发明名称 NOVEL METHODS
摘要 The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
申请公布号 US2016310502(A1) 申请公布日期 2016.10.27
申请号 US201415101874 申请日期 2014.12.03
申请人 INTRA-CELLULAR THERAPIES, INC. 发明人 Vanover Kimberly;Li Peng;Mates Sharon;Davis Robert;Wennogle Lawrence P.
分类号 A61K31/5383;A61K9/00;A61K31/4985;A61K45/06 主分类号 A61K31/5383
代理机构 代理人
主权项 1. A method for the treatment of residual symptoms, comprising administering to a patient in need thereof an effective amount of a compound of Formula I:wherein: X is —O—, —NH— or —N(CH3)—; Y is —O—, —C(R2)(OH)—, —C(R3)(OR1) or —C(O)—; and R1 is —C1-6 alkyl (e.g., methyl) or —C(O)—C1-21 alkyl (e.g., —C(O)—C1-5alkyl, —C(O)—C6-15alkyl or —C(O)—C16-21alkyl), preferably said alkyl is a straight chain, optionally saturated or unsaturated and optionally substituted with one or more hydroxy or C1-22alkoxy (e.g., ethoxy) groups, for example R1 is —C(O)—C6alkyl, —C(O)—C7alkyl, —C(O)—C9alkyl, —C(O)—C11alkyl, —C(O)—C13alkyl or —C(O)—C15alkyl wherein such compound hydrolyzes to form the residue of a natural or unnatural, saturated or unsaturated fatty acid, e.g., the compound hydrolyzes to form the hydroxy compound on the one hand and octanoic acid, decanoic acid, dodecanoic acid, tetradecanoic acid or hexadecanoic acid on the other hand); R2 is H or —C1-6alkyl (e.g., methyl); and R3 is H or —C1-6 alkyl (e.g., methyl);in free or pharmaceutically acceptable salt form.
地址 New York NY US