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    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS
    2.
    发明申请
    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
    一致的约束，全合成大环化合物

    公开(公告)号：US20120202821A1

    公开(公告)日：2012-08-09

    申请号：US13388891

    申请日：2009-08-05

    申请人： Daniel Obrecht ,  Philipp Ermert ,  Said Oumouch ,  Franck Lach ,  Anatol Luther ,  Karsten Marx ,  Kerstin Möhle

    发明人： Daniel Obrecht ,  Philipp Ermert ,  Said Oumouch ,  Franck Lach ,  Anatol Luther ,  Karsten Marx ,  Kerstin Möhle

    IPC分类号： A61K31/407 ,  A61K31/4985 ,  A61K31/4745 ,  A61P1/00 ,  A61P15/06 ,  A61P25/06 ,  A61P25/18 ,  A61P25/24 ,  A61P27/02 ,  A61P27/06 ,  C07D498/04 ,  A61P25/00

    CPC分类号： C07D498/04 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4985 ,  C07D497/18 ,  C07D498/18

    摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.

    摘要翻译： 构形限制的（I）型的空间定义的12-30元大环环体系由描述和权利要求书中详细描述的三个不同的构成单元构成：芳族模板a，构象调节剂b和间隔子部分c。 类型（I）的大环化合物容易通过平行合成或组合化学制备。 它们旨在与具体的生物目标相互作用。 特别地，它们表现出对胃动素受体（MR受体），5-HT2B（5-HT2B受体）5型血清素受体和前列腺素F2受体（FP受体）的激动作用或拮抗作用。 因此，它们可用于治疗胃肠道的运动障碍，如糖尿病性胃轻瘫和便秘型肠易激综合征; CNS相关疾病如偏头痛，精神分裂症，精神病或抑郁症; 的高眼压症如青光眼和早产。

    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS
    4.
    发明申请
    CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
    一致的约束，全合成大环化合物

    公开(公告)号：US20120270881A1

    公开(公告)日：2012-10-25

    申请号：US13508531

    申请日：2010-08-03

    申请人： Daniel Obrecht ,  Philipp Ermert ,  Said Oumouch ,  Franck Lach ,  Anatol Luther ,  Karsten Marx ,  Kerstin Möhle

    发明人： Daniel Obrecht ,  Philipp Ermert ,  Said Oumouch ,  Franck Lach ,  Anatol Luther ,  Karsten Marx ,  Kerstin Möhle

    IPC分类号： C07D273/02 ,  C07D273/00 ,  A61K31/4985 ,  A61K31/437 ,  A61P1/00 ,  A61P19/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61K31/407 ,  A61P25/06

    CPC分类号： C07D498/04 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4985 ,  C07D497/18 ,  C07D498/18

    摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib 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 the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the β-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.

    摘要翻译： 构型限制，式Ia和Ib的空间限定的12-30元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.这些大环Ia和Ib容易通过平行合成或组合化学 溶液或固相。 它们被设计为与多种特异性生物靶标类型相互作用，其实例是对G蛋白偶联受体（GPCR），离子通道和信号转导通路的激动或拮抗活性。 特别地，这些大环化合物作为拮抗剂作为拮抗剂，作为5-HT2B亚型的5-羟色胺受体的调节剂作为电压门控钾通道Kv1.3的阻断剂，作为抑制剂，作为拮抗剂受体，FP受体和嘌呤能受体P2Y1 连接蛋白依赖的规范Wnt通路。 因此，它们作为各种疾病的药物具有巨大的潜力。