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    Certain triphenylphosphinimide derivatives
    4.
    发明授权
    Certain triphenylphosphinimide derivatives 失效
    某些三苯基膦酰亚胺衍生物

    公开(公告)号：US4894368A

    公开(公告)日：1990-01-16

    申请号：US207846

    申请日：1988-06-17

    Applicant: Andrew S. Tomcufcik ,  John E. Emma ,  Nancy H. Eudy ,  Joseph W. Marsico ,  Howard Newman

    Inventor： Andrew S. Tomcufcik ,  John E. Emma ,  Nancy H. Eudy ,  Joseph W. Marsico ,  Howard Newman

    IPC: C07F9/535

    CPC classification number: C07F9/5355

    Abstract: Novel triarylphosphinimide derivatives having the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each at the ortho or meta position, represent mono- or disubstituents and are selected from the group consisting of hydrogen, alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), trifluoromethyl and halogen; and R.sub.4 is selected from the group consisting of alkyl (C.sub.1 -C.sub.3), alkenyl(C.sub.2 -C.sub.3), alkynyl(C.sub.2 -C.sub.4), alkynyl(C.sub.2 -C.sub.4), cycloalkyl(C.sub.3 -C.sub.5), cycloalkyl(C.sub.3 -C.sub.6)methyl, 4-oxopentyl, 3-tetrahydrofuranyl, 2,3-dihydro-1H-iden-1-yl, 1-alkyl(C.sub.1 -C.sub.3)cyclopentyl, trans-2-alkyl(C.sub.1 -C.sub.3)cyclopentyl, trans-2-alkoxy(C.sub.1 -C.sub.3)cyclopentyl, 1-cyclopropylethyl, 2-methylcyclopropylmethyl, dicyclopropylmethyl, 2-, 3- or 4-pyridinylmethyl, 2-cyclopenten-1-yl, tetrahydro-2H-pyran-4-yl and cis and trans-2-methoxycyclohexyl; with the proviso that when R.sub.4 is alkyl(C.sub.1 -C.sub.3), R.sub.1, R.sub.2 and R.sub.3 may not each be hydrogenor ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are each at the ortho or meta position and are selected from hydrogen and alkyl(C.sub.1 -C.sub.3), and X is an acid addition salt; processes for producing them, compositions containing them, and methods for using them in mammals to effect diuresis; to lower plasma renin levels and to increase cardiac contractility.

    Abstract translation: 具有式“IMAGE”的新型三芳基膦酰亚胺衍生物，其中R 1，R 2和R 3各自为邻或间位，代表单取代或未取代的，并且选自氢，烷基（C1-C3），烷氧基（C1- C3），三氟甲基和卤素; （C 2 -C 4），炔基（C 2 -C 4），环烷基（C 3 -C 5），环烷基（C 3 -C 6） 甲基，4-氧代戊基，3-四氢呋喃基，2,3-二氢-1H-己烯-1-基，（C1-C3）环戊基，反式-2-烷基（C1-C3）环戊基，反式-2- 烷氧基（C1-C3）环戊基，1-环丙基乙基，2-甲基环丙基甲基，二环丙基甲基，2-，3-或4-吡啶基甲基，2-环戊烯-1-基，四氢-2H-吡喃-4-基和顺式和反式 - 2-甲氧基环己基; 条件是当R 4是烷基（C 1 -C 3）时，R 1，R 2和R 3可以不是氢或者其中R 1，R 2和R 3各自在邻位或间位，并且选自氢和烷基（ C1-C3），X是酸加成盐; 生产它们的方法，含有它们的组合物，以及在哺乳动物中使用它们以产生利尿的方法; 降低血浆肾素水平并增加心脏收缩力。

    10,10-dihydro-10-[(substituted-carbonyl)imino]-10-phe nyl-10H-phenoxaphosphines
    5.
    发明授权
    10,10-dihydro-10-[(substituted-carbonyl)imino]-10-phe nyl-10H-phenoxaphosphines 失效
    10,10-二氢-10- [（取代羰基）亚氨基] -10-苯基-10H-苯氧基膦

    公开(公告)号：US4777290A

    公开(公告)日：1988-10-11

    申请号：US61981

    申请日：1987-07-27

    Applicant: Andrew S. Tomcufcik ,  Joseph W. Marsico ,  Nancy H. Eudy ,  Howard Newman

    Inventor： Andrew S. Tomcufcik ,  Joseph W. Marsico ,  Nancy H. Eudy ,  Howard Newman

    IPC: C07F9/6571 ,  C07F9/02

    CPC classification number: C07F9/657163

    Abstract: Novel 10,10-Dihydro-10-[(substituted carbonyl)imino]-10-phenyl-10H-phenoxaphines of the formula: ##STR1## wherein A is selected from the group consisting of hydrogen and COOR.sub.1, where, when A is hydrogen the compound is in the form of a water soluble salt HnX, where n is an integer 1 or 2 and X is selected from the group consisting of sulfate, trefluoroacetate, bromide and chloride and R.sub.1 is selected from the group consisting of straight or branched chain alkyl(C.sub.1 -C.sub.4), alkenyl(C.sub.2 -C.sub.4), alkynyl(C.sub.2 -C.sub.4), cycloalkyl(C.sub.3 -C.sub.6), cycloalkyl(C.sub.3 -C.sub.6)methyl, benzyl, pyridylmethyl and tetrahydro-3-furanyl; methods for using these compounds for effecting diuresis, treating hypertension and edema and lowering plasma renin activity in mammals; pharmaceutical compositions of matter containing these compounds and processes for their preparation.

    Abstract translation: 新的10,10-二氢-10- [（取代羰基）亚氨基] -10-苯基-10H-吩恶嗪，其结构式如下：其中A选自氢和COOR1，其中当A为氢时 该化合物为水溶性盐HnX的形式，其中n为整数1或2，X选自硫酸盐，三氟乙酸盐，溴化物和氯化物，R1选自直链或支链 烷基（C1-C4），烯基（C2-C4），炔基（C2-C4），环烷基（C3-C6），环烷基（C3-C6）甲基，苄基，吡啶基甲基和四氢-3-呋喃基; 使用这些化合物进行利尿，治疗高血压和水肿以及降低哺乳动物血浆肾素活性的方法; 含有这些化合物的物质的药物组合物及其制备方法。

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