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    Telomerase inhibitors
    2.
    发明授权
    Telomerase inhibitors 失效

    公开(公告)号：US5760062A

    公开(公告)日：1998-06-02

    申请号：US425043

    申请日：1995-04-18

    申请人： Federico C.A. Gaeta ,  Adam A. Galan ,  Michael R. Kozlowski ,  Karen R. Prowse ,  Elaine C. Stracker ,  Patricia A. Peterli-Roth

    发明人： Federico C.A. Gaeta ,  Adam A. Galan ,  Michael R. Kozlowski ,  Karen R. Prowse ,  Elaine C. Stracker ,  Patricia A. Peterli-Roth

    IPC分类号： C07D495/04 ,  A61K31/44 ,  C07D213/57 ,  C07D213/84

    CPC分类号： C07D495/04

    摘要： Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds that are derivatives of pyrido�b!thiophenes, pyrido�b!furans, pyridine ethers or pyridine thioethers. Such compounds are characterized by the following structure: ##STR1## X.sub.3 is oxygen or sulfur; and the double dashed lines between X.sub.4 and X.sub.5 indicate an optional double bond, which, when present, forms a fused, bicyclic pyrido�b!furan or pyrido�b!thiophene ring system, depending upon whether X.sub.3 is oxygen or sulfur, respectively. When the double bond is not present, the compound is a monocyclic pyridine ether or thioether, again depending upon whether X.sub.3 is oxygen or sulfur. X.sub.4 is --CH.sub.2 R.sub.21 or --CR.sub.21 --, where R.sub.21 is selected from the group consisting of aryl, heteroaryl, aralkyl, heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroalkylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylarninocarbonyl, arylalkylaminocarbonyl, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl and arylsulfonyl; and X.sub.5 is hydrogen, alkyl, hydroxyl, alkoxyl, aryloxyl, halogen, cyano, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, arylsulfonyl or --CR.sub.22 -- where R.sub.22 is selected from the group consisting of hydrogen, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, hydroxyl, halogen, cyano, carboxyl, alkoxycarbonyl and aryloxycarbonyl. When X.sub.4 is --CR.sub.21 --, X.sub.5 is --CR.sub.22 --, and X.sub.4 and X.sub.5 are joined by the above-mentioned double bond, to form thereby a fused, bicyclic pyrido�b!thiophene (X.sub.3 is sulfur) or pyrido�b!furan (X.sub.3 is oxygen) ring system. When X.sub.4 is --CH.sub.2 R.sub.21, X.sub.5 is not --CR.sub.22 --, thereby forming a pyridine ether (X.sub.3 is oxygen) or thioether (X.sub.3 is sulfur). R.sub.18 and R.sub.19 are selected independently from the group consisting of hydrogen, halogen, hydroxy, aryloxy, alkoxy, lower alkyl, aryl, heteroaryl, aralkyl and heteroaralkyl. R.sub.20 is selected from the group consisting of alkoxymethyl, dialkoxymethyl, arylalkylaminomethyl, arylaminomethyl, alkylaminomethyl, aminomethyl, diarylaminomethyl, dialkylaminomethyl, hydroximinyl, iminyl, aldehyde, alkylcarbonyl, arylcarbonyl, alkyliminyl, aryliminyl, aralkyliminyl, alkoximinyl, aryloximinyl, heterocycleimninyl, alkoxycarbonyl, aryloxycarbonyl, carboxyl, alkene, --HC.dbd.NNHR.sub.23 where R.sub.23 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, heterocycle, heterocyclealkyl, and --C(X.sub.6)NHR.sub.24 where X.sub.6 is oxygen or sulfur and R.sub.24 is selected from the group consisting of hydrogen, aryl, arylsulfonyl, aralkyl, heterocycle and heterocyclealkyl.

    Telomerase inhibitors
    7.
    发明授权
    Telomerase inhibitors 失效
    端粒酶抑制剂

    公开(公告)号：US5863936A

    公开(公告)日：1999-01-26

    申请号：US549597

    申请日：1995-10-27

    申请人： Federico C.A. Gaeta ,  Adam A. Galan ,  Elaine C. Stracker

    发明人： Federico C.A. Gaeta ,  Adam A. Galan ,  Elaine C. Stracker

    IPC分类号： C07D333/70 ,  C07D495/04 ,  C07D333/64 ,  A61K31/38 ,  C07D333/66

    CPC分类号： C07D495/04 ,  C07D333/70

    摘要： Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds characterized by the following structure: ##STR1## and their pharmaceutically acceptable salts. Y is selected from the group consisting of oxygen, sulfur, sulfonyl, sulfinyl, and --NR.sub.7 --. R.sub.1 is --TR.sub.8, where T is --C(X.sub.1)-- or --SO.sub.2 --, and R.sub.8 is selected from the group consisting of --OR.sub.9, --NHNHSO.sub.2 R.sub.9, --NHNHC(X.sub.2)OR.sub.9, --NR.sub.9 R.sub.10, --NHNHC(X.sub.2)NR.sub.9 R.sub.10, --NHCR.sub.9 R.sub.10 C(X.sub.2)NR.sub.11 R.sub.12, --NHC(X.sub.2)NR.sub.9 R.sub.10, and the piperazinyl moiety shown below: ##STR2## where n is 0 or 1, and Q.sub.n, for n=1, is --SO.sub.2 --, --C(X.sub.2)-- or --C(X.sub.2)NR.sub.10 --. R.sub.2 -R.sub.6 are selected independently from the group consisting of hydrogen, alkyl, aryl, hydroxyl, alkoxyl, aryloxyl, aralkoxyl, halogen, cyano, nitro, alkylcarbamido, arylcarbamido, dialkylcarbamido, diarylcarbamido, alkylarylcarbamido, alkylthiocarbamido, arylthiocarbamido, dialkylthiocarbamido, diarylthiocarbamido, alkylarylthiocarbamido, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, alkylcarbonyloxy, arylcarbonyloxy, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonylamido, arylsulfonylamido, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, and arylsulfinyl. X.sub.1 and X.sub.2 are selected independently from the group consisting of oxygen, and sulfur. R.sub.7 -R.sub.12 are selected independently from the group consisting of hydrogen, alkyl, aryl, aralkyl, heterocycle, and heterocyclealkyl.

    摘要翻译： 用于治疗癌症和其它疾病的方法和组合物，其中端粒酶活性的抑制可以改善疾病症状或预防或治疗该疾病涉及以下结构特征的化合物：其为药学上可接受的盐。 Y选自氧，硫，磺酰基，亚磺酰基和-NR 7 - 。 R 1是-TR 8，其中T是-C（X 1） - 或-SO 2 - ，R 8选自-OR 9，-NHNHSO 2 R 9，-NHNHC（X 2）OR 9，-NR 9 R 10，-NHNHC（X 2）NR 9 R 10 ，-NHCR9R10C（X2）NR11R12，-NHC（X2）NR9R10和如下所示的哌嗪基部分：其中n为0或1，Q n为n = 1时为-SO 2 - ， - C（X 2） - 或-C（X2）NR10-。 R2-R6独立地选自氢，烷基，芳基，羟基，烷氧基，芳氧基，芳烷基，卤素，氰基，硝基，烷基氨基甲酰基，芳基氨基甲酰氨基，二烷基氨基甲酰氨基，二芳基氨基甲酰氨基，烷基芳基氨基甲酰氨基，烷硫基氨基甲酰氨基，芳硫基氨基甲酰氨基，二烷基硫代氨基甲酰氨基，二芳基硫代氨基甲酰基， 氨基，烷基氨基，芳基氨基，二烷基氨基，二芳基氨基，芳基烷基氨基，氨基羰基，烷基氨基羰基，芳基氨基羰基，二烷基氨基羰基，二芳基氨基羰基，芳基烷基氨基羰基，烷基羰基氧基，芳基羰基氧基，羧基，烷氧基羰基，芳氧基羰基，磺基，烷基磺酰基氨基，芳基磺酰基氨基，烷基磺酰基，芳基磺酰基，烷基亚磺酰基和芳基亚磺酰基。 X1和X2独立地选自氧和硫。 R7-R12独立地选自氢，烷基，芳基，芳烷基，杂环和杂环烷基。

    Telomerase inhibitors
    9.
    发明授权
    Telomerase inhibitors 失效

    公开(公告)号：US5767278A

    公开(公告)日：1998-06-16

    申请号：US539934

    申请日：1995-10-06

    申请人： Federico C.A. Gaeta ,  Elaine C. Stracker

    发明人： Federico C.A. Gaeta ,  Elaine C. Stracker

    IPC分类号： C07D213/85 ,  C07D401/12 ,  C07D405/12 ,  A61K31/44 ,  C07D213/32

    CPC分类号： C07D401/12 ,  C07D213/85 ,  C07D405/12

    摘要： Compounds for treating cancer and other diseases involving telomerase activity are characterized by the following structure: ##STR1## Such compounds include those for which X.sub.1 is oxygen, sulfur, sulfone, or sulfinyl, and R.sub.1 is --Y.sub.n R.sub.6, where n is an integer between 0 and 10 and each Y.sub.n independently is methylene, methine, or quaternary carbon. R.sub.6, is alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroalkylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, arninocarbonyl, alkylarninocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, carboxaldehyde, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, or arylsulfinyl. R.sub.6 can also be a linker selected from the group consisting of alkyl, aryl, and heterocycle. R.sub.2 is hydrogen, alkyl, aryl, hydroxyl, alkoxyl, aryloxyl, halogen, cyano, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, alkylcarbonyl, arylcarbonyl, alkylcarbonyloxy, arylcarbonyloxy, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, or arylsulfonyl. R.sub.3 and R.sub.4 independently can be hydrogen, amino, alkylamino, arylamino, heterocycleamino, aralkylamino, dialkylamino, diarylamino, heterocylcealkylamino, alkylcarbonyl, arylcarbonyl, nitro, halogen, hydroxyl, aryloxyl, alkoxyl, lower alkyl, aryl, heteroaryl, aralkyl, cyano, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, or heteroaralkyl. R.sub.5 is selected from the group consisting of iminyl, hydroximinyl, alkyliminyl, aryliminyl, aralkyliminyl, alkoximinyl, aryloximinyl, heterocycleiminyl, and cyclic iminyl. Provided, however, that R.sub.5 is not 4-methylphenyliminyl when X.sub.1 is sulfur, n is 1, Y is methylene, R.sub.2 is cyano, R.sub.3 and R.sub.4 are hydrogen, and R.sub.6 is 4-chlorophenyl.