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    • 64. 发明申请
    • NOVEL INHIBITORS OF DIPEPTIDYL PEPTIDASE I
    • 脯氨酸肽的新型抑制剂I
    • WO2003022871A2
    • 2003-03-20
    • PCT/EP2002/010020
    • 2002-09-06
    • PROBIODRUG AGDEMUTH, Hans-UlrichHEISER, UlrichNIESTROJ, André
    • DEMUTH, Hans-UlrichHEISER, UlrichNIESTROJ, André
    • C07K5/00
    • C07K5/06
    • The present invention relates to new compounds that act as specific inhibitors of the cysteine protease dipeptidyl peptidase I (OP I). Those compounds are represented by the general formula (I) and the pharmaceutical salts thereof, in which R is an acyl-residue including urethane and, peptide, or a branched or unbranched C 1 -C 9 alkyl chain, a branched or unbranched C 2 -C 9 alkenyl chain, a branched or unbranched C 2 -C 9 alkynyl chain, a C 3 -C 9 cycloalkyl, C 4 -C 9 carbocyclic, C 5 -C 14 aryl, C 3 -C 9 heteroaryl, C 3 -C 9 heterocyclic, all of the above residues may be optionally substituted, or is H, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R' is a branched or unbranched C 1 -C 9 alkyl chain, a branched or unbranched C 2 -C 9 alkenyl chain, a branched or unbranched C 2 -C 9 alkynyl chain, a C 3 -C 9 cycloalkyl, C 4 -C 9 cycloalkenyl, C 2 -C 9 heterocycloalkyl, C 3 -C 9 heterocycloalkenyl, C 5 - C 14 aryl, C 3 -C 9 heteroaryl, C 3 -C 9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues my be optionally substituted, or is H.
    • 本发明涉及作为半胱氨酸蛋白酶二肽基肽酶I(OP I)的特异性抑制剂的新化合物。 那些化合物由通式(I)及其药用盐表示,其中R是包括氨基甲酸酯和肽,或支链或非支链C 1 -C 9烷基链的酰基残基,支链或非支链C 2 -C 9链烯基 链,支链或非支链C 2 -C 9炔基链,C 3 -C 9环烷基,C 4 -C 9碳环,C 5 -C 14芳基,C 3 -C 9杂芳基,C 3 -C 9杂环,所有上述残基均可任选被取代,或 H,AS是氨基酸或其模拟肽。 氨基酸是与R结合的肽,R'是支链或非支链C1-C9烷基链,支链或非支链C2-C9烯基链,支链或非支链C2-C9炔基链,C3-C9环烷基,C4- C 9环烯基,C 2 -C 9杂环烷基,C 3 -C 9杂环烯基,C 5 -C 14芳基,C 3 -C 9杂芳基,C 3 -C 9杂环基,而杂环烷基,杂环烯基,杂芳基,杂环残基可以具有多达6个杂环原子,氨基酸 或其肽模拟物,所有上述残基均可任意取代,或为H.