Nitrogen Attached Indirectly To The -c(=s)-group By Nonionic Bonding Patents (Class 514/586)
  • Patent number: 6262113
    Abstract: The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: July 17, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 6255351
    Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: July 3, 2001
    Assignee: ZymoGenetics, Inc.
    Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
  • Patent number: 6255349
    Abstract: Compounds having the formula:  wherein  R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z provided that at least one of R1-R5 is not hydrogen; or R2 and R3or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl;  R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl;  R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or  R7 an
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: July 3, 2001
    Assignee: American Home Products Corporation
    Inventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
  • Patent number: 6221913
    Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.
    Type: Grant
    Filed: January 20, 1999
    Date of Patent: April 24, 2001
    Assignee: ZymoGenetics, Inc.
    Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
  • Patent number: 6214881
    Abstract: The present invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (I-8).
    Type: Grant
    Filed: February 9, 1999
    Date of Patent: April 10, 2001
    Assignee: SmithKline Beecham Corporation
    Inventor: Jia-Ning Xiang
  • 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: 6180675
    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: January 29, 1999
    Date of Patent: January 30, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 6127414
    Abstract: There is provided pharmaceutically useful compounds of formula I, ##STR1## wherein Ar.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: October 3, 2000
    Assignee: Astra Aktiebolag
    Inventors: Nils-.ANG.ke Bergman, Thomas D'Ambra, Garry M Pilling
  • Patent number: 6103761
    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: October 19, 1994
    Date of Patent: August 15, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bradley Dean Tait, Michael William Wilson
  • 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: 5977177
    Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation and use of pharmaceutical preparations based on these compounds, and medicaments containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.
    Type: Grant
    Filed: June 4, 1998
    Date of Patent: November 2, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
  • Patent number: 5977049
    Abstract: An aqueous liquid composition comprisinga) an anionic surfactant or mixtures thereof in cleansing effective quantities,b) a primary ethoxylated alcohol of the structure R(OCH.sub.2 CH.sub.2).sub.n OH wherein R is an average alkyl of about 10 to about 14 carbon atoms, inclusive, and n is an average number of about 6 to about 10,c) a carbanilide antibacterial agent present in an antibacterial effective amount but no more than about 2 wt. % of the composition, the quantity of component c being in a wt. ratio to component b of about 1 to 6 to about 1 to 15, andd) the balance being water.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: November 2, 1999
    Assignee: Colgate-Palmolilve Co.
    Inventors: Laura B. Briceno, Nadia A. Soliman
  • Patent number: 5919825
    Abstract: Hydroximic acid derivatives, useful as pesticides, have the formula ##STR1## in which G is G1 or G2 having the formula: ##STR2## in which R.sub.4 and R.sub.5 are each lower alkyl; W is O, S, SO or SO.sub.2 ; X.sub.1, X.sub.2 and X.sub.3 are, independently, hydrogen or a variety of substituents; and R.sub.1, R.sub.2 and R.sub.3 are, independently, hydrogen or a variety of substituents.
    Type: Grant
    Filed: February 10, 1998
    Date of Patent: July 6, 1999
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Yoshie Kirio, Takako Maeda, Norio Sasaki, Norishige Toshima, Nobumitsu Sawai, Bruce Milligan, Joseph Perez, Jean-Pierre Vors, Daniel B. Gant
  • 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: 5880155
    Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation and use of pharmaceutical preparations based on these compounds, and medicaments containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.
    Type: Grant
    Filed: February 15, 1996
    Date of Patent: March 9, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Uwe Gerlach, Dieter Mania, Heinz Gogelein, Joachim Kaiser
  • Patent number: 5780483
    Abstract: This invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease scates mediated by the chemokine, Interleukin-8 (IL-8). In particular, this invention relates to the novel compounds of Formula (Ia) and their use in treating chemokine mediated diseases wherein the chemokine binds to an IL-8 a or b receptor. Compounds of Formula (Ia) are represented by the structure: ##STR1## wherein interalia, X is oxygen or sulfur;Rb is NR.sub.6 R.sub.7, alkcyl, aryl, arylC.sub.1-4 alkyl, aryl C.sub.2-4 alkenyl, heteroaryl, heteroarylC.sub.1-4 alkyl, heteroarylC.sub.2-4 alkenyl, heterocyclic or heterocyclic C.sub.1-4 alkyl, or a heterocyclic C.sub.2-4 alkenyl moiety, camphor, all of which may be optionally substituted;R.sub.1 is independently selected from hydrogen; halogen; nitro; cyano; C.sub.1-10 alkyl; halosubstituted C.sub.1-10 alkyl; C.sub.2-10 alkoxy; halosubstituted C.sub.1-10 alkoxy; azide; (CR.sub.8 R.sub.8)q S(O).sub.t R.sub.4 ; hydroxy; hydroxy substituted C.sub.
    Type: Grant
    Filed: August 21, 1996
    Date of Patent: July 14, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
  • Patent number: 5776980
    Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
    Type: Grant
    Filed: November 7, 1996
    Date of Patent: July 7, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
  • Patent number: 5716980
    Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: February 10, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
  • Patent number: 5698596
    Abstract: Substituted benzenesulfonylureas and -thioureas--processes for their preparation and their use as pharmaceuticalsBenzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --?CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
    Type: Grant
    Filed: September 3, 1996
    Date of Patent: December 16, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
  • Patent number: 5668180
    Abstract: A compound selected from those of formula (I): ##STR1## in which A, R, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description,and a medicinal product containing the same useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: September 16, 1997
    Assignee: Adir Et Compagnie
    Inventors: Daniel Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard
  • Patent number: 5629347
    Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R.sup.9 CR.sup.10 R.sup.11 or CH.sub.2 R.sup.9 CR.sup.10 R.sup.11 where R.sup.9 is H or OH and R.sup.10 and R.sup.11 are optionally substituted phenyl, optionally substituted benzyl, C.sub.5-7 cycoalkyl or (C.sub.5-7 cycloalkyl)methyl; R.sup.1 and R.sup.2 are H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, COR.sup.a, COOR.sup.a, COC.sub.1-6 alkylhalo, COC.sub.1-6 alkylNR.sup.a R.sup.b, CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b, CONR.sup.a R.sup.b, or SO.sub.2 R.sup.a, or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where one methylene group may optionally be replaced by O or NR.sup.x ; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is optionally substituted phenyl(C.sub.1-3 alkyl); X and Y are H, or X and Y together are .dbd.O; and Z is O, S, or NR.sup.7 ; are tachykinin antagonists.
    Type: Grant
    Filed: December 22, 1993
    Date of Patent: May 13, 1997
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
  • Patent number: 5624937
    Abstract: A compound of the formula I in which ##STR1## Z is O or S; R.sup.11 is a halogen atom;R.sup.12 is a halogen atom or a trifluoromethyl group; andX is S, SO, SO.sub.2, O or NH;R.sup.4 is naphthyl, quinolinyl, benzimidazolyl, pyridyl, pyradazinyl, benzoxazolyl or benzothiazolyl, unsubstituted or substituted by one or two substituents selected from a halogen atom, (1-4C)alkyl, (1-4C)alkoxy, nitro, (1-4C)alkoxycarbonyl, halo(1-4C)alkyl, and phenyl;or a pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of amyloid beta-protein production.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: April 29, 1997
    Assignee: Eli Lilly and Company
    Inventors: Jon K. Reel, Richard L. Simon, Celia A. Whitesitt
  • 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: 5574069
    Abstract: Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto) alk (oxy) yl, E is O or S; Y is --[CR(3).sub.2 ]n-, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: November 12, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser, Wolfgang Linz, David Wettlaufer
  • Patent number: 5559153
    Abstract: Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing themThere are described benzoylguanidines of the formula I ##STR1## where R(1), R(3) or R(4) is --NR(6) C.dbd.X NR(7)R(8); X is oxygen, sulfur, R(6), R(7) and R(8) are H, (perfluoro)alk(en)yl, where R(7) and R(8) can also together be 4 or 5 methylene groups,the substituents R(1) to R(5) remaining in each case are H, Hal, (fluoro) alk(en)yl, CN, NO.sub.2, NR(16)R(17).
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: September 24, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Hans-Jochen Lang, Heinz-Werner Kleemann, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • 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: 5430059
    Abstract: A butenoic acid compound of the following formula: ##STR1## in which Z is O, S, vinylene or azomethyne, A is an alkylene group and J is phenyl group, is a useful in treating heart disease.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: July 4, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Toshiaki Ogawa, Hideyuki Adachi, Takanori Kawamura
  • Patent number: 5403868
    Abstract: Novel capsaicin derivatives of general formula I ##STR1## wherein R, R.sub.1 to R.sub.7 and X may be a variety of substituents, processes for the production thereof, pharmaceutical compositions containing them and use thereof as pharmaceuticals.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: April 4, 1995
    Assignee: Sandoz Ltd.
    Inventors: Derek J. Reid, Christopher S. J. Walpole, Roger Wrigglesworth
  • 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: 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: 5190961
    Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.
    Type: Grant
    Filed: August 2, 1991
    Date of Patent: March 2, 1993
    Assignee: Terumo Kabushiki Kaisha
    Inventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
  • 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: 5114975
    Abstract: The invention relates to novel substituted aryloxyphenylthioureas, aryloxyphenylisothioureas and aryloxyphenylcarobodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH).sub.2, --CH.sub.2).sub.3 or --CH.sub.2).sub.4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.
    Type: Grant
    Filed: April 3, 1991
    Date of Patent: May 19, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund
  • 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: 5106872
    Abstract: The insecticidal and acaricidal activity of N-phenylthioureas can be enhanced and prolonged by the simultaneous application of photosensitizers, and this activity can also be effected within a shorter period of time after application.
    Type: Grant
    Filed: March 26, 1990
    Date of Patent: April 21, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Alex Alder, Alfred Rindlisbacher, Hans-Peter Streibert, Rudolf Banninger
  • Patent number: 5099030
    Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: March 24, 1992
    Assignee: The Procter & Gamble Company
    Inventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
  • 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: 5045565
    Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.
    Type: Grant
    Filed: September 8, 1989
    Date of Patent: September 3, 1991
    Assignee: The Procter & Gamble Company
    Inventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
  • 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: 5026730
    Abstract: The invention relates to novel substituted anilinophenylthioureas, anilinophenylisothioureas and anilinophenylcarbodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH--.sub.2, --CH.sub.2--3 or --CH.sub.2--4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: June 25, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund
  • Patent number: 5021429
    Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: June 4, 1991
    Assignee: Allen & Hansburys Limited
    Inventor: Michael Martin-Smith
  • 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: 5010104
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 4977170
    Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.
    Type: Grant
    Filed: May 3, 1989
    Date of Patent: December 11, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
  • Patent number: 4868210
    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: March 30, 1988
    Date of Patent: September 19, 1989
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 4857556
    Abstract: Substituted benzylcycloalkenylurea derivatives of the formula (I) ##STR1## wherein X represents a halogen atom or a lower alkyl group, Y represents an oxygen atom or a sulfur atom,R.sup.1 represents a cycloalkenyl group andR.sup.2 represents a lower alkyl group, a cycloalkyl group, a benzyl group or a phenyl group optionally substituted by 1 to 5 substituents selected from the group consisting of a hydroxyl group or a lower alkoxy groupand their use as fungicides. They can be synthesized, for example, by reacting of a substituted benzyl-cycloalkenylamine with an isocyanate or by reacting of a carbamoyl halide with an amine. The starting material, the substituted benzyl-cycloalkenyl amines, are also new.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: August 15, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Yasuo Yamada, Junichi Saito, Tatsuo Tamura, Shinji Sakawa
  • Patent number: 4810725
    Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: March 7, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Sandor L. Varga
  • Patent number: 4752615
    Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.
    Type: Grant
    Filed: November 13, 1986
    Date of Patent: June 21, 1988
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
  • Patent number: 4724235
    Abstract: N-(Arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue. The compounds are useful in the treatment of cardiac arrhythmia.
    Type: Grant
    Filed: March 31, 1986
    Date of Patent: February 9, 1988
    Assignee: A. H. Robins Company, Incorporated
    Inventors: James R. Shanklin, Jr., Christopher P. Johnson, III
  • Patent number: 4710516
    Abstract: The invention relates to an insecticidal and acaricidal composition comprising a benzoylurea compound of the general formula ##STR1## wherein R.sub.1 is a halogen atom,R.sub.2 is a hydrogen atom, a methoxy group or a halogen atom,R.sub.3 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of halogen, methyl and trifluoromethyl,R.sub.4 is a hydrogen atom or represents 1-3 substituents which are selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl and C.sub.1 -C.sub.4 haloalkoxy,X is an oxygen atom or a sulphur atom,n is 0 or 1, andR.sub.5 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.2 -C.sub.6 alkenyl group or a C.sub.3 -C.sub.6 cycloalkyl group,with the proviso, that, if n is 0 and R.sub.5 is a hydrogen atom, R.sub.3 is a hydrogen atom.The composition may be used for the control of insects and/or mites in a dosage of 1 to 5,000 grams of active substance per hectare.
    Type: Grant
    Filed: November 19, 1986
    Date of Patent: December 1, 1987
    Assignee: Duphar International Research B.V.
    Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt