Chalcogen Bonded Directly At 2- And 4-positions Patents (Class 544/285)
  • Patent number: 4521420
    Abstract: 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: Grant
    Filed: August 1, 1983
    Date of Patent: June 4, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Wilhelm Brandes, Karl-Heinz Kuck, Paul Reinecke, Hans Scheinpflug
  • Patent number: 4520196
    Abstract: .alpha.-Mercaptobenzylacetic acid derivatives of imidazole-containing compounds and analogues thereof, and their use as immunomodulating agents are disclosed.
    Type: Grant
    Filed: August 18, 1983
    Date of Patent: May 28, 1985
    Assignee: American Home Products Corporation
    Inventor: Peter H. L. Wei
  • Patent number: 4511722
    Abstract: 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: Grant
    Filed: February 16, 1983
    Date of Patent: April 16, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Krimm, Hans-Josef Buysch, Peter M. Lange, Reinhold Klipper
  • Patent number: 4432978
    Abstract: 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: Grant
    Filed: May 20, 1982
    Date of Patent: February 21, 1984
    Assignee: Pfizer Inc.
    Inventors: Willard M. Welch, Charles A. Harbert
  • Patent number: 4405623
    Abstract: 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: Grant
    Filed: May 15, 1981
    Date of Patent: September 20, 1983
    Assignee: Masayuki Ishikawa
    Inventors: Masayuki Ishikawa, Akiko Sugimoto, Yukuo Eguchi, Fujinori Sasaki, Hisashi Ebisawa, Soyao Moriguchi, Katsuhiko Gotoh
  • Patent number: 4395550
    Abstract: 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: Grant
    Filed: November 5, 1981
    Date of Patent: July 26, 1983
    Assignee: Sandoz Ltd.
    Inventor: Peter Funfschilling
  • Patent number: 4378361
    Abstract: 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: Grant
    Filed: July 22, 1981
    Date of Patent: March 29, 1983
    Assignee: Boehringer Ingelheim KG
    Inventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Ilse Streller
  • Patent number: 4335127
    Abstract: 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: Grant
    Filed: October 12, 1979
    Date of Patent: June 15, 1982
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Jan Vandenberk, Ludo Kennis, Marcel Van der Aa, Albert Van Heertum
  • Patent number: 4310527
    Abstract: 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: Grant
    Filed: March 8, 1979
    Date of Patent: January 12, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
  • Patent number: 4287341
    Abstract: 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: Grant
    Filed: March 3, 1980
    Date of Patent: September 1, 1981
    Assignee: Pfizer Inc.
    Inventors: Hans-Jurgen E. Hess, Jasjit S. Bindra, Praful K. Shah
  • Patent number: 4268511
    Abstract: 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: Grant
    Filed: March 11, 1980
    Date of Patent: May 19, 1981
    Assignee: Berri-Balzac
    Inventors: Rene Baronnet, Raymond Callendret
  • Patent number: 4267325
    Abstract: 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: Grant
    Filed: February 27, 1979
    Date of Patent: May 12, 1981
    Assignee: Cadbury-Schweppes Limited
    Inventor: Robin M. Black
  • Patent number: 4258187
    Abstract: 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: Grant
    Filed: November 13, 1978
    Date of Patent: March 24, 1981
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: William J. Middleton
  • Patent number: 4141979
    Abstract: A series of tetrazolo[a]quinazol-5-ones, methods for their production and use as antiallergy agents and antiulcer agents.
    Type: Grant
    Filed: December 22, 1977
    Date of Patent: February 27, 1979
    Assignee: Pfizer Inc.
    Inventor: Jasjit S. Bindra
  • Patent number: 4140789
    Abstract: 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: Grant
    Filed: December 16, 1976
    Date of Patent: February 20, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Knut A. Jaeggi, Franz Ostermayer, Herbert Schroter
  • Patent number: 4137331
    Abstract: 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: Grant
    Filed: December 16, 1976
    Date of Patent: January 30, 1979
    Assignee: Sandoz Ltd.
    Inventors: Richard Berthold, Franz Troxler
  • Patent number: 4116959
    Abstract: 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: Grant
    Filed: September 20, 1976
    Date of Patent: September 26, 1978
    Assignee: Ciba-Geigy Corporation
    Inventor: Jost von der Crone
  • Patent number: 4102885
    Abstract: 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: Grant
    Filed: June 20, 1977
    Date of Patent: July 25, 1978
    Assignee: Bristol-Myers Company
    Inventors: Ronnie Ray Crenshaw, George Michael Luke, Richard Anthony Partyka
  • Patent number: 4101548
    Abstract: 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: Grant
    Filed: February 22, 1977
    Date of Patent: July 18, 1978
    Assignee: Bristol-Myers Company
    Inventors: Ronnie R. Crenshaw, Richard A. Partyka
  • Patent number: 4093805
    Abstract: 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: Grant
    Filed: February 17, 1977
    Date of Patent: June 6, 1978
    Assignee: The Dow Chemical Company
    Inventors: Thomas C. Britton, Donald L. Trepanier
  • Patent number: 4093712
    Abstract: 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: Grant
    Filed: January 19, 1977
    Date of Patent: June 6, 1978
    Assignees: Mitsubishi Chemical Industries Limited, Shosuke Okamoto
    Inventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuno Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura