发明名称 Substituted 2-azabicycles and their use as orexin receptor modulators
摘要 The present invention is directed to compounds of Formula I:; Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
申请公布号 US9611262(B2) 申请公布日期 2017.04.04
申请号 US201514851909 申请日期 2015.09.11
申请人 Janssen Pharmaceutica NV 发明人 Shireman Brock T.;Lebold Terry P.;Dvorak Curt A.;Coate Heather R.;Ziff Jeannie M.;Preville Cathy;Gelin Christine;Chen Gang
分类号 A61K31/47;C07D413/14;C07D401/12;C07D401/14;C07D401/10;C07D471/08;A61K31/435;A61K31/444;A61K31/4436 主分类号 A61K31/47
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A compound of Formula I: or an enantiomer or diastereomer thereof; or a pharmaceutically acceptable salt thereof; wherein ring A is phenyl or a heteroaryl ring selected from pyridyl, thiazolyl, or isoquinolinyl; wherein when ring A is thiazolyl, ring A is optionally substituted with up to 3 substituents selected from R1, R2, R3 or R4, and wherein when ring A is phenyl, pyridyl, or isoquinolinyl, ring A is optionally substituted with up to 4 substituents selected from R1, R2, R3 or R4; R1 is H, alkoxy, halo, triazolyl, thiazolyl, pyridazinyl, pyrimidinyl, oxazolyl, isoxazolyl, oxadiazolyl, pyridyl, phenyl, or pyrazolyl, wherein triazolyl, thiazolyl, pyridazinyl, pyrimidinyl, oxazolyl, isoxazolyl, oxadiazolyl, pyridyl, phenyl or pyrazolyl is optionally substituted with up to two substituents selected from halo or alkyl; R2 is H, alkyl, alkoxy, or halo; Z is NH, N—CH3, N—CH2CH3, N—CH2-cyclopropyl, N—C(═O)CH3, N—CH2CH2OCH3 or O; R3 is H, alkyl, alkoxy, halo, triazolyl, thiazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, oxazolyl, isoxazolyl, oxadiazolyl, pyridyl, phenyl, or pyrazolyl, wherein triazolyl, thiazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, oxazolyl, isoxazolyl, oxadiazolyl, pyridyl, phenyl or pyrazolyl is optionally substituted with up to two substituents selected from halo, alkyl, NO2, or hydroxy-alkoxy; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, benzoxazolyl, pyridazinyl, naphthyridinyl, pyrimidinyl, quinoxalinyl, quinolinyl, or phenyl, wherein the pyridyl, pyrazinyl, benzoxazolyl, pyridazinyl, naphthyridinyl pyrimidinyl, quinoxalinyl, quinolinyl, or phenyl is optionally substituted with up to two substituents selected from halo, alkoxy, hydroxymethyl or alkyl; R6A and R6B are independently selected from H, alkyl, hydroxyalkyl, -alkyl-alkoxy, alkyl-alkoxy-alkoxy, or —CO2-alkyl; wherein one or both of R6A and R6B is other than H; and n is 1 or 2.
地址 Beerse BE