Plural Rings Bonded Directly To The Same Carbonyl In Acid Moiety Patents (Class 560/52)
  • Publication number: 20020099090
    Abstract: This invention relates to compounds of the formula: 1
    Type: Application
    Filed: March 22, 2002
    Publication date: July 25, 2002
    Inventors: Timothy A. Ayers, Paul W. Brown
  • Patent number: 6369026
    Abstract: The present invention describes a fragrance delivery system which releases fragrant alcohols upon exposure to light. Said system comprises 2-benzoyl benzoates of general formulae which can comprise various subtituents R1-R5 as defined in the application and a substituted R* which is the organic part of a fragrant alcohol. In a further embodiment, the present invention describes a fragrance delivery system which releases fragrant aldehydes or ketones and/or fragrant compounds containing an olefin function.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: April 9, 2002
    Assignee: Firmenich SA
    Inventors: Jana Pika, Andreas Herrmann, Christian Vial
  • Patent number: 6297260
    Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: October 2, 2001
    Assignee: NitroMed, Inc.
    Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang
  • Patent number: 6235923
    Abstract: Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.
    Type: Grant
    Filed: January 25, 2000
    Date of Patent: May 22, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
  • Patent number: 6225494
    Abstract: Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.
    Type: Grant
    Filed: September 16, 1999
    Date of Patent: May 1, 2001
    Assignee: Allergan Sales, Inc.
    Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
  • Patent number: 6143918
    Abstract: Methods for preparing novel dibenzoylresorcinol-based compounds are disclosed, wherein the dibenzoylresorcinol is bonded to the residue of either an alcohol or a carboxylic acid group, via a methylene carboxylate linking group; and wherein the dibenzoylresorcinol is bonded directly to a substituted or unsubstituted aryl group which does not include a pendent hydroxyl group. The groups attached to the dibenzoylresorcinol may contain a wide variety of functional sites which permit further reaction, e.g., copolymerization. The described compounds are very useful as UV light absorbers and may be used to form improved coating compositions which usually include a transparent, polymeric matrix material. The coating compositions may be applied to various substrates, e.g., thermoplastics, to afford a selection of enhanced properties, such as UV light resistance and abrasion resistance.
    Type: Grant
    Filed: July 2, 1999
    Date of Patent: November 7, 2000
    Assignee: General Electric Company
    Inventors: James Edward Pickett, Wen P Liao, Amy Kathleen Simonian, Gregory Ronald Gillette
  • Patent number: 6133228
    Abstract: A fragrance delivery system which releases fragrant alcohols upon exposure to light. The system comprises 2-benzoyl benzoates of general formulae ##STR1## which can comprise various subtituents R.sub.1 -R.sub.5 as defined in the application and a substituted R* which is the organic part of a fragrant alcohol.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: October 17, 2000
    Assignee: Firmenich SA
    Inventors: Jana Pika, Andreas Herrmann, Christian Vial
  • Patent number: 6121255
    Abstract: A phloroglucide derivative having the following formula: ##STR1## wherein Q is halogen; X is CH.sub.2 or C.dbd.O; Y is cephalosporin having a formula of ##STR2## wherein Ph is phenyl, Ac is acetoxy, or pharmaceutically acceptable salts thereof, and an antibacterial pharmaceutical composition derived thereof.
    Type: Grant
    Filed: May 4, 1998
    Date of Patent: September 19, 2000
    Assignee: National Science Council
    Inventors: Jih Ru Hwu, Shwu-Chen Tsay, Gholam H. Hakimelahi, Chun Chieh Lin, Wen Nan Tseng, Ali A. Moshfegh, Abdolmajid Azaripour, Hasan Mottaghian
  • Patent number: 6110955
    Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and particularly augmenting expression of a tumor suppressor gene, inducing tolerance to an antigen and treating, ameliorating or preventing protozoan infection. The methods of the invention use metabolically stabilized oxyalkylene esters.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: August 29, 2000
    Assignee: Beacon Laboratories, Inc.
    Inventors: Abraham Nudelman, Ada Rephaeli, Edward Neiss, Bernard Loev
  • Patent number: 6107517
    Abstract: Thyroid hormone analogues are disclosed. Methods of using such analogues and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: August 22, 2000
    Assignee: The Regents of the University of California
    Inventors: Thomas S. Scanlan, Hikari A.I. Yoshihara, Grazia Chiellini, Timothy J. Mitchison
  • Patent number: 6096920
    Abstract: Palladium-catalyzed arylation of an olefin (e.g., ethylene) with an aromatic halide (e.g., 2-bromo-6-methoxynaphthalene, m-bromobenzophenone, or 4-isobutyl-1-bromobenzene) is conducted in specified media. After a special acid or base phase separation procedure, palladium-catalyzed carbonylation of the olefinically-substituted aromatic intermediate is conducted in specified media using CO and water or an alcohol to form arylalkylcarboxylic acid or ester or substituted arylalkylcarboxylic acid or ester (e.g., racemic 2-(6-methoxy-2-naphthyl)propionic acid, 2-(3-benzoylphenyl)propionic acid, or 2-(4-isobutylphenyl)propionic acid). Catalyst recovery procedures enabling recycle of catalyst residues and efficient recovery of amine hydrogen halide scavenger and solvent used in the arylation reaction are described, as well as novel, highly efficient methods of conducting the carbonylation reaction.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: August 1, 2000
    Assignee: Albemarle Corporation
    Inventors: Robert H. Allen, R. Carl Herndon, Jr., Kannappan C. Chockalingam, W. Dirk Klobucar, Gary D. Focht, Tse-Chong Wu, Gary D. Heidebrecht, Joseph D. McLean, Yaping Zhong, Thorsten W. Brockmann, Ronny W. Lin, William J. Layman, Jr., Ranjit K. Roy
  • Patent number: 6063815
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein Y is ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl mono-, di- or tri-substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy;R.sup.3 and R.sup.4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, hydroxyalkanoyl of 1-6 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, aminoalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, alkylsulfanyl of 1-6 carbon atoms, nitrile, nitro, amino, --NHSO.sub.2 CF.sub.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 16, 2000
    Assignee: American Home Products Corporation
    Inventor: Paul J. Dollings
  • Patent number: 6054457
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: April 25, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
  • Patent number: 6037488
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.
    Type: Grant
    Filed: April 19, 1997
    Date of Patent: March 14, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
  • Patent number: 6027747
    Abstract: A process for the production of a solid dispersion of at least one therapeutic agent in a hydrophilic carrier having enhanced solubility in an aqueous media comprising dissolving at least one therapeutic agent in a volatile organic solvent containing a very hydrophilic polymer and evaporating the solvent to dryness; to form a co-precipitate of therapeutic agent and hydrophilic polymer. This invention relates to the resulting products and to their therapeutic method of use.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: February 22, 2000
    Inventors: Didier Terracol, Roselyne Duclos
  • Patent number: 5945557
    Abstract: Compounds with fungicidal and insecticidal properties having formula ##STR1## wherein A is N or CH; V is O or NH; m and n are the integers 0 and 1, provided that m+n is 0 or 1;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4)alkoxy;R is independently selected from hydrogen, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.12)alkenyl, (C.sub.2 -C.sub.12)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.12)alkenyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.12)alkynyl, (C.sub.1 -C.sub.12)alkyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.12)alkenyl(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.12)alkynyl(C.sub.3 -C.
    Type: Grant
    Filed: June 23, 1998
    Date of Patent: August 31, 1999
    Assignee: Rohm and Haas Company
    Inventors: Ronald Ross, Ted Tsutomu Fujimoto, Steven Howard Shaber
  • 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: 5883125
    Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein A is N or CH; V is O or NH; m and n are integers 0 and 1 provided that m+n is 1;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, and (C.sub.1 -C.sub.4) alkoxy;R is independently selected from, (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8) alkenyl, (C.sub.2 -C.sub.8)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7) cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl, aralkyl, and heterocyclic moieties;R is independently selected from (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8) alkenyl, (C.sub.2 -C.sub.8)alkynyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7) cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.4)alkyl, aryl, aralkyl, and heterocyclic;R.sub.1 and R.sub.2 are independently selected from hydrogen, (C.sub.1 -C.sub.6)alkyl, halo(C.sub.1 -C.sub.
    Type: Grant
    Filed: June 2, 1997
    Date of Patent: March 16, 1999
    Assignee: Rohm and Haas Company
    Inventors: Ronald Ross, Ted Tsutomu Fujimoto, Steven Howard Shaber
  • Patent number: 5863688
    Abstract: The present invention provides a naphthoquinone derivative represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are as defined in the specification. An electrophotosensitive material containing this naphthoquinone derivative as an electron transferring material has high sensitivity.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: January 26, 1999
    Assignee: Mita Industrial Co., Ltd
    Inventors: Yukimasa Watanabe, Sakae Saito, Hirofumi Kawaguchi, Akiyoshi Urano, Fumio Sugai, Atsushi Fujii, Yasufumi Mizuta, Toshiyuki Fukami, Ichiro Yamazato, Yuji Tanaka, Eiichi Miyamoto, Hideo Nakamori, Mitsuo Ihara
  • Patent number: 5801272
    Abstract: A mixture of (R)- and (S)-2-(4-alkanoylphenoxy)- or (R)- and (S)-2-(4-aroylphenoxy)propionic esters I ##STR1## with an enantiomeric excess of at least 90% is prepared by reacting a mixture of (R) and (S) enantiomer of a 2-phenoxypropionic ester II ##STR2## in which the appropriate (R) or (S) isomer is present in excess, with a carboxylic acid derivative of the formula IIIR.sup.1 --CO--X III,(X=OH, halogen, R.sup.1 COO or sulfonyloxy)in the presence of a Friedel-Crafts catalyst.The (R)- or (S)-2-(4-alkanoylphenoxy)propionic esters and (R)- or (S)-2-(4-hydroxyphenoxy)propionic esters are used for preparing crop protection agents and drugs.
    Type: Grant
    Filed: August 11, 1995
    Date of Patent: September 1, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Siegel, Hubert Sauter, Gerhard Schaefer
  • Patent number: 5716954
    Abstract: Benzo or pyridopyridazinones and pyridazinthiones of the formula ##STR1## wherein: X and Y are nitrogen or carbon, provided that at least one is carbon, and Z is oxygen or sulfur;R.sup.1 is hydrogen, lower alkyl, aryl, aralkyl, heterocyclo, heterocyclo lower-alkyl, heteroaryl, or heteroaralkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from hydrogen, lower alkyl, halo, carboxy, alkoxycarbonyl, carbamoyl, lower-alkyl carbonyl, halocarbonyl, thiomethyl, trifluoromethyl, cyano or nitro;or a pharmaceutically acceptable ester, ether or salt thereof, have been found to be useful as an anti-inflammatory, antasthmatic, immunosuppressive, anti-allograft rejection, anti-graft-vs-host rejection, autoimmune disease or analgetic agent(s).
    Type: Grant
    Filed: January 5, 1995
    Date of Patent: February 10, 1998
    Assignee: Syntex U.S.A. Inc.
    Inventors: Robert S. Wilhelm, Bradley E. Loe, Bruce H. Devens, Robert Alvarez, Michael G. Martin
  • Patent number: 5663412
    Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;R.sub.3 is --COOH or --COOR.sub.4 ;R.sub.4 has 1 to 6 carbon atoms;A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents.A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: September 2, 1997
    Assignee: Albany Molecular Research, Inc.
    Inventor: Thomas E. D'Ambra
  • 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: 5492917
    Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: February 20, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
  • Patent number: 5488134
    Abstract: This invention relates to a process for preparation of the compounds of lignan series in a regioselective manner. This invention provide a process for preparing a compound of the formula (I):which process is characterized by that a lactone compound represented by the formula (II) is allowed to react with a compound of the formula: R.sup.7 Cl in the presence of a base, then the resulting compound is subjected to addition reaction with an acetylenic compound of the formula (III), then the resulting compound is reduced;in which R.sup.1 is alkyl, cycloalkyl, cycloalkyl lower alkyl, or aralkyl and the like; R.sup.2 and R.sup.3 each is lower alkoxy and the like; R.sup.4 is lower alkoxy or hydrogen; and R.sup.5 and R.sup.6 each is lower alkyl; and R.sup.7 is tri(lower alkyl)silyl.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: January 30, 1996
    Assignee: Shionogi & Co., Ltd.
    Inventors: Sachio Mori, Shozo Takechi, Shiro Kida
  • Patent number: 5468904
    Abstract: A fluorine-containing benzophenone derivative of the formula (1), (2) or (3):.PHI..sup.1 (--X.sup.1 --Q.sup.1 --R.sub.f.sup.1).sub.n (1).PHI..sup.2 --X.sup.2 --Q.sup.2 --R.sub.f.sup.2 --Q.sup.3 --X.sup.3 --.PHI..sup.3 (2).PHI..sup.4 --X.sup.4 --Q.sub.f --X.sup.5 --.PHI..sup.5 (3)wherein .PHI..sup.1 is a 2-hydroxybenzophenone structure of the formula ka-1: ##STR1## (wherein Y is a hydrogen atom or a hydroxyl group, each of k and m indicates the number of bond sites, k is an integer of from 0 to 3, and m is an integer of from 0 to 3, provided that 1.ltoreq.(k+m).ltoreq.4), n corresponds to (k+m) and is an integer of from 1 to 4, each of .PHI..sup.2, .PHI..sup.3, .PHI..sup.4 and .PHI..sup.5 is a 2-hydroxybenzophenone structure of the formula ka-1 wherein (k+m) is 1, each of X.sup.1, X.sup.2, X.sup.3, X.sup.4 and X.sup.5 is a single bond or an oxygen atom, Q.sup.1 is a single bond or a bivalent linking group having a carbon atom directly bonded to X.sup.1, each of Q.sup.2 and Q.sup.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: November 21, 1995
    Assignee: Asahi Glass Company Ltd.
    Inventors: Ryoko Osawa, Takashige Maekawa, Tatsuo Momii, Satoshi Kamata
  • 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: 5334607
    Abstract: Antimycotics containing a compound of the formula ##STR1## where .dbd.Y is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, .dbd.CH--SCH.sub.3 or .dbd.N--OCH.sub.3, and X is oxygen, or X may also be NH if Y is .dbd.N--OCH.sub.3,Z is halogen, nitro, cyano, unsubstituted or substituted organic radicals, OR.sup.12, SR.sup.13, SOR.sup.14, SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22 R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--N.dbd.CR.sup.27 R.sup.28 andU, V, W can be hydrogen or one of the meanings given for Z, or where two of Z, U, V and W in adjacent positions on the phenyl ring can form an unsubstituted or substituted five- or six-membered, aromatic or aliphatic ring which may contain one to three hetero atoms (N, S, O), and R.sup.12 to R.sup.26 are identical or different and are hydrogen, unsubstituted or substituted organic radicals,are used for controlling mycoses.
    Type: Grant
    Filed: May 28, 1992
    Date of Patent: August 2, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Hubert Sauter, Gisela Lorenz, Gerd Steiner, Bernd Janssen, Timm Anke, Wolfgang Steglich
  • Patent number: 5322794
    Abstract: Fluorescence probes are described comprising coronene fluorophores chemically attached to lipids or membrane-mimetic molecules via hydrocarbon spacers of defined length. Also described is a method for determining lipid packing and dynamics in membranes, a method for estimating hydrodynamic properties of macromolecules and macromolecular complexes, and a method for measuring changes in Ca.sup.+2 concentrations in or near membranes.
    Type: Grant
    Filed: February 16, 1993
    Date of Patent: June 21, 1994
    Inventor: Lesley Davenport
  • Patent number: 5310757
    Abstract: Derivatives of 3,3,5-trimethylcyclohexanol methyl-2-propionate, preparation method, and therapeutical compositions containing them. Such derivatives have general formula (I).
    Type: Grant
    Filed: January 16, 1992
    Date of Patent: May 10, 1994
    Assignee: Panmedica
    Inventors: Claude Laruelle, Marcel Lepant
  • Patent number: 5302751
    Abstract: A process is disclosed that is useful for separating the enantiomers of a racemic mixture of an aliphatic carboxylic acid having the formula ##STR1## where R.sub.1 is hydrogen or alkyl, R.sub.2, R.sub.3 and R.sub.4 are independently different and are hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, substituted heteroaryl, haloalkyl, alkoxyalkyl, alkylthioalkyl, phenylalkyl, substituted phenylalkyl, heteroalkylalkyl, substituted heteroalkylalkyl or cycloalkylalkyl.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: April 12, 1994
    Assignee: Ethyl Corporation
    Inventors: Thanikavelu Manimaran, Alicia A. Potter
  • Patent number: 5288742
    Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    Type: Grant
    Filed: March 18, 1992
    Date of Patent: February 22, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Philip N. Edwards, David Waterson
  • Patent number: 5242996
    Abstract: A modified epoxy resin or compound of the formula: ##STR1## wherein A is the backbone reside of a glycidyl ether epoxy resin with removal of the glycidyloxy groups; R.sup.1 and R.sup.2 are independently a hydrogen atom or C.sub.1 -C.sub.12 alkyl; R.sup.3 is a glycidyl group; and n is an integer of greater than 1. A method for producing the modified epoxy resin is also disclosed.
    Type: Grant
    Filed: May 22, 1991
    Date of Patent: September 7, 1993
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Mitsuo Yamada, Kei Aoki, Ryuzo Mizuguchi
  • Patent number: 5196564
    Abstract: A novel compound of the formula (I): ##STR1## wherein R.sub.1 is esterified 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: February 27, 1991
    Date of Patent: March 23, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Kanamaru, Tsuneaki Hida, Masayuki Muroi
  • Patent number: 5182301
    Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.
    Type: Grant
    Filed: February 21, 1991
    Date of Patent: January 26, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
  • Patent number: 5179097
    Abstract: Novel choline salts of non-steroidal anti-inflammatory carboxylic acids and anti-lipidemic carboxylic acids are described. Additionally, blends of choline salts with the above carboxylic acids are also described. The new salts and compositions offer new therapeutic advantages.
    Type: Grant
    Filed: June 10, 1991
    Date of Patent: January 12, 1993
    Inventor: Isaac A. Angres
  • Patent number: 5177250
    Abstract: A process is disclosed for the enantioselective hydrogenation of olefins of the formula ##STR1## where R is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, Z is ##STR2## where R' is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, --CN, C(NH)OR" where R" is C.sub.1 to C.sub.6 linear or branched alkyl, or --C(O)NH.sub.2 ; and Ar is phenyl or naphthyl unsubstituted or substituted with benzoyl or substituted benzoyl, C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched alkoxy, halo, or carboxylic acid or C.sub.1 to C.sub.6 linear or branched alkyl ester thereof, which comprises contacting said aromatic-substituted olefin with a catalytically effective amount of a ruthenium phosphite complex.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: January 5, 1993
    Assignee: Ethyl Corporation
    Inventor: Kathleen S. Laurenzo
  • Patent number: 5175339
    Abstract: A process for producing a dialkyl ester (i.e. BTDE) from its corresponding dianhydride (i.e., BTDA) comprising mixing the dianhydride, an organic solvent, solid catalyst and an alcohol capable of reacting with the dianhydride stirring the solution until the dianhydride and alcohol have reacted to form the dialkyl ester, separating the dialkyl ester from the catalyst and drying the ester to form a solid paticulate product. The product has a purity of over 85%.
    Type: Grant
    Filed: May 14, 1990
    Date of Patent: December 29, 1992
    Assignee: The Standard Oil Company
    Inventors: Eduard P. Babayan, Douglas G. Soden, Anthony Bosch
  • 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: 5152826
    Abstract: An herbicide compound of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 alkoxy, nitro; cyano; C.sub.1 -C.sub.2 haloalkyl, or R.sup.a SO.sub.n -- wherein n is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are alkylene having 2 to 5 carbon atoms;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.3 and R.sup.4 together are oxo;R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.5 and R.sup.6 together are alkylene having 2 to 5 carbon atoms;R.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n --wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.
    Type: Grant
    Filed: October 16, 1991
    Date of Patent: October 6, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventor: Christopher G. Knudsen
  • 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: 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: 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: 5039308
    Abstract: Additives which improve the low-temperature properties of distillate fuels are the reaction products of (1) diaminodiols, and (2) the product of benzophenone tetracarboxylic dianhydride and aminoalcohols and/or amines with long-chain hydrocarbyl groups attached.
    Type: Grant
    Filed: December 13, 1989
    Date of Patent: August 13, 1991
    Assignee: Mobil Oil Corporation
    Inventors: David J. Baillargeon, Angeline B. Cardis, Dale B. Heck
  • Patent number: 5025017
    Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.
    Type: Grant
    Filed: September 28, 1989
    Date of Patent: June 18, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky