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chroman, isochroman and dihydroisobenzofuran derivatives as negative allosteric modulators of mglur2, compositions and their use

机译:chroman2的变构调节剂的苯并二氢吡喃,异苯并二氢吡喃和二氢异苯并呋喃衍生物,组合物及其用途

摘要

The present invention provides certain substituted chroman, isochroman and dihydroisobenzofuran compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein ring a is a moiety selected from: (ii), (iii), (iv) and ( v), and ring b, n, r1, r2, r2a, r3 and r3a are as defined herein. The compounds of the invention are useful as mglur2 inhibitors or mglur2 negative allosteric modulators (nams), and may be useful in methods of treating a patient for diseases or disorders in which the mglur2 nam receptor is involved, such as alzheimer's disease. cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention or a pharmaceutically acceptable salt thereof (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and to the use of the compounds and pharmaceutical compositions of the invention. in the treatment of such diseases.
机译:本发明提供了式(I)的某些取代的苯并二氢吡喃,异苯并二氢呋喃和二氢异苯并呋喃化合物或其药学上可接受的盐,其中环a是选自以下的部分:(ii),(iii),(iv)和(v),和环b,n,r1,r2,r2a,r3和r3a如本文所定义。本发明的化合物可用作mglur2抑制剂或mglur2阴性变构调节剂(nams),并且可用于治疗患者涉及mglur2 nam受体的疾病或失调的方法,例如阿尔茨海默氏病。认知障碍,轻度认知障碍,精神分裂症和其他情绪障碍,疼痛障碍和睡眠障碍,方法是向患者给药治疗有效量的本发明化合物或其药学上可接受的盐。本发明还涉及包含本发明的化合物或其药学上可接受的盐(任选地与一种或多种其他活性成分组合)和药学上可接受的载体的药物组合物,以及所述化合物和药物组合物的用途。本发明。在治疗这类疾病。

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