CAS: 74420-15-8; 3-Bromo-1H-Pyrrolo[2,3-B]Pyridine

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7-氮杂吲哚置于n-溴代丁二酰亚胺(Nbs)体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 4.0H,以96%的收率获得产物3-溴-7-氮杂吲哚
参考文献:发现一类针对蛋白激酶 Bmx 和 Btk 的新型共价双抑制剂
标题:发现一类针对蛋白激酶 Bmx 和 Btk 的新型共价双抑制剂
摘要:非受体酪氨酸 Tec 激酶是免疫系统的关键调节因子,在多种血液恶性肿瘤的发病机制中发挥着至关重要的作用.与布鲁顿酪氨酸激酶 (Btk) 抑制剂开发方面的大量努力相比,其他 Tec 激酶(包括 X 染色体上的骨髓酪氨酸激酶 (Bmx))的特异性抑制剂仍然很少.在这里,我们提出了一类新型的双 Bmx/btk 抑制剂,该抑制剂是由 Janus 激酶 (Jak) 3 的不可逆抑制剂设计而成,靶向位于 Atp 结合袋暴露于溶剂的前部区域内的半胱氨酸.利用看门残基差异的结构引导设计能够实现对 Jak3 和某些其他在此位置具有空间要求残基的激酶的高选择性.最活跃的化合物抑制 Bmx 和 Btk,表观 Ic50 值在个位数纳摩尔范围或以下,显示出 Tec 家族中的中等选择性和有效的细胞靶标参与.这些化合物代表了蛋白激酶 Bmx 选择性化学探针的重要第一步.
DOI:10.3390/ijms21239269

专利信息

专利号:US-9994567-B2
优先权日:2015-05-22
标 题:Synthesis of heterocyclic compounds
发明人：IBRAHIM PRABHA N; LIN JACK; SPEVAK WAYNE; ZHANG JIAZHONG
权利人:PLEXXIKON INC
摘要:Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): n nor a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P 1 and P 2 are as defined in this disclosure.

专利号:US-9695169-B2
优先权日:2012-05-31
标 题:Synthesis of heterocyclic compounds
发明人：IBRAHIM PRABHA N
权利人:PLEXXIKON INC
摘要:Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.

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-2022073513-A1
优先权日:2018-12-29
标题:1h-pyrrolo[2,3-b]pyridine derivatives and related compounds as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases
发明人：CHEN YI
权利人:NEWAVE PHARMACEUTICAL INC
摘要:The present invention relates to compounds of Formula (II) and more preferably to 1H-pyrrolo[2,3-b]pyridine derivatives of formula (III) and related compounds. The variables are defined in the claims. The compounds are BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis of exemplary compounds as well as pharmacological data thereof (pages 61 to 72; examples 1 to 4; tables). An exemplary compound is e.g. 4-(4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl]piperazin-1-yl)-2-[methyl(1H-pyrrolo[2,3-b]pyridin-5-yl)phosphoroso]-N-[3-nitro-4-[(oxan-4-yl methyl)amino]benzenesulfonyl]benzamide (example 1).

专利号:US-2018002332-A1
优先权日:2015-05-22
标题 :Synthesis of heterocyclic compounds

专利号:US-2012077802-A1
优先权日:2009-06-10
标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof
发明人：CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN
权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are spiro-cyclic 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, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.