首页> 外国专利> Truncated analogs of a glucose-dependent insulinotropic polypeptide

Truncated analogs of a glucose-dependent insulinotropic polypeptide

机译:葡萄糖依赖性促胰岛素多肽的截短类似物

摘要

A compound of formula (I), ** Formula ** in which: A1 is deleted; A2 is Ala, 4Hppa, or is deleted; A3 is Glu, 4Hyp, Pro, or is deleted; A4 is Gly, or is deleted; A5 is Thr, or is deleted; A6 is Phe, or is deleted; A7 is A5c or A6c; A8 is Ser or Chc-Ser; A9 is Asp; A10 is Tyr; A11 is Ser, A6c or Aib; A12 is Ile; A13 is Ala or Aib; A14 is Met, A6c, or Nle; A15 is Asp; A16 is Lys; A17 is Ile; A18 is His; A19 is Gln; A20 is Gln; A21 is Asp; A22 is Phe; A23 is Val; A24 is Asn; A21 is Trp; A26 is Leu; A27 is Leu; A28 is Ala; A29 is Gln; A30 is Lys; A31 is Gly, Cys (Hsu), Cys (Psu), 2Nal, D-2Nal, Orn (NC (O) - (CH2) 4-CH3), Orn (NC (O) - (CH2) 8-CH3), Orn (NC (O) - (CH2) 12-CH3), or is deleted; A32 is Lys, Cys (Psu), or is deleted; A33 is Lys, Cys (Psu), or is deleted; A34 is Asn, Cys (Psu), Orn (N-C (O) - (CH2) 8-CH3), or is deleted; A35 is Asp, Cys (Psu), or is deleted; A36 is Trp, Cys (Psu), or is deleted; A37 is Lys, Cys (Psu), or is deleted; A38 is His, Cys (Psu), or is deleted; A39 is Asn, Cys (Psu), or is deleted; A40 is Ile, Cys (Psu), or is deleted; A41 is Thr, or is deleted; A42 is Gln, or is deleted; A43 is Gln, or is deleted; R1 is OH or NH2; each of R2 and R3 is independently selected from the group consisting of H or acyl (C1-C30); with the proviso that when R2 is acyl (C1-C30), then R3 is H; and with the proviso that when A2 is 4Hppa, then R2 and R3 are deleted; and with the proviso that at least one of A2, A3, A4, A5, A6, A8, A9, A11, A13, A14, A31, A32, A33, A34, A35, A36, A37, A38, A39 and A40 do not it is the amino acid residue of the corresponding position of the native GIP; or its pharmaceutically acceptable salt.
机译:式(I)的化合物,式**,其中:A1被删除; A2是Ala,4Hppa或被删除; A3是Glu,4Hyp,Pro或已删除; A4是Gly,或被删除; A5是Thr,或被删除; A6是Phe,或被删除; A7是A5c或A6c; A8是Ser或Chc-Ser; A9是Asp; A10是Tyr; A11是Ser,A6c或Aib; A12是Ile; A13是Ala或Aib; A14是Met,A6c或Nle; A15是Asp; A16是赖氨酸; A17是Ile; A18是他的; A19是Gln; A20是Gln; A21是Asp; A22是Phe; A23为Val; A24是Asn; A21是色氨酸; A26是Leu; A27是Leu; A28是Ala; A29是Gln; A30是赖氨酸; A31是Gly,Cys(Hsu),Cys(Psu),2Nal,D-2Nal,Orn(NC(O)-(CH2)4-CH3),Orn(NC(O)-(CH2)8-CH3), Orn(NC(O)-(CH2)12-CH3),或被删除; A32是Lys,Cys(Psu)或被删除; A33是Lys,Cys(Psu)或已删除; A34是Asn,Cys(Psu),Orn(N-C(O)-(CH2)8-CH3),或被删除; A35是Asp,Cys(Psu)或被删除; A36是Trp,Cys(Psu)或被删除; A37是Lys,Cys(Psu)或已删除; A38是His,Cys(Psu),或被删除; A39是Asn,Cys(Psu)或被删除; A40是Ile,Cys(Psu)或被删除; A41是Thr,或被删除; A42是Gln,或被删除; A43是Gln,或被删除; R1是OH或NH2; R2和R3各自独立地选自H或酰基(C1-C30);条件是当R2为酰基(C1-C30)时,R3为H;前提是当A2为4Hppa时,R2和R3被删除;并且附带条件是A2,A3,A4,A5,A6,A8,A9,A11,A13,A14,A31,A32,A33,A34,A35,A36,A37,A38,A39和A40中的至少一个不它是天然GIP相应位置的氨基酸残基;或其药学上可接受的盐。

著录项

  • 公开/公告号ES2528599T3

    专利类型

  • 公开/公告日2015-02-10

    原文格式PDF

  • 申请/专利权人 IPSEN PHARMA S.A.S.;

    申请/专利号ES20090805288T

  • 发明设计人 DONG ZHENG;SHEN YEELANA;DEOLIVEIRA DANIEL;

    申请日2009-08-07

  • 分类号A61K38;

  • 国家 ES

  • 入库时间 2022-08-21 15:12:04

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