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US 2004/0171675 A1Published application
Antifungal agents of sordarin derivatives
AssigneeMerck & Co., Inc.
InventorsJames M. Balkovec, Bruno Tse
Life of this patent
Estimating the term…
Abstract
Sordarin derivatives prepared from C-11-hydroxysordarin 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.
Claims24
A compound of formula I:
- 59
- or a pharmaceutically or agriculturally acceptable salt thereof,
- wherein
- R is:
- (a) hydrogen,
- (b) C(O)OR1,
- (c) C(O)NR2R3,
- (d) C(O)R4,
- (e) CH(R2)OR5,
- (f) C(R6)(R7)(R8),
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- R1 is:
- (a) (C1-C14)alkyl,
- (b) (C2-C14)alkenyl,
- (c) (C2-C14)alkynyl,
- (d) (C3-C20)cycloalkyl,
- (e) aryl or
- (f) aryl-(C1-C6)alkyl;
- R2 and R3 are independently:
- (a) H or
- (b) R1;
- R4 is:
- (a) H,
- (b) R1 or
- (c) (CH2)mNR2R3;
- R5 is:
- (a) R1 or
- (b) (CH2)xO(CH2)yH;
- R6 is:
- (a) H,
- (b) (C1-C14)alkyl,
- (c) aryl,
- (d) aryl-(C1-C6)alkyl,
- (e) (CH2)yCHR9(CH2)zH,
- (f) (CH2)yC≡C(CH2)zH,
- (g) (CH2)yC(R7)═CH(CH2)zH,
- (h) (CH2)yC—C(CH2)mR9 or
- (i) (CH2)yC(R7)═CH(CH2)mR9;
- R7 and R8 are independently:
- (a) H or
- (b) (C1-C14)alkyl;
- R9 is:
- (a) OH or
- (b) NR2R3;
- R10 is:
- (a) C(O)H or
- (b) CN;
- R11 is:
- (a) H,
- (b) —CH2CH═CH2,
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- X1 and X2 are independently:
- (a) H, wherein X1 and X2 are not H simultaneously,
- (b) (C1-C6)alkyl,
- (c) (C1-C6)alkoxy,
- (d) (C2-C6)alkenyl optionally substituted with R1,
- (e) OH, wherein X1 and X2 are not OH simultaneously,
- (f) OC[(C1-C6)alkyl]3,
- (g) OC(O)(C1-C6)alkyl,
- (h) halo, wherein halo is F, Cl, Br or I,
- (i) SC(O)(C1-C6)alkyl,
- (j) S(C1-C6)alkyl,
- (k) SH,
- (l) N3,
- (m) N[(C1-C6)alkyl]2,
- (n) N[(C1-C6)alkyl]C(O)(C1-C6)alkyl or
- (o) CN;
- and
- wherein X1 and X2 together can be oxo or ═CH2;
- n is:
- 0 or 1;
- m is:
- 1-6;
- p is:
- 0-5;
- x is:
- 2-6;
- y is:
- 0-6;
- and
- z is:
- 0-6.
79 more elements
Dependencies are inferred from the claim text.