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1. 发明申请

WO2005085170A1 ESTER DERIVATIVES OF RHEIN AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：瑞芬及其治疗用途的ESTER衍生物
公开(公告)号：WO2005085170A1
公开(公告)日：2005-09-15
申请号：PCT/GB2005/000832
申请日：2005-03-04
申请人： ARAKIS LTD. , BAXTER, Andrew, Douglas , WALMSLEY, Andrea
发明人： BAXTER, Andrew, Douglas , WALMSLEY, Andrea
IPC分类号： C07C66/02
CPC分类号： C07C66/02
摘要： Compounds that may have anti-inflammatory activity are of general formula (I); wherein X 1 , is H or COR 1 , and X 2 is H or COR 2 but X 1 , and X 2 are not both H; R 1 and R 2 are the same or different and are each C 1-4 alkyl substituted with R 3 , or a four to seven-membered ring which can be optionally substituted with R 8 and can contain one or more additional heteroatoms selected from O, S(O) n and NR 9 ; is R 3 is F, CF 3 , OR 4 , NR 5 R 6 O, S(O) n R 7 ; R 4 , R 5 and R 6 are the same or different and are each H or C 1-4 alkyl optionally substituted with R 3 , or NR 5 R 6 is a C 4-6 heterocycloalkyl ring containing one or more heteroatoms selected from O, NR 8 and S(O) n ; each n is 0-2; R 7 is C 1-4 alkyl; R 8 is as defined for R 3 or C 1-4 alkyl optionally substituted with R 3 or halogen; and R 9 is H or C 1-4 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。

2. 发明申请

WO2005103019A1 BENZOXAZOCINES AND THEIR THERAPEUTIC USE AS MONOAMINE REUPTAKE INHIBITORS 审中-公开
标题翻译：苯并噻唑及其治疗用作单胺类药物抑制剂
公开(公告)号：WO2005103019A1
公开(公告)日：2005-11-03
申请号：PCT/GB2005/001519
申请日：2005-04-21
申请人： ARAKIS LTD. , BAXTER, Andrew, Douglas , WALMSLEY, Andrea , LASTERRA, Elena
发明人： BAXTER, Andrew, Douglas , WALMSLEY, Andrea , LASTERRA, Elena
IPC分类号： C07D267/22
CPC分类号： C07D413/04 , C07D273/00
摘要： Compounds having therapeutic utility are of general formula (1) wherein R, is H, C 1 -C 6 alkyl optionally substituted with F or C 3 -C 6 cycloalkyl or C 2 -C 4 alkenyl; A is O, CH 2 or S(O) n where n is 0-2; one of W, X, Y and Z is N, CH or CR 3 and the others are CH; R 2 is C5-C 6 heteroaryl, C 5 -C 10 cycloalkyl or cycloalkenyl optionally containing one or more heteroatoms selected from O, N and S(O) n where n is 0-2, and optionally substituted with R 3 ; or a phenyl group optionally substituted in one or more positions with one or more substituents independently selected from halogen, CN, CF 3 , C 1 -C 6 alkyl and OR 1 , or the phenyl group is fused to a five or six membered ring which may be carbocyclic, heterocyclic (containing 1-2 heteroatoms selected from O, N and S), aromatic or heteroaromatic (containing 1-2 heteroatoms selected from O and N); R 3 is selected from halogen; CF 3 ; CN; OR 5 ; SO 2 N(R 5 ) 2 ; COR 5 ; CO2R 5 ; CON(R 5 ) 2 ; NR 1 ,COR4; NR 1 SO 2 R 4 ; NR 1 CO 2 R 4 ; NR 1 ,CON(R 5 ) 2 ; OC 1 -C 6 alkyl substituted with R 3 ; C 1 -C 6 alkyl optionally substituted with unsubstituted R 3 ; C 3 -C 6 cycloalkyl optionally substituted with unsubstituted R 3 ; C 2 -C s alkenyl optionally substituted with unsubstituted R 3 ; C 2 -C s alkynyl optionally substituted with unsubstituted R 3 ; aryl optionally substituted with unsubstituted R 3 ; and five or six membered aromatic heterocycles containing 1-4 heteroatoms selected from N and O; R 4 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, aryl and heteroaryl; and R 5 is H, C 1 -C 6 alkyl; C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 6 cycloalkyl, aryl or heteroaryl and is the same as or different to another R 5 ; or a pharmaceutically acceptable salt thereof.
摘要翻译：具有治疗用途的化合物具有通式（1），其中R 1为H，任选被F或C 3 -C 6环烷基或C 2 -C 4烯基取代的C 1 -C 6烷基; A是O，CH 2或S（O）n，其中n是0-2; W，X，Y和Z之一为N，CH或CR 3，其余为CH; R2是C5-C6杂芳基，C5-C10环烷基或任选含有一个或多个选自O，N和S（O）n的杂原子的环烯基，其中n是0-2，并且任选被R 3取代; 或任选在一个或多个位置被一个或多个独立地选自卤素，CN，CF 3，C 1 -C 6烷基和OR 1的取代基取代的苯基，或者苯基与可以是碳环的五元或六元环稠合，杂环（含有1-2个选自O，N和S的杂原子），芳族或杂芳族（含有1-2个选自O和N的杂原子）; R3选自卤素; CF3; CN; OR5; SO 2 N（R 5）2; COR5; CO2R5; CON（R 5）2; NR1，COR4; NR1SO2R4; NR1CO2R4; NR1，CON（R 5）2; 用R3取代的OC1-C6烷基; 任选被未取代的R 3取代的C 1 -C 6烷基; 任选被未取代的R 3取代的C 3 -C 6环烷基; 任选被未取代的R 3取代的C 2 -C 8烯基; 任选被未取代的R 3取代的C 2 -C 8炔基; 任选被未取代的R 3取代的芳基; 和含有1-4个选自N和O的杂原子的五或六元芳族杂环; R 4是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 3 -C 6环烷基，芳基和杂芳基; 且R 5为H，C 1 -C 6烷基; C 2 -C 6烯基，C 2 -C 6炔基，C 3 -C 6环烷基，芳基或杂芳基，并且与另一个R 5相同或不同; 或其药学上可接受的盐。

3. 发明申请

WO2007017695A2 DIHYDROXYANTHRAQUINONES AND THEIR USE 审中-公开
标题翻译：二氢蒽醌及其用途
公开(公告)号：WO2007017695A2
公开(公告)日：2007-02-15
申请号：PCT/GB2006/002999
申请日：2006-08-10
申请人： SOSEI R & D LTD. , BAXTER, Andrew, Douglas , WALMSLEY, Andrea
发明人： BAXTER, Andrew, Douglas , WALMSLEY, Andrea
IPC分类号： C07D309/08
CPC分类号： C07D309/08
摘要： A compound of formula (1), wherein X is H or -OC R 1 and Y is H or -OCR 2 , provided that X and Y are not both H; and R is CH 2 OR 9 , CONR 11 R 12 , CN, tetrazole or COOR 17 ; or a salt thereof, has therapeutic utility.
摘要翻译：式（1）的化合物（其中X是H或-OCR 1且Y是H或-OCR 2）提供了式 X和Y不都是H; 并且R为CH 2 OR 9 9，CONR 11 R 12，CN，四唑或COOR 17 ; 或其盐，具有治疗效用。

4. 发明申请

WO2008071948A2 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：WO2008071948A2
公开(公告)日：2008-06-19
申请号：PCT/GB2007/004752
申请日：2007-12-12
申请人： SOSEI R & D LTD. , WALMSLEY, Andrea , LASTERRA, Elena
发明人： WALMSLEY, Andrea , LASTERRA, Elena
IPC分类号： C07C219/22 , C07D309/08 , A61K31/222 , A61K31/351 , A61P29/00
CPC分类号： C07D309/08 , C07B2200/07 , C07C219/22
摘要： A compound of formula (1 ) Including pharmaceutically acceptable salts thereof, wherein: R 1 is aryl or heteroaryl optionally substituted with R 8 ; R 2 is H or alkyl or CH 2 (when forming part of a ring with R 3 , R 4 or R 5 ); R 3 is H, alkyl, CH 2 OH or CH 2 OR 6 and can be part of a ring with R 2 ; R 4 is H, alkyl, CH 2 OH or CH 2 OR 6 and can be part of a ring with R 2 ; R 5 is H, alkyl, CH 2 OH or CH 2 OR 6 and can be part of a ring with R 2 ; R 6 is H, alkyl, COH, COOR 9 , CON(R 9 ) 2 , COR 9 , COR 10 , COR 11 , P(O) n R 9 , P(O) n R 10 S(O) n R 10 or S(O) n R 9 and can be part of a ring with R 2 , R 3 , R 4 or R 5 ; R 7 is H, alkyl, COOR 9 , COOR 11 , COR 9 or CON(R 9 ) 2 , and can be part of a ring with R 2 , R 3 , R 4 , R 5 or R 6 ; R 8 is alkyl, CF 3 , OR 9 , OCOR 9 , CONH 2 , CN, F, Cl, Br, I, N(R 9 ) 2 , NO 2 , NHCHO, NHCONH 2 , NHSO 2 R 9 , CON(R 9 ) 2 , S(O) n R 9 , CH 2 OH Or OCON(R 9 ) 2 ; R 9 is H, alkyl or cycloalkyl; R 10 is aryl or heteroaryl (optionally substituted with R 8 ) or a four to seven membered ring (which is optionally substituted with R 8 and can contain one or more additional heteroatoms selected from the list O, S(O) n and NR 9 ); R 11 is alkyl optionally substituted with R 8 or R 10 ; and n is O, 1 or 2; provided that when R 3 , R 4 or R 5 is CH 2 OH then R 6 is not H, and that when R 7 is H and R 3 , R 4 and R 5 are alkyl then R 6 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; R 2是H或烷基或CH 2（当形成具有R 3的环的一部分时，R 4是< 或R 5）; R 3是H，烷基，CH 2 OH或CH 2或OR 6，并且可以是环的一部分 R 2; R 4是H，烷基，CH 2 OH或CH 2或OR 6，并且可以是环的一部分 R 2; R 5是H，烷基，CH 2 OH或CH 2或OR 6，并且可以是环的一部分 R 2; R 6是H，烷基，COH，COOR 9，CON（R 9）2，COR COR 9，COR 11，COR 11，P（O）n R 9，P （O）N（R）N（O）n N（O）n N或S（O）n R 9可以是R 2，R 3，R 4，R 3，R 3，R 3，或R 5; R 7是H，烷基，COOR 9，COOR 11，COR 9或CON（R 1） 9）2，并且可以是R 2，R 3，R 4，R 4，R 3，R 3， R 5，R 5或R 6; R 8是烷基，CF 3或OR 9，OCOR 9，CONH 2 ，CN，F，Cl，Br，I，N（R 9）2，NO 2，NHCHO，NHCONH 2 NH 2 2 R 9，CON（R 9）2，S（O）2， R 2，R 2 OH或OCON（R 9）2; R 9是H，烷基或环烷基; R 10是芳基或杂芳基（任选被R 8 N取代）或4-7元环（其任选被R 8和R 8取代）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）。 R 11是任选被R 8或R 10取代的烷基; 且n为O，1或2; 条件是当R 3，R 4或R 5是CH 2 OH时，R 6， / SUB>不为H，当R 7为H且R 3，R 4和R 5

5. 发明申请

WO2008056156A1 SALTS OF DIHYDROXYANTHRAQUINONE CARBOXYLIC ACIDS AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：二羟基四氢喹啉羧酸的盐及其治疗用途
公开(公告)号：WO2008056156A1
公开(公告)日：2008-05-15
申请号：PCT/GB2007/004280
申请日：2007-11-09
申请人： SOSEI R & D LTD. , WALMSLEY, Andrea
发明人： WALMSLEY, Andrea
IPC分类号： C07C66/02 , A61K31/192 , A61K31/122 , A61P29/00 , A61P11/06 , A61P1/06 , A61P17/06 , A61P37/06
CPC分类号： C07C66/02
摘要： A compound of general formula (I): wherein Xi is H or COR 1 and X 2 is H or COR 2 but X 1 and X 2 are not both H; R 1 and R 2 are the same or different and are each C 1-4 alkyl substituted with R 3 , or a four to seven-membered ring which can be optionally substituted with R 8 and can contain one or more additional heteroatoms selected from O, S(O)n and NR 9 ; R 3 is F, CF 3 , OR 4 , NR 5 R 6 or S(O) n R 7 ; R 4 , R 5 and R 6 are the same or different and are each H or C 1-4 alkyl optionally substituted with R 3 , or NR 5 R 6 is a C 4-6 heterocycloalkyl ring containing one or more heteroatoms selected from O, NR 8 and S(O) n ; each n is 0-2; R 7 is C 1-4 alkyl; R 8 is as defined for R 3 or C 1-4 alkyl optionally substituted with R 3 or halogen; R 9 is H or C 1-4 alkyl; Y is NR 9 R 10 R 11 ; and R 10 and R 11 are the same or different and are each H or C 1-6 alkyl optionally substituted with R 3 or halogen, or NR 10 R 11 is a four to seven membered ring which can be optionally substituted with R 8 or COR 1 , and can contain one or more additional heteroatoms selected from O, S(O) n and NR 9 ; and hydrates thereof.
摘要翻译：通式（I）的化合物：其中X 1是H或COR 1 X和X 2是H或COR 2，但X 1和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，或者可以任选地被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和NR 9的另外的杂原子; R 3是F，CF 3或OR 4，NR 5 R 6，或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; R 9是H或C 1-4烷基; Y为NR 9 R 10 R 11; 且R 10和R 11相同或不同，并且各自为任选被R 3取代的H或C 1-6烷基或卤素，或NR 10 R 11是可以任选被R 8或COR取代的四元至七元环并且可以含有一个或多个选自O，S（O）n和NR 9的另外的杂原子。及其水合物。

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