Synthetic natriuretic peptides
    5.
    发明公开
    Synthetic natriuretic peptides 失效
    合成natriuretische肽。

    公开(公告)号:EP0246795A2

    公开(公告)日:1987-11-25

    申请号:EP87304163.6

    申请日:1987-05-11

    IPC分类号: C07K7/10 A61K37/24

    CPC分类号: C07K14/582 A61K38/00

    摘要: Synthetic natriuretic peptides (SNP) composed of 23 amino acid residues of which residues 2 - 23 have the natural L-configuration while the amino-terminal residue is derived from an unnatural amino acid having the D-configuration. The compounds possess diurectic, natriuretic, vasorelaxant, smooth muscle relaxant, hypotensive, and anti-­hypertensive activites, and a process for their preparation is also disclosed, together with pharmaceutical preparations thereof and with their use in the practice of medicine. Salts of said synthetic natriuretic peptides with pharmaceutically acceptable acids are also disclosed.

    摘要翻译: 由23个氨基酸残基组成的合成利钠肽(SNP),其中残基2-23具有天然的L-构型,而氨基末端残基源自具有D-构型的非天然氨基酸。 该化合物具有利尿,利尿钠,血管舒张剂,平滑肌松弛剂,降血压和抗高血压活性,并且还公开了其制备方法及其药物制剂及其在药物实践中的用途。 还公开了所述合成利钠肽与药学上可接受的酸的盐。

    Derivatives of alpha-hANP and their production
    8.
    发明公开
    Derivatives of alpha-hANP and their production 失效
    ALPHA-HANP及其生产的衍生物

    公开(公告)号:EP0269220A3

    公开(公告)日:1990-05-23

    申请号:EP87308586.4

    申请日:1987-09-29

    IPC分类号: C07K7/10 C07K1/00

    摘要: A peptide derivative of the formula
    wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the α-position; B is F-Gly wherein F is a neutral a-amino acid residue, or NH-(CH 2 )nCO wherein n is an integer of 1 to 4; C is a neutral a-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or lie, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.

    Atrial peptide derivatives
    9.
    发明公开
    Atrial peptide derivatives 失效
    阿特丽亚派克派克。

    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

    IPC分类号: C07K7/08 A61K37/02

    CPC分类号: C07K14/582 A61K38/00

    摘要: 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.

    摘要翻译: 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。

    Derivatives of alpha-hANP and their production
    10.
    发明公开
    Derivatives of alpha-hANP and their production 失效
    衍生的阿尔法ANP和我的Herstellung。

    公开(公告)号:EP0269220A2

    公开(公告)日:1988-06-01

    申请号:EP87308586.4

    申请日:1987-09-29

    IPC分类号: C07K7/10 C07K1/00

    摘要: A peptide derivative of the formula
    wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the α-position; B is F-Gly wherein F is a neutral a-amino acid residue, or NH-(CH 2 )nCO wherein n is an integer of 1 to 4; C is a neutral a-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or lie, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.

    摘要翻译: 式CHEM的肽衍生物,其中A是氢或被α位上的氨基取代的具有2至18个碳原子的烃酰基; B是F-Gly,其中F是中性α-氨基酸残基或NH-(CH 2)n CO,其中n是1至4的整数; C是中性α-氨基酸残基; E为L-Arg或D-Arg; 当A,B和C分别为氢,Gly-Gly和Met或Ile时,E为D-Arg,或其药理学上可接受的盐具有强烈的降血压和钠尿活性; 因此作为心血管和脑循环系统疾病的高血压,利尿剂,治疗药物的治疗药物是有用的。