DERIVADOS DE HETEROCICLILO OPCIONALMENTE CONDENSADOS DE PIRIMIDINA UTILES PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS, METABOLICAS, ONCOLOGICAS Y AUTOINMUNITARIAS
SCHRØDER GLAD, Sanne Ormholt,GRØN NØRAGER, Niels Henrik,SARVARY, Ian David,HAAHR GOULIAEV, Alex,TEUBER, Lene,STASI, Luigi Piero
申请号：
PE0001662017
公开号：
PE06842017A1
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 Condensed pyrimidine Derivative 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, R2 is H, among others Halogen, among others C1 - C6 R3A is alkyl, alkoxy optionally substituted C1 - C6, among others and R3C r3b are h, CNAmong others, or combine to form an oxo Group R4A is H, halogen, among others r4b is H, Oxo, among others R5 is por12 (cr8r9), among others n and P are integers from 0 to 4 r6a and R6B are h, halogen, alkyl of C1 - C6, among Others R8, R9 and R12 are H c1-c6 alkyl, optionally substituted, among other S b is a Ring system as aryl, heteroaryl, among others.It is a compound selected: N6 - 2-cyclopropyl-1 - 5 - fluoro - N4 - [[4 - (1h tetrazole - 5 - methyl) phenyl] methyl] - N6 - [[4 - (trifluoromethyl) phenyl] methyl] - 4.6 - pyrimidine diamine among others. It also relates to a composition. These compounds modulate the activity of an Orphan Receptor associated with the retinoic acid receptor (ROR).This Compound is useful in the treatment of inflammatory and autoimmune diseases, MetabolicSe refiere a un derivado de heterociclilo opcionalmente condensado de pirimidina 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 R3a es alquilo C1-C6, alcoxi C1-C6 opcionalmente sustituidos, entre otros R3b y R3c son H, -CN, entre otros o se combinan para formar un grupo oxo R4a es H, halogeno, entre otros R4b es H, oxo, entre otros R5 es (CR8R9)pOR12, entre otros n y p son enteros de 0 a 4 R6a y R6b son H, halogeno, alquilo C1-C6, entre otros R8, R9 y R12 son H, alquilo C1-C6 opcionalmente sustituido, entre otros B es un sistema de anillo tal como arilo, heteroarilo, entre otros. Es un compuesto seleccionado: N6-ciclopropil-5-fluoro-N4-[[4-(1H-tetrazol-5
