发明名称 TRICYCLIC GUANIDINE DERIVATIVE
摘要 Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same.;
申请公布号 US2016083400(A1) 申请公布日期 2016.03.24
申请号 US201514857682 申请日期 2015.09.17
申请人 Sunovion Pharmaceuticals Inc. ;Sumitomo Dainippon Pharma Co., Ltd. 发明人 Burdi Douglas F.;Tanaka Daisuke;Fujiwara Hiroaki
分类号 C07D498/14;C07D487/20;C07D487/14 主分类号 C07D498/14
代理机构 代理人
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are each independently C or N; Ring A is a 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen and sulfur; L1 is a covalent bond, or a C1-4 bivalent straight or branched hydrocarbon chain, wherein one or more hydrogen atoms of the chain are optionally and independently replaced by halogen, and wherein one or two methylene units of the chain are optionally and independently replaced by —N(R)—, —N(R)C(O)—, —C(O)N(R)—, —N(R)C(O)N(R)—, —N(R)C(S)N(R)—, —N(R)S(O)2—, —S(O)2N(R)—, —C(O)—, —OC(O)—, —C(O)O—, —O—, —S—, —S(O)— or S(O)2—; each R1 is independently halogen, —R, —OR, —SR, —N(R)2, —N(R)C(O)R, —C(O)N(R)2, —N(R)C(O)N(R)2, —N(R)C(S)N(R)2, —N(R)C(O)OR, —OC(O)N(R)2, —N(R)S(O)2R, —S(O)2N(R)2, —OC(O)OR, —C(O)OR, —OC(O)R, —C(O)R; —S(O)R, or —S(O)2R; R2 is halogen, —R, —OR, —SR, —N(R)2, —N(R)C(O)R, —C(O)N(R)2, —N(R)C(O)N(R)2, —N(R)C(S)N(R)2, —N(R)C(O)OR, —OC(O)N(R)2, —N(R)SO2R, —S(O)2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, —S(O)2R, or Cy; Cy is a ring, substituted with q instances of R4; wherein said ring is a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring; phenyl; an 8-10 membered bicyclic aromatic carbocyclic ring; a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur; a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur; or an 8-10 membered bicyclic heteroaromatic ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, and sulfur; each R is independently (i) a hydrogen,(ii) a C1-6 aliphatic (said group being optionally substituted with the same or different 1 to 4 group(s) selected from(a) a halogen,(b) a C1-6 alkyl (said group being optionally substituted with the same or different 1 to 3 halogen),(c) a C1-6 alkoxy (said group being optionally substituted with the same or different 1 to 3 halogen),(d) a hydroxy, and(e) an oxo), or(iii) a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring; phenyl; an 8-10 membered bicyclic aromatic carbocyclic ring; a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring; a 5-6 membered monocyclic heteroaromatic ring; or an 8-10 membered bicyclic heteroaromatic ring, wherein each of said groups is optionally substituted with the same or different 1 to 4 group(s) selected from (a) a halogen,(b) a C1-6 alkyl (said group being optionally substituted with the same or different 1 to 3 halogen),(c) a C1-6 alkoxy (said group being optionally substituted with the same or different 1 to 3 halogen),(d) a hydroxy, and(e) a cyano; each R3 is independently halogen, —R, —CN, —OR, —SR, —N(R)2, —N(R)C(O)R, —C(O)N(R)2, —C(O)N(R)S(O)2R, —N(R)C(O)N(R)2, —N(R)C(S)N(R)2, —N(R)C(O)OR, —OC(O)N(R)2, —N(R)S(O)2R, —S(O)2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, —S(O)2R, or —B(OR)2; each R4 is independently halogen, —R, —CN, —OR, —SR, —N(R)2, —N(R)C(O)R, —C(O)N(R)2, —C(O)N(R)S(O)2R, —N(R)C(O)N(R)2, —N(R)C(S)N(R)2, —N(R)C(O)OR, —OC(O)N(R)2, —N(R)S(O)2R, —S(O)2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, —S(O)2R, or —B(OR)2; or two R4 are taken together with their intervening atoms to form a 5-6 membered saturated, partially unsaturated, or aromatic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur; wherein one or more of {two instances of R1}, {R1 and an R2}, and {two instances of R3} may be taken together with their intervening atoms to form a ring, substituted with r instances of R4; wherein said ring is a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring; phenyl; a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur; or a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur; m is 0-4; n is 0-3; p is 0-2; q is 0-5; and r is 0-5.
地址 Marlborough MA US