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Resolvins: biological models for therapeutic interventions

机译:Resolvins:用于治疗干预的生物学模型

摘要

Compound having a structure of the formula: ** Formula ** in which P1 and P2 each individually is a hydrogen atom or a hydroxyl protecting group selected from an acyl group, an alkyl group, a tetrahydropyranyl group, a trialkylsilyl group, a glycol group and an allyl group; Z is -C (O) ORd, -C (O) NRcRc, -C (O) H, -C (NH) NRcRc, -C (S) H, -C (S) ORd, -C (S) NRcRc or -CN; each Ra is independently selected from hydrogen, (C1-C6) alkyl, cycloalkyl (C3-C8), cyclohexyl, cycloalkylalkyl (C4-C11), aryl (C5-C10), phenyl, arylalkyl (C6-C16), benzyl, 2 to 6 membered heteroalkyl, 3 to 8 membered cycloheteroalkyl, morpholinyl, piperazinyl, homopiperazinyl, piperidinyl, cycloheteroalkylalkyl of 4 to 11 members, heteroaryl of 5 to 10 members and heteroarylalkyl of 6 to 16 members; each Rb is a suitable group independently selected from = O, -ORd, haloalkyloxy (C1-C3), -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) Rd, -OC (O ) NRcRc, -OC (NH) NRcRc, -OC (NRa) NRcRc, - [NHC (O)] nRd, - [NRaC (O)] nRd, - [NHC (O)] nORd, - [NRaC (O) ] nORd, - [NRaC (O)] nNRcRc, - [NRaC (O)] nNRcRc, - [NHC (NH)] nNRcRc and - [NRaC (NRa)] nNRcRc; each Rc is independently a protective group or Ra, or, alternatively, each Rc is taken together with the nitrogen atom to which it is attached to form a 5- to 8-membered cycloheteroalkyl or heteroaryl which may optionally include one or more of the heteroatoms same or different additional ones and which may optionally be substituted with one or more of the same or different Ra groups or suitable Rb; each Rd is independently a protective group or Ra; and each n is independently an integer from 0 to 3, in which any carbon-carbon double bond can be cis or trans, or a pharmaceutically acceptable salt thereof, in which the protective group represented by Rc and Rd is independently selected. from allyl 2-trimethylsilyl-ethanesulfonyl formyl, acetyl, trifluoroacetyl, benzyl, benzyloxycarbonyl, tert-butoxycarbonyl, trimethylsilyl, trityl and substituted trityl groups, allyloxycarbonyl, 9- fluorenylmethyloxycarbonyl, nitro-veratryloxycarbonyl, tetrahydropyranyl, and glycol.
机译:具有下式结构的化合物:其中P1和P2分别为氢原子或选自酰基,烷基,四氢吡喃基,三烷基甲硅烷基,二醇基的羟基保护基和烯丙基; Z是-C(O)ORd,-C(O)NRcRc,-C(O)H,-C(NH)NRcRc,-C(S)H,-C(S)ORd,-C(S)NRcRc或-CN;每个Ra独立地选自氢,(C1-C6)烷基,环烷基(C3-C8),环己基,环烷基烷基(C4-C11),芳基(C5-C10),苯基,芳基烷基(C6-C16),苄基,2 6至6元杂烷基,3至8元环杂烷基,吗啉基,哌嗪基,高哌嗪基,哌啶基,环杂烷基烷基4至11元,杂芳基5至10元和杂芳基烷基6至16;每个Rb是合适的基团,其独立地选自= O,-ORd,卤代烷氧基(C1-C3),-OCF3,= S,-SRd,= NRd,= NORd,-NRcRc,卤素,-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)Rd,-OC(O) NRcRc,-OC(NH)NRcRc,-OC(NRa)NRcRc,-[NHC(O)] nRd,-[NRaC(O)] nRd,-[NHC(O)] nORd,-[NRaC(O)] nORd,-[NRaC(O)] nNRcRc,-[NRaC(O)] nNRcRc,-[NHC(NH)] nNRcRc和-[NRaC(NRa)] nNRcRc;每个R c独立地为保护基或Ra,或者,每个R c与与其相连的氮原子一起形成5至8元环杂烷基或杂芳基,其可任选地包括一个或多个杂原子相同或不同的附加基团,并且可以任选地被一个或多个相同或不同的Ra基团或合适的Rb取代;每个Rd独立地是保护基团或Ra; n为0〜3的整数,可以独立地选择Rc和Rd所表示的保护基,其中0〜3的整数可以为顺式或反式的碳-碳双键,或其药学上可接受的盐。由烯丙基2-三甲基甲硅烷基-乙磺酰基甲酰基,乙酰基,三氟乙酰基,苄基,苄氧羰基,叔丁氧羰基,三甲基甲硅烷基,三苯甲基和取代的三苯甲基,烯丙氧羰基,9-芴基甲氧羰基,硝基-藜芦基氧羰基,四氢吡喃基和乙二醇。

著录项

  • 公开/公告号ES2700133T3

    专利类型

  • 公开/公告日2019-02-14

    原文格式PDF

  • 申请/专利权人 BRIGHAM AND WOMENS HOSPITAL;

    申请/专利号ES20090009237T

  • 发明设计人 SERHAN CHARLES;

    申请日2003-08-12

  • 分类号A61K31/557;C07C69/732;A61K31/202;A61P29;C07C59/42;C07C59/48;C07F7/18;

  • 国家 ES

  • 入库时间 2022-08-21 11:59:32

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