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    Somatostatin analogues
    3.
    发明公开
    Somatostatin analogues 失效
    生长抑素类似物

    公开(公告)号：EP0363589A3

    公开(公告)日：1990-08-16

    申请号：EP89114365.3

    申请日：1989-08-03

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Nestor, John J. ,  Vickery, Brian H.

    IPC分类号： C07K7/26 ,  C07K1/00 ,  A61K37/43

    CPC分类号： C07K14/6555 ,  A61K38/00

    摘要： Pharmaceutical compounds having somatostatin-like activity which compounds comprise a peptide analog of somatostatin linked to a cationic anchor.

    摘要翻译： 具有生长激素抑制素样活性的药物化合物，所述化合物包含与阳离子锚连接的促生长素抑制素的肽类似物。

    N,N-dialkylguanidino dipeptides
    5.
    发明公开
    N,N-dialkylguanidino dipeptides 失效
    N，N-二烷基胍二肽

    公开(公告)号：EP0196841A1

    公开(公告)日：1986-10-08

    申请号：EP86302111.9

    申请日：1986-03-21

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Nestor, John J.

    IPC分类号： C07K5/06 ,  A61K37/02

    CPC分类号： C07K5/0222 ,  A61K38/00

    摘要： N G ,N G '-dialkylguanidino dipeptides with angiotension converting enzyme inhibiting activity are useful as antihypertensives. Proline and proline analogs are components of the dipeptides.

    摘要翻译： NG，具有血管紧张素转换酶抑制活性的NG'-二烷基胍二肽可用作抗高血压药。 脯氨酸和脯氨酸类似物是二肽的组分。

    Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists, their preparation and compositions containing them
    7.
    发明公开
    Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists, their preparation and compositions containing them 失效
    LHRH作为LHRH拮抗剂的非受体和非糖蛋白类似物，其制备和组合物

    公开(公告)号：EP0097031A3

    公开(公告)日：1984-11-07

    申请号：EP83303343

    申请日：1983-06-09

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Nestor, John J. ,  Vickery, Brian H.

    IPC分类号： C07C103/52 ,  A61K37/02

    CPC分类号： C07K7/23 ,  A61K38/00

    摘要： Nonapeptide and decapeptide analogs of LHRH which have the formula
    and the pharmaceutically acceptable salts thereof, wherein: A is an amino acyl residue selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, N-acyl-D,L-tryptophanyl, N-acyl-glycyl, N-Ac-D,L-Δ 3,4 -prolyl, N-Ac-D,L-prolyl, N-Ac-L-alkylprolyl, N-Ac-D,L-phenylalanyl, N-Ac-D,L-p-chlorophenylalanyl, N-Ac-D,L-seryl, N-Ac-D,L-threonyl, N-Ac-D,L-alanyl, 3-(1-naphthyl)-D,L-alanyl, 3-(2-naphthyl)-D,L-alanyl, 3-(2,4,6-trimethylphenyl)-D,L-alanyl, 3-(4-trifluoromethylphenyl)-D,L-alanyl, 3-(9-anthryl)-D,L-alanyl, 3-(2-fluorenyl)-D,L-alanyl, and 3-(Het)-D,L-alanyl wherein Het is a heterocyclic aryl containing radical selected from
    wherein A" and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine and bromine, and G is selected from the group consisting of oxygen, nitrogen and sulfur; B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-Cl-phenylalanyl, D-p-F-phenylalanyl, D-p-nitrophenylalanyl, 3-(3,4,5-trimethoxyphenyl)-D-alanyl, 2,2-diphenylglycine, D-a-methyl-p-Cl-phenylalanine and 3-(2,4,6-trimethylphenyl)-D-alanyl; C is an amino acyl residue selected from the group consisting of L-tryptophanyl, D-tryptophanyl, D-phenylalanyl, D-Me s phenylalanyl, 3-(2-pyridyl)-D-alanyl, 3-(3-pyridyl)D-alanyl, 3-(1-naphthyl)-D-alanyl, 3-(2-naphthyl)-D-alanyl and 3-(4-pyridyl)-D-alanyl. D is an amino acyl residue selected from the group consisting of L-seryl, and D-alanyl; E is an amino acyl residue selected from the group consisting of L-phenylalanyl and L-tyrosyl; F is an amino acyl selected from the group consisting of the radicals represented by the following structural formulas: wherein
    n is 1 to 5 ; R, is alkyl of 1 to 12 carbon atoms, -NRR 3 wherein R is hydrogen or alkyl of 1 to 4 carbon atoms, R 3 is alkyl of 1 to 12 carbon atoms, cycloalkyl, phenyl, benzyl, -(CH 2 ) n -morpholino or -(CH 2 ) n N(R 4 ) 2 wherein n is 1 to 5 and R 4 is lower alkyl; R 2 is hydrogen or R 3 ; or R, and R 2 comprise a ring represented by the following structural formulas:
    wherein n is 1 to 7; A is hydrogen, alkyl of 1 to 6 carbon atoms or cycloalkyl; and X is halo or A or b) H 2 N-CH-CO 2 H
    wherein R 5 is alkyl of 1 to 6 carbon atoms, benzyl, phenylethyl, cyclohexyl, cyclopentyl; and R 6 , R 7 and R 8 are hydrogen or alkyl of 1 to 4 carbon atoms; and n is the integer 2-5; or C) a substituent of the formula
    wherein R 9 is hydrogen, alkyl of 1 to 12 carbon atoms, phenyl or phenylloweralkyl; G is an amino acyl residue selected from the group consisting of L-leucyl, L-norleucyl and L-norvatyl; H is D-alaninamide, D-leucinamide, glycinamide or -NHR 5 wherein R 5 is lower alkyl, cycloalkyl, fluoro lower alkyl, or NHCONH-R 10 wherein R, o is hydrogen or lower alkyl; and the pharmaceutically acceptables salts thereof.

    Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists, their preparation and compositions containing them
    8.
    发明公开
    Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists, their preparation and compositions containing them 失效
    九肽和LHRH的Decapeptidanaloge有效作为LHRH拮抗剂，其制备方法和组合物含有它们。

    公开(公告)号：EP0097031A2

    公开(公告)日：1983-12-28

    申请号：EP83303343.4

    申请日：1983-06-09

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Nestor, John J. ,  Vickery, Brian H.

    IPC分类号： C07K7/06 ,  C07K7/20 ,  A61K37/02

    CPC分类号： C07K7/23 ,  A61K38/00

    摘要： Nonapeptide and decapeptide analogs of LHRH which have the formula
    and the pharmaceutically acceptable salts thereof, wherein:
    A is an amino acyl residue selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, N-acyl-D,L-tryptophanyl, N-acyl-glycyl, N-Ac-D,L-Δ 3,4 -prolyl, N-Ac-D,L-prolyl, N-Ac-L-alkylprolyl, N-Ac-D,L-phenylalanyl, N-Ac-D,L-p-chlorophenylalanyl, N-Ac-D,L-seryl, N-Ac-D,L-threonyl, N-Ac-D,L-alanyl, 3-(1-naphthyl)-D,L-alanyl, 3-(2-naphthyl)-D,L-alanyl, 3-(2,4,6-trimethylphenyl)-D,L-alanyl, 3-(4-trifluoromethylphenyl)-D,L-alanyl, 3-(9-anthryl)-D,L-alanyl, 3-(2-fluorenyl)-D,L-alanyl, and 3-(Het)-D,L-alanyl wherein Het is a heterocyclic aryl containing radical selected from
    wherein A" and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine and bromine, and G is selected from the group consisting of oxygen, nitrogen and sulfur;
    B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-Cl-phenylalanyl, D-p-F-phenylalanyl, D-p-nitrophenylalanyl, 3-(3,4,5-trimethoxyphenyl)-D-alanyl, 2,2-diphenylglycine, D-a-methyl-p-Cl-phenylalanine and 3-(2,4,6-trimethylphenyl)-D-alanyl;
    C is an amino acyl residue selected from the group consisting of L-tryptophanyl, D-tryptophanyl, D-phenylalanyl, D-Me s phenylalanyl, 3-(2-pyridyl)-D-alanyl, 3-(3-pyridyl)D-alanyl, 3-(1-naphthyl)-D-alanyl, 3-(2-naphthyl)-D-alanyl and 3-(4-pyridyl)-D-alanyl.
    D is an amino acyl residue selected from the group consisting of L-seryl, and D-alanyl;
    E is an amino acyl residue selected from the group consisting of L-phenylalanyl and L-tyrosyl;
    F is an amino acyl selected from the group consisting of the radicals represented by the following structural formulas:
    wherein

    n is 1 to 5 ;
    R, is alkyl of 1 to 12 carbon atoms, -NRR 3 wherein R is hydrogen or alkyl of 1 to 4 carbon atoms, R 3 is alkyl of 1 to 12 carbon atoms, cycloalkyl, phenyl, benzyl, -(CH 2 ) n -morpholino or -(CH 2 ) n N(R 4 ) 2 wherein n is 1 to 5 and R 4 is lower alkyl;
    R 2 is hydrogen or R 3 ; or R, and R 2 comprise a ring represented by the following structural formulas:
    wherein n is 1 to 7; A is hydrogen, alkyl of 1 to 6 carbon atoms or cycloalkyl; and X is halo or A or b) H 2 N-CH-CO 2 H
    wherein R 5 is alkyl of 1 to 6 carbon atoms, benzyl, phenylethyl, cyclohexyl, cyclopentyl; and R 6 , R 7 and R 8 are hydrogen or alkyl of 1 to 4 carbon atoms; and n is the integer 2-5; or
    C) a substituent of the formula
    wherein R 9 is hydrogen, alkyl of 1 to 12 carbon atoms, phenyl or phenylloweralkyl;
    G is an amino acyl residue selected from the group consisting of L-leucyl, L-norleucyl and L-norvatyl;
    H is D-alaninamide, D-leucinamide, glycinamide or -NHR 5 wherein R 5 is lower alkyl, cycloalkyl, fluoro lower alkyl, or NHCONH-R 10 wherein R, o is hydrogen or lower alkyl; and the pharmaceutically acceptables salts thereof.

    摘要翻译： 九肽和十肽LHRH的类似物具有下式和其药学上可接受的盐，worin：A是选自L-焦谷的，D-焦谷氨酰基，N-酰基 - D，L-中的氨基酸酰基残基 色氨，N-酰基 - 甘氨酰基，N-AC-D，L- DELTA <3> <，> <4>脯氨酰，N-AC-D，L-脯氨酰基，N-AC-L-alkylprolyl，N-AC -D，L-苯丙氨酰基，N-AC-D，LP-chlorophenylalanyl，N-AC-D，L-丝氨酰，N-AC-D，L-苏，N-AC-D，L-丙氨酰，3-（ 1-萘基）-D，L-丙氨酰，3-（2-萘基）-D，L-丙氨酰，3-（2,4,6-三甲基苯基）-D，L-丙氨酰，3-（4-三氟甲基苯基） -D，L-丙氨酰，3-（9-蒽基）-D，L-丙氨酰，3-（2-芴基）-D，L-丙氨酰和3-（杂）-D，L-丙氨酰worin Het是 杂环芳基仲和A分钟是unabhängig选自氢含由......组成自由基从 worin，低级烷基，氯和溴，和G是选自氧，氮和硫中选择的选择; B为选自D-苯丙，DP-CL-苯丙，DPS-苯丙，DP-硝基苯，3-（3,4,5-三甲氧基苯基）-D-丙氨酰中选出的氨基酰基残基，2,2- diphenylglycine，D-α-甲基 - 对 - 氯 - 苯丙氨酸和3-（2,4,6-三甲基苯基）-D-丙氨酰; C是选自L-色氨，D-色氨，D-苯丙，D-Me5phenylalanyl，3-（2-吡啶基）-D-丙氨酰，3中的氨基酸酰基残基 - （ - 3-吡啶基）D- 丙氨酰基，3-（1-萘基）-D-丙氨酰，3-（2-萘基）-D-丙氨酰和3-（4-吡啶基）-D-丙氨酰。 D为选自L-丝氨酰中选出的氨基酰基残基，和D-丙氨酰; E是选自-L-苯丙和L-酪氨酰中选出的氨基酰基残基; F是选自由以下结构式表示的化学基团中的氨基酸的酰基：