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1. 发明申请

WO2008075019A1 MODULATORS OF CB1 RECEPTORS 审中-公开
标题翻译： CB1受体的调节剂
公开(公告)号：WO2008075019A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004842
申请日：2007-12-17
申请人： 7TM PHARMA A/S , COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
发明人： COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
IPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D409/14 , C07D417/14 , C07D231/12 , A61K31/4725 , A61K31/497 , A61K31/4155 , A61P3/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A 1 is hydrogen, -COOH, or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R 4 and/or R 5 ; R 4 and R 5 are independently -R 9 , -CN, -F, -Cl, -Br, -OR 9 , -NR 7 R 8 , -NR 7 COR 6 , -NR 7 SO 2 R 6 , -COR 6 , -SR 9 , -SOR 9 , or -SO 2 R 6 ; R 6 is C 1 -C 4 alkyl, cycloalkyl, -CF 3 or -NR 7 R 8 ; R 7 and R 8 are independently hydrogen, C 1 -C 4 alkyl or cycloalkyl; R 9 is hydrogen, C 1 -C 4 alkyl, C 1 - C 4 alkoxy, C 1 -C 4 alkoxy(C 1 -C 4 alkyl)-, cycloalkyl, or fully or partially fluorinated C 1 -C 4 alkyl; R 1 (i) a bond; (ii) a divalent radical of formula -(CH 2 ) a B 1 (CH 2 ) b wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3, and B 1 is -CO-, -0-, -S-, -SO-, - SO 2 -, -CH 2 -, -CHCH 3 -, -CHOH- or -NR 7 -; or (iii) a divalent radical selected from - C(R 10 )(R 11 )-*, -C(R 10 )(R 11 )-O-*, -C(R 10 )(R 11 )CH 2 -*, -C(R 10 )(R 11 )CH 2 -O-*, -CH 2 C(R 10 )(R 11 )-*, -CH 2 C(R 10 )(R 11 )-O-*, -CH 2 -O-C(R 10 )(R 11 )-* and -C(R 10 )(R 11 )-O-CH 2 -*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is as defined in the specification; R 10 is hydrogen and R 11 is (C 1 -C 3 )alkyl or -OH; or R 10 and R 11 are both (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 -C 5 )cycloalkyl ring.
摘要翻译：式（I）化合物抑制正常的信号传导活性CB1受体，因此可用于治疗由CB1受体信号传导活性介导的疾病或病症，例如治疗肥胖和超重，预防体重增加，治疗疾病和直接或间接与肥胖和超重相关的病症：其中A 1是氢，-COOH或四唑基; p和q独立地为0或1; A3是苯基或环烷基，其任一个任选被R 4和/或R 5取代; R 4和R 5独立地是-R 9，-CN，-F，-Cl，-Br，-OR 9 -NR 7 R 8，-NR 7 COR 6，-NR N R 8， 7个SO 2，6个6， - 6个，-SR 9，-SOR， - SUB > 9 或-SO 2 R 6; R 6是C 1 -C 4烷基，环烷基，-CF 3或-NR 7 - [R _{8 ; R 7和R 8独立地是氢，C 1 -C 4烷基或环烷基; R 9是氢，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， C 1 -C 4烷氧基，C 1 -C 4烷氧基（C 1 -C 4烷基） - ，环烷基，或全部或部分氟化的C 1 -C 4烷基; R 1（i）键; （ii）式 - （CH 2）2的二价基团a（CH 2）2 N（CH 2）2 其中a和b独立地是0,1,2或3，条件是a + b是1,2或3，并且B 1是-CO - ， - O-， -S - ， - SO - ， - SO 2 - ， - CH 2 - ， - CHCH 3 - ， - CHOH-或-NR _{7 - ; 或（iii）选自-C（R 10）（R 11） - *， - C（R 10）（R 10） R 11） - O- *， - C（R 10）（R 11）CH 2 - * ，-C（R 10）（R 11）CH 2 -O-，-CH 2 C （R 10）（R 11） - *，-CH 2 C（R 10）（R 10）（R 11） - O *， - CH 2 - （R 10） - （R 11） - *和 -C（R 10）（R 11）-O-CH 2 - *，其中由星号表示的键连接到吡唑环 Z如规范中所定义; R 10是氢，R 11是（C 1 -C 3 -C 3）烷基或-OH; 或R 10和R 11均为（C 1 -C 3 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）烷基， / SUB）环烷基环。}}

2. 发明申请

WO2008075013A1 MODULATORS OF CANNABINOID RECEPTOR 审中-公开
标题翻译： CANNABINOID受体的调节剂
公开(公告)号：WO2008075013A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004835
申请日：2007-12-17
申请人： 7TM PHARMA A/S , COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
发明人： COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
IPC分类号： C07D231/18 , A61K31/415 , A61K31/4155 , A61P3/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: Wherein A 1 is hydrogen, -COOH, or tetrazolyl, and A 2 is hydrogen, -COOH, or tetrazolyl, provided that one of A 1 and A 2 is either -COOH or tetrazolyl; p is O or 1; A 3 is phenyl or cycloalkyl, either of which is optionally substituted with R 4 and/or R 5 ; q is O or 1; R 3 is hydrogen, C 1 C 4 alkyl, cycloalkyl, -CF 3 , or -OR 9 ; R 4 and R 5 independently -R 9 , -CN, -F, -Cl, -Br, -OR 9 , -NR 7 R 8 , -NR 7 COR 6 , -NR 7 SO 2 R 6 , -COR 6 , -SR 9 , -SOR 9 , Or -SO2R 6 , R 6 is C 1 -C4 alkyl, cycloalkyl, -CF 3 Or -NR 7 R 8 ; R 7 and R 8 are independently hydrogen, C 1 -C 4 alkyl or cycloalkyl; R 9 is hydrogen, C 1 -C 4 alkyl, cycloalkyl, fully or partially fluorinated C 1 -C 4 alkyl; R 1 is a divalent radical selected from -C(R 10 )(R 11 )-*, -C(R 10 )(R 11 )-O-*, -C(R 10 )(R 11 )CH 2 -*, -C(R 10 )(R 11 )CH 2 -O-*, -CH 2 C(R 10 )(R 11 )-*, -CH 2 C(R 10 )(R 11 )-O-*, -CH 2 -O-C(R 10 )(R 11 )-* and -C(R 10 )(R 11 )-O-CH 2 -*, wherein the bond indicated by an asterisk is attached to the pyrazole ring, and R 10 is hydrogen and R 11 is (C 1 -C 3 )alkyl or -OH; or R 10 and R 11 are both (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 - C 5 )cycloalkyl ring; and R 2 is a bond, -(CH 2 ) a B 1 (CH 2 ) b - or -[(CH 2 ) a B 1 (CH 2 )b] n -A 4 - [(CH 2 ) c B 2 (CH 2 ) d ] m - wherein a and b are independently 0, 1, 2 or 3 provided that a+b is not greater than 4, and B 1 and B 2 are independently is -CO-, -0-, -S-, -SO-, -SO 2 -, -CH 2 -, - CHOH- or -NR 7 -; c and d are independently 0,1, 2 or 3; with the proviso that a+b+c+d is not greater than 6, n and m are independently 0 or 1 and A 4 is (i) a monocyclic carbocyclic ring, having 3 to 8 ring atoms, optionally substituted with one or more of -F, -Cl, -Br, -CN, -CF 3 , C 1 -C 4 alkyl, cycloalkyl, -OR 9 , oxo or -NR 7 R 8 ; or (ii) a monocyclic heterocyclic ring, having 4 to 8 ring atoms, optionally substituted with one or more of -F, -Cl, -Br, -CN, -CF 3 , C 1 -C 4 alkyl, cycloalkyl, -OR 9 , oxo or -NR 7 R 8 .
摘要翻译：式（I）化合物抑制正常的信号传导活性CB1受体，因此可用于治疗由CB1受体信号传导活性介导的疾病或病症，例如治疗肥胖和超重，预防体重增加，治疗疾病和直接或间接与肥胖和超重相关的病症：其中A 1是氢，-COOH或四唑基，并且A 2 H 2是氢，-COOH或四唑基，提供 A 1和A 2之一是-COOH或四唑基; p是O或1; A 3是苯基或环烷基，其任一个任选被R 4和/或R 5取代; q是O或1; R 3是氢，C 1 -C 4烷基，环烷基，-CF 3 - 或-OR _{9 ; R 4和R 5独立地-R 9，-CN，-F，-Cl，-Br，-OR 9， NR 7，-NR 7 R 6，-NR 7，-NR 7，-NR 7 R 8，-NR 7， SO 2，-SOR 9，-SOR 9，-SOR 9，-SOR 9，-SOR 9， 9或-SO 2 R 6，R 6是C 1 -C 4烷基，环烷基，-CF 3，或-NR 7 R 8 8; R 7和R 8独立地是氢，C 1 -C 4烷基或环烷基; R 9是氢，C 1 -C 4烷基，环烷基，完全或部分氟化的C 1 -C 烷基; R 1是选自-C（R 10） - （R 11） - ， - C（R 10）的二价基团（R 11） - O - ， - C（R 10）（R 11）CH 2 -C（R 10）（R 11）CH 2 -O - ， - CH- （R 10） - （CH 2） - ， - CH 2 C（R 10）（R 11） - O - ， - CH 2 -OC（R 10）（R 11）（R 11） - 和-C（R 10）（R 11）-O-CH 2 - *，其中由一个星号连接到吡唑环上，R 10是氢，R 11是（C 1 -C 3）烷基，烷基或-OH; 或R 10和R 11均为（C 1 -C 3 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）烷基， / SUB）环烷基环; 和R 2是（CH 2）2 - （CH 2）2 - ， - b） - 或 - - （（CH 2）2）B 1（CH 2） b）N - - - - - - - （（CH 2））C b - 2其中a和b独立地为0,1,2或3，条件是a + b不大于4，并且B 1和B 2个独立地是-CO - ， - O - ， - S - ， - SO - ， - SO 2 -CH 2 - ， - CH 2 - ， - CH 2 - ， - NR 2 - ， - CH 2 - 或-NR 7 - 。 c和d独立地为0,1,2或3; 条件是a + b + c + d不大于6，n和m独立地为0或1，并且A 4是（i）具有3至8个环原子的单环碳环，任选被-F，-Cl，-Br，-CN，-CF 3 N，C 1 -C 4中的一个或多个取代。烷基，环烷基，-OR 9，氧代或-NR 7 R 8; 或（ii）具有4至8个环原子的单环杂环，任选被-F，-Cl，-Br，-CN，-CF 3， C 1 -C 4烷基，环烷基，-OR 9，氧代或-NR 7 R 8 >。}

3. 发明申请

WO2008075012A1 CB1 RECEPTOR MODULATORS 审中-公开
标题翻译： CB1受体调节剂
公开(公告)号：WO2008075012A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004831
申请日：2007-12-17
申请人： 7TM PHARMA A/S , COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
发明人： COOPER, Martin , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , NIELSEN, Peter, Aadal , LINGET, Jean-Michel , NOEREGAARD, Pia, Karina , MURRAY, Anthony , BJURLING, Emelie
IPC分类号： C07D231/12 , C07D231/18 , C07D401/12 , C07D403/06 , A61K31/415 , A61K31/4155 , A61P3/00
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A 1 is hydrogen, -COOH, or tetrazolyl, and A 2 is hydrogen, -COOH, or tetrazolyl, provided that one of A 1 and A 2 is either -COOH or tetrazolyl; p is O or 1 and A 3 is phenyl or cycloalkyl, either of which is optionally substituted with R 4 and/or R 5 ; q is O or 1; R 3 is hydrogen, C 1 -C 4 alkyl, cycloalkyi, -CF 3 , or -OR 9 ; R 4 and R 5 independently -R 9 , -CN, -F, -Cl, -Br, -OR 9 , - NR 7 R 8 , -NR 7 COR 6 , -NR 7 SO 2 R 6 , -COR 6 , -SR 9 , -SOR 9 , or -SO 2 R 6 ; R 6 is C 1 -C 4 alkyl, cycloalkyl, -CF 3 or -NR 7 R 8 ; R 7 and R 8 are independently hydrogen, C 1 -C 4 alkyl, -CF 3 , or cycloaikyL R 9 is hydrogen, C 1 -C 4 alkyl, cycloalkyl, fully or partially fluorinated C 1 -C 4 alkyl; R 1 is (i) a bond, or (ii) -(CH 2 ) a B 1 (CH 2 ) b - wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) -C(R 10 )(R 11 )-*, -C(R 10 )(R 11 )-O-*. -C(R 10 )(R 11 )CH 2 -*, -C(R 10 )(R 11 )CH 2 -O-*, - CH 2 C(R 10 )(R 11 )-*, -CH 2 C(R 10 )(R 11 )-O-*, -CH 2 -O-C(R 10 )(R 11 )-* or -C(R 10 )(R 11 )-O-CH 2 -*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q 1 A 4 -[Q 2 ]w- wherein Q 1 , A 4 , Q 2 and w are as defined in the specification; and R 10 is hydrogen and R 11 is (C 1 -C 3 )alkyl or -OH; or R 10 and R 11 are both (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 - C 5 )cycloalkyl ring.
摘要翻译：式（I）化合物抑制正常的信号传导活性CB1受体，因此可用于治疗由CB1受体信号传导活性介导的疾病或病症，例如治疗肥胖和超重，预防体重增加，治疗疾病和与肥胖和超重直接或间接相关的病症：其中A 1是氢，-COOH或四唑基，并且A 2 H 2是氢，-COOH或四唑基，提供 A 1和A 2之一是-COOH或四唑基; p是0或1，并且A 3是苯基或环烷基，其任一个任选被R 4和/或R 5取代; q是O或1; R 3是氢，C 1 -C 4烷基，环烷基，-CF 3或-OR 3， SUB> 9 ; R 4和R 5独立地-R 9，-CN，-F，-Cl，-Br，-OR 9， NR 7，-NR 7 R 6，-NR 7，-NR 7 R 6，-NR 7， SO 2，-SOR 9，-SOR 9，-SOR 9，-SOR 9，-SOR 9， 9或-SO 2 R 6; R 6是C 1 -C 4烷基，环烷基，-CF 3或-NR 7 - [R _{8 ; R 7和R 8独立地是氢，C 1 -C 4烷基，-CF 3 或R 3为氢，C 1 -C 4烷基，环烷基，完全或部分氟化的C 1 -C 6烷基， C 1 -C 4烷基; R 1是（i）键，或（ii） - （CH 2）2 - （CH 2）其中a和b独立地为O，1,2或3，条件是a + b为1,2或3; 或（iii）-C（R 10）（R 11） - *， - C（R 10）（R 11）） - O- *。 -C（R 10）（R 11）CH 2 - ， - （R 10）（R 10） R 11（CH 2）2 CH 2 -O - ， - CH 2 C（R 10）（R 11） - *，-CH 2 C（R 10）（R 11）-O - ， - CH （R 10） - *或-C（R 10）（R 10） - （R 10） O-CH 2 - *，其中由星号表示的键连接到吡唑环上; R 2是式-Q 1的二价基团，其中Q 1，R 2，R 2， A 4，Q 2和W如说明书中所定义; 并且R 10是氢，R 11是（C 1 -C 3 -C 3）烷基或-OH; 或R 10和R 11均为（C 1 -C 3 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）烷基， / SUB）环烷基环。}

4. 发明申请

WO2009074782A1 CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNABINOID受体调节剂
公开(公告)号：WO2009074782A1
公开(公告)日：2009-06-18
申请号：PCT/GB2008/004051
申请日：2008-12-08
申请人： 7TM PHARMA A/S , RECEVEUR, Jean Marie , BJURLING, Emelie , MURRAY, Anthony , HOEGBERG, Thomas , NEILSEN, Peter, Aadal , LINGET, Jean-Michel , NOERREGAARD, Pia, Karina , ALMHOLT, Dorthe
发明人： RECEVEUR, Jean Marie , BJURLING, Emelie , MURRAY, Anthony , HOEGBERG, Thomas , NEILSEN, Peter, Aadal , LINGET, Jean-Michel , NOERREGAARD, Pia, Karina , ALMHOLT, Dorthe
IPC分类号： C07D231/14 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/06 , A61K31/415 , A61K31/4155 , A61P3/04
CPC分类号： C07D413/06 , C07D231/14 , C07D401/12 , C07D401/14 , C07D403/04
摘要： Compounds of formula (I) are modulators of cannabinoid receptor CB1, useful inter alia for treatment of obesity: Formula (I). Wherein:X is a bond, or a divalent radical selected from -C(R 10 )(R 11 )-*, -C(R 10 )(R 11 )-O-*, -C(R 10 )(R 11 )CH 2 -*, -C(R 10 )(R 11 )CH 2 -O-*, -CH 2 C(R 10 )(R 11 )-*, -CH 2 C(R 10 )(R 11 ) -O-*. and -CH 2 -O-C(R 10 )(R 11 )-*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R 3 is hydrogen, (C 1 -C)aIkyI or (C 1 C 3 )fluoroalkyl; R 4 is a radical of formula -(AIk 1 ) P -(Q 1 ) r (L) s -Q 2 wherein p, r, s, AIk 1 , L, Q 1 and Q 2 are as specified; or R 3 and R 4 taken together with the nitrogen to which they are attached form a cyclic amino ring of 4 to 7 ring atoms which is optionally substituted by a radical of formula -(L) s -Q 2 wherein s, L and Q 2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, -NH 2 -, or mono- or di-(C 1 C 3 )alkylamino; R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen -F, -Cl, -Br, -CN, (C 1 -C 3 )alkyl, (C 1 C 3 )fluoroalkyl, cyclopropyl, and -OR 9 ; R 10 is hydrogen, (C 1 C 3 )alkyl, hydroxyl or NH 2 , and R 11 is hydrogen or (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 -C 5 )cycloalkyl ring.
摘要翻译：式（I）化合物是大麻素受体CB1的调节剂，尤其用于治疗肥胖症：式（I）。其中X为键或选自-C（R 10）（R 11） - *，-C（R 10）（R 11）-O- *，-C（R 10）（R 11）CH 2 - C（R10）（R11）CH2-O- *，-CH2C（R10）（R11） - *，-CH2C（R10）（R11）-O- *。和-CH 2 -O-C（R 10）（R 11） - *，其中由星号表示的键连接到吡唑环上; Z是选自指定组的羧基等价基团; R3是氢，（C1-C）aI1I或（C1C3）氟代烷基; R4是式 - （AIk1）P-（Q1）r（L）s -Q2的基团，其中p，r，s，Alk1，L，Q1和Q2如所规定; 或者R 3和R 4与它们所连接的氮原子一起形成4至7个环原子的环状氨基环，其任选被式 - （L）s-Q 2的基团取代，其中s，L和Q2如上定义或选自羟基，甲氧基，-NH 2 - 或单 - 或二 - （C 1 -C 3）烷基氨基的任选取代基; R5，R6，R7和R8各自独立地选自-F，-Cl，-Br，-CN，（C1-C3）烷基，（C1C3）氟烷基，环丙基和-OR9; R 10是氢，（C 1 -C 3）烷基，羟基或NH 2，R 11是氢或（C 1 -C 3）烷基; 或R 10和R 11与它们所连接的碳原子一起形成（C 3 -C 5）环烷基环。

5. 发明申请

WO2009153569A2 CB1 RECEPTOR MODULATORS 审中-公开
标题翻译： CB1受体调节剂
公开(公告)号：WO2009153569A2
公开(公告)日：2009-12-23
申请号：PCT/GB2009/001539
申请日：2009-06-18
申请人： 7TM PHARMA A/S , MURRAY, Anthony , HOEGBERG, Thomas , COOPER, Martin , BJURLING, Emelie , RECEVEUR, Jean-Marie , NOERREGAARD, Pia, Karina
发明人： MURRAY, Anthony , HOEGBERG, Thomas , COOPER, Martin , BJURLING, Emelie , RECEVEUR, Jean-Marie , NOERREGAARD, Pia, Karina
IPC分类号： C07D401/06 , C07D403/06 , A61K31/4178 , A61P3/04
CPC分类号： C07D401/06 , C07D403/06
摘要： Compounds of formula (I) suppress the normal signalling activity of cannabinoid receptor CB1 and are therefore useful inter alia in the treatment of conditions directly or indirectly associated with obesity and overweight, Wherein A 1 is -COOH or tetrazolyl; R 2 , R 3 , R' 2 and R' 3 are independently selected from -R 9 , - CN, -F, -Cl, -Br, -OR 9 , or -SR 9 ; R 9 is hydrogen, C 1 -C 3 alkyl, cycloalkyl, or fully or partially fluorinated C 1 -C 3 alkyl; R 1 is (i) a bond, or (ii) -C(R 10 )(R 11 )-*, -C(R 10 )(R 11 )-O-*, -C(R 10 )(R 11 )CH 2 -*, Or -CH 2 C(R 10 )(R 11 )-*, wherein the bond indicated by an asterisk is attached to Ring A ring; R 10 is hydrogen and R 11 is hydrogen, (C 1 -C 3 alkyl or -OH; or R 10 and R 11 are both (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 -C 5 )cycloalkyl ring; Ring A is an aromatic ring as specified ion the claims; Z 1 is a moncyclic group as specified in the claims.
摘要翻译：式（I）化合物抑制大麻素受体CB1的正常信号传导活性，因此特别可用于治疗与肥胖和超重直接或间接相关的病症，其中A1是-COOH或四唑基; R 2，R 3，R'2和R'3独立地选自-R 9，-CN，-F，-Cl，-Br，-OR 9或-SR 9; R9是氢，C1-C3烷基，环烷基或完全或部分氟化的C1-C3烷基; R 1是（i）键或（ii）-C（R 10）（R 11） - *，-C（R 10）（R 11）-O- *，-C（R 10）（R 11）CH 2 - CH2C（R10）（R11） - *，其中由星号表示的键连接到环A环上; R10是氢，R11是氢，（C1-C3烷基或-OH;或R10和R11都是（C1-C3）烷基;或R10和R11与它们所连接的碳原子一起形成（C3-C5 ）环烷基环;环A是权利要求书中规定的芳环; Z1是如权利要求中所指定的单环基团。

6. 发明申请

WO2010001166A1 THIAZOLE DERIVATIVES AS GPR 119 MODULATORS 审中-公开
标题翻译：作为GPR 119调节剂的噻唑衍生物
公开(公告)号：WO2010001166A1
公开(公告)日：2010-01-07
申请号：PCT/GB2009/050770
申请日：2009-07-01
申请人： PROSIDION LIMITED , ELSTER, Lisbeth , HOEGBERG, Thomas , MURRAY, Anthony , RECEVEUR, Jean Marie
发明人： ELSTER, Lisbeth , HOEGBERG, Thomas , MURRAY, Anthony , RECEVEUR, Jean Marie
IPC分类号： C07D417/04 , C07D417/14 , A61K31/454 , A61P3/00
CPC分类号： C07D417/14 , C07D417/04
摘要： Compounds of formula (I) or salts, hydrates, solvates or N-oxides thereof formula (I): wherein A, B, R 1 , R 2 and R 8 are as defined herein, are useful for treating or preventing diseases or conditions which are associated with GPR119 receptor signaling, such as diabetes, obesity and metabolic syndrome.
摘要翻译：式（I）化合物或式（I）的盐，水合物，溶剂合物或N-氧化物：其中A，B，R 1，R 2和R 8如本文所定义，可用于治疗或预防与 GPR119受体信号传导，如糖尿病，肥胖症和代谢综合征。

7. 发明申请

WO2007006761A1 DICYCLOALKYLCARBAMOYL UREAS AS GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007006761A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/064028
申请日：2006-07-07
申请人： NOVO NORDISK A/S , MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , JEPPESEN, Lone , KRISTIANSEN, Marit
发明人： MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , JEPPESEN, Lone , KRISTIANSEN, Marit
IPC分类号： C07C275/14 , C07C275/52 , C07C275/62 , A61K31/33
CPC分类号： C07C275/62 , C07C2601/02 , C07C2601/14
摘要： This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
摘要翻译：本发明涉及式（I）的二环烷基氨基甲酰基脲，其为葡糖激酶的活化剂，因此可用于治疗，治疗，控制或辅助治疗疾病，其中葡萄糖激酶活性增加是有益的。

8. 发明申请

WO2011003418A1 HETEROCYCLIC COMPOUNDS AS JAK RECEPTOR AND PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为JAK受体和蛋白酪氨酸激酶抑制剂的杂环化合物
公开(公告)号：WO2011003418A1
公开(公告)日：2011-01-13
申请号：PCT/DK2010/000105
申请日：2010-07-08
申请人： LEO PHARMA A/S , NIELSEN, Simon Feldbæk , GREVE, Daniel, Rodriguez , RYTTERSGAARD, Carsten , GRUE-SØRENSEN, Gunnar , OTTOSEN, Erik, Rytter , POULSEN, Tina, Dahlerup , SCHOU, Søren, Christian , MURRAY, Anthony
发明人： NIELSEN, Simon Feldbæk , GREVE, Daniel, Rodriguez , RYTTERSGAARD, Carsten , GRUE-SØRENSEN, Gunnar , OTTOSEN, Erik, Rytter , POULSEN, Tina, Dahlerup , SCHOU, Søren, Christian , MURRAY, Anthony
IPC分类号： C07D487/04 , C07D487/08 , C07D471/04 , A61K31/437 , A61K31/499 , A61K31/519 , A61P3/00 , A61P17/00 , A61P27/00 , A61P25/00 , A61P35/00 , A61P37/00
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of general formula (I) wherein A, R 1 , R 2 , R 3 , R 4 , R 5 , R 9 , m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.
摘要翻译：本发明涉及通式（I）的化合物，其中A，R 1，R 2，R 3，R 4，R 5，R 9，m和n如本文所定义，及其药学上可接受的盐，水合物或溶剂化物，或与治疗中的一种或多种其它药学活性化合物组合用作用于预防，治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂，包括例如牛皮癣，特应性皮炎，红斑痤疮，狼疮，多发性硬化，类风湿性关节炎，I型糖尿病，哮喘，癌症，自身免疫性甲状腺疾病，溃疡性结肠炎，克罗恩病，阿尔茨海默氏病，白血病，眼睛疾病如糖尿病性视网膜病变和黄斑变性以及其他自身免疫疾病和适应症，其中需要免疫抑制器官移植的例子。

9. 发明申请

WO2007125105A3 BENZAMIDE GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007125105A3
公开(公告)日：2007-11-08
申请号：PCT/EP2007/054173
申请日：2007-04-27
申请人： NOVO NORDISK A/S , MURRAY, Anthony , LAU, Jesper , JEPPESEN, Lone , VEDSØ, Per , POLISETTI, Dharma Rao , GADDAM, Bapu Reddy , CHRISTEN, Daniel P. , SANTHOSH, Kalpathy Chidambareswaran , COOPER, Jeremy T. , ANDREWS, Robert Carl
发明人： MURRAY, Anthony , LAU, Jesper , JEPPESEN, Lone , VEDSØ, Per , POLISETTI, Dharma Rao , GADDAM, Bapu Reddy , CHRISTEN, Daniel P. , SANTHOSH, Kalpathy Chidambareswaran , COOPER, Jeremy T. , ANDREWS, Robert Carl
IPC分类号： C07D277/44 , A61K31/4168 , A61P3/10
摘要： The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase.

10. 发明申请

WO2007006760A1 DICYCLOALKYL UREA GLUCOKINASE ACTIVATORS 审中-公开
公开(公告)号：WO2007006760A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/064026
申请日：2006-07-07
申请人： NOVO NORDISK A/S , MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , KRISTIANSEN, Marit , JEPPESEN, Lone
发明人： MURRAY, Anthony , LAU, Jesper , VEDSØ, Per , KRISTIANSEN, Marit , JEPPESEN, Lone
IPC分类号： C07D277/48 , C07D417/12 , C07D417/04 , C07D417/14 , C07D277/54 , A61K31/426 , A61K31/427 , A61P3/10
CPC分类号： C07D277/54 , C07D277/48 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Dicycloalkyl urea glucokinase activators compounds are glucokinase inhibitors useful for the treatment of diabetes. (I)
摘要翻译：二环烷基脲葡糖激酶活化剂化合物是可用于治疗糖尿病的葡糖激酶抑制剂。（一世）

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