3,3,5-Tribromo-2-Oxindole置于ammonium Chloride体系中,用 四氢呋喃,锌 用作溶剂,化学反应生成5-溴-7-氮杂氧化吲哚 参考文献:Substituted Oxidole Derivatives As Protein Tyrosine And As Protein Serine/threonine Kinase Inhibitors 标题:Substituted Oxidole Derivatives As Protein Tyrosine And As Protein Serine/threonine Kinase Inhibitors 摘要:本发明总体上涉及新颖的取代吲哚化合物和组合物.这类化合物和组合物作为治疗药物,在治疗通过抑制或拮抗蛋白激酶激活的信号通路而缓解的疾病或状况方面具有效用.特别是,本发明涉及一系列取代吲哚化合物,这些化合物表现出蛋白酪氨酸激酶和蛋白丝氨酸/苏氨酸激酶的抑制作用,并且可用于通过抑制这些激酶来抑制肿瘤生长,以及保护接受化疗的患者免受化疗引起的脱发.
专利号:US-7652137-B2 优先权日:2003-03-06 标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines 发明人:GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.
专利号:US-8404670-B2 优先权日:2009-02-11 标题:Histamine H3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:EP-1633750-B1 优先权日:2003-03-06 标题 :Synthesis of 5-substituted 7-azaindoles and 7-azaindolines
专利号:US-7772246-B2 优先权日:2007-08-01 标题:Pyrazole compounds as RAF inhibitors 发明人:CUI JINGRONG JEAN; DEAL JUDITH GAIL; GU DANLIN; GUO CHUANGXING; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; KEPHART SUSAN ELIZABETH; LINTON MARIA ANGELICA; MCALPINE INDRAWAN JAMES; PAIRISH MASON ALAN; PALMER CYNTHIA LOUISE 权利人:PFIZER 摘要:The present invention is directed to compounds of Formula (I), n nand to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
专利号:US-9834551-B2 优先权日:2013-04-18 标 题 :Substituted pyrrolo[2,3-b]pyrazines and substituted pyrazolo[3,4-b]pyridines as ITK and JAK kinase inhibitors 发明人:VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANGIREDDY PARAMAREDDY; APPALANENI RAJENDRA P 权利人:ARRIEN PHARMACEUTICALS LLC 摘要:The present invention relates to compounds described by Formula I: n nsalts thereof, their synthesis, and their use as ITK and JAK3 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such disease associated with abnormal cell growth such as autoimmune, inflammation, rheumatoid arthritis, systemic lupus erythematosus, atherosclerosis, ulcerative colitis, psoriatic arthritis, psoriasis, Crohn's, metabolic and cancer diseases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions and processes for preparing the compounds of the invention.