¬1,3|oxazino¬4,3-a|-isoquinoline derivatives, process for...

C - Chemistry – Metallurgy – 07 – D

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260/244.2

C07D 498/04 (2006.01) C07D 498/10 (2006.01)

Patent

CA 1238905

- 38 - A b s t r a c t The invention relates to new [1,3]oxazino[4,3-a]- isoquinoline derivatives of the formula (I) Image (I) wherein R1 and R2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms, R3 is hydrogen, alkyl having from 1 to 8 carbon atoms, cycloalkyl or cycloalkenyl having from 3 to 6 carbon atoms, optionally substituted phenyl, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or heteroaryl, R4 is hydrogen or alkyl having from 1 to 4 carbon atoms, or R3 and R4 together form a -(CH2)n- group, in which n is an integer from 3 to 7, R5 is hydroxyl, halogen or an Image group, in which R6 is optionally substituted phenyl, X is oxygen or sulfur, and salts thereof. Another aspect of the invention provides a process for the preparation of these compounds. Compounds of formula (I) are pharmaceutically active and exhibit immunsuppressive, antidepressive, analgesic, antipyretic or gastric acid secretion inhibiting activity. Pharmaceutical compositions containing them are also within the scope of the invention.

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