发明名称 Compounds useful as inhibitors of indoleamine 2,3-dioxygenase
摘要 The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications.;The compounds of this invention have formula I-A:; wherein the variables are as defined herein.
申请公布号 US9499497(B2) 申请公布日期 2016.11.22
申请号 US201514722413 申请日期 2015.05.27
申请人 Vertex Pharmaceuticals Incorporated 发明人 Boyall Dean;Davis Christopher;Dodd James;Everitt Simon;Miller Andrew;Weber Peter;Westcott James;Young Stephen;Settimo Luca
分类号 C07D249/04;C07D401/12;A61K31/4192;A61K45/06;A61K31/4439;C07D403/12;C07D413/12;C07D249/10 主分类号 C07D249/04
代理机构 Wolf, Greenfield & Sacks, P.C. 代理人 Wolf, Greenfield & Sacks, P.C.
主权项 1. A compound of formula I-A:or a pharmaceutically acceptable salt thereof, wherein:n is 0-4; X is halo; Z1, Z2, and Z3 are CH or N, wherein CH is optionally substituted with R1 or X; R1 is independently selected from halo; —CN; QX; or a C1-10aliphatic chain wherein up to four methylene units of the aliphatic chain are optionally replaced with —O—, —NR—, —S—, —C(O)—, S(O)—, or —S(O)2—; R1 is optionally substituted with 0-5 J1 groups; QX is a 3-7 membered monocyclic fully saturated, partially unsaturated, or aromatic ring containing 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; J1 is independently selected from halo; —CN; QY; or a C1-6aliphatic chain wherein up to three methylene units of the aliphatic chain are optionally replaced with —O—, —NR—, —S—, —C(O)—, S(O)—, or —S(O)2—; J1 is optionally substituted with 0-5 J2 groups; or two occurrences of J1 on the same atom, together with the atom to which they are attached, form a 3-6 membered non-aromatic monocyclic ring; the ring formed by two occurrences of J1 on the same atom is optionally substituted with 0-3 J2A groups; or two occurrences of J1, together with QX, form a bridged ring system; QY is independently selected from a 3-7 membered monocyclic fully saturated, partially unsaturated, or aromatic ring containing 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or an 8-12 membered bicyclic fully saturated, partially unsaturated, or aromatic ring containing 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; J2 is independently selected from halo; ═O; —CN; a 3-6 membered aromatic or non-aromatic ring containing 0-3 heteroatoms selected from oxygen, nitrogen, or sulfur; or C1-4aliphatic chain wherein up to two methylene units of the aliphatic chain are optionally replaced with —O—, —NR—, —S—, —C(O)—, S(O)—, or —S(O)2—; J2 is optionally substituted with 0-5 J3 groups; or two occurrences of J2, together with the atom or atoms to which they are attached, form a 3-6 membered aromatic or non-aromatic monocyclic ring; the ring formed by two occurrences of J2 is optionally substituted with 0-3 J3A groups; or two occurrences of J2, together with QY, form a bridged ring system; J2A is independently selected from halo or a C1-4aliphatic chain wherein up to two methylene units of the aliphatic chain are optionally replaced with —O—, —NR—, —S—, —S(O)—, —S(O)2, or —C(O); J3 and J3A are independently selected from halo or C1-4alkyl; and R is independently selected from H or C1-6aliphatic.
地址 Boston MA US