发明名称 IRAK inhibitors and uses thereof
摘要 The present invention provides compounds of the general formula I:; or a pharmaceutically acceptable salt thereof, wherein each variable is as defined and described herein, as inhibitors of one or more interleukin-1 receptor-associated kinases (“IRAK”).
申请公布号 US9518065(B2) 申请公布日期 2016.12.13
申请号 US201414496501 申请日期 2014.09.25
申请人 Nimbus Iris, Inc. 发明人 Romero Donna;Masse Craig E.;Robinson Shaughnessy;Greenwood Jeremy Robert;Harriman Geraldine C.
分类号 A01N43/90;A61K31/519;C07D239/00;C07D471/00;C07D487/00;C07D491/00;C07D513/04;C07D519/00 主分类号 A01N43/90
代理机构 Dechert LLP 代理人 Reid Andrea L. C.;Dechert LLP
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein:Q is N;X is N and Y is C—Rx;Ring A is a 3-7 membered saturated or partially unsaturated carbocyclic ring;R1 is Cy;each R1′ is independently —R2, halogen, —CN, —NO2, —OR, —SR, —N(R)2, —S(O)2R, —S(O)2N(R)2, —S(O)R, —C(O)R, —C(O)OR, —C(O)N(R)2, —C(O)N(R)OR, —N(R)C(O)OR, —N(R)C(O)N(R)2, Cy, or —N(R)S(O)2R;each Cy is an optionally substituted ring selected from a 3-7 membered saturated or partially unsaturated carbocyclic ring or a 4-10 membered saturated or partially unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur;each R is independently hydrogen, or an optionally substituted group selected from C1-6 aliphatic, phenyl, 4-7 membered saturated or partially unsaturated heterocyclic having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or: two R groups on the same nitrogen are taken together with their intervening atoms to form a 4-7 membered saturated, partially unsaturated, or heteroaryl ring having 0-3 heteroatoms, in addition to the nitrogen, independently selected from nitrogen, oxygen, or sulfur;each R2 is independently an optionally substituted group selected from C1-6 aliphatic, phenyl, 4-7 membered saturated or partially unsaturated heterocyclic having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; Rx is hydrogen, —R2, —CN, —NO2, halogen, —C(O)N(R)2, —C(O)OR, —C(O)R, —N(R)2, —NH[Ar], —OR, or —S(O)2N(R)2; Rz is hydrogen, —N(R)2, or —NH[Ar]; [Ar] is a 5-membered heteroaromatic ring substituted by m instances of R1′;L1 is a covalent bond or a C1-6 bivalent hydrocarbon chain 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)S(O)2—, —S(O)2N(R)—, —O—, —C(O)—, —OC(O)—, —C(O)O—, —S—, —S(O)— or —S(O)2—;m is 0-4; andn is 1.
地址 Cambridge MA US