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    • 4. 发明申请
    • Ester derivatives of rhein and their therapeutic use
    • 大黄酸的酯衍生物及其治疗用途
    • US20070185036A1
    • 2007-08-09
    • US10591157
    • 2005-03-04
    • Andrew BaxterAndrea Walmsey
    • Andrew BaxterAndrea Walmsey
    • A61K38/00
    • C07C66/02
    • Compounds that may have anti-inflammatory activity are of general formula (I); wherein X1, is H or COR1, and X2 is H or COR2 but X1, and X2 are not both H; R1 and R2 are the same or different and are each C1-4 alkyl substituted with R3, or a four to seven-membered ring which can be optionally substituted with R8 and can contain one or more additional heteroatoms selected from O, S(O)n and NR9; is R3 is F, CF3, OR4, NR5R6 O, S(O)n R7; R4, R5 and R6 are the same or different and are each H or C1-4 alkyl optionally substituted with R3, or NR5R6 is a C4-6 heterocycloalkyl ring containing one or more heteroatoms selected from O, NR8 and S(O)n; each n is 0-2; R7 is C1-4 alkyl; R8 is as defined for R3 or C1-4 alkyl optionally substituted with R3 or halogen; and R9 is H or C1-4 alkyl; or a salt, solvate or hydrate thereof.
    • 可具有抗炎活性的化合物具有通式(I); 其中X 1是H或COR 1,并且X 2是H或COR 2,但X 1 且X 2不同时为H; R 1和R 2各自相同或不同,并且各自是被R 3 3取代的C 1-4烷基, ,或可以任选被R 8'取代的4-7元环,并且可以含有一个或多个选自O,S(O)n N和NR的另外的杂原子 9 R 3是F,CF 3或OR 4,NR 5 R 6,或 > O,S(O)n R 7 R 7; R 4,R 5和R 6相同或不同,各自为H或C 1-4烷基, 任选被R 3 3或NR 5 R 6取代的烷基是含有一个的C 4-6 - 杂环烷基环 或更多选自O,NR 8和S(O)n的杂原子。 每个n为0-2; R 7是C 1-4烷基; R 8如R 3或C 1-4烷基所定义,任选被R 3或卤素取代; 并且R 9是H或C 1-4烷基; 或其盐,溶剂合物或水合物。
    • 5. 发明申请
    • Morpholine Dopamine Agonists
    • 吗啉多巴胺激动剂
    • US20060235016A1
    • 2006-10-19
    • US11425030
    • 2006-06-19
    • Charlotte AllertonAndrew BaxterAndrew CookDavid HepworthStephen Wong
    • Charlotte AllertonAndrew BaxterAndrew CookDavid HepworthStephen Wong
    • A61K31/5377C07D413/04
    • C07D265/30C07D413/04
    • The present invention provides for compounds of formula (I), (Ia) and (Ib) Wherein: A is selected from C—X and N, B is selected from C—Y and N, R1 is selected from H and (C1-C6)alkyl, R2 is selected from H and (C1-C6)alkyl, X is selected from H, HO, C(O)NH2, NH2 Y is selected from H, HO, NH2, Br, Cl and F Z is selected from H, HO F, CONH2 and CN; And pharmaceutically acceptable salts, solvates and prodrugs thereof; With the provisos that: for a compound of formula (I), (Ia) or (Ib), when A is C—X, B is C—Y, R1 is H or (C1-C6)alkyl and R2 is H or (C1-C6)alkyl at least one of X, Y and Z must be OH; for a compound of formula (I), when A is C—X and B is C—Y, Y is H, Z is H, R1 is H and R2 is H, then X cannot be OH; these compounds are useful as a medicament.
    • 本发明提供式(I),(Ia)和(Ib)的化合物,其中A选自CX和N,B选自CY和N,R 1选自H 和(C 1 -C 6 -C 6)烷基,R 2选自H和(C 1 -C 6烷基) C 1 -C 6烷基,X选自H,HO,C(O)NH 2,NH 2 Y选自H,HO, NH 2,Br,Cl和FZ选自H,HOF,CONH 2和CN; 其药学上可接受的盐,溶剂合物和前药; 条件是:对于式(I),(Ia)或(Ib)的化合物,当A为CX时,B为CY,R 1为H或(C 1 < C 1 -C 6烷基,R 2是H或(C 1 -C 6 -C 6)烷基, X,Y和Z中的至少一个必须是OH; 对于式(I)化合物,当A为CX且B为CY时,Y为H,Z为H,R 1为H且R 2为H, 那么X不能是OH; 这些化合物可用作药物。