Carbamate and thiocarbamate podophyllotoxin derivatives, preparation method and pharmaceutical compositions containing them
    1.
    发明授权
    Carbamate and thiocarbamate podophyllotoxin derivatives, preparation method and pharmaceutical compositions containing them 失效
    氨基甲酸酯和硫代氨基甲酸酯鬼臼毒素衍生物,制备方法和含有它们的药物组合物

    公开(公告)号:US06878746B2

    公开(公告)日:2005-04-12

    申请号:US10312175

    申请日:2001-06-19

    CPC分类号: C07D493/04 Y02P20/55

    摘要: A compound selected from these of formula (I): wherein: R1 represents hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl or phosphono, R2 represents oxygen or sulphur, R3 represents hydrogen or alkyl, cycloalkyl or arylalkyl, X represents linear or branched (C1-C6)alkylene, R4 represents a group selected from amino optionally substituted by one or two groups, —N(R3)—X1—OR5 wherein R3, X1 and R5 are as defined in the description, —N(R3)—X1—NR6R7 wherein R3, X1, R6 and R7 are as defined in the description, hydroxy, alkoxy, aryloxy, —O—X1—OR5 wherein R5 and X1 are as defined in the description, and —O—X1—NR6R7 wherein R6, R7 and X1 are as defined in the description, its isomers, and also addition salts thereof with a pharmaceutically acceptable acid or base, and medical products containing the same which are useful in the treatment of cancer.

    摘要翻译: 选自这些式(I)的化合物:其中:R1表示氢,烷基,芳基,芳基烷基,杂芳基,杂芳基烷基,烷氧基羰基,芳氧基羰基,芳基烷氧基羰基,杂环烷氧基羰基,烷基磺酰基,芳基磺酰基,芳基烷基磺酰基或膦酰基,R2表示氧或硫,R3 表示氢或烷基,环烷基或芳基烷基,X表示直链或支链(C1-C6)亚烷基,R4表示选自任选被一个或两个基团取代的氨基的基团-N(R3)-X1-OR5,其中R3,X1和 R 5如说明书中所定义,-N(R3)-X1-NR6R7,其中R3,X1,R6和R7如说明书中所定义,羟基,烷氧基,芳氧基,-O-X1-OR5,其中R5和X1为 和-O-X 1 -NR 6 R 7,其中R 6,R 7和X 1如说明书中所定义,其异构体及其与药学上可接受的酸或碱的加成盐,以及含有它们的医药产品可用 在治疗癌症。

    9-(3,5-dimethoxyphenyl)-5,8,8a,9-tetrahydrofuro-[3′,4′:6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one compounds
    2.
    发明授权
    9-(3,5-dimethoxyphenyl)-5,8,8a,9-tetrahydrofuro-[3′,4′:6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one compounds 失效
    9-(3,5-二甲氧基苯基)-5,8,8a,9-四氢呋喃(3',4':6,7)萘并(2,3-d)(1,3)二氧杂环戊烯-6(5aH) 一种化合物

    公开(公告)号:US06281198B1

    公开(公告)日:2001-08-28

    申请号:US09697248

    申请日:2000-10-26

    IPC分类号: A61K31365

    CPC分类号: C07D493/04 Y02P20/55

    摘要: Compound of formula (I): wherein: R represents: a group of formula (i):  wherein X, Y and W are as defined in the description, or a group of formula (ii): —A—G  (ii) wherein: A represents a single bond or an optionally substituted alkylene chain, G represents a group selected from hydrogen, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, —OR2, —O—T1—NR3R4, —O—T1—NR2—T′1—NR3R4, —NR3R4, —NR2—T1—NR3R4, —NR2—T1—OR5, —NR2—T1—CO2R6, —NR2—T1—C(O)R6, —C(O)—NR3R4, —C(O)—NR2—T2, —O—C(O)T2, —O—C(S)—T2, —NR2—C(O)—T2, —NR2—C(S)—T2, —O—C(O)—O—T2, —O—C(O)—NR2—T2, —O—C(S)—O—T2, —O—C(S)—NR2—T2, —NR2—C(O)—O—T2, —NR2—C(O)—NR—T2, —NR2—C(S)—O—T2, —NR2—C(S)—NR6—T2 and —NR2—SO2—T3,  wherein R2, R3, R4, R5, R6, T1, T′1, T2 and T3 are as defined in the description, R1 represents a group selected from hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, heterocycloalkylcarbonyl, alkylsulphonyl, arylsulphonyl, arylalkylsulphonyl, phosphono, aryloxycarbonyl, alkoxycarbonyl and arylalkoxycarbonyl, its isomers, and also addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of cancer.

    摘要翻译: 式(I)的化合物:其中:R表示:式(ⅰ)的基团:其中X,Y和W如说明书中所定义,或式(ⅱ)的基团:其中:A表示单键或 任选取代的亚烷基链,G表示选自氢,环烷基,杂环烷基,芳基,杂芳基,-OR2,-O-T1-NR3R4,-O-T1-NR2-T'1-NR3R4,-NR3R4,-NR2 -T 1 -NR 3 R 4,-NR 2 -T 1 -OR 5,-NR 2 -T 1 -CO 2 R 6,-NR 2 -T 1 -C(O)R 6,-C(O)-NR 3 R 4,-C(O)-NR 2 -T 2,-OC (O)T 2,-OC(S)-T 2,-NR 2 -C(O)-T 2,-NR 2 -C(S)-T 2,-OC(O)-O-T 2,-OC(O) -T 2,-OC(S)-O-T2,-OC(S)-NR2-T2,-NR2-C(O)-O-T2,-NR2-C(O)-NR-T2, C(S)-O-T2,-NR2-C(S)-NR6-T2和-NR2-SO2-T3,其中R2,R3,R4,R5,R6,T1,T'1,T2和T3为 R 1表示选自氢,烷基,芳基,芳基烷基,杂芳基,杂芳基烷基,烷基羰基,芳基羰基,芳基烷基羰基,杂环烷基羰基,烷基磺酰基,芳基磺酰基,芳基烷基磺酰基,膦酰基,芳氧基羰基,烷氧基羰基和 芳基烷氧基羰基,其异构体,以及其与药学上可接受的酸或碱的加成盐。含有该化合物的药物可用于治疗癌症。

    12,13-(pyranosyl)-indolo[2,3-a]pyrrolo[3,4-c]carbazole and 12,13-(pyranosyl)-furo[3,4-c]indolo[2,3-a]carbazoles
    3.
    发明授权
    12,13-(pyranosyl)-indolo[2,3-a]pyrrolo[3,4-c]carbazole and 12,13-(pyranosyl)-furo[3,4-c]indolo[2,3-a]carbazoles 失效
    12,13-(吡喃糖基) - 吲哚并[2,3-a]吡咯并[3,4-c]咔唑和12,13-(吡喃糖基) - 呋喃并[3,4-c]吲哚并[2,3-a] 咔唑

    公开(公告)号:US06569858B2

    公开(公告)日:2003-05-27

    申请号:US10010379

    申请日:2001-11-05

    IPC分类号: C07D49044

    CPC分类号: C07H19/23

    摘要: A compound selected from those of formula (I): wherein: R1 and R2, which may be identical or different, represent a group of formula U-V wherein U represents single bond, or alkylene which is optionally substituted and/or unsaturated, and V is as defined in the description, G represents oxygen, or NR3 wherein R3 is as defined in the description, X represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y represents hydrogen, or X+Y represents carbonyl, X1 represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1 represents hydrogen, or X1+Y1 represents carbonyl, R4, R5, and R6 are as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same are useful in the treatment of cancer.

    摘要翻译: 选自式(I)的化合物:其中:R 1和R 2可以相同或不同,表示其中U表示单键的式UV基团,或任选被取代和/或不饱和的亚烷基,V是 G表示氧或NR 3,其中R3如说明书中所定义,X表示氢,羟基,烷氧基,巯基或烷硫基,Y表示氢,或X + Y表示羰基,X1表示氢,羟基, 烷氧基,巯基或烷硫基,Y1表示氢,或X1 + Y1表示羰基,R4,R5和R6如说明书中所定义,其异构体及其药学上可接受的酸或碱加成盐,以及含有它们的药物 可用于治疗癌症。

    Compounds of 7-oxo-2,3,7,14-tetrahydro-1H-benzo[b]pyrano[3,2-h]acridin carboxylate
    4.
    发明授权
    Compounds of 7-oxo-2,3,7,14-tetrahydro-1H-benzo[b]pyrano[3,2-h]acridin carboxylate 失效
    7-氧代-2,3,7,14-四氢-1H-苯并[b]吡喃并[3,2-h]吖啶羧酸酯的化合物

    公开(公告)号:US06503919B1

    公开(公告)日:2003-01-07

    申请号:US09594853

    申请日:2000-06-15

    IPC分类号: C07D491052

    CPC分类号: C07D491/04

    摘要: A compound selected from those of formula (I): wherein: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted amino, R3 and R4 represent hydrogen, or alkyl, R5 and R6 represent —O—CO—U—V wherein U and V are as defined in the description, or Z as defined in the description, it being understood that at least one of the R5 and R6 groups represents —O—CO—U—V, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.

    摘要翻译: 选自式(I)的化合物:其中:X和Y表示氢,卤素,羟基,巯基,氰基,硝基,烷基,烷氧基,三卤代烷基,任选取代的氨基,亚甲二氧基或亚乙二氧基, ,R 2表示氢,羟基,烷基,烷氧基,烷基羰基氧基或任选取代的氨基,R 3和R 4表示氢或烷基,R 5和R 6表示-O-CO-UV,其中U和V如说明书中所定义,或Z 可以理解的是,R 5和R 6基团中的至少一个表示-O-CO-UV,它们的异构体,N-氧化物及其药学上可接受的酸或碱加成盐,以及含有 相同的可用于治疗癌症。

    Dihydrofuro[3,4-b]quinolin-1-one compounds
    5.
    发明授权
    Dihydrofuro[3,4-b]quinolin-1-one compounds 失效
    二氢呋喃并[3,4-b]喹啉-1-酮化合物

    公开(公告)号:US06548515B1

    公开(公告)日:2003-04-15

    申请号:US09718917

    申请日:2000-11-22

    IPC分类号: A61K314741

    摘要: The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or  wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its optical isomers, its hydrates, solvates, and also its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same are useful in the treatment of cancer.

    摘要翻译: 本发明涉及式(I)的化合物:其中:表示单键或双键,R 0表示氢或羟基或烷氧基,R 1和R 2相同或不同,各自表示氢或卤素或烷基,烷氧基,羟基,多卤代烷基,硝基或任选取代的氨基或 其中m表示1≤= m = 4的整数,或与带有带有5至12个环成员的芳族或非芳族单环或双环基团的碳原子一起形成,并且任选地含有1或 2个选自O,S和N的杂原子,R 3表示氢或芳基,杂芳基,环烷基,任选取代的烷基或式COR7基团,其中R7表示芳基,任选取代的烷基,任选取代的氨基或OR 10,其中R 10表示芳基或任选地 取代的烷基,X表示氧或硫或-CH 2 - 或-CH 2-CH 2 - ,Ar表示芳基,杂芳基或芳基烷基,其光学异构体,其水合物,溶剂合物,以及其与药学上可接受的酸的加成盐。含有它们的医药产品可用于治疗癌症。

    Acronycine derivatives, preparation method and pharmaceutical compositions
    6.
    发明授权
    Acronycine derivatives, preparation method and pharmaceutical compositions 失效
    Acronycine衍生物,制备方法和药物组合物

    公开(公告)号:US06288073B1

    公开(公告)日:2001-09-11

    申请号:US09581853

    申请日:2000-06-19

    IPC分类号: A61K314741

    CPC分类号: C07D491/04 C07D491/14

    摘要: A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.

    摘要翻译: 选自式(I)的化合物:其中:X和Y表示氢,卤素,羟基,巯基,氰基,硝基,烷基,烷氧基,三卤代烷基,任选取代的氨基,亚甲二氧基或亚乙二氧基, 烷基,R 2表示氢,羟基,烷基,烷氧基,烷基羰基氧基或任选取代的氨基,R3和R4表示氢或烷基,A表示-CH = CH-或-CH(R5)-CH(R6) - ,其中R5 和R6如说明书中所定义,它们的异构体,N-氧化物及其药学上可接受的酸或碱加成盐,以及其可用于治疗癌症的药物。