会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 8. 发明申请
    • MODULATORS OF CB1 RECEPTORS
    • CB1受体的调节剂
    • WO2008075019A1
    • 2008-06-26
    • PCT/GB2007/004842
    • 2007-12-17
    • 7TM PHARMA A/SCOOPER, MartinRECEVEUR, Jean-MarieHOEGBERG, ThomasNIELSEN, Peter, AadalLINGET, Jean-MichelNOEREGAARD, Pia, KarinaMURRAY, AnthonyBJURLING, Emelie
    • COOPER, MartinRECEVEUR, Jean-MarieHOEGBERG, ThomasNIELSEN, Peter, AadalLINGET, Jean-MichelNOEREGAARD, Pia, KarinaMURRAY, AnthonyBJURLING, Emelie
    • C07D401/06C07D401/14C07D403/06C07D403/14C07D413/14C07D409/14C07D417/14C07D231/12A61K31/4725A61K31/497A61K31/4155A61P3/00
    • C07D231/12C07D401/06C07D401/14C07D403/06C07D403/14C07D409/14C07D413/06C07D413/14C07D417/14
    • 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.
    • 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。