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    Certain hydroxy-phosphinyl-oxy-phenyl methyl-thiazolium hydroxide inner salts as PAF antagonists
    27.
    发明授权
    Certain hydroxy-phosphinyl-oxy-phenyl methyl-thiazolium hydroxide inner salts as PAF antagonists 失效
    某些羟基氧膦基 - 氧 - 苯基甲基 - 噻唑鎓氢氧化物内盐作为PAF拮抗剂

    公开(公告)号：US5215975A

    公开(公告)日：1993-06-01

    申请号：US763716

    申请日：1991-09-23

    Applicant: Allan Wissner ,  Robert E. Schaub ,  Phaik-Eng Sum

    Inventor： Allan Wissner ,  Robert E. Schaub ,  Phaik-Eng Sum

    IPC: C07C43/174 ,  C07C43/178 ,  C07C59/125 ,  C07C309/73 ,  C07D213/20 ,  C07D215/10 ,  C07D277/22 ,  C07D521/00 ,  C07F9/12 ,  C07F9/58 ,  C07F9/60 ,  C07F9/62 ,  C07F9/6509 ,  C07F9/6539

    CPC classification number: C07D213/20 ,  C07C309/73 ,  C07C43/1745 ,  C07C43/1785 ,  C07C59/125 ,  C07D215/10 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/22 ,  C07F9/12 ,  C07F9/581 ,  C07F9/60 ,  C07F9/62 ,  C07F9/650911 ,  C07F9/650958 ,  C07F9/6539

    Abstract: The invention is a compound of R or S enantiomers or racemic mixtures of compounds of the formula: ##STR1## wherein: (A) X is(i) C.sub.1 -C.sub.24(ii) C.sub.1 -C.sub.24 alkoxy;(iii) C.sub.1 -C.sub.24 carboamoyloxy; ##STR2## wherein n is an integer from 1 to 25 and m is an integer from 0 to 24 and the sum of n and m is less than or equal to 25;(v) phenyl;(vi) mono-or polysubstituted phenyl substituted with C.sub.1 -C.sub.20 alkoxy, halogen, trifluoromethyl, phenyl, or benzyloxy;(vii) phenoxy;(viii) mono- or polysubstituted phenoxy substituted with C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen, trifluoromethyl, phenyl, or benzyloxy;(ix) naphthaloxy;(x) mono- or polysubstituted naphthaloxy substituted with C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy or halogen;(B) i is an integer from 1 to 3 and j is an integer from 1 to 6;(C) Q is --OR.sub.2, ##STR3## or O--C--R.sub.2, wherein R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkenyl;(D) Y is the divalent radical ##STR4## (E) the moiety R.sub.3 represents one or more C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or halogen substituents of the aromatic ring;(F) the moiety --CH.sub.2 A may be in the ortho, meta or para position wherein A is the(i) ##STR5## which are PAF inhibitors.

    Abstract translation: 本发明是下式化合物的R或S对映异构体或外消旋混合物的化合物：其中：（A）X为（ⅰ）C 1 -C 24（ⅱ）C 1 -C 24烷氧基; （iii）C 1 -C 24甲酰氧基; （iiii） 其中n为1至25的整数，m为0至24的整数，n和m之和为 小于或等于25; （v）苯基; （vi）被C1-C20烷氧基，卤素，三氟甲基，苯基或苄氧基取代的单取代或多取代的苯基; （vii）苯氧基; （viii）被C 1 -C 20烷基，C 1 -C 20烷氧基，卤素，三氟甲基，苯基或苄氧基取代的单取代或多取代的苯氧基; （ix）萘氧基; （x）被C 1 -C 20烷基，C 1 -C 20烷氧基或卤素取代的单取代或多取代的萘​​氧基; （B）i为1〜3的整数，j为1〜6的整数。 （C）Q为-OR2，IMA或者O-C-R2，其中R2为氢，C1-C6烷基或C1-C6烯基; （D）Y是二价基团（E）部分R 3表示芳环的一个或多个C 1 -C 5烷基，C 1 -C 5烷氧基或卤素取代基; （F）部分-CH 2 A可以在邻位，间位或对位，其中A是作为PAF抑制剂的（i）IMA。

    Antihypertensive phosphate derivatives
    28.
    发明授权
    Antihypertensive phosphate derivatives 失效
    抗高血压磷酸盐衍生物

    公开(公告)号：US4697031A

    公开(公告)日：1987-09-29

    申请号：US679792

    申请日：1984-12-10

    Applicant: Allan Wissner ,  Phaik-Eng Sum

    Inventor： Allan Wissner ,  Phaik-Eng Sum

    IPC: C07F9/10

    CPC classification number: C07F9/10

    Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from the group consisting of a phenyl radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted by any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen, and a naphthalene radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Y is selected from the group of bivalent radicals consisting of --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer from 2 to 10 and the moiety --(CHR).sub.p -- represents an alkylene chain substituted with one or more C.sub.1 -C.sub.8 alkyl groups or phenyl groups; Z is selected from the group consisting of --N.sup.+ (R.sub.2).sub.3 and ##STR3## wherein q is an integer from 4-7 and R.sub.2 may be the same or different and is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl.

    Abstract translation: 描述了具有下式的抗高血压磷酸酯衍生物：其中X选自在任何位置与C 1 -C 20支链或直链烷氧基或苄氧基取代的苯基，并任选被任何其它位置取代的苯基 与一个或多个由C 1 -C 15支链或直链烷基，C 1 -C 15支链或直链烷氧基和卤素组成的基团，以及在任何位置被C1-C20支链或直链烷氧基或苄氧基取代的萘基和任选取代的 在一个或多个由C 1 -C 15支链或直链烷基，C 1 -C 15支链或直链烷氧基和卤素组成的基团的任何其它位置; T选自氢和其中R 1选自氢，C 1 -C 4支链或直链烷基，C 1 -C 4支链或直链烷氧基和C 1 -C 4支链或直链烷基氨基 ; Y选自由 - （CH 2）p - 和（CHR）p - 组成的二价基团，其中p是2至10的整数， - （CHR）p - 部分代表被一个 或更多的C 1 -C 8烷基或苯基; Z选自-N +（R2）3和，其中q是4-7的整数，R2可以相同或不同，并且选自氢和C 1 -C 4支链或 直链烷基。

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