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Chromane Derivatives, isocromano and dihidroisobenzofuranos as negative modulators of alostÉricos mGluR2, compositions and its use
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
申请号:
ARP170102642
公开号:
AR109714A1
申请日:
2017.09.25
申请国别(地区):
AR
年份:
2019
代理人:
摘要:
This application provides isocromano chromane Compounds, and dihidroisobenzofurano replaced or a pharmaceutically acceptable Salt of the same.The compounds are useful as non competitive antagonists of mGluR2 or negative allosteric modulators of mGluR2 (Nam),Procedures and may be useful in patient treatment for Diseases or disorders in which the Receiver - Nam mGluR2 is involved, such as Alzheimer's diseaseCognitive impairment, Schizophrenia, and other mood disorders, Pain Disorders and Sleep DisordersBy the Administration to the patient of a therapeutically effective amount of a compound of the present, or a pharmaceutically acceptable Salt thereof.It also relates to pharmaceutical compositions comprising a Compound, or a pharmaceutically acceptable Salt thereof,(optionally in combination with one or more additional Active Ingredients), and a pharmaceutically acceptable vehicle,And the use of the compounds and Pharmaceutical compositions in the treatment of such diseases.Claim 1: a compound of formula (1) or a stereoisomer thereof, or a pharmaceutically acceptable Salt of the compound or the stereoisomer,In which the ring is a rest: the selected Group compounds of formulas (2), in which: R² ciclopropilo is selected from h, alkyl, alkyl c₁₋₄ c₁₋₄, - Oh, - c₁₋₄ och₃ alkyl -,- halógenoalquilo c₁₋₄, c₁₋₄ - alkyl - or - halógenoalquilo c₁₋₄, CH (ch₃) ₂ ch₂ -, - or - halógenoalquilo c₁₋₄, CH (ch₃) - or - halógenoalquilo c₁₋₄,- ch₂ - NH - N - and - halógenoalquilo c₁₋₄ ch₂ (ch₃) - halógenoalquilo c₁₋₄; r²a is selected from H and H is selected r³ Methyl; Methyl; Methyl r³a is selected from H and B Ring; the rest is selectedHeteroaryl phenyl group consisting of,, and cicloalquenilo cycloalkyl - c₅₋₆ - c₅₋₆; n is 0, 1, 2 or 3,Under the condition that the value of n does not exceed the maximum number of hydrogen Atoms substituted in the B Ring; and each r¹ (when present) is selected regardless of the Group consisTente in Halogen, - CN, - Oh, - - c₁₋₆ alkyl, o-alkyl c₁₋₆, halóg
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