Chalcogen Or Nitrogen Attached Directly To Ring Carbon Of The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/135)
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Patent number: 4407749Abstract: Disclosed are azo dyes having the general formula ##STR1## in which A is the residue of an aniline, tetrahydroquinoline or benzomorpholine disperse dye coupling component, R is a divalent organic radical such as straight or branched, lower or cyclic aliphatic or arylene, each of which may be substituted, Z is SO.sub.3, SO.sub.4 or SSO.sub.3, and M is hydrogen, an alkali metal or ammonium. These dyes produce orange to bluish red shades and exhibit one or more improved properties such as dyeability, light fastness, blooming, pH stability, build, and the like on, for example, polyamide, wool, and cellulose ester fibers.Type: GrantFiled: June 1, 1982Date of Patent: October 4, 1983Assignee: Eastman Kodak CompanyInventors: Max A. Weaver, Clarence A. Coates, Jr., John G. Fisher
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Patent number: 4408055Abstract: Azolyloxy-carboxylic acid N-oxy-amide compound of the formula ##STR1## wherein R is a five-membered hetero-aromatic monocyclic radical which contains an oxygen atom or a sulphur atom and in addition 1 to 3 nitrogen atoms and which is optionally substituted by halogen, cyano, nitro, amino, alkylamino, arylamino, dialkylamino, alkylcarbonylamino, alkylcarbonyl, carboxyl, alkoxycarbonyl, carbamoyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl (which is optionally substituted by halogen, nitro or alkyl), aryl (which is optionally substituted by halogen, cyano, nitro, alkyl or alkoxy), by a radical which is optionally substituted by halogen and is selected from aralkyl, alkoxy, alkenoxy, alkynoxy, alkoxycarbonylalkoxy, aralkoxy, aryloxy, alkylthio, alkenylthio, alkoxycarbonylalkylthio, aralkylthio, arylthio, alkylsulphinyl, alkylsulphonyl, alkyl, alkenyl, alkynyl, alkoxyalkyl, aralkoxyalkyl, aryloxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, arylthioalkyl, arylsulphinylalkyl, arType: GrantFiled: November 5, 1980Date of Patent: October 4, 1983Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Fritz Maurer, Volker Mues, Ludwig Eue, Robert R. Schmidt
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Patent number: 4405621Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino), N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido)groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)isothioureido]p ropane. The compounds of this invention are inhibitors of H-2 histamine receptors.Type: GrantFiled: June 11, 1981Date of Patent: September 20, 1983Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin
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Patent number: 4395419Abstract: Amidinoformic acids and amidinosulphinic acids which are histamine H.sub.2 -antagonists. A specific compound of this invention is N-[2-(3-(1,2,5)-thiadiazolylmethylthio)ethyl]amidinoformic acid.Type: GrantFiled: August 10, 1981Date of Patent: July 26, 1983Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
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Patent number: 4394508Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.Type: GrantFiled: March 3, 1981Date of Patent: July 19, 1983Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4380639Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.Type: GrantFiled: June 23, 1981Date of Patent: April 19, 1983Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4380638Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.Type: GrantFiled: June 23, 1981Date of Patent: April 19, 1983Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4375472Abstract: Amidinosulphonic acid derivatives carrying an unsaturated nitrogen heterocycle-containing substituent, representative of which are N-methyl-N'[2-(5-methyl-4-imidazolylmethylthio)- ethyl] amidinosulphonic acid and N-methyl-N'-[2-(3-chloropyrid-2-ylmethylthio) ethyl] amidinosulphonic acid, are histamine H.sub.2 -receptor antagonists.Type: GrantFiled: November 24, 1980Date of Patent: March 1, 1983Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Rodney C. Young, Zev Tashma
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Patent number: 4374248Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anit-ulcer agents. Intermediates and processes for their preparation are disclosed.Type: GrantFiled: June 23, 1981Date of Patent: February 15, 1983Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4372963Abstract: Bisamidines carrying one unsaturated nitrogen heterocyclo-containing substituent, representative of which i; 1-[N'-(2-(5-methyl-4-imidazolyl)methylthio)ethyl)guanidino]-8-[N'-methylgu anidino]octane, are histamine H.sub.2 -antagonists.Type: GrantFiled: March 27, 1981Date of Patent: February 8, 1983Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Peter D. Miles
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Patent number: 4362877Abstract: 2,4-Disubstituted-1,2,5-thiadiazol-3(2H)-one antimicrobials have broad spectrum antibacterial and antifungal activity. They are found to be especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.Type: GrantFiled: April 21, 1980Date of Patent: December 7, 1982Assignee: Merck & Co., Inc.Inventors: Richard A. Dybas, Bruce E. Witzel, Nathaniel Grier
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Patent number: 4362726Abstract: Substituted-1,2,5-thiadiazole-1-oxides, their preparation and pharmaceutical use as elastase inhibitors are disclosed.Type: GrantFiled: April 24, 1981Date of Patent: December 7, 1982Assignee: Merck & Co., Inc.Inventors: Joseph S. Amato, Sandor Karady, Leonard M. Weinstock
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Patent number: 4331668Abstract: 3-Nitro-2-substituted aminopyrroles are histamine H.sub.2 -receptor antagonists. The 2- position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with alkyl group interrupted by sulfur or oxygen. The 4- and 5- positions of the pyrrole ring can also be substituted.Type: GrantFiled: June 16, 1980Date of Patent: May 25, 1982Assignee: Smith Kline & French Laboratories LimitedInventors: Michael L. Roantree, Rodney C. Young
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Patent number: 4324793Abstract: 4-Nitro-2-trichloromethylphenyl disulfides, their manufacture, agents containing these compounds as active ingredients for use on microorganisms, and the use of these compounds for protecting substrates against microorganisms.Type: GrantFiled: February 23, 1979Date of Patent: April 13, 1982Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Wolfgang Reuther, Ernst-Heinrich Pommer
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Patent number: 4315931Abstract: Unsubstituted or substituted 5-phenyl- and 5-benzyl-4-amino-pyrimidine-2-imidoacid esters, their preparation, drugs containing these compounds, and their use in infectious diseases.Type: GrantFiled: July 3, 1978Date of Patent: February 16, 1982Assignee: BASF AktiengesellschaftInventors: Peter Scharwaechter, Klaus Gutsche, Wilhelm Kohlmann, Gerd Kroemer, deceased, by Norma Kroemer, legal representative, by Helmut Kroemer, legal representative, by Maria M. Kroemer, legal representative
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Patent number: 4298613Abstract: Heterocyclic sulfenamides, such as N-[2-chloro-5-(trifluoromethyl)phenyl]-N-[2,4-dinitro-6-trifluoromethyl)ph enyl]-3-nitro-2-pyridinesulfenamide, are useful as miticides, insecticides, fungicides and ovicides.Type: GrantFiled: May 5, 1980Date of Patent: November 3, 1981Assignee: E. I. Du Pont de Nemours and CompanyInventor: Gerald E. Lepone
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Patent number: 4295876Abstract: Novel N-(2,5-diazolyl)-alkyl-halogenoacetanilides of the general formmula ##STR1## in which A represents oxygen, sulphur or the grouping >NR,whereinR represents alkyl,R.sup.1 represents hydrogen, alkyl or alkoxy,R.sup.2 represents hydrogen, alkyl, alkoxy or halogen,R.sup.3 represents hydrogen, alkyl, alkoxy or halogen,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen, alkyl, alkoxy, alkylthio, dialkylamino, halogen, cyano or alkoxycarbonyl andZ represents halogen, and acid addition salts and metal salt complexes thereof are outstandingly effective as herbicides.Furthermore novel N-(2,5-diazolyl)-alkyl-anilines of the general formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A have the above-mentioned meaning.Type: GrantFiled: April 23, 1980Date of Patent: October 20, 1981Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Klaus Ditgens, Rudolf Thomas, Ludwig Eue, Robert R. Schmidt
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Patent number: 4284640Abstract: The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-methylamino-2-[2-((4-methyl-5-imidazolyl)methylthio)ethylamino]e thylene.Type: GrantFiled: February 4, 1980Date of Patent: August 18, 1981Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin, Hunter D. Prain
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Patent number: 4282365Abstract: Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.Type: GrantFiled: November 24, 1978Date of Patent: August 4, 1981Assignee: Merck & Co., Inc.Inventors: Joshua Rokach, Edward J. Cragoe, Jr., Clarence S. Rooney
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Patent number: 4255437Abstract: 2-Aryl-5-alkyl-3,4-dioxo-1,2,5-thiadiazolidine-1-oxide of the formula ##STR1## in which Ar is optionally substituted aryl andR is alkyl,which possess fungicidal properties.Type: GrantFiled: November 19, 1979Date of Patent: March 10, 1981Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Knops, Wilhelm Brandes, Volker Paul
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Patent number: 4247550Abstract: The invention relates to a series of new compounds, salts thereof and to methods for the preparation of the compounds which have the general formula ##STR1## in which R.sub.1 stands for an unsubstituted or substituted phenoxy, phenylthio, benzyl, phenylsulfinyl, or anilino radical;R.sub.2 stands for a --YR.sub.2 ' radical, in which Y represents --O--, --S--, or --NH--, and R.sub.2 ' represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or -alkynyl; or methyl or ethyl substituted with phenyl, furyl, thienyl or pyridyl;R.sub.3 and R.sub.4 which can be the same or different, and unsubstituted or substituted, stand for hydrogen or for a straight or branched C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl or -alkynyl radical, a C.sub.5 -C.sub.7 -cycloalkyl, a phenyl, or a 5-, 6- or 7-membered heterocyclic ring system containing not more than two hetero atoms selected from the group consisting of oxygen, sulphur and nitrogen, or for a C.sub.1 -C.sub.Type: GrantFiled: December 21, 1977Date of Patent: January 27, 1981Assignee: Leo Pharmaceutical Products Ltd. A/S (Lovens Kemiske Fabrik Produktionsaktieselskab)Inventors: Peter W. Feit, Ole B. T. Nielsen, Herta Bruun, Claus A. S. Bretting
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Patent number: 4191769Abstract: The compounds are N-(heterocyclomethylthioalkyl) derivatives of alkylguanidines, C-alkyl and C-aryl amidines and S-alkylisothioureas. The compounds may also have N'-lower alkyl or N'(heterocyclomethylthioalkyl) substituents. Three compounds of the invention are S-methyl-N-[2-(5-methyl-4-imidazolylmethylthio)ethyl]isothiourea, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]acetamidine, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]N"-methylguanidine. The compounds of this invention are histamine H.sub.2 -antagonists.Type: GrantFiled: April 17, 1978Date of Patent: March 4, 1980Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
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Patent number: 4173644Abstract: The compounds are dithiocarbamates and isothioureas which are histamine H.sub.2 -antagonists. Two compounds of the invention are 2-(5-methyl-4-imidazolylmethylthio)ethyl N-methyldithiocarbamate and S-[2-(5-methyl-4-imidazolyl-methylthio)ethyl]-N-cyano-N'-methylisothiourea .Type: GrantFiled: July 28, 1978Date of Patent: November 6, 1979Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Graham J. Durant, Charon R. Ganellin, Robert J. Ife