Thiocarboxamides, (i.e., C(=s)-n) Patents (Class 514/599)
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Patent number: 5610191Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 are hydrogen or alky1,Y is a group ##STR2## R is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.Type: GrantFiled: November 22, 1995Date of Patent: March 11, 1997Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5602119Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 31, 1995Date of Patent: February 11, 1997Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5599803Abstract: Insecticidal compositions, comprising normally-employed insecticides but comprising also an effective activity-enhancing amount of capsaicin or other capsaicinoid, especially in the form of capsicum, exhibit synergistic effects against numerous insects, including especially bud worms, boll worms, cabbage loopers, army worms, beet army worms, and beetles, and are especially effective on cotton, soybeans, common garden vegetables, and flowers, when sprayed on the insect or its habitat, especially as an aqueous solution, suspension, or emulsion. Larger crop stands may be effectively treated by aerial spraying from the usual crop-dusting airplane.Type: GrantFiled: September 29, 1995Date of Patent: February 4, 1997Assignee: Kalamazoo Holdings, Inc.Inventors: Gary C. Hainrihar, James G. Dubberly, John T. Greenlee
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Patent number: 5597839Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## 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: GrantFiled: April 28, 1995Date of Patent: January 28, 1997Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5591775Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein for use in the treatment of a disorder of the melatoninergic system.Type: GrantFiled: December 6, 1994Date of Patent: January 7, 1997Assignee: Adir et CompagnieInventors: Patrick Depreux, Hamid A. Mansour, Daniel Lesieur, Fran.cedilla.ois Lefoulon, Pierre Renard, Gerard Adam, Philippe Delagrange
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Patent number: 5523325Abstract: This invention relates to amidrazones, insecticidal amidrazone compositions, and methods of using such compositions.Type: GrantFiled: September 9, 1993Date of Patent: June 4, 1996Inventor: Richard M. Jacobson
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Patent number: 5521160Abstract: The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.Type: GrantFiled: January 4, 1995Date of Patent: May 28, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Chucholowski, Jurgen Fingerle, Niggi Iberg, Hans P. Marki, Rita Muller, Michael Pech, Marianne Rouge, Gerard Schmid, Thomas Tschopp, Hans P. Wessel
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Patent number: 5519059Abstract: Disclosed is a topical antifungal formulation including a mixture of isopropyl alcohol, isopropyl myristate and polyethylene glycol or propylene glycol; and a pharmaceutically effective amount of tolnaftate. The formulation provides a solution of tolnaftate which is penetrating, emollient, and non-oily or greasy, non-irritating and rapidly drying. Optionally, aloe vera, vitamin E succinate and witch hazel may be included.Type: GrantFiled: August 17, 1994Date of Patent: May 21, 1996Inventor: Assad S. Sawaya
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Patent number: 5496812Abstract: A topical preparation of between 1% and 3% hydrocortisone and 1.5% and 4.5% tolnaftate, by weight, in a 2:3 ratio used for treating a fungal infection of the skin. The specified ratio provides an accelerated and non-toxic treatment.Type: GrantFiled: October 7, 1994Date of Patent: March 5, 1996Inventor: Chris E. Platt
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Patent number: 5478835Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.Type: GrantFiled: May 2, 1994Date of Patent: December 26, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
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Patent number: 5476874Abstract: Oligopeptide analogs containing sulfonamide, urea or carbamate linkages in the backbone are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: June 22, 1994Date of Patent: December 19, 1995Assignee: Merck & Co., Inc.Inventors: Randall W. Hungate, Joseph P. Vacca
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Patent number: 5475033Abstract: The present invention provides an anti-allergic pharmaceutical composition for ophthalmic topical administration comprising an IgE antibody production inhibitor as an active ingredient. The present invention also provides a process for producing an anti-allergic pharmaceutical composition for ophthalmic topical administration, which comprises mixing an IgE antibody production inhibitor with a pharmaceutically acceptable carrier, excipient or diluent.Type: GrantFiled: May 12, 1994Date of Patent: December 12, 1995Assignees: Taiho Pharmaceutical Co., Ltd, Senju Pharmaceutical Co., Ltd.Inventors: Hitoshi Ohmori, Takahiro Ogawa, Fuminori Tokumochi, Atsushi Okumura
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Patent number: 5472983Abstract: A group of benzamide compounds are disclosed that are formed into pharmaceutical compositions for oral or intravenous administration to patients suffering from neurodegenerative conditions associated with dopamine depletion.Type: GrantFiled: April 14, 1994Date of Patent: December 5, 1995Assignee: Centaur Pharmaceuticals, Inc.Inventors: William D. Flitter, Kirk R. Maples, Richard E. Paylor, Helming Tan, Allan L. Wilcox
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Patent number: 5459149Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.Type: GrantFiled: September 20, 1994Date of Patent: October 17, 1995Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5457083Abstract: Synergistic antimicrobial combinations of polyether polyamino methylene phosphonates and one or more members selected from the group consisting essentially of the following non-oxidizing biocides:didecyl dimethyl ammonium chloride;dodecylguanidine hydrochloride;methylene bisthiocyanate;2,2-dibromo-3-nitrilo-propionamide;2-(thiocyanomethylthio)benzothiazole glutaraldehyde;potassium dimethyldithiocarbamate;5-chloro-2-methyl-4-isothiazolin-3-one;2-methyl-4-isothiazolin-3-one;tetrahydro-3,5-dimethyl-2,H-1,3,5-thiadiazin-2-thione;1,2-dibromo-2,4-dicyanobutane;are useful for inhibiting microbial growth in a variety of aqueous systems.Type: GrantFiled: October 15, 1992Date of Patent: October 10, 1995Assignee: Calgon CorporationInventors: Ramon A. Muia, Nancy S. Sherwood
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Patent number: 5451607Abstract: There are disclosed hydrazone derivatives of the general formula [I]: ##STR1## wherein R.sup.1 is halogen, etc.; R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.5 is C.sub.1 -C.sub.6 alkyl, etc.; R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; A is (CH.sub.2).sub.t, O, S(O).sub.n, etc.; a is an integer of 1 to 4; n is an integer of 0 to 2; and t is an integer of 1 to 3; as well as production processes therefor, insecticides and/or acaricides containing the same as an active ingredient and intermediate compounds thereof.Type: GrantFiled: April 19, 1993Date of Patent: September 19, 1995Assignee: Sumitomo Chemical Co., Ltd.Inventors: Toshiaki Taki, Hirosi Kisida, Shigeru Saito, Shinji Isayama
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Patent number: 5449691Abstract: A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.Type: GrantFiled: June 24, 1993Date of Patent: September 12, 1995Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
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Patent number: 5439925Abstract: 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 is in human and veterinary medicine and in cosmetics.Type: GrantFiled: December 16, 1993Date of Patent: August 8, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
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Patent number: 5424333Abstract: This invention relates to the anthelmintic use of compositions containing N'-substituted-N,N'-disubstitutedhydrazines. Specifically, the invention relates to methods of controlling helminths by contacting the helminths with a compound having a nucleus of the formula ##STR1## wherein X and X' are the same or different O, S, or NR and A', B', R.sup.1 and R.sup.2 are a variety of substituents.Type: GrantFiled: July 5, 1991Date of Patent: June 13, 1995Assignee: Rohm and Haas CompanyInventor: Keith D. Wing
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Patent number: 5395853Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.Type: GrantFiled: November 24, 1993Date of Patent: March 7, 1995Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5393782Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 are hydrogen or alkyl,Y is a group ##STR2## and R is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.Type: GrantFiled: November 29, 1993Date of Patent: February 28, 1995Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5373021Abstract: This invention discloses a rapid-diffusion injectable formulation, comprising disulfiram or a suitable salt or analog of disulfiram. Unlike slow-release injectable formulations designed to ensure that chronic alcoholics have significant quantities of disulfiram in their blood at all time, the rapid-diffusion injectable formulation disclosed herein is designed to reduce the hypoxic or ischemic damage caused by crisis events such as stroke, heart attack, cardiac arrest, or asphyxiation. A rapid-diffusion injectable formulation can contain disulfiram mixed with water, an organic compound having a plurality of hydroxyl groups (such as pharmaceutically acceptable glycols or polysaccharides; propylene glycol, dextrans, and cyclodextrins are often used for such purposes), and a buffer.Type: GrantFiled: April 26, 1993Date of Patent: December 13, 1994Assignee: Cypros Pharmaceutical CorporationInventor: Paul J. Marangos
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Amide derivatives, their production processes and their compositions for the control of insect pests
Patent number: 5356930Abstract: An amide derivative of the formula: ##STR1## which is useful for control of insect pests.Type: GrantFiled: August 5, 1993Date of Patent: October 18, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Kisida, Akira Shuto, Noriyasu Sakamoto, Noritada Matsuo, Hiroaki Fujimoto, Kimitoshi Umeda -
Patent number: 5326755Abstract: The present application discloses pesticidally active compounds of formula I:QQ.sup.1 CR.sup.1 .dbd.CR.sup.2 CR.sup.3 .dbd.CR.sup.4 C(.dbd.X.sup.1)NR.sup.5 R.sup.6or a salt thereof, wherein Q is an monocyclic aromatic ring, or Q is a dihalovinyl group or a group R.sup.7 --C.dbd.C-- where R.sup.7 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X.sup.1 is oxygen or sulphur; R.sup.5 is C.sub.1-8 hydrocarbyl optionally substituted, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy; and R.sup.6 is selected from:(A) --Y.dbd.X.sup.2 --(R.sup.8).sub.a where X.sup.2 is O or S, Y is carbon, R.sup.8 is hydrogen, C.sub.Type: GrantFiled: September 10, 1992Date of Patent: July 5, 1994Assignee: Roussel UCLAFInventors: Robert J. Blade, George S. Cockerill
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5290814Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.Type: GrantFiled: November 5, 1992Date of Patent: March 1, 1994Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5270343Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 .dbd.CR.sup.2 .dbd.CR.sup.3 CR.sup.4 .dbd.CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or is (CH.sub.2).sub.7 ;a=0 or 1; b= 0 or 1;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl;X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from:a) C.sub.1-4 alkyl, C.Type: GrantFiled: June 15, 1992Date of Patent: December 14, 1993Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5248687Abstract: There is disclosed a compound of the formula (I): ##STR1## wherein X is a hydrogen atom or 1 to 5 substituents which may be the same or different and are selected from the group consisting of a hydrogen atom, alkyl, alkenyl, alkynyl, optionally substituted phenyl, an optionally substituted heterocyclic group, alkoxy, alkenyloxy, alkynyloxy, optionally substituted phenoxy, mono-, di- or tri-substituted halogenoalkyl and a halogen atom; Y is CH or N; m is 0 or 1; A is a group of the formula: ##STR2## (wherein R.sup.1 is a hydrogen atom or alkyl; n is 0 or 1; B is O, S or NR.sup.3 ; R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, alkyl, alkenyl, alkynyl, phenyl, benzyl, acyl or phenacyl). There are also disclosed the production thereof and an agricultural fungicide containing the compound as an active component.Type: GrantFiled: August 3, 1992Date of Patent: September 28, 1993Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hayase, Hideyuki Takenaka, Norihiko Tanimoto, Michio Masuko, Toshio Takahashi
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Patent number: 5229424Abstract: The present invention discloses pesticidally active compounds of formula (II) ##STR1## or a salt thereof, wherein Q is a monocylcic aromatic ring, or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each ring system being optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; and R.sup.1 is selected from hydrogen and C.sub.1-8 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy and X.sup.1 is hydrogen, fluoro or chloro.Type: GrantFiled: February 14, 1992Date of Patent: July 20, 1993Assignee: The Wellcome Foundation LimitedInventors: Robert J. Blade, George S. Cockerill, John E. Robinson
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Patent number: 5223509Abstract: This invention relates to certain .beta.-carbolines, which are antagonists of the functions of cholecystokinin (CCK) and gastrin, to pharmaceutical compositions comprising these compounds, and to the use of these compounds in the prevention and treatment of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.Type: GrantFiled: February 21, 1992Date of Patent: June 29, 1993Assignee: Merck & Co., Inc.Inventor: Ben E. Evans
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Patent number: 5206264Abstract: A method is disclosed for reducing cardiovascular damage caused by hypoxic or ischemic events such as heart attack and cardiac arrest. This method involves the administration of disulfiram, or a suitable salt or analog of disulfiram, to a mammal in need of such treatment. Disulfiram can inhibit enzymes such as xanthine oxidase which would otherwise generate oxygenated free radicals, which are highly reactive chemical compounds that non-specifically attack and damage essential molecules and cells. It can also chelate copper and iron, thereby suppressing lipid peroxidation and protecting cell membranes from destruction. It also generates metabolites such as tryptophol which reduce the rate of metabolic activity in neurons and affected tissue, which can be useful during cytotoxic events. This invention also discloses injectable formulations that rapidly release disulfiram into the circulating blood.Type: GrantFiled: November 4, 1991Date of Patent: April 27, 1993Assignee: Cypros Pharmaceutical CorporationInventor: Paul J. Marangos
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Patent number: 5202356Abstract: The present Application discloses pesticidally active compounds of the formula (I):Q Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 C (.dbd.X) NHR.sup.1or a salt thereof, wherein Q is an monocyclic aromatic ring. or fused bicyclic ring system of which at least one ring is aromatic containing 9 or 10 atoms of which one may be nitrogen and the rest carbon each optionally substituted, or Q is a dihalovinyl group or a group R.sup.6 --C.tbd.C-- where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl. halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.2,R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo. C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur; and R.sup.1 is selected from hydrogen and C.sub.Type: GrantFiled: July 12, 1991Date of Patent: April 13, 1993Assignee: The Wellcome Foundation LimitedInventors: Robert J. Blade, George S. Cockerill, John E. Robinston
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Patent number: 5185375Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: March 30, 1990Date of Patent: February 9, 1993Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
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Patent number: 5132326Abstract: Cyclopropanethiocarboxamides I ##STR1## (R.sup.1, R.sup.2 =H, CN, NO.sub.2, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy; R.sup.3, R.sup.4 =H, C.sub.1 -C.sub.4 -alkyl; n=0 or 1).The compounds I are suitable as pesticides.Type: GrantFiled: August 2, 1990Date of Patent: July 21, 1992Assignee: BASF AktiengesellschaftInventors: Uwe Kardorff, Joachim Leyendecker, Hans-Juergen Neubauer, Christoph Kuenast, Peter Hofmeister, Wolfgang Krieg
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Patent number: 5124354Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a special protein tyrosine kinase inhibitor; and(ii) a cosmetically acceptable vehicle for the inhibitor.Type: GrantFiled: June 11, 1990Date of Patent: June 23, 1992Assignee: Chesebrough Pond's USA Co., Division of Conopco, Inc.Inventor: Martin R. Green
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Patent number: 5099030Abstract: 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: GrantFiled: June 27, 1991Date of Patent: March 24, 1992Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5091420Abstract: Pesticidal compositions for use against insects and acarines comprising a compound of Formula (I):R.sup.1 --(CA.dbd.CA').sub.n C(.dbd.S)NR.sup.2 R.sup.3 (I)wherein R.sup.1 is: C.sub.1-14 alkyl optionally substituted by C.sub.1-6 alkoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.2-6 alkenyloxy, C.sub.2-6 alkynyloxy, aryl, aryloxy or aryl (C.sub.1-6) alkoxy; aryloxy or aryl (C.sub.1-6) alkoxy; any of which groups may be substituted by halo,n is 1 or 2,each A and A' is independently hydrogen, halo, C.sub.1-4 alkyl or halo (C.sub.1-4) alkyl and R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, either of which may be substituted by one or more of halo, C.sub.2-6 alkenyl, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkenyl, C.sub.1-6 alkoxy, C.sub.2-6 alkynyl or cyano, except that, when n is 1 and R.sup.2 is alkyl and R.sup.3 is hydrogen and A and A' are both hydrogen then R.sup.1 is not substituted alkyl.Most of the compounds of Formula (I) are novel.Type: GrantFiled: July 26, 1990Date of Patent: February 25, 1992Assignee: Burroughs Wellcome Co.Inventors: Robert J. Blade, Robert J. Peek
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Patent number: 5045565Abstract: 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: GrantFiled: September 8, 1989Date of Patent: September 3, 1991Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5021414Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 18, 1989Date of Patent: June 4, 1991Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 5006539Abstract: 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: GrantFiled: March 6, 1989Date of Patent: April 9, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4985461Abstract: This invention relates to insecticidal compositions containing N'-substituted-N,N'-diacylhydrazines, methods of using such compositions and certain novel insecticidal N'-substituted-N,N'-diacylhydrazines.Type: GrantFiled: October 21, 1985Date of Patent: January 15, 1991Assignee: Rohm and Haas CompanyInventors: Adam C. Hsu, Harold E. Aller
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Patent number: 4983630Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.Type: GrantFiled: November 28, 1988Date of Patent: January 8, 1991Assignee: Schering AktiengesellschaftInventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
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Patent number: 4957533Abstract: Compounds of the formula (I): ##STR1## wherein: X=O, S, or NOH;R.sup.1 is H or CH.sub.3 ;n=1, 2, or 3;R.sup.2, R.sup.3, and R.sup.4 are as defined in one of the following paragraphs(a) R.sup.2 and R.sup.3 are independently Cl or Br, and R.sup.4 is H;(b) R.sup.2, R.sup.3 and R.sup.4 are independently Cl or Br;(c) R.sup.2 is F, R.sup.3 is Cl, and R.sup.4 is H; or(d) R.sup.2 and R.sup.3 are CH.sub.3 or C.sub.2 H.sub.5, and R.sup.4 is H;R.sup.5, R.sup.6 and R.sup.7 are as defined in one of the following paragraphs(a) one of R.sup.6 and R.sup.7 is CF.sub.3, R.sup.5 and the other of R.sup.6 and R.sup.7 is H;(b) R.sup.5 and R.sup.6 are H; and R.sup.7 is F, Cl, or Br;(c) R.sup.5 and R.sup.7 are independently F, Cl or Br and R.sup.6 is H;(d) R.sup.5 and R.sup.6 are independently F, Cl, or Br, and R.sup.7 is H;(e) R.sup.6 and R.sup.7 are independently F, Cl, or Br, and R.sup.5 is H; or(f) R.sup.6 is phenoxy and R.sup.5 and R.sup.7 are Hare plant fungicides.Type: GrantFiled: September 1, 1988Date of Patent: September 18, 1990Assignee: Eli Lilly and CompanyInventors: Wendell R. Arnold, James D. Davenport
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Patent number: 4904661Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 16, 1987Date of Patent: February 27, 1990Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 4900349Abstract: A compound of the general formula (I): ##STR1## wherein R is C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkynyl, both optionally substituted by lower alkyl, halogen or trialkylsilyl; E is CN or CSNH.sub.2 ; and Y is C.sub.1 -C.sub.4 alkoxy, C.sub.3 -C.sub.4 alkenyloxy, C.sub.3 -C.sub.4 alkynyloxy, 1-pyrazolyl or 2-furyl. The compounds have fungicidal and plant growth regulating activity.Type: GrantFiled: April 5, 1988Date of Patent: February 13, 1990Assignee: Imperial Chemical Industries PLCInventors: Stephen P. Heaney, Patrick Crowley, Lawrence G. Reynolds
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Patent number: 4863966Abstract: Compounds of formula (I) are pesticides having activity against arthropods: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are H, alkyl, alkoxy, halo, cyano or trifluoromethyl, or two of R.sup.1, R.sup.2 and R.sup.3 are linked to form a 3 or 4 carbon atom group;X is O or NA where A is H or alkyl;R is H or alkyl; andR.sup.4 and R.sup.5 are H, alkenyl or haloalkenyl or optionally substituted alkyl, aryl or aralkyl, or NR.sup.4 R.sup.5 represents a heterocyclic ring; or an acid addition salt thereof.The invention further provides methods for the preparation of the compounds, pesticidal formulations containing them, and their use in controlling arthropod pests.Type: GrantFiled: February 17, 1981Date of Patent: September 5, 1989Assignee: Burroughs Wellcome Co.Inventors: Malcolm H. Black, Alexander D. Frenkel, Peter T. Roberts
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Patent number: 4752615Abstract: 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: GrantFiled: November 13, 1986Date of Patent: June 21, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4678809Abstract: The disclosure is of the use of an injectable formulation of disulfiram for the treatment of alcoholism. One formulation comprises disulfiram and a biodegradable polymer. Another formulation comprises a slurry of disulfiram in normal saline. After injection, disulfiram is released from the injection site in a sustained-release manner.Type: GrantFiled: February 1, 1985Date of Patent: July 7, 1987Inventor: Michael Phillips
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Patent number: 4672059Abstract: Disclosed herein are tolrestat and oxotolrestat amides and methods of preparation. The amides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.Type: GrantFiled: November 18, 1985Date of Patent: June 9, 1987Assignee: American Home Products CorporationInventors: Kazimir Sestanj, Eckhardt S. Ferdinandi
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Patent number: 4672058Abstract: Disclosed herein are tolrestat amides and methods of preparation. The amides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.Type: GrantFiled: June 10, 1985Date of Patent: June 9, 1987Assignee: American Home Products CorporationInventors: Francesco Bellini, Kazimir Sestanj, Michael Kraml