Thiocarboxamides, (i.e., C(=s)-n) Patents (Class 514/599)
  • Patent number: 5610191
    Abstract: 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: Grant
    Filed: November 22, 1995
    Date of Patent: March 11, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5602119
    Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: January 31, 1995
    Date of Patent: February 11, 1997
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 5599803
    Abstract: 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: Grant
    Filed: September 29, 1995
    Date of Patent: February 4, 1997
    Assignee: Kalamazoo Holdings, Inc.
    Inventors: Gary C. Hainrihar, James G. Dubberly, John T. Greenlee
  • Patent number: 5597839
    Abstract: 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: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5591775
    Abstract: 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: Grant
    Filed: December 6, 1994
    Date of Patent: January 7, 1997
    Assignee: Adir et Compagnie
    Inventors: Patrick Depreux, Hamid A. Mansour, Daniel Lesieur, Fran.cedilla.ois Lefoulon, Pierre Renard, Gerard Adam, Philippe Delagrange
  • Patent number: 5523325
    Abstract: This invention relates to amidrazones, insecticidal amidrazone compositions, and methods of using such compositions.
    Type: Grant
    Filed: September 9, 1993
    Date of Patent: June 4, 1996
    Inventor: Richard M. Jacobson
  • Patent number: 5521160
    Abstract: 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: Grant
    Filed: January 4, 1995
    Date of Patent: May 28, 1996
    Assignee: 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
  • Patent number: 5519059
    Abstract: 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: Grant
    Filed: August 17, 1994
    Date of Patent: May 21, 1996
    Inventor: Assad S. Sawaya
  • Patent number: 5496812
    Abstract: 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: Grant
    Filed: October 7, 1994
    Date of Patent: March 5, 1996
    Inventor: Chris E. Platt
  • Patent number: 5478835
    Abstract: 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: Grant
    Filed: May 2, 1994
    Date of Patent: December 26, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
  • Patent number: 5476874
    Abstract: 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: Grant
    Filed: June 22, 1994
    Date of Patent: December 19, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Randall W. Hungate, Joseph P. Vacca
  • Patent number: 5475033
    Abstract: 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: Grant
    Filed: May 12, 1994
    Date of Patent: December 12, 1995
    Assignees: Taiho Pharmaceutical Co., Ltd, Senju Pharmaceutical Co., Ltd.
    Inventors: Hitoshi Ohmori, Takahiro Ogawa, Fuminori Tokumochi, Atsushi Okumura
  • Patent number: 5472983
    Abstract: 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: Grant
    Filed: April 14, 1994
    Date of Patent: December 5, 1995
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: William D. Flitter, Kirk R. Maples, Richard E. Paylor, Helming Tan, Allan L. Wilcox
  • Patent number: 5459149
    Abstract: 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: Grant
    Filed: September 20, 1994
    Date of Patent: October 17, 1995
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5457083
    Abstract: 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: Grant
    Filed: October 15, 1992
    Date of Patent: October 10, 1995
    Assignee: Calgon Corporation
    Inventors: Ramon A. Muia, Nancy S. Sherwood
  • Patent number: 5451607
    Abstract: 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: Grant
    Filed: April 19, 1993
    Date of Patent: September 19, 1995
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Toshiaki Taki, Hirosi Kisida, Shigeru Saito, Shinji Isayama
  • Patent number: 5449691
    Abstract: 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: Grant
    Filed: June 24, 1993
    Date of Patent: September 12, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
  • Patent number: 5439925
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: August 8, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
  • Patent number: 5424333
    Abstract: 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: Grant
    Filed: July 5, 1991
    Date of Patent: June 13, 1995
    Assignee: Rohm and Haas Company
    Inventor: Keith D. Wing
  • Patent number: 5395853
    Abstract: 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: Grant
    Filed: November 24, 1993
    Date of Patent: March 7, 1995
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5393782
    Abstract: 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: Grant
    Filed: November 29, 1993
    Date of Patent: February 28, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5373021
    Abstract: 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: Grant
    Filed: April 26, 1993
    Date of Patent: December 13, 1994
    Assignee: Cypros Pharmaceutical Corporation
    Inventor: Paul J. Marangos
  • Patent number: 5356930
    Abstract: An amide derivative of the formula: ##STR1## which is useful for control of insect pests.
    Type: Grant
    Filed: August 5, 1993
    Date of Patent: October 18, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Kisida, Akira Shuto, Noriyasu Sakamoto, Noritada Matsuo, Hiroaki Fujimoto, Kimitoshi Umeda
  • Patent number: 5326755
    Abstract: 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: Grant
    Filed: September 10, 1992
    Date of Patent: July 5, 1994
    Assignee: Roussel UCLAF
    Inventors: Robert J. Blade, George S. Cockerill
  • Patent number: 5294616
    Abstract: 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: Grant
    Filed: March 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
  • Patent number: 5290814
    Abstract: 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: Grant
    Filed: November 5, 1992
    Date of Patent: March 1, 1994
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5270343
    Abstract: 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: Grant
    Filed: June 15, 1992
    Date of Patent: December 14, 1993
    Assignee: Roussel Uclaf
    Inventors: John E. Robinson, George S. Cockerill
  • Patent number: 5248687
    Abstract: 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: Grant
    Filed: August 3, 1992
    Date of Patent: September 28, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yoshio Hayase, Hideyuki Takenaka, Norihiko Tanimoto, Michio Masuko, Toshio Takahashi
  • Patent number: 5229424
    Abstract: 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: Grant
    Filed: February 14, 1992
    Date of Patent: July 20, 1993
    Assignee: The Wellcome Foundation Limited
    Inventors: Robert J. Blade, George S. Cockerill, John E. Robinson
  • Patent number: 5223509
    Abstract: 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: Grant
    Filed: February 21, 1992
    Date of Patent: June 29, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Ben E. Evans
  • Patent number: 5206264
    Abstract: 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: Grant
    Filed: November 4, 1991
    Date of Patent: April 27, 1993
    Assignee: Cypros Pharmaceutical Corporation
    Inventor: Paul J. Marangos
  • Patent number: 5202356
    Abstract: 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: Grant
    Filed: July 12, 1991
    Date of Patent: April 13, 1993
    Assignee: The Wellcome Foundation Limited
    Inventors: Robert J. Blade, George S. Cockerill, John E. Robinston
  • Patent number: 5185375
    Abstract: 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: Grant
    Filed: March 30, 1990
    Date of Patent: February 9, 1993
    Assignee: May & Baker Limited
    Inventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
  • Patent number: 5132326
    Abstract: 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: Grant
    Filed: August 2, 1990
    Date of Patent: July 21, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Uwe Kardorff, Joachim Leyendecker, Hans-Juergen Neubauer, Christoph Kuenast, Peter Hofmeister, Wolfgang Krieg
  • Patent number: 5124354
    Abstract: 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: Grant
    Filed: June 11, 1990
    Date of Patent: June 23, 1992
    Assignee: Chesebrough Pond's USA Co., Division of Conopco, Inc.
    Inventor: Martin R. Green
  • 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: 5091420
    Abstract: 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: Grant
    Filed: July 26, 1990
    Date of Patent: February 25, 1992
    Assignee: Burroughs Wellcome Co.
    Inventors: Robert J. Blade, Robert J. Peek
  • 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: 5021414
    Abstract: 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: Grant
    Filed: December 18, 1989
    Date of Patent: June 4, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 5006539
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: March 6, 1989
    Date of Patent: April 9, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4985461
    Abstract: 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: Grant
    Filed: October 21, 1985
    Date of Patent: January 15, 1991
    Assignee: Rohm and Haas Company
    Inventors: Adam C. Hsu, Harold E. Aller
  • Patent number: 4983630
    Abstract: 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: Grant
    Filed: November 28, 1988
    Date of Patent: January 8, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
  • Patent number: 4957533
    Abstract: 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: Grant
    Filed: September 1, 1988
    Date of Patent: September 18, 1990
    Assignee: Eli Lilly and Company
    Inventors: Wendell R. Arnold, James D. Davenport
  • Patent number: 4904661
    Abstract: 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: Grant
    Filed: December 16, 1987
    Date of Patent: February 27, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4900349
    Abstract: 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: Grant
    Filed: April 5, 1988
    Date of Patent: February 13, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: Stephen P. Heaney, Patrick Crowley, Lawrence G. Reynolds
  • Patent number: 4863966
    Abstract: 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: Grant
    Filed: February 17, 1981
    Date of Patent: September 5, 1989
    Assignee: Burroughs Wellcome Co.
    Inventors: Malcolm H. Black, Alexander D. Frenkel, Peter T. Roberts
  • 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: 4678809
    Abstract: 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: Grant
    Filed: February 1, 1985
    Date of Patent: July 7, 1987
    Inventor: Michael Phillips
  • Patent number: 4672059
    Abstract: 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: Grant
    Filed: November 18, 1985
    Date of Patent: June 9, 1987
    Assignee: American Home Products Corporation
    Inventors: Kazimir Sestanj, Eckhardt S. Ferdinandi
  • Patent number: 4672058
    Abstract: 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: Grant
    Filed: June 10, 1985
    Date of Patent: June 9, 1987
    Assignee: American Home Products Corporation
    Inventors: Francesco Bellini, Kazimir Sestanj, Michael Kraml