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    CRTH2 Receptor Ligands For Medicinal Uses
    2.
    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。

    CRTH2 Receptor Ligands For Therapeutic Use
    4.
    发明申请
    CRTH2 Receptor Ligands For Therapeutic Use 审中-公开
    CRTH2受体配体用于治疗用途

    公开(公告)号：US20090105218A1

    公开(公告)日：2009-04-23

    申请号：US11597938

    申请日：2005-05-30

    申请人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg

    发明人： Trond Ulven ,  Thomas Frimurer ,  Oystein Rist ,  Evi Kostenis ,  Thomas Hogberg

    IPC分类号： A61K31/196 ,  A61K31/44 ,  A61K31/381 ,  A61K31/341 ,  A61K31/5375 ,  A61K31/445 ,  A61K31/55 ,  A61P17/00 ,  A61P25/00 ,  A61P1/00 ,  A61P11/00

    CPC分类号： A61K31/245 ,  A61K31/196 ,  A61K31/341 ,  A61K31/40 ,  A61K31/4453 ,  A61K31/5375 ,  A61K31/55 ,  A61K31/63 ,  A61K31/635

    摘要： Compounds of formula (I) are useful in the treatment of disease responsive to modulation of CRTH2 receptor activity, wherein: A represents a carboxyl group —COOH, or a carboxyl bioisostere; L1 is a bond, —CH2—, —OCH2—, —CH2CH2— or —CH═CH—; L2 is CONH—, —NHCO—, SO2NR1—, —NR1SO2 wherein R1 is hydrogen or C1-C3 alkyl, or a divalent radical of formula (X) or (Y), wherein ring Q is a non aromatic heterocyclic ring containing 5 to 7 ring atoms, including the nitrogen shown; L3 is a divalent linker radical of formula -(Alk1)m-(Z)n-(Alk2)p as defined in the description; ring Ar1 is an optionally substituted divalent phenyl radical or divalent 5- or 6-membered monocyclic heteroaryl radical, in which L1 and the H[B]sL3L2Ar2CONH-radical are linked to adjacent ring carbon atoms; ring Ar2 is an optionally substituted 1,3-phenylene radical, or an optionally substituted divalent 5- or 6-membered monocyclic heteroaryl radical, in which AL1Ar1NHCO-radical and the H[B]sL3L2-radical are linked to ring carbon atoms which are not in ortho relationship; ring B is as defined for Ar2, or an optionally substituted cycloalkyl, N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; and s is 0 or 1.

    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，其中：A表示羧基-COOH或羧基生物电子等排体; L 1是键，-CH 2 - ， - OCH 2 - ， - CH 2 CH 2 - 或-CH-CH-; L2是CONH，-NHCO-，SO2NR1，-NR1SO2，其中R1是氢或C1-C3烷基，或式（X）或（Y）的二价基团，其中环Q是非芳族杂环， 7个环原子，包括所示的氮; L3是描述中定义的式 - （Alk1）m-（Z）n-（Alk2）p的二价连接基团; 环Ar1是任选取代的二价苯基或二价5-或6-元单环杂芳基，其中L1和H [B] sL3L2Ar2CONH-基团与相邻的环碳原子连接; 环Ar2是任选取代的1,3-亚苯基或任选取代的二价5-或6-元单环杂芳基，其中AL1Ar1NHCO-基和H [B] sL3L2-自由基与环碳原子连接， 不在邻近关系; 环B如Ar 2所定义，或任选取代的环烷基，N-吡咯烷基，N-哌啶基或N-氮杂环基; s为0或1。

    Substituted Thiazoleacetic Acid as Crth2 Ligands
    5.
    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。

    Ghrelin receptor inverse agonists for regulation of feeding behaviors
    6.
    发明申请
    Ghrelin receptor inverse agonists for regulation of feeding behaviors 审中-公开
    用于调节饲养行为的生长素释放肽受体反向激动剂

    公开(公告)号：US20060025344A1

    公开(公告)日：2006-02-02

    申请号：US11158348

    申请日：2005-06-20

    申请人： Birgitte Lange ,  Thue Schwartz ,  Thomas Frimurer ,  Oystein Rist

    发明人： Birgitte Lange ,  Thue Schwartz ,  Thomas Frimurer ,  Oystein Rist

    IPC分类号： A61K38/22 ,  C07K14/575

    CPC分类号： G01N33/74 ,  A61K31/00 ,  A61K38/046 ,  G01N2333/726 ,  G01N2500/02

    摘要： Compounds of the invention act as inverse agonist ghrelin receptors. Some of the compounds of the invention may have both inverse agonistic and antagonistic properties as they both decrease or eliminate the constitutive activity of he ghrelin receptor and block the effect of ghrelin. Other preferred compounds of the invention have inverse agonistic properties but have little or no antagonistic activity. The compounds are suitable for medical and/or cosmetic use in connection with modulation of feeding behaviors, body composition and reduction of body mass. The invention also relates to methods for identifying inverse agonists for the ghrelin receptor and for monitoring the further development of such compounds.

    摘要翻译： 本发明的化合物作为反向激动剂ghrelin受体。 本发明的一些化合物可以具有反向激动和拮抗性质，因为它们都降低或消除了生长素释放肽受体的组成型活性并阻断了生长素释放肽的作用。 本发明的其它优选化合物具有反向激动性质但具有很少或没有拮抗活性。 该化合物适用于与调节进食行为，身体组成和减少体重有关的医疗和/或化妆品用途。 本发明还涉及用于鉴定生长素释放肽受体的反向激动剂并监测这些化合物的进一步发展的方法。