公开(公告)号：EP0341603A3

公开(公告)日：1990-07-04

申请号：EP89108140.8

申请日：1989-05-05

Applicant: ABBOTT LABORATORIES

Inventor： Rockway, Todd W. ,  Kiso, Yoshiaki ,  Davidsen, Steven K. ,  Lucas, Scott D. ,  Thomas, A. Mitchell ,  Von Geldern, Thomas W.

IPC: C07K7/08 ,  A61K37/02

CPC classification number: C07K14/582 ,  A61K38/00

Abstract: Atrial peptides comprising the amino acid sequence as follows: wherein R₁ is hydrogen, Ser, Cit, SerSer, Arg, Carbamoyl Ser, Guanido-Ser-Ser, Amcca, Guanido-Amcca, Lys, ArgArg, Ser-Arg, Ser-Lys, Acetyl-Ser-Ser, D-Ser-Ser, Ser-D-Ser, Guanido-Aocta, Aunda, Aocta, Ahexa, HSer, Apenta, Papaa, Abuta, Mamba, Orn, D-Orn or Acetyl-apenta, Acetyl-Ahexa, Guanido;
R₂ is Cys, D-Cys or Pen;
R₃ is L-Phe, D-Ala, L-Ala, D-Val, D-Cha, Sar, D-Phg, Aib, β-Ala or Gly;
R₄ is Phe, Trp, D-Tic, L-Tic, N-MePhe, D-Ala, Tyr, 2-Thi, DimeDOPA or DOPA;
R₅ is Gly-Gly, Ala-Gly, D-Ala-Gly, Gly-Ala, Amcca, Mapaa or Papaa;
R₆ is Arg, D-Arg or Cit;
R₇ is Ile, Leu, D-Leu or Met;
R₈ is Asp, Asn, β-methylAsp, cycloAsp, Gly or Ser;
R₉ is Arg, D-Arg or Ala;
R₁₀ is Ile, Leu or Phe;
R₁₁ is Cys, D-Cys, HCys, Cys-4-thiomethylproline, or trans-4-thiomethylproline;
R₁₂ is absent, Phe, D-Ala-Phe, D-Phe, Cha, Pro, D-Pro, 2-Thi, Aic, D-Tic, trans-4-FPro, L-Tic, Leu, Ile or β-NAl;
R₁₃ is OH, Arg, Arg-NH₂, D-Arg, Gln, Lys, HomoArg, or Gly; or pharmaceutically acceptable salts, esters or amides thereof.

Abstract translation: 包含如下氨基酸序列的心房肽：其中R1是氢，Ser，Cit，SerSer，Arg，氨基甲酰基Ser，Guanido-Ser-Ser，Amcca，Guanido-Amcca，Lys，ArgArg，Ser-Arg，Ser -Lys，乙酰基Ser-Ser，D-Ser-Ser，Ser-D-Ser，Guanido-Aocta，Aunda，Aocta，Ahexa，HSer，Apenta，Papaa，Abuta，Mamba，Orn，D-Orn或乙酰 - ，乙酰基 - 六甲胺，胍基; R2是Cys，D-Cys或Pen; R3是L-Phe，D-Ala，L-Ala，D-Val，D-Cha，Sar，D-Phg，Aib，β-Ala或Gly; R4是Phe，Trp，D-Tic，L-Tic，N-MePhe，D-Ala，Tyr，2-Thi，DimeDOPA或DOPA; R5是Gly-Gly，Ala-Gly，D-Ala-Gly，Gly-Ala，Amcca，Mapaa或Papaa; R6是Arg，D-Arg或Cit; R7是Ile，Leu，D-Leu或Met; R8是Asp，Asn，β-methylAsp，cycloAsp，Gly或Ser; R9是Arg，D-Arg或Ala; R10是Ile，Leu或Phe; R11是Cys，D-Cys，HCys，Cys-4-硫代甲基脯氨酸或反式-4-硫代甲基脯氨酸; R12不存在，Phe，D-Ala-Phe，D-Phe，Cha，Pro，D-Pro，2-Thi，Aic，D-Tic，反式-4-FPro，L-Tic，Leu，Ile或β- NAL; R13是OH，Arg，Arg-NH2，D-Arg，Gln，Lys，HomoArg或Gly; 或其药学上可接受的盐，酯或酰胺。

公开(公告)号：EP0341603A2

公开(公告)日：1989-11-15

申请号：EP89108140.8

申请日：1989-05-05

Applicant: ABBOTT LABORATORIES

Inventor： Rockway, Todd W. ,  Kiso, Yoshiaki ,  Davidsen, Steven K. ,  Lucas, Scott D. ,  Thomas, A. Mitchell ,  Von Geldern, Thomas W.

IPC: C07K7/08 ,  A61K37/02

CPC classification number: C07K14/582 ,  A61K38/00

Abstract: Atrial peptides comprising the amino acid sequence as follows: wherein R₁ is hydrogen, Ser, Cit, SerSer, Arg, Carbamoyl Ser, Guanido-Ser-Ser, Amcca, Guanido-Amcca, Lys, ArgArg, Ser-Arg, Ser-Lys, Acetyl-Ser-Ser, D-Ser-Ser, Ser-D-Ser, Guanido-Aocta, Aunda, Aocta, Ahexa, HSer, Apenta, Papaa, Abuta, Mamba, Orn, D-Orn or Acetyl-apenta, Acetyl-Ahexa, Guanido;
R₂ is Cys, D-Cys or Pen;
R₃ is L-Phe, D-Ala, L-Ala, D-Val, D-Cha, Sar, D-Phg, Aib, β-Ala or Gly;
R₄ is Phe, Trp, D-Tic, L-Tic, N-MePhe, D-Ala, Tyr, 2-Thi, DimeDOPA or DOPA;
R₅ is Gly-Gly, Ala-Gly, D-Ala-Gly, Gly-Ala, Amcca, Mapaa or Papaa;
R₆ is Arg, D-Arg or Cit;
R₇ is Ile, Leu, D-Leu or Met;
R₈ is Asp, Asn, β-methylAsp, cycloAsp, Gly or Ser;
R₉ is Arg, D-Arg or Ala;
R₁₀ is Ile, Leu or Phe;
R₁₁ is Cys, D-Cys, HCys, Cys-4-thiomethylproline, or trans-4-thiomethylproline;
R₁₂ is absent, Phe, D-Ala-Phe, D-Phe, Cha, Pro, D-Pro, 2-Thi, Aic, D-Tic, trans-4-FPro, L-Tic, Leu, Ile or β-NAl;
R₁₃ is OH, Arg, Arg-NH₂, D-Arg, Gln, Lys, HomoArg, or Gly; or pharmaceutically acceptable salts, esters or amides thereof.

Abstract translation: 包含如下氨基酸序列的心房肽：其中R1是氢，Ser，Cit，SerSer，Arg，氨基甲酰基Ser，Guanido-Ser-Ser，Amcca，Guanido-Amcca，Lys，ArgArg，Ser-Arg，Ser -Lys，乙酰基Ser-Ser，D-Ser-Ser，Ser-D-Ser，Guanido-Aocta，Aunda，Aocta，Ahexa，HSer，Apenta，Papaa，Abuta，Mamba，Orn，D-Orn或乙酰 - ，乙酰基 - 六甲胺，胍基; R2是Cys，D-Cys或Pen; R3是L-Phe，D-Ala，L-Ala，D-Val，D-Cha，Sar，D-Phg，Aib，β-Ala或Gly; R4是Phe，Trp，D-Tic，L-Tic，N-MePhe，D-Ala，Tyr，2-Thi，DimeDOPA或DOPA; R5是Gly-Gly，Ala-Gly，D-Ala-Gly，Gly-Ala，Amcca，Mapaa或Papaa; R6是Arg，D-Arg或Cit; R7是Ile，Leu，D-Leu或Met; R8是Asp，Asn，β-methylAsp，cycloAsp，Gly或Ser; R9是Arg，D-Arg或Ala; R10是Ile，Leu或Phe; R11是Cys，D-Cys，HCys，Cys-4-硫代甲基脯氨酸或反式-4-硫代甲基脯氨酸; R12不存在，Phe，D-Ala-Phe，D-Phe，Cha，Pro，D-Pro，2-Thi，Aic，D-Tic，反式-4-FPro，L-Tic，Leu，Ile或β- NAL; R13是OH，Arg，Arg-NH2，D-Arg，Gln，Lys，HomoArg或Gly; 或其药学上可接受的盐，酯或酰胺。