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40 条记录 (耗时 0.042 秒)

    Telomerase inhibitors
    1.
    发明授权
    Telomerase inhibitors 失效

    公开(公告)号：US5656638A

    公开(公告)日：1997-08-12

    申请号：US554788

    申请日：1995-11-07

    申请人： Federico C. A. Gaeta ,  Elaine C. Stracker ,  Patricia A. Peterli-Roth

    发明人： Federico C. A. Gaeta ,  Elaine C. Stracker ,  Patricia A. Peterli-Roth

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

    CPC分类号： C07D333/70 ,  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 characterized by the following structure: ##STR1## and its pharmaceutically acceptable salts. Z is selected from the group consisting of oxygen, sulfur, sulfone, sulfinyl and --NR--, where R selected from the group consisting of hydrogen, alkyl, aryl, and aralkyl. R.sub.1 is --Y.sub.n R.sub.6, where n is an integer between 0 and 10 and each Y.sub.n for n greater than 0 independently is methylene, methine, or quaternary carbon, and R.sub.6, for any value of n, is alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroalkylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, or arylsulfinyl. R.sub.2 is hydrogen, alkyl, aryl, hydroxyl, alkoxyl, aryloxyl, halogen, cyano, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, alkylcarbonyloxy, arylcarbonyloxy, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, or arylsulfonyl. R.sub.3 and R.sub.4 are selected independently from the group consisting of hydrogen, amino, alkylamino, arylamino, heterocycleamino, aralkylamino, heterocylcealkylamino, dialkylamino, diarylamino, arylalkylamino, nitro, halogen, hydroxyl, aryloxyl, alkoxyl, lower alkyl, aryl, heteroaryl, aralkyl, cyano, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, and heteroaralkyl. Finally, R.sub.5 is selected from the group consisting of iminyl, hydroximinyl, alkyliminyl, aryliminyl, aralkyliminyl, alkoximinyl, aryloximinyl, heterocycleiminyl, cyclic iminyl, bis(alkylthio)methyl, bis(arylthio)methyl, bis(alkoxy)methyl, bis(aryloxy)methyl, carboxaldehyde, hydroxymethyl, alkoxymethyl, aryloxymethyl, aralkoxymethyl, heterocycleoxymethyl, heterocyclealkoxymethyl, and --HC.dbd.NNHR.sub.7 where R.sub.7 is selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, heterocycle, heterocyclealkyl, and --C(.dbd.X.sub.1)(X.sub.2).sub.p R.sub.8 where p is 0 or 1, X.sub.1 is oxygen or sulfur, X.sub.2 is selected from the group consisting of oxygen, sulfur, and --NR.sub.9 --, where R.sub.8 and R.sub.9 are selected independently from the group consisting of hydrogen, alkyl, aryl, aralkyl, and heterocycle.

    Telomerase inhibitors
    2.
    发明授权
    Telomerase inhibitors 失效

    公开(公告)号：US5770613A

    公开(公告)日：1998-06-23

    申请号：US535988

    申请日：1995-09-29

    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 ,  A61K31/44 ,  C07D213/64 ,  C07D213/643

    CPC分类号： C07D213/85

    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 pyridine aldehydes, thioaldehyde, acetals, or thioacetals. Such compounds are characterized by the following structure: ##STR1## X.sub.1 is selected from the group consisting of oxygen, sulfur, sulfone, sulfinyl, and --NR-- where R is hydrogen, alkyl, aryl, and aralkyl. R.sub.1 is --Y.sub.n R.sub.6, in which n is an integer between 0 and 10 and each Y.sub.n for n greater than 0 independently is methylene, methine, or quarternary carbon. R.sub.6, for any value of n (i.e., n is zero or non-zero), is alkyl, aryl, heterocycle, heteroaryl, aralkyl, heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroarylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, alkoxycarbonyl, aryloxycarbonyl, alkylcarbonyloxy, arylcarbonyloxy, aldehyde, sulfo, alkylsulfinyl, arylsulfinyl, alkylsulfonyl, and arylsulfonyl. R.sub.6 can also be a linker L selected from the group consisting of alkyl, aryl, aralkyl, heterocycle, and heterocyclealkyl, to which linker between 1 and 3 additional compounds having the structure shown as Compound I above are attached to form thereby homogeneous or heterogeneous poly pyridine aldehydes, acetals, or thioacetals as described in greater detail below. R.sub.2 is hydrogen, alkyl, aryl, hydroxyl, alkoxyl, aryloxyl, halogen, cyano, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, alkoxycarbonyl, aryloxycarbonyl, alkylcarbonyloxy, arylcarbonyloxy, aldehyde, sulfo, alkylsulfinyl, arylsulfinyl, alkylsulfonyl, or arylsulfonyl. R.sub.3 and R.sub.4 are selected independently from the group consisting of hydrogen, halogen, hydroxyl, aryloxyl, alkoxyl, lower alkyl, aryl, heteroaryl, aralkyl, cyano, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, heteroaralkyl, nitro, amino, alkylamino, arylamino, dialkylamino, diarylamino, and arylalkylamino. Finally, R.sub.5 is selected from the group consisting of bis(alkoxy)methyl, bis(alkylthio)methyl, and --HC.dbd.X.sub.2, where X.sub.2 is oxygen or sulfur.

    Telomerase Inhibitors
    3.
    发明授权
    Telomerase Inhibitors 失效
    端粒酶抑制剂

    公开(公告)号：US5703116A

    公开(公告)日：1997-12-30

    申请号：US424813

    申请日：1995-04-18

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

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

    IPC分类号： C07D495/04 ,  A61K31/38 ,  C07D333/56

    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 benzo�b!thiophenes. Such compounds are characterized by the following structure: ##STR1## In this compound, R.sub.1 is selected from the group consisting of --OR.sub.7, --NR.sub.8 R.sub.9, --NHNR.sub.10 R.sub.11, --NHNHC(X.sub.2)NHR.sub.12, --NHSO.sub.2 NR.sub.8 R.sub.9, --NHNHC(O)R.sub.12, --NHNHSO.sub.2 R.sub.12 and --NHC(O)NR.sub.8 R.sub.9. R.sub.7 -R.sub.12 are selected independently from the group consisting of hydrogen, alkyl, aryl, aralkyl, heteroaryl and heteroaralkyl. X.sub.1 and X.sub.2 are selected independently from the group consisting of oxygen and sulfur. R.sub.2 is hydrogen or halogen. R.sub.3 -R.sub.6 are selected independently from the group consisting of hydrogen, halogen, hydroxyl, --NR.sub.8 R.sub.9, nitro, cyano, alkoxyl, lower alkyl, aryl and aryloxyl.

    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作为苯并[b]噻吩衍生物的化合物。 这种化合物的特征在于以下结构：在该化合物中，R 1选自-OR 7，-NR 8 R 9，-NHNR 10 R 11，-NHNHC（X 2）NHR 12，-NHSO 2 NR 8 R 9，-NHNHC（O）R 12， -NHNHSO 2 R 12和-NHC（O）NR 8 R 9。 R7-R12独立地选自氢，烷基，芳基，芳烷基，杂芳基和杂芳烷基。 X1和X2独立于氧和硫组成的组中选择。 R2是氢或卤素。 R3-R6独立地选自氢，卤素，羟基，-NR8R9，硝基，氰基，烷氧基，低级烷基，芳基和芳氧基。

    Method for identifying and killing cancer cells
    4.
    发明授权
    Method for identifying and killing cancer cells 有权
    识别和杀死癌细胞的方法

    公开(公告)号：US07402307B2

    公开(公告)日：2008-07-22

    申请号：US10208243

    申请日：2002-07-30

    申请人： Federico C. A. Gaeta

    发明人： Federico C. A. Gaeta

    IPC分类号： A01N63/00 ,  C12N5/06

    CPC分类号： C12N9/1241 ,  A61K38/00 ,  A61K39/0011 ,  A61K2039/5154 ,  A61K2039/5158 ,  A61K2039/55522 ,  C12N9/1276

    摘要： The invention provides a method for activating a T lymphocyte by contacting the T lymphocyte with a dendritic cell (DC) that presents a telomerase reverse transcriptase (TRT) peptide in the context of an MHC class I or MHC class II molecule. The DC may be pulsed with a TRT polypeptide or may comprise a recombinant polynucleotide encoding a TRT such as hTRT. The invention also provides DCs comprising a recombinant TRT polynucleotide. The methods and compositions of the invention are used in prevention and treatment of cancers and other cell proliferation diseases or conditions.

    摘要翻译： 本发明提供了通过使T淋巴细胞与MHC I类或II类分子的上下文中呈现端粒酶逆转录酶（TRT）肽的树突状细胞（DC）接触来激活T淋巴细胞的方法。 DC可以用TRT多肽脉冲，或者可以包含编码TRT的重组多核苷酸，例如hTRT。 本发明还提供了包含重组TRT多核苷酸的DC。 本发明的方法和组合物用于预防和治疗癌症和其它细胞增殖疾病或病症。

    Cellular telomerase vaccine and its use for treating cancer
    10.
    发明授权
    Cellular telomerase vaccine and its use for treating cancer 有权
    细胞端粒酶疫苗及其用于治疗癌症

    公开(公告)号：US07824849B2

    公开(公告)日：2010-11-02

    申请号：US11413838

    申请日：2006-04-27

    申请人： Federico C. A. Gaeta

    发明人： Federico C. A. Gaeta

    IPC分类号： C12Q1/00

    CPC分类号： C12N9/1241 ,  A61K38/00 ,  A61K39/0011 ,  A61K2039/5154 ,  A61K2039/5158 ,  A61K2039/55522 ,  C12N9/1276

    摘要： The invention provides dendritic cell (DC) preparations that present a telomerase reverse transcriptase (TRT) peptide in the context of an MHC class I or MHC class II molecule. The DCs may be pulsed with a TRT polypeptide, or may comprise a recombinant polynucleotide encoding TRT. The invention also describes the use of such compositions for the prevention and treatment of cancers and other diseases.

    摘要翻译： 本发明提供了在MHC I类或II类分子的上下文中提供端粒酶逆转录酶（TRT）肽的树突状细胞（DC）制剂。 DC可以用TRT多肽脉冲，或者可以包含编码TRT的重组多核苷酸。 本发明还描述了这种组合物用于预防和治疗癌症和其它疾病的用途。