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    • 3. 发明授权
      US5215975A Certain hydroxy-phosphinyl-oxy-phenyl methyl-thiazolium hydroxide inner salts as PAF antagonists 失效
    • Certain hydroxy-phosphinyl-oxy-phenyl methyl-thiazolium hydroxide inner salts as PAF antagonists
    • 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
    • US5215975A
    • 1993-06-01
    • US763716
    • 1991-09-23
    • Allan Wissner , Robert E. Schaub , Phaik-Eng Sum
    • Allan Wissner , Robert E. Schaub , Phaik-Eng Sum
    • 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
    • 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
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明授权
      US4897385A Antihypertensive phosphate derivatives 失效
    • Antihypertensive phosphate derivatives
    • 抗高血压磷酸盐衍生物
    • US4897385A
    • 1990-01-30
    • US96945
    • 1987-09-15
    • Allan Wissner , Phaik-Eng Sum
    • Allan Wissner , Phaik-Eng Sum
    • C07F9/10
    • C07F9/10
    • 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 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, 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 ##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.
    • 描述了具有下式的抗高血压磷酸酯衍生物：其中X选自在任何位置被C 1 -C 20支链或直链烷氧基或苄氧基取代的苯基，并且任选在任何其它位置被取代的苯基 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和在任何位置被C 1 -C 20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; 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 5. 发明授权
      US4697031A Antihypertensive phosphate derivatives 失效
    • Antihypertensive phosphate derivatives
    • 抗高血压磷酸盐衍生物
    • US4697031A
    • 1987-09-29
    • US679792
    • 1984-12-10
    • Allan Wissner , Phaik-Eng Sum
    • Allan Wissner , Phaik-Eng Sum
    • C07F9/10
    • C07F9/10
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明授权
      US4981989A Antihypertensive phosphate derivatives and intermediates thereof 失效
    • Antihypertensive phosphate derivatives and intermediates thereof
    • 抗高血压磷酸酯衍生物及其中间体
    • US4981989A
    • 1991-01-01
    • US434967
    • 1989-11-08
    • Allan Wissner , Phaik E. Sum , Robert E. Schaub
    • Allan Wissner , Phaik E. Sum , Robert E. Schaub
    • C07F9/10
    • C07F9/10
    • Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from one or more of: (a) C.sub.1 -C.sub.24 branched or straight chain alkyl; (b) C.sub.1 -C.sub.24 branched or straight chain alkoxy; (c) ##STR2## wherein n and m are integers from 0 to 25 and the sum of n and m is less than or equal to 25; phenyl; substituted phenyl wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, trifluoromethyl, phenyl, and substituted phenyl, phenoxy; and substituted phenoxy, wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, halogen, trifluoromethyl, phenyl and substituted phenyl; Q is selected from the group consisting of: ##STR3## 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 and wherein R.sub.3 is C.sub.1 -C.sub.4 alkyl, with the proviso that when Q is ##STR4## then R.sub.1 is C.sub.1 -C.sub.4 branched or straight chain alkyl; T is a bivalent radical selected from the group consisting of --(CHR).sub.p -- and ##STR5## wherein p is an integer from 1 to 15, the moiety --(CHR).sub.p -- represents an alkylene chain substituted at any position with one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups, and the moiety ##STR6## is bound with the oxygen atom attached directly to the aromatic ring; and Z is ##STR7## wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an integer from 4 to 7; in either the racemic or optically active forms.
    • 描述了具有下式的抗高血压磷酸酯衍生物：其中X选自以下中的一种或多种：（a）C 1 -C 24支链或直链烷基; （b）C 1 -C 24支链或直链烷氧基; （c） 其中n和m是0至25的整数，n和m的总和小于或等于25; 苯基; 取代基苯基，其中取代基选自C 1 -C 20支链或直链烷基，C 1 -C 20支链或直链烷氧基，卤素，三氟甲基，苯基和取代的苯基，苯氧基; 和取代的苯氧基，其中取代基选自C 1 -C 20支链或直链烷基，卤素，三氟甲基，苯基和取代的苯基; Q选自：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和 其中R 3为C 1 -C 4烷基，条件是当Q为“IMA”时，R 1为C 1 -C 4支链或直链烷基; T是选自 - （CHR）p - 和的二价基团，其中p是1至15的整数， - （CHR）p - 部分代表在任何位置被一个或多个 更多的C 1 -C 10烷基或苯基，并且部分“IMAGE”与直接与芳环连接的氧原子结合; 并且Z为，其中R 2为氢或C 1 -C 4支链或直链烷基，q为4至7的整数; 以外消旋或旋光形式。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明授权
      US4827011A Antihypertensive phosphate derivatives 失效
    • Antihypertensive phosphate derivatives
    • 抗高血压磷酸盐衍生物
    • US4827011A
    • 1989-05-02
    • US679790
    • 1984-12-10
    • Allan Wissner , Robert E. Schaub
    • Allan Wissner , Robert E. Schaub
    • C07F9/10 , A61K31/685
    • C07F9/10
    • Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is a C.sub.1 -C.sub.24 branched or straight chain alkyl group; R is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl, with the proviso that at least one R group is not hydrogen; 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; Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR.sup.1).sub.p --, wherein p is an integer from 2 to 12 and the moiety --(CHR.sup.1).sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein R.sub.2 may be chain alkyl and q is an integer from 4 to 7; in either the racemic or in the optically active form.
    • 描述了具有下式的抗高血压磷酸酯衍生物：其中X是C 1 -C 24支链或直链烷基; R选自氢和C 1 -C 4烷基，条件是至少一个R基团不是氢; 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 ; Q是选自 - （CH 2）p - 和（CHR 1）p - 的二价基团，其中p是2至12的整数，并且 - （CHR 1）p - 部分代表被取代的亚烷基链 通过一个或多个C 1 -C 10烷基或苯基; Z选自，其中R 2可以是链烷基，q是4至7的整数; 以外消旋或旋光形式。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US4762942A Antihypertensive phosphate derivatives 失效
    • Antihypertensive phosphate derivatives
    • 抗高血压磷酸盐衍生物
    • US4762942A
    • 1988-08-09
    • US679788
    • 1984-12-10
    • Allan Wissner , Phaik E. Sum , Robert E. Schaub
    • Allan Wissner , Phaik E. Sum , Robert E. Schaub
    • C07F9/10
    • C07F9/10
    • Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from one or more of: (a) C.sub.1 -C.sub.24 branched or straight chain alkyl; (b) C.sub.1 -C.sub.24 branched or straight chain alkoxy; (c) ##STR2## wherein n and m are integers from 0 to 25 and the sum of n and m is less than or equal to 25; phenyl; substituted phenyl wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, trifluoromethyl, phenyl, and substituted phenyl, phenoxy; and substituted phenoxy, wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, halogen, trifluoromethyl, phenyl and substituted phenyl; Q is selected from the group consisting of: ##STR3## 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 and wherein R.sub.3 is C.sub.1 -C.sub.4 alkyl, with the proviso that when Q is ##STR4## then R.sub.1 is C.sub.1 -C.sub.4 branched or straight chain alkyl; T is a bivalent radical selected from the group consisting of --(CHR).sub.p -- and ##STR5## wherein p is an integer from 1 to 15, the moiety --(CHR).sub.p -- represents an alkylene chain substituted at any position with one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups, and the moiety ##STR6## is bound with the oxygen atom attached directly to the aromatic ring; and Z is ##STR7## wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 branched or straight chain alkyl and q is an interger from 4 to 7; in either the racemic or optically active forms.
    • 描述了具有下式的抗高血压磷酸酯衍生物：其中X选自以下中的一种或多种：（a）C 1 -C 24支链或直链烷基; （b）C 1 -C 24支链或直链烷氧基; （c） 其中n和m是0至25的整数，n和m的总和小于或等于25; 苯基; 取代基苯基，其中取代基选自C 1 -C 20支链或直链烷基，C 1 -C 20支链或直链烷氧基，卤素，三氟甲基，苯基和取代的苯基，苯氧基; 和取代的苯氧基，其中取代基选自C 1 -C 20支链或直链烷基，卤素，三氟甲基，苯基和取代的苯基; Q选自：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和 其中R 3为C 1 -C 4烷基，条件是当Q为“IMA”时，R 1为C 1 -C 4支链或直链烷基; T是选自 - （CHR）p - 和的二价基团，其中p是1至15的整数， - （CHR）p - 部分代表在任何位置被一个或多个 更多的C 1 -C 10烷基或苯基，并且部分“IMAGE”与直接与芳环连接的氧原子结合; 并且Z是，其中R 2是氢或C 1 -C 4支链或直链烷基，q是4至7的整数; 以外消旋或旋光形式。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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