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US 5,162,335 AGranted
Di- and tetrahydroisoquinoline derivatives
AssigneeDuphar International Research B.V.
InventorsMaurits E. A. Vandewalle, Johan T. A. Van der Eycken, Ineke van Wijngaarden, Roelof van Hes, Antonius Hulkenberg, Christophorus M. J. F. Keet
Life of this patent
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Abstract
The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.
Claims6
Di- and tetrahydroisoquinoline derivatives of the formula (I):
- ##STR47## wherein:
- R, R.sub.1, R.sub.2, and R.sub.13 are independently selected from the group consisting of hydrogen, halogen and trifluoromethyl;
- or
- R+R.sub.1 together with the carbon atoms to which they are bound represent a ring selected form the group consisting of:
- an aromatic carbocyclic ring, ethylenedioxide, methylenedioxide and propylenedioxide;
- or
- R.sub.1 +R.sub.2 together with the carbon atoms to which they are bound represent a ring selected from the group consisting of:
- a saturated carbocyclic ring, ethylenedioxide, methylenedioxide and propylenedioxide;
- or
- R.sub.2 +R.sub.13 together with the carbon atoms to which they are bound represent a ring selected from the group consisting of:
- an aromatic carbocyclic ring, ethylenedioxide, methylenedioxide and propylenedioxide;
- R.sub.3 is selected from the group consisting of:
- hydrogen, hydroxymethyl, alkoxy or alkanoyloxy having 1-4 carbon atoms, and hydroxy;
- R.sub.4 is selected from the group consisting of:
- methyl, aminomethyl, -CH.sub.2 -OR.sub.12, an alkanoyloxy group of 2 to 6 C-atoms, an alkoxycarbonyl group with 1 to 3 C-atoms in the alkoxy moiety, and -CO-N(R.sub.11).sub.2,
- wherein R.sub.11 is selected from the group consisting of hydrogen and alkyl having 1 to 3 carbon atoms;
- and
- R.sub.12 is selected from the group consisting of hydrogen and tetrahydropyran-2-yl;
- R.sub.5 is selected from the group consisting of hydrogen, hydroxy, alkanoyl or alkyl having 1-4 C-atoms, and the group ##STR48## R.sub.6 is hydrogen;
- R.sub.5 +R.sub.6 together constitute a double bond;
- R.sub.7 and R.sub.9, independently of each other, are hydrogen or alkoxy having 1-2 C-atoms;
- R.sub.8 is selected from the group consisting of:
- hydrogen, alkoxy or alkanoyloxy having 1-2 C-atoms, and hydroxy;
- R.sub.7 +R.sub.8 or R.sub.8 +R.sub.9 together constitute a methylenedioxy group or ethylenedioxy group;
- R.sub.10 is hydrogen or methoxy;
- R.sub.14 is hydrogen or methyl;
- and
- R.sub.3 +R.sub.14 together constitute a double bond;
- and acid addition salts and prodrugs thereof.
26 more elements
Dependencies are inferred from the claim text.