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Claims for Patent: 6,107,458

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Claims for Patent: 6,107,458

Title: Cyclic hexapeptides having antibiotic activity
Abstract:This invention relates to new polypeptide compounds represented by the following formula (I): ##STR1## wherein R.sup.1 is as defined in the description and pharmaceutically acceptable salt thereof which have antimicrobial activities (especially, antifungal activities), inhibitory activity on .beta.-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for the prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
Inventor(s): Ohki; Hidenori (Takarazuka, JP), Tomishima; Masaki (Minoo, JP), Yamada; Akira (Fujiidera, JP), Takasugi; Hisashi (Sakai, JP)
Assignee: Fujisawa Pharmaceutical Co., Ltd. (Osaka, JP)
Application Number:08/809,723
Patent Claims: 1. A polypeptide compound of the following general formula (I): ##STR133## wherein R.sup.1 is benzoyl substituted with isoxazolyl which has phenyl having lower alkoxy, or a salt thereof.

2. A compound of claim 1, wherein R.sup.1 is ##STR134##

3. A process for the preparation of a polypeptide compound of the formula (I): wherein R.sup.1 is benzoyl substituted with isoxazolyl which has phenyl having lower alkoxy, or a salt thereof, said process comprising:

1) reacting a compound of the formula (II): ##STR135## or its reactive derivative at the amino group or a salt thereof, with a compound of formula (III):

or its reactive derivative at the carboxy group or a salt thereof, wherein R.sup.1 is defined above, to give a compound of formula (I).

4. A pharmaceutical composition which comprises, as an active ingredient, a compound of claim 1, or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable carrier or excipient.

5. A method for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms, comprising administering an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof, to a human being or animal.
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