Two Rings Bonded Directly To The Same Carbonyl Patents (Class 562/460)
  • Patent number: 6001877
    Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.
    Type: Grant
    Filed: May 20, 1998
    Date of Patent: December 14, 1999
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
  • Patent number: 5962731
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: October 5, 1999
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Marcus F. Boehm, Richard A. Heyman
  • Patent number: 5932763
    Abstract: 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: Grant
    Filed: May 15, 1997
    Date of Patent: August 3, 1999
    Assignee: Bayer Corporation
    Inventors: William J. Scott, Margaret A. Popp, David S. Hartsough
  • Patent number: 5922904
    Abstract: Benzoyl phthalic acids of the formula ##STR1## useful as intermediates in the preparation of quinophthalone dyestuffs.
    Type: Grant
    Filed: September 15, 1998
    Date of Patent: July 13, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventor: Stephan Michaelis
  • Patent number: 5886022
    Abstract: 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: Grant
    Filed: May 30, 1997
    Date of Patent: March 23, 1999
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, William Harrison Bullock, Brian Richard Dixon, Stephan Schneider, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin
  • Patent number: 5883294
    Abstract: 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: Grant
    Filed: June 18, 1997
    Date of Patent: March 16, 1999
    Assignee: The Regeants of the University of California
    Inventors: Thomas S. Scanlan, Grazia Chiellini, Hikari Yoshihara, James Apriletti, John D. Baxter, Ralff C. J. Ribeiro
  • Patent number: 5808124
    Abstract: 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: Grant
    Filed: June 21, 1996
    Date of Patent: September 15, 1998
    Assignee: Allergan
    Inventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5739352
    Abstract: 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: Grant
    Filed: October 19, 1995
    Date of Patent: April 14, 1998
    Assignee: United Carbide Chemicals & Plastics Technology Corporation
    Inventors: Bruce Armin Barner, Jonathan Joshua Kurland
  • Patent number: 5677469
    Abstract: 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: Grant
    Filed: May 18, 1995
    Date of Patent: October 14, 1997
    Assignee: Sepracor, Inc.
    Inventors: Paul van Eikeren, Francis X. McConville, Jorge L. Lopez
  • Patent number: 5583221
    Abstract: 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: Grant
    Filed: February 23, 1995
    Date of Patent: December 10, 1996
    Assignee: Eli Lilly and Company
    Inventors: Hong Hu, G. Erik Jagdmann, Jr., Jose S. Mendoza
  • Patent number: 5554789
    Abstract: 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: Grant
    Filed: May 23, 1995
    Date of Patent: September 10, 1996
    Assignee: Laboratorios Menarini S.A.
    Inventors: Germano Carganico, David Mauleon Casellas, M. Luisa Garcia Perez
  • Patent number: 5504244
    Abstract: 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: Grant
    Filed: December 14, 1993
    Date of Patent: April 2, 1996
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl D. Hargrave, John P. Devlin
  • Patent number: 5461045
    Abstract: 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: Grant
    Filed: July 14, 1992
    Date of Patent: October 24, 1995
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
  • Patent number: 5432198
    Abstract: 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: Grant
    Filed: August 18, 1994
    Date of Patent: July 11, 1995
    Assignee: Sphinx Pharmaceuticals Corporation
    Inventor: G. Erik Jagdmann, Jr.
  • Patent number: 5426215
    Abstract: 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: Grant
    Filed: March 16, 1994
    Date of Patent: June 20, 1995
    Assignee: Rhone-Poulenc Rorer, S.A.
    Inventors: Claude Bertrand, Elie Fouque, Isidore Le Fur, Jean-Paul Richard
  • Patent number: 5347047
    Abstract: 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: Grant
    Filed: December 1, 1993
    Date of Patent: September 13, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Siegel, Irene Troetsch-Schaller
  • Patent number: 5344843
    Abstract: 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: Grant
    Filed: March 13, 1992
    Date of Patent: September 6, 1994
    Assignee: 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
  • Patent number: 5338881
    Abstract: 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: Grant
    Filed: July 23, 1990
    Date of Patent: August 16, 1994
    Assignee: Eastman Chemical Company
    Inventors: Theodore R. Walker, Jr., Winston J. Jackson, Jr., Jean C. Fleischer
  • Patent number: 5294646
    Abstract: 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: Grant
    Filed: June 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Muller, Wolfgang Podszun, Werner Finger, Jens Winkel
  • Patent number: 5254728
    Abstract: Complexes containing S(+)-ibuprofen, method for the production of these complexes and pharmaceutical preparations containing these complexes are described.
    Type: Grant
    Filed: November 15, 1991
    Date of Patent: October 19, 1993
    Assignee: Medice Chem.-pharm. Fabrik Putter GmbH & Co. KG
    Inventor: Henrich H. Paradies
  • Patent number: 5241081
    Abstract: 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: Grant
    Filed: August 9, 1991
    Date of Patent: August 31, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Muller, Wolfgang Podszun, Werner Finger, Jens Winkel
  • Patent number: 5218124
    Abstract: 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: Grant
    Filed: June 1, 1992
    Date of Patent: June 8, 1993
    Assignee: American Home Products Corporation
    Inventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah, Dennis M. Kubrak
  • Patent number: 5191112
    Abstract: 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: Grant
    Filed: August 24, 1990
    Date of Patent: March 2, 1993
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Hiroyuki Nohira, Kazutaka Arai
  • Patent number: 5189208
    Abstract: 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: Grant
    Filed: July 1, 1991
    Date of Patent: February 23, 1993
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 5171882
    Abstract: 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: Grant
    Filed: October 16, 1990
    Date of Patent: December 15, 1992
    Assignee: Eli Lilly and Company
    Inventor: D. Mark Gapinski
  • Patent number: 5164527
    Abstract: 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: Grant
    Filed: April 3, 1991
    Date of Patent: November 17, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventor: Alan B. Newton
  • Patent number: 5162576
    Abstract: 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: Grant
    Filed: April 15, 1991
    Date of Patent: November 10, 1992
    Assignee: Ethyl Corporation
    Inventors: Thanikavelu Manimaran, Alicia A. Potter
  • Patent number: 5136089
    Abstract: 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: Grant
    Filed: April 8, 1991
    Date of Patent: August 4, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Jochem Henkelmann, Hardo Siegel
  • Patent number: 5124478
    Abstract: 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: Grant
    Filed: December 20, 1988
    Date of Patent: June 23, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Breipohl, Jochen Knolle, Werner Stuber
  • Patent number: 5107029
    Abstract: 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: Grant
    Filed: July 23, 1990
    Date of Patent: April 21, 1992
    Assignee: Eastman Kodak Company
    Inventors: Theodore R. Walker, Jr., Winston J. Jackson, Jr., Jean C. Fleischer
  • Patent number: 5097064
    Abstract: 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: Grant
    Filed: August 30, 1990
    Date of Patent: March 17, 1992
    Assignee: Rhone-Poulenc Sante
    Inventor: Jean-Michel Grosselin
  • Patent number: 5093516
    Abstract: 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: Grant
    Filed: April 3, 1987
    Date of Patent: March 3, 1992
    Assignee: L'Oreal
    Inventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
  • Patent number: 5089654
    Abstract: 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: Grant
    Filed: August 3, 1990
    Date of Patent: February 18, 1992
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Sadakazu Yokomori, Keiko Saijo, Tohru Matsunaga, Yoshimoto Nakashima, Katsuo Hatayama
  • Patent number: 5081279
    Abstract: 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: Grant
    Filed: November 6, 1990
    Date of Patent: January 14, 1992
    Assignee: Nippon Petrochemicals Company, Limited
    Inventors: Isoo Shimizu, Yasuo Matsumura, Yoshihisa Inomata
  • Patent number: 5081282
    Abstract: Bicyclo prostaglandin analogues have been prepared.
    Type: Grant
    Filed: January 13, 1988
    Date of Patent: January 14, 1992
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 5077309
    Abstract: 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: Grant
    Filed: March 28, 1990
    Date of Patent: December 31, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 5073552
    Abstract: 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: Grant
    Filed: September 4, 1990
    Date of Patent: December 17, 1991
    Assignee: Ethyl Corporation
    Inventors: Mark W. Beltz, Venkataraman Ramachandran
  • Patent number: 5061810
    Abstract: 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: Grant
    Filed: November 28, 1989
    Date of Patent: October 29, 1991
    Assignee: Ethyl Corporation
    Inventor: Venkataraman Ramachandran
  • Patent number: 5023363
    Abstract: An aromatic compound of the formula ##STR1## These compounds are useful in human and veterinary medicines and in cosmetic compositions.
    Type: Grant
    Filed: April 1, 1988
    Date of Patent: June 11, 1991
    Assignee: L'Oreal
    Inventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
  • Patent number: 5013757
    Abstract: 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: Grant
    Filed: April 13, 1990
    Date of Patent: May 7, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
  • Patent number: 4992576
    Abstract: 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: Grant
    Filed: March 27, 1990
    Date of Patent: February 12, 1991
    Assignee: Eli Lilly and Company
    Inventor: D. Mark Gapinski
  • Patent number: 4983765
    Abstract: 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: Grant
    Filed: June 27, 1989
    Date of Patent: January 8, 1991
    Assignee: PAZ Arzneimittel-Entwicklungsgesellschaft mbH
    Inventors: Helmut Lukas, Otto Schuster, Gunther Rau
  • Patent number: 4970336
    Abstract: 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: Grant
    Filed: May 31, 1989
    Date of Patent: November 13, 1990
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yoshikazu Yoshioka, Isao Hashiba, Suketoshi Tsukamoto
  • Patent number: 4965405
    Abstract: 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: Grant
    Filed: February 27, 1989
    Date of Patent: October 23, 1990
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Susumu Funakoshi, Eigoro Murayama
  • Patent number: 4943310
    Abstract: 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: Grant
    Filed: December 16, 1988
    Date of Patent: July 24, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Alfred Angermann, Helga Franke, Gerhard Johann
  • Patent number: 4935543
    Abstract: 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: Grant
    Filed: May 18, 1989
    Date of Patent: June 19, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
  • Patent number: 4922015
    Abstract: 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: Grant
    Filed: April 6, 1988
    Date of Patent: May 1, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Breipohl, Jochen Knolle, Werner Stuber
  • Patent number: 4916147
    Abstract: 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: Grant
    Filed: June 21, 1986
    Date of Patent: April 10, 1990
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
  • Patent number: 4910337
    Abstract: .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: Grant
    Filed: January 27, 1989
    Date of Patent: March 20, 1990
    Assignee: Mine Safety Appliances Company
    Inventors: Kuen-Wai Chiu, Mary H. Staruch, David H. Ellenberger
  • Patent number: 4898864
    Abstract: 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: Grant
    Filed: October 27, 1987
    Date of Patent: February 6, 1990
    Assignee: L'Oreal
    Inventors: Jean Maignan, Gerard Lang, Gerard Malle, Philippe Vingler