Sulfur Containing Hetero Ring Patents (Class 548/527)
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Patent number: 4499094Abstract: Compounds with the formula: ##STR1## in which R.sub.1 and R.sub.2 represent independently, a linear or branched alkyl, cycloalkyl, phenylalkyl or cycloalkylalkyl group. R.sub.1 and R.sub.2 may also represent an alkenyl or alkynyl group. R.sub.1 and R.sub.2 may also represent a group of the formula --R.sub.3 --Z--R.sub.4 in which R.sub.3 represents an alkylene group, on condition that at least 2 carbon atoms separate the nitrogen atom from the group Z; R.sub.4 represents an alkyl group, and Z an atom of oxygen, sulphur or the group >N--R.sub.5, R.sub.5 representing a hydrogen atom or an alkyl group. R.sub.1 and R.sub.2 may form, with the nitrogen atom to which they are attached, a heterocyclic ring. Ar represents a phenyl, pyridyl or thienyl group, or a substituted phenyl group, A and B representing independently, N or CH--, the group C representing the residue of a benzene or thiophene ring. These compounds can be used as medicaments, in particular, for the various applications of benzodiazepines.Type: GrantFiled: April 5, 1983Date of Patent: February 12, 1985Assignee: Pharmuka LaboratoiresInventors: Marie-Christine Dubroeucq, Christian Renault, Gerard Le Fur
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Patent number: 4499287Abstract: Compounds of the formula ##STR1## are useful as intermediates in the preparation of various hypotensive agents.Type: GrantFiled: July 29, 1982Date of Patent: February 12, 1985Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4499286Abstract: Novel derivatives of thienylacetic acid amides of the general formula ##STR1## in which the two nitrogens on the cyclohexane ring are transconnected, the basic acetic acid amide radical is in position 2 or 3 of the thiophene nucleus, R is C.sub.1 -C.sub.3 alkyl, R.sub.1 and R.sub.2 are independently C.sub.1 -C.sub.3 -alkyl or represent together with the nitrogen atom to which they are attached a pyrrolidine or piperidine ring and X and Y are independently hydrogen, chlorine or bromine in position 2 to 5 of the thiophene nucleus in dependence on the position of the basic acetic acid amide group, and their pharmaceutically acceptable acid addition salts are .mu.-specific analgetics, which do not cause any physical dependence. Therefore, they are suitable for protracted treatment of pain conditions.Type: GrantFiled: November 22, 1983Date of Patent: February 12, 1985Assignee: Leavoson-Gesellschaft m.b.H. & Co. KGInventor: Dieter Binder
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Patent number: 4499089Abstract: 2-Alkylthio-1-aminoalkyl-2-pyrroline-3-carbonitriles and pharmaceutically acceptable acid addition salts, processes for their preparation and formulation into pharmaceutical compositions as well as their activity as thrombocyte aggregation-inhibitors are described. The compounds are thus useful for the prophylaxis and therapy of thrombotic states.Type: GrantFiled: May 10, 1984Date of Patent: February 12, 1985Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Johannes Hartenstein, Gerhard Satzinger, Edgar Fritschi, Volker Ganser, Horst-Dietmar Tauschel, Gunter Wolf
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Patent number: 4497964Abstract: A process for the production of an N-acyl-.alpha.-amino acid represented by the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, independently from each other, represent a hydrogen atom, an alkyl or cycloalkyl group which may be substituted, or an aryl or heteroaromatic group selected from the group consisting of furyl, pyrrolyl, pyridinyl, thienyl and indolyl which may be substituted, which comprises reacting an oxirane represented by the general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, an amide compound represented by the general formulaR.sup.3 CONHR.sup.4 (III)wherein R.sup.3 and R.sup.4 are as defined above, and carbon monoxide in the presence of hydrogen, a cobalt-containing catalyst, and a promoter composed of a compound containing a metal selected from Groups I, II, III and IV of the periodic table.Type: GrantFiled: November 15, 1982Date of Patent: February 5, 1985Assignee: Sagami Chemical Research CenterInventors: Iwao Ojima, Kenji Hirai
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Patent number: 4496542Abstract: Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy and lower alkoxy,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hydrogen or lower alkyl,R.sub.6 is heterocyclic and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts, possess antihypertensive activity.Type: GrantFiled: April 13, 1983Date of Patent: January 29, 1985Assignee: USV Pharmaceutical CorporationInventors: Jerry W. Skiles, Raymond D. Youssefyeh, John T. Suh, Howard Jones
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Patent number: 4496578Abstract: Novel S-substituted mercapto-lower alkanoyl-4-thiazolidinecarboxylic acids, -2-pyrrolidinecarboxylic acids and their esters represented by the general formula ##STR1## wherein Q is methylene or sulfur;Z is straight or branched alkylene with 1 to 3 carbon atoms, their process for manufacturing, the antihypertensive composition comprising these compounds and the method for reducing blood pressure.Type: GrantFiled: July 6, 1982Date of Patent: January 29, 1985Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Jun-ichi Iwao, Masayuki Oya, Tadashi Iso
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Patent number: 4492710Abstract: What are disclosed are pyrrolidinylsulfamoylbenzoic acid compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 denote C.sub.1 -C.sub.4 alkyl and one of the radicals R.sup.1 or R.sup.2 may be hydrogen, R.sup.3 and R.sup.3' denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a C--C linkage, R.sup.4 and R.sup.4' denote hydrogen, halogen, CF.sub.3, alkyl or C.sub.1 -C.sub.2 alkoxy, hydroxy, amino or dimethylamino in the various positions of the aryl nucleus, or together denote 3,4-methylenedioxy, R.sup.5 and R.sup.6 denote hydrogen, C.sub.1 -C.sub.4 alkyl or benzyl, Ar denotes phenyl or a 5-membered or 6-membered heteroaromatic ring containing a O, S or N atom and X is omitted or denotes oxygen, sulfur, NH, or CH.sub.2, and their pharmaceutically acceptable salts with bases or acids. The compounds and salts have a salidiuretic action and can be used for the treatment of edematous diseases.Type: GrantFiled: September 22, 1982Date of Patent: January 8, 1985Assignee: Hoechst AktiengesellschaftInventors: Wulf Merkel, Dieter Bormann, Roman Muschaweck
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Patent number: 4486444Abstract: (Hydroxybenzoyl)thiophenesulfonamide and acyl derivatives thereof are useful for the topical treatment of elevated intraocular pressure in ophthalmic compositions including drops and inserts.Type: GrantFiled: June 20, 1983Date of Patent: December 4, 1984Assignee: Merck & Co., Inc.Inventor: Kenneth L. Shepard
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4482563Abstract: 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 27, 1983Date of Patent: November 13, 1984Assignee: Smith Kline & French Laboratories LimitedInventors: Michael L. Roantree, Rodney C. Young
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Patent number: 4477466Abstract: Novel acyloxy derivatives of [phenylsulfonyl(or sulfinyl)]thiophenesulfonamides are useful for the topical treatment of elevated intraocular pressure in ophthalmic compositions including drops and inserts.Type: GrantFiled: June 20, 1983Date of Patent: October 16, 1984Assignee: Merck & Co., Inc.Inventor: Kenneth L. Shepard
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Patent number: 4472425Abstract: The invention provides novel N-acylamino thiophene derivatives, e.g. N-(methoxyacetyl)-N-(5-bromo-4-methyl-2-methylthiothien-3-yl)alanine methyl ester, which are useful as fungicides. Other objects of the invention are fungicidal compositions comprising such novel compounds and methods of combatting phytopathogenic fungi with the acid of said novel compounds.Type: GrantFiled: September 6, 1983Date of Patent: September 18, 1984Assignee: Sandoz Ltd.Inventors: Rudolf Sandmeier, Karl Seckinger
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Patent number: 4468521Abstract: Novel .gamma.-lactone derivatives are provided. These lactone derivatives, when reacted with hydrogen halide in alcohol, yield .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters. This ring-opening process is useful for the purpose of increasing the yield of pyrethrin analogs which are of value as insecticides and agricultural chemicals. Thus, the .gamma.-lactone derivatives by-produced in the production process for dihalogenovinyl chrysanthemumates are caused to undergo ring-opening reaction to yield the corresponding .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters which are important intermediates for said pyrethrin analogs.Type: GrantFiled: February 22, 1982Date of Patent: August 28, 1984Assignee: Kuraray Co., Ltd.Inventors: Mori Fumio, Omura Toshiaki, Nishida Takashi, Itoi Kazuo
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Patent number: 4464536Abstract: Antiinflammatory compounds of the following formula are disclosed: ##STR1## wherein R is lower alkyl; R.sup.1 is selected from the group consisting of lower alkyl, benzyl, and N,N-dimethylaminoethyl; or R and R.sup.1 are fused to form an optionally-substituted five- or six-membered heterocyclic ring; and X is hydrogen, methyl or halogen; and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions containing the antiinflammatory compounds and methods of using the antiinflammatory compounds are also described as are a synthetic process and synthetic intermediates for preparing the antiinflammatory compounds.Type: GrantFiled: November 5, 1982Date of Patent: August 7, 1984Assignee: Riker Laboratories, Inc.Inventors: Robert A. Scherrer, George G. I. Moore
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Patent number: 4463176Abstract: A process for resolving a racemic modification of .beta.-adrenergic aryl- or hetaryl-oxypropanolamines such as (.+-.)-2-[2-hydroxy-3-[[2-(1H-indol-3-yl)-1,1-dimethylethyl]amino]propoxy] benzonitrile into its individual enantiomers is described. The process comprises converting the racemic modification into a pair of diastereomeric urea derivatives by reaction with a chiral aralkylisocyanate; separation into the individual diastereomers; and facile regeneration of the starting amine by cleavage of the intermediate urea compound using hydrazine. This final step is improved by the addition of an .alpha.-keto carboxylic acid, such as pyruvic acid, which functions as a scavenger of nucleophilic by-products.Type: GrantFiled: September 13, 1982Date of Patent: July 31, 1984Assignee: Mead Johnson & CompanyInventors: Ronald D. Dennis, Terence M. Dolak, William E. Kreighbaum
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Patent number: 4459410Abstract: Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkysulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylmino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.Type: GrantFiled: October 5, 1981Date of Patent: July 10, 1984Assignee: Sumitomo Chemical Company, LimitedInventors: Keiichi Ono, Hajime Kawakami, Junki Katsube
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Patent number: 4458090Abstract: Novel .gamma.-lactone derivatives are provided. These lactone derivatives, when reacted with hydrogen halide in alcohol, yield .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters. This ring-opening process is useful for the purpose of increasing the yield of pyrethrin analogs which are of value as insecticides and agricultural chemicals. Thus, the .gamma.-lactone derivatives by-produced in the production process for dihalogenovinyl chrysanthemumates are caused to undergo ring-opening reaction to yield the corresponding .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters which are important intermediates for said pyrethrin analogs.Type: GrantFiled: October 15, 1981Date of Patent: July 3, 1984Assignee: Kuraray Co., Ltd.Inventors: Mori Fumio, Omura Yoshiaki, Nishida Takashi, Itoi Kazuo
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Patent number: 4456761Abstract: Compounds of the formula ##STR1## are useful as intermediates in the preparation of various hypotensive agents.Type: GrantFiled: July 29, 1982Date of Patent: June 26, 1984Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4454131Abstract: This invention relates to new thiophene derivatives and their use as fungicides in agriculture and horticulture.Type: GrantFiled: April 26, 1983Date of Patent: June 12, 1984Assignees: Ube Industries, Ltd., Hokko Chemical Industry Co., Ltd.Inventors: Yojiro Hirota, Koichi Shinhama, Katsumi Sato, Takuo Wada
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Patent number: 4452979Abstract: A process for preparing antiinflammatory enamines of the following formula ##STR1## wherein R is lower alkyl; R.sup.1 is selected from the group consisting of lower alkyl, benzyl, and N,N-dimethylaminoethyl; or R and R.sup.1 are fused to form an optionally-substituted five- or six-membered heterocyclic ring; and X is hydrogen, methyl or halogen, comprising (a) reacting a 3,5-bis(t-butyl)-4- hydroxybenzoyl-substituted thiophene with a chlorine source selected from thionyl chloride and phosphorus pentachloride; and (b) reacting the resulting intermediate with an amine to provide the enamine.Type: GrantFiled: November 5, 1982Date of Patent: June 5, 1984Assignee: Riker Laboratories, Inc.Inventor: Robert A. Scherrer
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Patent number: 4451658Abstract: Alkyl 1,4-dialkylpyrrole-2-alkanoates are prepared by the selective decarboxylation of a 1,4-dialkyl-3-carboxypyrrole-2-alkanoic acid or an alkyl ester or alkali metal salt thereof under moderate conditions with a mixture of a strong mineral acid, an alkanol, and water. The products are useful for the preparation of anti-inflammatory agents.Type: GrantFiled: December 9, 1982Date of Patent: May 29, 1984Assignee: Ethyl CorporationInventor: G. Patrick Stahly
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Patent number: 4451285Abstract: The present disclosure relates to a new class of 2-haloacetanilide derivatives which are useful as herbicides. This disclosure further relates to herbicidal compositions containing such 2-haloacetanilides and to herbicidal methods of use employing such compounds and compositions.Type: GrantFiled: May 28, 1982Date of Patent: May 29, 1984Assignee: Monsanto CompanyInventor: Gerhard H. Alt
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Patent number: 4438111Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans--CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturtaed heterocyclic amino group; andR.sup.4 is thienylalkyl or furanylalkyl in which the ring may be substituted.These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis
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Patent number: 4438112Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4433154Abstract: Bis(carboxamide) derivatives being useful as histamine H.sub.2 receptor antagonists or anti-peptic ulcer agents are provided from certain dicarboxylic acid derivatives.Type: GrantFiled: December 7, 1981Date of Patent: February 21, 1984Assignee: Shionogi & Company, LimitedInventor: Kentaro Hirai
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Patent number: 4427685Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: a is 1 to 3;b is 0 to 2;c is 2 to 4;d is 1 to 5;X is sulphur, oxygen or --CH.sub.2 --;Y is oxygen, sulphur, NR.sub.4 or CHR.sub.5 wherein R.sub.4 is hydrogen, C.sub.1-4 alkyl, NO.sub.2 or CN, C.sub.1-4 alkylsulphonyl or phenylsulphonyl optionally substituted in the phenyl moiety by one or two substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, fluorine, chlorine or bromine, and R.sub.5 is NO.sub.2, C.sub.1-4 alkylsulphonyl or optionally substituted phenylsulphonyl as defined for R.sub.4 ;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-4 alkyl, or C.sub.3-6 cycloalkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached represent a pyrrolidino or piperidino ring;R.sub.6 and R.sub.7 are independently hydrogen or C.sub.Type: GrantFiled: February 3, 1982Date of Patent: January 24, 1984Assignee: Beecham Group P.L.C.Inventor: Geoffrey Stemp
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Patent number: 4421761Abstract: Thiophene derivatives of the formula ##STR1## wherein X, Y and Z are as herein defined, said compounds being useful as fungicides, are described.Type: GrantFiled: January 27, 1981Date of Patent: December 20, 1983Assignees: Hokko Chemical Industry Co. Ltd., Ube Industries, Ltd.Inventors: Shigeki Nagai, Takashi Yorie, Hisao Sugiura, Toru Hibi, Katsumi Sato, Takuo Wada, Masahiko Miyahara
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Patent number: 4410521Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 16, 1982Date of Patent: October 18, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter
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Patent number: 4407797Abstract: New compounds of the formula: ##STR1## wherein X.sup..crclbar. is an anion, R is (C.sub.1-7) alkyl [unsubstituted or substituted by hydroxy, carboxy, alkoxycarbonyl, cyano, dialkylamino, alkylcarbonyl, or benzoyl which is unsubstituted or substituted by one or more halogen atoms or radicals selected from alkyl (optionally substituted by one or more halogens), alkoxy, hydroxy, amino, alkylamino, dialkylamino, cyano and nitro, or by a thenoyl radical (which is unsubstituted or substituted by one or more halogens or radicals selected from alkyl, cyano and nitro), or a pyridinecarbonyl, carbamoyl or dialkylcarbamoyl radical (the alkyl radicals of which can form a 5-membered or 6-membered heterocyclic ring) or a pyridyl radical], dialkylcarbamoyl (the alkyl radicals of which can form a 5-membered or 6-membered heterocyclic ring), (C.sub.2-4) alkenyl, (C.sub.2-4) alkynyl, alkoxycarbonyl or a 2-oxotetrahydrofuran-3-yl or 2-oxotetrahydropyran-3-yl ring, and either R.sub.1 and R.sub.Type: GrantFiled: August 10, 1982Date of Patent: October 4, 1983Assignee: Rhone-Poulenc SanteInventors: Claude Cotrel, Daniel Farge, Gerard Taurand
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Patent number: 4405624Abstract: 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably dihydropyrroles or tetrahydropyrridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.Type: GrantFiled: December 2, 1981Date of Patent: September 20, 1983Assignee: Smith Kline & French Laboratories LimitedInventors: Michael L. Roantree, Rodney C. Young
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Patent number: 4396626Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts and pro-drugs thereof, wherein: Ar is a phenyl group optionally substituted by one or two moieties selected from halogen, C.sub.1-4 alkyl, methoxy, methylthio or trifluoromethyl, or a 2-thienyl group or N-methyl-2-pyrryl group optionally substituted by one or two C.sub.1-4 alkyl groups;R is hydrogen or methyl; andn is 0 or 1having useful anti-inflammatory and/or analgesic activity, pharmaceutical compositions containing them, and processes for their preparation.Type: GrantFiled: September 28, 1981Date of Patent: August 2, 1983Assignee: Beecham Group LimitedInventors: Robert W. Ward, Alexander C. Goudie
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Patent number: 4385063Abstract: A compound of formula (I): ##STR1## wherein: R is C.sub.1-4 alkyl;R.sub.1 is hydrogen or C.sub.1-4 alkyl;one of A and B is sulphur, and the other of A and B is carbon doubly bound to the carbon spacing A and B; andthe dotted line represents an optionally present double bond;and pro-drugs thereof; and pharmaceutically acceptable salts thereof;have useful anti-inflammatory and analgesic activity.Type: GrantFiled: March 5, 1981Date of Patent: May 24, 1983Assignee: Beecham Group LimitedInventors: Alexander C. Goudie, Robert W. Ward, Howard E. Rosenberg
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Patent number: 4382929Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, and R.sub.5 represents hydrogen or a C.sub.1-4 alkyl group or R.sub.4 and R.sub.5 may, together with the nitrogen atom to which they are attached, form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.Type: GrantFiled: October 23, 1980Date of Patent: May 10, 1983Assignee: Glaxo Group LimitedInventors: John Bradshaw, Duncan B. Judd, Barry J. Price, John W. Clitherow
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Patent number: 4382143Abstract: This disclosure described novel (monosubstituted-amino)heteroaryl carboxylic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: July 23, 1979Date of Patent: May 3, 1983Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4374254Abstract: A process for preparing 5-aroylpyrrole compounds and recovering them from crude solutions by extracting with a mixed organic extractant such as an aromatic hydrocarbon-alkanol mixture followed by aqueous extraction with a base, decolorizing, and recovering the 5-aroylpyrrole compound for final purification.Type: GrantFiled: January 23, 1981Date of Patent: February 15, 1983Assignee: Ethyl CorporationInventors: James T. F. Kao, Wayne D. Jensen
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Patent number: 4371530Abstract: Compounds are described of the formula ##STR1## in which R.sup.1 is unsubstituted or substituted phenylalkyl, thienylalkyl or naphthylalkyl, or cinnamyl;R.sup.2 is a hydrogen atom, methyl or alkyl substituted by alkoxy or --COOH;W is alkylene;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; andY is a saturated heterocyclic amino group having 5-8 ring members;and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.Type: GrantFiled: July 2, 1981Date of Patent: February 1, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallet, Christopher J. Wallis, Norman F. Hayes
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Patent number: 4366164Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached from a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.Type: GrantFiled: December 5, 1980Date of Patent: December 28, 1982Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Barry Price, John Bradshaw, Michael Martin-Smith
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Patent number: 4356182Abstract: This invention is directed to compounds of the formula ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.Type: GrantFiled: February 2, 1981Date of Patent: October 26, 1982Assignee: E. R. Squibb & Sons, Inc.Inventor: John Krapcho
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Patent number: 4341894Abstract: Sensitizers for photoconductive compositions and elements are disclosed. The sensitizers are 2,4,6 tri substituted pyrylium dye salts wherein at least one of said substituents is a 5 or 6 membered heterocyclic ring having at least one atom selected from the group consisting of N, O and S.Type: GrantFiled: April 26, 1979Date of Patent: July 27, 1982Assignee: Eastman Kodak CompanyInventors: Michael T. Regan, George A. Reynolds, Donald P. Specht, James A. VanAllan
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Patent number: 4332724Abstract: There is provided a process for the preparation of an amido or an ureido derivative of certain 4,5,6,7-tetrahydro-7-oxobenzo[b]thiophenes or certain 1,2,3,4-tetrahydro-4-oxonaphthalenes which can be employed as an animal growth regulant. The process comprises: oxidizing in the presence of a cobalt catalyst a compound having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each a substituent selected from the group consisting of alkanoyl C.sub.1 -C.sub.7, halogen-substituted alkanoyl C.sub.1 -C.sub.7, carboalkoxy C.sub.1 -C.sub.4, ##STR2## and ##STR3## R.sub.3 is selected from the group consisting of hydrogen and alkyl C.sub.1 -C.sub.4 ; R.sub.4 is selected from the group consisting of hydr ogen, alkyl C.sub.1 -C.sub.8, alkanoyl C.sub.2 -C.sub.4, halogen-substituted alkanoyl (C.sub.2 -C.sub.Type: GrantFiled: November 16, 1977Date of Patent: June 1, 1982Assignee: American Cyanamid Co.Inventors: Terence J. Bentley, William H. Gastrock, Goro Asato