发明名称 THERAPEUTIC BISPHOSPHONATES
摘要 The invention provides novel pyrophosphate synthase inhibitors of formula I and formula II as well salts thereof; the invention also provides compositions comprising such inhibitors and methods for their use.;
申请公布号 US2015322099(A1) 申请公布日期 2015.11.12
申请号 US201314412578 申请日期 2013.07.03
申请人 UNIVERSITY OF IOWA RESEARCH FOUNDATION 发明人 Wiemer David
分类号 C07F9/38;C07F9/6506;C07F9/653 主分类号 C07F9/38
代理机构 代理人
主权项 1. A compound of formula I or formula II:wherein: X is (C1-C6)alkyl; Y is (C1-C6)alkyl; R1 is a saturated or unsaturated (C1-C20)alkyl chain that optionally comprises one or more aryl or heteroaryl rings in the chain wherein (C1-C20)alkyl is optionally substituted with one or more halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, NRmRa, or S(O)2NRpRq and wherein any aryl or heteroaryl is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRaRb, or S(O)2NRcRd; R2 is H or a saturated or unsaturated (C1-C20)alkyl chain that optionally comprises one or more aryl or heteroaryl rings in the chain wherein (C1-C20)alkyl is optionally substituted with one or more halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, NRmRn, or S(O)2NRpRq and wherein any aryl or heteroaryl is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRaRb, or S(O)2NRcRd; each R3, R4, R5, and R6 is independently OH or (C1-C6)alkoxy; R7 is a saturated or unsaturated (C1-C20)alkyl chain that optionally comprises one or more aryl or heteroaryl rings in the chain wherein (C1-C20)alkyl is optionally substituted with one or more halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, NRmRn, or S(O)2NRpRq and wherein any aryl or heteroaryl is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRaRb, aryl, heteroaryl, or S(O)2NRcRd; R8 is a saturated or unsaturated (C1-C20)alkyl chain that optionally comprises one or more aryl or heteroaryl rings in the chain wherein (C1-C20)alkyl is optionally substituted with one or more halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, NRmRn, or S(O)2NRpRq and wherein any aryl or heteroaryl is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRaRb, aryl, heteroaryl, or S(O)2NRcRd; R9 is a saturated or unsaturated (C1-C20)alkyl chain that optionally comprises one or more aryl or heteroaryl rings in the chain wherein (C1-C20)alkyl is optionally substituted with one or more halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, NRmRn, or S(O)2NRpRq and wherein any aryl or heteroaryl is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRaRb, or S(O)2NRcRd; R10 is H or a saturated or unsaturated (C1-C20)alkyl chain that optionally comprises one or more aryl or heteroaryl rings in the chain wherein (C1-C20)alkyl is optionally substituted with one or more halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, aryl, heteroaryl, NRmRn, or S(O)2NRpRq and wherein any aryl or heteroaryl is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRaRb, or S(O)2NRcRd; each Ra and Rb is independently H, (C1-C6)alkyl, or aryl; or Ra and Rb together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino, or thiomorpholino ring; each and Rd is independently H, (C1-C6)alkyl, or aryl; or Rc and Rd together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino, or thiomorpholino ring; each Rm and Rn is independently H, (C1-C6)alkyl, or aryl; or Rm and Rn together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino, or thiomorpholino ring; each Rp and Rq is independently H, (C1-C6)alkyl, or aryl; or Rp and Rq together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino, or thiomorpholino ring; and wherein any aryl of Ra, Rb, Rc, Rd, Rm, Rn, Rp or Rq is optionally substituted with one or more (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NRsRt, or S(O)2NRsRt wherein each Rs and Rt is independently H or (C1-C6)alkyl; or a salt thereof.
地址 Iowa City IA US