发明名称 Phosphorus-containing compounds and uses thereof
摘要 This disclosure concerns a new family of phosphorus-containing compounds of Formula (I):; and pharmaceutically acceptable derivatives thereof. Compositions containing such compounds and uses thereof are also provided.
申请公布号 US9024014(B2) 申请公布日期 2015.05.05
申请号 US201113295826 申请日期 2011.11.14
申请人 Ariad Pharmaceuticals, Inc. 发明人 Berstein David L.;Rozamus Leonard W.;Wang Yihan;Metcalf, III Chester A.
分类号 C07D267/00;A61K45/06;A61K31/675;C07F9/6561 主分类号 C07D267/00
代理机构 Garrett & Duncan LLP 代理人 Garrett & Duncan LLP
主权项 1. A method for treating endometrial or colorectal cancer in a subject in need thereof by administering to the subject a treatment effective amount of a compound of the formula:or a pharmaceutically acceptable salt thereof, wherein: A is —O—, —S— or —NR2— or is absent; Q is absent or, if A is —O—, —S—or —NR2—, Q is absent or is —V—, —OV—, —SV—, or —NR2V—, where V is an unsubstituted aliphatic, heteroaliphatic, aryl, or 5-14 membered heteroaryl moiety having 1-4 heteroatoms selected from nitrogen, oxygen, or sulfur, such that J is linked to the cyclohexyl ring directly, through A, or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, or —NR2—, or is absent; each occurrence of R2 and R5 is independently H or an aliphatic, a heteroaliphatic, an aryl, or a 5-14 membered heteroaryl moiety having 1-4 heteroatoms selected from nitrogen, oxygen, or sulfur; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2 or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; wherein each aliphatic moiety contains 1 -8 contiguous aliphatic carbon atoms, each heteroaliphatic moiety is an aliphatic moiety which contains an O, S, N, P or Si atom in place of one or more carbon atoms, and each of the foregoing aliphatic and heteroaliphatic moieties is independently linear or branched, or cyclic or acyclic, and unsubstituted or substituted with one or more groups selected from halogen, —YR2, —Y—C(═O)R2, —NR2C(═O)R5, —NR2C(═O)NR5, —NR2C(═O)OR5, —NR2C(═NH)NR5, —Y—C(═O)OR2, —Y—C(═O)NR2R5, —Y—C(═NR2)NR2R5, —COCOR2, —COMCOR2, J, —CN, —S(═O)R2, —SO2R2, —SO2NR2R5, —NO2, —NR5SO2R2—NR5SO2NR2R, ═O, ═S, ═NR2, ═NNR2R5, ═NNHC(O)R2, ═NNHCO2R2, and ═NNHSO2R2, and each of the aryl, heteoraryl, acyl, aroyl or heteroaroyl moieties is independently unsubstituted or substituted with one or more groups selected from halogen, —YR2, —Y—C(═O)R2, —NR2C(═O)R5, —NR2C(═O)NR5, —NR2C(═O)OR5, —NR2C(═NH)NR5 —Y—C(═O)OR2, —Y—C(═O)NR2R5, —Y—C(═NR2)NR2R5, —COCOR2, —COMCOR2, J, —CN, —S(═O)R2, —SO2R, —SO2NR2R5, —NO2, —NR5SO2R2, and —NR5SO2NR2R; with the proviso that: J-Q-A- is not (HO)2(P═O)O—or (MeO)2(P═O)O—.
地址 Cambridge MA US