会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 1. 发明申请
    • BIOREDUCTIVELY-ACTIVATED PRODRUGS
    • 生物活性物质
    • WO2004085421A3
    • 2005-03-24
    • PCT/GB2004001330
    • 2004-03-26
    • ANGIOGENE PHARM LTDGRAY LAB CANCER RES TRUSTDAVIS PETER DAVIDNAYLOR MATTHEW ALEXANDERTHOMSON PETEREVERETT STEVEN ALBERTSTRATFORD MICHAEL RICHARD LACEWARDMAN PETER
    • DAVIS PETER DAVIDNAYLOR MATTHEW ALEXANDERTHOMSON PETEREVERETT STEVEN ALBERTSTRATFORD MICHAEL RICHARD LACEWARDMAN PETER
    • A61K31/445C07D233/54C07D233/91C07D333/42C07D409/04C07D473/38C07D519/00C07D333/36C07D417/04
    • C07D409/04A61K31/445C07D233/91C07D333/42C07D473/38
    • The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: Ar is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is a group of formula (2) or (3) wherein R1, and R2, which may be the same or different are independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, aryl, COR3 or, together with the intervening carbon atom, form an optionally substituted heterocycloalkyl or carbocyclic ring ; L is -OC(O)- or -OP(O)(OR6)-; n is0or1;X is 0, S, NR7 or a single covalent bond; R3 is OR4 or NR4R5; R4, R5, R6 and R7 are each independently hydrogen or optionally substituted alkyl or, where Rr is NR4R5, R4 and R5 can be joined to form, together with the intervening nitrogen atom, a heterocycloalkyl ring; R8 is hydrogen, alkoxy or diatkylaminoalkyl; R9 is optionally substituted alkyl; R10 is hydrogen, alkyl, alkoxy or dialkylaminoalkyl; R11 and R12 are independently hydrogen, alkyl, alkoxy, thioatkoxy, amino, alkylamino, dialkylamino, morpholino, piperidino,piperazino or l-aziridinyl; A is an optionally substituted aryl or heteroaryl ring; and Dr is a moiety such that DrXH represents a cytotoxic or cytostatic compound.
    • 本发明涉及式(1)化合物或其药学上可接受的盐,其中:Ar是具有至少一个硝基或叠氮基的取代的芳基或杂芳基,或者是式(2)或(3)的基团 )其中可以相同或不同的R 1和R 2独立地是任选取代的烷基,任选取代的烯基,任选取代的炔基,芳基,COR 3或与中间碳原子一起形成任选取代的杂环烷基或碳环; L是-OC(O) - 或-OP(O)(OR 6) - ; n为0或1; X为0,S,NR 7或单个共价键; R3是OR4或NR4R5; R 4,R 5,R 6和R 7各自独立地为氢或任选取代的烷基,或其中R r为NR 4 R 5,可以连接R 4和R 5与杂环氮原子一起形成杂环烷基环; R8是氢,烷氧基或二烷基氨基烷基; R9是任选取代的烷基; R 10是氢,烷基,烷氧基或二烷基氨基烷基; R 11和R 12独立地是氢,烷基,烷氧基,硫代烷氧基,氨基,烷基氨基,二烷基氨基,吗啉代,哌啶子基,哌嗪基或1-氮杂环丁烷基; A是任选取代的芳基或杂芳基环; Dr是一个部分,使得DrXH代表细胞毒性或细胞抑制性化合物。
    • 5. 发明申请
    • BENZIMIDAZOLE VASCULAR DAMAGING AGENTS
    • 苯并咪唑血管损伤剂
    • WO0041669A3
    • 2000-11-16
    • PCT/GB0000099
    • 2000-01-14
    • ANGIOGENE PHARM LTDDAVIS PETER DAVID
    • DAVIS PETER DAVID
    • A61K31/4184A61K31/675A61P9/00A61P17/06A61P19/02A61P27/02A61P29/00A61P35/00A61P43/00C07D235/32C07F9/6506
    • C07F9/65068A61K31/4184A61K31/675C07D235/32
    • 5(6)-substituted benzimidazole-2-carbamates of formula (I) wherein Alk is an alkyl group, X is oxygen, sulphur, sulphinyl, sulphonyl, carbonyl (CO), thiocarbonyl (CS), sulphonyloxy, NH, iminomethylene (C=NH), N-hydroxyiminomethylene, N-alkoxyiminomethylene, dialkoxymethylene, 1,3-dioxolan-2yl, 1,1-ethenyl, a group CHR or a bond, R is hydrogen, alkylaminocarbonyl or alkoxycarbonyl, R is hydrogen, alkoxycarbonyl, cyanomethyl, cyanoethyl, alkoxymethyl or acetoxymethyl. R is hydrogen, hydroxy, alkoxy or amino, A is an optionally substituted aromatic, optionally substituted heteroaromatic, optionally substituted heterocycloalkyl, optionally substituted alkyl or optionally substituted cycloalkyl group and the pharmaceutically acceptable salt, solvates and hydrates thereof, can be used in the preparation of medicaments for the treatment of diseases involving neovascularisation.
    • 其中Alk是烷基,X是氧,硫,亚磺酰基,磺酰基,羰基(CO),硫代羰基(CS),磺酰氧基,NH,亚氨基亚甲基(C)的5(6) - 取代的苯并咪唑-2-氨基甲酸酯 = NH),N-羟基亚氨基亚甲基,N-烷氧基亚氨基亚甲基,二烷氧基亚甲基,1,3-二氧戊环-2-基,1,1-乙烯基,基团CHR 3或键,R 1是氢,烷基氨基羰基或烷氧基羰基,R 2是氢,烷氧基羰基,氰基甲基,氰基乙基,烷氧基甲基或乙酰氧基甲基。 R 3是氢,羟基,烷氧基或氨基,A是任选取代的芳族,任选取代的杂芳族,任选取代的杂环烷基,任选取代的烷基或任选取代的环烷基及其药学上可接受的盐,溶剂化物和水合物 在制备用于治疗涉及新血管形成的疾病的药物中。