4-[2-(2-Substituted phenyl)ethenyl]-N-alkenyl or alkinyl substit

Details 4-[2-(2-Substituted phenyl)ethenyl]-N-alkenyl or alkinyl substit 4-[2-(2-Substituted phenyl)ethenyl]-N-alkenyl or alkinyl substit

1978-02-06

1980-06-17

Waddell, Frederic E.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

542455, A61K 3144, C07D21170

Patent

active

042084156

ABSTRACT:
Compounds of the formula and their pharmaceutically acceptable acid addition salts ##STR1## wherein X is lower alkoxy, Cl, Br, or F; R is ##STR2## or --C.tbd.C--R.sub.4 ; R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from hydrogen and methyl; n is an integer from 1 to 3 provided that when n is 3 at least two of R.sub.1, R.sub.2 and R.sub.3 are hydrogen and R.sub.4 is hydrogen, and further provided that when n is 2 at least one of R.sub.1, R.sub.2 and R.sub.3 is hydrogen; are disclosed. These compounds possess useful pharmaceutical activities due to their ability to inhibit the prostaglandin-inactivating enzyme 15-.alpha.-hydroxyprostaglandin dehydrogenase.

REFERENCES:
patent: 3898236 (1975-08-01), Hauck et al.
patent: 3953434 (1976-04-01), Hauck et al.
patent: 3965102 (1976-06-01), Hauck et al.
patent: 4016223 (1977-04-01), Rajadhyaksha et al.
patent: 4038415 (1977-07-01), Rajadhyaksha et al.
Gauthier, (Ph.D. Thesis, Univ. of New Hampshire, 1966), pp. 116, 117 & 135.
Peskar et al., J. Pharm. Pharmac., 1976, 28, 146.
Anggard et al., Methods in Enzymology, vol. 14, (1969), pp. 215-219.

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