Plural Rings Bonded Directly To The Same Carbon Patents (Class 562/441)
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Patent number: 5238958Abstract: The present invention is novel substituted .alpha.-amino acids, pharmaceutical compositions, methods of use, and preparations therefore having utility for treating disorders which benefit from blockade of aspartate and glutamate receptors.Type: GrantFiled: April 23, 1990Date of Patent: August 24, 1993Assignee: Warner-Lambert CompanyInventors: Graham Johnson, Thomas C. Malone, Perry M. Novak
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Patent number: 5202483Abstract: Ethylenically unsaturated compounds of the general formula I ##STR1## where R.sub.1 is alkyl of 1 to 4 carbon atoms, cyclopropyl, cyclopentyl, cyclohexyl, phenyl or phenyl in which some or all of the hydrogen atoms have been replaced by radicals R.sup.4, not more than two substituents R.sup.4 being identical, or R.sup.1 together with R.sup.2 or together with R.sup.6 forms a --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --CH.sub.2 -- bridge,R.sup.4 is alkyl of 1 to 24 carbon atoms, --OH, --O--R.sup.7, --S--R.sup.7, ##STR2## R.sup.2 or R.sup.6, independently of one another, both are hydrogen, or one of the radicals R.sup.4, or, where R.sup.1 is aryl,R.sup.2 or R.sup.6 is a direct bond to R.sup.1 in the ortho-position with respect to the carbonyl group, andR.sup.3 and R.sup.5 are each hydrogen, one of the radicals R.sup.4 or a group the general formula II ##STR3## where R.sup.7 and R.sup.8 are each alkyl of 1 to 4 carbon atoms,R.sup.9 is cycloalkyl of 5 or 6 carbon atoms,R.sup.Type: GrantFiled: March 1, 1991Date of Patent: April 13, 1993Assignee: BASF AktiengesellschaftInventors: Gerd Rehmer, Kaspar Bott
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Patent number: 5198548Abstract: A process for the preparation of D(-) and L(+)-3,3-diphenylalanine and D(-) and L(+)-substituted 3,3-diphenylalanines is described where N-protected DL-3,3-diphenylalanine or N-protected-DL-substituted 3,3-diphenylalanine are treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.Type: GrantFiled: January 30, 1992Date of Patent: March 30, 1993Assignee: Warner-Lambert CompanyInventors: Vladimir Beylin, Huai G. Chen, Om P. Goel, John G. Topliss
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Patent number: 5189181Abstract: A process for the preparation of a polycyclic dye of the Formula (1): ##STR1## by reacting a substituted acetic acid of the Formula (2): ##STR2## with a compound of the Formula (3): ##STR3## and oxidation of the intermediate leuco compound to dehydrogenate the peripheral heterocyclic rings whereinY is an optionally substituted aromatic or heteroaromatic radical;Ring A is unsubstituted or is substituted by from one to five groups;Z is --NR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently H or are independently selected from optionally substituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl and heteroaryl; orR.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring; orR.sup.1 and R.sup.2 each independently together with the nitrogen to which they are attached and the adjacent carbon atom of Ring B form a heterocyclic ring; andX.sup.1 and X.sup.Type: GrantFiled: January 7, 1992Date of Patent: February 23, 1993Assignee: Imperial Chemical Industries PLCInventors: Nigel Hall, Nigel Hughes, Prakash Patel
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Patent number: 5182301Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: February 21, 1991Date of Patent: January 26, 1993Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
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Patent number: 5149709Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.Type: GrantFiled: July 3, 1990Date of Patent: September 22, 1992Assignee: Schering CorporationInventors: John Clader, Sundeep Dugar, Timothy Kogan, Bradley Tait, Wayne Vaccaro
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Patent number: 5136081Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.Type: GrantFiled: September 11, 1989Date of Patent: August 4, 1992Assignee: Shell Internationale Research Maatschappij B.V.Inventor: Paul H. Briner
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Patent number: 5132312Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: November 27, 1990Date of Patent: July 21, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Kent E. Neuenschwander
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Patent number: 5124478Abstract: The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl, R.sup.2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R.sup.3 denotes hydrogen or (C.sub.1 -C.sub.4)-alkyl, and Y.sup.1 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy or --O--(CH.sub.2).sub.n --COOH (with n=1 to 6), with one of these radicals being --O--(CH.sub.2).sub.n --COOH, or Y.sup.1, Y.sup.2 and Y.sup.5 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-alkoxy, Y.sup.3 denotes hydrogen or (C.sub.1 -C.sub.8)-alkoxy and Y.sup.4 denotes --(CH.sub.2).sub.n --COOH or --NH--CO--(CH.sub.2).sub.n --COOH (with n=1 to 6).Type: GrantFiled: December 20, 1988Date of Patent: June 23, 1992Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breipohl, Jochen Knolle, Werner Stuber
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Patent number: 5118839Abstract: A process for preparing nitro substituted polyarylketones of the formula: ##STR1## is disclosed. The process involves the condensation of ##STR2## where R.sub.A is hydrogen, --COOH, or C.sup.1 to C.sub.12 linear or branched alkyl, Y and Y' are the same or different and are a chemical bond ##STR3## or --Si(CH.sub.3).sub.2 -- and m is 0 or 1 and X is halo. These nitro groups of these compounds can be reduced to provide the corresponding amines, which are useful for the preparation of thermally stable high melting polyimides.Type: GrantFiled: September 4, 1990Date of Patent: June 2, 1992Assignee: Ethyl CorporationInventors: Allan A. Eisenbraun, Venkataraman Ramachandran
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Patent number: 5110983Abstract: Compounds of the formula I ##STR1## can be prepared by various process steps from 2-(4-methylphenyl)-2-hexafluoroisopropanol.Hexafluoroisopropyl-containing monomers are important starting compounds in the preparation of linear polycarboxamides and polycarboximides.Type: GrantFiled: March 22, 1990Date of Patent: May 5, 1992Assignee: Hoechst AktiengesellschaftInventors: Jurgen Lau, Gunter Siegemund, Freimund Rohrscheid
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Patent number: 5093366Abstract: A cinnamoylamide derivative of general formula: ##STR1## [wherein, (i) in case that R.sup.2 represents a methyl group and R.sup.3 represents a hydrogen atom,(R.sup.1).sub.n represents a group selected out of3-pentyl group,4-pentyl group,4-neopentyl group,4-(2-ethylbutyl) group,4-(2-methylpentyl) group,2-fluoro-4-pentyloxy group,4-butylthio group,4-cyclobutylmethyl group,4-cyclohexylmethyl group,4-(4-phenylbutyl) group and4-phenoxy group, and(ii) in case that R.sup.2 represents a hydrogen atom and R.sup.3 represents a methyl group,(R.sup.1).sub.n represents a group selected out of3-pentyl group and4-penethyl group.]or non-toxic salts thereof possess an inhibitory activity on 5.alpha.-reductase, and therefore be useful for treating and/or preventing agent for alopecia, acnes or prostatic hyperfrophy.Type: GrantFiled: April 25, 1991Date of Patent: March 3, 1992Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
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Patent number: 5051526Abstract: Novel benzhydrylamine derivatives represented by general formulas (I) and (II) are useful as reaction reagents for the solid-phase synthesis of polypeptide amides making use of 9-fluorenylmethyloxycarbonyl group ("Fmoc"). An intermediate for these derivatives represented by the general formula (III) is also disclosed: ##STR1## where R.sub.1 and R.sub.2 each independently represents a C.sub.1-3 lower alkyl; n is an integer of 1-4; l is 1 or 2; and m is 1 or 2.Type: GrantFiled: May 24, 1990Date of Patent: September 24, 1991Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Susumu Funakoshi, Eigoro Murayama
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Patent number: 5047420Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.Type: GrantFiled: August 21, 1989Date of Patent: September 10, 1991Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
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Patent number: 5017710Abstract: Fluoran compounds represented by the general formula (I) ##STR1## (where R is an alkyl group having 9 to 12 carbon atoms) and coloring recording materials containing the said compounds as coloring components, and benzoic acid derivatives represented by the general formula (II) ##STR2## (where R is an alkyl group having 9 to 12 carbon atoms).Type: GrantFiled: October 24, 1989Date of Patent: May 21, 1991Assignee: Nippon Soda Co., Ltd.Inventors: Tetsuo Igaki, Akio Kaneko, Sumio Manaka, Kimiaki Kinoshita
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Patent number: 5013757Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and X is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active component the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.Type: GrantFiled: April 13, 1990Date of Patent: May 7, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
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Patent number: 4992576Abstract: This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.Type: GrantFiled: March 27, 1990Date of Patent: February 12, 1991Assignee: Eli Lilly and CompanyInventor: D. Mark Gapinski
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Patent number: 4988730Abstract: The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group;orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.Type: GrantFiled: July 21, 1989Date of Patent: January 29, 1991Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyar RTInventors: Dezso Korbonits, Pal Kiss, Laszlo Szekeres, Gyula Papp, Gabor Kovacs, Andrea Santane Csutor, Sandor Virag, Eva Udvari, Imre Bata, Katalin Marmarosi nee Kellner, Laszlo Tardos, Peter Kormoczy, Vera Gergely, Zoltan Vargai
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Patent number: 4965405Abstract: Novel benzhydrylamine derivatives represented by general formulas (I) and (II) are useful as reaction reagents for the solid-phase synthesis of polypeptide amides making use of 9-fluorenylmethyloxycarbonyl group ("Fmoc"). An intermediate for these derivatives represented by the general formula (III) is also disclosed: ##STR1## where R.sub.1 and R.sub.2 each independently represents a C.sub.1 -C.sub.3 lower alkyl; n is an integer of 1-4; l is 1 or 2; and m is 1 or 2.Type: GrantFiled: February 27, 1989Date of Patent: October 23, 1990Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Susumu Funakoshi, Eigoro Murayama
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Patent number: 4962230Abstract: A process for producing an optically active carboxylic acid represented by formula (I): ##STR1## wherein R.sup.1, and R.sup.2, and R.sup.3 each represents a hydrogen atom, an alkyl group, an alkenyl group, or a phenyl or naphthyl group which may have a substituent, provided that all of R.sup.1, R.sup.2, and R.sup.3 are not simultaneously a hydrogen atom; when R.sup.1 and R.sup.2 are simultaneously a hydrogen atom, then R.sup.3 is not a methyl group; and that when R.sup.3 is a hydrogen atom, then R.sup.1 and R.sup.2 are each a group other then a hydrogen atom,is disclosed, comprising asymmetrically hydrogenating an .alpha.,.beta.-unsaturated carboxylic acid represented by formula (II): ##STR2## wherein R.sup.1, R.sup.2, and R.sup.3 are the same as defined above, in the presence of a ruthenium-optically active phosphine complex as a catalyst.Type: GrantFiled: November 16, 1987Date of Patent: October 9, 1990Assignee: Takasago International CorporationInventors: Hidemasa Takaya, Tetsuo Ohta, Ryoji Noyori, Noboru Sayo, Hidenori Kumobayashi, Susumu Akutagawa
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Patent number: 4935543Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is optionally esterified or amidated carboxyl; R.sub.2, R.sub.3 and R.sub.4 are the same or different and are hydrogen or halogen or alkyl; A is formyl, hydroxyiminomethyl or carboxyl; and A is hydrogen or halogen, or a salt thereof, which is useful as an aromatase inhibitor or an intermediate of its production. Processes for producing the compound of the formula (I) and an aromatase inhibitor containing as an active compound the compound of the formula (I) wherein A is formyl and X is hydrogen or, a salt thereof as well as Penicillium funiculosum capable for producing the compound (I) wherein R.sub.1 is carboxyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen and X is formyl are also disclosed.Type: GrantFiled: May 18, 1989Date of Patent: June 19, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
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Patent number: 4925958Abstract: The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which R.sup.1 denotes (substituted) aryl or (substituted) cyclohexyl and R.sup.2 =alkyl, in which a compound of the formula R.sup.1 --NH.sub.2 is reacted with at least twice the molar amount of glyoxylic acid in the presence of water and the resulting acid is then esterified.Type: GrantFiled: June 16, 1988Date of Patent: May 15, 1990Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Rudolf Kunstmann
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Patent number: 4923888Abstract: The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 acylamino group;R.sub.1 means hydrogen or a carboxyl-protective group; andR.sub.2 represents a --(CH.sub.2).sub.n --CO.sub.2 R.sub.5 group, whereinn is 1, 2, 3 or 4; andR.sub.5 stands for hydrogen or a carboxyl-protective group; orR.sub.2 means a --(CH.sub.2).sub.n --NH.sub.2 group, whereinn is 1, 2, 3 or 4of E and/or Z configurtion as well as their salts.The compounds according to the invention show a cytoprotective effect and promote the healing of the stomach ulcer. Their toxicity is low.Type: GrantFiled: September 26, 1988Date of Patent: May 8, 1990Assignee: Richter Gedeon Vegyeszeti Gyar RTInventors: Tamas Fodor, Laaszlo Dobay, Jaanos Fischer, Bela Stefkoo, Elemeer Ezer, Judit Matuz, Katalin Saghy, Laaszlo Szporny
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Patent number: 4898941Abstract: A process for preparing a diphenylalkene derivative of the formula [II] ##STR1## which comprises oxidizing a diphenylalkanoic acid derivative of the formula [I] ##STR2## wherein R.sub.1 and R.sub.2 are each substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or substituted or unsubstituted aryl, R.sub.1 and R.sub.2 may form a heteroring together theirwith or with an adjacent benzene ring, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are each hydrogen atom, halogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyl or substituted or unsubstituted amino, R.sub.12 and R.sub.13 are each hydrogen atom or substituted or unsubstituted alkyl, X is carboxyl, amide, ester or halide thereof.Type: GrantFiled: August 11, 1987Date of Patent: February 6, 1990Assignee: Kanzaki Paper Manufacturing Co., Ltd.Inventors: Nobuo Kanda, Haruo Omura, Yukihiro Abe, Mitsuru Kondo
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Patent number: 4889947Abstract: Sunscreen compositions are described which contain certain substituted naphthalenylidenes which act as UV filters when incorporated in a carrier in amounts ranging from 0.1-50% by weight.Type: GrantFiled: July 28, 1988Date of Patent: December 26, 1989Assignee: ICI Americas Inc.Inventors: Charalambos J. Phalangas, Thomas P. Cleary
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Patent number: 4883815Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.Type: GrantFiled: July 5, 1988Date of Patent: November 28, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
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Patent number: 4845245Abstract: Disclosed herein is a process for producing 3,3-bis-(4-dimethylaminophenyl)-6-dimethylaminophthalide, which process comprises oxidizing 2-[4,4'-bis-(dimethylamino)-benzhydryl]-5-dimethylaminobenzoic acid in an aqueous solution of a mineral acid of pH of from 2.0 to 4.0 with air, oxygen or a gas containing oxygen in the presence of at least one catalyst selected from the group consisting of compounds of iron, copper, cobalt, nickel, chromium, vanadium and manganese.Type: GrantFiled: July 23, 1987Date of Patent: July 4, 1989Assignee: Yamada Chemical Co., Ltd.Inventors: Yoshiharu Fujino, Hajime Kawai, Katsuhiko Tsunemitsu
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Patent number: 4826876Abstract: This invention relates to chemical compounds which have selective thyromimetic activity. A compound of this invention is 3,5-dibromo-3'-[6-oxo-3(1H)-pyridazinyl-methyl]-thyronine.Type: GrantFiled: December 21, 1987Date of Patent: May 2, 1989Assignee: Smith Kline & French Laboratories LimitedInventors: David Ellis, John C. Emmett, Anthony H. Underwood, Paul D. Leeson
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Patent number: 4808732Abstract: Amino-tetraalkylbenzoylphthalic acids are intermediates for preparing homopolyimides and copolyimides which contain structural elements of the formula I ##STR1## in which R.sup.1 and R.sup.2 are halogen, nitro, aryl, aryloxy, alkyl or alkoxy, m is 0 or a number from 1 to 4, n is 0 or a number from 1 to 3 and p is 0, 1 or 2, the free carbonyl groups are bonded in the ortho-position relative to one another and R is a divalent aromatic radical which is substituted by at least one alkyl group or aralkyl group, are autophotocrosslinkable. They are suitable for the production of protective films and photographic relief images.Type: GrantFiled: October 28, 1987Date of Patent: February 28, 1989Assignee: Ciba-Geigy CorporationInventor: Josef Pfeifer
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Patent number: 4801722Abstract: There are described stable fluorescent labels comprising a complex of lanthanide metal and a chelating agent comprising a nucleus which is a triplet sensitizer having a triplet energy greater than that of said lanthanide metal and at least two heteroatom-containing groups which form coordinate complexes with lanthanide metals and a third heteroatom-containing group or heteratom in or appended to the triplet sensitizer. Labeled physiologically active materials useful in specific binding assays such as labeled antigens, heptens, antibodies, hormones and the like comprising the stable fluorescent labels having physiologically active materials adsorbed or bonded thereto are also described.Type: GrantFiled: January 27, 1987Date of Patent: January 31, 1989Assignee: Eastman Kodak CompanyInventors: Jerald C. Hinshaw, John L. Toner, George A. Reynolds
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Patent number: 4762881Abstract: Provided is a benzoylphenylalanine of the formula: ##STR1## wherein ##STR2## is in the m or p position; and Pr is a protecting group which is easily cleavable in the presence of a peptide bond by a mild acid or base.This benzoylphenylalanine group is incorporated into a peptide chain which can be attached to a solid substrate having a reactive hydrogen by exposure to low energy ultraviolet light.Type: GrantFiled: January 9, 1987Date of Patent: August 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: James C. Kauer
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Patent number: 4670572Abstract: There are described stable fluorescent labels comprising a complex of lanthanide metal and a chelating agent comprising a nucleus which is a triplet sensitizer having a triplet energy greater than that of said lanthanide metal and at least two heteroatom-containing groups which form coordinate complexes with lanthanide metals and a third heteroatom-containing group or heteratom in or appended to the triplet sensitizer. Labeled physiologically active materials useful in specific binding assays such as labeled antigens, heptens, antibodies, hormones and the like comprising the stable fluorescent labels having physiologically active materials adsorbed or bonded thereto are also described.Type: GrantFiled: February 3, 1986Date of Patent: June 2, 1987Assignee: Eastman Kodak CompanyInventors: Jerald C. Hinshaw, John L. Toner, George A. Reynolds
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Patent number: 4603145Abstract: This disclosure describes novel diaryl-alkanamides. These compounds are useful as pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial wall of mammals.Type: GrantFiled: May 6, 1983Date of Patent: July 29, 1986Assignee: American Cyanamid CompanyInventors: Vern G. DeVries, Robert G. Shepherd, Janis Upeslacis
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Patent number: 4602023Abstract: The present invention provides various novel diphenic acid monoamide compounds, novel pharmaceutical compositions and methods of use thereof, as well as novel methods of synthesis therefor. The novel diphenic acid monoamides of the present invention are leukotriene antagonists, 5-lipoxygenase inhibitors, and mediator release inhibitors providing activity useful for treating asthma, allergies, cardiovascular diseases, migraines, and immunoinflammatory conditions.Type: GrantFiled: June 3, 1985Date of Patent: July 22, 1986Assignee: Warner-Lambert CompanyInventors: John S. Kiely, Suchin Huang
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Patent number: 4568695Abstract: Novel 2-amino-3-benzoylphenethylalcohols are provided having the formula: ##STR1## wherein; X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andY is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, --S--loweralkyl, ##STR2## The compounds exhibit anti-inflammatory activity.Type: GrantFiled: December 7, 1983Date of Patent: February 4, 1986Assignee: A. H. Robins Company, IncorporatedInventors: Henry W. Moran, William J. Welstead, Jr.
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Patent number: 4564685Abstract: This disclosure describes compounds of Formula I. ##STR1## (including their pharmaceutically acceptable salts and esters) which have potent antihistamine activity which are substantially free from sedative effects.Type: GrantFiled: March 10, 1983Date of Patent: January 14, 1986Inventors: John W. A. Findlay, Geoffrey G. Coker
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Patent number: 4528397Abstract: An aminocarboxylic acid derivative represented by the formula ##STR1## wherein R.sub.1 and R.sub.2, independently from each other, represent a hydrogen atom or an alkyl group which may have a substituent, and Y represents --NH-- or --S--, provided that when Y represents --NH--, at least one of R.sub.1 and R.sub.2 represents an alkyl group which may have a substituent. These compounds have excellent inhibitory activity on dipeptidase in animals, and are useful for administration in combination with carbapenem antibiotics.Type: GrantFiled: March 29, 1983Date of Patent: July 9, 1985Assignee: Sanraku-Ocean Co., Ltd.Inventors: Norio Shibamoto, Takeo Yoshioka, Yasuo Fukagawa, Tomoyuki Ishikura
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Patent number: 4507497Abstract: Michler's ketone analogs and salts thereof, which are photosensitizers in water-soluble photoinitiator systems used to induce polymerization in free-radically-curable, ethylenically-unsaturated materials, are disclosed. The Michler's ketone analogs have the formula: ##STR1## wherein each R is an alkyl group of 1 to 8 carbon atoms,R.sup.1 is an alkylene group having 1 to 8 carbon atoms,Z is R.sup.1 COOH or R.sup.1 H, andn is an integer having a value of 1 or 2.The photoinitiator systems are useful in imaging systems.Type: GrantFiled: March 3, 1983Date of Patent: March 26, 1985Assignee: Minnesota Mining and Manufacturing CompanyInventor: Laurence W. Reilly, Jr.
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Patent number: 4489094Abstract: This disclosure describes novel [Bis(phenyl or substituted phenyl)alkyl]amino benzoic acids, esters, and derivatives thereof. These compounds are useful pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial walls of mammals.Type: GrantFiled: May 6, 1983Date of Patent: December 18, 1984Assignee: American Cyanamid CompanyInventors: Robert G. Shepherd, Janis Upeslacis
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Patent number: 4451669Abstract: Novel compositions comprising acetylenic polyhemi-amic acid compositions and processes for their preparation are disclosed herein. These new compositions are primarily derivatives of anhydride-terminated aromatic polyimides from which they are prepared by amidation to provide acetylenic amide groups having terminal --C.tbd.CH groups as hemi-amic acid groups or their derivatives. These new compositions are more tractable than the original anhydride-terminated polyimides and can be converted at appropriate lower temperatures to crosslinked, insoluble, infusible polymers without by-product formation thereby extending greatly the applications for which the aromatic polyimides can be employed. Also included are monomeric compounds containing acetylenic amide groups derived from monomeric tetracarboxylic dianhydrides. These are particularly useful as crosslinking agents.Type: GrantFiled: November 16, 1981Date of Patent: May 29, 1984Assignee: Plastics Engineering CompanyInventors: Gaetano F. D'Alelio, Phillip A. Waitkus
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Patent number: 4431840Abstract: Substituted 2-benzoylbenzoic acids, useful as intermediates for preparing valuable chromogenic phthalide compounds, are prepared by reacting certain substituted 3,3-diphenylphthalides with a lower alkanoic acid and water.Type: GrantFiled: October 22, 1982Date of Patent: February 14, 1984Assignee: Sterling Drug Inc.Inventors: Gordon J. Sterken, Ramamurthi Kannan, James E. Kassner
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Patent number: 4409213Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: November 10, 1982Date of Patent: October 11, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton, Christopher J. Wallis
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Patent number: 4407823Abstract: Phenylacetic acid derivatives of the formula ##STR1## wherein n is an integer of 2 to 5; ##STR2## R.sub.1 is hydrogen, halogen, trifluoromethyl, nitro or amino; R.sub.2 and R.sub.3 each independently is hydrogen or lower alkyl; or together form an ethylene group;X.sub.1 represents two hydrogen atoms or an oxo group; andY.sub.1 is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl or carboxyl;and for derivatives wherein Y is carboxyl, salts thereof with physiologically compatible bases, esters thereof from physiologically acceptable alcohols and amides thereof from physiologically acceptable amines have valuable pharmacological activity, e.g., as antiinflammatory agents.Type: GrantFiled: November 5, 1979Date of Patent: October 4, 1983Assignee: Schering AktiengesellschaftInventors: Gerald Kirsch, Joachim-Friedrich Kapp, Clemens Rufer
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Patent number: 4405358Abstract: Aralkylaniline derivatives of the general formula ##STR1## where R is alkoxy, cycloalkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, haloalkoxy, alkylthio, alkenylthio or alkynylthio or unsubstituted or substituted alkyl, cycloalkyl, alkenyl or alkynyl, Y is hydrogen, alkyl, halogen, alkoxy or haloalkyl, A is unsubstituted or substituted alkylene, Z is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, a C.sub.4 H.sub.4 -chain which is fused to the benzene radical to form an unsubstituted or substituted naphthyl radical, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, ##STR2## R' and R" each, independently of one another, being hydrogen, alkyl, alkoxy, alkylthio, cycloalkyl or unsubstituted or substituted phenyl, and n is an integer from 1 to 4, and herbicides containing these compounds.Type: GrantFiled: May 1, 1981Date of Patent: September 20, 1983Assignee: BASF AktiengesellschaftInventors: Ulrich Schirmer, Wolfgang Rohr, Bruno Wuerzer
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Patent number: 4402975Abstract: A compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, an acyl group or an alkoxycarbonyl group; X.sup.1 represents an alkylene group having 3 to 6 carbon atoms, a 1,4-cyclohexylene group, or a 1,4-phenylene group, the alkylene group may be substituted by an alkyl group having 1 to 6 carbon atoms, and the 1,4-phenylene group may be substituted by 1 or 2 substituents selected from halogen atoms and alkoxy groups having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom or a hydroxyl group and R.sup.3 represents hydrogen atom, or R.sup.2 and R.sup.3 together may form an oxo group (.dbd.O), and when X.sup.1 is other than the 1,4-phenylene group, R.sup.2 represents a hydrogen atom and R.sup.3 represents a bond between the carbon atoms to which R.sup.3 is bonded and that carbon atom of X.sup.1 which is adjacent to said carbon atom; X.sup.Type: GrantFiled: July 17, 1981Date of Patent: September 6, 1983Assignee: Teijin LimitedInventors: Toru Takeshita, Kenji Hoshina, Akira Ohtsu, Tatsuyuki Naruchi
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Patent number: 4399291Abstract: Process comprises the combination of the two steps of condensing Y-benzaldehyde with N--R.sup.2 --N--R.sup.3 -aniline and 3--N--R--N--R.sup.1 -benzoic acid, under acidic conditions to produce 2-[(Y-phenyl) (4--N--R.sup.2 --N--R.sup.3 -aminophenyl)methyl]-5--N--R--N--R.sup.1 -aminobenzoic acid, and oxidizing said benzoic acid to produce 3-(Y-phenyl)-3-(4--N--R.sup.2 --N--R.sup.3 -aminophenyl)-6--N--R--N--R.sup.1 -aminophthalide.Type: GrantFiled: December 9, 1981Date of Patent: August 16, 1983Assignee: Sterling Drug Inc.Inventors: Paul J. Schmidt, Patrick J. Jefferies
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Patent number: 4390714Abstract: Tertiary aromatic amines derived from aminoglutethimide or para-aminophenylacetic acid act as accelerators for the peroxide catalyzed polymerization of acrylic resins, especially methacrylates, acrylates and unsaturated polyesters. The amines are characterized by good hardening, strength, color and toxicity characteristics, and are thereby particularly suited for use in the filling and restoration of human teeth and the cementing of bone.Type: GrantFiled: July 7, 1980Date of Patent: June 28, 1983Assignee: American Dental Association Health FoundationInventor: Harold Argentar
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Patent number: 4389416Abstract: Described are compounds of the formula ##STR1## wherein R is hydrogen, loweralkyl, aminomethyl or halo; R.sub.1 is carboxy, carboxyloweralkyl, aminocarbonyl, hydroxymethyl, anilinomethyl, or aminomethyl; A is oxygen, CH.sub.2, Sulfur or a single bond; X is oxygen, CH.sub.2, sulfur or sulfoxide; and Y is hydrogen, loweralkyl or halo and may be the same or different, and pharmaceutically acceptable salts thereof.The compounds are effective as diuretic agents.Type: GrantFiled: October 9, 1981Date of Patent: June 21, 1983Assignee: Abbott LaboratoriesInventor: Jacob J. Plattner
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Patent number: 4378373Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.Type: GrantFiled: April 20, 1981Date of Patent: March 29, 1983Assignee: Alfa Farmaceutici S.p.A.Inventors: Valerio Borzatta, Manlio Cristofori, Mauro Morotti, Giuseppe Mascellani
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Patent number: 4377536Abstract: Novel compositions comprising unsaturated polyhemi-amic acid compositions and processes for their preparation are disclosed herein. These new compositions are primarily derivatives of anhydride-terminated aromatic polyimides from which they are prepared by amidation to provide unsaturated amide groups having terminal --CH.dbd.CH.sub.2 groups as hemi-amic acid groups or their derivatives. These new compositions are more tractable than the original anhydride-terminated polyimides and can be converted at appropriate lower temperatures to crosslinked, insoluble, infusible polymers without by-product formation thereby extending greatly the applications for which the aromatic polyimides can be employed. Also included are monomeric compounds containing unsaturated amide groups derived from monomeric tetracarboxylic dianhydrides. These are particularly useful as crosslinking agents.Type: GrantFiled: November 16, 1981Date of Patent: March 22, 1983Assignee: Plastics Engineering CompanyInventors: Phillip A. Waitkus, Gaetano F. D'Alelio