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Generated: January 18, 2018

DrugPatentWatch Database Preview

Claims for Patent: 4,572,909

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Summary for Patent: 4,572,909
Title: 2-(Secondary aminoalkoxymethyl) dihydropyridine derivatives as anti-ischaemic and antihypertensive agents
Abstract:A dihydropyridine compound of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein Y is --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --; R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; and R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, 2-(C.sub.1 -C.sub.4 alkoxy)ethyl, cyclopropylmethyl, benzyl, or --(CH.sub.2).sub.m COR.sup.4 where m is 1, 2 or 3 and R.sup.4 is hydroxy, C.sub.1 -C.sub.4 alkoxy or --NR.sup.5 R.sup.6 where R.sup.5 and R.sup.6 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl can be employed for treating or preventing a heart condition or hypertension.
Inventor(s): Campbell; Simon F. (Deal, GB2), Cross; Peter E. (Canterbury, GB2), Stubbs; John K. (Deal, GB2)
Assignee: Pfizer Inc. (New York, NY)
Application Number:06/576,982
Patent Claims: 1. A dihydropyridine compound of the formula ##STR58## or a pharmaceutically acceptable acid addition salt thereof, wherein Y is --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.sub.2 CH(CH3)-- or --CH.sub.2 C(CH.sub.3)2--;

R is aryl; R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; and R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, 2-(C.sub.1 -C.sub.4 alkoxy)ethyl, cyclopropylmethyl, benzyl, or --(CH.sub.2).sub.m COR.sup.4 where m is 1, 2 or 3 and R.sup.4 is hydroxy, C.sub.1 -C.sub.4 alkoxy or --NR.sup.5 R.sup.6 where R.sup.5 and R.sup.6 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; wherein aryl is phenyl; phenyl substituted by one or two of nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, trifluoromethyl or cyano; 1-naphthyl; or 2-naphthyl.

2. A compound according to claim 1 wherein the aryl is 2-chlorophenyl or 2,3-dichlorophenyl.

3. A compound according to claim 1 wherein R.sup.3 is H, CH.sub.3 or --(CH.sub.2).sub.m COR.sup.4 wherein m is 1.

4. A compound according to claim 1 wherein R.sup.1 is CH.sub.3.

5. A compound according to claim 1 wherein R.sup.2 is C.sub.2 H.sub.5.

6. A compound according to claim 1 wherein Y is --(CH.sub.2).sub.2 --.

7. A compound according to claim 1 wherein R is 2-chlorophenyl or 2,3-dichlorophenyl, R.sup.1 is CH.sub.3, R.sup.2 is C.sub.2 H.sub.5, Y is --(CH.sub.2).sub.2 -- and R.sup.3 is H or CH.sub.3.

8. A compound according to claim 7 wherein R is 2-chlorophenyl and R.sup.3 is H.

9. A compound according to claim 1 wherein R.sup.1 and R.sup.2 are each alkyl.

10. A compound according to claim 9 wherein Y is --(CH.sub.2).sub.2 --.

11. A compound according to claim 10 wherein R.sup.3 is hydrogen.

12. A compound according to claim 11 wherein R.sup.1 is ethyl, R.sup.2 is methyl and R is 2,3-dichlorophenyl.

13. A compound according to claim 11 wherein R.sup.1 is methyl, R.sup.2 is ethyl and R is 2-chloro-3-trifluoromethylphenyl.

14. A pharmaceutical composition comprising an anti-ischaemic or antihypertensive effective amount of a compound according to claim 1 and a pharmaceutically acceptable diluent or carrier.

15. A pharmaceutical composition comprising an anti-ischaemic or antihypertensive effective amount of a compound according to claim 7 and a pharmaceutically acceptable diluent or carrier.

16. A method of treating or preventing ischaemic heart disease in man which comprises administering an anti-ischaemic effective amount of a compound according to claim 1.

17. A method of treating or preventing hypertension in man which comprises administering an antihypertensive effective amount of a compound according to claim 1.

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