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2. 发明授权

US06218378B1 Anti-tumor agents comprising pyridyl-substituted metal-diphosphine complex 失效
标题翻译：抗肿瘤剂包括吡啶基取代的金属 - 二膦配合物
公开(公告)号：US06218378B1
公开(公告)日：2001-04-17
申请号：US08860518
申请日：1997-08-22
申请人： Susan Jane Berners-Price , Richard John Bowen , Peter Gordon Parsons
发明人： Susan Jane Berners-Price , Richard John Bowen , Peter Gordon Parsons
IPC分类号： A01N5502
CPC分类号： A61K31/675 , C07F9/5059 , C07F9/5068 , C07F9/58 , Y10T428/12396 , Y10T428/12444
摘要： A method of treatment or inhibition of tumors including the steps of: (i) exchanging one or more of the eight phenyl substituents in the compound [M(dppe)2]+ where M is selected from Au(I), Ag(I) and Cu(I) by 2, 3, or 4 pyridyl substituents to provide a compound having anti-tumor activity and an octanol/water partition coefficient between 0.01 and 25.5; and (ii) administering said compound to a subject requiring treatment which compound has selective toxicity to cancer cells including cisplatin resistant human carcinoma cell lines. The invention also includes within its scope compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are the same or different and may be selected from phenyl, 4-pyridyl, 3-pyridyl, 2-pyridyl wherein each of the 4-pyridyl, 3-pyridyl and 2-pyridyl may optionally be substituted; A is selected from —(CH2)— wherein n is 2 or 3 or cis —CH═CH— or (a) where R9 represents carboxylate and in such case R1, R2, R3, R4, R5, R6, R7 and R8, may be all phenyl; M is Au(I), Ag(I) or Cu(I); X is monovalent anion such as nitrate or bromide, chloride, iodine or any other non-toxic anion; with the following provisos: (i) R1 through R8 cannot be all phenyl; (ii) when R1 through R8 is 2-pyridyl, and A is —(CH2)2—, M cannot be Au(I); or (iii) when R1 through R8 is the same and is 4-pyridyl, X is Cl and A is —(CH2)2—, M cannot be Au(I).
摘要翻译：一种治疗或抑制肿瘤的方法，包括以下步骤：（i）在化合物[M（dppe）2] +中交换一个或多个八个苯基取代基，其中M选自Au（I），Ag（I）和Cu（I）2,3或4个吡啶基取代基，以提供具有抗肿瘤活性和辛醇/水分配系数在0.01至25.5之间的化合物; 和（ii）向需要治疗的受试者施用所述化合物，所述化合物对包括顺铂耐药性人癌细胞系的癌细胞具有选择性毒性。本发明还包括其范围内的式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8相同或不同，并且可以选自苯基，4-吡啶基，3-吡啶基， - 吡啶基，其中每个4-吡啶基，3-吡啶基和2-吡啶基可任选被取代; A选自 - （CH 2） - ，其中n为2或3或顺式-CH = CH-或（a）其中R9表示羧酸盐，在这种情况下，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8，可能全部为苯基; M是Au（I），Ag（I）或Cu（I）; X是一价阴离子，如硝酸盐或溴化物，氯化物，碘或任何其他无毒阴离子; 具有以下条件：（i）R 1至R 8不能全部为苯基; （ii）当R 1至R 8为2-吡啶基且A为 - （CH 2）2 - 时，M不能为Au（I）; 或（iii）当R 1至R 8相同且为4-吡啶基时，X为Cl且A为 - （CH 2）2 - ，M不能为Au（I）。

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