Aminoacylates of glycerol acetal
    7.
    发明授权
    Aminoacylates of glycerol acetal 失效
    甘油缩醛的氨基酰化酶

    公开(公告)号:US4921865A

    公开(公告)日:1990-05-01

    申请号:US203733

    申请日:1988-06-07

    CPC分类号: C07D405/12 C07D417/12

    摘要: The invention relates to new aminoacylates of glycerol acetal of the general formula I ##STR1## wherein R.sub.1 represents a substituted phenyl group or a group of the formula C.sub.m H.sub.2m+1, m being an integer of from 9 to 25,R.sub.2 represents a hydrogen atom, a phenyl group or a group of the formula C.sub.n H.sub.2n+1, n being an integer of from 1 to 10,p is a integer of from 3 to 10, ##STR2## represents a nitrogen containing heterocyclic group and X.sup..crclbar. means a pharmaceutically acceptable anion to a preparation process of said compounds and to therapeutic compositions of matter containing the same.

    摘要翻译: 本发明涉及通式Ⅰ的甘油缩醛的新氨基酰化物,其中R1代表取代的苯基或式CmH2m + 1的基团,m为9-25的整数,R2代表氢原子 苯基或式CnH2n + 1的基团,n为1〜10的整数,p为3〜10的整数,< IMAGE>表示含氮杂环基,X( - )表示 所述化合物的制备方法的药学上可接受的阴离子和含有该阴离子的物质的治疗组合物。

    Octahydro indenofuran derivatives and their therapeutic compositions
    8.
    发明授权
    Octahydro indenofuran derivatives and their therapeutic compositions 失效
    八氢吲哚呋喃衍生物及其治疗组合物

    公开(公告)号:US4904693A

    公开(公告)日:1990-02-27

    申请号:US267438

    申请日:1988-11-04

    CPC分类号: C07D307/93

    摘要: This invention relates to indenofuran derivatives of the formula: ##STR1## wherein R stands for H or for a ##STR2## group optionally substituted on the phenyl ring by Alk, OH or OAlk, Alk being a lower straight or branched alkyl group up to C.sub.5, to the preparation of these compounds and to therapeutic compositions containing the same in the field of anaphylaxis.

    摘要翻译: 本发明涉及下式的茚诺呋喃衍生物:其中R代表H或任选在苯环上被Alk,OH或OAlk取代的基团,Alk是直至C5的低级直链或支链烷基 ,涉及这些化合物的制备及其在过敏反应领域中含有该组合物的治疗组合物。

    Method for inhibiting blood vessel blockage using octapeptide
compositions
    10.
    发明授权
    Method for inhibiting blood vessel blockage using octapeptide compositions 失效
    使用八肽组合物抑制血管阻塞的方法

    公开(公告)号:US5147856A

    公开(公告)日:1992-09-15

    申请号:US329854

    申请日:1989-03-28

    IPC分类号: A61K38/00 C07K14/655

    CPC分类号: C07K14/6555 A61K38/00

    摘要: A method for inhibiting blood vessel blockage in a mammal particularly after a procedure such as angioplasty, an arterial bypass operation or an allograft transplant operation which comprises: administering to a mammal before, during and/or after the procedure an effective blood vessel blockage inhibiting amount of an octapeptide having the formula ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o-, m- or, more preferably, p-substituted X-Phe (where X is a halogen, H, NH.sub.2, NO.sub.2, OH , or C.sub.1-13 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile; A.sub.7 is Thr, Trp, or .beta.-Nal (and can be either the D- or L-isomer); and Z is NH.sub.2 or OH; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 一种抑制哺乳动物血管阻塞的方法,特别是在诸如血管成形术,动脉旁路操作或同种异体移植手术的手术之后,包括:在手术之前,期间和/或之后向哺乳动物施用有效的血管阻塞抑制量 具有式 + TR LA7Z的八肽,其中每个A1和A2独立地是H,C1-12烷基,C7-10苯基烷基,R1CO(其中R1是C1-20烷基,C3-20烯基,C3- 20个炔基,苯基,萘基或C7-10苯基烷基)或R2OCO(其中R2是C1-10烷基或C7-10苯基烷基),条件是当A1或A2之一为R1CO或R2OCO时,另一个必须为H; A3是CH2A6(其中A6是五氟苯基,萘基,吡啶基或苯基); A4是邻 - ,间 - 或更优选对取代的X-Phe(其中X是卤素,H,NH 2,NO 2,OH或C 1-13烷基),五氟-Phe或β-Nal; A5是Thr,Ser,Phe,Val,α-氨基丁酸或Ile; A7是Thr,Trp或β-Nal(并且可以是D-或L-异构体); Z是NH 2或OH; 或其药学上可接受的盐。