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2. 发明申请

WO2005084653A2 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗化合物
公开(公告)号：WO2005084653A2
公开(公告)日：2005-09-15
申请号：PCT/GB2005000800
申请日：2005-03-04
申请人： CAMBRIDGE BIOTECHNOLOGY LTD , PRITCHARD MARTYN , OUZMAN JACQUELINE , SAVORY EDWARD , BROWN GILES
发明人： PRITCHARD MARTYN , OUZMAN JACQUELINE , SAVORY EDWARD , BROWN GILES
IPC分类号： C07H19/16 , A61K31/00
CPC分类号： C07H19/16
摘要： Use of compounds of general formula (A) as medicaments is described, in particular for the treatment of pain or inflammation; wherein: (I) when X = OH, R2 = NH2, R5 = CH2OH, R6 = H , R1 is C5-C6 alkoxy, OCH2Cyclopropyl, O-(2,2,3,3-tetrafluoro-cycloButyl), phenoxy, substituted phenoxy, OCH2CH2OH, or OCH2CHF2, (5-indanyl)oxy, C1, C2, C5, or C6 alkylamino, (R) or (S)-sec-Butylamino, C5 or C6 cycloalkylamino, exo-norbornane amino, (N-methyl, N-isoamylamino), phenylamino, phenylamino with either rnethoxy or fluoro substituents, a C2 sulfone group, a C2 alkyl group, a cyano group, a CONH2 group, or 3,5-dimethylphenyl; or when X = H, R2 = NH2, R5 = CH2OH , R6 = H, R1 is n-hexyloxy; or (II) when X = OH , R1 = H, R5 = CH2OH, R6 = H, R2 is NMe2, N-(2-isopentenyl), piperazinyl, (N-Me, N-benzyl), (N-Me, N-CH2Ph(3-Br)), (N-Me, N-CH2Ph(3-CF3)), or (N-Me, N-(2-rnethoxyethyl)), or OCH2Cyclopentyl; or (III) when X = OH, R5 = CONHR3, R6 = H: R1 is H, R3 is an isopropyl group, and R2 is either NH2 or a methylamino group (NHMe) or an isoamyl group (CH2CH2CHMe2); or R1 is H, R3 is H, and R2 is NH2; or R1 is OMe, R3 is Ph, and R2 is NH2; or R1 is NHCH2CH2CH2CH2CH2Me, R3 is CH2CH2CH2Me, and R2 is NH2; or (IV) when X = OH, R1 = H, R2 = NH2, R5 = CH2NHCOR.4, R6 = H, R4 is n-propyl or NHCH2CH3; or (V) when X = OH, R5 = CH2OH, R6 = H: R1 is NHCyclohexyl when R2 is NMe2; or R1 is OMe when R2 is NHBenzyl; or (VI) when X = OH , R2 = NH2, R5 = CH2OH, R6 = Me, R1 is NHCyclohexyl or NHCyclopentyl.
摘要翻译：描述了通式（A）的化合物作为药物的用途，特别是用于治疗疼痛或炎症; 其中：（I）X = OH时，R2 = NH2，R5 = CH2OH，R6 = H，R1为C5-C6烷氧基，OCH2环丙基，O-（2,2,3,3-四氟环丁基）苯氧基，OCH2CH2OH或OCH2CHF2，（5-二氢化茚基）氧基，C1，C2，C5或C6烷基氨基，（R）或（S） - 仲丁氨基，C5或C6环烷基氨基，外降冰片烷基氨基，（N-甲基，N-异戊基氨基），苯基氨基，具有甲氧基或氟取代基的苯基氨基，C2砜基，C2烷基，氰基，CONH2基或3,5-二甲基苯基; 或当X = H时，R 2 = NH 2，R 5 = CH 2 OH，R 6 = H，R 1为正己氧基; 或（II）当X = OH时，R1 = H，R5 = CH2OH，R6 = H，R2是NMe2，N-（2-异戊烯基），哌嗪基，（N-Me，N-苄基），（N-Me， N-CH 2 Ph（3-Br）），（N-Me，N-CH 2 Ph（3-CF 3））或（N-Me，N-（2-甲氧基乙基））或OCH 2环戊基; 或（III）当X = OH时，R5 = CONHR3，R6 = H：R1是H，R3是异丙基，R2是NH2或甲基氨基（NHMe）或异戊基（CH2CH2CHMe2）; 或R1为H，R3为H，R2为NH2; 或R1是OMe，R3是Ph，R2是NH2; 或R1是NHCH2CH2CH2CH2CH2Me，R3是CH2CH2CH2Me，R2是NH2; 或（IV）当X = OH时，R1 = H，R2 = NH2，R5 = CH2NHCOR4，R6 = H，R4为正丙基或NHCH2CH3; 或（Ⅴ）当X = OH时，R5 = CH2OH，R6 = H：当R2为NMe2时，R1为NHCyclohexyl; 或当R 2为NH苄基时，R 1为OMe; 或（Ⅵ）当X = OH时，R 2 = NH 2，R 5 = CH 2 OH，R 6 = Me，R 1为NHC环己基或NHC环戊基。

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