Title:
MODIFIED CYCLOSPORINE WHICH CAN BE USED AS A PRO-DRUG AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO2002085928
Kind Code:
A3
Abstract:
The invention relates to a pro-drug comprising a cyclic undecapeptide wherein the peptide chain thereof comprises at least one amino acid residue of general formula (1) wherein the carbon atom C is one of the links in said undecapeptide cycle; - substituents Y individually represent a hydrogen atom or form a bond together; - substitutents R<1> and R<3> independently represent a hydrogen atom, an aralkyl group, an alkaryl group, a heteroalkyl group, a heterocyclic group, a heterocyclic alkyl group, an alkyl heterocyclic group or an alkyl group having 1-6 carbon atoms which is linear or branched, and which is optionally substituted by at least one of the groups chosen from among -COOH, -CONHR<8>, -NHC0=NH(NH2), -NHC=NR<8>(NH2), -NH2, -NHR<8>, -NR<8>2, -N<+>R<8>3, -OH, -OPO(OR<8>)2, -OPO(OH)(OR<8>), -OPO(OH)2, -OSO(OR<8>)2, -OSO(OH)(OR<8>), -OSO(OH)2, and the different salts produced therefrom, each of the substituents R<8> independently representing an alkyl group which is linear or ramified having 1 - 6 carbon atoms; - substituents R<2> and R<4> independently represent a hydrogen atom, an alkaryl group or an alkyl group having 1 - 6 carbon atoms which is linear or branched; - the substituents R<5> and R<6> individually represent a hydrogen atom, an aralkyl group, an alkyl group having 1-6 carbon atoms which is linear or branched; and substituent R<7> represents an alkaryl group, a heteroalkyl group, a heterocylic group,a heterocylic alkyl group, an alkyl heterocyclic group or an alkyl group having1 - 6 carbon atoms which is linear or branched.
Inventors:
WENGER ROLAND (CH)
MUTTER MANFRED (CH)
HAMEL ARNAUD (CH)
HUBLER FRANCIS (CH)
MUTTER MANFRED (CH)
HAMEL ARNAUD (CH)
HUBLER FRANCIS (CH)
Application Number:
PCT/CH2002/000222
Publication Date:
April 17, 2003
Filing Date:
April 22, 2002
Export Citation:
Assignee:
DEBIOPHARM SA (CH)
WENGER ROLAND (CH)
MUTTER MANFRED (CH)
HAMEL ARNAUD (CH)
HUBLER FRANCIS (CH)
WENGER ROLAND (CH)
MUTTER MANFRED (CH)
HAMEL ARNAUD (CH)
HUBLER FRANCIS (CH)
International Classes:
A61K38/13; A61P27/02; A61P31/18; A61K38/00; A61P43/00; C07K7/64; (IPC1-7): C07K7/64; A61K38/13; A61K47/48
Domestic Patent References:
| WO2001005818A1 | 2001-01-25 | |||
| WO2001005819A1 | 2001-01-25 | |||
| WO2000008033A1 | 2000-02-17 | |||
| WO2000067801A2 | 2000-11-16 |
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