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 Phthalidyl-isoquinoline derivatives

Details
Inventors: Chazerain, Jacques A.; Cotereau, Hubert Y.; Lallouette, Pierre H.; Legger, Hugues A.; Lepape, Pierre A. C.;
Assignee: Laborec Laboratoire de Recherches Biologiques (Asnieres, FR); Calaire Chimie, S.A. (Calais, FR)
Primary Examiner: Daus; Donald G.
Assistant Examiner: Turnipseed; James H.
Attorney, Agent or Firm: Wegner & Bretschneider

The phthalidyl-isoquinoline derivatives have the formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.4, R.sub.5 and R.sub.6 each denotes a lower alkoxy group, R.sub.3 denotes a hydrogen atom or a lower alkoxy group and R.sub.7 denotes a lower alkyl group and also include their diastereoisomers and their addition salts with pharmaceutically acceptable acids. These compounds have antiallergic activities and may be used to treat allergic symptoms in human beings and other animals.

DETAILED DESCRIPTION We claim: 1.
A compound of the formula ##STR6## wherein each of R.
sub.
1, R.
sub.
2, R.
sub.
4, R.
sub.
5 and R.
sub.
6 is lower alkoxy; R.
sub.
3 is hydrogen or lower alkoxy; and R.
sub.
7 is lower alkyl or a diasterioisomer thereof or a pharmaceutically acceptable acid addition salt thereof.
2.
2-methyl-6, 7-dimethoxy-1-[4,5,6-triethoxy-7-amino-3-phthalidyl]-1,2,3,4-tetrahydro-iso quinoline.
3.
A compound of claim 1, wherein R.
sub.
1, R.
sub.
2, R.
sub.
3, R.
sub.
4, R.
sub.
5 and R.
sub.
6 are each independently methoxy or ethoxy.
4.
A compound of claim 1, wherein R.
sub.
7 is methyl.
5.
2-methyl-6,7,8-trimethoxy-1-[4,5,6-triethoxy-7-am ino-3-phthalidyl]-1,2,3,4-tetrahydro-isoquinoline.
6.
A pharmaceutical composition for inhibiting an allergic condition in a patient which comprises a compound of claim, 2, 1, 3 or 4 and a physiologically acceptable carrier or diluent.
7.
A pharmaceutical composition in dosage unit form for the treatment of allergies which comprises an effective amount of 2-methyl-6,7,8-trimethoxy-1-[4,5,6-triethoxy-7-amino-3-phthalidyl]-1,2,3,4 -tetrahydro-isoquinoline and a pharmaceutically acceptable carrier or diluent therefor.
8.
A pharmaceutical composition of claim 7, wherein said dosage unit is a tablet.
9.
A method for retarding an allergic condition in a patient which comprises administering to said patient an effective amount of a compound of claim 4 or 6.




Description:
The present invention relates to derivatives of phthalidyl-isoquinolines, their preparation, and their use as medicaments, in particular for treating allergy conditions.
Noscapine has been known for a long time, which is an alkaloid used on account of its antitussive properties.
A derivative structurally similar to this latter compound, namely tritoqualine (see French Pat.
No.
1 295 309) has been noted for its anti-allergy properties (HAHN et al, Arz.
Forsch.
20, 1490 (1970)).
It has now been found that new compounds of this type have a similar but even more useful activity, and may thus be used in therapeutics



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