Polycyclic guanine derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 473/02 (2006.01) A61K 31/52 (2006.01) A61K 31/53 (2006.01) A61K 31/535 (2006.01) C07D 487/14 (2006.01)

Patent

CA 2085733

Novel polycyclic guanine derivatives of formula (I) and (I'), wherein J is oxygen or sulfur, R1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy; R2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino, or -(CH2)mTCOR20 wherein m is an integer from 1 to 6, T is oxygen or -NH- and R20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl; R3 is hydrogen, ha- lo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydrox- yalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with aryl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino; Ra, Rb, Rc and Rd independently represent hydrogen, alkyl, cycloalkyl or aryl; or (Ra and Rb) or (Rc and Rd) or (Rb and Rc) can complete a saturated ring of 5- to 7- carbon atoms, or (Ra and Rb) taken to- gether and (Rb and Rc) taken together, each complete a saturated ring of 5- to 7- carbon atoms, wherein each ring optionally can contain a sulfur or oxygen atom and whose carbon atoms may be optionally substituted with one or more of the follow- ing: alkenyl, alkynyl, hydroxy, carboxy, alkoxycarbonyl, alkyl or alkyl substituted with hydroxy, carboxy or alkoxycarbo- nyl; or such saturated ring can have two adjacent carbon atoms which are shared with an adjoining aryl ring; and n is zero or one. The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.

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