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19 条记录 (耗时 0.026 秒)

    CB1 receptor modulators
    7.
    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.

    Quinoline compounds for use in mch receptor related disorders
    8.
    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。

    CRTH2 receptor ligands for medicinal uses
    9.
    发明授权
    CRTH2 receptor ligands for medicinal uses 失效
    用于药用的CRTH2受体配体

    公开(公告)号：US08022063B2

    公开(公告)日：2011-09-20

    申请号：US11597873

    申请日：2005-05-30

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

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

    IPC分类号： A01N43/00 ,  C07D231/00

    CPC分类号： A61K31/415 ,  A61K31/454 ,  C07D231/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/34

    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 A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, 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; t is 0 or 1; L2 and L3 are linker radicals 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，其中A表示羧基-COON或羧基生物电子等排体; A1，是氢或甲基; 环Ar1是任选取代的苯环5-或6-元单环杂芳基环，其中AA1CHO-和L2与相邻的环原子连接; 环A 2，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-元碳环或杂环组成的双环系统，其被苯并稠合或稠合至5-或 6元单环杂芳基环，所述环或环系统任选被取代; t为0或1; L2和L3是如说明书中定义的连接基团。

    CRTH2 Receptor Ligands For Medicinal Uses
    10.
    发明申请
    CRTH2 Receptor Ligands For Medicinal Uses 失效
    CRTH2受体配体用于药用

    公开(公告)号：US20090099189A1

    公开(公告)日：2009-04-16

    申请号：US11597873

    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 ,  C07D263/32 ,  A61K31/421 ,  C07D403/02 ,  C07D231/12 ,  A61K31/415

    CPC分类号： A61K31/415 ,  A61K31/454 ,  C07D231/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/34

    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 A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, 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; t is 0 or 1; L2 and L3 are linker radicals 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，其中A表示羧基-COON或羧基生物电子等排体; A1，是氢或甲基; 环Ar1是任选取代的苯环5-或6-元单环杂芳基环，其中AA1CHO-和L2与相邻的环原子连接; 环A 2，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-元碳环或杂环组成的双环系统，其被苯并稠合或稠合至5-或 6元单环杂芳基环，所述环或环系统任选被取代; t为0或1; L2和L3是如说明书中定义的连接基团。