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1. 发明申请

WO2005080316A3 MODULATORS OF CANNABINOID RECEPTORS 审中-公开
标题翻译：大麻素受体的调节因子
公开(公告)号：WO2005080316A3
公开(公告)日：2005-11-03
申请号：PCT/GB2005000605
申请日：2005-02-21
申请人： UNIV 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： C07C63/04 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/68 , C07C233/69 , C07C233/77 , C07C235/42 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , A61K31/167 , A61K31/192 , A61K31/216 , A61K31/235
CPC分类号： C07C235/42 , 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 or NR R wherein each of R and R 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, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR , COOR , NR R , CONR R , SO3H, SO2-R , SO2NR R and CF3, where each of R and R is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)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-(CH2)2CO2H, meta-C=-C-(CH2)2OH, meta-C=C-(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X-Y is other than meta-C=C-(CH2)4OH. 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，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，它们中的每一个可以任选被取代; 并且B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A为苯基，n为0且Z为OH时，XY不是间位C = -C-（CH 2）2 CO 2 H，间位C = -C-（CH 2）2 OH，（CH 2）2 CO 2 H，间 - （CH 2）4 CO 2 H，邻 - CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - 和（ii）当A是苯基时，n是0，并且Z是OMe，X-Y不同于间位C = C-（CH 2）4 OH。本发明的其他方面涉及这些化合物在制备用于治疗肌肉疾病，胃肠疾病或用于控制痉挛状态或震颤的药物中的用途。

2. 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。

3. 发明申请

WO2009027679A1 PROCESS FOR THE PREPARATION OF GUANIDINO SUBSTITUTED BI-AND POLYPHENYLS THAT ARE SUITABLE AS SMALL MOLECULE CARRIERS 审中-公开
标题翻译：制备适合作为小分子载体的胍基取代的双和双酚的方法
公开(公告)号：WO2009027679A1
公开(公告)日：2009-03-05
申请号：PCT/GB2008/002911
申请日：2008-08-29
申请人： UCL BUSINESS PLC , SELWOOD, David, L. , REBSTOCK, Anne-Sophie , VISINTIN, Cristina
发明人： SELWOOD, David, L. , REBSTOCK, Anne-Sophie , VISINTIN, Cristina
IPC分类号： C07D213/71 , C07C279/08 , A61K47/48
CPC分类号： C07D213/71 , A61K47/543 , C07C279/08
摘要： A process for the production of a compound of formula (I), or a pharmaceutically acceptable salt thereof, Formula (I) which process comprises:(a) coupling a compound of formula (II) to a compound of formula (III) to form a compound of formula (IV).
摘要翻译：制备式（I）化合物或其药学上可接受的盐的方法，式（I）的方法包括：（a）将式（II）化合物与式（III）化合物偶联形成式（IV）的化合物。

4. 发明申请

WO2006067450A3 MODULATOR 审中-公开
标题翻译：调制器
公开(公告)号：WO2006067450A3
公开(公告)日：2006-09-14
申请号：PCT/GB2005004990
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： C07C39/15 , A61K31/05 , A61K31/055 , A61K31/165 , A61K31/167 , A61P21/00 , C07C37/055 , C07C37/11 , C07C37/62 , C07C39/06 , C07C39/27 , C07C39/367 , C07C45/00 , C07C59/90 , C07C67/343 , C07C233/03 , C07C233/25 , C07C235/26 , C07C235/34 , C07D213/02 , 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, 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，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; 其中所述化合物不是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。

5. 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。

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