Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/142)
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Patent number: 4349677Abstract: The compound 3,4-dihydro-3,4-isoquinolinedione 4-oxime is useful as an antifungal agent.Type: GrantFiled: November 9, 1981Date of Patent: September 14, 1982Assignee: Morton-Norwich Products, Inc.Inventors: Thomas J. Schwan, Homer A. Burch, Joseph E. Gray
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Patent number: 4344949Abstract: Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids and the pharmaceutically acceptable salts thereof are produced by coupling a suitably substituted 1,2,3,4-tetrahydroisoquinoline with a suitably substituted amino acid and when desired hydrolyzing or removing protecting groups of the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.Type: GrantFiled: February 20, 1981Date of Patent: August 17, 1982Assignee: Warner-Lambert CompanyInventors: Milton L. Hoefle, Sylvester Klutchko
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Patent number: 4315855Abstract: Dyes of the formula ##STR1## where X and Y, for example, can be hydrogen or halogen and R can be alkyl among other substituents. The dyes are derived from an O-nitroaniline diazo component and an N-substituted homophthalimide as coupling component. The dyes are greenish yellow to orange and give clear dyeings of good color strength and having good general fastness properties on polyesters, cellulose esters and in some cases also on polyamides. The fastness to light and the fastness to heat setting are excellent and may easily be influenced by the choice of substituents.Type: GrantFiled: July 22, 1976Date of Patent: February 16, 1982Assignee: BASF AktiengesellschaftInventor: Ernst Schefczik
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Patent number: 4291042Abstract: Compounds of formula: ##STR1## and pharmaceutically acceptable acid addition or quaternary ammonium salts thereof wherein the piperidine ring is substituted in the 3 or 4 position; X represents .dbd.CH-- or .dbd.N--; Y represents --NR.sup.5 --, --O-- or --S-- wherein R.sup.5 is hydrogen or lower alkyl; A is lower alkylene or hydroxy lower alkylene, Z and Z.sup.1 independently represent ##STR2## Z may also represent --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CHMe-- or --CMe.sub.2 --; R.sup.1, R.sup.2, R.sup.3 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino, trifluoromethyl, lower-alkanoylamino, hydroxy or aryl lower alkoxy; or R.sup.1 and R.sup.2 when adjacent together with the carbons to which they are attached form a six membered carbocyclic ring; and R.sup.4 represents hydrogen or lower alkyl, are disclosed which possess psychotropic activity and are useful as anti-depressants.Type: GrantFiled: January 21, 1980Date of Patent: September 22, 1981Assignee: John Wyeth & Brother LimitedInventor: Terence J. Ward
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Patent number: 4289882Abstract: This invention relates to the production of 4a-aryldecahydroisoquinolines where the aryl group is selected as 3-methoxy phenyl and intermediates. These compounds are morphine analogs and show utility similar to the known morphine, codeine, and thebaine.Type: GrantFiled: September 5, 1978Date of Patent: September 15, 1981Assignee: The United States of America as represented by the Department of Health & Human ServicesInventors: Henry Rapoport, Dwight D. Weller, Richard D. Gless
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Patent number: 4283539Abstract: Novel isoquinoline acetic acids and derivatives thereof useful as aldose reductase inhibitors and as therapeutic agents for the treatment of chronic diabetic complications, especially diabetic cataracts are disclosed. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of treatment of diabetic cataracts by administration of effective amounts of the novel compounds described herein.Type: GrantFiled: December 18, 1979Date of Patent: August 11, 1981Assignee: Pfizer Inc.Inventor: Rodney C. Schnur
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Patent number: 4264619Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## and functional derivatives thereof, are anti-inflammatory agents.Type: GrantFiled: November 21, 1978Date of Patent: April 28, 1981Assignee: Ciba-Geigy CorporationInventors: Richard W. J. Carney, George deStevens
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Patent number: 4260762Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth,are described.Type: GrantFiled: September 10, 1979Date of Patent: April 7, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Leo Berger, Gary L. Olson
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Patent number: 4251609Abstract: Electrophotosensitive materials having the structure ##STR1## wherein R represents a basic heterocyclic nucleus as well as groups such as hydrogen, alkyl, aryl, aralkyl, etc.;A.sub.1 represents a wide variety of basic heterocyclic nuclei;A.sub.2 represents aryl or may be the same as A.sub.1 ;G represents O or S;M is 0 to 3;N is 0 to 1; andL.sup.1, L.sup.2, L.sup.3, L.sup.4 and L.sup.5 represetn hydrogen, alkyl or aryl.Type: GrantFiled: April 9, 1979Date of Patent: February 17, 1981Assignee: Eastman Kodak CompanyInventors: James R. Nonnemacher, Michael T. Regan, Frank G. Webster
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Patent number: 4230711Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl groups containing 1 to 6 carbon atoms; R.sup.3 is a haloalkyl group of the formula C.sub.m Y.sub.(m-1) X.sub.(m+2) wherein X is fluoro, chloro, bromo or iodo and m=1 or 2; Y is hydrogen, fluoro, chloro, bromo or iodo; R.sup.4 is hydrogen, an alkyl group containing 1 to 6 carbon atoms, alkoxy containing 1 to 6 carbon atoms, alkenyl containing 2 to 6 carbon atoms, nitro, hydroxy, alkoxyalkyl containing 2 to 6 carbon atoms, fluoro, bromo, chloro or iodo and n-1, 2, 3 or 4, have fungicidal activity.Type: GrantFiled: January 31, 1979Date of Patent: October 28, 1980Assignee: Chevron Research CompanyInventor: Stephen D. Ziman
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Patent number: 4202982Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorphinan has been found to possess potent agonist/antagonist activity as a non-narcotic analgesic. A new and efficient total synthesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline.Type: GrantFiled: March 22, 1979Date of Patent: May 13, 1980Assignee: Bristol-Myers CompanyInventors: Ivo Monkovic, Carol Bachand, Henry Wong
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Patent number: 4198512Abstract: Novel 1-oxo-1,2-dihydroisoquinoline compounds of the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a phenyl lower alkyl group; R.sub.2 represents a lower alkyl group; R.sub.3 represents a hydrogen atom, a lower alkanoyl group, a lower alkyl group or a hydroxy lower alkyl group; and n is 0, 1 or 2 and the pharmacologically acceptable non-toxic salts thereof.The compounds of this invention are strong analgesic anti-inflammatory agents.Type: GrantFiled: July 17, 1978Date of Patent: April 15, 1980Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuo Kubo, Noriki Ito, Isao Souzu, Yasuo Isomura, Hiroshige Homma
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Patent number: 4179508Abstract: Compounds of the formula ##STR1## wherein A is lower alkylene,R is lower alkyl, andn is 0, 1 or 2;the compounds are useful as anti-hyperlipidemics and anti-convulsants.Type: GrantFiled: July 18, 1978Date of Patent: December 18, 1979Assignee: Boehringer Ingelheim GmbHInventors: Volkhard Austel, Eberhard Kutter, Wolfgang Eberlein, Joachim Heider, Joachim Kahling
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Patent number: 4176184Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl; phenyl-lower alkyl; cycloalkyl of 3 to 6 carbon atoms; phenyl; mono- or di-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, hydroxyl, methoxy, methylmercapto, methylsulfinyl, methylsulfonyl or benzyloxy; andA is hydrogen or ##STR2## where R.sub.2 is hydrogen or lower alkyl;R.sub.3 is lower alkyl or dimethoxyphenyl-lower alkyl; orR.sub.2 and R.sub.3, together with each other and the nitrogen atom to which they are attached, are piperidino, morpholino or N'-lower alkyl-piperazino; andn is 2 or 3;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as cardiotonics, hypotensives, antithrombotics and antiarrhythmics.Type: GrantFiled: July 17, 1978Date of Patent: November 27, 1979Assignee: Boehringer Ingelheim GmbHInventors: Volkhard Austel, Eberhard Kutter, Joachim Heider, Wolfgang Eberlein, Walter Kobinger, Christian Lillie, Willi Diederen, Walter Haarmann
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Patent number: 4163788Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## R.sub.1 =H or alkyl, Ph=a phenylene radical R.sub.2 =H, alk(en)yl, cycloalk(en)yl or cycloalk(en)yl-alkyl ##STR2## =bicyclic alkenyleneimino with 1-3 double bonds AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.Type: GrantFiled: November 7, 1977Date of Patent: August 7, 1979Assignee: Ciba-Geigy CorporationInventors: Richard W. J. Carney, George DE Stevens
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(.+-.)-2-Cyclobutylmethyl-9.alpha.,10.beta.-dihydroxy-1.beta.-(p-alkox y-benzyl)perhydroisoquinoline
Patent number: 4153603Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorphinan has been found to possess potent agonist/antagonist activity as a non-narcotic analgesic. A new and efficient total synthesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline.Type: GrantFiled: September 28, 1977Date of Patent: May 8, 1979Assignee: Bristol-Myers CompanyInventors: Ivo Monkovic, Carol Bachand, Henry Wong -
Patent number: 4150135Abstract: 4A-Aryl-cis-decahydroisoquinolines, such as N-phenethyl-4a-(m-hydroxyphenyl)-cis-decahydroisoquinoline, useful as analgesics.Type: GrantFiled: March 4, 1977Date of Patent: April 17, 1979Assignee: E. I. Du Pont de Nemours and CompanyInventor: William C. Ripka
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Patent number: 4139534Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorpinan has been found to posess potent agonist/antagonist activity as a non-narcotic analgesic. An improved total snythesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline. A preferred feature of the process involves borane reduction of 2-cyclobutylcarbonyl-9,10-dihydroxy-1-(p-methoxybenzyl)perhydroisoquinolin e (Va) to provide the corresponding cyclobutylmethyl derivative complexed with borane which is converted directly to N-cyclobutylmethyl-14.beta.-hydroxy-3-methoxymorphinan (LVa) by treating with acid.Type: GrantFiled: February 17, 1977Date of Patent: February 13, 1979Assignee: Bristol-Myers CompanyInventors: Gary Lim, Ivo Monkovic
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Patent number: 4133955Abstract: A one-stage process for the production of a 2-equivalent acylacetamide yellow coupler, in which one hydrogen atom of the .alpha.-methylene group of the acyl acetamide coupler molecule is substituted by a group which is attached through an oxygen or nitrogen atom and which can be split off during chromogenic development with an oxidized color developer containing a primary aromatic amino group, which process is carried out by reactingA 4-equivalent acylacetamide yellow coupler withA compound containing an aromatic hydroxyl group or an --NH-- group in a heterocyclic ringIn the presence of a halogen, or an agent which releases halogen, andA basic condensation agentIn a substantially aprotic solvent.Type: GrantFiled: October 6, 1976Date of Patent: January 9, 1979Assignee: AGFA-Gevaert AktiengesellschaftInventor: Gunter Renner
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Patent number: 4129565Abstract: Isocarbostyrils of the formula ##STR1## wherein R.sub.1 represents a lower alkyl group having 1 to 4 carbon atoms, and R.sub.3 and R.sub.4, same or different, individually means hydrogen or an alkyl, aralkyl or cycloalkyl group provided at least either one of R.sub.3 and R.sub.4 should not be hydrogen, or R.sub.3 and R.sub.4 together with the adjacent nitrogen atom may form a heterocyclic ring, having anti-arrhythmic activity and low toxicity are prepared by reacting a 4-substituted isocarbostyril derivative of the formula ##STR2## wherein R.sub.1 is the same as defined above and R.sub.2 represents ##STR3## or its functional equivalent, e.g. --Ch.sub.2 --CH(OH)CH.sub.2 X in which X represents a halogen atom, with an alkyl amine of the general formula ##STR4## wherein R.sub.3 and R.sub.4 are same as defined above..Type: GrantFiled: December 16, 1976Date of Patent: December 12, 1978Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Hideo Fukushima, Yoshikuni Suzuki
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Patent number: 4126691Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.Type: GrantFiled: December 6, 1976Date of Patent: November 21, 1978Assignee: Ciba-Geigy CorporationInventors: Richard W. J. Carney, George DEStevens