Benzene Ring Is Part Of A Substituent Which Contains Oxygen Patents (Class 514/598)
  • Patent number: 6093742
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: July 25, 2000
    Assignee: Vertex Pharmaceuticals, Inc.
    Inventors: Francesco Gerald Salituro, Guy W. Bemis, Jeremy Green, James L. Kofron
  • Patent number: 6075049
    Abstract: Phenylcarbamates of the formula I ##STR1## where the substituents and the index have the following meanings: R is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2;R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and, in the event that X is NR.sup.a, additionally hydrogen;X is a direct bond, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.2 is hydrogen,substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl;R.sup.3 and R.sup.4 independently of one another are hydrogen, cyano, nitro, hydroxyl, amino, halogen, hetaryloxy, hetarylthio, hetarylamino or N-hetaryl-N-alkylamino, andR.sup.5 is one of the groups mentioned under R.sup.3 or a group CR.sup.d .dbd.NOR.sup.e ;processes and intermediates for their preparation, and their use.
    Type: Grant
    Filed: April 23, 1998
    Date of Patent: June 13, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Muller, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Klaus Oberdorf, Franz Rohl, Norbert Gotz, Michael Rack, Ruth Muller, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
  • Patent number: 6043284
    Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: February 5, 1998
    Date of Patent: March 28, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
  • Patent number: 6025384
    Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.
    Type: Grant
    Filed: February 13, 1998
    Date of Patent: February 15, 2000
    Assignee: LeukoSite, Inc.
    Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
  • Patent number: 6005008
    Abstract: This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: August 15, 1997
    Date of Patent: December 21, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 5990043
    Abstract: An anti-fouling composition comprising a carrier, and a binder, the improvement which comprises an effective amount of at least one insecticide. The composition is applied to the surfaces of articles which come into contact with seawater or brackish water, especially wood. Other conventional anti-fouling agents may also be present.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: November 23, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Martin Kugler, Michael Londershausen, Heinrich Schrage, Hermann Uhr, Franz Kunisch
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5922767
    Abstract: Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: July 13, 1999
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
  • Patent number: 5919824
    Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.
    Type: Grant
    Filed: September 12, 1997
    Date of Patent: July 6, 1999
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
  • Patent number: 5886044
    Abstract: This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: March 23, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Phillip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 5866609
    Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: February 2, 1999
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
  • Patent number: 5851988
    Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## whereineach A is independently a proton-accepting substituent;each R is independently a noninterfering substituent;n is 0, 1, or 2; andeach linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--.Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
    Type: Grant
    Filed: January 15, 1997
    Date of Patent: December 22, 1998
    Assignee: Terrapin Technologies, Inc.
    Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M. Kauvar, Wayne R. Spevak
  • Patent number: 5801178
    Abstract: An aniline derivative of the formula (1) ##STR1## wherein R.sup.1 is an eicosapentaenoyl or docosahexaenoyl; R.sup.2 and R.sup.3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R.sup.4 is a hydrogen atom, an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; and A is a single bond, --C(.dbd.O)NH--(CH.sub.2).sub.n --NH-- wherein n is 2 or 3, or a bivalent group of the following formula ##STR2## wherein m and p are each independently 0 or 1. The aniline derivative of the present invention has high inhibitory activity against and high selectivity for ACAT derived from macrophage and is useful as an agent for the prophylaxis and treatment of arteriosclerosis.
    Type: Grant
    Filed: February 7, 1996
    Date of Patent: September 1, 1998
    Assignees: Nippon Shoji Kaish Ltd., Sagami Chemical Research
    Inventors: Kazunaga Yazawa, Kazuo Watanabe, Yasuharu Ijuin, Mayumi Shikano, Yasuji Soda, Tetsuya Kosaka, Naoto Matsuyama, Koji Mizuno
  • Patent number: 5750565
    Abstract: Tetrahydrofurans tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: May 12, 1998
    Assignee: Cytomed, Inc.
    Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
  • Patent number: 5696138
    Abstract: A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinX, Z, Y, A, D, E, F, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12 have the meanings set forth in the specification, pharmaceutical compositions comprising the same, and a method of treating therewith.The compounds are useful as potassium channel openers.
    Type: Grant
    Filed: December 27, 1995
    Date of Patent: December 9, 1997
    Assignee: NeuroSearch A/S
    Inventors: S.o slashed.ren-Peter Olesen, Peter Moldt, Ove Pedersen
  • Patent number: 5670143
    Abstract: The preferred oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geomentry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of AIDS and ARC.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: September 23, 1997
    Assignees: Merrell Pharmaceuticals Inc., The Dow Chemical Company
    Inventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
  • Patent number: 5668136
    Abstract: A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.
    Type: Grant
    Filed: September 11, 1991
    Date of Patent: September 16, 1997
    Assignee: Eisai Co., Ltd.
    Inventors: Teiji Kimura, Nobuhisa Watanabe, Yasutaka Takase, Kenji Hayashi, Makoto Matsui, Hironori Ikuta, Youji Yamagishi, Kozo Akasaka, Hiroshi Tanaka, Issei Ohtsuka, Takao Saeki, Motoji Kogushi, Tohru Fujimori, Isao Saito
  • Patent number: 5658952
    Abstract: 1-[4-(4'-sulfanilyl)phenyl]urea and its various substituted derivatives can be used to decrease the infectiousness of and reduce the mortality associated with organisms of the genus Leishmania which are responsible for a group of conditions known as Leishmaniasis. This heretofore unrecognized use extends to the known derivatives of ureidodiaminodiphenyl sulfones and includes the novel aryl-ring hydroxylated series of sulfanilylphenylureas of the formula: ##STR1## wherein m and n can be the same or different and may each =0 or 1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are the same or different and are selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 to C.sub.6 straight or branch chain alkyl, halo alkyl, polyhalo alkyl, alkoxy, cyano, amino, alkanoylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, carbamoyl, acyl, R.sup.7, and R.sup.8 are the same or different and are selected from the group consisting of hydrogen, and C.sub.1 to C.sub.
    Type: Grant
    Filed: August 29, 1995
    Date of Patent: August 19, 1997
    Assignee: Jacobus Pharmaceutical Co., Inc.
    Inventor: David Jacobus
  • Patent number: 5621010
    Abstract: Urea derivatives of formula (I) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: May 18, 1994
    Date of Patent: April 15, 1997
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Noriyoshi Sueda, Kazuhiko Yamada, Makoto Yanai, Katsutoshi Miura, Masato Horigome, Norio Oshida, Shigeru Hiramoto, Koichi Katsuyama, Fumihisa Nakata, Nobuhiro Kinoshita, Yoko Tsukada
  • Patent number: 5614550
    Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.
    Type: Grant
    Filed: February 27, 1996
    Date of Patent: March 25, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
  • Patent number: 5612377
    Abstract: A method of inhibiting leukotriene biosynthesis, involving administering a compound of the formula: ##STR1## wherein M, R, R', R", and n are as defined herein. Also, a pharmaceutical composition involving such a compound and the use of such compounds in the manufacture of a pharmaceutical composition for inhibiting leukotriene biosynthesis.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: March 18, 1997
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Stephen L. Crooks, Bryon A. Merrill, Paul D. Wightman
  • Patent number: 5583091
    Abstract: A composition comprises (a) halogenated aromatic 1,2- or 1,3- dinitrile, (b) a substituted urea and (c) a halogen-containing aromatic alkyl sulphoxide or sulphone. The composition may include other materials for example inorganic diluents such as silica, alumina, titanium, dioxide, zinc oxide, etc. and may also include other anti-microbial agents such are anti-bacterial agents. The composition has anti-microbial properties, particularly anti-fungal and anti-algal properties. The composition can be incorporated into materials such as paint or plastics to provide anti-microbial properties.
    Type: Grant
    Filed: December 7, 1994
    Date of Patent: December 10, 1996
    Assignee: Zeneca Limited
    Inventors: Bryan S. Backhouse, Malcolm Greenhalgh
  • Patent number: 5575993
    Abstract: Ionene polymers having biologically-active organic and/or inorganic anions are described. Methods to prepare the ionene polymers, compositions containing them and their methods of use are also described.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: November 19, 1996
    Assignee: Buckman Laboratories International, Inc.
    Inventors: James A. Ward, Fernando Del Corral
  • Patent number: 5576335
    Abstract: Urea derivatives of formula (1) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: November 19, 1996
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Noriyoshi Sueda, Kazuhiko Yamada, Makoto Yanai, Katsutoshi Miura, Masato Horigome, Norio Oshida, Shigeru Hiramoto, Koichi Katasuyama, Fumihisa Nakata, Nobuhiro Kinoshita, Yoko Tsukada
  • Patent number: 5567721
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: October 22, 1996
    Assignee: Centre International de Recherches Dermatologiques
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5534529
    Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: July 9, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Takashi Kasai, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
  • Patent number: 5530026
    Abstract: The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein: A is O or NH; andB is an aryl group selected from the group consisting of phenyl, indane, fluorene, indazole, indole, and pyridine, the aryl group being substituted with at least one substituent selected from the group consisting of hydrogen, C.sub.1-16 alkyl optionally substituted with one or more OH or SH, lower alkoxy, C.sub.3-6 cycloalkyl, lower alkylthio, nitro, cyano, lower alkene, lower alkyne, OH, SH, carboxy lower alkyl, carboxy lower alkyl esters, amino, N-lower alkyl, N,N-dilower alkyl and halogen;or a prodrug thereof, with the provisos that when A is NH and B is phenyl:a) B is substituted with at least one substituent other than hydrogen;b) B is not:1) mono-substituted in the 4 position with C.sub.1-2 alkyl, tert-butyl or n-butyl, halogen, OH, carboxy C.
    Type: Grant
    Filed: January 6, 1995
    Date of Patent: June 25, 1996
    Assignee: Universite Laval
    Inventors: Rene C. Gaudreault, Patrick Poyet
  • Patent number: 5498635
    Abstract: This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: March 12, 1996
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Hiromu Hara, Tatsuya Maruyama, Munetoshi Saito, Toshiyasu Mase
  • Patent number: 5475027
    Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: December 12, 1995
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
  • Patent number: 5470882
    Abstract: This invention relates to the novel pharmaceutical compositions of Formulas (I) and (II) each of which comprises a compound of Formula (I) or (II) and a pharmaceutically acceptable diluent or carrier.This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of Formula (I) or (II).
    Type: Grant
    Filed: June 2, 1994
    Date of Patent: November 28, 1995
    Assignee: SmithKline Beecham Corp.
    Inventors: James S. Dixon, Raplh F. Hall, Lisa A. Marshall, Floyd H. Chilton, III, Ruth J. Mayer, James D. Winkler
  • Patent number: 5423905
    Abstract: The invention relates to a formulation for protecting keratinous material from attack by pests that feed on keratin, comprising (A) at least one diphenylurea of formula ##STR1## wherein R.sub.1 is hydrogen or 4-chlorophenoxy-6-sulfonate,R.sub.2 is hydrogen or chloro,R.sub.3 is chloro or trifluoromethyl,R.sub.4 is hydrogen or chloro, andR.sub.5 is hydrogen or trifluoromethyl, and(B) at least one glycol, and to a process for protecting keratinous material against attack by pests that feed on keratin with the novel formulation.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: June 13, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Werner Fringeli
  • Patent number: 5422373
    Abstract: Diaryl urea compounds having anti-atherosclerosis activity are disclosed. Preferred compounds include the compounds 1-[4-(1,2-dimethoxyethoxy)benzyl-3-(2,4-dimethoxyphenyl)-l-heptylumea and 1-heptyl-3-(2,4-dimethoxyphenyl)-l-[4-(2-methoxyethoxymethoxy)-benzyl]urea .
    Type: Grant
    Filed: March 23, 1993
    Date of Patent: June 6, 1995
    Assignee: Burroughs Wellcome Co.
    Inventor: Karl W. Franzmann
  • Patent number: 5407959
    Abstract: Compounds of structure ##STR1## where W is selected from the group consisting of ##STR2## where Q is oxygen or sulfur, R.sup.7 and R.sup.8 are independently selected from hydrogen and alkyl, or R.sup.7 and R.sup.8, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## L.sup.1 and L.sup.2 are independently selected from a valence bond, alkylene, propenylene, and propynylene; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is oxygen, >NR.sup.11, where R.sup.11 is hydrogen or alkyl, or ##STR4## where n=0, 1, or 2; and R.sup.5 and R.sup.6 are alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
    Type: Grant
    Filed: November 12, 1993
    Date of Patent: April 18, 1995
    Assignee: Abbott Laboratories
    Inventors: Joseph F. Dellaria, Anwer Basha, Lawrence A. Black, Linda J. Chernesky, Wendy Lee
  • Patent number: 5401757
    Abstract: A composition comprises (a) halogenated aromatic 1,2- or 1,3-dinitrile, (b) a substituted urea and (c) a halogen-containing aromatic alkyl sulphoxide or sulphone. The composition may include other materials for example inorganic diluents such as silica, alumina, titanium, dioxide, zinc oxide, etc. and may also include other anti-microbial agents such as anti-bacterial agents. The composition has anti-microbial properties, particularly anti-fungal and anti-algal properties. The composition can be incorporated into materials such as paint or plastics to provide anti-microbial properties.
    Type: Grant
    Filed: October 18, 1993
    Date of Patent: March 28, 1995
    Assignee: Zeneca Limited
    Inventors: Bryan S. Backhouse, Malcolm Greenhalgh
  • Patent number: 5401775
    Abstract: This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: March 28, 1995
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Hiromu Hara, Tatsuya Maruyama, Munetoshi Saito, Toshiyasu Mase
  • Patent number: 5389682
    Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.
    Type: Grant
    Filed: September 13, 1993
    Date of Patent: February 14, 1995
    Assignee: Warner-Lambert Company
    Inventors: Bradley D. Tait, Michael W. Wilson
  • Patent number: 5312820
    Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.
    Type: Grant
    Filed: July 17, 1992
    Date of Patent: May 17, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee, Steven M. Hutchins, Ralph A. Rivero
  • Patent number: 5264441
    Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: November 23, 1993
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Paolo Cozzi, Danielle Fancelli, Dino Severino, Augusto Chiari, Giancarlo Ghiselli
  • Patent number: 5246951
    Abstract: Compounds of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.4, A and B are defined in the description. Medicinal products.
    Type: Grant
    Filed: November 22, 1991
    Date of Patent: September 21, 1993
    Assignee: Adir et Compagnie
    Inventors: Vincent Galet, Marie-Pierre Vaccher, Daniel Lesieur, Pierre Renard, Daniel H. Caignard, Jean-Francois Renaud de la Faverie, Gerard Adam
  • Patent number: 5236953
    Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.ident.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent or each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --;and wherein R.sup.9 is alkyl of up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: August 17, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Leslie R. Hughes, Howard Tucker
  • Patent number: 5116848
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: May 26, 1992
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5106873
    Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds contain two urea or thiourea, amide, or amine moieties or combinations of said moieties and have the following general formula: ##STR1## wherein m and n are zero or one, W and YNH and ##STR2## form the urea, thiourea, amide or amine moieties; and R.sub.1 and R .sub.2 are hydrogen or a hydrocarbon radical.
    Type: Grant
    Filed: June 26, 1990
    Date of Patent: April 21, 1992
    Assignee: Warner-Lambert Company
    Inventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
  • Patent number: 5091419
    Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.
    Type: Grant
    Filed: October 2, 1990
    Date of Patent: February 25, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5064827
    Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: November 12, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
  • Patent number: 5063247
    Abstract: Novel diphenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 is an alkyl group of 5 to 18 carbon atoms, each of R.sub.2 and R.sub.3 is independently an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sub.4 is hydrogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, and X is oxygen atom or sulfur atom, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: November 5, 1991
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Sekiya, Shinya Inoue, Masao Taniguchi, Kohei Umezu, Kazuo Suzuki
  • Patent number: 5057539
    Abstract: An agent for proofing keratinous material against attack by pests that feed on keratin, which contains as active compound at least one diphenylurea of the formula ##STR1## and one synthetic pyrethroid and also, if desired, further auxiliaries, and also a process for proofing keratinous material against attack by keratin pests.
    Type: Grant
    Filed: April 23, 1990
    Date of Patent: October 15, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Alfred J. Neukom, Dieter Reinehr, Werner Schmid
  • Patent number: 5030653
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: July 9, 1991
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5015644
    Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: May 14, 1991
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Bharat K. Trivedi
  • Patent number: 5006539
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: March 6, 1989
    Date of Patent: April 9, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4994490
    Abstract: N-(sulfomethyl)-N'-arylureas inhibit or suppress bitter and sweet tastes when mixed with sweet and/or bitter tasting compositions, such as foods, beverages and pharmaceutical preparations.
    Type: Grant
    Filed: April 3, 1989
    Date of Patent: February 19, 1991
    Assignee: The NutraSweet Company
    Inventors: Glenn Roy, Chris Culberson, George Muller, Srinivasan Nagarajan