Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Isatins, Etc.) Patents (Class 548/485)
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Patent number: 4863949Abstract: The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.Type: GrantFiled: September 21, 1987Date of Patent: September 5, 1989Assignee: Boehringer Mannheim GmbHInventors: Herbert Simon, Helmut Michel, Wolfgang Bartsch, Klaus Strein
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Patent number: 4859230Abstract: There are described new halocyclopropyl compounds of the general formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, independently of each other, are hydrogen or C.sub.1-4 -alkyl,X is hydrogen or halogen,Y is halogen,n is 0, 1, 2 or 3,U and V are hydrogen or halogen, andW is a heterocyclic group of formula ##STR2## in which T is halogen, C.sub.1-4 -alkyl, C.sub.1-4 -haloalkyl, CN or OR.sub.9Q is CH or N,Z is O or S,R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each a straight, branched or cyclic C.sub.1-7 -alkyl group optionally substituted by up to six halogen atoms, orR.sub.4 and R.sub.5, can also together form a 4 to 7 membered ring that is saturated or unsaturated and can contain further hetero atoms, such as O, S or N, and can optionally be substituted by one to three methyl groups or one to six halogen atoms, andR.sub.9 is hydrogen, C.sub.1-4 -alkyl or C.sub.1-4 -haloalkyl,processes for their preparation and their use as herbicide with high selectivity.Type: GrantFiled: October 14, 1987Date of Patent: August 22, 1989Assignee: Schering AktiengesellschaftInventors: Friedhelm Blume, Wilfried Franke, Friedrich Arndt, Richard Rees
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Patent number: 4855298Abstract: A quinazolinone derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a halogen atom, or a salt thereof and processes for preparing the same are disclosed. The quinazolinone derivative (I) is useful for treatment of diabetic complications.Type: GrantFiled: October 29, 1987Date of Patent: August 8, 1989Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Yoshihisa Yamada, Yuzo Matsuoka
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Patent number: 4847381Abstract: Substituted 4-quinoline-carboxylic acids useful in the treatment of arthritis and inhibition of progressive joint deterioration are disclosed together with methods of use and synthesis thereof.Type: GrantFiled: August 31, 1987Date of Patent: July 11, 1989Assignee: American Cyanamid CompanyInventors: Leslie H. Sutherland, Adolph E. Sloboda, Ralph G. Child, John F. Poletto, Dennis W. Powell
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Patent number: 4841057Abstract: An anthraquinone compound represented by formula: ##STR1## wherein R and X are as defined in the specification, and a polarizing film containing the same. The anthraquinone compound exhibits satisfactory compatibility with organic polymers and high dichroism, and the polarizing films have excellent performance characteristics.Type: GrantFiled: January 12, 1988Date of Patent: June 20, 1989Assignee: Mitsubishi Chemical Industries LimitedInventors: Konoe Miura, Tetsuo Ozawa, Seigo Okumura, Shinji Kubo
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Patent number: 4835166Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.Type: GrantFiled: December 7, 1987Date of Patent: May 30, 1989Assignee: Pfizer Inc.Inventors: Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
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Patent number: 4833270Abstract: This disclosure describes a novel process for preparing 2-chloro-4,5-difluorobenzoic acid which is useful in the preparation of 7-(substituted)piperazinyl-1-substituted-6-fluoro-1,4-dihydro-4-oxo-3-quin oli necarboxylic acid antibacterial agents.Type: GrantFiled: December 21, 1987Date of Patent: May 23, 1989Assignee: American Cyanamid CompanyInventors: Panayota Bitha, Yang-I Lin
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Patent number: 4826994Abstract: Production of indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at positions 5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.Type: GrantFiled: February 26, 1988Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: Alan H. Katz, Christopher A. Demerson, Leslie G. Humber
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Patent number: 4803207Abstract: Pyrimidoindoles of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl a mono- or bicyclic aryl radical or a group of mormula R.sup.3 O--B--[where R.sup.3 O is (lower)alkoxy,aryl(lower)alkoxy or hydroxy and B is a lower alkylene chain optionally containing one double or triple bond], R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower) alkylamino and A, together with the carbon atom to which it is attached, represents 5, 6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as hypoglyceamics.Type: GrantFiled: March 9, 1987Date of Patent: February 7, 1989Assignee: John Wyeth & Brother Ltd.Inventors: Alan C. White, Ian A. Cliffe, Richard S. Todd
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Patent number: 4795757Abstract: Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.Type: GrantFiled: November 20, 1986Date of Patent: January 3, 1989Assignee: Rorer Pharmaceutical CorporationInventors: John R. Regan, Jeffrey N. Barton, John T. Suh, Jerry W. Skiles
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Patent number: 4780477Abstract: This invention provides novel isatin compounds which are useful as therapeutic agents. The invention isatin compounds and the pharmaceutically acceptable salts thereof exhibit anti-ulcer activities which are applicable for propylaxis and treatment of ulcer diseases in the digestive tract of animals.Type: GrantFiled: May 29, 1986Date of Patent: October 25, 1988Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Michihiro Kobayashi, Makio Kitazawa, Masuo Akahane, Tsutomu Tsukamoto, Ryoji Yamamoto, Yasushi Nakano
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Patent number: 4772614Abstract: Quinolones with antihypertensive activity have the general formula I, ##STR1## wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease.Type: GrantFiled: June 13, 1986Date of Patent: September 20, 1988Assignee: The Boots CompanyInventors: Roy V. Davies, James Fraser, Kenneth J. Nichol
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Patent number: 4762839Abstract: Novel quinazolinone compounds of the formula: ##STR1## wherein R is hydrogen atom or a lower alkyl, R.sup.1 is a lower alkyl, a substituted or unsubstituted phenyl or an aralkyl, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom, a halogen atom, a lower alkyl, a lower alkoxy, a lower alkoxycarbonyl or a lower alkoxycarbonyl-lower alkenyl, or two adjacent groups of R.sup.2,R.sup.3, R.sup.4 and R.sup.5 when taken together form methylenedioxy and the other two are hydrogen atom, and a salt thereof, which are useful for the prophylaxis and treatment of various diabetic complications, and processes for the preparation thereof, and a pharmaceutical composition containing said compound as an active ingredient.Type: GrantFiled: May 22, 1986Date of Patent: August 9, 1988Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Yoshihisa Yamada, Yuzo Matsuoka, Mamoru Matsumoto
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Patent number: 4750908Abstract: The invention relates to the use of 2,3-indolinedione of formula: ##STR1## for dyeing keratinous fibres, especially human hair.Type: GrantFiled: October 16, 1986Date of Patent: June 14, 1988Assignee: L'OrealInventors: Gorges Rosenbaum, Jean Cotteret
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Patent number: 4670566Abstract: This invention relates to novel compounds having the formula: ##STR1## wherein; R.sup.1 is fluoro, chloro, bromo, lower-alkyl or nitro,R.sup.2 is lower alkyl, lower alkoxy, fluoro, chloro, bromo, nitro or trifluoromethyl, andm and n are 0-2 with the proviso that when R.sup.1 or R.sup.2 are tertiary butyl or a sterically hindering lower alkyl radical, m and/or n are 1. These compounds are intermediates in the preparation of 2-aminobiphenylacetic acids, esters and metal salts thereof.Type: GrantFiled: January 19, 1984Date of Patent: June 2, 1987Assignee: A. H. Robins Company, IncorporatedInventor: David A. Walsh
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Patent number: 4663453Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.Type: GrantFiled: August 28, 1985Date of Patent: May 5, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 4654360Abstract: Disclosed are compounds of the formula ##STR1## wherein the several groups are defined herein. These compounds are useful for treating inflammation.Type: GrantFiled: June 1, 1984Date of Patent: March 31, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Robert J. Greenhouse, Joseph M. Muchowski
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Patent number: 4636575Abstract: Compounds of formula II and X ##STR1## wherein X is O, S, SO.sub.2, methylene, isopropylidene or NCOR.sub.7 where R.sub.7 is alkyl or phenyl, Y is a direct bond or methylene, n is 1 or 2, R.sub.4 is alkyl, phenyl, naphthyl, cycloalkyl, aralkyl, camphoryl, CF.sub.3, CCl.sub.3, F or NH.sub.2 ; or is alkylene, phenylene or naphthylene, R.sub.5 is hydrogen or halogen, R.sub.6 is hydrogen, alkyl, phenyl or cyano, R.sub.8 is substituted phenyl, substituted naphthyl, anthryl or phenanthryl, R.sub.9 is alkyl R.sub.10 is alkyl or substituted phenyl, and R.sub.11 is alkyl, substituted phenyl, naphthyl, camphoryl, alkylene, phenylene or naphthylene, are latent curing catalysts for acid-curable stoving lacquers. They are distinguished by satisfactory solubility in the acid-curable resin systems, can be stored virtually indefinitely in the dark and, when exposed to shortwave light, make it possible to cure the resins by acid catalysts at a relatively low temperature.Type: GrantFiled: December 17, 1984Date of Patent: January 13, 1987Assignee: Ciba-Geigy CorporationInventor: Rudolf Kirchmayr
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Patent number: 4593106Abstract: 4-[2-(Dialkylamino)ethyl]-7-hydroxyisatins are prepared by internal condensation of an oxime followed by removal of protecting groups. The compounds are D.sub.2 -agonists and, thereby, have anti-hypertensive activity. A species of the group is 4-[2-(di-n-propylamino)ethyl]-4-hydroxyisatin.Type: GrantFiled: June 4, 1984Date of Patent: June 3, 1986Assignee: SmithKline Beckman CorporationInventors: Orum D. Stringer, Joseph Weinstock, James W. Wilson
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Patent number: 4581366Abstract: The invention concerns 1'-(4-bromo-2-fluorobenzyl)-7'-chloro-spiro[imidazolidine-4,3'-indoline]-2 ,2',5-trione in racemic or dextrorotatory form; pharmaceutical compositions thereof for use in the treatment or prophylaxis of certain complications of diabetes; and processes for its manufacture.Type: GrantFiled: March 19, 1984Date of Patent: April 8, 1986Assignee: Imperial Chemical Industries PLCInventors: David R. Brittain, Robin Wood
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Patent number: 4545806Abstract: Cyclohexane-1,3-dione derivatives of the formula ##STR1## where A is an unsubstituted or substituted, saturated or unsaturated 4-membered to 7-membered heterocyclic structure which contains from 1 to 3 nitrogen atoms and may be fused to an aromatic radical, R.sup.1 is hydrogen, methoxycarbonyl, ethoxycarbonyl, methyl or cyano, R.sup.2 is alkyl and R.sup.3 is alkyl, haloalkenyl or propargyl, and salts of these compounds, are useful for controlling undesirable plant growth.Type: GrantFiled: March 15, 1984Date of Patent: October 8, 1985Assignee: BASF AktiengesellschaftInventors: Dieter Jahn, Rainer Becker, Michael Keil, Wolfgang Spiegler, Bruno Wuerzer
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Patent number: 4539329Abstract: The invention concerns novel trifluoromethyl derivatives of 1'-halogenobenzyl-spiro[imidazolidine-4,3'-indoline]-2,2',5-trione (I), their pharmaceutically acceptable salts, and non-toxic, biodegradable precursors thereof. The derivatives are potent inhibitors of the enzyme aldose reductase and are useful in treating or preventing certain complications of diabetes. The invention also provides pharmaceutical compositions and processes for the manufacture of the derivatives.Type: GrantFiled: May 6, 1983Date of Patent: September 3, 1985Assignee: Imperial Chemical Industries, plcInventors: David R. Brittain, David Brown, Robin Wood
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Patent number: 4476132Abstract: Quinolinone derivatives of the formula (I) ##STR1## in which X represents oxy or a direct bond, R.sub.1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical or hydrogen, Ph represents an optionally additionally substituted 1,2-phenylene radical containing the group R.sub.1 --X--C(O)--, and one of the radicals R.sub.2 and R.sub.3 represents an optionally esterified or amidated carboxy group R.sub.4 and the other represents hydrogen or an aliphatic radical or, in the case of a radical R.sub.3, hydroxy, and in which either R.sub.A and R.sub.B together represent oxo, R.sub.C and R.sub.D together represent an additional bond, or, when R.sub.2 represents a radical R.sub.4, R.sub.C is hydrogen and R.sub.3 and R.sub.D together represent oxo, and R.sub.E represents a radical R.sub.5 which represents hydrogen or an aliphatic, cycloaliphatic, araliphatic heterocyclic-aliphatic radical, or R.sub.A represents an optionally etherified hydroxy group and R.sub.Type: GrantFiled: March 19, 1982Date of Patent: October 9, 1984Assignee: Ciba-Geigy CorporationInventors: Richard Goschke, Pier G. Ferrini, Alfred Sallmann
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Patent number: 4443614Abstract: A process is described for preparing triarylmethane derivatives of a high purity in an extremely high yield from 3-phenylphthalide derivatives and aniline derivatives or indole derivatives with Friedel-Crafts type catalyst or Friedel-Crafts type catalyst and an oxidizing agent.Type: GrantFiled: June 24, 1980Date of Patent: April 17, 1984Assignee: Kanzaki Paper Manufacturing Co., Ltd.Inventors: Mitsuru Kondo, Kiyoshi Yasui, Makoto Miyake, Hiroshi Iwasaki, Tetsuo Shiraishi
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Patent number: 4439610Abstract: A process is described for preparing triarylmethane derivatives of a high purity in an extremely high yield from 3-phenylphthalide derivatives and aniline derivatives or indole derivatives with Friedel-Crafts type catalyst or Friedel-Crafts type catalyst and an oxidizing agent.Type: GrantFiled: March 4, 1977Date of Patent: March 27, 1984Assignee: Kanzaki Paper Manufacturing Company, Ltd.Inventors: Mitsuru Kondo, Kiyoshi Yasui, Makoto Miyake, Hiroshi Iwasaki, Tetsuo Shiraishi
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Patent number: 4395559Abstract: 2,3-Indoledione derivatives of the formula ##STR1## wherein R is isopropyl or tert.butyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl or lower aralkyl, and their pharmaceutically acceptable acid addition salts, prepared from a compound of the formula ##STR2## wherein R.sup.3 is hydroxy and R.sup.4 is chlorine or bromine or R.sup.3 and R.sup.4, taken together, are oxygen, and R.sup.1 and R.sup.2 are as previously set forth, are described. The compounds of formula I and their pharmaceutically acceptable addition salts are useful as .beta.-adrenergic blocking agents and antihypertensive agents.Type: GrantFiled: December 1, 1980Date of Patent: July 26, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Graham A. Fothergill, John M. Osbond