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1. 发明申请

US20080306162A1 Treatment of Inflammatory Disorders and Pain 审中-公开
标题翻译：治疗炎症和疼痛
公开(公告)号：US20080306162A1
公开(公告)日：2008-12-11
申请号：US11993910
申请日：2006-06-30
申请人： Andrew Douglas Baxter , Michael Harvey Lyne , Robin Mark Bannister , Elena Lasterra
发明人： Andrew Douglas Baxter , Michael Harvey Lyne , Robin Mark Bannister , Elena Lasterra
IPC分类号： A61K31/135 , C07C215/68 , C07C215/20 , A61P25/00 , A61P11/00 , A61P29/00 , C07D215/00
CPC分类号： C07C215/68 , A61K31/133 , C07C215/30
摘要： A compound that is useful for the treatment or prevention of a condition such as pain, that is associated with T-cell proliferation or that is mediated by pro- and/or anti-inflammatory cytokines, is of formula (I) wherein R1 is aryl or heteroaryl optionally substituted with R5; R2 is H, alkyl or CH2OH and can be part of a ring with R4; R3 is H, alkyl or CH2OH and can be part of a ring with R4; R4 is H or alkyl or CH2 (when forming part of a ring with R2 or R3); and R5 is alkyl, CF3, OH, Oalkyl, OCOalkyl, CONH2, CN, F, Cl, Br, I, NH2, NHCHO, NHCONH2, NHSO2alkyl, CONH2, SOMe, CH2OH or OCONalkyl2; or a salt thereof.
摘要翻译：可用于治疗或预防与促进和/或抗炎细胞因子介导的T细胞增殖相关的疾病如疼痛的化合物是式（I），其中R 1是芳基或任选被R 5取代的杂芳基; R2是H，烷基或CH2OH，并且可以是与R4的环的一部分; R3是H，烷基或CH2OH，并且可以是与R4的环的一部分; R4是H或烷基或CH2（当与R2或R3形成环的一部分时）; 并且R 5是烷基，CF 3，OH，O烷基，OCO烷基，CONH 2，CN，F，Cl，Br，I，NH 2，NHCHO，NHCONH 2，NHSO 2烷基，CONH 2，SOMe，CH 2 OH或OCON烷基2; 或其盐。

2. 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。

3. 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。

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