Two Rings Bonded Directly To The Same Carbonyl Patents (Class 562/460)
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Patent number: 6001877Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: May 20, 1998Date of Patent: December 14, 1999Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5962731Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.Type: GrantFiled: June 7, 1995Date of Patent: October 5, 1999Assignee: Ligand Pharmaceuticals IncorporatedInventors: Marcus F. Boehm, Richard A. Heyman
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Patent number: 5932763Abstract: The present invention provides pharmaceutical compositions and methods for treating certain conditions comprising administering an amount of a compound or composition of the invention which is effective to inhibit the activity of at least one matrix metalloprotease, resulting in achievement of the desired effect. The compounds of the present invention are of the generalized formula ##STR1## where v is 1, 2, 3 or 4 and Ar represents a substituted aromatic moiety.Type: GrantFiled: May 15, 1997Date of Patent: August 3, 1999Assignee: Bayer CorporationInventors: William J. Scott, Margaret A. Popp, David S. Hartsough
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Patent number: 5922904Abstract: Benzoyl phthalic acids of the formula ##STR1## useful as intermediates in the preparation of quinophthalone dyestuffs.Type: GrantFiled: September 15, 1998Date of Patent: July 13, 1999Assignee: Bayer AktiengesellschaftInventor: Stephan Michaelis
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Patent number: 5886022Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent g roup; x is 0, 1, or 2; the group D represents ##STR2## the subscript "e" is 2 or 3; the group R.sup.14 represents a variety of possible substituent groups of the cycloalkyl ring between D and G; the subscript "k" is 0-2; and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: March 23, 1999Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, William Harrison Bullock, Brian Richard Dixon, Stephan Schneider, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin
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Patent number: 5883294Abstract: Selective thyroid hormone agonists are disclosed that are highly selective for the TR.beta. subtype with high binding affinity. Methods of using such agonists and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.Type: GrantFiled: June 18, 1997Date of Patent: March 16, 1999Assignee: The Regeants of the University of CaliforniaInventors: Thomas S. Scanlan, Grazia Chiellini, Hikari Yoshihara, James Apriletti, John D. Baxter, Ralff C. J. Ribeiro
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Patent number: 5808124Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: June 21, 1996Date of Patent: September 15, 1998Assignee: AllerganInventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5739352Abstract: This invention relates to a process for preparing carboxylic acids by oxidizing an aldehyde with a peracid in the presence of an amine and/or amine N-oxide catalyst selected from the group consisting of a substituted or unsubstituted alkyl amine, alkyl amine N-oxide, aromatic amine, aromatic amine N-oxide, heterocyclic amine, heterocyclic amine N-oxide and mixtures thereof, to produce the carboxylic acid. Such carboxylic acids have utility for example as chemical intermediates.Type: GrantFiled: October 19, 1995Date of Patent: April 14, 1998Assignee: United Carbide Chemicals & Plastics Technology CorporationInventors: Bruce Armin Barner, Jonathan Joshua Kurland
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Patent number: 5677469Abstract: A process for the full or partial resolution of a mixture of enantiomers of a genus of chiral carboxylic acids is disclosed. The process uses a pure enantiomer of 1-aminoindan-2-ol as the resolving agent and achieves separation of the diastereomeric salts by fractional crystallization followed by liberation of the chiral acid from the salt by treatment with mineral acid. Diastereomeric salts and solyates of those salts are disclosed. The production of ketoprofen, flurbiprofen and other chiral medicaments and precursors thereto is disclosed.Type: GrantFiled: May 18, 1995Date of Patent: October 14, 1997Assignee: Sepracor, Inc.Inventors: Paul van Eikeren, Francis X. McConville, Jorge L. Lopez
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Patent number: 5583221Abstract: Compounds having the formula ##STR1## methods for using such compounds to inhibit protein kinase C in animals, including man are useful as inhibitors of protein kinase C. Also disclosed are pharmaceutical compositions including such compounds and compounds having the formula.Type: GrantFiled: February 23, 1995Date of Patent: December 10, 1996Assignee: Eli Lilly and CompanyInventors: Hong Hu, G. Erik Jagdmann, Jr., Jose S. Mendoza
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Patent number: 5554789Abstract: A novel arylpropionic derivative, i.e. the (+)-(S)-2-(3-Benzoylphenyl)propionic acid tromethamine salt, the process for the preparation thereof and the use thereof as an analgesic and antiinflammatory agent.Type: GrantFiled: May 23, 1995Date of Patent: September 10, 1996Assignee: Laboratorios Menarini S.A.Inventors: Germano Carganico, David Mauleon Casellas, M. Luisa Garcia Perez
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Patent number: 5504244Abstract: Disclosed are novel alkylarylketocarboxylic acids and 5-substituted tetrazoles represented by the formula ##STR1## wherein Z is aryl or an alkyl of the structure ##STR2## W is a carboxyl moiety or a tetrazole moiety bound to Z at the 5-position of the tetrazole;R.sub.1 is C.sub.4 -C.sub.12 alkyl where Z is aryl and X is oxygen or is C.sub.5 -C.sub.12 alkyl where Z is alkyl and where Z is aryl and X is a bond;R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy, C.sub.1 -C.sub.4 alkoxy, halogen, trihalomethyl, nitro, cyano or C.sub.1 -C.sub.4 acyl;R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl or R.sub.4 and R.sub.6 or R.sub.5 and R.sub.7 can combine to form a carbocyclic ring;X is oxygen, or a bond at the ortho or para position;m is 0, 1 or 2; andn is 0 or 1, and nontoxic, pharmaceutically acceptable addition salts and carboxylic acid esters thereof.Type: GrantFiled: December 14, 1993Date of Patent: April 2, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, John P. Devlin
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Patent number: 5461045Abstract: A fused benzeneoxyacetic acid derivative of the formula: ##STR1## wherein ##STR2## is (i) ##STR3## (ii) ##STR4## (iii) ##STR5## or (iv) ##STR6## A is (i) ##STR7## or (ii) ##STR8## R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl or phenyl;R.sup.3 is(i) C.sub.1-15 alkyl,(ii) C.sub.1-8 alkyl substituted by one or two of benzene, C.sub.4-7 cycloalkane or 4-7 ring-membered monocyclic ring which contains one nitrogen atom or(iii) C.sub.10-15 condensed tricyclic ring;e is 3-5;f is 1-3;p is 0-4;q is 0-2;s is 0-3With the proviso that, ring(s) in R.sup.3 may be substituted by one to three of C.sub.1-4 alkyl, .sub.1-4 alkoxy, halogen atom, nitro or trihalomethyl. And, when D--B is the formula (iii) or (iv), --(CH2)p- or .dbd.CH--(CH2)s- is attached at the position of a or b on the ring.Type: GrantFiled: July 14, 1992Date of Patent: October 24, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5432198Abstract: Compounds having the formula ##STR1## are useful as inhibitors of protein kinase C. Also disclosed are pharmaceutical compositions including such compounds and methods for using such compounds to inhibit protein kinase C in animals, including man.Type: GrantFiled: August 18, 1994Date of Patent: July 11, 1995Assignee: Sphinx Pharmaceuticals CorporationInventor: G. Erik Jagdmann, Jr.
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Patent number: 5426215Abstract: Process for transforming (benzoyl-3-phenyl)-2-propionic-R(-) acid into an S(+) isomer through the action of a base either in situ during the splitting of racemic ketoprofen or on the crystallization mother liquor of a (benzoyl-3-phenyl)-2-propionic-S(+) acid salt.Type: GrantFiled: March 16, 1994Date of Patent: June 20, 1995Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Claude Bertrand, Elie Fouque, Isidore Le Fur, Jean-Paul Richard
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Patent number: 5347047Abstract: Acylaromatic compounds are prepared from aromatic compounds and carboxylic acids by reacting the starting compounds with phosgene in the presence of an aliphatic phosphine oxide or of an N,N-dialkylformamide and of an Fe(II), Fe(III) or Zn(II) compound.Type: GrantFiled: December 1, 1993Date of Patent: September 13, 1994Assignee: BASF AktiengesellschaftInventors: Wolfgang Siegel, Irene Troetsch-Schaller
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Patent number: 5344843Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.Type: GrantFiled: March 13, 1992Date of Patent: September 6, 1994Assignee: Hoffman-La Roche Inc.Inventors: Robert W. Guthrie, John G. Mullin, Jr., David F. Kachensky, Richard W. Kierstead, Jefferson W. Tilley, Guy P. Heathers, Alan J. Higgins, Ronald A. LeMahieu
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Patent number: 5338881Abstract: This invention concerns a process for preparing diketones and keto-acids by reacting a dicarboxylic acid and an aromatic compound in the presence of an alkylsulfonic acid such as methanesulfonic acid and a phosphorus pentoxide. The diketones and keto-acids can be used to prepare polyketones which are useful as molding plastics, coatings, films, fibers, and the like.Type: GrantFiled: July 23, 1990Date of Patent: August 16, 1994Assignee: Eastman Chemical CompanyInventors: Theodore R. Walker, Jr., Winston J. Jackson, Jr., Jean C. Fleischer
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Patent number: 5294646Abstract: The invention relates to new N-alkyl-N-(meth)acryloyloxyalkylcarboxamides of aromatic carboxylic acids and aromatic carboxylic acid anhydrides, their preparation and formulations of these compounds for use as adhesives for the treatment of dental hard substance.Type: GrantFiled: June 25, 1992Date of Patent: March 15, 1994Assignee: Bayer AktiengesellschaftInventors: Michael Muller, Wolfgang Podszun, Werner Finger, Jens Winkel
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Patent number: 5254728Abstract: Complexes containing S(+)-ibuprofen, method for the production of these complexes and pharmaceutical preparations containing these complexes are described.Type: GrantFiled: November 15, 1991Date of Patent: October 19, 1993Assignee: Medice Chem.-pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 5241081Abstract: The invention relates to new N-alkyl-N-(meth)acryloyloxyalkylcarboxamides of aromatic carboxylic acids and aromatic carboxylic acid anhydrides, their preparation and formulations of these compounds for use as adhesives for the treatment of dental hard substance.Type: GrantFiled: August 9, 1991Date of Patent: August 31, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Muller, Wolfgang Podszun, Werner Finger, Jens Winkel
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Patent number: 5218124Abstract: There are disclosed compounds of the formulaA(CH.sub.2).sub.n O--BwhereinA is a group having the formula ##STR1## wherein X is --N-- or ##STR2## Z is ##STR3## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring, with the proviso that when X is --N--, Z is other than ##STR4## R.sup.3 is hydrogen or lower alkyl; n is 1-2;B is ##STR5## wherein Y is OR.sup.5 or N(OH)R.sup.8 ;R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or nitro;R.sup.7 is ##STR6## R.sup.Type: GrantFiled: June 1, 1992Date of Patent: June 8, 1993Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah, Dennis M. Kubrak
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Patent number: 5191112Abstract: Optical resolution of (.+-.)-2-(3-benzoyl)-phenylpropionic acid is attained effeciently in high yield by the use of a specific optically active amine which is represented by the general formula [I]: ##STR1## wherein R.sup.1 either stands for a hydrogen atom, a chlorine atom, a bromine atom, a methyl group, or an isopropyl group or participates, as a divalent group, in forming a benzene ring in combination with two carbon atoms adjoining each other in a benzene ring to which the substituent, R.sup.1, is bonded, R.sup.2 stands for a lower alkyl group, a hydroxymethyl group, an .alpha.-hydroxybenzyl group, or a ##STR2## group (R.sup.3 standing for a hydrogen atom, a chlorine atom, a bromine atom, or a methyl group), n for 0 or 1, and * for the center of optical activity.Type: GrantFiled: August 24, 1990Date of Patent: March 2, 1993Assignee: Nissan Chemical Industries, Ltd.Inventors: Hiroyuki Nohira, Kazutaka Arai
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Patent number: 5189208Abstract: A process for obtaining a substantially pure enantiomer of ibuprofen is described. The process utilizes first an enantiomerically enriched mixture of ibuprofen obtained from kinetic resolution, diastereomeric crystallization or asymmetric synthesis processes. This enriched mixture is dissolved in a solvent and solid racemic ibuprofen is separated, leaving a mother liquid comprising the solvent and the enriched enantiomer substantially free of the other enantiomer.Type: GrantFiled: July 1, 1991Date of Patent: February 23, 1993Assignee: Ethyl CorporationInventor: G. Patrick Stahly
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Patent number: 5171882Abstract: 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: October 16, 1990Date of Patent: December 15, 1992Assignee: Eli Lilly and CompanyInventor: D. Mark Gapinski
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Patent number: 5164527Abstract: Acylation or sulphonylation of aromatic compounds, one of which is selected from aromatic carboxylic and sulphonic acids and esters and anhydrides thereof, using an aluminosilicate catalyst having acidic sites.Type: GrantFiled: April 3, 1991Date of Patent: November 17, 1992Assignee: Imperial Chemical Industries PLCInventor: Alan B. Newton
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Patent number: 5162576Abstract: A method for resolving (.+-.)-(.alpha.)-(3-benzoylphenyl) propionic acid is disclosed. The method comprises:i) converting said propionic acid with (-)-cinchonidine in a solvent comprising a mixture of an aliphatic ester and an alkyl alcohol;ii) separating teh diastereomeric salt from such conversion;iii) purifying said separated diastereomeric salt by a single recrystallization; andiv) isolating highly pure (+)-.alpha.-(3-benzoylphenyl) propionic acid without any further recrystallization.Type: GrantFiled: April 15, 1991Date of Patent: November 10, 1992Assignee: Ethyl CorporationInventors: Thanikavelu Manimaran, Alicia A. Potter
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Patent number: 5136089Abstract: A process for the acylation of an alkyl aromatic hydrocarbon with a derivative of carboxylic acid by the Friedel-Crafts method in the presence of a Friedel-Crafts catalyst and an organo-aluminum compound, wherein the organo-aluminum compound is an alumoxane.Type: GrantFiled: April 8, 1991Date of Patent: August 4, 1992Assignee: BASF AktiengesellschaftInventors: Jochem Henkelmann, Hardo Siegel
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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: 5107029Abstract: This invention concerns a process for preparing diketones and keto-acids by reacting a dicarboxylic acid and an aromatic compound in the presence of an alkylsulfonic acid such as methanesulfonic acid and an organic anhydride compound such as methanesulfonic anhydride or trifluoroacetic anhydride. The diketones and keto-acids can be used to prepare polyketones which are useful as molding plastics, coatings, films, fibers, and the like.Type: GrantFiled: July 23, 1990Date of Patent: April 21, 1992Assignee: Eastman Kodak CompanyInventors: Theodore R. Walker, Jr., Winston J. Jackson, Jr., Jean C. Fleischer
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Patent number: 5097064Abstract: This invention relates to a process for preparing an optically active 2-arylpropionic acid of general formula (I), by the hydrogenation, in a heterogeneous aqueous-organic medium, of a 2-arylacrylic acid of general formula (II) in the presence of a catalyst consisting of a rhodium derivative and a water-soluble chiral ligand.Type: GrantFiled: August 30, 1990Date of Patent: March 17, 1992Assignee: Rhone-Poulenc SanteInventor: Jean-Michel Grosselin
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Patent number: 5093516Abstract: An aromatic compound of the formula ##STR1## wherein n is 0 or 1,(1) when n is 1,R' represents hydrogen or C.sub.1 -C.sub.4 alkoxy,R" represents hydrogen, OH, C.sub.1 -C.sub.4 acyloxy, C.sub.1 -C.sub.4 alkoxy or amino,or R' and R" taken together form an oxo, methano or hydroxy-imino radical,R.sub.1 represents--CH.sub.2 OH or --COR.sub.10,R.sub.10 represents hydrogen, OR.sub.11 or ##STR2## R.sub.11 represents hydrogen, C.sub.1 -C.sub.20 alkyl, monohydroxyalkyl, polyhydroxy alkyl, aryl, aralkyl, the residue of a sugar or ##STR3## p is 1,2 or 3, r' and r" represent hydrogen, lower alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, benzyl, the residue of an amino acid or the residue of an aminated sugar, of r' and r" taken together form a heterocycle,R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent hydrogen, OH, C.sub.1 -C.sub.12 alkyl, cycloalkyl, cycloalkenyl, phenyl or a radical of the formulas (i)--X--C.sub.6 H.sub.5, (ii)--X--R.sub.12 or (iii)--NHCOR.sub.13,X is --0--,--S--,--SO--,--SO.sub.Type: GrantFiled: April 3, 1987Date of Patent: March 3, 1992Assignee: L'OrealInventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
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Patent number: 5089654Abstract: Chalcone derivatives represented by the formula ##STR1## wherein R.sup.1 is a straight chain, branched chain or cyclic alkyl group having 4 to 15 carbon atoms or an alkenyl group having 3 to 15 carbon atoms, and occurs at the 2- or 4-position, R.sup.2 is a hydrogen atom, a straight or branched chain alkyl group having 1 to 3 carbon atoms, and X is a straight or branched chain alkylene group having 1 to 3 carbon atoms, are disclosed. These compounds have anti-ulcer effect, gastric mucosal protection effect and antisecretory effect.Type: GrantFiled: August 3, 1990Date of Patent: February 18, 1992Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Sadakazu Yokomori, Keiko Saijo, Tohru Matsunaga, Yoshimoto Nakashima, Katsuo Hatayama
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Patent number: 5081279Abstract: This invention provides a method of producing highly pure .alpha.-(3-benzoylphenyl)propionic acid derivatives, which are medicines per sec or which can easily afford the same, from readily available 3-ethylbenzophenone in a very simplified manner efficiently and economically. The method comprises dehydrogenating 3-ethylbenzophenone in vapor phase in the presence of an inert gas and carbonylating the formed 3-ethenylbenzophenone in the presence of a carbonylation catalyst comprising a transition metal complex.Type: GrantFiled: November 6, 1990Date of Patent: January 14, 1992Assignee: Nippon Petrochemicals Company, LimitedInventors: Isoo Shimizu, Yasuo Matsumura, Yoshihisa Inomata
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Patent number: 5081282Abstract: Bicyclo prostaglandin analogues have been prepared.Type: GrantFiled: January 13, 1988Date of Patent: January 14, 1992Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5077309Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5073552Abstract: Substituted benzophenones are disclosed having the following formula ##STR1## where R.sub.A and R.sub.B are each independently COOH, C.sub.1 to C.sub.12 linear or branched alkyl or taken together to form an anhydride ring, R is nitro or amino unsubstituted or substituted with at least one C.sub.1 to C.sub.6 linear or branched alkyl, phenyl or substituted phenyl, the substituents being one or more C.sub.1 to C.sub.6 linear or branched alkyl or C.sub.6 to C.sub.10 aryl, Y and Y' are the same or different and are a chemical bond ##STR2## and m is 0 or 1 with the proviso that both R.sub.A and R.sub.B can not be hydrogen.Processes to produce these benzophenones are also disclosed.Type: GrantFiled: September 4, 1990Date of Patent: December 17, 1991Assignee: Ethyl CorporationInventors: Mark W. Beltz, Venkataraman Ramachandran
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Patent number: 5061810Abstract: Substituted benzophenones are disclosed having the following formula ##STR1## where R.sub.A and R.sub.B are --OH, C.sub.1 to C.sub.12 linear or branched alkoxy or taken together with the adjacent carbonyl carbons form an anhydride ring, R.sub.1 and R.sub.2 are the same or different and are hydrogen, C.sub.1 to C.sub.6 linear or branched alkyl, halo, aryl unsubstituted or substituted with one or more aryloxy groups or R.sub.1 and R.sub.2 taken together are (CH.sub.2).sub.x where x is an integer from 3 to 6 with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen.Processes to produce these benzophenones are also disclosed.Type: GrantFiled: November 28, 1989Date of Patent: October 29, 1991Assignee: Ethyl CorporationInventor: Venkataraman Ramachandran
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Patent number: 5023363Abstract: An aromatic compound of the formula ##STR1## These compounds are useful in human and veterinary medicines and in cosmetic compositions.Type: GrantFiled: April 1, 1988Date of Patent: June 11, 1991Assignee: L'OrealInventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
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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: 4983765Abstract: A process is described in which a mixture of enantiomeric arylpropionic acid is split and one of enantiomeric forms of the acid is recovered. The mixture is transformed into a diastereoisomeric salt by a reaction with a chiralic base and an inert solvent, and the desired acid enantiomer is removed from the reaction product. The transformation to a diastereoisomeric salt takes place in a polar solvent. The salt produced is recrystallized several times and the thus purified salt is split in a dilute mineral acid.Type: GrantFiled: June 27, 1989Date of Patent: January 8, 1991Assignee: PAZ Arzneimittel-Entwicklungsgesellschaft mbHInventors: Helmut Lukas, Otto Schuster, Gunther Rau
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Patent number: 4970336Abstract: This invention relates to methods of preparing and purifying .alpha.-substituted acetic acids, which comprise treating an .alpha.aromatic-substituted acetic acid represented by a specific general formula with a weak alkali while shielding light, or subjecting an .alpha.-aromatic-substituted acetonitrile represented by a specific general formula to acid hydrolysis, followed by treatment with a weak alkali while shielding light; and treating the alkali salt of .alpha.-substituted acetic acid thus formed with a decolorizing agent.Type: GrantFiled: May 31, 1989Date of Patent: November 13, 1990Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshikazu Yoshioka, Isao Hashiba, Suketoshi Tsukamoto
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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: 4943310Abstract: The invention relates to new 4-benzoyl-3-hydroxy-5-oxo-3-cyclohexenecarboxylic acid derivatives of general formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.2 and R.sup.3 have the meanings given in the description, and their use as plant growth regulants.Type: GrantFiled: December 16, 1988Date of Patent: July 24, 1990Assignee: Schering AktiengesellschaftInventors: Alfred Angermann, Helga Franke, Gerhard Johann
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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: 4922015Abstract: The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl or optionally substituted (C.sub.6 -C.sub.14)-aryl, R.sup.2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off 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), one of these radicals being -O-(CH.sub.2).sub.n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.Type: GrantFiled: April 6, 1988Date of Patent: May 1, 1990Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breipohl, Jochen Knolle, Werner Stuber
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Patent number: 4916147Abstract: Novel compounds of the general formula: ##STR1## [wherein X represents an oxygen atom or sulfur atom, R.sup.1, R.sup.2 and R.sup.3 represent a hydrogen atom, a halogen atom or an alkyl group of from 1 to 4 carbon atom(s) independently or a formula: R.sup.3' ##STR2## (wherein R.sup.3' represents a hydrogen atom or an alkyl group of from 1 to 4 carbon(s))in place of a formula: ##STR3## R.sup.4 represents a general formula: ##STR4## or --N(R.sup.9).sub.2 (in which W represents an oxygen atom or sulfur atom, R.sup.6, R.sup.7 and R.sup.8 represent a hydrogen atom, a halogen atom, a nitro group, an alkyl group of from 1 to 4 carbon atom(s), a hydroxy group or an alkoxy group of from 1 to 4 carbon atom(s) independently, each of R.sup.9 represents a hydrogen atom, an alkyl group of from 1 to 4 carbon atom(s) or a phenyl group and Y represents a single bond or an alkylene group or an alkenylene group of from 1 to 4 carbon atom(s).), and R.sup.5 represents a 5-tetrazolyl group or a general formula: --COOR.sup.Type: GrantFiled: June 21, 1986Date of Patent: April 10, 1990Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
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Patent number: 4910337Abstract: .alpha.-Arylalkanoic acids are prepared by a method comprising the step of reacting an alkylaromatic compound corresponding to the desired .alpha.-arylalkanoic acid with a new metallation reagent solution. The reagent comprises the reaction product of alkyllithium or aryllithium and about two to five molar equivalents of potassium tert-alkoxide in a trialkylamine solvent.Type: GrantFiled: January 27, 1989Date of Patent: March 20, 1990Assignee: Mine Safety Appliances CompanyInventors: Kuen-Wai Chiu, Mary H. Staruch, David H. Ellenberger
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Patent number: 4898864Abstract: Bicyclic aromatic compound having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen or alkyl, at least two of R.sub.1 -R.sub.4 radicals being other than hydrogen,A represents methylene or dimethylene; when A represents dimethylene, R.sub.1 and R.sub.3 together can form a methylene or dimethylene radical,R.sub.5 and R.sub.6 represent hydrogen, halogen, lower alkyl, lower alkoxy or hydroxy,R' represents hydrogen, hydroxy, alkoxy, C.sub.1 -C.sub.4 cicyloxy or amino,R" represents hydrogen or lower alkoxy, or R' and R" together form an oxo, methano or hydroxyimino radical,B represents cyclohexyl, cyclohexenyl, cyclohexadienyl or phenyl, substituted or not,R represents --CH.sub.2 OH or --COR.sub.7,R.sub.7 represents hydrogen, --OR.sub.8 or ##STR2## R.sub.8 represents hydrogen, C.sub.1 -C.sub.20 alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, aralkyl or a sugar residue.Type: GrantFiled: October 27, 1987Date of Patent: February 6, 1990Assignee: L'OrealInventors: Jean Maignan, Gerard Lang, Gerard Malle, Philippe Vingler