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US 6,040,463 AGranted
Sordarin derivatives
AssigneeMerck & Co., Inc.
InventorsJames M. Balkovec, Bruno Tse
Life of this patent
Estimating the term…
Abstract
Sordarin 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.
Claims15
A compound having the formula I:
- ##STR38## 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), ##STR39## with the proviso that when R.sup.12 is CHO, R is not (g);
- 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) C.sub.3 -C.sub.20 cycloalkenyl,
- (f) aryl or
- (g) 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) R.sup.1,
- (c) --(CH.sub.2).sub.y CHR.sub.11 (CH.sub.2).sub.z H,
- (d) --(CH.sub.2).sub.y C.tbd.--C(CH.sub.2).sub.z H,
- (e) --(CH.sub.2).sub.y C(R.sup.7).dbd.CH(CH.sub.2).sub.z H,
- (f) --(CH.sub.2).sub.y C.tbd.C(CH.sub.2).sub.m R.sup.11,
- (g) --(CH.sub.2).sub.y C(R.sup.7).dbd.CH(CH.sub.2).sub.m R.sup.11,
- R.sup.7 and R.sup.8 are independently
- (a) H, or
- (b) C.sub.1 -C.sub.14 alkyl;
- R.sup.9 and R10 are independently
- (a) H,
- (a) C.sub.1 -C.sub.14 alkyl,
- (a) C.sub.2 -C.sub.14 alkenyl,
- (a) aryl C.sub.1-6 alkyl;
- R.sup.11 is
- (a) OR.sup.7,
- (b) OCH.sub.2 CH.sub.2 (CH.sub.2).sub.n OR.sup.7, or
- (c) NR.sup.2 R.sup.3 ;
- R.sup.12 is
- (a) --C(.dbd.O)R.sup.14,
- (b) --CH.dbd.NOH, or
- (c) --CH.sub.2 OCH.sub.3 ;
- R.sup.13 is
- (a) H,
- (b) --CH.sub.2 C.sub.6 H.sub.5,
- (c) --CH.sub.2 CH.dbd.CH.sub.2, ##STR40## R.sup.14 is (a) H,
- (b) C.sub.1 -C.sub.4 alkyl,
- (c) --CCl.sub.3,
- (d) --CBr.sub.3,
- (e) --CF.sub.3, or
- (f) OH;
- 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.
60 more elements
Dependencies are inferred from the claim text.