Back to results
US 5,965,612 AGranted
4-cyano-4-deformylsordaricin derivatives
AssigneeMerck & Co., Inc.
InventorBruno Tse
Life of this patent
Estimating the term…
Abstract
4-Cyano-4-deformylsordaricin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.
Claims16
A compound having the formula I:
- ##STR24## wherein:
- R is
- (a) C(.dbd.O)OR.sup.1,
- (b) C(.dbd.O)NR.sup.2 R.sup.3,
- (c) C(.dbd.O)R.sup.4,
- (d) CH(R.sup.2)OR.sup.5,
- (e) C(R.sup.6)(R.sup.7)(R.sup.8),
- (f) ##STR25## or (g) H;
- R.sup.1 is
- (a) C.sub.1 -C.sub.14 alkyl,
- (b) C.sub.2 -C.sub.14 alkenyl,
- (c) C.sub.2 -C.sub.14 alkynyl,
- (d) C.sub.3 -C.sub.20 cycloalkyl,
- (e) aryl or
- (f) aryl C.sub.1-6 alkyl;
- R.sup.2 and R.sup.3 are independently
- (a) H or
- (b) R.sup.1 ;
- R.sup.4 is
- (a) H,
- (b) R.sup.1 or
- (c) --(CH.sub.2).sub.m NR.sup.2 R.sup.3 ;
- R.sup.5 is
- (a) R.sup.1 or
- (b) --(CH.sub.2).sub.x O(CH.sub.2).sub.y H;
- R.sup.6 is
- (a) H,
- (b) C.sub.1 -C.sub.14 alkyl,
- (c) aryl,
- (d) aryl C.sub.1-6 alkyl,
- (e) --(CH.sub.2).sub.y CHR.sup.9 (CH.sub.2).sub.z H,
- (f) --(CH.sub.2).sub.y C.tbd.C(CH.sub.2).sub.z H,
- (g) --(CH.sub.2).sub.y C(R.sup.7).dbd.CH(CH.sub.2).sub.z H,
- (h) --(CH.sub.2).sub.y C.tbd.C(CH.sub.2).sub.m R.sup.9,
- (i) --(CH.sub.2).sub.y C(R.sup.7).dbd.CH(CH.sub.2).sub.m R.sup.9,
- R.sup.7 and R.sup.8 are independently
- (a) H, or
- (b) C.sub.1 -C.sub.14 alkyl;
- R.sup.9 is
- (a) OH or
- (b) NR.sup.2 R.sup.3 ;
- R.sup.10 is
- (a) H;
- (b) --CH.sub.2 C.sub.6 H.sub.5,
- (c) --CH.sub.2 CH.dbd.CH.sub.2, ##STR26## n is 0 or 1;
- m is 1-6;
- x is 2-6;
- y is 0-6;
- z is 0-6;
- or
- a pharmaceutically or agriculturally acceptable salt thereof.
48 more elements
Dependencies are inferred from the claim text.