发明名称 Guanine analogs as telomerase substrates and telomere length affectors
摘要 This invention relates to compounds useful for inhibiting telomere elongation. More specifically, the invention provides nucleotide analogs that are incorporated into telomeres by telomerase thereby inhibiting elongation of telomeres. The compounds are useful in treating cancer and other cell proliferative diseases.
申请公布号 US9593137(B2) 申请公布日期 2017.03.14
申请号 US201214366218 申请日期 2012.12.21
申请人 Geron Corporation 发明人 Gryaznov Sergei M.;Pruzan Ronald A.;Pongracz Krisztina
分类号 C07D473/18;C07F9/6561 主分类号 C07D473/18
代理机构 Bozicevic, Field & Francis LLP 代理人 Foulds Glenn J.;Francis Carol L.;Bozicevic, Field & Francis LLP
主权项 1. A compound of formula (I): wherein R1 and R2 are independently selected from —NR1aR1b and OR1c; wherein R1a and R1b are independently selected from hydrogen, optionally substituted C1-20alkyl, optionally substituted polyamine, and —CH(R1d)—C(O)OR1e, wherein R1d is selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, and substituted heteroarylalkyl; andR1e is hydrogen or C1-6alkyl;R1c is selected from hydrogen, alkyl, and aryl; wherein at least one of R1 and R2 is —NR1aR1b; wherein R1 is different from R2: R3a and R3b are independently selected from hydrogen and halo; W is O, S, or NH; R4 is selected from hydrogen, —OH, —NH2, N3, —CH═CH2, and optionally substituted C1-2 alkyl, wherein alkyl is optionally substituted with —OH, —NH2, N3, or halogen; R5a and R5b are independently selected from hydrogen, —OH, —NH2, N3, —CH═CH2, and optionally substituted C1-2 alkyl, wherein alkyl is optionally substituted with —OH, —NH2, N3, or halogen; or R4 is selected from hydrogen, —OH, —NH2, N3, —CH═CH2, and optionally substituted C1-2 alkyl, wherein alkyl is optionally substituted with —OH, —NH2, N3, or halogen; R5a is selected from hydrogen —OH, —NH2, N3, —CH═CH2, and optionally substituted C1-2 alkyl, wherein alkyl is optionally substituted with —OH, —NH2, N3, or halogen; and R5b is selected from —OH, —NH2, N3, —CH═CH2, and optionally substituted C1-2 alkyl, wherein alkyl is optionally substituted with —OH, —NH2, N3, or halogen; R7 is hydrogen or fluoro; and X is O or S; or a salt or a tautomer thereof.
地址 Menlo Park CA US