发明名称 Selective octahydro-cyclopenta[C] pyrrole negative modulators of NR2B
摘要 Compounds that selectively negatively modulate NMDA receptors containing an NR1/NR2B subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
申请公布号 US9540324(B2) 申请公布日期 2017.01.10
申请号 US201414498462 申请日期 2014.09.26
申请人 LUC THERAPEUTICS, INC. 发明人 Anderson David R.;Volkmann Robert A.;Menniti Frank S.
分类号 C07D209/52;C07D403/12;C07D401/04;C07D401/06;C07D401/10;C07D401/12;C07D403/04;C07D403/06;C07D403/10;C07D403/14;C07D413/06;C07D205/04;C07D401/14;C07D487/04 主分类号 C07D209/52
代理机构 Brinks Gilson & Lione 代理人 Brinks Gilson & Lione
主权项 1. A compound of Formula I: or pharmaceutically acceptable salt, tautomer, or stereoisomer thereof wherein: L1 is straight or branched C2-C4 alkyl optionally substituted with one or more substituents selected from the group consisting of OH, D, OR10, NH2, NHR10, and N(R10)(R10′), provided that no more than one oxygen or nitrogen is attached to any carbon; or L1 is selected from the group consisting of —CO—C1-C2alkylenyl-, —S(O)2—, —S(O)2NH—, —C(O)NH—, —C(O)NR10—, —C1-C3alkylenyl-C(O)—C1-C3alkylenyl-, and a bond, wherein the C1-C2 alkylenyl and C1-C3 alkylenyl is optionally substituted with C1-C4 alkyl; Each R10 and R10′ is independently selected from the group consisting of H; O—C1-C5 alkyl; C1-C6 alkyl optionally substituted with one or more substituents selected from the group consisting of OH, O—C1-C5 alkyl, —OP(O)(OH)2, OP(O)O2−2M2, —OC(O)alkyl, —OC(O)Oalkyl, and aryl; and cycloalkyl optionally substituted with one or more substituents selected from the group consisting of OH and O—C1-C5 alkyl;provided that no more than one oxygen is attached to any carbon of R10 and R10′;M is a monovalent metal cation; R1 is aryl optionally substituted with one or more substituents selected from the group consisting of OH, CN, halogen, —O—R10, —OP(O)(OH)2, OP(O)O2−2M2, —SH, —S—R10, C1-C5 alkyl, branched alkyl, —C1-C6haloalkyl, NH2, NHR10, —C1-C6hydroxyalkyl, N(R10)(NR10′), —NHS(O)2R10, —O-alkylaryl, —O—(CH2)—C(O)-aryl, and NHCOR10; M is a monovalent metal cation; or R1 is cycloalkyl; X is selected from the group consisting of H, halogen, OH, O—C1-C6 alkyl, O-branched alkyl, C1-C5 straight alkyl and C1-C5 branched alkyl; Y and Y′ are independently H, F, or methyl; L2 is —(CH2)n— or —(CHR11)n—, or a bond; Each R11 is independently selected from the group consisting of H, —C1-C5 alkylenyl-, —C(O)—C1-C5alkylenyl-, and -alkylenyl-CO-alkylenyl-; R2 is C3-C8cycloalkyl; phenyl, or naphthyl, each of which is optionally substituted with one or more substituents selected from the group consisting of halogen, OH, C1-C6alkyl, OR10, CN, NH2, NHR10, N(R10)(R10′), SH, SR10, SOR10, SO2R10, SO2NHR10, SO2N(R10)(R10′), CONH2, CONR10, and CON(R10)(R10′); and n is 1, 2, or 3.
地址 Cambridge MA US