Antihypertensive activity of 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives
摘要:
A series of 51 6-arylpyrido[2,3-d]pyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat. A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyrido[2,3-d]pyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg. Normalized blood pressure levels could then be maintained by single daily oral doses. The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.
PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS
申请人:Incyte Holdings Corporation
公开号:EP3272738A2
公开(公告)日:2018-01-24
The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
本发明涉及制备式 III 的手性取代吡唑基吡咯并[2,3-d]嘧啶和相关合成中间体化合物的工艺。手性取代的吡唑基吡咯并[2,3-d]嘧啶可用作蛋白酪氨酸激酶 Janus Kinase 家族(JAKs)的抑制剂,用于治疗炎症性疾病、骨髓增生性疾病和其他疾病。
6-Substituted-arylpyrido(2,3-d)pyrimidin-7-amines, derivatives and salts thereof, pharmaceutical compositions containing any of the foregoing, and processes for producing any of the foregoing