Quinoline derivatives as EP4 antagonists
    24.
    发明授权
    Quinoline derivatives as EP4 antagonists 有权
    喹啉衍生物作为EP4拮抗剂

    公开(公告)号:US08013159B2

    公开(公告)日:2011-09-06

    申请号:US11920275

    申请日:2006-05-15

    IPC分类号: C07D471/00

    CPC分类号: C07D471/04

    摘要: The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R5) group. Pharmaceutical compositions comprising the derivatives of formula (I) are also included.

    摘要翻译: 本发明涉及可用于治疗EP4介导的疾病或病症(例如急性和慢性疼痛,骨关节炎,类风湿性关节炎和癌症)的前列腺素E型受体拮抗剂的喹啉衍生物。 衍生物具有式(I)的以下结构:其中A和B表示氮原子或CH基团,条件是它们不能同时为CH,Q可以表示氮或碳原子,Y和Z 是氮原子,N(O)基或C(R5)基团。 还包括包含式(I)的衍生物的药物组合物。

    EP4 Receptor Agonist, Compositions and Methods Thereof
    26.
    发明申请
    EP4 Receptor Agonist, Compositions and Methods Thereof 审中-公开
    EP4受体激动剂,组合物和方法

    公开(公告)号:US20090105234A1

    公开(公告)日:2009-04-23

    申请号:US11989643

    申请日:2006-07-28

    CPC分类号: C07D413/06

    摘要: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.

    摘要翻译: 本发明涉及前列腺素E2受体的EP4亚型的有效选择性激动剂,它们在治疗青光眼和其它病症中的用途或其制剂,其与患者眼睛中的眼内压升高有关。 本发明还涉及本发明化合物用于介导成骨细胞和破骨细胞的骨建模和重塑过程的用途。