CAS: 55052-28-3; 4-Chloro-7-Azaindole

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945599-50-8 348640-05-1 2438941-56-9

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CAS号271-63-6 7-氮杂吲哚 | CAS号55052-24-9 7-氮杂吲哚-7-氧化物 | CAS号74420-18-1 7-Hydroxy-1H-py... | CAS号124-63-0 甲基磺酰氯 | CAS号744209-63-0 4-氯-1-苯磺酰基-1H-吡... | CAS号1033809-58-3 1H-pyrrolo[2,3-... | CAS号74420-00-1 4-氨基-7-氮杂吲哚 | CAS号348640-26-6 4-氯-2-碘-1-[(4-甲... | CAS号319474-34-5 4-碘-7-氮杂吲哚 | CAS号443729-67-7 1-(4-碘-1H-吡咯并[2... | CAS号344327-11-3 7-氮杂吲哚-4-甲腈 | CAS号346599-62-0 4-氯-1H-吡咯并[2,3-... | CAS号936549-95-0 7-N-杂吲哚-3-甲醇 | CAS号918519-53-6 4-氯-3-硝基-1H-吡咯并... | CAS号940948-29-8 4-氯-2-碘-1H-吡咯[2... | CAS号918515-16-9 4-氯-1H-吡咯并[2,3-... | CAS号942919-26-8 7-氮杂吲哚-4-硼酸频哪醇酯

7-氮杂吲哚置于间氯过氧苯甲酸,三氯氧磷,Sodium Hydroxide体系中,用 甲醚,正庚烷,水 作为反应溶剂,以84%的收率获得产物4-氯-7-氮杂吲哚
参考文献:4-Amino-Pyrrolopyridine-5-Carboxamide: A Novel Scaffold For Jak1-Selective Inhibitors
标题:4-Amino-Pyrrolopyridine-5-Carboxamide: A Novel Scaffold For Jak1-Selective Inhibitors
摘要:尽管对选择性janus激酶1(jak1)抑制剂及其在治疗炎症性疾病(如类风湿关节炎(ra))中的潜力充满高度兴趣,但迄今为止仅有少数此类抑制剂被报告.在本研究中,通过对强效jak1选择性抑制剂c2-甲基咪唑并吡啶的结构改造,设计了一种新的4-氨基-1H-吡咯并[2,3-B]吡啶-5-羧酰胺支架.在研究的系列中,4-(2-氨基乙基)氨基吡咯并吡啶衍生物2J表现出显著的24.7倍jak1/jak2选择性,同时对jak1具有合理的抑制活性(ic50=2.2 μm).2J的显著jak1选择性随后通过分子对接研究进行了解释,该研究表明,2J的氨基乙基功能在识别jak1和jak2之间配体结合位点尺寸细微但重要的差异方面定位非常好.
DOI:10.1248/cpb.C13-00807

专利信息

专利号:WO-03000690-A1
优先权日:2001-06-25
标题:Synthesis of heterocyclic compounds employing microwave technology
发明人：MAJID TAHIR NADEEM; DEPRETS STEPHANIE D; PEDGRIFT BRIAN L
权利人:AVENTIS PHARMA INC; MAJID TAHIR NADEEM; DEPRETS STEPHANIE D; PEDGRIFT BRIAN L
摘要:This invention provides for processes for preparing compounds of the formula (I) comprising employing microwave energy.

专利号:US-11952342-B2
优先权日:2020-12-03
标 题:Aza-substituted psilocin analogs and methods of synthesizing the same
发明人：HOYER DENTON W; ROSCOW ROBERT F
权利人:MYDECINE INNOVATIONS GROUP INC
摘要:The present invention is directed to novel chemical compositions of matter and their methods of synthesis, and in particular novel analogs of Psilocin having enhanced physical and pharmacokinetic characteristics.

专利号:US-9951062-B2
优先权日:2012-12-14
标 题 :Substituted 1 H-pyrrolo [2, 3-b] pyridine and 1 H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
发明人：VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANIPISETTY VENU BABU; TALLURI SURESHKUMAR; APPALANENI RAJENDRA P
权利人:ARRIEN PHARMACEUTICALS LLC
摘要:Compounds according to Formulas I, IA or IB: n nto pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.

专利号:US-9695191-B2
优先权日:2009-08-05
标题 :Conformationally constrained, fully synthetic macrocyclic compounds
发明人：OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN
权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG
摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.

专利号:US-9617257-B2
优先权日:2012-06-29
标题:Fused pyridine derivatives useful as c-Met tyrosine kinase inhibitors
发明人：HU SHAOJING; WANG FEI; XU ZHIGUO; WANG YANPING; WANG YINXIANG
权利人:BETA PHARMACEUTICALS CO LTD; BETTA PHARMACEUTICALS CO LTD
摘要:This invention relates to novel fused quinazoline derivatives of Formula I as c-Met inhibitors, their synthesis and uses for treating c-Met mediated disorders.