Use of tetrahydrothienopyridine derivatives as angiogenesis inhibitors
    43.
    发明授权
    Use of tetrahydrothienopyridine derivatives as angiogenesis inhibitors 失效
    四氢吡啶衍生物作为血管生成抑制剂的使用

    公开(公告)号:US5225420A

    公开(公告)日:1993-07-06

    申请号:US833765

    申请日:1992-02-11

    CPC分类号: A61K31/44

    摘要: The invention relates to the use of compounds of the formula ##STR1## in which p is 2 and q is 1 or p is q and q is 2; Ar represents an optionally substituted phenyl, and Z represents NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2, which may be identical or different, represent H or optionally substituted alkyl or, with the nitrogen atom, form a saturated heterocycle, or Z represents OR in which R is H or optionally substituted alkyl, or their addition salts, in the form of pure enantiomer or of mixtures thereof, for administration in a human patient for preventing or treating pathologies involving or dependent upon a neovascularization.

    摘要翻译: 本发明涉及式(Ⅰ)化合物,其中p为2且q为1或p为q且q为2的化合物; Ar表示任选取代的苯基,Z表示NR1R2,其中R1和R2可以相同或不同,表示H或任选取代的烷基,或与氮原子形成饱和杂环,或Z表示OR,其中R为 H或任选取代的烷基或其加成盐,以纯对映体或其混合物的形式用于在人类患者中施用以预防或治疗涉及或依赖于新生血管形成的病状。

    Heterocycle-coupled substituted pyrrolo[3,2-c]pyridin-2-carboxylic acids
    45.
    发明授权
    Heterocycle-coupled substituted pyrrolo[3,2-c]pyridin-2-carboxylic acids 失效
    杂环偶联取代的吡咯并[3,2-c]吡啶-2-羧酸

    公开(公告)号:US5468750A

    公开(公告)日:1995-11-21

    申请号:US273943

    申请日:1994-07-12

    摘要: A compound of formula ##STR1## in which A represents S;R.sub.1 is selected from the group consisting of OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, phenyl, benzyl (C.sub.1 -C.sub.4)alkyl NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 ;R.sub.2 is selected from the group consisting of OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, and NZ.sub.1 Z.sub.2 ;R.sub.3 is selected from the group consisting of H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl, and benzyl;B is selected from the group consisting of phenyl; pyridyl; phenyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl or --NZ.sub.1 Z.sub.2 is selected from the group consisting of pyrrolidinyl, piperidinyl, morpholino, hexahydroazepino, ##STR2## piperazino, piperazino substituted in position 4 by (C.sub.1 -C.sub.8)alkyl, benzyl or diphenylmethyl; and pyridyl substituted by one or more groups selected from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2, and NZ.sub.1 Z.sub.2 wherein Z.sub.1 and Z.sub.2 are selected, independently of each other, from the group consisting of H, (C.sub.1 -C.sub.6)alkyl, formyl, and benzyl, or NZ.sub.1 Z.sub.2 is selected from the group consisting of pyrrolidinyl, piperidinyl, morpholino, hyxahydroazepino, ##STR3## piperazino, and piperazino substituted in position 4 by (C.sub.1 -C.sub.8)alkyl, benzyl or diphenylmethyl; or its salt with an acid or a base.

    摘要翻译: 其中A表示S的式(Ⅰ)化合物; R1选自OH,(C1-C12)烷基,(C1-C12)烷氧基,苄氧基,苯基,苄基(C1-C4)烷基NZ1Z2和NZ1Z2; R2选自OH,SH,(C1-C4)烷氧基,(C1-C4)烷硫基和NZ1Z2; R 3选自H,(C 1 -C 4)烷基,(C 1 -C 4)烷硫基,(C 1 -C 4)烷氧基,苯基和苄基; B选自苯基; 吡啶基 被选自卤素,(C1-C6)烷基,(C1-C6)烷氧基,CF3,CH2NZ1Z2和NZ1Z2中的一个或多个基团取代的苯基,其中Z1和Z2彼此独立地选自H, (C 1 -C 6)烷基,甲酰基和苄基或-NZ 1 Z 2选自吡咯烷基,哌啶基,吗啉代,六氢氮杂环庚烷,哌嗪子基,哌嗪基,其在第4位被(C 1 -C 8)烷基取代,苄基或二苯基甲基 ; 和被一个或多个选自卤素,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,CF 3,CH 2 NZ 1 Z 2和NZ 1 Z 2的基团取代的吡啶基,其中Z 1和Z 2彼此独立地选自H ,(C 1 -C 6)烷基,甲酰基和苄基,或NZ 1 Z 2选自吡咯烷基,哌啶基,吗啉代,杂环吖庚因,哌嗪子基和在位置4上被(C 1 -C 8)烷基取代的哌嗪基,苄基 或二苯基甲基; 或其与酸或碱的盐。

    Indolizine derivatives, with pharmaceutical activity
    46.
    发明授权
    Indolizine derivatives, with pharmaceutical activity 失效
    具有药物活性的中氮衍生物

    公开(公告)号:US5403933A

    公开(公告)日:1995-04-04

    申请号:US80173

    申请日:1993-06-23

    CPC分类号: C07D471/04

    摘要: The invention relates to indolizine derivatives of general formula: ##STR1## in which: X denotes an --S or --SO.sub.2 -- group, each of R.sub.1 and R.sub.2, which are identical or different, denotes hydrogen, the methyl or ethyl radical or a halogen atom,R.sub.3 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl radical,R.sub.4 denotes a precursor radical of a carboxyl group,R denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or phenyl radical, and their use as intermediates for the preparation of pharmaceutically active aminoalkoxybenzenesulphonylindolizine derivatives.

    摘要翻译: 本发明涉及以下通式的中氮茚衍生物:其中:X表示-S或-SO 2 - 基,R 1和R 2各自相同或不同,表示氢,甲基或乙基或 卤素原子,R3表示氢或C1-C4烷基,R4表示羧基的前体基团,R表示C1-C6烷基,C3-C6环烷基或苯基,它们用作制备药物的中间体 活性氨基烷氧基苯磺酰基吲嗪衍生物。

    Substituted thienyl- or pyrrolylcarboxyclic acid derivatives, their
preparation and medicines containing them
    48.
    发明授权
    Substituted thienyl- or pyrrolylcarboxyclic acid derivatives, their preparation and medicines containing them 失效
    取代的噻吩基或吡咯基羧基酸衍生物,其制备方法和含有它们的药物

    公开(公告)号:US5360799A

    公开(公告)日:1994-11-01

    申请号:US109073

    申请日:1993-08-19

    摘要: Compounds of formula ##STR1## in which R.sub.1 represents OH, (C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy, benzyloxy, benzyl, phenyl, (C.sub.1 -C.sub.4)alkylNZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; R.sub.2 represents OH, SH, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio or NZ.sub.1 Z.sub.2 ; R.sub.3 represents H, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy, phenyl or benzyl; A represents N and R represents H or (C.sub.1 -C.sub.4)alkyl which can be substituted by phenyl or NZ.sub.1 Z.sub.2 ; B represents phenyl which is coupled to the pyridyl ring and is optionally substituted by one or more groups chosen from halo, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, CF.sub.3, CH.sub.2 NZ.sub.1 Z.sub.2 or NZ.sub.1 Z.sub.2 ; and Z.sub.1 and Z.sub.2 represent, independently of each other, H, (C.sub.1 -C.sub.6) alkyl, formyl or benzyl, or they form with the nitrogen atom to which they are attached an optionally substituted saturated heterocycle and their salts.

    摘要翻译: 其中R 1表示OH,(C 1 -C 12)烷基,(C 1 -C 12)烷氧基,苄氧基,苄基,苯基,(C 1 -C 4)烷基NZ 1 Z 2或NZ 1 Z 2的式I化合物; R2代表OH,SH,(C1-C4)烷氧基,(C1-C4)烷硫基或NZ1Z2; R3表示H,(C1-C4)烷基,(C1-C4)烷硫基,(C1-C4)烷氧基,苯基或苄基; A表示N,R表示H或可被苯基或NZ1Z2取代的(C1-C4)烷基; B表示与吡啶基环偶联并且任选被一个或多个选自卤素,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,CF 3,CH 2 NZ 1 Z 2或NZ 1 Z 2的基团取代的苯基; 并且Z 1和Z 2彼此独立地表示H,(C 1 -C 6)烷基,甲酰基或苄基,或者与它们所连接的氮原子一起形成任选取代的饱和杂环及其盐。

    Kit for the specific assay of angiotensin II
    49.
    发明授权
    Kit for the specific assay of angiotensin II 失效
    血管紧张素II特异性检测试剂盒

    公开(公告)号:US5296354A

    公开(公告)日:1994-03-22

    申请号:US726376

    申请日:1991-07-05

    CPC分类号: C07K7/14 C07K16/26 G01N33/74

    摘要: The present invention relates to a kit for the specific assay of Angiotension II, comprising:the anti-Ang II antibody,a solution of labelled Ang II,solutions containing the Ang II standards at known and increasing concentrations,the requisite washing solution(s),a solution of anti-Ang III antibody, the said antibody exhibiting a cross-reaction with Ang II of less than 10% and preferably less than 5%,and, optionally, a solution of anti-Ang I antibody and/or a solution of anti-pentapeptide antibody and/or a solution of anti-hexapeptide antibody, the said antibodies exhibiting a cross-reaction with Ang II of less than 10% and preferably less than 5%.

    摘要翻译: 本发明涉及用于血管紧张素II特异性测定的试剂盒,其包含:抗Ang II抗体,标记的Ang II溶液,以已知浓度和浓度增加的含有Ang II标准品的溶液,所需的洗涤溶液, ,抗Ang III抗体的溶液,所述抗体与Ang II交叉反应小于10%,优选小于5%,以及任选地,抗Ang I抗体和/或溶液的溶液 的抗五肽抗体和/或抗六肽抗体的溶液,所述抗体与Ang II交叉反应小于10%,优选小于5%。