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1. 发明申请

WO2005080316A2 MODULATOR 审中-公开
标题翻译： CANNABINOID受体的调节剂
公开(公告)号：WO2005080316A2
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000605
申请日：2005-02-21
申请人： UNIVERSITY COLLEGE LONDON , OKUYAMA, Masahiro , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth
发明人： OKUYAMA, Masahiro , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth
IPC分类号： C07C233/68
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR 1 or NR 1 R 2 wherein each of R 1 and R 2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO 2 -alkyl, alkenyl, CN, NH 2 , hydroxy, halo, alkoxy, CF 3 and nitro; Y is a polar functional group selected from OH, NO 2 , CN, COR 3 , COOR 3 , NR 3 R 4 , CONR 3 R 4 , SO 3 H, SO 2 -R 3 , SO 2 NR 3 R 4 and CF 3 , where each of R 3 and R 4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH 2 ) n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X-Y is other than meta -C≡-C-(CH 2 ) 2 CO 2 H, meta -C≡-C-(CH 2 ) 2 OH, meta -C≡C-(CH 2 ) 2 CO 2 Me, meta -(CH 2 ) 4 CO 2 H, ortho -CH 2 CO 2 H, ortho -(CH 2 ) 2 CO 2 H and ortho -(CH 2 ) 4 CO 2 H; and (ii) when A is phenyl, n is 0, and Z is OMe, X-Y is other than meta -C≡C-(CH 2 ) 4 OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为 H或烃基; X是亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO 2，CN，COR 3，COOR 3，NR 3 R 4，CONR 3 R 4，SO 3 H，SO 2 -R 3的极性官能团。，SO 2 NR 3 R 4和CF 3，其中R 3和R 4各自独立地为H或烃基; A是芳基或杂芳基，其各自可以任选被取代; 和B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A是苯基时，n是0，Z是OH，XY不是间位-C = -C-（CH 2）2 CO 2 H，间位C = -C-（CH 2）2 OH，间 - C（C-（CH 2）2 CO 2 Me，间 - （CH 2）4 CO 2 H，邻-CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - （CH 2）4 CO 2 H; 和（ii）当A是苯基时，n是0，Z是OMe，X-Y不是间位C = C-（CH 2）4 OH。本发明的其它方面涉及这些化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

2. 发明申请

WO2006067450A2 MODULATOR 审中-公开
标题翻译：调制器
公开(公告)号：WO2006067450A2
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004990
申请日：2005-12-21
申请人： UCL BIOMEDICA PLC , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth , OKUYAMA, Masahiro
发明人： SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth , OKUYAMA, Masahiro
IPC分类号： C07C37/055 , C07C37/11 , C07C37/62 , C07C39/06 , C07C39/15 , C07C39/27 , C07C39/367 , C07C45/00 , C07C59/90 , C07C67/343 , C07C233/25 , C07C235/34 , C07D213/30
CPC分类号： C07D213/30 , C07C37/055 , C07C37/18 , C07C37/62 , C07C39/15 , C07C39/367 , C07C41/30 , C07C45/004 , C07C59/90 , C07C67/343 , C07C233/25 , C07C235/34 , C07C49/84 , C07C69/738 , C07C43/205 , C07C39/06 , C07C39/27 , C07C39/12
摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof, Formula (I), wherein R 1 and R 2 are each independently H or alkyl; Y is an alkyl group, CONR 3 R 4 , COOR 5 SO 2 NR 16 R 17 , NHSO 2 R 18 or CN; X is an aryl or heteroaryl group, each of which may be optionally substituted with one or more substituents selected from (CH2) m Z where Z is halogen, OH, CN, alkyl, alkoxy, NO 2 , CF 3 , CONR 6 R 7 , CN, NR 8 R 9 , COOR 10 or NHCOR 11, and m is 0 to 3; R 3 to R 11 are each independently H, alkyl or aryl, wherein said alkyl and aryl groups are optionally substituted by one or more substituents selected from halogen, OH, CN, alkyl, alkoxy, NO 2 , CF 3 , CONR 12 R 13 , CN, NH 2 , COOR 14 , NHCOR 15 , and CN; R 12 to R 18 are each independently H or alkyl, more preferably H or Me; n is 1 to 6; wherein the compound is other than 3' ,5'-dimethyl-4-(1,1-dimethylheptyl)-1,1'-biphenyl-2-ol. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，式（I）其中R 1和R 2各自独立地为H或烷基; Y是烷基，CONR 3，R 4，COOR 5，SO 2，NR 16，或者CN;其中R 1，R 2，R 3，R 4， X是芳基或杂芳基，其各自可以任选地被一个或多个选自（CH 2）m Z的取代基取代，其中Z是卤素，OH，CN，烷基，烷氧基，NO > 2 ，CF 3，CONR 6，R 7，CN，NR 8 R SUP > 9，COOR 10或NHCOR 11，和m为0至3; R 3至R 11各自独立地为H，烷基或芳基，其中所述烷基和芳基任选被一个或多个选自以下的取代基取代：卤素，OH，CN，烷基，烷氧基，NO 2，CF 3，CONR 12，R 13，CN，NH 2 COOR 14，NHCOR 15和CN; R 12至R 18各自独立地为H或烷基，更优选为H或Me; n为1至6; 其中该化合物不是3'，5'-二甲基-4-（1,1-二甲基庚基）-1,1'-联苯-2-醇。本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

3. 发明申请

WO2005123676A1 BI- OR TETRA-GUANIDINO-BIPHENYL COMPOUNDS AS SMALL MOLECULE CARRIERS 审中-公开
标题翻译：作为小分子载体的双 - 或四联苯醌二联苯化合物
公开(公告)号：WO2005123676A1
公开(公告)日：2005-12-29
申请号：PCT/GB2005/002399
申请日：2005-06-17
申请人： UNIVERSITY COLLEGE LONDON , SELWOOD, David , VISINTIN , Christina , LAMAN, Heike , OKUYAMA, Masahiro
发明人： SELWOOD, David , VISINTIN , Christina , LAMAN, Heike , OKUYAMA, Masahiro
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , A61K47/54 , C07C279/08 , C07C279/24 , C07D213/70 , C07D213/71 , C07D311/86 , Y02P20/55
摘要： The invention relates to compounds of formula: I, or pharmaceutically acceptable a salts thereof, I wherein X 1 X 2 and X 3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF 3 , OH, alkoxy, NH 2 , CN, NO 2 and COOH; W is absent or is O, S or NH; R l , R 2 , R 3 and R 4 are each independently selected from H, alkyl, aryl and a protecting group P l ; R 7 , R 8 and R 9 are each independently selected from H, alkyl, halo, CF 3 , OH, alkoxy, NH 2 , CN, NO 2 and COOH; q and r are each independently 1, 2, 3 or 4; q' and r' are each independently 0, 1, 2 or 3, where q + q' and r + r' each equal 4; p is 1, 2, 3, 4 or 5, and p' is 0, 1, 2, 3 or 4, where p + p' is 5; n is 0, 1, 2, 3....6; L is (Z) m NR 5 R 6 where Z is a hydrocarbyl group and m is 0 or 1; where R 5 and R 6 are each independently H, CO(CH 2 ) j Q 1 or C=S(NH)(CH 2 ) k Q 2 where j and k are each independently 0, 1, 2, 3, 4 or 5, and Q 1 and Q 2 are each independently selected from COOH, a chromophore or R 5 , R 6 and the nitrogen to which they are attached together form.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中X1 X2和X3各自独立地为Y为亚烷基，亚烯基或亚炔基，其各自可任选被一个或多个选自下列的取代基取代：烷基，卤素，CF 3，OH，烷氧基，NH 2，CN，NO 2和COOH; W不存在或是O，S或NH; R1，R2，R3和R4各自独立地选自H，烷基，芳基和保护基P1; R 7，R 8和R 9各自独立地选自H，烷基，卤素，CF 3，OH，烷氧基，NH 2，CN，NO 2和COOH; q和r各自独立地为1,2,3或4; q'和r'各自独立地为0,1,2或3，其中q + q'和r + r'各自等于4; p为1,2,3,4或5，p'为0,1,2,3或4，其中p + p'为5; n为0,1,2,3 ... 6; L是（Z）mNR 5 R 6，其中Z是烃基，m是0或1; 其中R 5和R 6各自独立地为H，CO（CH 2）j Q 1或C = S（NH）（CH 2）k Q 2，其中j和k各自独立地为0,1,2,3,4或5，并且Q1和Q2各自为独立地选自COOH，发色团或R 5，R 6和与它们相连的氮形成。

4. 发明申请

WO2011061469A1 INDAZOLE DERIVATIVES AND THEIR USE FOR BLOCKADING VOLTAGE DEPENDENT SODIUM CHANNELS 审中-公开
标题翻译：吲哚衍生物及其用于阻断电压依赖性钠通道的用途
公开(公告)号：WO2011061469A1
公开(公告)日：2011-05-26
申请号：PCT/GB2010/001842
申请日：2010-09-30
申请人： UNIVERSITY COLLEGE LONDON , POSADA, Cristina, Garcia , SELWOOD, David , GARTHWAITE, John , BAKER, David , CLUTTERBUCK, Lisa
发明人： POSADA, Cristina, Garcia , SELWOOD, David , GARTHWAITE, John , BAKER, David , CLUTTERBUCK, Lisa
IPC分类号： C07D413/14 , C07D417/14 , A61K31/4245 , A61P25/00 , A61P23/00
CPC分类号： C07D413/14 , C07D417/14
摘要： The invention provides an indazole derivative of formula (1), or a pharmaceutically acceptable salt or N-oxide thereof, wherein R 1 , R 2 , R 3 and R 4 are as defined herein. The indazole derivatives are capable of blockading voltage dependent sodium channels and they are useful in the treatment or prevention of normal tension glaucoma, multiple sclerosis, a motorneurone disease, stroke, spinal cord injury, Alzheimer's disease, Parkinson's disease or pain.
摘要翻译：本发明提供式（1）的吲唑衍生物或其药学上可接受的盐或N-氧化物，其中R 1，R 2，R 3和R 4如本文所定义。吲唑衍生物能够阻断电压依赖性钠通道，并且它们可用于治疗或预防正常张力性青光眼，多发性硬化，运动神经元疾病，中风，脊髓损伤，阿尔茨海默病，帕金森病或疼痛。

5. 发明申请

WO2011010084A2 CYCLOSPORIN CONJUGATES 审中-公开
标题翻译：环孢素联合
公开(公告)号：WO2011010084A2
公开(公告)日：2011-01-27
申请号：PCT/GB2010/001369
申请日：2010-07-19
申请人： UCL BUSINES PLC , SELWOOD, David , CROMPTON, Martin
发明人： SELWOOD, David , CROMPTON, Martin
IPC分类号： A61K47/48
CPC分类号： C07K7/64 , A61K47/54 , A61K47/545 , A61K47/55 , A61K47/64 , G01N33/9493 , G01N2410/08
摘要： A conjugate which comprises a cyclosporin moiety of formula (I) linked to one or more mitochondrial targeting groups, or a pharmaceutically acceptable salt thereof: wherein: A represents or, B represents methyl or ethyl, one Of R 1 and R 1* represents hydrogen and the other represents methyl, R2 represents ethyl or isopropyl, R3 represents hydrogen or methyl, and R4 represents -CH 2 CH(CH 3 )CH 3 , -CH 2 CH(CH 3 )CH 2 CH 3 , -CH(CH 3 )CH 3 or -CH(CH 3 )CH 2 CH 3 .
摘要翻译：一种缀合物，其包含与一个或多个线粒体靶向基团连接的式（I）的环孢菌素部分或其药学上可接受的盐：其中：A表示或者，B表示甲基或乙基，R1和R1 *表示氢，其他代表甲基，R2代表乙基或异丙基，R3代表氢或甲基，R4代表-CH2CH（CH3）CH3，-CH2CH（CH3）CH2CH3，-CH（CH3）CH3或-CH（CH3）CH2CH3。

6. 发明申请

WO2010097604A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2010097604A2
公开(公告)日：2010-09-02
申请号：PCT/GB2010/000359
申请日：2010-03-01
申请人： UCL BUSINESS PLC , SELWOOD, David , WORTHINGTON, Roberta , REBSTOCK, Anne-Sophie , SIMONE, Michela , GOODING, Matt , DUBE, Henry , STOEBER, Kai , TUDZAROVA, Slavica , BOSHOFF, Christoffer , WILLIAMS, Gareth , KINGSBURY, Sarah , LAGOS, Dimitrios , MANUEL FUNES QUESADA, Juan
发明人： SELWOOD, David , WORTHINGTON, Roberta , REBSTOCK, Anne-Sophie , SIMONE, Michela , GOODING, Matt , DUBE, Henry , STOEBER, Kai , TUDZAROVA, Slavica , BOSHOFF, Christoffer , WILLIAMS, Gareth , KINGSBURY, Sarah , LAGOS, Dimitrios , MANUEL FUNES QUESADA, Juan
IPC分类号： C07C279/08
CPC分类号： C07D277/18 , C07C279/08 , C07C279/24 , C07C323/60 , Y02P20/55
摘要： A compound of formula I, or a pharmaceutically acceptable salt thereof, wherein - X 1 , X 2 and X 3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF 3 , OH, alkoxy, NH 2 , CN, NO 2 and COOH; W is absent or is O, S or NH; R 1 , R 2 , R 3 and R 4 are each independently selected from H, alkyl, aryl and a protecting group Pi; R 7 , R 8 and R 9 are each independently selected from H, alkyl, halo, CF 3 , OH, alkoxy, CN, NO 2 and COOH; - q is 1, 2, 3 or 4; q' is 0, 1, 2 or 3, where q + q' equals 4; p and r are each independently 1, 2, 3, 4 or 5; p' and r' are each independently 0, 1, 2, 3 or 4, where p + p' and r + r' each equal 5; and - n is 0, 1, 2, 3, 4, 5 or 6.
摘要翻译：式I化合物或其药学上可接受的盐，其中-X 1，X 2和X 3各自独立地为Y为亚烷基，亚烯基或亚炔基，其各自可任选被一个或多个选自烷基，卤素，CF 3，OH，烷氧基，NH 2，CN，NO 2和COOH; W不存在或是O，S或NH; R1，R2，R3和R4各自独立地选自H，烷基，芳基和保护基团Pi; R 7，R 8和R 9各自独立地选自H，烷基，卤素，CF 3，OH，烷氧基，CN，NO 2和COOH; - q是1,2,3或4; q'为0,1,2或3，其中q + q'等于4; p和r各自独立地为1,2,3,4或5; p'和r'各自独立地为0,1,2,3或4，其中p + p'和r + r'各自等于5; 和 - n是0，1，2，3，4，5或6。

7. 发明申请

WO2008009935A1 PHARMACEUTICAL COMPOSITIONS AND THEIR USE 审中-公开
标题翻译：药物组合物及其用途
公开(公告)号：WO2008009935A1
公开(公告)日：2008-01-24
申请号：PCT/GB2007/002722
申请日：2007-07-19
申请人： UCL BUSINESS PLC , SELWOOD, David , RIDDAL, Dieter , GRIFFITHS, Charmaine , KEYNES, Robert , BELLAMY, Tomas , GARTHWAITE, John
发明人： SELWOOD, David , RIDDAL, Dieter , GRIFFITHS, Charmaine , KEYNES, Robert , BELLAMY, Tomas , GARTHWAITE, John
IPC分类号： A61K31/5415 , A61P25/16 , A61P25/28 , A61P9/10 , A61P11/06
CPC分类号： A61K31/5415
摘要： The invention relates to use of a phenothiazine derivative which is (a) a compound of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for use in treating a disorder mediated by lipid peroxidation wherein R 1 , R 2 , R 3 , R 4 , R 5 , S’, m, n, p and q are as defined herein.
摘要翻译：本发明涉及吩噻嗪衍生物的用途，其为（a）式（I）化合物或其互变异构体，或（b）其药学上可接受的盐，用于制备用于治疗由脂质过氧化，其中R 1，R 2，R 3，R 4，R 5， SUP>，S'，m，n，p和q如本文所定义。

8. 发明申请

WO2003082918A1 VEGF PEPTIDES AND THEIR USE 审中-公开
标题翻译： VEGF PEPTIDES及其用途
公开(公告)号：WO2003082918A1
公开(公告)日：2003-10-09
申请号：PCT/GB2003/001375
申请日：2003-03-28
申请人： ARK THERAPEUTICS LTD. , SELWOOD, David , LÖHR, Marianne , ZACHARY, Ian
发明人： SELWOOD, David , LÖHR, Marianne , ZACHARY, Ian
IPC分类号： C07K14/475
CPC分类号： C07K14/52 , A61K38/00
摘要： A novel peptide having the amino acid sequence SCKNTDSRCKARQLELNERTCRCDKPRR or a fragment thereof that substantially retains NP-1 antagonist activity, in cyclic form, is proposed for use in therapy.
摘要翻译：提出了一种具有基本保持NP-1拮抗剂活性的氨基酸序列SCKNTDSRCKARQLELNERTCRCDKPRR或其片段的新型肽用于治疗。

9. 发明申请

WO2011024001A1 NP-1 ANTAGONISTS AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： NP-1拮抗剂及其治疗用途
公开(公告)号：WO2011024001A1
公开(公告)日：2011-03-03
申请号：PCT/GB2010/051413
申请日：2010-08-25
申请人： ARK THERAPEUTICS LIMITED , CRAWSHAW, Melanie Jayne , FALLON, Philip Spencer , JARVIS, Ashley Nicholas , POWELL, Jonathan Raymond , WINFIELD, Natalie Louise , SELWOOD, David , ZACHARY, Ian Charles , JIA, Haiyan
发明人： CRAWSHAW, Melanie Jayne , FALLON, Philip Spencer , JARVIS, Ashley Nicholas , POWELL, Jonathan Raymond , WINFIELD, Natalie Louise , SELWOOD, David , ZACHARY, Ian Charles , JIA, Haiyan
IPC分类号： C07D333/36 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , A61P3/00 , A61P25/00 , A61P35/00 , A61K31/381
CPC分类号： C07D417/12 , C07D333/36 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14
摘要： Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C=O or-C=O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR 2 , OR 1 , CN or CO 2 R; Z 1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中：W是亚芳基，亚杂芳基或式（a），每个L独立地是亚烷基，亚烯基，亚炔基，直接键，亚芳基，亚环烷基，亚烷基亚芳基， C = O或-C = O; 每个X独立地是含N的杂亚芳基，含N的亚环烷基或NR; Y是含N的杂芳基，含N的环烷基，NR2，OR1，CN或CO2R; Z1是式（b）; 可用于治疗，特别是治疗神经变性和癌症。

10. 发明申请

WO2008040979A1 ARGININE DERIVATIVES WITH NP-I ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有NP-I拮抗活性的ARGININE衍生物
公开(公告)号：WO2008040979A1
公开(公告)日：2008-04-10
申请号：PCT/GB2007/003766
申请日：2007-10-04
申请人： ARK THERAPEUTICS LTD. , JIA, Haiyan , ZACHARY, Ian , TICKNER, Michelle , CHENG, Lili , CHAPMAN, Chris , ELLARD, Katie , HARTZOULAKIS, Basil , JARVIS, Ashley , LYNCH, Rosemary , NALLY, Jamie , SELWOOD, David , STEWART, Mark
发明人： JIA, Haiyan , ZACHARY, Ian , TICKNER, Michelle , CHENG, Lili , CHAPMAN, Chris , ELLARD, Katie , HARTZOULAKIS, Basil , JARVIS, Ashley , LYNCH, Rosemary , NALLY, Jamie , SELWOOD, David , STEWART, Mark
IPC分类号： C07D277/56 , C07D307/68 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/06 , C07K5/08 , A61P3/00 , A61P25/00 , A61P35/00 , C07C279/04
CPC分类号： C07D333/38 , C07C279/12 , C07D277/56 , C07D307/68 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
摘要翻译：本发明是适合作为NP-1拮抗剂的式（I）或式（II）的化合物。

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