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1. 发明授权

US6022307A Substituted dibenzothiophenes having antiangiogenic activity 失效
标题翻译：具有抗血管生成活性的取代的二苯并噻吩
公开(公告)号：US6022307A
公开(公告)日：2000-02-08
申请号：US340353
申请日：1999-06-28
申请人： Mark E. Salvati , Nancy H. Eudy , William A. Hallett , Dennis William Powell
发明人： Mark E. Salvati , Nancy H. Eudy , William A. Hallett , Dennis William Powell
IPC分类号： C07D333/76 , C07D409/14 , C07D495/04 , C07D519/00 , C07F9/6553 , A61K31/38 , A61K31/41 , A61K31/44 , C07D333/00 , C07D333/74
CPC分类号： C07D409/14 , C07D333/76 , C07D495/04 , C07F9/655354
摘要： The invention provides novel substituted dibenzothiophenes of Formulae (I), (II), (III) and (IV) which have antiangiogenic activity and further provides a method using substituted dibenzothiophenes of Formula (V) as antiangiogenic agents.
摘要翻译：本发明提供具有抗血管生成活性的式（I），（II），（III）和（IV）的新的取代的二苯并噻吩并进一步提供使用式（V）的取代的二苯并噻吩作为抗血管生成剂的方法。

2. 发明授权

US4689324A 10,10-dihydro-10-[(substituted-carbonyl)imino]-10-ph enyl-10H-phenoxaphosphines compositions containing same and therapeutic methods of use 失效
标题翻译： 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。

3. 发明授权

US5079247A N.sup.1 -substituted benz(cd)indol-2-imine compounds as cardiovascular agents 失效
标题翻译：作为心血管药物的N1替代苄基（CD）吲哚-2-酮化合物
公开(公告)号：US5079247A
公开(公告)日：1992-01-07
申请号：US495815
申请日：1990-03-14
申请人： Andrew S. Tomcufcik , Walter E. Meyer , Nancy H. Eudy
发明人： Andrew S. Tomcufcik , Walter E. Meyer , Nancy H. Eudy
IPC分类号： A61K31/40 , A61K31/403 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/535 , A61P7/02 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D209/90 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D521/00 , C12N9/99
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14
摘要： N.sup.1 substituted benz [cd] indol -2(1H)-imines useful as inhibitors of Thromboxane synthetase enzyme, hypertension and arrhythmia are described.

4. 发明授权

US4499097A 2-(Pyridyl)imidazolyl ketones 失效
标题翻译： 2-（吡啶基）咪唑基酮
公开(公告)号：US4499097A
公开(公告)日：1985-02-12
申请号：US473939
申请日：1983-03-10
申请人： Andrew S. Tomcufcik , Walter E. Meyer , Nancy H. Eudy
发明人： Andrew S. Tomcufcik , Walter E. Meyer , Nancy H. Eudy
IPC分类号： C07D401/04 , A61K31/415
CPC分类号： C07D401/04
摘要： This disclosure describes novel substituted 2-(pyridyl)imidazol-4-yl ketones and derivatives thereof which possess activity as hypotensive agents.
摘要翻译：本公开内容描述了作为降血压剂具有活性的新型取代的2-（吡啶基）咪唑-4-基酮及其衍生物。

5. 发明授权

US4894368A Certain triphenylphosphinimide derivatives 失效
标题翻译：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。

6. 发明授权

US4777290A 10,10-dihydro-10-[(substituted-carbonyl)imino]-10-phe nyl-10H-phenoxaphosphines 失效
标题翻译： 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。

7. 发明授权

US4914234A 10,10-Dihydro-10-(( substituted-carbonyl)imino)-10-phenyl-10H-phenoxaphosphine, hydrochloride 失效
标题翻译： 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。

8. 发明授权

US4782064A 2-heteroaryl-alkyl-1H-benz[de]-isoquinoline-1,3(2H)-diones 失效
标题翻译： 2-杂芳基 - 烷基-1H-苯并[de] - 异喹啉-1,3（2H） - 二酮
公开(公告)号：US4782064A
公开(公告)日：1988-11-01
申请号：US887688
申请日：1986-07-21
申请人： William B. Wright, Jr. , Andrew S. Tomcufcik , Nancy H. Eudy
发明人： William B. Wright, Jr. , Andrew S. Tomcufcik , Nancy H. Eudy
IPC分类号： C07D401/04 , C07D521/00 , A61K31/47 , C07D233/61 , C07D249/08 , C07D401/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： This invention concerns novel 2-heteroarylalkyl-1H-benz[de]isoquinoline-1,3(2H)-diones which are useful as inhibitors of thromboxane synthetase and/or as hypotensive agents in the treatment of hypertension and myocardial ischemia.
摘要翻译：本发明涉及新颖的2-杂芳基烷基-1H-苯并[de]异喹啉-1,3（2H） - 二酮，其可用作血栓素合成酶的抑制剂和/或用作治疗高血压和心肌缺血的低血压剂。

9. 发明授权

US4767749A Ester of (triarylphosphoranylidene)carbamic acid having diuretic and ability to lower plasma renin properties 失效
标题翻译：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。

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