|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.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.