The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/510)
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Patent number: 4791109Abstract: Novel indole-carboxamides of the formula ##STR1## wherein R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted with 1 to 3 members of the group consisting of halogen, methyl, ethyl, methoxy, ethoxy, --CF.sub.3, CH.sub.3 S--, --NH.sub.2 and --NO.sub.2 or R.sub.1 and R taken together with the nitrogen atom form an optionally unsaturated heterocycle optionally containing a member of the group consisting of --O--, --S-- and ##STR2## R' is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, naphthyl, aralkyl of 7 to 12 carbon atoms and substituted phenyl, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, chlorine, bromine, iodine, --NO.sub.2, --NH.sub.Type: GrantFiled: July 10, 1986Date of Patent: December 13, 1988Assignee: Roussel UclafInventors: Francois Clemence, Jacques Guillaume, Gilles Hamon
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Patent number: 4740519Abstract: 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: GrantFiled: March 13, 1986Date of Patent: April 26, 1988Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 4729986Abstract: 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: GrantFiled: March 18, 1987Date of Patent: March 8, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Richard E. Olson
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Patent number: 4675405Abstract: 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: GrantFiled: January 27, 1986Date of Patent: June 23, 1987Assignee: American Home Products CorporationInventors: John H. Musser, Dennis M. Kubrak, Anthony F. Kreft, III
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Patent number: 4661511Abstract: 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: GrantFiled: July 27, 1984Date of Patent: April 28, 1987Assignee: Degussa AktiengesellschaftInventors: Erwin von Angerer, Helmut Schonenberger
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Patent number: 4647666Abstract: 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: GrantFiled: July 15, 1985Date of Patent: March 3, 1987Assignee: Iowa State University Research Foundation, Inc.Inventor: Richard C. Larock
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Patent number: 4634716Abstract: 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: GrantFiled: May 16, 1983Date of Patent: January 6, 1987Assignee: Merck & Co., Inc.Inventors: William H. Parsons, David Taub
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Patent number: 4581457Abstract: 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: GrantFiled: September 21, 1984Date of Patent: April 8, 1986Assignee: American Home Products CorporationInventors: John H. Musser, Dennis M. Kubrak
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Patent number: 4510158Abstract: 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: GrantFiled: March 5, 1984Date of Patent: April 9, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4500341Abstract: 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: GrantFiled: October 21, 1981Date of Patent: February 19, 1985Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Ludwig Eue, Robert R. Schmidt
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Patent number: 4496742Abstract: 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: GrantFiled: October 4, 1982Date of Patent: January 29, 1985Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4493843Abstract: 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: GrantFiled: May 21, 1982Date of Patent: January 15, 1985Assignee: May & Baker LimitedInventors: Michael J. Ashton, Andrew W. Bridge, Robert F. Chapman, Garry Fenton, Anthony H. Loveless, David Riddell
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Patent number: 4491664Abstract: 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: GrantFiled: March 12, 1982Date of Patent: January 1, 1985Assignee: Sandoz Ltd.Inventor: Wolfgang Oppolzer
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Patent number: 4465851Abstract: 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: GrantFiled: January 4, 1982Date of Patent: August 14, 1984Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mutsumi Muramatsu, Toshio Satoh, Hiroyasu Sekine, Atsushi Tendo
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Patent number: 4425355Abstract: 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: GrantFiled: June 29, 1981Date of Patent: January 10, 1984Assignee: Warner-Lambert CompanyInventors: Milton L. Hoefle, George Bobowski
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Patent number: 4424365Abstract: 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: GrantFiled: June 22, 1982Date of Patent: January 3, 1984Assignee: The Upjohn CompanyInventor: Wendell Wierenga
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Patent number: 4423229Abstract: 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: GrantFiled: February 8, 1982Date of Patent: December 27, 1983Assignee: The Upjohn CompanyInventor: Wendell Wierenga
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Patent number: 4372970Abstract: There are provided benzofuran-substituted acetic acid esters and compositions thereof having arthropocidal activity.Type: GrantFiled: July 9, 1981Date of Patent: February 8, 1983Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Malcolm R. Hadler, David R. Woodward, Andrew A. Godfrey
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Patent number: 4366102Abstract: 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: GrantFiled: May 6, 1981Date of Patent: December 28, 1982Assignee: Bayer AktiengesellschaftInventors: Gunter Rauchschwalbe, Heinz U. Blank, Karl Mannes, Dietmar Mayer
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Patent number: 4340540Abstract: 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: GrantFiled: June 26, 1980Date of Patent: July 20, 1982Assignee: Bayer AktiengesellschaftInventor: Karl H. Hermann