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147 条记录 (耗时 0.029 秒)

    Pharmaceutical peptides, preparation, use and intermediates
    5.
    发明授权
    Pharmaceutical peptides, preparation, use and intermediates 失效
    药物肽，制剂，用途和中间体

    公开(公告)号：US4540682A

    公开(公告)日：1985-09-10

    申请号：US613868

    申请日：1984-05-23

    申请人： George W. Hardy ,  Lawrence A. Lowe ,  Terence W. Smith

    发明人： George W. Hardy ,  Lawrence A. Lowe ,  Terence W. Smith

    IPC分类号： C07K5/08 ,  A61K38/00 ,  A61P1/12 ,  A61P9/06 ,  A61P9/12 ,  A61P11/14 ,  A61P25/04 ,  A61P25/30 ,  C07K1/113 ,  C07K5/065 ,  C07K5/087 ,  C07K5/10 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/0812 ,  C07K5/06078 ,  Y10S514/809

    摘要： Novel peptides of formula (I) ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1 or 2 carbon atoms or an amidino group,R.sup.2 is alkyl of 1 or 2 carbon atoms,R.sup.3 is hydrogen or carbamyl,X.sup.2 is a D-radical having the structure: ##STR2## Z.sup.1 and Z.sup.2 are the same or different and each is hydrogen, halo, nitro or trifluoromethyl and at least one is other than hydrogen,m is 2, 3 or 4 andn is 0, 1 or 2,provided that when R.sup.3 is carbamyl then n is always 1;and salts thereof.The compounds have a selectively peripheral analgesic effect when administered to mammals and also exhibit antidiarrhoeal and antitussive activity and may thus be used in human or veterinary medicine for the relief or prevention of pain, for the treatment of diarrhoea or dysentery and for the suppression of cough.

    摘要翻译： 式（I）的新肽其中R1是氢，1或2个碳原子的烷基或脒基，R2是1或2个碳原子的烷基，R3是氢或氨基甲酰基，X2是D 具有以下结构的化合物：＆lt; IMAGE＆gt; Z1和Z2相同或不同，各自为氢，卤素，硝基或三氟甲基，至少一个不是氢，m为2,3或4，n为0,1或 2，条件是当R 3为氨甲酰基时，则n总是为1; 及其盐。 当给予哺乳动物时，这些化合物具有选择性的外周止痛作用，并且还具有抗腹泻和镇咳作用，因此可用于人或兽医学用于缓解或预防疼痛，用于治疗腹泻或痢疾以及抑制咳嗽 。

    Conformationally constrained cyclic enkephalin analogs with delta receptor specificity
    6.
    发明授权
    Conformationally constrained cyclic enkephalin analogs with delta receptor specificity 失效
    具有δ受体特异性的构象约束环状脑啡肽类似物

    公开(公告)号：US4518711A

    公开(公告)日：1985-05-21

    申请号：US494982

    申请日：1983-05-16

    申请人： Victor J. Hruby ,  Henry Mosberg

    发明人： Victor J. Hruby ,  Henry Mosberg

    IPC分类号： C07K14/655 ,  A61K38/00 ,  A61K38/22 ,  A61P25/04 ,  C07K14/575 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/702 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/26

    摘要： Novel compounds which are capable of binding with enhanced specificity to the delta receptor are disclosed. The compounds are a series of cyclic, conformationally constrained analogs of enkephalins which display exceptional delta receptor specificity. The compounds of the present invention are polypeptides of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, methyl, or lower alkyl having 1 to 5 carbon atoms;R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, methyl, or lower alkyl having 1 to 5 carbon atoms, provided, however that R.sup.1, R.sup.2, R.sup.3, and R.sup.4 may not all be hydrogen when both n and m are zero;R.sup.5 is hydrogen, L-tyrosine, D-tyrosine, or L-tyrosine or D-tyrosine substituted on the N.sup..alpha. -amino with 1 or 2 lower alkyl or alkenyl groups;R.sup.6 is a substituted or unsubstituted aromatic;R.sup.7 is hydrogen or methyl;R.sup.8 is carboxylate, carboxamide or amino acid residue;X and Y are hydrogen or methyl; and,n and m, which may be the same or different, are 0 or 1.The novel compounds include those which have either agonist or antagonist activity. The compounds may be used to induce pharmacological or therapeutic effects, including analgesia, in humans and other animals.

    摘要翻译： 公开了能够结合增强的δ受体特异性的新型化合物。 这些化合物是一系列环状，构象约束的脑啡肽类似物，显示异常的δ受体特异性。 本发明的化合物是下式的多肽：其中R 1和R 2可以相同或不同，为氢，甲基或具有1-5个碳原子的低级烷基; R 3和R 4可以相同或不同，是氢，甲基或具有1至5个碳原子的低级烷基，但是当n和m均为n时，R 1，R 2，R 3和R 4可以不全部为氢。 零; R5是在具有1或2个低级烷基或烯基的Nα-氨基上取代的氢，L-酪氨酸，D-酪氨酸或L-酪氨酸或D-酪氨酸; R6是取代或未取代的芳族; R7是氢或甲基; R8是羧酸酯，羧酰胺或氨基酸残基; X和Y是氢或甲基; 和n和m可以相同或不同，为0或1.新化合物包括具有激动剂或拮抗剂活性的那些化合物。 该化合物可用于在人和其他动物中诱导药理或治疗作用，包括止痛。

    Aminoacyl derivatives
    8.
    发明授权
    Aminoacyl derivatives 失效
    氨基酰基衍生物

    公开(公告)号：US4421744A

    公开(公告)日：1983-12-20

    申请号：US379614

    申请日：1982-05-18

    申请人： James J. Gormley

    发明人： James J. Gormley

    IPC分类号： G01N33/52 ,  A61K38/00 ,  A61P25/00 ,  A61P25/20 ,  A61P43/00 ,  C07K5/02 ,  C07K5/04 ,  C07K5/065 ,  C07K5/087 ,  C07K5/107 ,  C07K7/06 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/70 ,  C07K5/0207 ,  C07K5/0212 ,  C07K5/06078 ,  C07K5/0812 ,  C07K5/1016 ,  A61K38/00 ,  Y10S514/809

    摘要： Peptide and pseudopeptide derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 stand for defined hydrocarbyl or halo-hydrocarbyl substituents, for example alk-2-enyl radicals; .dbd.N--A-- stands for a defined amino acid residue; B, D and E, which may be the same or different, stand for a valency bond or a defined amino acid residue; F stands for a defined amino acid residue; X stands for a carboxy, ester or amide group; and the linkages between the amino acid residues are peptide linkages or at least one of said linkages is a defined pseudo linkage; and pharmaceutically-acceptable salts thereof. Processes for the manufacture of the compounds. Pharmaceutical compositions comprising one of the compounds and a pharmaceutical diluent or carrier. The compounds are antagonists at the opiate receptors, and most of them are selective .delta.-receptor antagonists.

    摘要翻译： 下式的肽和假肽衍生物：其中R 1和R 2代表定义的烃基或卤代烃基取代基，例如烷-2-烯基; = N-A-代表定义的氨基酸残基; B，D和E可以相同或不同，代表价键或限定的氨基酸残基; F代表定义的氨基酸残基; X代表羧基，酯或酰胺基; 氨基酸残基之间的连接是肽键，或至少一个所述键是定义的假键; 及其药学上可接受的盐。 用于制造化合物的方法。 包含化合物之一和药物稀释剂或载体的药物组合物。 这些化合物是阿片受体的拮抗剂，其中大多数是选择性的δ-受体拮抗剂。

    Novel pentapeptides, processes for their production, pharmaceutical compositions comprising said pentapeptides and their use
    9.
    发明授权
    Novel pentapeptides, processes for their production, pharmaceutical compositions comprising said pentapeptides and their use 失效
    新型五肽，其制备方法，包含所述五肽的药物组合物及其用途

    公开(公告)号：US4405607A

    公开(公告)日：1983-09-20

    申请号：US282045

    申请日：1981-07-10

    申请人： Francois Cardinaux ,  Rene Huguenin ,  Janos Pless

    发明人： Francois Cardinaux ,  Rene Huguenin ,  Janos Pless

    IPC分类号： A61K38/00 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/702 ,  A61K38/00 ,  Y10S514/809

    摘要： Pentapeptides of formula I, ##STR1## wherein Z.sup.1 =H, CH.sub.3 or amidino; R.sub.1 =H or alkyl and R.sub.2 =H or R.sub.1 +R.sub.2 =--CH.sub.2 --CH.sub.2 --; R.sub.3 =m- or p--OH or -alkoxy; B=residue of a (D)-.alpha.-amino acid; R.sub.4 =H or alkyl; Z.sup.2 =optionally substituted phenyl; and E=.beta.-amino alcohol residue (whereby when Z.sup.1 =H or CH.sub.3, R.sub.4 =C.sub.3-4 -alkyl) as well as their esters and the acid addition salts and complexes of such peptides and esters. Compounds according to the invention have valuable pharmacological, in particular LH-secretion inhibiting activity.

    摘要翻译： 式I的五肽，其中Z1 = H，CH3或脒基; R1 = H或烷基，R2 = H或R1 + R2 = -CH2-CH2-; R3 = m-或对 - OH或 - 烷氧基; B =（D）-α-氨基酸的残基; R4 = H或烷基; Z2 =任选取代的苯基; 和E =β-氨基醇残基（当Z1 = H或CH3，R4 = C3-4-烷基时），以及它们的酯和这些肽和酯的酸加成盐和配合物。 根据本发明的化合物具有有价值的药理学，特别是LH-分泌抑制活性。