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    CB1 receptor modulators
    1.
    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.

    Cannabinoid Receptor Modulators
    2.
    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。

    Quinoline compounds for use in mch receptor related disorders
    3.
    发明申请
    Quinoline compounds for use in mch receptor related disorders 审中-公开
    用于mch受体相关疾病的喹啉化合物

    公开(公告)号：US20060111357A1

    公开(公告)日：2006-05-25

    申请号：US10538455

    申请日：2003-12-11

    申请人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Pia Norregaard ,  Paul Little ,  Jean-Marie Receveur

    发明人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Pia Norregaard ,  Paul Little ,  Jean-Marie Receveur

    IPC分类号： A61K31/519 ,  A61K31/517 ,  A61K31/498 ,  A61K31/4745 ,  A61K31/525 ,  A61K31/4709

    CPC分类号： C07D401/04 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519

    摘要： The present invention relates to the use of quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel quinoline compounds per se. The quinoline compounds have been found to interact with a melanin-concentrating hormone receptor, a MCH receptor. The compounds have modulating activity on the MCH receptor such as e.g. antagonistic, agonistic or allosteric activity and are useful for medicinal or cosmetic purposes such as, e.g. in the treatment or prevention of feeding disorders like obesity, metabolic syndrome, Type II diabetes, bulimia, etc. or in the treatment or prevention of depression.

    摘要翻译： 本发明涉及喹啉化合物在制备药物和/或化妆品组合物中的用途，用于治疗，预防和/或诊断由黑色素浓缩激素引起或涉及的病症。 本发明还涉及新的喹啉化合物本身。 已发现喹啉化合物与黑色素浓缩激素受体MCH受体相互作用。 这些化合物对MCH受体具有调节活性，例如。 拮抗，激动或变构活性，并且可用于药物或化妆品目的，例如。 治疗或预防肥胖症，代谢综合征，II型糖尿病，食欲过盛等进食障碍，或治疗或预防抑郁症。

    CB1 RECEPTOR MODULATORS
    7.
    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。

    Oxadiazole Derivatives with Crth2 Receptor Activity
    8.
    发明申请
    Oxadiazole Derivatives with Crth2 Receptor Activity 审中-公开
    具有Crth2受体活性的恶二唑衍生物

    公开(公告)号：US20080312220A1

    公开(公告)日：2008-12-18

    申请号：US12094907

    申请日：2006-11-22

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

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

    IPC分类号： A61K31/541 ,  C07D271/06 ,  A61K31/4245 ,  A61K31/454 ,  C07D417/12 ,  C07D413/12 ,  A61K31/5377

    CPC分类号： C07D271/06 ,  C07D413/04

    摘要： Compounds of formula are CRTH2 ligands, useful for treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein R1 is hydrogen or methyl and R2 is optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having to 6 ring atoms; or R1 and R2, taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl having 4 to 6 ring atoms: or R1 and R2, taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl, or optionally substituted cycloalkyl, or optionally substituted non-aromatic heterocyclyl ring having 4 to 6 ring atoms; R is hydrogen or an optional substitutent by 1, 2 or 3 optional substituents; A is hydrogen or C1-C3 alkyl; and ring Ar is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring.

    摘要翻译： 式的化合物是可用于治疗炎性，自身免疫，呼吸或过敏疾病的CRTH2配体：其中R1是氢或甲基，R2是任选取代的环烷基，或任选取代的具有6个环原子的非芳族杂环基; 或R 1和R 2与它们所连接的碳原子一起形成任选取代的环烷基，或任选取代的具有4-6个环原子的非芳族杂环基：或R 1和R 2与它们所在的碳原子一起 连接形成任选取代的环烷基，或任选取代的环烷基，或任选取代的具有4-6个环原子的非芳族杂环基; R是氢或任选的1,2或3个任选取代基的取代基; A是氢或C 1 -C 3烷基; 并且环Ar是任选取代的苯基或5-或6-元单环杂芳基环。

    Substituted Thiazoleacetic Acid as Crth2 Ligands
    9.
    发明申请
    Substituted Thiazoleacetic Acid as Crth2 Ligands 审中-公开
    取代噻唑乙酸作为Crth2配体

    公开(公告)号：US20080119456A1

    公开(公告)日：2008-05-22

    申请号：US11597839

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg ,  Jean-Marie Receveur ,  Marie Grimstrup

    IPC分类号： A61K31/53 ,  A61K31/506 ,  A61K31/55 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D277/30 ,  C07D417/04 ,  C07D417/06

    摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N═N—. —NR7—, —CR7═CR8—, —CR7═N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.

    摘要翻译： 式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎; 其中X 1是-S - ， - O - ， - N-N-。 -NR 7 - ，-CR 7 -CR 8 - ，-CR 7-N-，其中R R 7和R 8独立地是氢或C 1 -C 3烷基; A是羧基-COOH或羧基生物电子等排体; 环Ar 2和Ar 3各自独立地表示苯基或5或6元单环杂芳基环，或由5-或6-元环组成的双环系统 苯并稠合或稠合到5-或6-元单环杂芳基环的碳环或杂环，所述环或环系统任选被取代; 环B如Ar 2和Ar 3所定义，或任选取代的N-吡咯烷基，N-哌啶基或N-氮杂环丁基环; s为0或1; L1，L2和L4是描述中定义的连接基团; Q 1和Q 2表示如说明书中定义的取代基。