发明名称 Diazepinone derivatives
摘要 The invention relates to compound of the formula I; or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
申请公布号 US9284331(B2) 申请公布日期 2016.03.15
申请号 US201414462813 申请日期 2014.08.19
申请人 Novartis AG 发明人 Behnke Dirk;Carcache David;Ertl Peter;Koller Manuel;Orain David
分类号 A61K31/551;C07D498/04;C07D471/04;A61K45/06;C07D471/14 主分类号 A61K31/551
代理机构 代理人 Madden Laura K.
主权项 1. A method for the treatment of a substance-related disorder through mGluR5 antagonism comprising administration of a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof to a patient in need of treatment thereofwherein A is a fused five- to seven-membered monocyclic ring system which may be aromatic, saturated or unsaturated non-aromatic and which may contain from 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur; R1 is —X2—B2; X2 is bond or C1-3alkylene, wherein one carbon atom of the C1-3alkylene may be replaced by a group selected from carbonyl; oxygen; sulfur; —S(O)—; —S(O)2—; amino, which may be substituted by C1-4alkyl; —NH—C(O)—; —C(O)—NH—; —C(O)—O—; —O—C(O)—; —NH—S(O)2—; —S(O)2—NH—; and —NHC(O)NH—; B2 is a three- to seven-membered monocyclic ring system which may be aromatic, saturated or unsaturated non-aromatic and which may contain from 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur, wherein the ring system may in turn be substituted once or more than once by R6; each R6 independently is halogen, hydroxy, cyano, C1-4alkyl, C1-4halogenalkyl, C1-4alkoxy, or C1-4halogenalkoxy; or two R6 at the same ring atom together are oxo; m is 0, 1, 2, 3 or 4; each R2 independently is halogen, cyano, hydroxy, amino, C1-4alkyl; C1-4halogenalkyl; C1-4hydroxyalkyl; C1-4aminoalkyl; C1-4alkylamino-C1-4alkyl; di-(C1-4alkyl)amino-C1-4alkyl; C1-4alkoxy-C1-4alkyl; C2-4alkenyl; C2-4halogenalkenyl; C2-4alkinyl; C2-4halogenalkinyl; C1-4alkoxy; C1-4halogenalkoxy; C1-4alkyl-amino; di-(C1-4alkyl)amino or C3-6cycloalkyl, wherein one carbon atom of the C3-6cycloalkyl may be replaced by an oxygen atom and wherein the C3-6cycloalkyl may be attached directly to the ring system or via a C1-2alkylene or an oxygen; n is 0, 1, 2, 3 or 4; each R3 independently is halogen, cyano, hydroxy, amino, C1-4alkyl; C1-4halogenalkyl; C1-4hydroxyalkyl; C1-4aminoalkyl; C1-4alkylamino-C1-4alkyl; di-(C1-4alkyl)amino-C1-4alkyl; C1-4alkoxy-C1-4alkyl; C2-4alkenyl; C2-4halogenalkenyl; C2-4alkinyl; C2-4halogenalkinyl; C1-4alkoxy; C1-4halogenalkoxy; C1-4alkyl-amino; di-(C1-4alkyl)amino or C3-6cycloalkyl, wherein one carbon atom of the C3-6cycloalkyl may be replaced by an oxygen atom and wherein the C3-6cycloalkyl may be attached directly to the ring system or via a C1-2alkylene or an oxygen; R4 is hydrogen, halogen, cyano, hydroxy, amino, C1-4alkyl; C1-4halogenalkyl; C1-4hydroxyalkyl; C1-4aminoalkyl; C1-4alkylamino-C1-4alkyl; di-(C1-4alkyl)amino-C1-4alkyl; C1-4alkoxy-C1-4alkyl; C2-4alkenyl; C2-4halogenalkenyl; C2-4alkinyl; C2-4halogenalkinyl; C1-4alkoxy; C1-4halogenalkoxy; C1-4alkyl-amino; di-(C1-4alkyl)amino or C3-6cycloalkyl, wherein one carbon atom of the C3-6cycloalkyl may be replaced by an oxygen atom and wherein the C3-6cycloalkyl may be attached directly to the ring system or via a C1-2alkylene or an oxygen; B1 is a five- to six-membered aromatic ring system, which may contain from 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur, wherein the ring system may in turn be substituted once or more than once by R7; each R7 independently is halogen, cyano, hydroxy, amino, C1-4alkyl; C1-4halogenalkyl; C1-4hydroxyalkyl; C1-4aminoalkyl; C1-4alkylamino-C1-4alkyl; di-(C1-4alkyl)amino-C1-4alkyl; C1-4alkoxy-C1-4alkyl; C2-4alkenyl; C2-4halogenalkenyl; C2-4alkinyl; C2-4halogenalkinyl; C1-4alkoxy; C1-4alkoxy-C1-4alkoxy C1-4halogenalkoxy; C1-4alkyl-amino; di-(C1-4alkyl)amino; C1-4alkoxycarbonyl; or a three- to seven-membered monocyclic ring system which may be aromatic, saturated or unsaturated non-aromatic and which may contain from 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur, wherein the ring system may in turn be substituted once or more than once by R8; each R8 independently is halogen, hydroxy, cyano, C1-4alkyl, C1-4halogenalkyl, C1-4alkoxy, or C1-4halogenalkoxy; or two R8 at the same ring atom together are oxo; or two R7 at adjacent ring atoms atoms form together with said ring atoms a fused five- to seven-membered monocyclic unsaturated non-aromatic ring system which may contain from 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur, wherein the ring system may in turn be substituted once or more than once by R9; each R9 independently is halogen, hydroxy, cyano, C1-4alkyl, C1-4halogenalkyl, C1-4alkoxy, or C1-4halogenalkoxy; or two R9 at the same ring atom together are oxo.
地址 Basel CH