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Glucose-dependent insulinotropic polypeptide analogs

机译:葡萄糖依赖性促胰岛素多肽类似物

摘要

A compound of formula (I), ** Formula ** wherein: A4 is Gly; A5 is Thr; A6 is Phe; A7 is Ile or A6c; A8 is Being; A9 is Asp; A10 is Tyr; A11 is A5c or A6c; A12 is Ile; A13 is Ala or Aib; A14 is Met, A5c, 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; A25 is Trp; A26 is Leu; A27 is Leu; A28 is Ala; A29 is Gln; A30 is Lys; A31 is Gly, His, Orn (N-C (O) - (CH2) 12-CH3) or is deleted; A32 is Lys, Cys, Cys (succinimide-N- (CH2) 11-CH3), Cys (succinimide-N- (CH2) 15-CH3), Orn (NC (O) - (CH2) 10-CH3) or Orn (NC (O) - (CH2) 14-CH3) or is deleted; A33 is Lys, Cys, Cys (succinimide-N- (CH2) 11-CH3), Cys (succinimide-N- (CH2) 15-CH3), Orn (NC (O) - (CH2) 10-CH3) or Orn (NC (O) - (CH2) 14-CH3) or is deleted; A34 is Asn or is deleted; A35 is Asp, Orn (N-C (O) - (CH2) 12-CH3) or is deleted; A36 is Trp or is deleted; A37 is Lys or is deleted; A38 is His or is deleted; A39 is Asn or is deleted; A40 is Ile, A5c, A6c or is deleted; A41 is Thr, A5c, A6c or is deleted; A42 is Gln, Cys (Psu) or is deleted; A43 is Ado, Ala, Asn, Asp, Cys, Cys (succinimide-N- (CH2) 11- (CH3), Cys (succinimide-N- (CH2) 15-CH3), His, Lys (NC (O) - (CH2) 10-CH3), Lys (NC (O) - (CH2) 14-CH3), Orn (NC (O) - (CH2) 14-CH3), Phe, Thr, Trp or is deleted; R1 is OH , NH2, (C1-C30) alkoxy or NH-X2-CH2-Z0, where X2 is a hydrocarbon residue (C0-C30) and Z0 is H, OH, CO2H or CONH2, each of R2 and R3 is H; provided that at least one of A7, A11, A13, A14, A31, A35, A40, A41 and A42 is not the amino acid residue of the corresponding position of natural GIP, or a pharmaceutically acceptable salt thereof.
机译:式(I)的化合物,式**,其中:A4为Gly; A5是苏氨酸; A6是Phe; A7是Ile或A6c; A8是存在; A9是Asp; A10是Tyr; A11是A5c或A6c; A12是Ile; A13是Ala或Aib; A14是Met,A5c,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; A25是色氨酸; A26是Leu; A27是Leu; A28是Ala; A29是Gln; A30是赖氨酸; A31是Gly,His,Orn(N-C(O)-(CH2)12-CH3)或已删除; A32是Lys,Cys,Cys(琥珀酰亚胺-N-(CH2)11-CH3),Cys(琥珀酰亚胺-N-(CH2)15-CH3),Orn(NC(O)-(CH2)10-CH3)或Orn (NC(O)-(CH2)14-CH3)或被删除; A33是Lys,Cys,Cys(琥珀酰亚胺-N-(CH2)11-CH3),Cys(琥珀酰亚胺-N-(CH2)15-CH3),Orn(NC(O)-(CH2)10-CH3)或Orn (NC(O)-(CH2)14-CH3)或被删除; A34是Asn或已删除; A35是Asp,Orn(N-C(O)-(CH2)12-CH3)或已删除; A36是Trp或被删除; A37是Lys或被删除; A38是他的或被删除; A39是Asn或被删除; A40是Ile,A5c,A6c或已删除; A41是Thr,A5c,A6c或已删除; A42是Gln,Cys(Psu)或已删除; A43是Ado,Ala,Asn,Asp,Cys,Cys(琥珀酰亚胺-N-(CH2)11-(CH3),Cys(琥珀酰亚胺-N-(CH2)15-CH3),His,Lys(NC(O)- (CH2)10-CH3),Lys(NC(O)-(CH2)14-CH3),Orn(NC(O)-(CH2)14-CH3),Phe,Thr,Trp或被删除; R1为OH ,NH2,(C1-C30)烷氧基或NH-X2-CH2-Z0,其中X2为烃基残基(C0-C30),Z0为H,OH,CO2H或CONH2,R2和R3均为H; A7,A11,A13,A14,A31,A35,A40,A41和A42中的至少一个不是天然GIP的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ES2574835T3

    专利类型

  • 公开/公告日2016-06-22

    原文格式PDF

  • 申请/专利权人 IPSEN PHARMA S.A.S.;

    申请/专利号ES20090805291T

  • 发明设计人 DONG ZHENG XIN;

    申请日2009-08-07

  • 分类号A61K38;

  • 国家 ES

  • 入库时间 2022-08-21 14:22:08

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