Robert R. Schmidt
  • Patent number: 4496742
    Abstract: Novel structural analogues of 5,6-dihydro PGI.sub.2 of the formula: ##STR1## and the corresponding 10,11-didehydro-11-deoxy derivatives are useful as antiallergy agents.
    Type: Grant
    Filed: October 4, 1982
    Date of Patent: January 29, 1985
    Assignee: The Upjohn Company
    Inventor: Herman W. Smith
  • Patent number: 4493843
    Abstract: Indole and indoline derivatives of the formula: ##STR1## wherein indicates a double bond or a single bond between carbon atoms, R.sup.1 represents hydrogen, alkyl of 1 through 6 carbon atoms, or alkyl of 1 through 6 carbon atoms substituted by one or more than one of the same type of substituents selected from the hydroxy group, alkenyl groups of 2 through 5 carbon atoms, and alkanoyloxy groups of 2 through 7 carbon atoms, and one of the symbols R.sup.2 represents alkyl of 6 through 24 carbon atoms and the other symbol R.sup.2 represents alkyl of 1 through 24 carbon atoms or hydrogen, and R.sup.3 represents alkyl of 1 through 6 carbon atoms or hydrogen, are new compounds possessing useful pharmacological properties. They are of use in the treatment of diabetes mellitus, hyperlipoproteinaemic states, of atherosclerosis, and of associated conditions.
    Type: Grant
    Filed: May 21, 1982
    Date of Patent: January 15, 1985
    Assignee: May & Baker Limited
    Inventors: Michael J. Ashton, Andrew W. Bridge, Robert F. Chapman, Garry Fenton, Anthony H. Loveless, David Riddell
  • Patent number: 4491664
    Abstract: A process for the production of an ergot alkaloid comprising intramolecularly cyclizing a 3-iminoethyl-4-trans-buta-1',3'-dienylindole to produce an 8-ergolene and as necessary converting the resultant ergolene into the desired ergot alkaloid.
    Type: Grant
    Filed: March 12, 1982
    Date of Patent: January 1, 1985
    Assignee: Sandoz Ltd.
    Inventor: Wolfgang Oppolzer
  • Patent number: 4465851
    Abstract: A compound having the formula ##STR1## wherein R.sub.1 represents an indanyl, indolyl, quinolyl or chromonyl group, the group of the formula ##STR2## (in which R.sub.2 represents a halogen atom or a nitro group), or the group of the formula ##STR3## (in which R.sub.3 represents a halogen atom, or an alkyl, nitro, cyano, acetamino, aminosulfonyl, benzoyl, phenoxy or trifluoromethyl group, R.sub.4 represents a hydrogen or halogen atom, or an alkyl group, and R.sub.5 represents a hydrogen or halogen atom, or an alkyl group), or a pharmaceutically acceptable salt thereof. The compound is obtained by reacting 4-guanidinomethylcyclohexanecarboxylic acid or a reactive derivative thereof with a compound of the formula R.sub.1 --OH wherein R.sub.1 is the same as defined above, or a reactive derivative thereof.
    Type: Grant
    Filed: January 4, 1982
    Date of Patent: August 14, 1984
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mutsumi Muramatsu, Toshio Satoh, Hiroyasu Sekine, Atsushi Tendo
  • Patent number: 4425355
    Abstract: Substituted acyl derivatives of octahydro-1H-indole-2-carboxylic acid and the pharmaceutically acceptable salts thereof are produced by acylating a suitably substituted octahydro-1H-indole with a suitably activated substituted carboxylic acid and when desired hydrolyzing the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.
    Type: Grant
    Filed: June 29, 1981
    Date of Patent: January 10, 1984
    Assignee: Warner-Lambert Company
    Inventors: Milton L. Hoefle, George Bobowski
  • Patent number: 4424365
    Abstract: Novel antibacterially active compound, 1,2,8,8a-cyclopropa?c!benzo?1,2-b:-4,3-b'!dipyrrol-4(5H)-one, prepared by a novel chemical process. This compound, as well as antibacterially-active intermediates, can be used to eradicate or control susceptible bacteria, for example B. subtilis, K. pneumonia, S. lutea, S. aureus, and M. avium.
    Type: Grant
    Filed: June 22, 1982
    Date of Patent: January 3, 1984
    Assignee: The Upjohn Company
    Inventor: Wendell Wierenga
  • Patent number: 4423229
    Abstract: Novel antibacterially-active compound, 1,2,8,8a-cyclopropa[ c]-benzo[1,2-b:-4,3-b']dipyrol-4(5H)-one, prepared by a novel chemical process. This compound, as well as antibacterially-active intermediates, can be used to eradicate or control susceptible bacteria, for example, B. subtilis, K. pneumonia, S. lutea, S. aureus, and M. avium.
    Type: Grant
    Filed: February 8, 1982
    Date of Patent: December 27, 1983
    Assignee: The Upjohn Company
    Inventor: Wendell Wierenga
  • Patent number: 4372970
    Abstract: There are provided benzofuran-substituted acetic acid esters and compositions thereof having arthropocidal activity.
    Type: Grant
    Filed: July 9, 1981
    Date of Patent: February 8, 1983
    Assignee: Shell Internationale Research Maatschappij B.V.
    Inventors: Malcolm R. Hadler, David R. Woodward, Andrew A. Godfrey
  • Patent number: 4366102
    Abstract: In a process for the preparation of an aromatic chloroformic acid ester by contacting a phenol and phosgene, the improvement wherein the reaction is carried out in a homogeneous liquid phase at a temperature of 60.degree. to 180.degree. C. in the presence of organic phosphorus compound of the formulaR.sup.1 R.sup.2 R.sup.3 PR.sup.4.sub.n X.sub.nin whichR.sup.1, R.sup.2 and R.sup.3 independently of one another represent hydrogen, alkyl, alkenyl, aralkyl, aryl or halogen and two of the said radicals together with the phosphorus atom can form a 5-membered or 6-membered phosphorus-containing saturated or unsaturated heterocyclic radical,X represents OH, homopolar-bonded halogen or an inorganic or organic acid anion,R.sup.4 denotes hydrogen or alkyl or, if X denotes halogen, can also denote halogen and n denotes 0 or 1,and in which, furthermore,R.sup.4 and X together can represent oxygen or sulfur.
    Type: Grant
    Filed: May 6, 1981
    Date of Patent: December 28, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Rauchschwalbe, Heinz U. Blank, Karl Mannes, Dietmar Mayer
  • Patent number: 4340540
    Abstract: To prepare basic dyestuffs of the general formula ##STR1## in which A and B independently of one another represent a hetero-aromatic radical or a radical of the general formula ##STR2## compounds of the general formulaA--CH.sub.2 --BA and B have the abovementioned meaning,are oxidized with oxygen in the presence of a nucleophilic compound of the general formulaD--Hand in the presence of catalytic amounts of benzoquinones substituted by halogen or cyano or of phenanthrenequinones substituted by nitro, and in the presence of catalytic amounts of nitrogen oxides--with the exception of dinitrogen monoxide--or of substances which produce such nitrogen oxides under the reaction conditions.
    Type: Grant
    Filed: June 26, 1980
    Date of Patent: July 20, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventor: Karl H. Hermann