Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 540/490)
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Patent number: 5071845Abstract: A benzoxazepine derivative suitable for use as a psychotropic composition having the formula: ##STR1## wherein A and B are both carbonyl groups, or one thereof represents a methylene group and the other a carbonyl group, R represents an aromatic group or a heterocyclic group, which may be substituted, X represents a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.5 lower alkyl group, a C.sub.1 -c.sub.5 lower alkoxy group, a C.sub.7 -C.sub.9 arylalkoxy group, a hydroxyl group, a nitro group, or an ester group, and n is an integer of 2 to 10 and salts thereof.Type: GrantFiled: December 21, 1989Date of Patent: December 10, 1991Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kayoko Nomura, Makoto Shibata
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Patent number: 5064825Abstract: Novel substituted imidazo-fused 7-member ring heterocycles of the formulae (I) and (Ia), which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: May 16, 1990Date of Patent: November 12, 1991Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, William Schoen, Thomas F. Walsh
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Patent number: 5055464Abstract: Benzolactam compounds of the general formula ##STR1## or isomers thereof as well as salts thereof inclusive of hydrates and/or solvates forms thereof, and benzolactam compounds of the general formula ##STR2## wherein each of the symbols is as defined in the specification. The compound (I) exhibit antiamnesic activity, and are useful as brain function-improving drugs. The compounds (a) and (b) are useful as an intermediate for said compounds (I). Futher, the compound (a) show diuretic or antiulcer activity, and are useful as a diuretic or antiulcer agent.Type: GrantFiled: January 25, 1990Date of Patent: October 8, 1991Assignee: Yoshitomi Pharmaceutical Industries Ltd.Inventors: Shu Murakami, Tsuguo Ikebe, Ichiro Hakamada, Koretake Anami
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5015638Abstract: This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.Type: GrantFiled: November 3, 1989Date of Patent: May 14, 1991Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla, Thomas Tucker
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Patent number: 4950670Abstract: A pyrimidinedione derivative which is a compound of formula (I): ##STR1## in which: R1 denotes hydrogen, a halogen, a methyl group or a methoxy group,R2 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a benzyl group,n denotes 2, 3 or 4,X denotes a CH group or nitrogen, andR3 denotes hydrogen, a halogen or a methoxy group when X denotes a CH group, with the proviso that R3 denotes hydrogen when X denotes nitrogen,or a pharmacologically acceptable acid addition salt thereof.Type: GrantFiled: May 16, 1989Date of Patent: August 21, 1990Assignee: SynthelaboInventors: Jonathan Frost, Bernard Gaudilliere, Jean Rousseau, Regis Dupont, Philippe Manoury, Daniel Obitz
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Patent number: 4939251Abstract: Novel 1-azaspiro[4.4] lactams are produced by reaction of at least one hydroxy-containing primary amino compound with a 4-ketodiacid compound or a 1,6-dioxaspiro[4.4]lactone. Molar excesses of amion compound result in production of spirodilactams, while limited molar quantities of amino compound results in production of a spirolactam-lactone which reacts further with hydroxy-containing primary amino compound or with hydroxy-free primary amino compound to produce a spirodilactam. Certain of the spirolactams are useful as precursors for glycidyloxy derivatives which react with epoxy curing agents to form insoluble thermoset resins while others are useful as curing agents and yet others are converted to glycidyloxy derivatives useful as reactive diluents in epoxy resin applications.Type: GrantFiled: September 16, 1988Date of Patent: July 3, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4935513Abstract: An amide is thiated to the corresponding thioamide by reacting it with phosphorus pentasulfide in the presence of a Group IIA metal fluoride as an adjuvant.Type: GrantFiled: June 7, 1989Date of Patent: June 19, 1990Assignee: Ethyl CorporationInventor: Barbara C. Stahly
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Patent number: 4935510Abstract: Ammonium hydroxide is used in the recovery of a thiono compound prepared by reacting an organic carbonyl compound with phosphorus pentasulfide to improve the product yield.Type: GrantFiled: June 7, 1989Date of Patent: June 19, 1990Assignee: Ethyl CorporationInventor: Barbara C. Stahly
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Patent number: 4935514Abstract: An amide is thiated to the corresponding thioamide by reacting it with phosphorus pentasulfide in the presence of an adjuvant selected from diatomaceous earth, zeolites, and molecular sieves.Type: GrantFiled: June 6, 1989Date of Patent: June 19, 1990Assignee: Ethyl CorporationInventor: Barbara C. Stahly
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Patent number: 4895942Abstract: Novel epoxyalkoxy-containing [4.4] spirodilactams having ring nitrogen atoms in the 1- and the 6- ring positions and having a substituent on each ring nitrogen atom, at least one of which substituents contains an epoxyalkyl moiety. Such epoxy compounds are produced by reaction of a 1-halo-2,3-epoxyalkane and the corresponding hydroxy-containing spirodilactam followed by treatment with strong base.Type: GrantFiled: September 16, 1988Date of Patent: January 23, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4829066Abstract: This invention relates to substituted pyridooxazinone pyridazinone and pyrazolone compounds, which are useful as cardiotonic agents for the treatment of congestive heart failure. This invention also relates to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including said compound.Type: GrantFiled: May 8, 1987Date of Patent: May 9, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla
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Patent number: 4822794Abstract: This invention relates to substituted pyridooxazinone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.Type: GrantFiled: May 8, 1987Date of Patent: April 18, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla
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Patent number: 4812565Abstract: This invention is directed to compounds having the formula: ##STR1## wherein: A represents an aromatic or heterocyclic ring having two of its carbon atoms held mutually with the oxazepine, thiazepine or diazepine moiety selected from the group consisting of benzene, naphthalene, a quinoline, a pyridine in any of its four positions, any of which rings are optionally substituted by one or two Y radicals selected from the group consisting of halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, lower acylamino, trilfuoromethyl, phenyl or phenyl substituted by one to three Y' groups selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl,E is selected from oxygen, sulfur or ##STR2## B is selected from the group consisting of loweralkyl, cycloalkyl or phenyl-loweralkyl wherein phenyl is optionally substituted by one or two radicals selected from halo, loweralkyl, loweralkoxy, nitro or trifuoromethyl,N is 1 or 2,R.sup.4 and R.sup.Type: GrantFiled: February 25, 1987Date of Patent: March 14, 1989Assignee: A. H. Robins Company, IncorporatedInventor: Albert D. Cale, Jr.
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Patent number: 4800200Abstract: Novel 4,8-dihydro-8-arylisoxazolo[4,3-e][1,4]oxazepin-5(6H)-ones and methods for treating hypertension utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: December 21, 1987Date of Patent: January 24, 1989Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Kirk D. Shoger
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Patent number: 4766210Abstract: Antihypertensive compounds of the structure ##STR1## wherein: n is an integer from 0 to 2 inclusive,R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, alkynyl having from 2 to 6 carbon atoms, cycloalkyl having from 3 to 16 carbon atoms, phenyl, benzyl, tolyl, naphthyl, phenethyl, indanyl, tetrahydronaphthyl, decahydronaphthyl, pyridyl, quinolyl, pyrrolidyl, pyrrolyl, morpholinyl, thiomorpholinyl, furyl, furfuryl, tetrahydrofurfuryl, benzimidazole, thienyl, imidolyl, or tetrahydroindolyl, and where the R.sub.1 to R.sub.7 groups are alkyl, said groups carrying a substituent selected from hydroxy, alkoxy, amino, carboxy, or carbalkoxy, the alkyl group in alkoxy and carbalkoxy having from 1 to 6 carbon atoms, or R.sub.2 taken together with R.sub.3 and the carbons to which they are attached is tetrahydronapthyl or phenyl, and when phenyl R.sub.1 and R.sub.4 are absent, or R.sub.6 and R.sub.Type: GrantFiled: July 29, 1981Date of Patent: August 23, 1988Inventors: John T. Suh, Bruce E. Williams, Jerry W. Skiles, Bernard Loev
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Patent number: 4705853Abstract: Aromatic azepinones and thiones having the formula ##STR1## wherein; A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur;E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen-containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl;Y is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracetylamino, trifluoromethyl, phenyl or phenyl substituted by one to three Y' radicals selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.Type: GrantFiled: March 3, 1986Date of Patent: November 10, 1987Assignee: A. H. Robins Company, Inc.Inventor: Albert D. Cale, Jr.
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Patent number: 4680052Abstract: The invention relates to new benzodisultams of the general formula (I) ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen or an optionally substituted radical from the series comprising alkyl, alkemyl, alkinyl and aralkyl, andR.sup.3 represents an optionally substituted and/or optionally fused six-membered aromatic heterocyclic radical which contains at least one nitrogen atom,a process for their preparation and their use as herbicides.Type: GrantFiled: August 23, 1985Date of Patent: July 14, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 4667031Abstract: Oxazepinones and thiazepinones correspoding to the formula: ##STR1## are prepared by mixing an alkali metal salt corresponding to the formula ##STR2## with oxalyl chloride or bromide in an inert solvent and heating to effect halogenation and fusion, A in the formulas representing a substituted or unsubstituted benzene, naphthalene, or pyridine ring bearing up to two Y substituents; E being oxygen or sulfur; R being an alkyl, cycloalkyl, or phenalkyl group or a substituted phenalkyl group bearing up to two ar-Y substituents; X being chloro or bromo; M being an alkali metal; n being one or two; and Y being a substituent selected from alkyl, alkoxy, trifluorimethyl, nitro, and halo. The products are useful as pharmaceutical intermediates.Type: GrantFiled: October 15, 1985Date of Patent: May 19, 1987Assignee: Ethyl CorporationInventor: Kenneth C. Lilje
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Patent number: 4663452Abstract: An organic carbonyl compound is thiated to the corresponding thiono compound by reacting it with phosphorus pentasulfide in the presence of an alkali metal bicarbonate and a hydrocarbon diluent. In preferred embodiments of the invention, the carbonyl compound is an amide, especially an aromatic amide, and the diluent is an inert hydrocarbon having a boiling point in the range of about 50.degree.-150.degree. C.Type: GrantFiled: August 29, 1985Date of Patent: May 5, 1987Assignee: Ethyl CorporationInventor: Kenneth C. Lilje
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Patent number: 4642343Abstract: Aromatic azepinones and thiones having the formula ##STR1## wherein: A is benzene, naphthalene, quinoline or pyridine;B is oxygen or sulfur;E is oxygen, sulfur or ##STR2## n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen containing radical;R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl;and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.Type: GrantFiled: March 3, 1986Date of Patent: February 10, 1987Assignee: A. H. Robins Company, IncorporatedInventor: Albert D. Cale, Jr.
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Patent number: 4610819Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.Type: GrantFiled: September 19, 1984Date of Patent: September 9, 1986Assignee: A. H. Robins Company, Inc.Inventors: Young S. Lo, Albert D. Cale, Jr.