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    Preparation of camptothecin analogs
    4.
    发明授权
    Preparation of camptothecin analogs 失效
    喜树碱类似物的制备

    公开(公告)号：US5541327A

    公开(公告)日：1996-07-30

    申请号：US340034

    申请日：1994-11-14

    申请人： Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen ,  Craig A. Coburn

    发明人： Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen ,  Craig A. Coburn

    IPC分类号： C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07H17/00

    CPC分类号： C07D491/14 ,  C07H17/00

    摘要： Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H, OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO.sub.2 R, nitro, cyano, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, OR.sup.13 ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R.sup.13 is glycosyl; n is 0 or 1; with the proviso that when R.sup.1 is ethyl, and n is 0, E, R.sup.2, R.sup.3, and R.sup.4 are not all H. Intermediate compounds leading to the camptothecin analogues comprise substituted tricyclic compounds which consist of rings C, D, and E fused together. Methods for preparing the analogues involve condensation of such intermediates with variably substituted protected .alpha.-aminobenzaldehydes.

    摘要翻译： 具有一般结构的具有对癌细胞的细胞毒性活性的喜树碱的取代类似物：其中E是H，CO 2 R，CONH 2，CONHR，CONR 2，酰基或CN; X是H，OH或OR; R 1，R 2，R 3和R 4独立地相同或不同，为H，或直链或支链烷基，烷基芳基或羟烷基或芳基; R 5，R 6，R 7，R 8和R 9独立地相同或不同，为H，或直链或支链烷基，烷基芳基，烷氧基，羟基烷基或氨基烷氧基，或芳基或芳氧基或C- ，或CO 2 R，硝基，氰基，Cl，F，Br，I，SR10，NR 11 R 12，OR 13; R为H或直链或支链烷基，烷基芳基或羟烷基或芳基; R 10，R 11和R 12独立地相同或不同，为H，或直链或支链烷基，烷基芳基，羟基烷基或酰基或芳基; R13是糖基; n为0或1; 条件是当R 1为乙基且n为0时，E，R 2，R 3和R 4不全为H.导致喜树碱类似物的中间体化合物包含由稠合在一起的环C，D和E组成的取代的三环化合物 。 制备类似物的方法涉及这种中间体与可变取代的被保护的α-氨基苯甲醛的缩合。

    Camptothecin analogues
    5.
    发明授权
    Camptothecin analogues 失效
    喜树碱类似物

    公开(公告)号：US5446047A

    公开(公告)日：1995-08-29

    申请号：US919188

    申请日：1992-07-23

    申请人： Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen

    发明人： Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen

    IPC分类号： C07D491/14 ,  C07D491/22 ,  C07H17/00 ,  A61K31/435

    CPC分类号： C07D491/14 ,  C07H17/00

    摘要： Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H, OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl, or aryl; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, linear or branched alkyl, linear or branched alkylaryl, aryl, CO.sub.2 R, alkoxy, aryloxy, hydroxyalkyl, C-glycal, nitro, cyano, aminoalkoxy, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, or OR.sup.13 ; R is H, alkyl, aryl, alkylaryl, hydroxyalkyl, or hydroxyalkyl; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, alkyl, aryl, alkylaryl, hydroxyalkyl, or acyl; R.sup.13 is glycosyl; n is 0 or 1; with the proviso that when R.sup.1 is ethyl, and n is 0, E, R.sup.2, R.sup.3, and R.sup.4 are not all H. Intermediate compounds leading to the camptothecin analogues comprise substituted tricyclic compounds which consist of rings C, D, and E fused together. Methods for preparing the analogues involve condensation of such intermediates with variably substituted protected .alpha.-aminobenzaldehydes.

    摘要翻译： 具有一般结构的具有对癌细胞的细胞毒性活性的喜树碱的取代类似物：其中E是H，CO 2 R，CONH 2，CONHR，CONR 2，酰基或CN; X是H，OH或OR; R 1，R 2，R 3和R 4独立地相同或不同，为H，直链或支链烷基，直链或支链烷基芳基，羟基烷基或芳基; R 5，R 6，R 7，R 8和R 9各自独立地相同或不同，为H，直链或支链烷基，直链或支链烷基芳基，芳基，CO 2 R，烷氧基，芳氧基，羟基烷基，C-缩醛，硝基，氰基，氨基烷氧基， Cl，F，Br，I，SR10，NR11R12或OR13; R是H，烷基，芳基，烷基芳基，羟烷基或羟烷基; R 10，R 11和R 12独立地相同或不同，为H，烷基，芳基，烷基芳基，羟基烷基或酰基; R13是糖基; n为0或1; 条件是当R 1为乙基且n为0时，E，R 2，R 3和R 4不全为H.导致喜树碱类似物的中间体化合物包含由稠合在一起的环C，D和E组成的取代的三环化合物 。 制备类似物的方法涉及这种中间体与可变取代的被保护的α-氨基苯甲醛的缩合。

    Methods of preparation of camptothecin analogs
    6.
    发明授权
    Methods of preparation of camptothecin analogs 失效
    喜树碱类似物的制备方法

    公开(公告)号：US5391745A

    公开(公告)日：1995-02-21

    申请号：US2996

    申请日：1993-01-11

    申请人： Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen ,  Craig A. Coburn

    发明人： Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen ,  Craig A. Coburn

    IPC分类号： C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07H17/00 ,  C07D491/52

    CPC分类号： C07D491/14 ,  C07H17/00

    摘要： Substituted analoguss of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO.sub.2 R, nitro, cyano, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, or OR.sup.13 ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R.sup.13 is glycosyl; n is 0 or 1; with the proviso that when R.sup. 1 is ethyl, and n is 0, E, R.sup.2, R.sup.3, and R.sup.4 are not all H. Intermediate compounds leading to the camptothecin analogues comprise substituted tricyclic compounds which consist of rings C, D, and E fused together. Methods for preparing the analoguss involve condensation of such intermediates with variably substituted protected .alpha.-aminobenzaldehydes.

    摘要翻译： 具有一般结构的具有对癌细胞的细胞毒性活性的喜树碱的取代类似物：其中E是H，CO 2 R，CONH 2，CONHR，CONR 2，酰基或CN; X是H OH或OR; R 1，R 2，R 3和R 4独立地相同或不同，为H，或直链或支链烷基，烷基芳基或羟烷基或芳基; R 5，R 6，R 7，R 8和R 9独立地相同或不同，为H，或直链或支链烷基，烷基芳基，烷氧基，羟基烷基或氨基烷氧基，或芳基或芳氧基或C- ，或CO 2 R，硝基，氰基，Cl，F，Br，I，SR10，NR 11 R 12或OR 13; R为H或直链或支链烷基，烷基芳基或羟烷基或芳基; R 10，R 11和R 12独立地相同或不同，为H，或直链或支链烷基，烷基芳基，羟基烷基或酰基或芳基; R13是糖基; n为0或1; 条件是当R 1为乙基且n为0时，E，R 2，R 3和R 4不全为H.导致喜树碱类似物的中间体化合物包括取代的三环化合物，其由环C，D和E稠合 一起。 制备类似物的方法涉及这种中间体与可变取代的保护的α-氨基苯甲醛的缩合。

    Asymmetric synthesis of (S,S,R)-(-)-actinonin and its analogs and uses therefor
    8.
    发明授权
    Asymmetric synthesis of (S,S,R)-(-)-actinonin and its analogs and uses therefor 失效
    （S，S，R） - （ - ） - 肌动蛋白及其类似物的不对称合成及其用途

    公开(公告)号：US06660741B2

    公开(公告)日：2003-12-09

    申请号：US10102593

    申请日：2002-03-19

    申请人： William G. Bornmann ,  Francis Sirotnak ,  Howard Scher ,  Ephraim Vidal ,  Christopher Borella ,  David Scheinberg

    发明人： William G. Bornmann ,  Francis Sirotnak ,  Howard Scher ,  Ephraim Vidal ,  Christopher Borella ,  David Scheinberg

    IPC分类号： A61K31497

    CPC分类号： C07D207/08 ,  A61K38/00 ,  C07D207/06 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D403/06 ,  C07K5/06052

    摘要： The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: where R1 is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said R1 further comprising a cyclic or bicyclic structure; R2 is methyl, CH2CH3, (CH2)2CH3, C(CH3)3, phenyl, 3,4-dichiorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH2-(N-Boc-4-piperidine), 4-tetrahydropyran, CH2-4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; R3 is R2 or C3-8alkyl, R4 is C1-3alkyl; and R5 is NH2, OH, NHOH, NHOCH3, N(CH3)OH, N(CH3)OCH3, NHCH2CH3, NH(CH2CH3), NHCH2(2,4-(OCH3)2Ph, NHCH2(4-NO2)Ph, NHN(CH3)2, proline, or 2-hydroxymethyl pyrrolidine. Additionally, a method for the treatment of a neoplastic disease or for the inhibition of tumor cell growth each comprising the step of administering to an individual in need of such treatment a pharmacologically effective dose of the compounds of the present invention are provided.

    摘要翻译： 本发明提供了（S，S，R） - （ - ） - 锕系元素及其类似物的不对称合成方法和由此合成的具有以下结构式的化合物：其中R 1为任选取代或卤化的烷基，芳基 杂杂烷基或杂芳基胺，所述R 1还包含环状或双环结构; R 2是甲基，CH 2 CH 3，（CH 2）2 CH 3，C（CH 3）3，苯基，3,4-二氯苯基，联苯基，苄基，4-羟基苄基，哌啶，N-Boc-4-哌啶， -Boc-4-哌啶），4-四氢吡喃，CH 2 4-四氢吡喃，3-甲基吲哚基，2-萘基，3-吡啶基，4-吡啶基，3-噻吩基; R 3是R 2或C 3-8烷基，R 4是C 1-3烷基; 并且R 5是NH 2，OH，NHOH，NHOCH 3，N（CH 3）OH，N（CH 3）OCH 3，NHCH 2 CH 3，NH（CH 2 CH 3），NHCH 2（2,4-（OCH 3）2 Ph，NHCH 2（4-NO 2） Ph，NHN（CH 3）2，脯氨酸或2-羟甲基吡咯烷。另外，用于治疗肿瘤疾病或抑制肿瘤细胞生长的方法包括向需要这种治疗的个体施用步骤 提供本发明化合物的药理学有效剂量。