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    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS
    2.
    发明申请
    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 审中-公开
    一致的约束，全合成的大环化合物

    公开(公告)号：WO2013139697A1

    公开(公告)日：2013-09-26

    申请号：PCT/EP2013/055368

    申请日：2013-03-15

    Applicant: POLYPHOR AG

    Inventor： OBRECHT, Daniel ,  ERMERT, Philipp ,  OUMOUCH, Said ,  PIETTRE, Arnaud ,  GOSALBES, Jean-François ,  THOMMEN, Marc

    IPC: C07D273/02 ,  C07D498/04 ,  C07D498/18 ,  C07D515/06 ,  C07D515/18 ,  C07D515/22 ,  C07D291/08 ,  A61K31/395 ,  A61P31/04

    CPC classification number: C07D273/02 ,  C07D291/08 ,  C07D498/04 ,  C07D498/08 ,  C07D498/18 ,  C07D515/06 ,  C07D515/08 ,  C07D515/18 ,  C07D515/22

    Abstract: The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1 ) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

    Abstract translation: 式（I）的构象限制的空间定义的大环环系由三个不同的分子部分构成：模板A，构象调节剂B和桥C.由该环系统I描述的大环通过平行合成或组合化学在溶液中容易地制备 或固相。 它们被设计为与各种特异性生物靶标类型相互作用，例如对G-蛋白偶联受体（GPCR）具有激动作用或拮抗活性，对酶或抗微生物活性的抑制活性。 特别地，这些大环化合物显示对亚型1（ECE-1）和/或半胱氨酸蛋白酶组织蛋白酶S（CatS）的内皮素转化酶的抑制活性，和/或作为催产素（OT）受体的拮抗剂，促甲状腺激素释放激素 （TRH）受体和/或白三烯B4（LTB4）受体和/或作为铃蟾肽3（BB3）受体的激动剂，和/或显示针对至少一种细菌菌株的抗微生物活性。 因此，它们作为各种疾病的药物具有巨大的潜力。

    ヘテロアリールスルホン酸アニリド誘導体及びそれを含有する医薬組成物
    3.
    发明申请
    ヘテロアリールスルホン酸アニリド誘導体及びそれを含有する医薬組成物 审中-公开
    含有它们的异氟烷基衍生物和药物组合物

    公开(公告)号：WO2004089936A1

    公开(公告)日：2004-10-21

    申请号：PCT/JP2004/005056

    申请日：2004-04-08

    Applicant: 大日本製薬株式会社 ,  原田 博史 ,  澤 匡明 ,  水野 和弘 ,  立石 浩貴 ,  賀登 志朗 ,  大植 まゆみ ,  辻内 宏

    Inventor： 原田 博史 ,  澤 匡明 ,  水野 和弘 ,  立石 浩貴 ,  賀登 志朗 ,  大植 まゆみ ,  辻内 宏

    IPC: C07D401/12

    CPC classification number: C07D409/12 ,  C07D209/32 ,  C07D515/06

    Abstract: A novel heteroarylsulfonanilide derivative represented by the general formula [I]. It has potent ß3 receptor-stimulating activity, shows excellent selectivity, and is useful as a ß3 adrenergic receptor agonist having excellent pharmacokinetic activity. [I] [R is optionally substituted heteroaryl; R and R are the same or different and each is hydrogen or lower alkyl; and W is a group represented by the formula [II] or the general formula [III]: [II] (R is hydrogen, etc. and R is optionally substituted lower alkyl, etc., or R and R may be bonded to each other to form linear or branched lower alkylene; and R is hydrogen, halogeno, etc.) [III] (R is hydrogen, etc. and R is hydrogen, optionally substituted lower alkyl, etc., or R and R may be bonded to each other to form linear or branched lower alkylene; R is hydrogen, halogeno, etc.; A is a single bond or optionally fluorinated, linear or branched lower alkylene, etc.; and X is a single bond, oxygen, or sulfur.).]

    Abstract translation: 由通式[I]表示的新型杂芳基磺酰苯胺衍生物。 它具有强大的β3受体刺激活性，显示出优异的选择性，并且可用作具有优异药代动力学活性的β3肾上腺素能受体激动剂。 [I] [R 1]是任选取代的杂芳基; R 2和R 3相同或不同，各自为氢或低级烷基; W为由式[II]或通式[III]表示的基团：[II]（R 4a）为氢等，R 5a为任选取代的低级烷基等， （R 4a）和R 5a彼此键合以形成直链或支链的低级亚烷基; R 6a是氢，卤素等）[III]（R 4b）是氢等， R 5b是氢，任选取代的低级烷基等，或者R 4b和R 5b可以彼此键合形成直链或支链的低级亚烷基; R 6b是氢，卤素等; A 是单键或任选氟化的直链或支链低级亚烷基等; X是单键，氧或硫）。]

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