公开(公告)号：EP3082819A1

公开(公告)日：2016-10-26

申请号：EP14871136.9

申请日：2014-12-19

申请人： Signal Pharmaceuticals, LLC

发明人： CASHION, Daniel ,  MORTENSEN, Deborah ,  HUANG, Dehua ,  TORRES, Eduardo ,  PARNES, Jason ,  SAPIENZA, John ,  HANSEN, Joshua ,  LEFTHERIS, Katerina ,  CORREA, Matthew ,  DELGADO, Maria, Mercedes ,  RAHEJA, Raj ,  PAPA, Patrick ,  BAHMANYAR, Sogole ,  HEGDE, Sayee ,  NORRIS, Stephen Tyson ,  PLANTEVIN-KRENITSKY, Veronique ,  CALABRESE, Andrew, Antony ,  CATHERS, Brian, Edwin ,  WHITEFIELD, Brandon, Wade ,  BENNETT, Brydon

IPC分类号： A61K31/506 ,  C07D239/48

CPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.

摘要翻译： 本文提供具有以下结构的二氨基嘧啶化合物：其中X，L，R 1和R 2如本文所定义，包含有效量的二氨基嘧啶基化合物的组合物，以及治疗或预防PKC-θ介导的病症的方法或病症 可通过抑制激酶例如PKC-θ治疗或预防。

公开(公告)号：EP3736268A1

公开(公告)日：2020-11-11

申请号：EP20178220.8

申请日：2014-12-19

申请人： Signal Pharmaceuticals, LLC

发明人： CASHION, Daniel Kurt ,  MORTENSEN, Deborah ,  HUANG, Dehua ,  TORRES, Eduardo ,  PARNES, Jason ,  SAPIENZA, John ,  HANSEN, Joshua ,  LEFTHERIS, Katerina ,  CORREA, Matthew ,  DELGADO, Maria Mercedes ,  RAHEJA, Raj ,  PAPA, Patrick ,  BAHMANYAR, Sogole ,  HEGDE, Sayee ,  NORRIS, Stephen Tyson ,  PLANTEVIN-KRENITSKY, Veronique ,  CALABRESE, Andrew Antony ,  CATHERS, Brian Edwin ,  WHITEFIELD, Brandon Wade ,  BENNETT, Brydon

IPC分类号： C07D239/48 ,  C07D403/06 ,  A61K31/506 ,  A61P3/00 ,  A61P11/00 ,  A61P11/06 ,  A61P17/00 ,  A61P19/00 ,  A61P21/00 ,  A61P37/06 ,  C07D405/14 ,  A61K31/505 ,  A61K31/5377 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： The invention provides a method for preparing a compound of formula (I):

comprising contacting a compound of formula (Ia)

or a compound of formula (Ic)

with R 1 -L-NH 2 , in an organic solvent, in the presence of a base, under conditions as defined herein. Also provided are reaction intermediates involved in said method as defined herein.