Chalcogen Bonded Directly At 2- And 4-positions Patents (Class 544/285)
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Patent number: 4521420Abstract: An oxoquinazoline carbamate of the formula ##STR1## in which R represents hydrogen, alkyl, alkoxy, alkoxyalkyl, alkylthio, alkylthioalkyl, halogenoalkyl or optionally substituted aryl,R.sup.1 represents alkyl,R.sup.2 represents halogenoalkyl,R.sup.3 represents alkyl or halogen andn represents a number from 0 to 4,which possess fungicidal and microbicidal activity.Type: GrantFiled: August 1, 1983Date of Patent: June 4, 1985Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Wilhelm Brandes, Karl-Heinz Kuck, Paul Reinecke, Hans Scheinpflug
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Patent number: 4520196Abstract: .alpha.-Mercaptobenzylacetic acid derivatives of imidazole-containing compounds and analogues thereof, and their use as immunomodulating agents are disclosed.Type: GrantFiled: August 18, 1983Date of Patent: May 28, 1985Assignee: American Home Products CorporationInventor: Peter H. L. Wei
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Patent number: 4511722Abstract: Cyclic N-vinylacylamines are prepared by heating carbonic acid esters of cyclic N-2-hydroxyethylacylamines in the presence of a catalytic amount of alkali or alkaline earth metal compound having an alkaline reaction and subsequently distilling the reaction mixture.Cyclic N-vinylacylamines are valuable precursors for preparing plant protection agents and medicaments and serve as polymerization and copolymerization components for preparing plastics, surface coatings, paints and ion exchange materials.Type: GrantFiled: February 16, 1983Date of Patent: April 16, 1985Assignee: Bayer AktiengesellschaftInventors: Heinrich Krimm, Hans-Josef Buysch, Peter M. Lange, Reinhold Klipper
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Patent number: 4432978Abstract: Derivatives of 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]-indole and of (+)enantiomeric, mixtures of (+) and (-)enantiomeric or (.+-.)racemic 2,3,4,4a,5,9b-hexahydro-4a,9b-trans-1H-pyrido[4,3-b]indole, substituted at the 5-position with an aryl group and at the 2-position with a carbonylaminoalkyl group or an aminoalkyl group, are neuroleptic agents useful in the treatment of certain psychoses and neuroses.Type: GrantFiled: May 20, 1982Date of Patent: February 21, 1984Assignee: Pfizer Inc.Inventors: Willard M. Welch, Charles A. Harbert
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Patent number: 4405623Abstract: A 5,6,7-substituted-2,4(1H,3H)-quinazolinedione compound of the formula (I), ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, A and B are as defined in claim 1 and its acid addition salt; and a vasodilating and hypotensive composition containing the aforesaid compound.Type: GrantFiled: May 15, 1981Date of Patent: September 20, 1983Assignee: Masayuki IshikawaInventors: Masayuki Ishikawa, Akiko Sugimoto, Yukuo Eguchi, Fujinori Sasaki, Hisashi Ebisawa, Soyao Moriguchi, Katsuhiko Gotoh
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Patent number: 4395550Abstract: A process for the production of 4-phenyl-2(1H)-quinazolinones and -4a,5,6,8a-tetrahydro-2(1H)-quinazolinones which comprises introducing the desired phenyl radical into a corresponding quinazolin-2,4(1H,3H)-dione by way of a Grignard reaction and hydrolysis of the resulting product.Type: GrantFiled: November 5, 1981Date of Patent: July 26, 1983Assignee: Sandoz Ltd.Inventor: Peter Funfschilling
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Patent number: 4378361Abstract: Compounds of the formula ##STR1## wherein Het is ##STR2## n is an integer from 1 to 4, inclusive, preferably 2 or 3, R.sub.1 is H or acyl,R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN,R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7,R.sub.2 and R.sub.3 together with each other are ##STR3## R.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5, R.sub.5 and R.sub.6 are each H or --CH.sub.3,R.sub.7 is C.sub.1 -C.sub.4 alkyl,R.sub.8 is H or C.sub.1 -C.sub.4 alkyl,R.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen,R.sub.10 and R.sub.12 are each H, CH.sub.3, Cl or OCH.sub.3, or together methylenedioxy,X is ##STR4## or N, and Z is --CH.sub.2 or --CO;in the form of racemates, enantiomers, diastereoisomeric antipode pairs, and non-toxic, pharmacologically acceptable acid addition salts thereof.Type: GrantFiled: July 22, 1981Date of Patent: March 29, 1983Assignee: Boehringer Ingelheim KGInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Ilse Streller
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Patent number: 4335127Abstract: Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.Type: GrantFiled: October 12, 1979Date of Patent: June 15, 1982Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Vandenberk, Ludo Kennis, Marcel Van der Aa, Albert Van Heertum
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Patent number: 4310527Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower alkyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a --(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.a represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases.Type: GrantFiled: March 8, 1979Date of Patent: January 12, 1982Assignee: Ciba-Geigy CorporationInventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
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Patent number: 4287341Abstract: 2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such that when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;taken separately, R.sup.1 and R.sup.2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms, when taken together with the nitrogen atom to which they are attached R.sup.1 and R.sup.2 form a substituted or unsubstituted heterocyclic group optionally containing an atom of oxygen, sulfur or a second atom of nitrogen as a ring member; their use as antihypertensive agents, pharmaceutical compositions containing them and intermediates for their production.Type: GrantFiled: March 3, 1980Date of Patent: September 1, 1981Assignee: Pfizer Inc.Inventors: Hans-Jurgen E. Hess, Jasjit S. Bindra, Praful K. Shah
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Patent number: 4268511Abstract: This invention relates to compounds having the formula: ##STR1## in which R.sub.1 and R.sub.2 are independently hydrogen, a C.sub.1-4 alkyl group or an aliphatic or aromatic acyl group, provided R.sub.1 and R.sub.2 are not simultaneously hydrogen, or, together with the nitrogen atom to which they are attached, R.sub.1 and R.sub.2 form a 5- or 6-membered ring which may carry another heteroatom; R.sub.3 is a C.sub.1-4 alkyl group; and R.sub.4 and R.sub.5 represent independently a hydrogen or halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group; and the acid addition salts of the above compounds. Said new compounds have an anxiolytic and diuretic action, together with a spasmolytic action of non-.alpha.-adrenalytic nature on the unstriated muscle fibers.Type: GrantFiled: March 11, 1980Date of Patent: May 19, 1981Assignee: Berri-BalzacInventors: Rene Baronnet, Raymond Callendret
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Patent number: 4267325Abstract: N-chlorinated sulphonic acids of the formula ##STR1## (wherein R is group ##STR2## and their salts, particularly their sodium and potassium salts, are disclosed. These compounds are chlorine release agents and may be used as bleaching or germicidal agents either alone or in cleansing or detergent compositions. Preferred compounds are those wherein R is a group ##STR3## in the form of their sodium or potassium salts.Type: GrantFiled: February 27, 1979Date of Patent: May 12, 1981Assignee: Cadbury-Schweppes LimitedInventor: Robin M. Black
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Patent number: 4258187Abstract: Improved process for the preparation of 6-substituted-4-phenylquinazolinone 3-oxides. Such compounds are useful as intermediates in the preparation of 3-fluorobenzodiazepines, which are useful as tranquilizers, muscle relaxants and sedatives.Type: GrantFiled: November 13, 1978Date of Patent: March 24, 1981Assignee: E. I. Du Pont de Nemours and CompanyInventor: William J. Middleton
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Patent number: 4141979Abstract: A series of tetrazolo[a]quinazol-5-ones, methods for their production and use as antiallergy agents and antiulcer agents.Type: GrantFiled: December 22, 1977Date of Patent: February 27, 1979Assignee: Pfizer Inc.Inventor: Jasjit S. Bindra
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Patent number: 4140789Abstract: A compound of the formula ##STR1## in which R.sub.1 denotes optionally substituted lower akyl which is optionally branched at the linking carbon atom, R.sub.2 represents hydrogen or lower alkanoyl and R.sub.3 is a group of the formula --R.sub.3.sup.a -(R.sub.3.sup.b).sub.n -- (Ia), in which R.sub.3.sup.1 represents the radical of the formula --N(R.sub.4)-- or --O-- and R.sub.4 represents hydrogen or lower alkyl, R.sub.3.sup.b denotes the radical of the formula --CH.sub.2 -- or, if R.sub.3.sup.a represents --N(R.sub.4)--, denotes the radical of the formula --C(.dbd.O)-- and n represents nought or 1, and a group of the formula Ia, in which n represents 1, can be linked to the carbonyl group of the carbamoyl grouping either via the group R.sub.3.sup.a or the group R.sub.3.sup.b, or acid addition salts thereof, which can be used pharmaceutically can be used as beta-receptor blocking agents for the treatment of disorders in the cardiac rhythm and coronary heart diseases.Type: GrantFiled: December 16, 1976Date of Patent: February 20, 1979Assignee: Ciba-Geigy CorporationInventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
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Patent number: 4137331Abstract: This invention provides new compounds of formula I, ##STR1## wherein Het is a radical formed by removing one of the hydrogens from the phenyl ring of 2-indolinone or fluorenone, andR is the group A, B, C or D, ##STR2## wherein N IS THE NUMBER 2 OR 3,n' is the number 1, 2, 3 or 4, andX-x' is ethylene or vinylene,Wherein in group D each of the two C atoms adjacent to the N atom are identically substituted by hydrogen or by one or two alkyl groups of 1 to 4 carbon atoms useful as antiarrhythmic agents.Type: GrantFiled: December 16, 1976Date of Patent: January 30, 1979Assignee: Sandoz Ltd.Inventors: Richard Berthold, Franz Troxler
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Patent number: 4116959Abstract: Isoindoline pigment of the formula ##STR1## wherein R denotes a heterocyclic aromatic radical, X.sub.1 -X.sub.4 denote hydrogen or halogen atoms or one or two of the radicals X.sub.1 -X.sub.4 denote nitro, alkyl, alkoxy or phenoxy groups and the others denote hydrogen atoms which are useful for pigmenting high molecular organic material.Type: GrantFiled: September 20, 1976Date of Patent: September 26, 1978Assignee: Ciba-Geigy CorporationInventor: Jost von der Crone
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Patent number: 4102885Abstract: A one-step process for the preparation of 2,4-dihaloquinazolines is disclosed beginning with methoxycarbonyl- or phenoxycarbonyl-derivatives of substituted phenylureas which are cyclized and concomitantly halogenated with a cyclizing-halogenating reagent such as N,N-dimethylaniline in phosphorus oxychloride. The 2,4-dihaloquinazolines of the instant process are particularly valuable as intermediates in the preparation of 4-amino-2-(4-substituted-piperazin-1-yl) quinazolines useful in the treatment of cardiovascular disorders such as hypertension.Type: GrantFiled: June 20, 1977Date of Patent: July 25, 1978Assignee: Bristol-Myers CompanyInventors: Ronnie Ray Crenshaw, George Michael Luke, Richard Anthony Partyka
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Patent number: 4101548Abstract: A series of novel 4-amino-2-(thiadiazole-carbonyl piperazinyl)-6,7-dimethoxyquinazolines is disclosed having antihypertensive properties. The thiadiazole substituent may be optionally substituted with alkyl or lower alkoxy carbonylamino groups. A representative embodiment of the invention is 4-amino-6,7-dimethoxy-2-[4-(5-ethoxy-carbonylamino-1,2,3-thiadiazole-4-car bonyl)-piperazin-1-yl]-quinazoline.Type: GrantFiled: February 22, 1977Date of Patent: July 18, 1978Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Richard A. Partyka
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Patent number: 4093805Abstract: A two-step process for preparing quinazolinethiones by reacting a 2-aminobenzophenone with thiophosgene to give a 2-benzoylisothiocyanate and treating this compound with a predetermined primary amine. A series of substituted quinazolinethiones which display antidepressant and antianxiety properties also are disclosed.Type: GrantFiled: February 17, 1977Date of Patent: June 6, 1978Assignee: The Dow Chemical CompanyInventors: Thomas C. Britton, Donald L. Trepanier
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Patent number: 4093712Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: January 19, 1977Date of Patent: June 6, 1978Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuno Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura