NEW COMPOUNDS OF PYRROLOPYRIMIDINE AS INHIBITORS OF PROTEIN KINASES

FIELD: pharmacology.SUBSTANCE: invention relates to new pyrrolopyrimidine derivatives of the general formula (VIII) having the properties of a cell proliferation inhibitor mediated by the activity of EGFR, BLK, BMX / ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC, or TXK kinase, that can be used to treat and/or prevent a proliferative disorder, cancer or tumour associated with the activity of the said kinases. Such diseases can be represented by sarcoma, squamous cell carcinoma, fibrosarcoma, cervical cancer, stomach cancer, skin cancer, leukemia, lymphoma, lung cancer, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, kidney cancer, prostate cancer, breast cancer, liver cancer, head and neck cancer and pancreatic cancer. In the general formula (VIII) Xis O or NH; Rand Rare hydrogen; n is 0; Ris selected from hydrogen, Calkyl, Ccycloalkyl and -NRR; where alkyl or cycloalkyl is unsubstituted or substituted by hydroxyl or amino; and where each Rand Rare independently selected from hydrogen and Calkyl or Rand Rcan be combined to form a 3 to 10-membered ring; Ris hydrogen; Ris selected from hydrogen and Calkoxy; Ris selected from hydrogen and Calkoxy; Ris selected from hydrogen and halogen; Q is a CRor N; Ris selected from hydrogen, halogen and Calkyl; Ris hydrogen; Ris selected from hydrogen and Calkyl; Ris selected from hydrogen, Calkyl, Cacyl, SO-Calkyl and Ccycloalkyl, wherein each alkyl is unsubstituted or substituted by hydroxyl or halogen; and -NRRisor, where Ris selected from hydrogen and Calkyl; Ris unsubstituted methyl or represents Calkyl, unsubstituted or substituted by halogen; and m is 1 or 2; or Rand Rtaken together, form a 5- or 6-membered heteroaryl ring optionally substituted by Calkyl which is unsubstituted or substituted by amino; and Ris hydrogen or Calkyl or absent to satisfy the valency of the heteroaryl ring.EFFECT: improved compounds properties.29 cl, 23 dwg, 24 tbl, 9 ex Изобретение относится к новым производным пирролопиримидина общей формулы (VIII), обладающим свойствами ингибитора клеточной пролиферации, опосредованной активностью киназ EGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC или TXK, которые могут быть использованы для лечения и/или профилактики расстройства пролиферации, рака или опухоли, связанной с активностью указанных киназ. Такими заболеваниями могут быть саркома, плоскоклеточный рак, фибросаркома, рак шейки матки, рак желудка, рак кожи, лейкемия, лимфома, рак легки