CAS: 1095382-05-0; 3-((4-(6-Bromo-2-(4-(4-Methylpiperazin-1-yl)Phenyl)-3H-Imidazo[4,5-B]Pyridin-7-yl)Piperazin-1-yl)Methyl)-5-Methylisoxazole

上下游产品

CAS号27913-99-1 4-(4-甲基哌嗪)苯甲醛

📜5-Bromo-4-[4-[(5-Methyl-Isoxazol-3-yl)Methyl]Piperazin-1-Yl]-3-Nitro-Pyridin-2-Ylamine,4-(4-甲基哌嗪)苯甲醛置于sodium Dithionite体系中,用 乙醇,水 用作溶剂,化学反应 18.0H,以31%的收率获得3-[[4-[6-溴-2-[4-(4-甲基哌嗪-1-基) 苯基]-3H-咪唑并[4,5-B]吡啶-7-基]哌嗪-1-基]甲基]-5-甲基异恶唑
参考文献:Imidazo[4,5-B]Pyridine Derivatives As Inhibitors Of Aurora Kinases: Lead Optimization Studies Toward The Identification Of An Orally Bioavailable Preclinical Development Candidate
标题:Imidazo[4,5-B]Pyridine Derivatives As Inhibitors Of Aurora Kinases: Lead Optimization Studies Toward The Identification Of An Orally Bioavailable Preclinical Development Candidate
摘要:Lead Optimization Studies Using 7 As The Starting Point Led To A New Class Of Imidazo[4,5-B]Pyridine-Based Inhibitors Of Aurora Kinases That Possessed The 1-Benzylpiperazinyl Motif At The 7-Position,And Displayed Favorable In Vitro Properties. Cocrystallization Of Aurora-A With 40C (Cct137444) Provided A Clear Understanding Into The Interactions Of This Novel Class Of Inhibitors With The Aurora Kinases. Subsequent Physicochemical Property Refinement By The Incorporation Of Solubilizing Groups Led To The Identification Of 3-((4-(6-Bromo-2-(4-(4-Methylpiperazin-1-yl)Phenyl)-3H-Imidazo[4,5-B]Pyridin-7-yl)Piperazin-1-yl)Methyl)-5-Methylisoxazole (51,Cct137690) Which Is A Potent Inhibitor Of Aurora Kinases (Aurora-A Ic(50) = 0.015 +/-0.003 Mum,Aurora-B Ic(50) = 0.025 Mum,Aurora-C Ic(50) = 0.019 Mum). Compound 51 Is Highly Orally Bioavailable,And In In Vivo Efficacy Studies It Inhibited The Growth Of Sw620 Colon Carcinoma Xenografts Following Oral Administration With No Observed Toxicities As Defined By Body Weight Loss.
Doi:10.1021/jm100262J

专利信息

专利号:WO-2024132278-A1
优先权日:2022-12-20
标题:Synthesis, pharmacology and use of new water-soluble and selective fms-like tyrosine kinase 3 (flt3) inhibitors
发明人：MAHBOOBI SAVOSH; WIRTH LUKAS; PONGARTZ HERWIG; SELLMER ANDREAS
权利人:UNIV REGENSBURG
摘要:The present application relates to compounds of formula (I) for inhibiting FLT3. The present application further relates to a composition, preferably pharmaceutical composition, comprising a compound or a pharmaceutically acceptable salt thereof and comprising a pharmaceutically acceptable excipient and/or carrier. The present application also relates to a compound or composition for use in medicine. The present application also relates to a compound or composition for use in a method of preventing or treating cancer, preferably blood cancer, more preferably leukemia, even more preferably acute myeloid leukemia (AML). Furthermore, the present application relates to a method of preparing a compound.

专利号:US-11384076-B2
优先权日:2017-08-18
标 题:Synthesis, pharmacology and use of new and selective FMS-like tyrosine kinase 3 (FLT3) FLT3 inhibitors
发明人：MAHBOOBI SIAVOSH; SELLMER ANDREAS; PONGRATZ HERWIG; PILSL BERNARDETTE; KRÄMER OLIVER; KINDLER THOMAS; BEYER MANDY
权利人:UNIV REGENSBURG; UNIV DER JOHANNES GUTENBERG UNIV MAINZ
摘要:The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the compounds and methods of treatment.

专利号:EP-4389223-A1
优先权日:2022-12-20
标 题 :Synthesis, pharmacology and use of new water-soluble and selective fms-like tyrosine kinase 3 (flt3) inhibitors

专利号:US-2020190075-A1
优先权日:2017-08-18
标 题:Synthesis, pharmacology and use of new and selective fms-like tyrosine kinase 3 (flt3) flt3 inhibitors

专利号:EP-3668867-B1
优先权日:2017-08-18
标 题 :Synthesis, pharmacology and use of new and selective fms-like tyrosine kinase 3 (flt3) flt3 inhibitors