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|Title:||Aza cyclohexapeptide compounds|
|Abstract:||Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.|
|Inventor(s):||Balkovec; James M. (North Plainfield, NJ), Bouffard; Frances Aileen (Scotch Plains, NJ), Black; Regina M. (Cranford, NJ)|
|Assignee:||Merck & Co., Inc. (Rahway, NJ)|
1. A compound having the formula ##STR19## wherein: R.sub.1 is H or OH;
R.sub.2 is H, CH.sub.3 or OH;
R.sub.3 is H, CH.sub.3, CH.sub.2 CN, CH.sub.2 CH.sub.2 NH.sub.2 or CH.sub.2 CONH.sub.2 ;
R.sup.I is C.sub.9 -C.sub.21 alkyl, C.sub.9 -C.sub.21 alkenyl, C.sub.1 -C.sub.10 alkoxyphenyl or C.sub.1 -C.sub.10 alkoxynaphthyl;
R.sup.II is H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, (CH.sub.2).sub.2-4 OH, (CH.sub.2).sub.2-4 NR.sup.IV R.sup.V, CO(CH.sub.2).sub.1-4 NH.sub.2 ;
R.sup.III is H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, (CH.sub.2).sub.2-4 OH, (CH.sub.2).sub.2-4 NR.sup.IV R.sup.V, or
R.sup.II and R.sup.III taken together are --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 --, --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 --NH--(CH.sub.2).sub.2 --;
R.sup.IV is H or C.sub.1 -C.sub.4 alkyl,
R.sup.V is H or C.sub.1 -C.sub.4 alkyl; and acid addition salts thereof.
2. An antimicrobial composition comprising a compound of claim 1 in admixture with a pharmaceutically acceptable carrier.
3. A method for treatment of mycotic infections comprising administering to mammalian subject in need of treatment, an antimycotic amount of a compound of claim 1.
4. A method for treatment of pneumocystis pneumonia in immune-compromised patients comprising administering a therapeutically effective amount of a compound of claim 1.
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