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    • 7. 发明专利
      DE10020852A1 Antitumor agents having antimitotic and tubulin polymerization inhibiting action, comprising new or known 2-acyl-indole derivatives or aza analogs 未知
    • Antitumor agents having antimitotic and tubulin polymerization inhibiting action, comprising new or known 2-acyl-indole derivatives or aza analogs
    • DE10020852A1
    • 2001-10-31
    • DE10020852
    • 2000-04-28
    • ASTA MEDICA AG
    • BECKERS THOMAS , BAASNER SILKE , KLENNER THOMAS , MAHBOOBI SIAVOSH , PONGRATZ HERWIG , FRIESER MARKUS , HUFSKY HARALD , HOCKEMEYER JOERG , FIEBIG HEINZ-HERBERT , BURGER ANGELIKA , BOEHMER FRANK-D
    • A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/4709 , C07D209/42 , A61K31/52 , C07D401/02 , C07D471/04 , C07D487/04
    • The use of 2-acyl-indole derivatives (including aza analogs) (I) as antitumor agents is new. Most compounds (I) are new. The use of indole derivatives of formula (I) (including their stereoisomers, tautomers, mixtures and salts) is claimed in the preparation of medicaments for treating tumor diseases. R1 = H, alkylcarbonyl, alkyl, alkylamino-T-, dialkylamino-T- (where the dialkylamino group may form a ring, optionally containing one or more NH, N(alkyl), O or S members), arylalkyl or arylalkoxyalkyl; T = 1-4C alkyl; R2 = H, halo, CN or NO2, alkyl or alkoxy (both optionally substituted (os) by one or more halo), or alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, ST, SOT, SO2T, alkoxyalkyl, NH2, alkylamino, dialkylamino (possibly forming a ring as in R1), aryl, aryloxy, aryl-T-, aryl-T-O-T-, alkylcarbonyl, alkoxycarbonyl or OH; A1-A4 = C-R3 or N; R3 = H, halo, CN or NO2, alkyl or alkoxy (both os by one or more halo); or alkenyl, alkynyl, cycloalkyl, alkoxy, 1-6C alkylenedioxy, alkoxycarbonyloxy, alkylcarbonyloxy, ST, SOT, SO2T, COOH, alkoxycarbonyl, CONH2, CONHT, CON(T)2, alkoxyalkyl, NH2, alkylamino, dialkylamino (possibly forming a ring as in R1), aryl, aryloxy, aryl-T-, aryl-T-O-T-, alkylcarbonyl or OH, or two adjacent R3 groups may be bonded, specifically as 1-6C alkylenedioxy; Y = aryl (preferably phenyl or naphthyl), 1-13C heteroaryl (containing 1-4 of N, NH, N(alkyl), O and/or S as ring members) or cycloalkyl, all os by one or more Q; Q = halo, CN, cyanoalkyl, OH, mono- or polyhydroxyalkyl, COOH, alkoxycarbonyl, CONH2, alkylcarbamoyl, CON(T)2, NO2, alkyl or alkoxy (both os by one or more halo), alkenyl, alkynyl, cycloalkyl, SH, alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxyalkyl, NH2, alkylamino, dialkylamino (possibly forming a ring as in R1), aryl, aryloxy, arylalkyl, arylalkoxyalkyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonyloxy, mono- or dialkylcarbonylamino, mono- or dialkoxycarbonylamino, N-alkylcarbonyl-N-alkylamino, N-alkoxycarbonyl-N-alkylamino, NHCHO or CHO; or two adjacent Q groups may be bonded, specifically as 1-6C alkylenedioxy, and X = O, S, NH or (H, OH); unless specified otherwise, alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C, cycloalkyl moieties 3-8C and aryl moieties 6-14C. Independent claims are included for the following: (a) new (I) (including their stereoisomers, tautomers, mixtures and salts), with the exception of (I; R1, R2 = H; A1, A3, A4 = CH; X = O or (if A2 = CH) CH(OH); Y = 3-carboxy-pyridin-4-yl; A2 = CH or C(OMe)), 2-cyclopropylcarbonyl-indole and 2-cyclohexylcarbonyl-indole; and (b) preparation of the new compounds (I).
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明专利
      DE10102629A1 Antitumor agents having antimitotic and tubulin polymerization inhibiting action, comprising new or known 2-acyl-indole derivatives or aza analogs 未知
    • Antitumor agents having antimitotic and tubulin polymerization inhibiting action, comprising new or known 2-acyl-indole derivatives or aza analogs
    • DE10102629A1
    • 2002-07-25
    • DE10102629
    • 2001-01-20
    • ASTA MEDICA AG
    • BECKERS THOMAS , BAASNER SILKE , KLENNER THOMAS , MAHBOOBI SIAVOSH , PONGRATZ HERWIG , FRIESER MARKUS , HUFSKY HARALD , HOCKEMEYER JOERG , FIEBIG HEINZ-HERBERT , BURGER ANGELIKA , BOEHMER FRANK-D
    • A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/4709 , C07D209/12 , A61K31/519 , A61K31/53 , C07D215/14 , C07D401/06 , C07D471/04 , C07D487/04
    • The use of 2-acyl-indole derivatives (including aza analogs) (I) as antitumor agents is new. Most compounds (I) are new. The use of indole derivatives of formula (I) (including their stereoisomers, tautomers, mixtures and salts) is claimed in the preparation of medicaments for treating tumor diseases. R1 = H, alkylcarbonyl, alkyl, alkylamino-T-, dialkylamino-T- (where the dialkylamino group may form a ring, optionally containing one or more NH, N(alkyl), O or S members), arylalkyl or arylalkoxyalkyl; T = 1-4C alkyl; R2 = H, halo, CN or NO2, alkyl or alkoxy (both optionally substituted (os) by one or more halo), or alkenyl, alkynyl, cycloalkyl, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, ST, SOT, SO2T, alkoxyalkyl, NH2, alkylamino, dialkylamino (possibly forming a ring as in R1), aryl, aryloxy, aryl-T-, aryl-T-O-T-, alkylcarbonyl, alkoxycarbonyl or OH; A1-A4 = C-R3 or N; R3 = H, halo, CN or NO2, alkyl or alkoxy (both os by one or more halo); or alkenyl, alkynyl, cycloalkyl, alkoxy, 1-6C alkylenedioxy, alkoxycarbonyloxy, alkylcarbonyloxy, ST, SOT, SO2T, COOH, alkoxycarbonyl, CONH2, CONHT, CON(T)2, alkoxyalkyl, NH2, alkylamino, dialkylamino (possibly forming a ring as in R1), aryl, aryloxy, aryl-T-, aryl-T-O-T-, alkylcarbonyl or OH, or two adjacent R3 groups may be bonded, specifically as 1-6C alkylenedioxy; Y = aryl (preferably phenyl or naphthyl), 1-13C heteroaryl (containing 1-4 of N, NH, N(alkyl), O and/or S as ring members) or cycloalkyl, all os by one or more Q; Q = halo, CN, cyanoalkyl, OH, mono- or polyhydroxyalkyl, COOH, alkoxycarbonyl, CONH2, alkylcarbamoyl, CON(T)2, NO2, alkyl or alkoxy (both os by one or more halo), alkenyl, alkynyl, cycloalkyl, SH, alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxyalkyl, NH2, alkylamino, dialkylamino (possibly forming a ring as in R1), aryl, aryloxy, arylalkyl, arylalkoxyalkyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonyloxy, mono- or dialkylcarbonylamino, mono- or dialkoxycarbonylamino, N-alkylcarbonyl-N-alkylamino, N-alkoxycarbonyl-N-alkylamino, NHCHO or CHO; or two adjacent Q groups may be bonded, specifically as 1-6C alkylenedioxy, and X = O, S, NH or (H, OH); unless specified otherwise, alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C, cycloalkyl moieties 3-8C and aryl moieties 6-14C. Independent claims are included for the following: (a) new (I) (including their stereoisomers, tautomers, mixtures and salts), with the exception of (I; R1, R2 = H; A1, A3, A4 = CH; X = O or (if A2 = CH) CH(OH); Y = 3-carboxy-pyridin-4-yl; A2 = CH or C(OMe)), 2-cyclopropylcarbonyl-indole and 2-cyclohexylcarbonyl-indole; and (b) preparation of the new compounds (I).
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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