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    10,10-dihydro-10-[(substituted-carbonyl)imino]-10-ph enyl-10H-phenoxaphosphines compositions containing same and therapeutic methods of use
    3.
    发明授权
    10,10-dihydro-10-[(substituted-carbonyl)imino]-10-ph enyl-10H-phenoxaphosphines compositions containing same and therapeutic methods of use 失效
    10,10-二氢-10- [（取代 - 羰基）亚氨基] -10-苯基-10H-苯氧基膦组合物及其治疗方法

    公开(公告)号：US4689324A

    公开(公告)日：1987-08-25

    申请号：US836278

    申请日：1986-03-05

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

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

    IPC分类号： A61K31/675 ,  A61P7/10 ,  A61P9/12 ,  A61P43/00 ,  C07F9/6571 ,  C07F9/02 ,  A61K33/42 ,  C07F9/58

    CPC分类号： C07F9/657163

    摘要： 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 or which 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.

    摘要翻译： 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，吡啶基甲基或四氢-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。

    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

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

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

    IPC分类号： C07F9/535

    CPC分类号： C07F9/5355

    摘要： 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.

    摘要翻译： 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

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

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

    IPC分类号： C07F9/6571 ,  C07F9/02

    CPC分类号： C07F9/657163

    摘要： 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.

    摘要翻译： 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。

    10,10-Dihydro-10-(( substituted-carbonyl)imino)-10-phenyl-10H-phenoxaphosphine, hydrochloride
    6.
    发明授权
    10,10-Dihydro-10-(( substituted-carbonyl)imino)-10-phenyl-10H-phenoxaphosphine, hydrochloride 失效
    10,10-二氢-10 - （（取代羰基）亚氨基）-10-苯基-10H-苯氧基膦，盐酸盐

    公开(公告)号：US4914234A

    公开(公告)日：1990-04-03

    申请号：US228894

    申请日：1988-08-04

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

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

    IPC分类号： C07F9/6571

    CPC分类号： C07F9/657163

    摘要： 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.

    摘要翻译： 新型10,10-二氢-10- [取代的羰基）亚氨基] -10-苯基-10H-吩恶嗪的下式：其中A选自氢和COOR1，其中当A是氢时， 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，R 1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。

    Ester of (triarylphosphoranylidene)carbamic acid having diuretic and ability to lower plasma renin properties
    8.
    发明授权
    Ester of (triarylphosphoranylidene)carbamic acid having diuretic and ability to lower plasma renin properties 失效
    具有利尿作用的（三芳基亚正膦基）氨基甲酸酯和降低血浆肾素性质的能力

    公开(公告)号：US4767749A

    公开(公告)日：1988-08-30

    申请号：US888613

    申请日：1986-07-23

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

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

    IPC分类号： C07F9/535 ,  C07C125/06 ,  A61K31/66

    CPC分类号： C07F9/5355

    摘要： 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), cycloalkyl(C.sub.3 -C.sub.5), cycloalkyl(C.sub.3 -C.sub.6)methyl, 4-oxopentyl, 3-tetrahydrofuranyl, 2,3-dihydro-1H-inden-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 hydrogen ##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.

    摘要翻译： 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; 并且R 4选自烷基（C 1 -C 3），烯基（C 2 -C 3），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， （C 1 -C 3）环戊基，反式-2-烷基（C 1 -C 3）环戊基，反式-2-烷氧基（C 1 -C 3）环戊基 ，1-环丙基甲基，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。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 -C 3），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。