发明名称 Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors
摘要 Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
申请公布号 US8952037(B2) 申请公布日期 2015.02.10
申请号 US201113105873 申请日期 2011.05.11
申请人 Amgen Inc. 发明人 Allen Jennifer R.;Frohn Michael J.;Harrington Paul E.;Hu Essa;Pickrell Alexander J.;Rzasa Robert M.;Sham Kelvin K. C.
分类号 C07D401/12;C07D405/14;A61K31/4433;A61K31/4439;C07D471/04;C07D401/14;C07D403/14;C07D413/14;C07D417/12;C07D417/14;C07D487/04 主分类号 C07D401/12
代理机构 代理人 LeMoine Elsa D.
主权项 1. A compound of formula I: a stereoisomer, or a pharmaceutically-acceptable salt thereof, m is 1, 2, 3, or 4; each of p and q is independently 1; the ring containing p and q is in cis or trans configuration; R1 is C0-4alk-L1; R2 is —C(═O)R5; R3 is H, F, Cl, Br, CN, OH, OC1-4alk, C1-4alk, or C1-4haloalk; R4a is H, C1-4alk, or C1-4haloalk; each R4b and R4c is independently H, F, Cl, Br, CN, OH, OC1-4alk, C1-4alk, or C1-4haloalk; R5 is C0-8alk-L3; Ra is independently H or Rb; Rb is independently phenyl, benzyl, or C1-6alk, wherein said phenyl, benzyl, and C1-6alk are being substituted by 0, 1, 2 or 3 substituents selected from halo, C1-4alk, C1-3haloalk, —OH, —OC1-4alk, —NH2, —NHC1-4alk, —OC(═O)C1-4alk, or —N(C1-4alk)C1-4alk; and L1 is cyclobutyl, cyclohexyl, cyclopentyl, cycloheptyl, phenyl, dihydropyranyl, or tetrahydropyranyl, and L3 is benzimidazolyl, wherein each of L1 and L3 is independently substituted by 0, 1, 2 or 3 R8 groups which are F, Cl, Br, C1-6alk, C1-4haloalk, —ORa, —OC1-4haloalk, CN, —C(═O)Rb, —C(═O)ORa, —C(═O)NRaRa, —C(═NRa)NRaRa, —OC(═O)Rb, —OC(═O)NRaRa, —OC2-6alkNRaRa, —OC2-6alkORa, —SRa, —S(═O)Rb, —S(═O)2Rb, —S(═O)2NRaRa, —NRaRa, —N(Ra)C(═O)Rb, —N(Ra)C(═O)ORb, —N(Ra)C(═O)NRaRa, —N(Ra)C(═NRa)NRaRa, —N(Ra)S(═O)2Rb, —N(Ra)S(═O)2NRaRa, —NRaC2-6alkNRaRa, —NRaC2-6alkORa, —C1-6alkNRaRa, —C1-6 alkORa, —C1-6 alkN(Ra)C(═O)Rb, —C1-6 alkOC(═O)Rb, —C1-6 alkC(═O)NRaRa, —C1-6alkC(═O)ORa or oxo.
地址 Thousand Oaks CA US