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Claims for Patent: 5,376,634

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Claims for Patent: 5,376,634

Title: Polypeptide compound and a process for preparation thereof
Abstract:A polypeptide compound having antimicrobial activity of the following general formula: ##STR1## wherein R.sup.1 is hydrogen or acyl group, R.sup.2 is hydroxy or acyloxy, R.sup.3 is hydroxysulfonyloxy, and R.sup.4 is hydrogen or carbamoyl, with proviso that R.sup.1 is not palmitoyl, when R.sup.2 is hydroxy, R.sup.3 is hydroxysulfonyloxy and R.sup.4 is carbamoyl, and a pharmaceutically acceptable salt thereof.
Inventor(s): Iwamoto; Toshiro (Tsukuba, JP), Fujie; Akihiko (Tsuchiura, JP), Nitta; Kumiko (Tsuchiura, JP), Tsurumi; Yasuhisa (Tsukuba, JP), Shigematsu; Nobuharu (Tsukuba, JP), Kasahara; Chiyoshi (Ikeda, JP), Hino; Motohiro (Tsuchiura, JP), Okuhara; Masakuni (Tsukuba, JP), Sakane; Kazuo (Kawanishi, JP), Kawabata; Kohji (Kawanishi, JP), Ohki; Hidenori (Ikeda, JP)
Assignee: Fujisawa Pharmaceutical Co., Ltd. (Osaka, JP)
Application Number:07/715,961
Patent Claims: 1. A polypeptide compound having antimicrobial activity of the following formula: ##STR63## wherein R.sup.1 is a hydrogen or acyl group,

R.sup.2 is hydroxy or acyloxy,

R.sup.3 is hydroxysulfonyloxy, and

R.sup.4 is hydrogen or carbamoyl,

with proviso that

R.sup.1 is not palmitoyl, when R.sup.2 is hydroxy,

R.sup.3 is hydroxysulfonyloxy and

R.sup.4 is carbamoyl,

and a salt thereof.

2. A polypeptide compound of claim 1, which is shown by the following formula (SEQ ID NO: 1): ##STR64## wherein R.sup.1 is as defined above.

3. A compound of claim 2, wherein

R.sup.1 is lower alkanoyl which may have one or more suitable substituent(s); higher alkanoyl, lower alkenoyl which may have one or more suitable substituent(s); higher alkenoyl; lower alkoxycarbonyl; higher alkoxycarbonyl; aryloxycarbonyl; arylglyoxyloyl; ar(lower)alkoxycarbonyl which may have one or more suitable substituent(s); lower alkylsulfonyl; arylsulfonyl which may have one or more suitable substituent(s); ar(lower)alkylsulfonyl; or aroyl which may have one or more suitable substituent(s).

4. A compound of claim 3, wherein

R.sup.1 is lower alkanoyl; halo(lower)alkanoyl; ar(lower)alkanoyl which may have 1 to 3 suitable substituent(s) selected from the group consisting of hydroxy, lower alkoxy, higher alkoxy, aryl, amino, protected amino, di(lower)alkylamino, lower alkoxyimino and ar(lower)alkoxyimino which may have 1 to 3 higher alkoxy; heterocyclicthio(lower)alkanoyl which may have 1 to 3 higher alkyl; heterocyclic(lower)alkanoyl which may have 1 to 3 suitable substituent(s) selected from the group consisting of lower alkoxyimino, higher alkyl, amino and protected amino; ar(lower)alkoxyimino(lower)alkanoyl which may have 1 to 3 higher alkoxy; higher alkanoyl; ar(lower)alkenoyl which may have 1 to 3 higher alkoxy; higher alkenoyl; lower alkoxycarbonyl; higher alkoxycarbonyl; aryloxycarbonyl; arylsulfonyl which may have 1 to 3 suitable substituent(s) selected from the group consisting of lower alkyl and higher alkoxy; or aroyl which may have 1 to 5 suitable substituent(s) selected from the group consisting of halogen, lower alkyl, higher alkyl, carboxy, lower alkoxy which may have 1 to 10 halogen, lower alkoxy(lower)alkoxy, ar(lower)alkoxy, higher alkoxy which may have 1 to 17 halogen, higher alkenyloxy, aryl which may have 1 to 3 higher alkoxy and aryloxy which may have 1 to 3 lower alkoxy or higher alkoxy.

5. A compound of claim 4, wherein

R.sup.1 is lower alkanoyl; halo(lower)alkanoyl; phenyl(lower)alkanoyl or naphthyl(lower)alkanoyl, each of which may have 1 to 3 suitable substituent(s) selected from the group consisting of hydroxy, lower alkoxy, higher alkoxy, phenyl, amino, lower alkoxycarbonylamino, di(lower)alkylamino, lower alkoxyimino and phenyl(lower)alkoxyimino which may have 1 to 3 higher alkoxy;

pyridylthio(lower)alkanoyl which may have 1 to 3 higher alkyl; imidazolyl(lower)alkanoyl or thiazolyl(lower)alkanoyl, each of which may have 1 to 3 suitable substituent(s) selected from the group consisting of lower alkoxyimino, higher alkyl, amino and lower alkoxycarbonylamino;

phenyl(lower)alkoxyimino(lower)alkanoyl which may have 1 to 3 higher alkoxy; higher alkanoyl;

phenyl(lower)alkenoyl which may have 1 to 3 higher alkoxy; higher alkenoyl; lower alkoxycarbonyl, higher alkoxycarbonyl; phenoxycarbonyl; phenylsulfonyl or naphthylsulfonyl, each of which may have 1 to 3 suitable substituent(s) selected from the group consisting of lower alkyl and higher alkoxy; or, benzoyl, naphthoyl or anthrylcarbonyl, each of which may have 1 to 5 suitable substituent(s) selected from the group consisting of halogen, lower alkyl, higher alkyl, carboxy, lower alkoxy, which may have 6 to 10 halogen, lower alkoxy(lower)alkoxy, phenyl(lower)alkoxy, higher alkoxy which may have 12 to 17 halogen, higher alkenyloxy, phenyl which may have 1 to 3 higher alkoxy, and phenoxy which may have 1 to 3 lower alkoxy or higher alkoxy.

6. A compound of claim 5, wherein

R.sup.1 is phenyl(lower)alkenoyl which may have 1 to 3 higher alkoxy; or benzoyl, naphthoyl or anthrylcarbonyl, each of which may have 1 to 5 suitable substituent(s) selected from the group consisting of halogen, lower alkyl, higher alkyl, carboxy, lower alkoxy which may have 6 to 10 halogen, lower alkoxy(lower)alkoxy, phenyl(lower)alkoxy, higher alkoxy which may have 12 to 17 halogen, higher alkenyloxy, phenyl which may have 1 to 3 higher alkoxy, and phenoxy which may have 1 to 3 lower alkoxy or higher alkoxy.

7. A compound of claim 6, wherein R.sup.1 is phenyl(lower)alkenoyl which may have higher alkoxy; or benzoyl or naphthoyl, each of which may have higher alkoxy, higher alkenyloxy, or phenyl which may have higher alkoxy.

8. A compound of claim 7, wherein R.sup.1 is benzoyl which has higher alkoxy.

9. A compound of claim 8, wherein R.sup.1 is 4-octyloxybenzoyl.

10. A compound of Claim 7, wherein R.sup.1 is phenyl(lower)alkenoyl which has higher alkoxy; or naphthoyl which was higher alkoxy or higher alkenyloxy.

11. A pharmaceutical composition having antimicrobial activity which comprises an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable carrier or excipient.
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