Hoffmann-la Roche Inc.

Ado Kaiser

Frank Kienzle

Madhukar Subraya Chodnekar

Marcel Scheer

Marcel Muller

Werner Bollag

Ulf Fischer

Paul Zeller

Wolfgang Koch

Leo Marti

Uwe Wolcke

Balthasar Hegedus

Hugo Gutmann

Albert Langemann

Werner Hausermann

Pyrimidone derivatives of the formula ##STR1## wherein n is the integer 1 or 0; A.sup.1 and A.sup.2 are independently methylene or mono-lower alkyl or di-lower alkyl methylene; X is methylene, mono-lower alkyl or di-lower alkyl methylene, nitrogen or lower alkyl nitrogen; R is hydrogen or lower alkyl; and Y and Z taken together are the group .dbd.NR.sup.5, or R and Z taken together form a N--C--bond and Y is a group --N(H)R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 are hydrogen, lower alkyl or lower alkoxy, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 taken together are methylenedioxy or ethylenedioxy; R.sup.4 is hydrogen or lower-alkyl; R.sup.5 is phenyl or phenyl substituted by one or more of R.sup.6, R.sup.7 and R.sup.8 which, independently, are chlorine, fluorine, bromine, lower-alkyl or lower-alkoxy; and provided that at least one of the methylene groups A.sup.1 and A.sup.2 is mono-lower alkyl or di-lower alkyl methylene, when R.sup.4 is hydrogen and n is 0, and physiologically compatible salts thereof which have blood platelet aggregation-inhibiting activity or have activity on the circulatory system, are described. The compounds of formula I are obtained starting from corresponding chlorinated or brominated pyrimidone derivatives.

Substituted

Imidazoquinazolines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen, halogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.2-5 -alkoxyalkyl; or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy; and R.sup.4 and R.sup.5 are hydrogen or C.sub.1-4 -alkyl, and their tautomers, as well as their physiologically compatible acid addition salts, are described. The compounds of formula I inhibit the aggregation of the blood platelets, as well as gastric acid secretion, and have activity on the circulatory system.

Imidazoquinazolines having pharmaceutical activity

Compounds of the formula ##STR1## wherein R.sup.1,R.sup.2,R.sup.3 and R.sup.4 are as hereinafter described, tautomers and salts thereof, are disclosed. The foregoing compounds inhibit the aggregation of blood platelets which renders them useful as therapeutic agents in the prophylaxis of thromboses. Furthermore, they are useful for the treatment and prophylaxis of cardiac insufficiency and cardiac failure, due to their inotropic activity without substantial tachycardia.

Imidazo[2,1-b]quinazolin-2(3H)-ones and pharmaceutical compositions for

Thiocarbamoylthio fatty acid derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Y and n are as hereinafter set forth, are described. The compounds of formula I are useful as lipid-lowering agents.

Thiocarbamoylthio fatty acids

The present invention is directed to preparing L-Dopa, an agent effective in the treatment of Parkinson's Disease, from a D,L-N-benzoyl-3-(4-hydroxy-3-methoxyphenyl) alanine utilizing dehydroabietylamine as a resolving agent and intermediates in this process.

Process for the preparation of l-dopa

Process for obtaining 5,6 or 6,7 or 7,8 dihydroxy coumarin or derivatives thereof, which are useful for lower blood pressure and for chemical sympathectomy by oxidizing 2,3 or 3,4 or 4,5 dihydroxyphenyl-propionic acid or derivatives thereof, and novel coumarin derivatives of the process.

Dihydrocoumarin derivatives

Benzene-ring substituted (2-methylhydrazino)methylbenzene compounds and intermediates therefor are described. The former compounds are useful as cytostatic agents.

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Lausen, Switzerland

Ado Kaiser