The Benzene Ring Is Part Of A Substituent Which Contains Sulfur Patents (Class 564/49)
  • Publication number: 20030013835
    Abstract: A polyurea composition free from polyol linkages. A composition and process for producing a two component spray 100% polyurea elastomeric system wherein an A and a B component are mixed, wherein said A component is a prepolymer produced by an aromatic isocyanate and amine terminated materials and wherein said B component is 100% amine terminated reactive ingredients. The instant invention can be used as a spray system for lining and coating surfaces.
    Type: Application
    Filed: April 25, 2001
    Publication date: January 16, 2003
    Inventors: Anastasios Zahariadis, Gerald Thermos
  • Patent number: 6506802
    Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: January 14, 2003
    Assignee: Alcon Universal Ltd.
    Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
  • Patent number: 6500864
    Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: December 31, 2002
    Assignee: Alcon Universal Ltd.
    Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
  • Patent number: 6498253
    Abstract: Compounds of the formula (I) and salts thereof in which W1, W2, R, n, R1, R2, R4, X, Y and Z are as defined in claim 1 and R3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: December 24, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Publication number: 20020193634
    Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.
    Type: Application
    Filed: May 22, 2002
    Publication date: December 19, 2002
    Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
  • Publication number: 20020193633
    Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.
    Type: Application
    Filed: May 22, 2002
    Publication date: December 19, 2002
    Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
  • Patent number: 6492552
    Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: December 10, 2002
    Assignee: Alcon Universal Ltd.
    Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
  • Publication number: 20020165412
    Abstract: N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also useful as radioprotective agents.
    Type: Application
    Filed: February 28, 2002
    Publication date: November 7, 2002
    Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
  • Patent number: 6458998
    Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
    Type: Grant
    Filed: May 25, 2000
    Date of Patent: October 1, 2002
    Assignee: Telik, Inc.
    Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum
  • Publication number: 20020137774
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: July 19, 2001
    Publication date: September 26, 2002
    Applicant: BAYER CORPORATION
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
  • Patent number: 6444691
    Abstract: The invention relates to 1,3-disubstituted ureas of general formula (I) where R1 is an aryl, R2 is nitro and/or amino, and X is oxygen and/or sulfur, and the method of preparing thereof which consists in treating aromatic amines with isocyanates. Isocyanates may be formed in situ and the reaction carried out in toluene, at 80° C. If the nitro group is formed, it is reduced with hydrogen in the presence of palladium catalyst to the amino group. The obtained 1,3-disubstituted ureas are inhibitors of the activity of the acyl co-enzyme A: cholesterol acyltransferase (ACAT) enzyme, and may be used to inhibit cholesterol esterification and absorption in hypercholesterolemia.
    Type: Grant
    Filed: July 10, 2000
    Date of Patent: September 3, 2002
    Assignee: Solvakofarma, a.s.
    Inventors: Vladi{acute over (m)}ir Oremus, Vendelín {haeck over (S)}mahovský, Viera Fáberová, Ivan Kakalík, {haeck over (L)}udmila Schmidtová, Marián Zemánek
  • Publication number: 20020082255
    Abstract: The invention is directed to physiologically active compounds of general formula (I): 1
    Type: Application
    Filed: November 2, 2001
    Publication date: June 27, 2002
    Inventor: Paul Robert Eastwood
  • Publication number: 20020058709
    Abstract: Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The disulfide derivatives act as mast cell stabilizers.
    Type: Application
    Filed: April 25, 2001
    Publication date: May 16, 2002
    Applicant: Alcon Universal Ltd.
    Inventors: Zixia Feng, Mark R. Hellberg, Steven T. Miller
  • Patent number: 6372933
    Abstract: This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: April 16, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Neil H. Baine, Ann Marie Eldridge, Marvin Sungwhan Yu
  • Patent number: 6362183
    Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: March 26, 2002
    Assignee: G. D. Searle & Company
    Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
  • Patent number: 6316478
    Abstract: This invention relates to novel spiro compound derivatives of benzoisothiazolyl-urea and -thiourea and compositions thereof. These compounds are useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: November 13, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine L. Widdowson, Hong Nie
  • Publication number: 20010027211
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Application
    Filed: February 21, 2001
    Publication date: October 4, 2001
    Applicant: Tularik Inc.
    Inventor: Jonathan B. Houze
  • Patent number: 6214880
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: April 10, 2001
    Assignee: Tularik Inc.
    Inventor: Jonathan B. Houze
  • Patent number: 6211373
    Abstract: This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: April 3, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 6152968
    Abstract: The use of water-soluble quinacridones of the formula I ##STR1## where M.sup..sym. is a lithium, sodium, potassium or ammonium cation,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, sulfamoyl, mono- or di-(C.sub.1 -C.sub.4)-alkylsulfamoyl, carbamoyl, mono- or di-(C.sub.1 -C.sub.4)-alkylcarbamoyl, unsubstituted or substituted mono- or diphenylsulfamoyl, unsubstituted or substituted mono- or diphenylcarbamoyl, halogen, nitro or cyano,n is 0, 1 or 2 andm is 0, 1 or 2 and the sum n+m is at least 1,for dyeing and printing natural and synthetic fiber material.
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: November 28, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl-Heinz Etzbach, Carolin Kranz, Rudiger Sens
  • Patent number: 6133319
    Abstract: This invention relates to the use of phenyl ureas of formulas (I) and (II) in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). The variables of (I) and (II) are defined herein.
    Type: Grant
    Filed: August 19, 1999
    Date of Patent: October 17, 2000
    Assignee: SmithKline Beecham Corporation
    Inventor: Katherine L. Widdowson
  • Patent number: 6121323
    Abstract: Bishydroxyureas are provided that inhibit the enzyme 5-lipoxygenase. These compounds have the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and M are defined herein. Also disclosed are pharmaceutical compositions containing such compounds and methods of inhibiting the enzyme 5-lipoxygenase using such compounds.
    Type: Grant
    Filed: December 3, 1997
    Date of Patent: September 19, 2000
    Assignee: 3M Innovative Properties Company
    Inventor: Bryon A. Merrill
  • 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: 6083986
    Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
    Type: Grant
    Filed: July 15, 1997
    Date of Patent: July 4, 2000
    Assignees: ICAgen, Inc., Eli Lilly & Company
    Inventors: Neil Alexander Castle, Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, George Salvatore Amato, Serge Beaudoin, Michael Gross, Grant McNaughton-Smith
  • Patent number: 6057269
    Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: May 2, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
  • 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: 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: 5994398
    Abstract: Arylsulfonamides which have the general structure: with the symbols R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and n representing the groups and integers provided in the detailed description are provided herein. These compounds have activity as inhibitors of phospholipase A2, inhibitors of cytokine release and as inhibitors of neurodegeneration.
    Type: Grant
    Filed: December 11, 1996
    Date of Patent: November 30, 1999
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Russell E. Rydel, Eugene D. Thorsett
  • Patent number: 5986044
    Abstract: The narrow poly- or mono-dispersed oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a recurring unit of from 3 to 50. These oligomers are water-soluble, preferably have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geometry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The narrow poly- or mono-dispersed oligomers are useful for the treatment and/or diagnosis of AIDS and/or ARC or HSV.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: November 16, 1999
    Assignees: The Dow Chemical Co., Merrell Pharmaceuticals Inc.
    Inventors: Alan D. Cardin, Michael J. Mullins, William A. Fordyce, Thomas A. Chamberlin, Michael J. Fazio
  • 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: 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: 5883091
    Abstract: The invention relates to new 1,3,4-oxadiazine derivatives of the formula (I) ##STR1## in which Ar.sup.1 represents in each case optionally substituted aryl or hetaryl,Ar.sup.2 represents in each case optionally substituted aryl or hetaryl andX represents the group --(CHR.sup.1).sub.m --(CHR.sup.2).sub.n in whichR.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,m represents 0 or 1 andn represents 0 or 1,to a plurality of processes for their preparation, and to their use for combating animal pests.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: March 16, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerd Kleefeld, Johannes Kanellakopulos, Ulrike Wachendorff-Neumann
  • Patent number: 5866611
    Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: February 2, 1999
    Assignee: Zeneca Limited
    Inventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
  • Patent number: 5824705
    Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 20, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5739398
    Abstract: A process for preparing N-alkenylureas of the general formula I ##STR1## where R.sup.1 and R.sup.2 are hydrogen, C.sub.1 - to C.sub.40 -alkyl, C.sub.2 - to C.sub.40 -alkenyl, C.sub.3 - to C.sub.20 -cycloalkyl, C.sub.4 - to C.sub.20 -alkylcyc1oalkyl, C.sub.4 - to C.sub.20 -cycloalkylalkyl, aryl, C.sub.7 - to C.sub.20 -alkylaryl or C.sub.7 - to C.sub.20 -aralkyl, or aryl, C.sub.7 - to C.sub.20 -alkylaryl or C.sub.7 - to C.sub.20 -aralkyl which are mono- to pentasubstituted by C.sub.1 - to C.sub.8 -alkyl, C.sub.1 - to C.sub.8 -alkoxy or halogen, together are a C.sub.2 - to C.sub.10 -alkylene chain which is unsubstituted or mono- to hexasubstituted by C.sub.1 - to C.sub.8 -alkyl, andR.sup.3 and R.sup.4 are hydrogen or C.sub.1 - to C.sub.8 -alkyl,by reaction of ureas of the general formula II ##STR2## where R.sup.1 and R.sup.2 have the abovementioned meanings, with an alkenyl carboxylate of the general formula III ##STR3## where R.sup.3 and R.sup.4 have the abovementioned meanings and R.sup.5 is hydrogen, C.sub.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Jochem Henkelmann, Marc Heider, Thomas Ruhl
  • Patent number: 5728874
    Abstract: The present invention relates to achiral polyurea oligomers, their uses and formulations as anti-HIV pharmaceuticals and to a process for the preparation of narrow mono- and polydispersed oligomers as an emodiment of the invention. The achiral oligomers are derived from repeating units of the monomer 4,4'-diamino-biphenyl-3,3'-disulfonic acid and are water soluble, have a rigid backbone, possess ordered anionic spacing and have a number average molecular weight of <20,000. The process relates to the synthesis of narrow poly- and mono-dipersed oligomers comprising the steps of: 1) restricting the crude olydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture; and/or 2) isolating the monodispersed anionic oligomer; and 3) optionally converting the narrow poly- or mono-dispersed anionic oligomer salt from Step 1 or 2 to a desired pharmaceutically-acceptable salt, especially a solim or potassium salt.
    Type: Grant
    Filed: December 27, 1993
    Date of Patent: March 17, 1998
    Assignees: Merrell Pharmaceuticals, Inc., The Dow Chemical Co.
    Inventors: Michael J. Mullins, Ray E. Drumright, Alan D. Cardin, Norton P. Peet
  • 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: 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: 5585518
    Abstract: Useful ureas have the formula ##STR1##
    Type: Grant
    Filed: April 10, 1995
    Date of Patent: December 17, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Claus Marschner, Knut Kessel, Manfred Patsch
  • 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: 5463083
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl 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. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
    Type: Grant
    Filed: January 6, 1994
    Date of Patent: October 31, 1995
    Assignee: Cytomed, Inc.
    Inventors: Tesfaye Biftu, Xiong Cai, Sajjet Hussion, Gurmit Grewal, T. Y. Shen
  • Patent number: 5449812
    Abstract: The compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: September 12, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5442060
    Abstract: Carboxamide derivatives of the following general formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 are C.sub.1 -C.sub.3 alkyl group or both taken together C.sub.1 -C.sub.3 alkylene group,R.sup.3 is hydrogen atom, dialkylamino group, etc.,R.sup.4 is hydrogen atom, C.sub.1 -C.sub.10 alkyl group,R.sup.5 is C.sub.1 -C.sub.10 alkyl group,m, n, q are an integer from 0-3,p is 0, 1,A ring is ##STR2## B ring is 5 or 6 membered nitrogen containing aromatic ring, are provided, which are useful as medicinals for treating hyperlipemia or atherosclerosis.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: August 15, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Jikihara, Tadashi Shirasaka, Kazuo Suzuki, Hiroko Suzuki, Masao Taniguchi, Shinya Inoue
  • 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: 5310634
    Abstract: A p-phenylenediamine series color developing agent or a precursor thereof having a substituent A at the ortho-position; Substituent A: ##STR1## wherein R.sup.1 represents a hydrogen atom or an alkyl group and X represents --O--R.sup.7 or ##STR2## wherein R.sup.7 represents an alkyl group, an aryl group, or a heterocyclic ring and R.sup.8 and and R.sup.9, which may be the same or different, each represents a hydrogen atom, an alkyl group, an aryl group, or a heterocyclic ring, R.sup.8 and R.sup.9 may combine with each other to form a heterocyclic ring, and a process for forming an image which comprises imagewise exposing a silver halide color photographic material and thereafter color developing the color photographic material in the presence of a p-phenylenediamine series color developing agent or a precursor thereof having the aforesaid substituent A.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: May 10, 1994
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Mitsugu Tanaka, Kei Sakanoue
  • Patent number: 5276182
    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 ARC.
    Type: Grant
    Filed: June 10, 1991
    Date of Patent: January 4, 1994
    Assignees: The Dow Chemical Company, Merrell Dow Pharmaceuticals Inc.
    Inventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
  • Patent number: 5223529
    Abstract: Compounds of formula: ##STR1## in which R.sub.1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R.sub.8)--COOR.sub.4, (c) a chain --CH.sub.2 --CO--NR.sub.5 R.sub.6 or (d) a phenylalkyl radical, R.sub.2 is a methylene or ethylene radical or a radical --CH(R.sub.7)--, R.sub.3 is a 1- or 2-naphthyl radical, 2- or 3-indolyl or phenylamino radical in which the phenyl ring is optionally substituted on the understanding that, when R.sub.3 is 1- or 2-naphthyl or 2- or 3-indolyl radical, R.sub.7 cannot represent a benzyl, alkylthioalkyl or phenyl radical, as well as, when R.sub.2 is a radical --CH(R.sub.7)--, their racemates and their stereoisomers, and medicinal products containing them.
    Type: Grant
    Filed: May 11, 1990
    Date of Patent: June 29, 1993
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Gerard Roussel, Franco Manfre
  • Patent number: 5215570
    Abstract: The N-acylsulfamoylphenylureas of formula I below are suitable as counter-agents (antidotes or safeners) for protecting cultivated plants from the phytotoxic action of herbicides. Suitable crops are preferably cereals, soybeans, sorghum, maize and rice, and suitable herbicides are sulfonylureas, chloroacetanilides and aryloxyphenoxypropionic acid derivatives.The N-acylsulfamoylphenylureas have the formula I ##STR1## wherein A is a radical selected from the group ##STR2## R.sub.1 is C.sub.1 -C.sub.4 -alkoxy or each of R.sub.1 and R.sub.2, independently of the other, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, ##STR3## or C.sub.1 -C.sub.4 alkyl substituted by C.sub.1 -C.sub.4 alkoxy or by ##STR4## or R.sub.1 and R.sub.2 together form a C.sub.4 -C.sub.6 alkylene bridge, or a C.sub.4 -C.sub.6 alkylene bridge interrupted by oxygen, sulfur, SO, SO.sub.2, NH or by --N(C.sub.1 -C.sub.4 alkyl)-, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.
    Type: Grant
    Filed: January 3, 1991
    Date of Patent: June 1, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Urs Burckhardt, Raafat Soliman, Werner Topfl, Hans-Rudolf Waespe