ДЖЕНКИНС Томас Э. (US),СЕРУДЖИ Джули Д. (US),РЭЙ Джонатан В. (US)
申请号：
RU2011119643/15
公开号：
RU2011119643A
申请日:
2009.10.16
申请国别(地区):
RU
年份:
2012
代理人:
摘要：
1. A pharmaceutical composition which comprises a trypsin inhibitor and a compound of general formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is a residue of a phenolic opioid, wherein the hydrogen atom of a phenolic hydroxyl group is replaced by a covalent bond to C (O) -NR- (C (R) (R)) - NH-C (O) -CH (R) -NH (R) R is (1-4C) alkyl group each independently represent a hydrogen atom or a (1-4C) alkyl group n is 2 or 3 R is -CHCHCHNH (C = NH) NHili -CHCHCHCHNH, configuration of the carbon atom to which is attached R, corresponds to such from L-amino acids iRpredstavlyaet a hydrogen atom, N-acyl group or the residue of an amino acid, dipeptide, or N-acyl derivative of an amino acid or dipeptida.2. A pharmaceutical composition according to claim 1, wherein the phenolic opioid is selected from oxymorphone, hydromorphone and morfina.3. A pharmaceutical composition according to claim 1, wherein the compound of general formula (I) has the general formula (IV): or a pharmaceutically acceptable salt thereof, wherein: R is hydrogen or hydroxy R is oxo (= O) or OH dotted line represents a double bond or a single bond R is (1-4C) alkyl group each independently represent a hydrogen atom or a (1-4C) alkyl group n is 2 or 3 R is -CHCHCHNH (C = NH) NHili -CHCHCHCHNH , the configuration of the carbon atom to which is attached R, corresponds to that of L-ami okisloty iRpredstavlyaet a hydrogen atom, N-acyl group or the residue of an amino acid, dipeptide, or N-acyl derivative of an amino acid or dipeptida.4. A pharmaceutical composition according to any one of claims 1-3, wherein R methyl or ethyl gruppu.5. Pharmaceutical
