C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
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.
Lindo Neil A.
Mckittrick Brian A.
Neustadt Bernard R.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
Schering Corporation
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