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    Bis-arylphosphate ester antagonists of platelet activating factor
    4.
    发明授权
    Bis-arylphosphate ester antagonists of platelet activating factor 失效
    血小板激活因子的双芳基磷酸酯拮抗剂

    公开(公告)号：US5147864A

    公开(公告)日：1992-09-15

    申请号：US599580

    申请日：1990-10-18

    申请人： Allan Wissner ,  Kenneth Green ,  Robert E. Schaub

    发明人： Allan Wissner ,  Kenneth Green ,  Robert E. Schaub

    IPC分类号： C07F9/58 ,  C07F9/60 ,  C07F9/62 ,  C07F9/6506 ,  C07F9/6509 ,  C07F9/6512 ,  C07F9/6539

    CPC分类号： C07F9/60 ,  C07F9/581 ,  C07F9/62 ,  C07F9/65061 ,  C07F9/650911 ,  C07F9/650958 ,  C07F9/65121 ,  C07F9/6539

    摘要： The invention is novel compounds of the formula: ##STR1## wherein: X is a phenyl or naphthyl ring optionally substituted in any position with one to four substituents of;(i) --R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, C.sub.1 -C.sub.25 alkoxy, C.sub.1 -C.sub.25 thioalkyl, C.sub.1 -C.sub.25 alkenyloxy, phenyl, phenoxy, substituted phenyl or substituted phenoxy wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen and trifluoremethyl;(ii) hydrogen, halogen, trifluoromethyl, cyano and nitro;(iii) --CO.sub.2 R.sub.3, --CONHR.sub.3, --CHO, OCONHR.sub.3, and --NHCOR.sub.3 wherein R.sub.3 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, phenyl or substituted phenyl wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen or trifluoromethyl;R.sub.1 is one to four substituents on the aromatic ring which may be in any position and are hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or halogen;--CH.sub.2 --Y is a single substituent of the aromatic ring which may occupy any position where Y is ##STR2## wherein R.sub.4 represents one to four substituents of the heterocyclic ring which may occupy a non-hetero atom position and is C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, hydrogen or halogen; and n is the integer 0 or 1 which are antagonists of platelet activating factor.

    摘要翻译： 本发明是下式的新化合物：其中：X是任选在任何位置被一至四个取代基取代的苯基或萘基环; （i）-R2，其中R2是C1-C25烷基，C1-C25烯基，C1-C25烷氧基，C1-C25硫代烷基，C1-C25烯氧基，苯基，苯氧基，取代的苯基或取代的苯氧基，其中取代基是C1-C20 烷基，C 1 -C 20烷氧基，卤素和三氟甲基; （ii）氢，卤素，三氟甲基，氰基和硝基; （iii）-CO 2 R 3，-CONHR 3，-CHO，OCONHR 3和-NHCOR 3，其中R 3是C 1 -C 25烷基，C 1 -C 25烯基，苯基或取代的苯基，其中取代基是C 1 -C 20烷基，C 1 -C 20烷氧基，卤素或 三氟甲基 R 1是芳环上一至四个可以在任何位置并且是氢，C 1 -C 5烷基，C 1 -C 5烷氧基或卤素的取代基; -CH 2 -Y是芳环的单个取代基，其可以占据任何位置，其中Y是可以占据非杂原子位置的杂环的一至四个取代基， 是C 1 -C 5烷基，C 1 -C 5烷氧基，氢或卤素; 并且n是作为血小板活化因子的拮抗剂的整数0或1。

    Antihypertensive phosphate derivatives
    6.
    发明授权
    Antihypertensive phosphate derivatives 失效
    抗高血压磷酸盐衍生物

    公开(公告)号：US4762942A

    公开(公告)日：1988-08-09

    申请号：US679788

    申请日：1984-12-10

    申请人： Allan Wissner ,  Phaik E. Sum ,  Robert E. Schaub

    发明人： Allan Wissner ,  Phaik E. Sum ,  Robert E. Schaub

    IPC分类号： C07F9/10

    CPC分类号： C07F9/10

    摘要： 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.

    摘要翻译： 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。

    Certain hydroxy-phosphinyl-oxy-phenyl methyl-thiazolium hydroxide inner salts as PAF antagonists
    7.
    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

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

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

    IPC分类号： 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分类号： 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

    摘要： 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.

    摘要翻译： 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
    8.
    发明授权
    Antihypertensive phosphate derivatives 失效
    抗高血压磷酸盐衍生物

    公开(公告)号：US4900731A

    公开(公告)日：1990-02-13

    申请号：US97100

    申请日：1987-09-15

    申请人： Allan Wissner ,  Robert E. Schaub

    发明人： Allan Wissner ,  Robert E. Schaub

    IPC分类号： C07F9/10

    CPC分类号： C07F9/10

    摘要： Antihypertensive phosphate derivatives are described having the following formula: ##STR1## wherein n is an integer 1 or 2; m is an integer 1 or 2, and the sum of n and m must be 3; X is selected from the group consisting of C.sub.1 -C.sub.24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of 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, phenyl and substituted phenyl; 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).sub.p --, where p is an integer from 2 to 12 and the moiety --(CHR).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 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 and q is an integer from 4 to 7.

    摘要翻译： 抗高血压磷酸酯衍生物被描述为具有下列结构式：其中n是整数1或2; m为整数1或2，n和m之和必须为3; X选自C 1 -C 24支链或直链烷氧基和取代苯氧基，其中取代基选自C1-C20支链或直链烷基，C1-C20支链或直链烷氧基中的一个或多个 ，卤素，苯基和取代的苯基; 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）p - 的二价基团，其中p是2至12的整数，并且 - （CHR）p - 部分代表亚烷基链， 被一个或多个C 1 -C 10烷基或苯基取代; Z选自，其中R 2可以相同或不同，并且选自氢和C 1 -C 4支链或直链烷基，q是4至7的整数。