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    Cannabinoid Receptor Modulators
    1.
    发明申请
    Cannabinoid Receptor Modulators 失效
    大麻素受体调节剂

    公开(公告)号：US20100292273A1

    公开(公告)日：2010-11-18

    申请号：US12745708

    申请日：2008-12-08

    申请人： Jean Marie Receveur ,  Emelie Bjurling ,  Anthony Murray ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noerregaard ,  Dorthe Almholt

    发明人： Jean Marie Receveur ,  Emelie Bjurling ,  Anthony Murray ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noerregaard ,  Dorthe Almholt

    IPC分类号： A61K31/454 ,  C07D413/06 ,  A61K31/4245 ,  C07D413/14 ,  C07D409/06 ,  C07D231/24 ,  A61K31/415 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P1/16 ,  A61P15/10 ,  A61P25/00

    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(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*. and —CH2—O—C(R10)(R11)—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R3 is hydrogen, (C1-C)alkyl or (C1C3)fluoroalkyl; R4 is a radical of formula -(Alk1)p-(Q1)r (L)s-Q2 wherein p, r, s, Alk1, L, Q1 and Q2 are as specified; or R3and R4 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-Q2 wherein s, L and Q2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, —NH2—, or mono- or di-(C1C3)alkylamino; R5, R6, R7 and R8 are each independently selected from hydrogen —F, —Cl, —Br, —CN, (C1-C3)alkyl, (C1C3)fluoroalkyl, cyclopropyl, and —OR9; R10 is hydrogen, (C1C3)alkyl, hydroxyl or NH2, and R11 is hydrogen or (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)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）烷基或（C1C3）氟烷基; R4是式 - （Alk1）p-（Q1）r（L）s-Q2的基团，其中p，r，s，Alk1，L，Q1和Q2如所规定; 或R 3和R 4与它们所连接的氮一起形成4至7个环原子的环状氨基，其任选被式 - （L）s-Q 2的基团取代，其中s，L和Q2如上所定义 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。

    Cannabinoid receptor modulators
    2.
    发明授权
    Cannabinoid receptor modulators 失效
    大麻素受体调节剂

    公开(公告)号：US08173680B2

    公开(公告)日：2012-05-08

    申请号：US12745708

    申请日：2008-12-08

    申请人： Jean-Marie Receveur ,  Emelie Bjurling ,  Anthony Murray ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noerregaard ,  Dorthe Almholt

    发明人： Jean-Marie Receveur ,  Emelie Bjurling ,  Anthony Murray ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noerregaard ,  Dorthe Almholt

    IPC分类号： A61K31/445 ,  A61K31/41 ,  A61K31/415 ,  C07D401/02 ,  C07D271/06 ,  C07D231/00

    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(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, and —CH2—O—C(R10)(R11)—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is a carboxyl isostere radical selected from the group specified; R3 is hydrogen, (C1-C)alkyl or (C1C3)fluoroalkyl; R4 is a radical of formula -(Alk1)p-(Q1)r (L)s-Q2 wherein p, r, s, Alk1, L, Q1 and Q2 are as specified; or R3and R4 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-Q2 wherein s, L and Q2 are as defined above, or by an optional substituent selected from hydroxy, methoxy, —NH2—, or mono- or di-(C1C3)alkylamino; R5, R6, R7 and R8 are each independently selected from hydrogen —F, —Cl, —Br, —CN, (C1-C3)alkyl, (C1C3)fluoroalkyl, cyclopropyl, and —OR9; R10 is hydrogen, (C1C3)alkyl, hydroxyl or NH2, and R11 is hydrogen or (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)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-CH2-O-C（R10）（R11） - *，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）烷基或（C1C3）氟烷基; R4是式 - （Alk1）p-（Q1）r（L）s-Q2的基团，其中p，r，s，Alk1，L，Q1和Q2如所规定; 或R 3和R 4与它们所连接的氮一起形成4至7个环原子的环状氨基，其任选被式 - （L）s-Q 2的基团取代，其中s，L和Q2如上所定义 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。

    CB1 RECEPTOR MODULATORS
    4.
    发明申请
    CB1 RECEPTOR MODULATORS 有权
    CB1受体调节剂

    公开(公告)号：US20100010061A1

    公开(公告)日：2010-01-14

    申请号：US12519432

    申请日：2007-12-17

    申请人： Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    发明人： Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    IPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/41 ,  C07D257/04 ,  A61P3/10 ,  A61P3/06 ,  A61P9/00 ,  A61P3/00 ,  A61P1/16 ,  A61P25/30 ,  A61P25/00 ,  A61P15/00

    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 A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is (i) a bond, or (ii) —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* or —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q1-A4-[Q2]w- wherein Q1, A4 Q2 and w are as defined in the specification; and R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)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A1是氢，-COOH或四唑基，A2是氢，-COOH或四唑基，条件是A1和A2之一是-COOH或四唑基; p是0或1，A3是苯基或环烷基，其中任一个任选被R 4和/或R 5取代; q为0或1; R3是氢，C1-C4烷基，环烷基，-CF3或-OR9; R4和R5独立地为-R9，-CN，-F，-Cl，-Br，-OR9，-NR7R8，-NR7COR6，-NR7SO2R6，-COR6，-SR9，-SOR9或-SO2R6; R6是C1-C4烷基，环烷基，-CF3或-NR7R8; R7和R8独立地是氢，C1-C4烷基，-CF3或环烷基; R9是氢，C1-C4烷基，环烷基，完全或部分氟化的C1-C4烷基; R1是（i）键或（ii） - （CH2）aB1（CH2）b-，其中a和b独立地为0,1,2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） （R 11） - *，-CH 2 C（R 10）（R 11）-O- *，-CH 2 -O（R 10）（R 11） - *或-C（R 10）（R 11） O-CH2- *，其中由星号表示的键连接到吡唑环上; R2是式-Q1-A4- [Q2] w-的二价基团，其中Q1，A4 Q2和w如说明书中所定义; 和R 10是氢，R 11是（C 1 -C 3）烷基或-OH; 或R 10和R 11均为（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。

    CB1 receptor modulators
    5.
    发明授权
    CB1 receptor modulators 有权

    公开(公告)号：US08124634B2

    公开(公告)日：2012-02-28

    申请号：US12519432

    申请日：2007-12-17

    申请人： Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    发明人： Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    IPC分类号： A61K31/415 ,  A61K31/41 ,  C07D231/12 ,  C07D257/04

    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 A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is (i) a bond, or (ii) —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* or —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q1-A4-[Q2]w- wherein Q1, A4 Q2 and w are as defined in the specification; and R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.

    Modulators of CB1 receptors
    6.
    发明授权
    Modulators of CB1 receptors 有权

    公开(公告)号：US08148404B2

    公开(公告)日：2012-04-03

    申请号：US12518446

    申请日：2007-12-17

    申请人： Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    发明人： Martin Cooper ,  Jean-Marie Receveur ,  Thomas Hoegberg ,  Peter Aadal Nielsen ,  Jean-Michel Linget ,  Pia Karina Noeregaard ,  Anthony Murray ,  Emelie Bjurling

    IPC分类号： A61K31/445 ,  C07D401/14

    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 A1 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 R4 and/or R5; R4 and R5 are independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkoxy(C1-C4 alkyl)-, cycloalkyl, or fully or partially fluorinated C1-C4 alkyl; R1 (i) a bond; (ii) a divalent radical of formula —(CH2)aB1(CH2)b wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3, and B1 is —CO—, -0-, —S—, —SO—, —SO2—, —CH2—, —CHCH3—, —CHOH— or —NR7—; or (iii) a divalent radical selected from —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* and —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is as defined in the specification; R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.

    MEDICINAL USE OF RECEPTOR LIGANDS
    7.
    发明申请
    MEDICINAL USE OF RECEPTOR LIGANDS 审中-公开
    受体配体的药物使用

    公开(公告)号：US20090062317A1

    公开(公告)日：2009-03-05

    申请号：US11658307

    申请日：2005-07-05

    申请人： Jean-Marie Receveur ,  Emelie Bjurling ,  Ann Christensen ,  Thomas Hoegberg

    发明人： Jean-Marie Receveur ,  Emelie Bjurling ,  Ann Christensen ,  Thomas Hoegberg

    IPC分类号： A61K31/517 ,  C07D401/12 ,  A61K31/454 ,  A61K31/4709

    CPC分类号： C07D401/12 ,  C07D239/72 ,  C07D405/14

    摘要： Compounds of formula (I) are ligands of the melanin concentrating hormone-1 receptor (MCH-1R), useful in the treatment of diseases responsive to modulation of melanin concentrating hormone (MCH) activity, for example feeding disorders and diseases for which obesity is a risk factor (I): wherein ring B is selected from specific substituted phenyl or benz-fused 5 membered N-containing heterocycles defined in the specification; R, is attached to a ring carbon of ring B, and represents hydrogen, F, Cl, or —OCH3; X is ═CH— or ═N—; L, is —CH2— or —CH2CH2—; L2 is a bond, —CH2— or —CO—; R2 is H or C, —C3 alkyl, or —N(R2) L, —is selected from specific cyclic amino linker radicals as defined in the specification; ring A is selected from specific N-containing heterocyclic rings as defined in the specification.

    摘要翻译： 式（I）化合物是黑色素浓缩激素-1受体（MCH-1R）的配体，其可用于治疗对黑色素浓缩激素（MCH）活性的调节作用的疾病，例如喂食障碍和肥胖症 风险因子（I）：其中环B选自说明书中定义的特定取代的苯基或苯并稠合的5元N型杂环; R 2连接到环B的环碳上，代表氢，F，Cl或-OCH 3; X是-CH-或-N-; L，是-CH 2 - 或-CH 2 CH 2 - ; L 2是键，-CH 2 - 或-CO-; R2是H或C 1 -C 3烷基或-N（R 2）L - 选自如说明书中所定义的特定的环状氨基接头基团; 环A选自说明书中定义的特定的含N的杂环。