Cyclic peptide antifungal agents

Details Cyclic peptide antifungal agents Cyclic peptide antifungal agents

1995-07-25

1997-05-13

Tsang, Cecilia

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 9, 530317, 530318, A61K 3812

Patent

active

056292899

ABSTRACT:
Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: ##STR1## wherein: R.sup.z1 is hydrogen, --CH.sub.2 OH, --CHOHCH.sub.3 or --CHOHCH.sub.2 C(O)NH.sub.2 ;
R.sup.z2 is hydrogen, --CH.sub.2 OH or --CHOHCH.sub.3 ;
R.sup.z3 is hydrogen or methyl;
R.sup.x1 is hydrogen, hydroxy or O--R.sup.x1' ;
R.sup.x1' is C.sub.1 -C.sub.6 alkyl, benzyl, --(CH.sub.2).sub.2 Si(CH.sub.3).sub.3, --CH.sub.2 CH.dbd.CH.sub.2, --CH.sub.2 CHOHCH.sub.2 OH, --(CH.sub.2).sub.a COOH, --(CH.sub.2).sub.b NR.sup.w1 R.sup.w2, --(CH.sub.2).sub.c POR.sup.w3 R.sup.w4 or --[(CH.sub.2).sub.2 O].sub.d --(C.sub.1 -C.sub.6)alkyl;
a, b and c are independently 1, 2, 3, 4, 5 or 6;
R.sup.w1 and R.sup.w2 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, or R.sup.w1 and R.sup.w2 combine to form --CH.sub.2 (CH.sub.2).sub.e CH.sub.2 --;
R.sup.w3 and R.sup.w4 are independently hydroxy, or C.sub.1 -C.sub.6 alkoxy;
d is 1 or 2;
e is 1, 2 or 3;
R.sup.x2, R.sup.y1, R.sup.y2, R.sup.y3 and R.sup.y4 are independently hydroxy or hydrogen;
R.sup.0 is hydroxy, --OP(O)(OH).sub.2 or a group of the formulae: ##STR2## R.sup.1 is C.sub.1 -C.sub.6 alkyl, phenyl, p-halo-phenyl, p-nitrophenyl, benzyl, p-halo-benzyl or p-nitro-benzyl;
R.sup.2 is ##STR3## R.sup.3 is ##STR4## R.sup.3a, R.sup.3b, R.sup.3c and R.sup.3d are independently hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkynyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, halo, --O--(CH.sub.2).sub.m --[O--(CH.sub.2).sub.n ].sub.p --O--(C.sub.1 -C.sub.12 alkyl) or --O--(CH.sub.2).sub.q --X--R.sup.4 ;
m is 2, 3 or 4;
n is 2, 3 or 4;
p is 0 or 1;
q is 2, 3 or 4;
X is pyrrolidino, piperidino or piperazino; and
R.sup.4 is hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.12 cycloalkyl, benzyl or C.sub.3 -C.sub.12 cycloalkylmethyl;
with the proviso that at least one of R.sup.z1 and R.sup.z2 must be hydrogen;
or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 5057493 (1991-10-01), Takesako et al.
patent: 5059540 (1991-10-01), Bailey
patent: 5158876 (1992-10-01), Takesako et al.
patent: 5166135 (1992-11-01), Schmatz
patent: 5200505 (1993-04-01), Takesako et al.
patent: 5260214 (1993-11-01), Takesako et al.
patent: 5376634 (1994-12-01), Iwamoto et al.
J. Org. Chem., 1981, 46, 4789-4791.
J. Antibiotics, Sep. 1991, vol. 44, No. 9, 925-933.
J. Antibiotics, Sep. 1991, vol. 44, No. 9, 919-924.
J. Molecular Structure (Theochem), 180 (1988) 383-387.
U.S. application Ser. No. 08/339,525, Filing Date Nov. 15, 1994.

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