N.sup.6 -substituted adenosines

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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536 24, 536 27, 536 28, 536 29, 514 46, 514 47, A61K 3170, C07H 19167

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active

047555947

ABSTRACT:
The present inventions are novel N.sup.6 -substituted adenosines wherein the N substituent is ##STR1## wherein Ar is an unsubstituted or substituted (1) phenyl, (2) 1- or 2-naphthalenyl, (3) 2- or 3-thienyl, (4) 2- or 3-furanyl, (5) 2-, 4-, or 5-thiazyl, (6) 2-, 3-, or 4-pyridyl, or (7) 2-pyrimidyl wherein the substituents include at least one of lower alkyl, halo, trifluoromethyl, hydroxy, lower alkoxy, lower acyloxyamino, N-lower monoalkyl or N,N-lower dialkylamino, lower thioalkyl, lower alkylsulfonyl, or nitro and R' is hydrogen or alkyl, A is ##STR2## wherein q, q', or q" are one to four, n and m are independently zero to three provided if A is a bond then n and m is at least 2 and if A is other than a bond then n and m is at least one. These novel adenosines have highly desirable central nervous system and cardiovascular activities and therefore the present invention also includes pharmaceutical compositions and methods of use therefor.

REFERENCES:
patent: 4590180 (1986-05-01), Imscher et al.
patent: 4593019 (1986-06-01), Bristol et al.
patent: 4614732 (1986-09-01), Hamilton et al.
patent: 4616003 (1986-10-01), Hamilton et al.
patent: 4657897 (1987-04-01), Bristol et al.
patent: 4657898 (1987-04-01), Bristol et al.

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