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    Method for inhibiting neoplastic cells and related conditions by exposure thienopyrimidine derivatives
    7.
    发明授权
    Method for inhibiting neoplastic cells and related conditions by exposure thienopyrimidine derivatives 失效
    通过暴露噻吩并嘧啶衍生物抑制肿瘤细胞和相关病症的方法

    公开(公告)号：US6133271A

    公开(公告)日：2000-10-17

    申请号：US197216

    申请日：1998-11-19

    申请人： Rifat Pamukcu ,  Gary A. Piazza

    发明人： Rifat Pamukcu ,  Gary A. Piazza

    IPC分类号： A61K31/519

    CPC分类号： A61K31/519

    摘要： Benzothienopyrimidine derivatives for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and specifically for arresting and treating neoplasia, including precancerous and cancerous lesions of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, A, OA, alkenyl, alkynyl, --NO.sub.2, --CF.sub.3 or halogen, with the proviso that one of R.sub.1 or R.sub.2 is not hydrogen; R.sub.3 and R.sub.4 are independently selected from the group consisting of hydrogen, A, --OA, halogen, --NO.sub.2, --NH.sub.2, --NHA or --NAA', or R.sub.3 and R.sub.4 are together form a moiety selected from the group consisting of --O--CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 --O-- or --O--CH.sub.2 --CH.sub.2 --O; X is selected from the group consisting of an unsubstituted or a substituted 5-7 membered saturated or unsaturated ring, wherein the ring is selected from the group consisting of phenyl, cyclopentyl, cyclohexyl, cycloheptyl, furyl, dioxolanyl, thienyl, pyrrolyl, pyrrolidinyl, imidazolyl, pyrazolyl, pyridyl, piperidinyl, morpholinyl, pyranyl, dioxanyl, pyridazinyl, pyrimidinyl, piperazinyl, quinolyl, and isoquinolyl and wherein the substitutents on the "X" ring are one or two selected from the group consisting of lower alkyl, COOH, --COOA, --CONH.sub.2, --CONAA', --CONHA, --CN, --CH.sub.2 COOH or --CH.sub.2 CH.sub.2 COOH; A and A' are independently selected from the group consisting of hydrogen or C.sub.1-6 alkyl; and n is 0, 1, 2 or 3; and physiologically acceptable salts thereof.

    摘要翻译： 苯并噻吩并嘧啶衍生物，用于诱导或促进凋亡和阻止不受控制的肿瘤细胞增殖，特别是用于阻滞和治疗肿瘤形成，包括式I的癌前期和癌性病变：其中R1和R2独立地选自氢，A，OA， 烯基，炔基，-NO 2，-CF 3或卤素，条件是R 1或R 2中的一个不是氢; R 3和R 4独立地选自氢，A，-OA，卤素，-NO 2，-NH 2，-NHA或-NAA'，或者R 3和R 4一起形成选自-O -CH 2 -CH 2 - ， - O-CH 2 -O-或-O-CH 2 -CH 2 -O; X选自未取代或取代的5-7元饱和或不饱和环，其中环选自苯基，环戊基，环己基，环庚基，呋喃基，二氧戊环基，噻吩基，吡咯基，吡咯烷基， 咪唑基，吡唑基，吡啶基，哌啶基，吗啉基，吡喃基，二烷基，哒嗪基，嘧啶基，哌嗪基，喹啉基和异喹啉基，其中“X”环上的取代基是选自下列的一个或两个：低级烷基，COOH， COOA，-CONH 2，-CONAA'，-CONHA，-CN，-CH 2 COOH或-CH 2 CH 2 COOH; A和A'独立地选自氢或C 1-6烷基; 并且n为0,1,2或3; 及其生理上可接受的盐。