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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

WO2005041964A1 THE USE OF IFENPRODRIL IN THE TREATMENT OF PAIN 审中-公开
标题翻译：使用芬太尼治疗疼痛
公开(公告)号：WO2005041964A1
公开(公告)日：2005-05-12
申请号：PCT/GB2004/004459
申请日：2004-10-21
申请人： ARAKIS LTD. , BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas , ROTHAUL, Alan , LYNE, Michael, Harvey
发明人： BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas , ROTHAUL, Alan , LYNE, Michael, Harvey
IPC分类号： A61K31/445
CPC分类号： A61K31/445
摘要： Ifenprodil is useful for the treatment of pain.
摘要翻译： Ifenprodil可用于治疗疼痛。

5. 发明申请

WO2004050625A1 RESOLUTION OF MEFLOQUINE WITH O,O-DI-P-AROYLTARTARIC ACID 审中-公开
标题翻译： MEFLOQUINE与O，O-DI-P-AROYLTARTARIC酸的分离
公开(公告)号：WO2004050625A1
公开(公告)日：2004-06-17
申请号：PCT/GB2003/005286
申请日：2003-12-04
申请人： ARAKIS LTD. , BAXTER, Andrew, Douglas , HARRIS, Michael, John , BROWN, Stuart
发明人： BAXTER, Andrew, Douglas , HARRIS, Michael, John , BROWN, Stuart
IPC分类号： C07D215/14
CPC分类号： C07D401/06
摘要： A process for increasing the optical purity of a mixture of enantiomers of mefloquine, used a substantially single enantiomer of a O, O-di-p-aroyltartaric acid as a resolving agent.
摘要翻译：用于提高甲氟喹对映异构体混合物的光学纯度的方法，使用作为拆分剂的O，O-二对 - 芳基酒石酸的基本上单一的对映异构体。

6. 发明申请

WO2003092689A1 THE TREATMENT OF PAIN WITH IFENDROPIL 审中-公开
标题翻译：用IFENDROPIL治疗疼痛
公开(公告)号：WO2003092689A1
公开(公告)日：2003-11-13
申请号：PCT/GB2003/001906
申请日：2003-05-06
申请人： ARAKIS LTD. , BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas , ROTHAUL, Alan , LYNE, Michael, Harvey
发明人： BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas , ROTHAUL, Alan , LYNE, Michael, Harvey
IPC分类号： A61K31/445
CPC分类号： A61K31/445 , A61K9/0043
摘要： Ifenprodil is useful for the treatment of pain, e.g. on administration intranasally or by another route that avoids first-pass metabolism.
摘要翻译： Ifenprodil可用于治疗疼痛，例如在鼻内给药或通过避免首次代谢的另一种途径。

7. 发明申请

WO2006027579A2 THE TREATMENT OF INFLAMMATORY DISORDERS AND PAIN 审中-公开
标题翻译：治疗炎症性疾病和疼痛
公开(公告)号：WO2006027579A2
公开(公告)日：2006-03-16
申请号：PCT/GB2005/003452
申请日：2005-09-07
申请人： ARAKIS LTD. , BAXTER, Andrew, Douglas , BREW, John
发明人： BAXTER, Andrew, Douglas , BREW, John
IPC分类号： A61K31/137 , A61K31/138 , A61K31/37 , A61K31/4458 , A61K31/4704 , A61P1/00 , A61P1/02 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/02 , A61P29/02 , A61P37/06
CPC分类号： A61K31/138 , A61K31/137 , A61K31/37 , A61K31/4458 , A61K31/4704
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): wherein R 1 is CHR 4 -OR 5 or CHR 4 -SR 5 , or aryl or heteroaryl optionally substituted with one or more groups R 6 ; R 2 is alkyl or is part of a ring with R 3 ; R 3 is H, alkyl or CH 2 (when forming part of a ring with R 2 ); R 4 is H or alkyl or is part of a ring with R 5 ; R 5 is aryl or heteroaryl optionally substituted with R 7 ; each R 6 is independently alkyl, CF 3 , OH, Oalkyl, OCOalkyl, CONH 2 , CN, halogen, NH 2 , NO 2 , NHCHO, NHCONH 2 , NHSO 2 alkyl, CONH 2 , SOMe, SO 2 NH 2 , Salkyl, CH 2 SO 2 alkyl or OCONalkyl 2 ; R 7 is R 8 or (CH 2 ) n OR 8 , R 9 , CF 3 , OH, OR 9 , OCOR 9 , COR 9 , COOR 9 , CONH 2 , CH 2 CONH 2 , CN, halogen, NH 2 , NO 2 , NHCHO, NHCONH 2 , NHCONHR 7 , NHCON(R 9 ) 2 , NHCOR 9 , NHCOaryl, NHSO 2 Me, CONH 2 , SMe, SOMe or SO 2 NH 2 ; R 8 is (CH 2 ) n OR 9 , (CH) n OR 9 , (CH 2 ) n COOR 9 or (CH 2 ) n COaryI; R 9 is alkyl or cycloalkyl; and n is 1 to 4; or a salt thereof.
摘要翻译：可用于治疗或预防与T细胞增殖相关或由促炎细胞因子介导的病症的化合物具有式（I）：其中R

8. 发明申请

WO2005084658A1 DERIVATIVES OF ACTARIT AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： ACTARIT及其治疗用途的衍生物
公开(公告)号：WO2005084658A1
公开(公告)日：2005-09-15
申请号：PCT/GB2005/000834
申请日：2005-03-04
申请人： ARAKIS LTD. , BAXTER, Andrew, Douglas
发明人： BAXTER, Andrew, Douglas
IPC分类号： A61K31/167
CPC分类号： C07C237/22 , C07C233/54 , C07C257/04 , C07D257/04 , C07D295/13 , C07D295/185
摘要： Compounds that may have anti-inflammatory activity are of general formula wherein X is O or NR 1 ; Y isOorNR 1 ; R 2 is OR 1 or C, 1-4 alkyl substituted with R 3 , and R 2 is optionally substituted With R 4 ; each R 1 is the same or different and is H or C 1-4 alkyl, or R 1 and R 2 are joined to form a four to seven-membered ring containing one or more additional heteroatoms selected from O, N and S, and is optionally substituted with R 7 ; R 3 is OR 4 , NR 5 R 6 or a four to seven- embered ring which can contain .one or morte heteroatoms selected from O, N and S, and is optionally substituted with R 7 ;R 4 is H or C 1-4 alkyl optionally substituted with OR 8 ; R 5 and R 6 are the same or different and are each selected from H and C 1-4 alkyl optionally substituted with OR 8 ; R 7 is C 1-4 alkyl optionally substituted with OR 8 , halogen, CF 3 , NR 5 R 6 , or S(O) n R 9 where n is 0-2; each R 8 is H or C 1-4 alkyl optionally substituted with halogen or OH; and R 9 is C 1-4 alkyl; and the salts, solvates and hydrates thereof.
摘要翻译：可具有抗炎活性的化合物具有通式，其中X为O或NR 1; Y是ORNR1; R2是OR 1或被R 3取代的C 1-4烷基，R 2任选被R 4取代; 每个R 1相同或不同，为H或C 1-4烷基，或R 1和R 2连接形成含有一个或多个选自O，N和S的其它杂原子的四元至七元环，并且任选被 R7; R3是OR4，NR5R6或可以含有一个或多个选自O，N和S的杂原子的四至七个环，并且任选被R 7取代; R 4是H或任选被OR 8取代的C 1-4烷基; R5和R6相同或不同，各自选自H和任选被OR 8取代的C 1-4烷基; R 7是任选被OR 8，卤素，CF 3，NR 5 R 6或S（O）n R 9取代的C 1-4烷基，其中n是0-2; 每个R 8为H或任选被卤素或OH取代的C 1-4烷基; 并且R 9为C 1-4烷基; 及其盐，溶剂化物和水合物。

9. 发明申请

WO2005041963A1 THE USE OF NON-OPIATES FOR THE POTENTATION OF OPIATES 审中-公开
标题翻译：使用不透明度进行评估
公开(公告)号：WO2005041963A1
公开(公告)日：2005-05-12
申请号：PCT/GB2004/004446
申请日：2004-10-21
申请人： ARAKIS LTD. , BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas , ROTHAUL, Alan , LYNE, Michael, Harvey
发明人： BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas , ROTHAUL, Alan , LYNE, Michael, Harvey
IPC分类号： A61K31/445
CPC分类号： A61K31/445 , A61K31/135 , A61K31/137 , A61K31/165 , A61K31/381 , A61K31/395 , A61K31/485 , A61K31/5513 , A61K2300/00
摘要： A non-opioid analgesic is used for the treatment of intermittent or episodic pain experienced by a patient undergoing chronic pain treatment with an opioid analgesic.
摘要翻译：非阿片类镇痛药用于治疗由阿片类镇痛药进行慢性疼痛治疗的患者经历的间歇性或间歇性疼痛。

10. 发明申请

WO2004006903A1 THE TREATMENT OF EMESIS 审中-公开
标题翻译：治疗EMESIS
公开(公告)号：WO2004006903A1
公开(公告)日：2004-01-22
申请号：PCT/GB2003/003002
申请日：2003-07-11
申请人： ARAKIS LTD. , LYNE, Michael, Harvey , BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas
发明人： LYNE, Michael, Harvey , BREW, John , BANNISTER, Robin, Mark , BAXTER, Andrew, Douglas
IPC分类号： A61K31/137
CPC分类号： A61K31/137
摘要： A single enantiomer of venlafaxine is used to treat nausea, dizziness, blurred vision or emesis.
摘要翻译：文拉法辛的单一对映异构体用于治疗恶心，眩晕，视力模糊或呕吐。

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