MOLLARD Aleksis (US),МОЛЛАРД Алексис (US),UORNER Stiven L. (US),УОРНЕР Стивен Л. (US),FLINN Geri A. (US),ФЛИНН Гэри А. (US),VANKAYALAPATI Khariprasad (US),ВАНКАЯЛАПАТИ Харипрасад (US),BIRSS Devid Dzh.
申请号：
RU2015143542
公开号：
RU0002693480C2
申请日:
2014.03.13
申请国别(地区):
RU
年份:
2019
代理人:
摘要：
FIELD: chemistry； pharmaceutics.SUBSTANCE: invention relates to a new compound of formula (I) or a pharmaceutically acceptable salt thereof. Compounds have the properties of ALK2 and/or JAK2 kinase inhibitors. Compounds show selective activity with respect to ALK2 relative to JAK2. Inhibition of ALK2 activity reduces the number of sudden exacerbations of a child's genetic disease, called progressive ossificating fibrodysplasia (FOR). In formula (I)A denotes 6-member heteroaryl ring containing a nitrogen atom； X is -NH-； R1 is H, halogen or C1-C6 alkoxy group； R2 is halogen or C1-C6 alkoxy group； R3 is halogen, C1-C6 alkoxy group or -(CH2)nNRaRb； R4 is H； R5 is H； each of R6 and R7 independently is H, halogen, hydroxyl, C1-C6 alkyl, C1-C6 cyanoalkyl or C3-C6 cyanocycloalkyl； R8 is 6-member heteroaryl containing a nitrogen atom, optionally substituted alkylaminoalkyl； each of Ra and Rb independently is -H, C1-C6 alkyl, C1-C6 hydroxyalkyl, or Ra and Rb together with nitrogen atom, to which they are attached, form 5- or 6-member is a saturated carbocyclic or heterocyclic ring optionally substituted with one or more substituents selected from C1-C6 alkyl, C1-C6 carboxyalkylcarbonyl and C1-C6 hydroxyalkyl； n equals 0 or 1； and z equals 0 or 1. Invention also relates to a method of producing compounds of formula I. Method is carried out according to the following scheme.Values of radicals correspond to values specified above. LG and LG' represents a leaving group - halogen.EFFECT: compounds can be used for treating anemia of a chronic disease, anemia of chronic inflammation, anemia of oncological disease or progressive ossificating fibrodysplasia, as well as for treating myeloproliferative disorder, lymphoma, solid tumor, glioma, fibrodysplasia.44 cl, 9 dwg, 2 tbl, 2 exИзобретение относится к новому соединению формулы (I) или его фармацевтически приемлемой соли. Соединения обладают свойствами ингибиторов киназы ALK2 и/или киназы JAK2. При этом соединения проявляют селекти
