5-溴-4,7-二氮杂吲哚置于palladium Diacetate,Sodium Hydride,Potassium Carbonate,4,5-双二苯基膦-9,9-二甲基氧杂蒽体系中,用 N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应生成N-[5-[(4-甲基苯基)磺酰基]-5H-吡咯并[2,3-B]吡嗪-2-基]氨基甲酸乙酯 参考文献:Upadacitinib Tartrate. Tyrosine-Protein Kinase Jak1 Inhibitor,Treatment Of Autoimmune Inflammatory Diseases,Treatment Of Rheumatoid Arthritis 标题:Upadacitinib Tartrate. Tyrosine-Protein Kinase Jak1 Inhibitor,Treatment Of Autoimmune Inflammatory Diseases,Treatment Of Rheumatoid Arthritis 摘要:Upadacitinib Tartrate (Abt-494) Is A Potent And Selective Tyrosine-Protein Kinase Jak1 Inhibitor Being Developed For The Treatment Of Systemic Autoimmune Inflammatory Diseases,Including Rheumatoid Arthritis (Ra),Crohn'S Disease,Ulcerative Colitis And Psoriatic Arthritis. In Vitro,Upadacitinib Demonstrated Higher Selectivity For Inhibiting Jak1 Over Jak2 And Jak3,Suggesting A Potentially Improved Therapeutic Profile In Treating Patients With Inflammatory Diseases Compared To Nonselective Jak Inhibitors. Upadacitinib Has Demonstrated Safety And Efficacy In Phase Ii Trials In Patients With Ra And Inflammatory Bowel Disease,And Is Currently In Phase Iii Development For These Indications. Doi:10.1358/dof.2018.043.10.2849626
专利号:US-11976077-B2 优先权日:2015-10-16 标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof 发明人:PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.
专利号:US-9963459-B1 优先权日:2015-10-16 标 题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-alpla]pyrrolo[2,3-e]-pyrazin-8-YL)-N-(2,2,2-Trifluoroethyl)pyrrol and solid state forms thereof 发明人:JAYANTH JAYANTHY; MARROUM PATRICK J; MAYER PETER T; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.