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41. 发明申请

US20090318562A1 Use of Bupropion Metabolites for the Treatment of Inflammatory Disorders 失效
标题翻译：使用安非他酮代谢物治疗炎性疾病
公开(公告)号：US20090318562A1
公开(公告)日：2009-12-24
申请号：US12282274
申请日：2007-03-09
申请人： John Brew , Robin Mark Bannister , Andrew Douglas Baxter
发明人： John Brew , Robin Mark Bannister , Andrew Douglas Baxter
IPC分类号： A61K31/138 , A61P29/00
CPC分类号： A61K31/135
摘要： Compounds that may be used for the treatment or prevention of a condition associated with T-cell proliferation or that is mediated by pro-inflammatory cytokines are of formula (1) or a salt thereof.
摘要翻译：可用于治疗或预防与T细胞增殖相关的或由促炎细胞因子介导的病症的化合物具有式（1）或其盐。

42. 发明申请

US20090270384A1 MORPHOLINE DOPAMINE AGONISTS 有权
标题翻译：吗啡多巴胺激动剂
公开(公告)号：US20090270384A1
公开(公告)日：2009-10-29
申请号：US12496864
申请日：2009-07-02
申请人： Charlotte Moria Norfor Allerton , Andrew Douglas Baxter , Andrew Simon Cook , David Hepworth , Stephen Kwok-Fung Wong
发明人： Charlotte Moria Norfor Allerton , Andrew Douglas Baxter , Andrew Simon Cook , David Hepworth , Stephen Kwok-Fung Wong
IPC分类号： A61K31/5375 , C07D265/30
CPC分类号： C07D265/30 , C07D413/04
摘要： 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.
摘要翻译：本发明提供式（I），（Ia）和（Ib）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）烷基， R2选自H和（C1-C6）烷基，X选自H，HO，C（O）NH2，NH2Y选自H，HO，NH2，Br，Cl和FZ选自H，HO， F，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是CX时，B是CY，R 1是H或（C 1 -C 6）烷基，R 2是H或（C 1 -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C-X且B为C-Y时，Y为H，Z为H，R 1为H且R 2为H，则X不能为OH; 这些化合物可用作药物。

43. 发明申请

US20090093509A1 Methods and Compositions for the Treatment of Pruritus 审中-公开
标题翻译：治疗瘙痒的方法和组成
公开(公告)号：US20090093509A1
公开(公告)日：2009-04-09
申请号：US12247618
申请日：2008-10-08
申请人： Tahir Nazir , Andrew Douglas Baxter , Alan Rothaul
发明人： Tahir Nazir , Andrew Douglas Baxter , Alan Rothaul
IPC分类号： A61K31/485
CPC分类号： A61K31/485
摘要： The present invention is based on the discovery that a nalmefene salt or a peripherally acting analogue of nalmefene is capable of providing long-acting activity against pruritus, when applied topically. In addition, treatment with a nalmefene salt or peripherally acting analogue of nalmefene, can provide disease-modifying effects against the chronic symptoms of atopic dermatitis, including reductions of inflammatory cell infiltrate into the skin, epidermal hyperplasia and trans-epidermal water loss. Compositions of the invention have an inhibitory effect on the itch-scratch-cycle, leading to both relief of pruritus and disease-modifying activity.
摘要翻译：本发明是基于这样的发现，当局部应用时，纳美芬盐或纳美芬的外周作用类似物能够提供抗瘙痒的长效作用。此外，用纳美芬盐或外周作用的纳美芬类似物治疗可以对特应性皮炎的慢性症状提供改善疾病的功效，包括炎症细胞浸润进入皮肤的减少，表皮增生和反式表皮水分流失。本发明的组合物对瘙痒周期具有抑制作用，导致瘙痒和疾病改变活性的缓解。

44. 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。

45. 发明授权

US08846954B2 Crystallisation and purification of glycopyrronium bromide 有权
标题翻译：溴化格隆溴铵的结晶和纯化
公开(公告)号：US08846954B2
公开(公告)日：2014-09-30
申请号：US11817166
申请日：2006-03-03
申请人： Andrew Douglas Baxter , Kenneth Walter Sinden , Stefan Kleinebekel
发明人： Andrew Douglas Baxter , Kenneth Walter Sinden , Stefan Kleinebekel
IPC分类号： C07D207/12
CPC分类号： C07D207/12
摘要： A method for the production of crystalline glycopyrronium bromide, comprises the reaction of glycopyrronium base with methyl bromide in a solvent, in which the solvent is selected such that the diastereoisomeric ratio of the product favors the R,S and S,R diastereoisomers over the R,R, and S,S diastereoisomers, and separating the desired diastereoisomers by one or more controlled crystallization steps. This method gives a product having a particle size of narrow distribution.
摘要翻译：制备结晶格隆溴铵的方法包括将糖基溴与甲基溴反应在溶剂中，其中选择溶剂使得产物的非对映异构体比有利于R，S和S，R非对映异构体在R ，R和S，S非对映异构体，并通过一个或多个受控结晶步骤分离所需的非对映异构体。该方法得到粒度分布窄的产物。

46. 发明授权

US08030357B2 Use of bupropion metabolites for the treatment of inflammatory disorders 失效
标题翻译：使用安非他酮代谢物治疗炎症性疾病
公开(公告)号：US08030357B2
公开(公告)日：2011-10-04
申请号：US12282274
申请日：2007-03-09
申请人： John Brew , Robin Mark Bannister , Andrew Douglas Baxter
发明人： John Brew , Robin Mark Bannister , Andrew Douglas Baxter
IPC分类号： A61K31/138
CPC分类号： A61K31/135
摘要： Compounds that may be used for the treatment or prevention of a condition associated with T-cell proliferation or that is mediated by pro-inflammatory cytokines are of formula (I) or a salt thereof.
摘要翻译：可用于治疗或预防与T细胞增殖相关的或由促炎细胞因子介导的病症的化合物是式（I）或其盐。

47. 发明授权

US07902188B2 Morpholine dopamine agonists 有权
标题翻译：吗啉多巴胺激动剂
公开(公告)号：US07902188B2
公开(公告)日：2011-03-08
申请号：US12496864
申请日：2009-07-02
申请人： Charlotte Moira Norfor Allerton , Andrew Douglas Baxter , Andrew Simon Cook , David Hepworth , Stephen Kwok-Fung Wong
发明人： Charlotte Moira Norfor Allerton , Andrew Douglas Baxter , Andrew Simon Cook , David Hepworth , Stephen Kwok-Fung Wong
IPC分类号： A61K31/5375 , C07D265/30
CPC分类号： C07D265/30 , C07D413/04
摘要： 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.
摘要翻译：本发明提供式（I），（Ia）和（Ib）的化合物，其中A选自C-X和N，B选自C-Y和N，R 1选自H和（C1- C6）烷基，R2选自H和（C1-C6）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，HO，F，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是C-X时，B是C-Y，R1是H或（C1-C6）烷基，R2是H或（C1-C6）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C-X且B为C-Y时，Y为H，Z为H，R 1为H且R 2为H，则X不能为OH; 这些化合物可用作药物。

48. 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。

49. 发明申请

US20090012178A1 Benzoxazocines and Their Therapeutic Use 审中-公开
标题翻译：苯并恶嗪及其治疗用途
公开(公告)号：US20090012178A1
公开(公告)日：2009-01-08
申请号：US11817200
申请日：2006-03-10
申请人： Andrew Douglas Baxter
发明人： Andrew Douglas Baxter
IPC分类号： A61K31/166 , C07D267/14 , A61P13/00 , A61P25/00
CPC分类号： C07D267/22
摘要： A compound selected from (1S)-8-cyano-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1R)-8-cyano-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1S)-8-cyclopropyl-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1S)-8-cyclopropyl-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1S)-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine-8-carboxamide; (1R)-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine-8-carboxamide; and the salts thereof. These compounds have therapeutic utility.
摘要翻译：选自（1S）-8-氰基-5-甲基-1-（3-甲氧基）苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛; （1R）-8-氰基-5-甲基-1-（3-甲氧基）苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛; （1S）-8-环丙基-5-甲基-1-（3-甲氧基）苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛; （1S）-8-环丙基-5-甲基-1-（3-甲氧基）苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛; （1S）-5-甲基-1-（3-甲氧基）苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑烷-8-甲酰胺; （1R）-5-甲基-1-（3-甲氧基）苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑烷-8-甲酰胺; 及其盐。这些化合物具有治疗效用。

50. 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。

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