Abstract: New 4H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidin-5(8H)on e and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: Pharmaceutical composition for chelating excess iron in a mammal and facilitating the removal of excess iron from the mammalian body are disclosed which comprise as active ingredient an iron-chelating agent selected from the group consisting of 5H-pyrimido(2',1':2,3)imidazo(4,5-b)indole having the formula ##STR1## 5H-pyrido(2',1':2,3)imidazo(4,5-b) indole having the formula ##STR2## or lower alkyl and/or halogen substituted derivatives thereof and pharmaceutically acceptable acid addition salts thereof. Furthermore the preparation of novel 5H-pyrimido(2',1':2,3)imidazo(4,5-b)indoles and intermediates thereof are disclosed.
Abstract: The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxy-quinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxy-quinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxy-pyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.
Abstract: Propenimidates are provided having the formula: ##STR1## wherein X and Y are independently O or S; andR.sup.1 and R.sup.2 are independently C.sub.1 -C.sub.4 alkyl, (CH.sub.2).sub.n OR.sup.3 where R.sup.3 is C.sub.1 -C.sub.4 alkyl and n is 1 or 2, CH.sub.2 CH.sub.2 Cl, or CH.sub.2 CF.sub.3, provided that when R.sup.1 or R.sup.2 is CH.sub.2 CH.sub.2 Cl or CH.sub.2 CF.sub.3, then the respective X or Y is O.Preferred propenimidates have X and Y as O and R.sup.1 and R.sup.2 as methyl or ethyl.The propenimidates are made by preparing a monohydrohalide salt from a dihydrohalide salt of the formula: ##STR2## and then contacting the monohydrohalide salt with cyanamide. The propenimidates upon heating ring close to pyrimidines which are useful in preparing herbicidal compounds.
Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: Anti-allergy novel 1-oxo-1H-pyrimido[6,1-b]benzthiazole derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each independently is hydrogen, halogen, hydroxy, nitro, trifluoromethyl, or lower alkyl, alkoxy or alkylthio, orR.sub.2 and R.sub.3 together are alkylenedioxy, andX is hydroxy, alkoxy or tetrazolyl-5-amino,or salts thereof, as well as their production by saponification of ##STR2## or tautomers thereof, followed by acidification.
Type:
Grant
Filed:
February 26, 1979
Date of Patent:
November 4, 1980
Assignee:
Boehringer Mannheim GmbH
Inventors:
Werner Winter, Herman Hindermayr, Egon Roesch, Androniki Roesch, Otto-Henning Wilhelms
Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]-pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: Tricyclic quinazolines of the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined in the specification, such as 4,5-dihydro-5-arylimidazo[1,2-a]quinazolines, 4,5-dihydro-5-aryl-s-triazolo[4,3-a]quinazolines and 4,5-dihydro-5-aryltetrazolo[1,5-a]quinazolines having anti-inflammatory and analgesic activity are, for example, prepared by reducing the corresponding 4,5-unsaturated compounds, and then, if necessary, by alkylating the thus produced compounds.
Abstract: Imidazo- and pyrimido[2,1-b]quinazolines of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or R.sub.1 and R.sub.2 may together represent methylenedioxy; R.sub.3 is hydrogen, C.sub.1-4 alkyl, phenyl or substituted phenyl of the formula, ##STR2## (wherein R is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy); R.sub.4 is hydrogen, C.sub.1-4 alkyl or aralkyl; and A is C.sub.2-3 alkylene wich may be optionally substituted by one or two C.sub.1-2 alkyl radicals, and pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined above; and X is oxygen or sulfur, with a halogenating agent at a temperature of about 30.degree. C. to about 180.degree. C. In the above imidaxo- and pyrimido[2,1-b]quinazolines, those having C.sub.1-4 alkyl, or ##STR4## as R.sub.
Abstract: Thiazolidine derivatives of the formula I ##STR1## in which the substituents R.sup.1 to R.sup.7 have the meanings as indicated in the following and which have in the free form or in the form of their non toxic acid addition salts valuable pharmaceutical properties, processes for preparing them, pharmaceutical preparations on the basis of these compounds and their use as medicines.
Abstract: The invention concerns 3,4-dihydropyrimido [1,2-a]benzimidazole derivatives bearing one or more substituents at positions 6, 7, 8 or 9; processes for their preparation and manufacture; and pharmaceutical compositions thereof. The compounds inhibit the aggregation of blood-platelets and may be used in vivo, in the treatment or prophylaxis of thrombosis or occlusive vascular disease, or in vitro, in helping to stabilize preparations of blood platelets. Representative compounds of the invention are 7- and 8- acetyl-3,4-dihydropyrimido[1,2-a]benzimidazol-2(1H)-one.
Abstract: Fused heterocyclic ring systems in which a quinoline or a pyridine component is "fused" to a pyrimidine having a 2-methyl, 2-ethyl, or 2-acetyl group and a 4-keto group, and to similar ring systems in which a quinoline, a naphthalene or a pyridine component is "fused" to a pyrimidine having a 2-carboxy group and a 4-keto group, derivatives, and pharmaceutically-acceptable cationic salts thereof, and their use as antiallergy agents, and intermediates therefor.
Type:
Grant
Filed:
October 27, 1977
Date of Patent:
January 16, 1979
Assignee:
Pfizer Inc.
Inventors:
Thomas H. Althuis, Leonard J. Czuba, Hans-Jurgen E. Hess, Saul B. Kadin
Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: New derivatives of 8H-pyrazolo[4',3':5,6]pyrido[3,4-e]-[1,2,4]triazolo[1,5-a]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: A series of novel pyrimido[2,1-a]isoquinoline derivatives is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration.
Type:
Grant
Filed:
September 21, 1977
Date of Patent:
November 28, 1978
Assignee:
Bristol-Myers Company
Inventors:
Peter F. Juby, Thomas W. Hudyma, Richard A. Partyka
Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',4':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Abstract: New derivatives of 8H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.