C-o- Group In R Patents (Class 514/622)
  • Patent number: 5948418
    Abstract: Novel sulfhydryl group-containing amides and disulfide group-containing bis-amides useful for treating or preventing an abnormal biological condition or a disease, and/or improving the texture or appearance of the skin, as well as compositions containing amides and bis-amides and methods for their use are described. Such types of abnormal biological conditions or diseases include skin atrophy, i.e., the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells, and other maladies including, but are not limited to dry skin, severe dry skin, dandruff, acne, keratoses, psoriasis, eczema, skin flakiness, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses, age-related skin changes and skin in need of cleansers.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: September 7, 1999
    Assignee: Estee Lauder, Inc.
    Inventors: Daniel H. Maes, Jules Zecchino, Althea Knight
  • Patent number: 5948819
    Abstract: An .alpha.-substituted phenylacetic acid derivative useful as an agricultural fungicide, represented by general formula (I), or a salt thereof, a process for producing the same, an intermediate for the production thereof, and an agricultural fungicide containing the same as the active ingredient, wherein R.sup.1 represents halogen, alkyl, OH, alkylthio, alkylsulfinyl, alkylsulfonyl, amino or nitro; Q represents aryl, heterocycle, mono- or disubstituted methyleneamino, (substituted amino-)methyl, alkyl, alkenyl, alkynyl, substituted carbonyl or substituted sulfonyl; X represents hydrogen, halogen, alkyl or OH; Y represents OH, alkylthio or amino; Z represents oxygen or sulfur; M represents oxygen, S(O)i (i being 0, 1 or 2), NR.sup.2 (R.sup.2 being hydrogen, alkyl or acyl) or a single bond; and n represents 0, 1 or 2.
    Type: Grant
    Filed: October 7, 1996
    Date of Patent: September 7, 1999
    Assignee: Shionogi & Co., Ltd
    Inventors: Toshikazu Ohtsuka, Takami Murashi, Shinji Suzuki, Michio Masuko, Hideyuki Takenaka
  • Patent number: 5932618
    Abstract: Compounds having utility as anti-viral agents in general and, more specifically, to methods for treating a viral condition in an animal are disclosed. The compounds are naphthalene derivatives, and are preferably administered to the patient in the form of a pharmaceutical composition. Viruses treatable by the methods of this invention include viruses of the herpes virus family, such as cytomegalovirus, herpes simplex virus and human lymphotrophic herpes virus.
    Type: Grant
    Filed: November 4, 1996
    Date of Patent: August 3, 1999
    Assignee: Signal Pharmaceuticals, Inc.
    Inventors: Carla M. Suto, Jun Wu, Leah M. Gayo
  • Patent number: 5929117
    Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: July 27, 1999
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire
  • Patent number: 5929119
    Abstract: A composition which is suitable for controlling fungal pests, comprising conventional additives and an effective amount of a p-hydroxyaniline derivative of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted bicycloalkyl, unsubstituted or substituted bicycloalkenyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy,and a liquid or solid carrier, its use, the use of the compounds I for controlling fungal pests, and the use of the compounds I for the preparation of the compositions.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: July 27, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5922771
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
  • Patent number: 5916922
    Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: November 24, 1997
    Date of Patent: June 29, 1999
    Assignee: Eli Lilly and Company
    Inventors: Theodore Goodson, Jr., Richard Waltz Harper, David Kent Herron
  • Patent number: 5910512
    Abstract: A water-based topical analgesic and method of application wherein the analgesic contains capsicum, capsicum oleoresin and/or capsaicin. This analgesic is applied to the skin to provide relief for rheumatoid arthritis, osteoarthritis, and the like.
    Type: Grant
    Filed: August 2, 1996
    Date of Patent: June 8, 1999
    Assignee: Healthline Laboratories, Inc.
    Inventor: Dale Conant
  • Patent number: 5908861
    Abstract: The present invention is directed to a method for treating inflammation or inflammatory disease in an animal or mammal, which comprises the steps of administering an effective amount of an pADPRT inhibitory compound to said animal or mammal.
    Type: Grant
    Filed: May 13, 1997
    Date of Patent: June 1, 1999
    Assignee: Octamer, Inc.
    Inventor: Ernestt Kun
  • Patent number: 5891918
    Abstract: A method for controlling phytopathogenic fungi is disclosed. The method uses a fungicidal composition which has been found to be effective against strains of fungi which are resistant to benzimidazole fungicides. When combined with one or more of benzimidazole, thiophanate, or dicarboximide fungicides, and applied to a mixed population of sensitive and resistant fungi, the fungicidal compound of the present invention is more effective against the mixed population of fungi than either of the fungicidal compounds alone.
    Type: Grant
    Filed: June 18, 1997
    Date of Patent: April 6, 1999
    Assignee: Rohm and Haas Company
    Inventors: Enrique Luis Michelotti, David Hamilton Young, James Allen Quinn
  • Patent number: 5889059
    Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sub.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: March 30, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5886046
    Abstract: This invention relates to chemical compounds that contain adjacent carbonyl groups, which effectively inhibit the biological, chemical, and/or physical properties of enzymes and other medicinally-significant proteins. In particular, the invention relates to dicarbonyl compounds that are capable of acting as enzyme inhibitors, including irreversible inhibitors of HIV-1 protease.
    Type: Grant
    Filed: January 19, 1996
    Date of Patent: March 23, 1999
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Ralph F. Hirschmann, Amos B. Smith, III, Paul Sprengeler, Wenqing Yao, Paul Anderson
  • Patent number: 5883133
    Abstract: Compounds of the formula I ##STR1## are described in which at least one of the substituents R(1), R(2), R(3), R(4) and R(5) is a nitrogen-containing heterocyclic radical. They are outstanding cardiovascular therapeutic agents. They are obtained by reaction of a compound II ##STR2## with guanidine.
    Type: Grant
    Filed: July 24, 1996
    Date of Patent: March 16, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Udo Albus, Wolfgang Scholz
  • Patent number: 5866610
    Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them.Described are benzoylguanidines of the formula I ##STR1## where R(1) to R(3) are H, Hal, (cyclo)alkyl, N.sub.3, CN or OH, alkyloxy, phenyl, phenoxy or benzoyl, and their pharmacologically acceptable salts, but with the exception of the compounds benzoylguanidine, 4-chlorobenzoylguanidine, 3,4-dichlorobenzoylguanidine and 3- or 4-methylbenzoylguanidine.They are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group.
    Type: Grant
    Filed: July 18, 1996
    Date of Patent: February 2, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Andreas Weichert, Heinz-Werner Kleemann, Jan-Robert Schwark, Wolfgang Scholz, Udo Albus
  • Patent number: 5856354
    Abstract: The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: January 5, 1999
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
  • Patent number: 5849775
    Abstract: Benzoylguaridines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: December 15, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5840761
    Abstract: Alkylbenzoylguanidines of the formula I ##STR1## in which A, R.sup.1, R.sup.2 and R.sup.3 have the given meanings, and their physiologically harmless salts exhibit antiarrhythmic properties and act as inhibitor of the cellular Na.sup.+ /H.sup.+ antiporter.
    Type: Grant
    Filed: August 30, 1995
    Date of Patent: November 24, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Rolf Gericke, Dieter Dorsch, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
  • Patent number: 5834468
    Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.
    Type: Grant
    Filed: July 2, 1996
    Date of Patent: November 10, 1998
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Patent number: 5801195
    Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.
    Type: Grant
    Filed: December 30, 1994
    Date of Patent: September 1, 1998
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire, David I. Stirling
  • Patent number: 5789431
    Abstract: The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: ##STR1## where R.sub.1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX where m is 2 or 3 and X is H, methyl, or ethyl; R.sub.2 is halo or NHY, where Y is hydrogen, lower alkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R.sub.3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX, where m and X are as defined for R.sub.1 above; and R.sub.4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.
    Type: Grant
    Filed: February 16, 1996
    Date of Patent: August 4, 1998
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Sheng-Chu Kuo, Toshiro Ibuka
  • Patent number: 5773469
    Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: June 30, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
  • Patent number: 5750783
    Abstract: Benzyloxy-substituted phenylglycinolamides are prepared by reaction of benzyloxy-substituted phenylacetic acids with phenylglycinols. The benzyloxy-substituted phenylglycinolamides are suitable as active compounds in medicaments, in particular in medicaments for the treatment of atherosclerosis.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: May 12, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Ulrich Muller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Martin Beuck
  • Patent number: 5747541
    Abstract: The present invention relates to substituted benzoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and medicament comprising them.
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: May 5, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
  • Patent number: 5747539
    Abstract: Fluorine-containing benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated, and their physiologically acceptable salts, have antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter, for example.
    Type: Grant
    Filed: May 15, 1996
    Date of Patent: May 5, 1998
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Dieter Dorsch, Manfred Baumgarth, Rolf Gericke, Klaus-Otto Minck, Norbert Beier
  • Patent number: 5747540
    Abstract: Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 21, 1996
    Date of Patent: May 5, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Craig A. Coburn, Randall W. Hungate, Richard C. A. Isaacs, Joseph P. Vacca, Mary Beth Young
  • Patent number: 5739140
    Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: April 14, 1998
    Assignee: Monsanto Company
    Inventors: William P. Clinton, Jim I. McLoughlin, Anita E. Otal, John J. Parlow, Dennis P. Phillion, Ajit S. Shah
  • Patent number: 5736570
    Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: April 7, 1998
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire, David I. Stirling
  • Patent number: 5733935
    Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: March 31, 1998
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
  • Patent number: 5731352
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: March 24, 1998
    Assignee: Adir Et Compagnie
    Inventors: Daniel Lesieur, Veronique Leclerc, Patrick Depreux, Philippe Delagrange, Pierre Renard
  • Patent number: 5728737
    Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 23, 1997
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 5710314
    Abstract: Compounds of formula I ##STR1## and possible isomers and isomeric mixtures thereof, wherein a)X is CH.sub.2 F or CHF.sub.2 ;Y is CH andZ is OMe, orb)X is CH.sub.2 F or CHF.sub.2 ;Y is a nitrogen atom andZ is OMe or NHCH.sub.3,and wherein alsom is 0, 1, 2, 3, 4 or 5 andU represents identical or different substituents selected from halogen, cyano, nitro, C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkenyloxyiminomethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxyiminomethyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy and unsubstituted or substituted benzyl or represents substituents at two adjacent positions of the phenyl ring of formula I that define a fused hydrocarbon bridge so as to form a larger hydrocarbon ring having up to 14 carbon atoms, are suitable for controlling and preventing microorganisms, insects and Acarina on plants.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: January 20, 1998
    Assignee: Novartis Corporation
    Inventors: Albert Pfiffner, Stephan Trah
  • Patent number: 5708033
    Abstract: A compound of formula (I), wherein R.sup.1 and R.sup.2 are independently selected from chloro, fluoro, bromo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 haloalkyl provided that both R.sup.1 and R.sup.2 are not fluoro; R.sup.3 and R.sup.4 are independently selected from hydrogen and C.sub.1-6 alkyl, and pharmaceutically acceptable salts, solvates or physiologically functional derivatives thereof, their use in medicine, particularly the phrophylaxis or treatment of conditions associated with inflammation, arthritis, or pain, pharmaceutical compositions comprising them, and processes for their preparation are disclosed.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: January 13, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: James Leroy Kelley, David Lee Musso
  • Patent number: 5705528
    Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: January 6, 1998
    Assignee: Ramot University Authority for Applied Research & Industrial Development
    Inventor: Yoel Kloog
  • Patent number: 5691376
    Abstract: A compound of the following structure: ##STR1## wherein R.sub.8 =H: R.sub.1 =alkyl, cycloalkyl, arylalkyl, aryl;R.sub.2 =cycloalkyl, aryl, C.sub.3 -C.sub.10 alkyl;X,Y=O, S(O).sub.n, NH;Z=CO.sub.2 R.sub.3, C(O)CO.sub.2 R.sub.3, CH(OH)CO.sub.2 R.sub.3, CHFCO.sub.2 R.sub.3, CF.sub.2 CO.sub.2 R.sub.3, CONR.sub.3 R.sub.4, CONR.sub.3 OR.sub.4, CONR.sub.3 NR.sub.4 R.sub.5, 1-tetrazole, C(O)CONR.sub.3 R.sub.4, CH(OH)CONR.sub.3 R.sub.4, CF.sub.2 CONR.sub.3 R.sub.4R.sub.3, R.sub.4, R.sub.5 =hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl;halo=Cl, Br, or I;fluoroalkyl=CF.sub.3, CHF.sub.2, CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5 ;cycloalkyl=C.sub.3 -C.sub.6 cycloalkyl;arylalkyl=C.sub.1 -C.sub.4 alkyl aryl;aryl=phenyl, furanyl, thienyl, or pyridyl; andn=0-2;or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, and allergic and inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.
    Type: Grant
    Filed: October 17, 1996
    Date of Patent: November 25, 1997
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Caggiano, Joseph Prol, Jr.
  • Patent number: 5683705
    Abstract: Novel sulfhydryl group-containing amides and disulfide group-containing bis-amides useful for treating or preventing an abnormal biological condition or a disease, and/or improving the texture or appearance of the skin, as well as compositions containing amides and bis-amides and methods for their use are described. Such types of abnormal biological conditions or diseases include skin atrophy, i.e., the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells, and other maladies including, but are not limited to dry skin, severe dry skin, dandruff, acne, keratoses, psoriasis, eczema, skin flakiness, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses, age-related skin changes and skin in need of cleansers.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: November 4, 1997
    Assignee: Estee Lauder, Inc.
    Inventors: Daniel H. Maes, Jules Zecchino, Althea Knight
  • Patent number: 5679712
    Abstract: Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: October 21, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5677303
    Abstract: Enolethers and thioenolethers of formula I ##STR1## are disclosed. The compounds are useful for combatting phytopathogenic fungi.
    Type: Grant
    Filed: June 20, 1996
    Date of Patent: October 14, 1997
    Assignee: American Cyanamid Company
    Inventors: Juergen Curtze, Guido Albert
  • Patent number: 5677333
    Abstract: A method for controlling phytopathogenic fungi comprises applying a selected fungicidally active N-acetonylbenzamide compound and a second fungicidally active compound selected from the group consisting of manganese-zinc ethylenebis(dithiocarbamate), manganese ethylenebis(dithiocarbamate), zinc ammoniate ethylenebis(dithiocarbamate), zinc ethylenebis(dithiocarbamate), 2-cyano-N-((ethylamino)carbonyl)-2-(methoxyimino)acetamide, and (E,Z) 4-(3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)acryloyl)morpholine to plant seed, to plant foliage or to a plant growth medium and provides higher fungicidal activity than separate use of the same compounds.
    Type: Grant
    Filed: July 8, 1996
    Date of Patent: October 14, 1997
    Assignee: Rohm and Haas Company
    Inventors: Daniel Louis Loughner, Enrique Luis Michelotti, Willie Joe Wilson, David Hamilton Young
  • Patent number: 5670546
    Abstract: N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: September 23, 1997
    Assignee: Korean Research Institute of Chemical Technology
    Inventors: No-Sang Park, Young-Sik Jung, Churl-Min Seong, Jong-Cheol Lee, Jin-Il Choi, Seung-Won Choi, Yeon-Joo Choi, Kwang-Sook Lee
  • Patent number: 5667792
    Abstract: A cosmetic or dermatological composition with a depigmenting action comprises derivatives of 2,5-dihydroxyphenylcarboxylic acids, their homologs, and their salts, with the derivatives having the following structural formula: ##STR1## wherein: R.sub.1 represents OR.sub.5, OH, or ##STR2## R.sub.5 is a linear or branched C.sub.1 -C.sub.20 alkyl radical, a linear or branched C.sub.2 -C.sub.20 alkenyl radical, or a C.sub.1 -C.sub.20 alkyl radical substituted by one or more hydroxy or alkoxy groups;r' and r", identical or different, represent a hydrogen atom, a C.sub.1 -C.sub.20 alkyl radical, a C.sub.2 -C.sub.6 hydroxyalkyl radical, or a C.sub.3 -C.sub.6 polyhydroxyalkyl, or r' and r" taken together, with the nitrogen atom, form a heterocycle;the number of carbon atoms in the --(CH.sub.2).sub.n --COR.sub.1 chain is less than or equal to 21;R.sub.2 and R.sub.3, identical or different, represent a hydrogen atom, a linear or branched C.sub.1 -C.sub.4 alkyl radical, or a C.sub.1 -C.sub.4 alkoxy; R.sub.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: September 16, 1997
    Assignee: L'Oreal
    Inventors: Alex Junino, Alain Lagrange, Quang Lan N'Guyen, Marie-Alix Bourboulon
  • Patent number: 5661178
    Abstract: The present invention provides a method of effecting vasodilation, comprising:administering to a warm blooded animal in need of such treatment, an effective amount of a (1,5-inter) aryl prostaglandin derivative represented by the Formula I ##STR1## wherein n is 0 or an integer of from 1 to 6, R is selected from the group of radicals represented by the formulae:CO.sub.2 R', CONR'.sub.2, CH.sub.2 OR' and SO.sub.2 NR'.sub.2'wherein R' is hydrogen or a lower alkyl radical having from one to six carbon atoms; R" is hydrogen or an acyl radical having the formula (CO)R'" wherein R'" is a saturated or unsaturated acyclic hydrocarbon radical having from 1 to about 10 carbon atoms, or --(CH.sub.2).sub.m R"" wherein m is 0 or an integer of from 1 to 6 and R"" is an aliphatic ring having from 3 to 7 carbon atoms or an aryl group, e.g. phenyl, or a heteroaryl group, e.g.
    Type: Grant
    Filed: September 1, 1995
    Date of Patent: August 26, 1997
    Assignee: Allergan
    Inventors: June Chen, Robert M. Burk, David F. Woodward
  • Patent number: 5654329
    Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5 R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CH(OR.sub.9 O), --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 5, 1997
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5646184
    Abstract: Disclosed is a preparation for external application to the skin characterized by containing at least one of benzoic acid derivatives represented by formula (I) or pharmacologically acceptable salts thereof as an active ingredient, the preparation having sufficient sebaceous secretion inhibitory activity with no substantial side effect and high safety for human body. ##STR1## wherein R.sup.1 represents --OH, --OR.sup.3 or --NHR.sup.3 ; R.sup.2 represents a hydrogen atom, a lower alkyl group or a lower acyl group; R represents --O--R.sup.4 or ##STR2## R.sup.3 represents an alkyl group, an alkenyl group or a hydroxyalkyl group; R.sup.4 represents a straight-chain or branched, saturated or mono-unsaturated alkyl group or cycloalkylalkyl group having from 4 to 10 carbon atoms; X represents --O-- or --NH--; and n represents 1 or 2.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: July 8, 1997
    Assignee: Kao Corporation
    Inventors: Akira Sakaguchi, Takashi Kitahara, Keiko Koizumi, Noriko Sato, Kimihiko Hori, Hiroyuki Shinta
  • Patent number: 5643943
    Abstract: Methods for treating vascular inflammatory pathologies are disclosed. Particularly, the methods utilize pharmaceutical compositions containing certain compounds having an anti-inflammatory and anti-oxidant moiety covalently linked by an amide or ester bond. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 1, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Daniel A. Gamache, Mark R. Hellberg, Jon C. Nixon, Gustav Graff
  • Patent number: 5633282
    Abstract: The use of a poly(ADP-ribose) polymerase inhibitor for the treatment of a subject against infection by a virus, in which the viral or proviral DNA integrates into the chromosome or chromosomes during its replication cycle.
    Type: Grant
    Filed: September 8, 1994
    Date of Patent: May 27, 1997
    Assignee: British Technology Group Limited
    Inventors: Mary K. L. Collins, Farzin Farzaneh, Sydney Shall, Manoochehr Tavassoli
  • Patent number: 5629346
    Abstract: Certain N-acetonylbenzamides exhibit low toxicity to plants are particularly useful for control of fungi, especially Phycomycetes.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 13, 1997
    Assignee: Rohm and Haas Company
    Inventors: H. Edwin Carley, Ashok K. Sharma, Colin Swithenbank
  • Patent number: 5591776
    Abstract: Rolipram-based PDE IV inhibitors containing phenyl- or benzyl-substituted moieties of the formula: ##STR1## wherein X.sub.1 and X.sub.2 may be the same or different and each is O or S;R.sub.1 is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C.sub.2-12 alkyl groups, cycloalkyl and cycloalkyl-alkyl groups containing from 3 to 10 carbon atoms in the cycloalkyl moiety;R.sub.2 =R.sub.1 or --CH.sub.3 ;R.sub.3 is hydrogen, halogen, or a saturated or unsaturated straight-chain or branched C.sub.1-12 alkyl group, a cycloalkyl or cycloalkyl-alkyl groups containing from 3 to 7 carbon atoms in the cycloalkyl moiety;Z is a linkage selected from --CH.sub.2 CONH-- or --CH.sub.2 NHCO--, andR.sub.
    Type: Grant
    Filed: January 10, 1995
    Date of Patent: January 7, 1997
    Assignee: Euro-Celtique, S.A.
    Inventors: David J. Cavalla, Lloyd J. Dolby, Mark Chasin
  • Patent number: 5571844
    Abstract: The invention relates to amidinophenylalanine derivatives, to the synthesis of these compounds, to their use and to pharmaceutical compositions which contain these compounds which act as thrombin inhibitors.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: November 5, 1996
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner St uber, Rainer Koschinsky
  • Patent number: 5567734
    Abstract: Phenyl-substituted alkylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## are described where R(A) and R(B) are H, Hal, CN, OR(6), alkyl, O.sub.r -perfluoroalkyl or NR(7)R(8); R(6) is hydrogen, (cyclo)alk(en)yl, perfluoroalkyl, phenyl or benzyl; R(7) and R(8) are defined as R(6); X is 1-3; R(1) is H, alkyl or --O.sub.0-1 (CH.sub.2)O.sub.0-1 perfluoroalkyl; R(2), R(3), R(4) and R(5) are defined as R(1), with the condition, however, that R(1), R(2), R(3), R(4) and R(5) are not simultaneously hydrogen and that R(1), R(2), R(3), R(4) and R(5) can only be alkyl when at least one of the substituents R(A) or R(B) contains a O.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+1 group; as are the pharmaceutically acceptable salts thereof. Methods of preparation of compounds of formula I are also described.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: October 22, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: RE36068
    Abstract: Various effects of photoaging or sundamage of skin including impairment of differentiation of epidermal epithelial cells and loss of collagen fibers, abnormal changes in elastic fibers and deterioration of small blood vessels in the dermis of the skin are retarded by applying topically to the epidermis in a maintenance therapy program effective amounts of retinoids including retinoid derivatives and stereoisomers thereof such that epithelial growths are substantially reduced and prevented and the skin substantially regains and maintains its firmness, turgor and elasticity. Moreover, with persistent treatment dermal blood cells and vessels increase and the epidermis and dermis thicken, resulting in improved ability of the skin to sense, resist and recover from irritation or injury. Further, hyperpigmentation, lines and wrinkles due to aging are reduced and prevented. The treatment is particularly useful for human facial skin and preferably applied in amounts insufficient to cause excessive irritation.
    Type: Grant
    Filed: April 2, 1996
    Date of Patent: January 26, 1999
    Inventor: Albert M. Kligman