DERIVADOS DE PIRIMIDINA SUSTITUIDOS CON HETEROCICLILO OPCIONALMENTE CONDENSADOS UTILES PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS, METABOLICAS, ONCOLOGICAS Y AUTOINMUNITARIAS
SCHRØDER GLAD, Sanne Ormholt,BIRKEBÆK JENSEN, Kim,GRØN NØRAGER, Niels Henrik,SARVARY, Ian David,VESTERGAARD, Mikkel,HAAHR GOULIAEV, Alex,TEUBER, Lene,STASI, Luigi Piero
申请号：
PE0001672017
公开号：
PE06822017A1
申请日:
2015.07.31
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to a heterociclilo optionally substituted pyrimidine derivative with condensate of formula (i), or salts, solvates, hydrates and polymorphs of stereoisomers thereof, wherein: and nr or R is H or c1-c4 alkyl, optionally substituted r1 is H, Oh, among others R2 is H Halogen, Among others R3 is hidogeno, halogen, among others R4A is H, halogen, r4b is H, among othersHalogen, Oxo, among others R5 is por12 (cr8r9), among others m, N and q are integers from 0 to 4 r6a and R6B are h, halogen, alkyl of C1 - C6 optionally replaced, among others, R8, R9 and R12 are H c1-c6 alkyl, optionally substituted, among others B is a Ring system as aryl, heteroaryl,Among others, C is a Ring System between heteroaliciclilo C2 - C9 in which B is attached to a carbon Atom adjacent to the N of the C Ring System the exception is the compound (i).The preferred compounds are the following: - Dimethyl 4,4 - (2R) - 2 - [[4 - [2 - [4 - (trifluoromethyl) phenyl] pyrrolidin-1-yl] pyrimidin-4-yl] amino] pentanamide, (2R) - 2 - [[2 - (5 - fluoro trifluoromethyl) - 6 - (2 - [4 - (trifluoromethyl) phenyl] pyrrolidin-1-yl] pyrimidin-4-yl] amino] - 4.4 - dimethyl pentanamide, among others.These compounds modulate the activity of an Orphan Receptor associated with the retinoic acid receptor (ROR). It also relates to a composition. This Compound is useful in the treatment of inflammatory and autoimmune diseases, MetabolicSe refiere a un derivado de pirimidina sustituido con heterociclilo opcionalmente condensado de formula (I) o las sales, hidratos, solvatos, polimorfos y estereoisomeros de los mismos, donde: Y es NR u O R es H o alquilo C1-C4 opcionalmente sustituido R1 es H, -OH, entre otros R2 es H, halogeno, entre otros R3 es hidogeno, halogeno, entre otros R4a es H, halogeno, entre otros R4b es H, halogeno, oxo, entre otros R5 es (CR8R9)pOR12, entre otros m, n y p son enteros de 0 a 4 R6a y R6b son H, halogeno, alquilo C1-C6 opcionalmente sustituido, entre otros R8, R9 y R12 son H, alquilo C1-C
