Nitrogen Double Bonded Directly To Carbon (e.g., Amidine, Ketimine, Etc.) Patents (Class 562/440)
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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Patent number: 5498755Abstract: Compounds of the formula ##STR1## wherein the R.sub.1 groups independently are hydrogen, lower alkyl, or two geminal R.sub.1 groups jointly represent an oxo (.dbd.O) or a thio (.dbd.S) group; R.sub.2 is hydrogen or lower alkyl, or halogen; M is or --N.dbd.CR.sub.4 -- or --R.sub.4 C.dbd.N-- where R.sub.4 is hydrogen or lower alkyl; X is C(R.sub.1).sub.2 ; Y is phenyl optionally substituted with an R.sub.3 group which is lower alkyl or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl, cycloalkyl, alkenyl, alkynyl; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.Type: GrantFiled: August 23, 1994Date of Patent: March 12, 1996Inventors: Roshantha A. Chandraratna, Min Teng
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Patent number: 5495043Abstract: Novel compounds which are 2,6-di-t-butylphenols substituted on the 4 position by an anilino group, which anilino group is substituted by a carboxyl substituent, a tetrazolyl substituent or an N-methyltetrazolyl substituent, are useful antiallergic agents. Pharmaceutical compositions containing and pharmacological methods of using such compounds are also disclosed, as are synthetic intermediates for preparing such compounds. Certain of the synthetic intermediates also exhibit useful antiallergic activity.Type: GrantFiled: May 5, 1995Date of Patent: February 27, 1996Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
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Patent number: 5480998Abstract: An oxime derivative (I): ##STR1## that D ring and B bonding to D ring are (i)-(iv), wherein R.sup.1 is hydrogen, lower alkyl; R.sup.2 is hydrogen, alkyl, phenyl, cycloalkyl, monocyclic ring containing nitrogen, lower alkyl substituted by benzene ring or cycloalkyl, lower alkyl substituted by monocyclic ring containing nitrogen; R.sup.3 is alkyl, phenyl, cycloalkyl, monocyclic ring containing nitrogen, lower alkyl substituted by benzene ring or cycloalkyl, lower alkyl substituted by monocyclic ring containing nitrogen; e is 3-5, f is 1-3, p is 1-4, q is 1-2, r is 1-3; the position of the bond to D ring in (iii) and (iv) is a or b, and the ring in R.sup.2 and R.sup.3 may be substituted by lower alkyl, alkoxy, halogen, nitro, trihalomethyl; and salts thereof, possess an agonistic activity on PGl2 receptor, and therefore are useful for prevention and/or treatment of thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertension.Type: GrantFiled: March 17, 1994Date of Patent: January 2, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5480999Abstract: The invention relates to compounds of the general formula AB, which may be a salt or an amide, wherein:A represents a cyclooxygenase inhibitor having an accessible acidic function andB represents the L-form of arginine analogues of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent various substituents, process for the preparation of such compounds and pharmaceutical composition thereof.Type: GrantFiled: December 23, 1992Date of Patent: January 2, 1996Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre-Etienne Chabrier De Lassauniere, Pierre Braquet, Colette Broquet, Serge Auvin
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Patent number: 5481021Abstract: This invention relates to phenyl amidine derivatives having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.Type: GrantFiled: December 22, 1994Date of Patent: January 2, 1996Assignee: G. D. Searle & Co.Inventors: Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki, Lori A. Schretzman
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Patent number: 5455274Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(=NOH)-NH.sub.2 group may be in tautomeric form, and pharmaceutically acceptable salts thereof, in which:R.sub.1 is amino or amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen;R.sub.2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical or hydroxy; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol, araliphatic alcohol, or aromatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy;X.sub.1 and X.sub.Type: GrantFiled: December 9, 1992Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventor: Hongsuk Suh
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Patent number: 5453440Abstract: This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.Type: GrantFiled: October 15, 1993Date of Patent: September 26, 1995Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Robert B. Garland, Masateru Miyano, Joseph G. Rico, Thomas E. Rogers, Jeffery A. Zablocki
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Patent number: 5449809Abstract: Acetylene derivatives of the general formula I ##STR1## where U, V and W are hydrogen, halogen, nitro, cyano, alkyl or alkoxy,A is alkylidene, alkoxymethylidene, alkylthiomethylidene or alkoximino,B is OH, alkoxy or alkylamino andR is hydrogen, halogen, cyano, CF.sub.3, alkyl, cycloalkyl, haloalkyl, aryl, alkenyl, alkynyl, heterocyclyl, hetaryl, arylalkyl, arylalkenyl, arylethynyl, hetaryl-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, aryloxyalkyl, hetaryloxyalkyl, arylamino-alkyl, arylthiomethyl, hetarylthiomethyl, C(O)R.sup.1, C(O)NR.sup.2 R.sup.3, C(S)NR.sup.4 R.sup.5, C(O)SR.sup.6, C(S)OR.sup.7, C(S)SR.sup.8, CH(OH)R.sup.9, CH(OR.sup.10)R.sup.11, SiR.sup.12 R.sup.13 R.sup.14, SnR.sup.15 R.sup.16 R.sup.17, C(OR)R.sup.18 or C(.dbd.N--OR.sup.19)R.sup.20 andR.sup.1 -R.sup.17, R.sup.19 and R.sup.20 are hydrogen, alkyl, aryl, hetaryl, arylalkyl or hetarylalkyl and R.sup.18 is OH, C.sub.1 -C.sub.4 -alkoxy or aryl-C.sub.1 -C.sub.4 -alkoxy, and fungicides containing these compounds.Type: GrantFiled: July 30, 1993Date of Patent: September 12, 1995Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Beate Hellendahl, Reinhard Kirstgen, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5424334Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions--of such phenyl amidines derivatives.Type: GrantFiled: December 19, 1991Date of Patent: June 13, 1995Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Robert B. Garland, Masateru Miyano
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Patent number: 5410056Abstract: The present invention is directed to a novel process for the production of folic acid in high yield utilizing a novel diimine as an intermediate. This diimine is formed by reacting 2-substituted malondialdehyde with p-aminobenzoyl-L-glutamic acid. This diimine may be converted into folic acid by reacting said diimine with triaminopyrimidinone in the presence of sulphite.Type: GrantFiled: January 6, 1994Date of Patent: April 25, 1995Assignee: Hoffman-La Roche Inc.Inventor: Christof Wehrli
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Patent number: 5393920Abstract: A process for preparing an o-iminooxymethylbenozic acid of the general formula I ##STR1## comprises reacting an oxime of the general formula II ##STR2## with a lactone of the general formula III ##STR3## if appropriate in the presence of a base or of a diluent, and o-iminooxymethylbenzoic acids of the abovementioned formula.Type: GrantFiled: April 2, 1993Date of Patent: February 28, 1995Assignee: BASF AktiengesellschaftInventors: Remy Benoit, Hubert Sauter
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Patent number: 5393921Abstract: A process for synthesizing O-substituted oxime compounds, which includes (a) reacting an alkali metal or alkaline earth metal hydroxide compound and a solution of an oxime compound to form a first mixture including the alkali metal or alkaline earth metal salt of the oxime compound and water; and (b) adding an organohalide compound while stirring to the first mixture to form a second mixture including an O-substituted oxime compound, the alkali metal or alkaline earth metal salt of the oxime compound, water, unreacted organohalide compound and excess oxime compound. The second mixture is heated in the presence of an amount of water sufficient to react hydroxide with the unreacted organohalide compound to obtain an O-substituted oxime compound substantially free of unreacted organohalide compound.In a further embodiment, the O-substituted oxime compound can be hydrolyzed to the corresponding O-substituted hydroxylamine.Type: GrantFiled: July 7, 1993Date of Patent: February 28, 1995Assignee: The Gillette CompanyInventor: Harvey A. Lazar
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Patent number: 5358956Abstract: Novel fibrinogen receptor antagonists of the formula: ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.Type: GrantFiled: October 14, 1992Date of Patent: October 25, 1994Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko
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Patent number: 5344957Abstract: Novel substituted .beta. amino acid derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.Type: GrantFiled: October 6, 1992Date of Patent: September 6, 1994Assignees: G.D. Searle & Co., Monsanto CompanyInventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
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Patent number: 5319122Abstract: This invention relates to a novel process for preparing benzylformimidates which are useful in the production of certain carbapenem antibiotics. The process of this invention provides a means of producing a high-yield, high-purity product.Type: GrantFiled: November 12, 1992Date of Patent: June 7, 1994Assignee: Merck & Co., Inc.Inventor: Joel J. Friedman
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Patent number: 5312826Abstract: Disclosed are a dicarboxylic acid compound represented by the formula (I): ##STR1## wherein R represents hydrogen atom, a lower alkyl group, phenyl group or hydroxyl group; R.sup.1 represents a straight or branched alkyl group having 1 to 10 carbon atoms or a lower alkyl group substituted by a group selected from aryl group, a sulfur- or nitrogen-containing heterocyclic monocyclic group and a cycloalkyl group having 4 to 8 carbon atoms; R.sup.2 represents a substituted or unsubstituted aryl group, a cycloalkyl group having 4 to 8 carbon atoms or a sulfur-containing or nitrogen-containing heterocylcic group; X represents sulfur atom, oxygen atom or a substituted or unsubstituted imino group; Y.sup.1 represents imino group, oxygen atom or sulfur atom and Y.sup.2 represents nitrogen atom, or Y.sup.1 represents a vinylene group and Y.sup.2 represents a group: --CH.dbd.Type: GrantFiled: June 19, 1992Date of Patent: May 17, 1994Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Ken-ichi Nunami, Tameo Iwasaki, Kazuo Matsumoto, Koji Yano, Isao Yamaguchi
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Patent number: 5310620Abstract: Novel nitrone compounds of the following formula are provided ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 may be the same or different and represent an alkyl group, an aryl group or a hydrogen atom, R.sup.4 to R.sup.8 may be the same or different and represent an alkyl group, a hydrogen atom or a carboxyl group provided that at least one of R.sup.4 to R.sup.8 is a carboxyl group, X represents an alkoxy group of the formula, R.sup.9 O--, wherein R.sup.9 represents an alkyl group, a dialkylamino group of the formula, R.sup.10 R.sup.11 N--, wherein R.sup.10 and R.sup.11 may be the same or different and represent an alkyl group, or a hydrogen atom, and n is a value of 0, 1 or 2. A contrast enhanced material comprising the nitrone compound is also provided, which is able to enhance a contrast when exposed to light having a wavelength of 300 to 450 nm.Type: GrantFiled: November 5, 1992Date of Patent: May 10, 1994Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Satoshi Watanabe, Toshinobu Ishihara, Ken'Ichi Itoh
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Patent number: 5302739Abstract: Compounds of the formula ##STR1## as intermediates for the preparation of pyrimidine or triazine herbicides.Type: GrantFiled: October 29, 1992Date of Patent: April 12, 1994Assignees: Kumiai Chemical Industry Co., Ihara Chemical Industry Co., Ltd.Inventors: Masatoshi Tamaru, Norihiro Kawamura, Masahiro Sato, Fumiaki Takabe, Shigehiko Tachikawa, Ryo Yoshida
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Patent number: 5298527Abstract: .alpha.-Phenylacrylic acid derivatives I ##STR1## n=0 to 4; y=a;R.sup.1 =H; alkyl; alkenyl; alkynyl; substituted or unsubstituted cycloalkyl; vinyl or ethynyl when W is a direct bond;R.sup.2 =CN; alkenyl; alkynyl; substituted or unsubstituted cycloalkyl; substituted or unsubstituted alkyl;R.sup.3 =H; NO.sub.2 ; CN; halogen; alkyl; alkoxy; haloalkyl; haloalkoxy; alkylthio;or when n is 2, 3 or 4, two adjacent substituents R.sup.3 together form substituted or unsubstituted 1,3-butadien-1,4-diyl;R.sup.4 is phenyl which carries a radical --CR.sup.7 .dbd.NO--R.sup.8 and which may further carry one or two radicals;W=direct bond; oxygen; sulfur; substituted or unsubstituted nitrogen;and A can be an oxygen or sulfur radical.Type: GrantFiled: August 9, 1993Date of Patent: March 29, 1994Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Reinharad Kirstgen, Klaus Oberdorf, Hubert Sauter, Franz Roehl, Rainer Otter, Eberhard Ammermann, Gisela Lorenz, Uwe Kardorff, Christoph Kuenast
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Patent number: 5258398Abstract: This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease and disseminated intravascular coagulation, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.Type: GrantFiled: December 16, 1991Date of Patent: November 2, 1993Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Scott I. Klein, Bruce F. Molino
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Patent number: 5256812Abstract: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.Type: GrantFiled: September 6, 1991Date of Patent: October 26, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
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Patent number: 5254717Abstract: Compound of the formula I ##STR1## where R is hydrogen or alkyl,R.sup.1 is hydrogen, alkyl, haloalkyl or aryl,Z.sup.1 and Z.sup.2 are hydrogen, halogen, alkoxy, alkenyloxy, cyano, nitro, haloalkyl, haloalkenyloxy, alkenyl, haloalkoxy, alkyl or alkynyl,Y is O or NR.sup.3, where R.sup.3 is hydrogen or alkyl,R.sup.2 is H, alkyl, cycloalkyl, alkenyl, aryl, alkynyl, cycloalkenyl, arylalkyl, aryloxyalkyl, hetaryl, hetarylalkyl, hetaryloxyalkyl, acyl, arylalkenyl, hetarylalkenyl, heterocyclyl, arylcarbonyl, hetarylcarbonyl or alkoxycarbonylalkyl,Y and R.sup.2 may form a ring, andX is CH.sub.2, CH-alkyl, CH-alkoxy, CH-alkylthio, N-alkoxy or NOH,and fungicides containing these compounds.Type: GrantFiled: January 24, 1992Date of Patent: October 19, 1993Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Albrecht Harreus, Hubert Sauter, Beate Hellendahl, Reinhard Doetzer, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5246965Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.Type: GrantFiled: September 17, 1992Date of Patent: September 21, 1993Assignee: Ciba-GeigyInventor: Alan J. Main
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Patent number: 5239113Abstract: Novel substituted .beta. amino acid derivatives are provided which inhibit platelet aggregation and intermediates thereof. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.Type: GrantFiled: April 10, 1992Date of Patent: August 24, 1993Assignees: Monsanto Company, G. D. Searle & Co.Inventors: Phillipe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
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Patent number: 5233047Abstract: Hydrazide functionalized benzotrialzole and oxanilide ultraviolet absorbers (Formulas I and II) useful for stabilizing coreactive or inert polymeric compositions and novel intermediates (Formula III used to make certain types of compounds of Formula I) are disclosed and have the general formulas: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, all substituents thereof, and n are set forth in the Summary of the Invention.Type: GrantFiled: May 1, 1991Date of Patent: August 3, 1993Assignee: Elf Atochem North America, Inc.Inventors: Ronald E. MacLeay, Terry N. Myers
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Patent number: 5220050Abstract: This invention relates to having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.Type: GrantFiled: November 12, 1991Date of Patent: June 15, 1993Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Dudley E. McMackins, Joseph G. Rico, Foe S. Tjoeng, Mihaly V. Toth, Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki
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Patent number: 5220023Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: April 10, 1992Date of Patent: June 15, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5208388Abstract: 2,2-Difluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl andX represents hydroxymethyl, 2-hydroxyethyl, isocyanato, amino, amino hydrohalide or a radical of the formula --CO--R.sup.1, whereR.sup.1 represents hydrogen, hydroxyl, alkoxy, alkyl, halogen or amino,are intermediates for fungicides.Type: GrantFiled: September 20, 1991Date of Patent: May 4, 1993Assignee: Bayer AktiengesellschaftInventors: Karl-Rudolf Gassen, Bernd Baasner
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Patent number: 5198566Abstract: Disclosed herein are N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives of the formula (I): ##STR1## wherein R.sup.1 and CF.sub.3, COOH or CCl=CClCOOH, R.sup.2 is H, Cl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.4 alkoxycarbonyl; Z is CH or N; X.sup.1 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxyl or Cl; and X.sup.2 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxyl, a process for the preparation thereof, and herbicidal compositions containing the N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives as active ingredients.Type: GrantFiled: June 3, 1992Date of Patent: March 30, 1993Assignee: Kureha Kagaku Kogyo K.K.Inventors: Hideo Arabori, Shiro Yamazaki, Masato Arahira, Aiko Murakami
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Patent number: 5194663Abstract: An aromatic derivative of butyric acid has the formula ##STR1## These aromatic derivatives of butyric acid are useful in human and veterinary medicines as well as in cosmetic compositions.Type: GrantFiled: August 9, 1991Date of Patent: March 16, 1993Assignee: Societe Anonyme Dite: L'OrealInventors: Jean Maignan, Gerard Malle, Gerard Lang
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Patent number: 5177259Abstract: The present invention is novel diarylalkanoids having activity as lipoxygenase inhibitors, novel pharmaceutical compositions therefor, and novel methods of use in treating asthma, allergies, cardiovascular diseases, migraines, psoriasis and immunoinflammatory diseases for diarylalkanoids. The compounds of this invention are also useful as cytoprotective agents.Type: GrantFiled: August 27, 1991Date of Patent: January 5, 1993Assignee: Warner-Lambert CompanyInventors: David T. Connor, Daniel L. Flynn
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Patent number: 5169986Abstract: The present invention provides an organic nonlinear optical material including a benzylidene-aniline derivative having an electron-donating substituent introduced at the 4-position and an electron-accepting substituent introduced at the 4'-position, by selecting as the conjugated .pi. electronic system a benzylidene-aniline derivative having a large molelcular hyperpolarizability and yet a dipole moment as small as those of benzene derivatives, and introducing a molecular alignment-regulating substituent. The centrosymmetry in the bulk state of the material, for example, in the crystal state, is destroyed and the molecular alignment is regulated to such a bulk structure so that the optical nonlinearity possessed by the molecule is effectively utilized. The material exhibit a large optical nonlinearity never attained by conventional techniques.the intermolecular cohesive force due to the .pi. electron interaction between the molecules in the present invention is larger than that between a benzene derivative.Type: GrantFiled: October 19, 1990Date of Patent: December 8, 1992Assignee: Toray Industries, Inc.Inventors: Tetsuya Tsunekawa, Tetsuya Gotoh, Keiichi Egawa
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Patent number: 5149859Abstract: A naphthalene derivative having the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or a non-toxic salt moiety; R.sup.2 and R.sup.3 independently represent a hydrogen atom or --OR.sup.4 where R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group;A represents a group: ##STR2## [where X.sup.1 and X.sup.2 represents an oxygen atom or N--OR.sup.5 (where R.sup.5 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], a group: ##STR3## [where Y.sup.1 and Y.sup.2 independently an oxygen atom or a group N--OR.sup.6 (where R.sup.6 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], or a group: ##STR4## (where n is 0 or 1); and B represents --(CH.sub.2).sub.m --wherein m is an integer of 1, to 8,--(CH.sub.2).sub.m.sbsb.1 --O--(CH.sub.2).sub.m.sbsb.2 --wherein m.sub.1 and m.sub.2 are independently 1 or 2, or ##STR5## wherein m.sub.3 is 0 or 1.Type: GrantFiled: September 14, 1990Date of Patent: September 22, 1992Assignee: Teijin LimitedInventors: Atsuo Hazato, Takumi Takeyasu, Koji Tomimori, Yoshinori Kato
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Patent number: 5147892Abstract: Benzyl ketones of the formula ##STR1## where X is CH or N,Y is O or NR.sup.4,R.sup.1, R.sup.2 are H or alkyl,R.sup.3 is halogen, cyano, nitro, alkyl, cycloalkyl, alkoxy, haloalkyl, arylalkyl, arylalkoxy, aryloxy or aryl, and the aryl groups in turn may be substituted,R.sup.4 is OH, alkoxy or arylalkoxy andR.sup.5 is H, methyl, halogen or methoxy,and fungicides containing these compounds.Type: GrantFiled: June 27, 1991Date of Patent: September 15, 1992Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5118697Abstract: Novel cyclic beta-ketoamides which contain an aryl moiety having utility as blood cholesterol lowering agents rendering them useful in the treatment of atherosclerosis.Type: GrantFiled: March 6, 1991Date of Patent: June 2, 1992Assignee: Warner-Lambert CompanyInventors: Corinne E. Augelli-Szafran, Bharat K. Trivedi
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Patent number: 5095147Abstract: 2,2-Difluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl andX represents hydroxymethyl, 2-hydroxyethyl, isocyanato, amino, amino hydrohalide or a radical of the formula --CO--R.sup.1, whereR.sup.1 represents hydrogen, hydroxyl, alkoxy, alkyl, halogen or amino,are intermediates for fungicides.Type: GrantFiled: April 26, 1991Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Karl-Rudolf Gassen, Bernd Baasner
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Patent number: 5089661Abstract: A new process is described for the preparation of a 2-aryl-propionic acid, such as for instance 2-[4-(2-methyl-propyl)phenyl]propionic or 2-(6'-methoxy-2'-naphthyl)propionic acid, through hydrogenation of a complex salt which consists of the mono- and/or di-valent anion of the corresponding 2-hydroxy-2-aryl-propionic acid, a di- or tri-valent metal cation, such as for instance Al(+3), Fe(+3), Zn(+2), or Mg(+2), and optionally other anonic or neutral ligands.This new process is particularly advantageous in that the starting salt can be obtained directly via electrocarboxylation of the corresponding aryl methyl ketone, e.g. 4-(2-methyl-propyl)acetophenone or (6-methoxy-2-naphthyl) methyl ketone, with metal anodes which dissolve during the electrolysis.Type: GrantFiled: September 10, 1990Date of Patent: February 18, 1992Assignee: Enichem Synthesis S.p.A.Inventors: Federico Maspero, Oreste Piccolo, Ugo Romano, Salvatore Gambino
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Patent number: 5081283Abstract: Novel intermediates for fungicides, comprising fluorocyclopropyl derivatives of the formula ##STR1## in which R represents alkyl, optionally substituted aryl or optionally substituted aralkyl,X represents hydrogen, chlorine or bromine andR.sup.1 represents hydroxyl, alkoxy, alkyl or halogen.Type: GrantFiled: April 26, 1991Date of Patent: January 14, 1992Assignee: Bayer AktiengesellschaftInventors: Karl-Rudolf Gassen, Bernd Baasner
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Patent number: 5079245Abstract: The compounds 2-trifluoromethyl-7-substituted-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes are disclosed and disclosed to be useful in the treatment of metabolic illnesses such as diabetes, obesity, and their complications. A perferred compound is 2-trifluoromethyl-7-amino-6,7,8,9-tetrahydro-[5H-benzocycloheptane.Type: GrantFiled: July 5, 1989Date of Patent: January 7, 1992Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour
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Patent number: 5055582Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: October 8, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 5045541Abstract: Fused pyridazine compounds ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and respectively hydrogen, a halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, and alkyl, an alkoxy or an alkanoylamino; one of R.sub.a and R.sub.b is a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are the same or different and respectively hydrogen, an alkyl, a phenylalkyl or a substituted phenylalkyl or a group forming a heterocycle together with the adjacent nitrogen atom and Y stands for a straight- or branched-chain alkylene which may have hydroxy group as a substituent on the chain, and the other is hydrogen, or both of R.sub.a and R.sub.b are the same or different and respectively a group of the formula--O--Y--NR.sup.5 R.sup.6wherein R.sup.5 and R.sup.6 are of the same meanings as defined above; W is .dbd.CH-- or .dbd.N; X is CH.sub.2, S, SO, SO.sub.Type: GrantFiled: July 2, 1989Date of Patent: September 3, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Toru Nakao, Minoru Kawakami, Masao Hisadome, Tetsuya Tahara
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Patent number: 5041663Abstract: The invention relates to novel oxime ethers of the formula I ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkylthio, lower haloalkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower haloalkylsulfinyl, lower haloalkylsulfonyl or nitro, each of R.sub.2 and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or lower haloalkoxy, and Q is an unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl or cycloalkyl group, a lower alkanoyl radical, an aliphatic, cycloaliphatic, aromatic or heterocyclic acyl radical which may be substituted or unsubstituted, a carbonyl or thiocarbonyl radical, an aryl or aralkyl radical, an acylimidomethyl radical, a phthalimidomethyl radical or a heterocyclic radical.These compounds are able to act as antidotes or safeners for protecting cultivated plants from the phytotoxic action of aggressive herbicides.Type: GrantFiled: December 11, 1990Date of Patent: August 20, 1991Assignee: Ciba-Geigy CorporationInventors: Henry Martin, Urs Fricker
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Patent number: 5041644Abstract: New peptide derivatives .beta.-chloro-L-(Z)-dehydroglutamic acid are described which display antibacterial activity.Type: GrantFiled: June 27, 1988Date of Patent: August 20, 1991Assignee: Merck & Co., Inc.Inventors: Yoshiharu Morita, Ryoichi Ando, Junko Takashima, Louis Chaiet
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Patent number: 5026905Abstract: The present invention describes a class of dyes for use in staining cell samples and methods of making such dyes. A preferred class of dyes known as detergent dyes which possess the ability to stain cells in whole blood and are only slowly leached or lost from the stained cells over time are described. The present invention has application, for example, to blood typing for the determination of the presence of blood group antigens A, B, AB, O, and D (Rh.sub.o) and antibodies to such antigens.Type: GrantFiled: August 19, 1988Date of Patent: June 25, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Thomas L. Tarnowski, Mae W. Hu, Maureen Laney, John S. Pease, Vartan Ghazarossian
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Patent number: 5025034Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.Type: GrantFiled: February 7, 1990Date of Patent: June 18, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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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: 5011628Abstract: Substituted benzamidines and their hydrochloride salts are useful as ultraviolet light absorbers, the benzamidines having the formula ##STR1## wherein: A.sup.1 and A.sup.2 may be the same or different and represent --COOR.sup.1, --CONR.sup.1 R.sup.2, --C.tbd.N or --C.sub.6 H.sub.5 ;A.sup.3 represents --H, --OH, --OR, --Cl, --NO.sub.2, --C.tbd.N, --C.sub.6 H.sub.5, or an alkyl group of one to five carbon atoms;R.sup.1 and R.sup.2 may be the same or different and represent hydrogen or an alkyl group of one to ten carbon atoms; and,R represents an alkyl group of one to ten carbon atoms.Type: GrantFiled: April 11, 1989Date of Patent: April 30, 1991Assignee: Givaudan CorporationInventors: Isaac D. Cohen, Joseph A. Virgilio
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Patent number: 5006160Abstract: In accordance with the present invention, there are provided novel compounds represented by the following general formula [I], and herbicides containing as their active ingredients. ##STR1## wherein X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are each hydrogen, halogen or methyl, and R is hydrogen or a lower alkyl.There are also provided herbicides containing as their active ingredients compounds represented by the following general formula [II]. ##STR2## wherein R is hydrogen or a lower alkyl.Type: GrantFiled: July 5, 1989Date of Patent: April 9, 1991Assignee: SDS Biotech Kabushiki KaishaInventors: Yuichi Sugiyama, Takashi Isono, Yukihiro Nakamura, Akihiro Takaiwa, Kenichi Komatsubara
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Patent number: RE33989Abstract: Oxime ethers of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or alkyl, X(m=1 to 5) is halogen, cyano, trifluoromethyl, nitro, allyl, alkoxy, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, unsubstituted or substituted benzyloxy or hydrogen, and Y is methyleneoxy, oxymethylene, ethylene, ethynylene or oxygen, and fungicides containing these compounds.Type: GrantFiled: June 11, 1990Date of Patent: July 7, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Wenderoth, Timm Anke, Costi Rentzes, Eberhard Ammermann, Ernst-Heinrich Pommer, Wolfgang Steglich