发明名称 Docosahexaenoyl ethanolamides
摘要 The invention describes novel mono or dihydroxy docosahexaenoic acid (DHA) analogs, their preparation, isolation, identification, purification and uses thereof.
申请公布号 US9416118(B2) 申请公布日期 2016.08.16
申请号 US201214124761 申请日期 2012.06.08
申请人 The Brigham and Women's Hospital, Inc. 发明人 Serhan Charles N.;Yang Rong
分类号 A61K31/335;A61K31/16;C07D303/08;C07D303/46;A61K47/48;C07C235/28;C07K5/02;C07D303/14 主分类号 A61K31/335
代理机构 Christensen Fonder, P.A. 代理人 Christensen Fonder, P.A. ;Fairman Colin L.
主权项 1. A compound comprising one of the formulae selected from (I) through (VIIIa): wherein each of P1 and P2 individually, if present, is a protecting group or a hydrogen atom; wherein is a double bond if present; wherein Z is —C(O)NRcRc, —C(O)NRcRc—OH, —C(NH)NRcRc or —C(S)NRcRc; each Ra, is independently hydrogen, (C1-C6) alkyl, (C3-C8) cycloalkyl, cyclohexyl, (C4-C11) cycloalkylalkyl, (C5-C10) aryl, phenyl, (C6-C16) arylalkyl, benzyl, 2-6 membered heteroalkyl, 3-8 membered cycloheteroalkyl, morpholinyl, piperazinyl, homopiperazinyl, piperidinyl, 4-11 membered cycloheteroalkylalkyl, 5-10 membered heteroaryl or 6-16 membered heteroarylalkyl; each Rc, is independently a protecting group or Ra, or, alternatively, each Rc is taken together with the nitrogen atom to which it is bonded to form a 5 to 8-membered cycloheteroalkyl or heteroaryl which may optionally have one or more of the same or different additional heteroatoms and which may optionally be substituted with one or more of the same or different Ra or suitable Rb groups; each Rb is independently ═O, —ORd, (C1-C3) haloalkyloxy, —OCF3, ═S, —SRd, ═NRd, ═NORd, —NRcRc, halogen, —CF3, —CN, —NC, —OCN, —SCN, —NO, —NO2, ═N2, —N3, —S(O)Rd, —S(O)2Rd, —S(O)2ORd, —S(O)NRcRc, —S(O)2NRcRc, —OS(O)Rd, —OS(O)2Rd, —OS(O)2ORd, —OS(O)2NRcRc, —C(O)Rd, —C(O)ORd, —C(O)NRcRc, —C(NH)NRcRc, —C(NRa)NRcRc, —C(NOH)Ra, —C(NOH)NRcRc, —OC(O)Rd, —OC(O)ORd, —OC(O)NRcRc, —OC(NH)NRcRc, —OC(NRa)NRcRc, —[NHC(O)]nRd, —[NRaC(O)]nRd, —[NHC(O)]nORd, —[NRaC(O)]nORd, —[NHC(O)]nNRcRc, —[NRaC(O)]nNRcRc, —[NHC(NH)]nNRcRc or —[NRaC(NRa)]nNRcRc; each n, independently is an integer from 0 to 3; and each Rd, independently is a protecting group or Ra; or a pharmaceutically acceptable salt thereof.
地址 Boston MA US