Hoffmann-la Roche Inc.

Roche Vitamins Inc.

Urs O Hengartner

Henri Ramuz

Jean-Claude Muller

Kurt Bernhard

Paul Kreienbuhl

Jiri Broz

Katharina Schiedt

David L Coffen

A method of pigmenting certain parts and products of poultry, fish and crustacea by including in the feed of the pertinent animal one or more of the carotenoids 2'-dehydroplectaniaxanthin, desmethylspheroidenone, spheroidenone, 1-hydroxy-3,4-didehydro-1,2-dihydro-.psi.,.psi.-caroten-2-one, 5'-hydroxy-5',6'-dihydro-4'-apo-.beta.-caroten-6'-one, 1'-hydroxy-3',4'-didehydro-1',2'-dihydro-.beta.,.psi.-carotene-4,2'-dione and 5'-hydroxy-5',6'-dihydro-4'-apo-.beta.-carotene-4,6'-dione, poultry, fish and crustacea feeds for pigmenting certains parts and products of these animals, beadlets and premixes for adding to poultry, fish and crustacea feeds, and the carotenoids 1-hydroxy-3,4-didehydro-1,2-dihydro-.psi.,.psi.-caroten-2-one, 5'-hydroxy-5',6'-dihydro-4'-apo-.beta.-caroten-6'-one, 1'-hydroxy-3',4'-didehydro-1',2'-dihydro-.beta.,.psi.-carotene-4,2'-dione and 5'-hydroxy-5',6'-dihydro-4'-apo-.beta.-carotene-4,6'-dione.

Pigmentation with carotenoids

Novel compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, lower-alkoxy-lower-alkyl, lower-alkylthio-lower-alkyl or furyl, R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylenedioxy or ethylenoxy and n is an integer from 1 to 3, have a pronounced activity in counteracting cerebral insufficiency or improving cognitive functions and also reduce the multiple-resistance towards cytostatics in the treatment of tumors or of chloroquine resistance in the treatment of malaria. They can accordingly be used as medicaments, especially for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions. The novel compounds of formula I can be manufactured by O-acylating a likewise novel compound of the formula ##STR2## wherein R.sup.2 is lower-alkyl, phenyl-lower-alkyl or cyclohexyl-lower-alkyl, each of R.sup.3 and R.sup.6 independently is hydrogen or fluorine, each of R.sup.4 and R.sup.5 independently is hydrogen or lower-alkoxy or together are methylenedioxy, ethylendioxy or ethylenoxy and n is an integer from 1 to 3.

Tetrahydronaphthalene derivatives for improving short-term memory

Tetrahydronaphthalene derivatives of the formula ##STR1## wherein Y, m, n, R and R.sup.1 to R.sup.9 are as set forth herein, are described. These compounds have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias and high blood pressure. The compounds of formula I can be prepared by the amination of a compound of the formula ##STR2## with a corresponding N-methyl-phenylalkylamine and optional subsequent O-acylation. Compounds of formula II and IV are also described and are within the scope of the invention.

Tetrahydronaphthalene derivatives

The preparation of bicyclic diketones of the formula ##STR1## wherein R.sub.1 is lower alkyl or ar-lower alkyl from a compound of the formula ##STR2## wherein R.sub.1 is as previously described or a salt thereof, and a di-lower alkyl malonate is described. The reactants are combined in a reaction sequence consisting of Michael addition, cyclization, hydrolysis, and decarboxylation. The preparation of the compounds of formula II is also described.

Process for bicyclic diketones

Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable, long-lasting vasodilating and/or blood pressure-lowering properties and are useful for the treatment of vascular-conditioned hypertensions or as vasodilators in peripheral blood supply disorders. The compounds are prepared, inter alia, by carbamoylating the corresponding derivative containing a free amino group and optional salt formation.

Growing community of inventors

Basel, Switzerland

Urs O Hengartner