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1. 发明申请

US20100076068A1 Aminoalcohol Derivatives and Their Therapeutic Use 审中-公开
标题翻译：氨基醇衍生物及其治疗用途
公开(公告)号：US20100076068A1
公开(公告)日：2010-03-25
申请号：US12517272
申请日：2007-12-12
申请人： Andrea Walmsley , Elena Lasterra
发明人： Andrea Walmsley , Elena Lasterra
IPC分类号： A61K31/216 , C07C69/003 , C07C69/67 , C07D309/02 , A61K31/351 , A61P37/06 , A61P27/02 , A61P25/00 , A61P17/00 , A61P11/00 , A61P1/00
CPC分类号： C07D309/08 , C07B2200/07 , C07C219/22
摘要： A compound of formula (1) Including pharmaceutically acceptable salts thereof, wherein: R1 is aryl or heteroaryl optionally substituted with R8; R2 is H or alkyl or CH2 (when forming part of a ring with R3, R4 or R5); R3 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R4 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R5 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R6 is H, alkyl, COH, COOR9, CON(R9)2, COR9, COR10, COR11, P(O)nR9, P(O)nR10S(O)nR10 or S(O)nR9 and can be part of a ring with R2, R3, R4 or R5; R7 is H, alkyl, COOR9, COOR11, COR9 or CON(R9)2, and can be part of a ring with R2, R3, R4, R5 or R6; R8 is alkyl, CF3, OR9, OCOR9, CONH2, CN, F, Cl, Br, I, N(R9)2, NO2, NHCHO, NHCONH2, NHSO2R9, CON(R9)2, S(O)nR9, CH2OH Or OCON(R9)2; R9 is H, alkyl or cycloalkyl; R10 is aryl or heteroaryl (optionally substituted with R8) or a four to seven membered ring (which is optionally substituted with R8 and can contain one or more additional heteroatoms selected from the list O, S(O)n and NR9); R11 is alkyl optionally substituted with R8 or R10; and n is O, 1 or 2; provided that when R3, R4 or R5 is CH2OH then R6 is not H, and that when R7 is H and R3, R4 and R5 are alkyl then R6 is not H. is of therapeutic use in the treatment of a condition associated with T-cell proliferation or that is mediated by pro- and/or anti-inflammatory cytokines.
摘要翻译：式（1）的化合物包括其药学上可接受的盐，其中：R 1是任选被R 8取代的芳基或杂芳基; R2是H或烷基或CH2（当与R3，R4或R5形成环的一部分时）; R3是H，烷基，CH2OH或CH2OR6，可以是R2的环的一部分; R4是H，烷基，CH2OH或CH2OR6，并且可以是具有R2的环的一部分; R5是H，烷基，CH2OH或CH2OR6，并且可以是具有R2的环的一部分; R6是H，烷基，COH，COOR9，CON（R9）2，COR9，COR10，COR11，P（O）nR9，P（O）nR10S（O）nR10或S（O）nR9，并且可以是环的一部分 R2，R3，R4或R5; R7是H，烷基，COOR9，COOR11，COR9或CON（R9）2，并且可以是R2，R3，R4，R5或R6的环的一部分; R8是烷基，CF3，OR9，OCOR9，CONH2，CN，F，Cl，Br，I，N（R9）2，NO2，NHCHO，NHCONH2，NHSO2R9，CON（R9）2，S（O）nR9，CH2OH或 OCON（R9）2; R9为H，烷基或环烷基; R 10是芳基或杂芳基（任选被R 8取代）或4-7元环（其任选被R 8取代并且可以含有一个或多个选自列表O，S（O）n和NR 9的另外的杂原子）; R11是任选被R8或R10取代的烷基; 并且n为O，1或2; 条件是当R 3，R 4或R 5为CH 2 OH时，R 6不为H，当R 7为H且R 3，R 4和R 5为烷基时，R 6不为H.在治疗与T- 细胞增殖或由促炎和/或抗炎细胞因子介导的细胞增殖。

2. 发明申请

US20060019940A1 Novel benzoxazocines and their therapeutic use 审中-公开
标题翻译：新型苯并恶嗪及其治疗用途
公开(公告)号：US20060019940A1
公开(公告)日：2006-01-26
申请号：US11156969
申请日：2005-06-20
申请人： Andrew Baxter , Andrea Walmsley , Elena Lasterra
发明人： Andrew Baxter , Andrea Walmsley , Elena Lasterra
IPC分类号： C07D491/02 , A61K31/33
CPC分类号： C07D267/22 , C07D413/04
摘要： Compounds of the general formula (1), wherein one of W, X, Y and Z is N or CR4 and the others are each CH; and R4 is a specified substituent. These compounds inhibit monocamine reuptake, and are useful in the treatment of pain, emesis depression, post traumatic stress disorders, attention deficit disorders, obsessive compulsive disorders, pre-menstrual syndrome, substance abuse and sexual dysfunction.
摘要翻译：通式（1）的化合物，其中W，X，Y和Z中的一个为N或CR 4，其余各自为CH; R 4是指定的取代基。这些化合物抑制单胺再摄取，并且可用于治疗疼痛，呕吐抑郁，创伤后应激障碍，注意力缺陷障碍，强迫症，前月经综合征，药物滥用和性功能障碍。

3. 发明申请

US20090270494A1 Salts of Dihydroxyanthraquinone Carboxylic Acids and Their Therapeutic Use 审中-公开
标题翻译：二羟基蒽醌羧酸盐及其治疗用途
公开(公告)号：US20090270494A1
公开(公告)日：2009-10-29
申请号：US12513819
申请日：2007-11-09
申请人： Andrea Walmsley
发明人： Andrea Walmsley
IPC分类号： A61K31/351 , C07D309/32
CPC分类号： C07C66/02
摘要： A compound of general formula (I): wherein Xi 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; R3 is F, CF3, OR4, NR5R6 or S(O)nR7; 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; R9 is H or C1-4 alkyl; Y is NR9R10R11; and R10 and R11, are the same or different and are each H or C1-6 alkyl optionally substituted with R3 or halogen, or NR10R11, is a four to seven membered ring which can be optionally substituted with R8 or COR1, and can contain one or more additional heteroatoms selected from O, S(O)n and NR9; and hydrates thereof.
摘要翻译：通式（I）的化合物：其中X 1为H或COR 1且X 2为H或COR 2，但X 1和X 2不均为H; R 1和R 2相同或不同，并且各自被R 3取代的C 1-4烷基或可任选被R 8取代的四元至七元环，并且可含有一个或多个选自O，S（O） n和NR9; R3是F，CF3，OR4，NR5R6或S（O）nR7; R 4，R 5和R 6相同或不同，各自为H或任选被R 3取代的C 1-4烷基，或NR 5 R 6为含有一个或多个选自O，NR 8和S（O）n的杂原子的C 4-6异构烷基环; 每个n为0-2; R7是C1-4烷基; R8如R3或C1-4烷基所定义，任选被R3或卤素取代; R 9为H或C 1-4烷基; Y为NR9R10R11; 和R 10和R 11相同或不同，各自为H或任选被R 3或卤素取代的C 1-6烷基，或NR 10 R 11为可任选被R 8或COR 1取代的四元至七元环，并且可以含有一个或更多选自O，S（O）n和NR 9的其它杂原子; 及其水合物。

4. 发明授权

US07728035B2 Ester derivatives of rhein and their therapeutic use 失效
标题翻译：大黄酸的酯衍生物及其治疗用途
公开(公告)号：US07728035B2
公开(公告)日：2010-06-01
申请号：US10591157
申请日：2005-03-04
申请人： Andrew Douglas Baxter , Andrea Walmsley
发明人： Andrew Douglas Baxter , Andrea Walmsley
IPC分类号： A61K31/21 , C07C49/593
CPC分类号： C07C66/02
摘要： 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.
摘要翻译：可具有抗炎活性的化合物具有通式（I）; 其中X1是H或COR1，X2是H或COR2，但X 1和X 2都不是H; R 1和R 2相同或不同，并且各自被R 3取代的C 1-4烷基或可任选被R 8取代的四元至七元环，并且可含有一个或多个选自O，S（O） n和NR9; R3为F，CF3，OR4，NR5R6O，S（O）n R7; R 4，R 5和R 6相同或不同，各自为H或任选被R 3取代的C 1-4烷基，或NR 5 R 6为含有一个或多个选自O，NR 8和S（O）n的杂原子的C 4-6异构烷基环; 每个n为0-2; R7是C1-4烷基; R8如R3或C1-4烷基所定义，任选被R3或卤素取代; 并且R 9为H或C 1-4烷基; 或其盐，溶剂合物或水合物。

5. 发明申请

US20080234258A1 Dihydroxyanthraquinones and Their Use 审中-公开
标题翻译：二羟基蒽醌及其用途
公开(公告)号：US20080234258A1
公开(公告)日：2008-09-25
申请号：US11997660
申请日：2006-08-10
申请人： Andrew Douglas Baxter , Andrea Walmsley
发明人： Andrew Douglas Baxter , Andrea Walmsley
IPC分类号： A61K31/5377 , C07D413/14 , C07D407/12 , A61K31/351 , A61P35/04 , A61P1/00 , A61P17/00 , A61P3/00
CPC分类号： C07D309/08
摘要： A compound of formula (1) wherein X is H or —OCR1 and Y is H or —OCR2, provided that X and Y are not both H; and R is CH2OR9, CONR11R12, CN, tetrazole or COOR17; or a salt thereof, has therapeutic utility.
摘要翻译：式（1）的化合物，其中X为H或-OCR 1，Y为H或-OCR 2，条件是X和Y不同时为H; 和R为CH 2或N 9，CONR 11 R 12，CN，四唑或COOR 17 或其盐具有治疗效用。

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