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    • 2. 发明申请
    • TRICYCLIC COMPOUNDS WITH PHARMACEUTICAL ACTIVITY
    • 具有药物活性的三元化合物
    • WO1994011354A1
    • 1994-05-26
    • PCT/GB1993002281
    • 1993-11-04
    • ZENECA LIMITEDBRITISH TECHNOLOGY GROUP LTD.BOYLE, Francis, ThomasCROOK, James, WilliamMATUSIAK, Zbigniew, Stanley
    • ZENECA LIMITEDBRITISH TECHNOLOGY GROUP LTD.
    • C07D239/70
    • C07D401/12C07D239/70C07D403/12
    • The invention relates to tricyclic compounds of formula (I) wherein R is hydrogen, amino, (1-4C)alkyl, (1-4C)alkoxy, hydroxy-(1-4C)alkyl or fluoro-(1-4C)alkyl; R is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(2-4C)alkyl, halogeno-(2-4C)alkyl or cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl; and R includes a group of the formula -NHCH(CO2H)-A -Y wherein A is (1-6C)alkylene and Y is carboxy, tetrazol-5-yl, N &cir& _-[(1-4C)alkylsulphonyl]carbamoyl, N &cir& _(phenylsulphonyl)carbamoyl, tetrazol-5-ylthio, tetrazol-5-ylsulphinyl or tetrazol-5-ylsulphonyl; or pharmaceutically-acceptable salts or esters thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-cancer agents.
    • 本发明涉及式(I)的三环化合物,其中R 1是氢,氨基,(1-4C)烷基,(1-4C)烷氧基,羟基 - (1-4C)烷基或氟 - (1-4C) )烷基; R 2是氢,(1-4C)烷基,(3-4C)烯基,(3-4C)炔基,羟基 - (2-4C)烷基,卤代 - (2-4C)烷基或氰基 - (1 -4C)烷基; Ar是任选取代的亚苯基,噻吩二基,噻唑二基,吡啶二基或嘧啶二基; 并且R 3包括其中A 1为(1-6C)亚烷基且Y 1为羧基的式-NHCH(CO 2 H)-A 1 -Y 1的基团,四唑-5-基, (1-4C)烷基磺酰基]氨基甲酰基,N,(苯基磺酰基)氨基甲酰基,四唑-5-基硫基,四唑-5-基亚磺酰基或四唑-5-基磺酰基; 或其药学上可接受的盐或酯; 制造过程; 含有它们的药物组合物; 并将其用作抗癌剂。
    • 5. 发明申请
    • INDOLOQUINONE DERIVATIVES AS BIOREDUCTIVE AGENTS
    • 吲哚喹啉衍生物作为生物降解剂
    • WO1997023456A1
    • 1997-07-03
    • PCT/GB1996003176
    • 1996-12-20
    • BRITISH TECHNOLOGY GROUP LTD.STRATFORD, Ian, JamesNAYLOR, Matthew, AlexanderJAFFAR, MohammedADAMS, Gerald, Edward
    • BRITISH TECHNOLOGY GROUP LTD.
    • C07D209/42
    • C07D209/12A61K31/404
    • Use of a compound of general formula (I) or salt thereof wherein R and R are independently selected from hydrogen, halogen and C1-6 alkyl or haloalkyl, C2-6 alkenyl or haloalkenyl, C1-6 alkoxy, phenoxy, C1-6 alkylthio, phenylthio, primary and secondary amino or hydroxy groups and R is hydrogen, hydroxy, a C1-6 alkyl or haloalkyl, C2-6 alkenyl or haloalkenyl or C1-6 alkoxy or haloalkoxy group is provided for the manufacture of a medicament for the treatment of neoplasms, particularly solid cancerous tumours characterised in that R is selected from a C1-6 alkyl or haloalkyl group, -CO2R where R is hydrogen or a C1-6 alkyl or haloalkyl group, or a group -CH2-X where X is selected from groups of formula -S-R , -O-R , and (a) where R is a hydrogen or a leaving group, the acid HR6 of which has a pKa of 10 or less and R and R are the same or different and are selected from C1-6 alkyl or haloalkyl or together with the interjacent nitrogen form a heterocyclic ring of 5 to 7 atoms optionally substituted by C1-4 alkyl or haloalkyl and R is selected from hydrogen, C1-4 alkyl and haloalkyl or groups-(CH2)nCHR R of more than four carbon atoms where n is an integer of 0 to 2 and R and R are independently selected from a C1-4 alkyl or haloalkyl group, or R and R together with the interjacent carbon atom form a C3-7 cycloalkyl or cycloalkenyl ring optionally substituted with one or more C1-4 alkyl or haloalkyl, or C2-4 alkenyl or haloalkenyl groups.
    • 使用通式(I)的化合物或其盐,其中R和R 4独立地选自氢,卤素和C 1-6烷基或卤代烷基,C 2-6烯基或卤代烯基,C 1-6烷氧基,苯氧基,C 1 -6烷硫基,苯硫基,伯和仲氨基或羟基,R 3为氢,羟基,C 1-6烷基或卤代烷基,C 2-6烯基或卤代链烯基或C 1-6烷氧基或卤代烷氧基,用于制备 用于治疗肿瘤,特别是固体癌性肿瘤的药物,其特征在于R 1选自C 1-6烷基或卤代烷基,-CO 2 R 5,其中R 5是氢或C 1-6烷基 或卤代烷基,或基团-CH 2 -X(其中X选自式-SR 6,-OR 6)和(a)其中R 6为氢或离去基团的基团,该酸 HR6的pKa为10以下,R 7和R 8相同或不同,选自C 1-6烷基或卤代烷基,或与中间的氮一起形成杂环 任选被C 1-4烷基或卤代烷基取代的5至7个原子,R 2选自氢,C 1-4烷基和卤代烷基或多于四个碳原子的基团 - (CH 2)n CHR 9 R 10,其中 n为0〜2的整数,R 9和R 10独立地选自C 1-4烷基或卤代烷基,或R 9和R 10与中间碳原子一起形成C 3 -7环烷基或环烯基,任选被一个或多个C 1-4烷基或卤代烷基取代,或C 2-4链烯基或卤代烯基。
    • 8. 发明申请
    • DIAMOND FILM DEPOSITION
    • 金刚石膜沉积
    • WO1993024676A1
    • 1993-12-09
    • PCT/GB1993001082
    • 1993-05-26
    • BRITISH TECHNOLOGY GROUP LTD.JOHN, PhillipWILSON, John, Ivor, BarrettDRUMMOND, Iain, Cameron
    • BRITISH TECHNOLOGY GROUP LTD.
    • C23C16/26
    • C23C16/274B24C3/32B24C5/08B24C11/00C23C16/0254
    • The invention provides an improved method and apparatus for pre-treating a substrate surface (19) to prepare it for subsequent deposition upon it of a film of diamond. The method of pre-treating a surface according to the invention comprises the steps of positioning a quantity of diamond dust (16) in relation to the surface, producing a shock wave in gas adjacent the dust, subjecting the dust to the shock wave, and thereby causing the diamond dust to impinge at high velocity on to the surface. The apparatus according to the invention comprises means for holding a charge of diamond dust (15), means for generating a shock wave in gas adjacent the charge of diamond dust (17), and means for directing the shock wave at the diamond dust (12) and causing the diamond dust to be expelled at high velocity for impingement on the substrate surface. The invention also provides a method depositing a diamond film on a substrate, including pre-treatment by the aforesaid method or apparatus.
    • 本发明提供了一种改进的方法和装置,用于预处理衬底表面(19)以准备其用于随后沉积在金刚石膜上。 根据本发明的预处理表面的方法包括以下步骤:相对于表面定位一定数量的金刚石粉尘(16),在靠近灰尘的气体中产生冲击波,使粉尘受到冲击波的影响;以及 从而使金刚石粉尘以高速撞击到表面。 根据本发明的装置包括用于保持金刚石粉尘(15)的装置的装置,用于在靠近金刚石粉尘(17)的充电的气体中产生冲击波的装置,以及用于将冲击波引导到金刚石粉尘(12) )并使金刚石粉尘以高速度排出以冲击衬底表面。 本发明还提供了一种在衬底上沉积金刚石膜的方法,包括通过前述方法或装置的预处理。