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1. 发明授权

US06200962B1 Thionophosphate derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：硫代磷酸酯衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US06200962B1
公开(公告)日：2001-03-13
申请号：US08849122
申请日：1997-08-07
申请人： Oren Tirosh , Joshua Katzhendler , Isaac Ginsburg , Yehezkel Barenholz , Ron Kohen
发明人： Oren Tirosh , Joshua Katzhendler , Isaac Ginsburg , Yehezkel Barenholz , Ron Kohen
IPC分类号： A61K31664
CPC分类号： A61Q17/00 , A61K8/55 , A61K31/664 , A61K2800/522
摘要： The invention relates to a compound of formula (I) in which X1 and X2 each independently represents an oxygen or nitrogen atom; p,m and n are each independently an integer of at least 2; R, R1 and R2 each independently represents a hydrogen atom; a halogen atom; an optionally substituted straight-chained or branched alkyl alkenyl or alkynyl radical; a group R3O in which R3 is hydrogen atom, an optionally substituted straight-chained or branched alkyl alkenyl or alkynyl radical; optionally substituted acyl or optionally substituted aryl or heteroaryl; a group R4O(O)C in which R4 is a hydrogen atom or an optionally straight-chained or branched alkyl, alkenyl or allkynyl radical; a group —SR5 is a hydrogen atom or an optionally substituted straight-chained or branched alkyl alkenyl or alkynyl radical; a group —NR6R7 in which R6 and R7 each independently represents a hydrogen atom, an optionally substituted straight-chained or branched alkyl, alkenyl or alkynyl radical; optionally substituted acyl; or an optionally substituted phosphate ester group. The invention also relates to processes., for The preparation of compounds of the formula and to pharmaceutical compositions containing the same.
摘要翻译：本发明涉及式（I）化合物，其中X 1和X 2各自独立地表示氧或氮原子; p，m和n各自独立地为至少2的整数; R，R 1和R 2各自独立地表示氢原子; 卤素原子; 任选取代的直链或支链烷基烯基或炔基; R 3为氢原子的基团R 3 O，任选取代的直链或支链烷基烯基或炔基; 任选取代的酰基或任选取代的芳基或杂芳基; R 4是氢原子或任选的直链或支链烷基，烯基或全炔基的基团R4O（O）C; 基团-SR 5是氢原子或任选取代的直链或支链烷基烯基或炔基; R 6和R 7各自独立地表示氢原子的基团-NR 6 R 7，任选取代的直链或支链烷基，烯基或炔基; 任选取代的酰基; 或任选取代的磷酸酯基团。本发明还涉及制备下式化合物和含有该化合物的药物组合物的方法。

2. 发明授权

US06506739B1 Bis-(N,N'-bis-(2-haloethyl)amino)phosphoramidates as antitumor agents 有权
标题翻译：作为抗肿瘤剂的二 - （N，N'-双 - （2-卤代乙基）氨基）氨基磷酸酯
公开(公告)号：US06506739B1
公开(公告)日：2003-01-14
申请号：US09847533
申请日：2001-05-01
申请人： R. Jason Herr , Robert T. Lum , Steven R. Schow , Fanying Meng , Michael R. Kozlowski , Pavel Zhichkin
发明人： R. Jason Herr , Robert T. Lum , Steven R. Schow , Fanying Meng , Michael R. Kozlowski , Pavel Zhichkin
IPC分类号： A61K31664
CPC分类号： A61K45/06 , A61K31/664 , C07F9/2458 , A61K2300/00
摘要： Bis-(N,N′-bis-(2-haloethyl)amino)phosphoramidates, pharmaceutical compositions containing them, methods of treatment using them, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities; and this invention relates to the use of the compounds in methods for the treatment of tumors and, especially, for the treatment of cancer.
摘要翻译：双（（N，N'-双 - （2-卤代乙基）氨基）氨基磷酸酯，含有它们的药物组合物，使用它们的治疗方法及其制备方法。该化合物具有抗肿瘤活性或能够被修饰以具有抗肿瘤活性; 本发明涉及化合物在治疗肿瘤，特别是用于治疗癌症的方法中的用途。

3. 发明授权

US06242433B1 Geranylgeranyl-derivatives, process for the preparation thereof and related pharmaceutical compositions 失效
标题翻译：香叶基香叶基香叶基衍生物，其制备方法和相关的药物组合物
公开(公告)号：US06242433B1
公开(公告)日：2001-06-05
申请号：US09077196
申请日：1998-09-15
申请人： Aldo Balsamo , Bruno Macchia , Marco Macchia , Massimo Baldacci , Romano Danesi , Mario Del Tacca
发明人： Aldo Balsamo , Bruno Macchia , Marco Macchia , Massimo Baldacci , Romano Danesi , Mario Del Tacca
IPC分类号： A61K31664
CPC分类号： C07F9/3808 , C07C307/04 , C07C307/06 , C07F9/3821 , C07F9/3826 , C07F9/4006
摘要： The present invention relates to novel geranylgeranyl derivatives and the pharmaceutically acceptable salts thereof having antiproliferative activity in eukaryotic cells with respect to the inhibition of protein geranygeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process of preparation thereof.
摘要翻译：本发明涉及新颖的香叶基香叶基香叶基衍生物及其在真核细胞中具有抗增殖活性的药学上可接受的盐，涉及抑制蛋白质龙胆神经酰化。本发明还涉及含有新衍生物的药物组合物及其制备方法。

4. 发明授权

US06197760B1 Isophosphoramide mustard analogs and use thereof 有权
标题翻译：异磷酰胺芥菜类似物及其用途
公开(公告)号：US06197760B1
公开(公告)日：2001-03-06
申请号：US09577349
申请日：2000-05-24
申请人： Robert F. Struck
发明人： Robert F. Struck
IPC分类号： A61K31664
CPC分类号： C07F9/2458
摘要： Isophosphoramide mustard analogs useful for treating cancer are provided.
摘要翻译：提供了可用于治疗癌症的异磷酰胺芥菜类似物

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