CAS: 4214-73-7; 2-Amino-5-Cyanopyridine

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902837-44-9 329-89-5 69879-22-7

上下游产品

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6-氨基烟酰胺置于三乙胺,三氟乙酸酐,Potassium Carbonate体系中,用 甲醇,水 作为反应溶剂,化学反应 4.0H,以80%的收率获得产物2-氨基-5-氰基吡啶
参考文献:Synthesis And Biological Evaluation Of Sulfonylhydrazone-Substituted Imidazo[1,2-A]Pyridines As Novel Pi3 Kinase P110α Inhibitors
标题:Synthesis And Biological Evaluation Of Sulfonylhydrazone-Substituted Imidazo[1,2-A]Pyridines As Novel Pi3 Kinase P110α Inhibitors
摘要:We Have Previously Reported The Imidazo[1,2-A]Pyridine Derivative 4 As A Novel P110 Alpha Inhibitor; However,Although 4 Is A Potent Inhibitor Of P110 Alpha Enzymatic Activity And Tumor Cell Proliferation In Vitro,It Is Unstable In Solution And Ineffective In Vivo. To Increase Stability The Pyrazole Of 4 Was Replaced With A Hydrazone And A Moderately Potent P110 Alpha Inhibitor 7A Was Obtained. Subsequent Optimization Of 7A Afforded Exceptionally Potent P110 Alpha Inhibitors,Including 8C And 8H,With Ic(50) Values Of 0.30 Nm And 0.26 Nm,Respectively; To The Best Of Our Knowledge,These Compounds Are The Most Potent Pi3K P110 Alpha Inhibitors Reported To Date. Compound 8C Was Also Stable In Solution And Exhibited Significant Anti-Tumor Effectiveness In Vivo. (C) 2007 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2007.05.070

专利信息

专利号:US-7405310-B2
优先权日:2001-03-05
标 题:Non-nucleoside reverse transcriptase inhibitors
发明人：LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA
权利人:MEDIVIR AB
摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.

专利号:US-10308615-B2
优先权日:2015-05-29
标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
发明人：CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-11731956-B2
优先权日:2018-10-22
标 题:Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors

专利号:US-8344010-B2
优先权日:2008-12-26
标 题 :Fused imidazole derivatives as TRPV3 antagonist
发明人：LINGAM V S PRASADARAO; THOMAS ABRAHAM; PHATANGARE SHANTARAM KASHINATH; MINDHE AJIT SHANKAR; KHATIK JAVED YUSUF; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
权利人:GLENMARK PHARMACEUTICALS SA; LINGAM V S PRASADARAO; THOMAS ABRAHAM; PHATANGARE SHANTARAM KASHINATH; MINDHE AJIT SHANKAR; KHATIK JAVED YUSUF; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.

专利号:US-8318928-B2
优先权日:2008-12-15
标题 :Fused imidazole carboxamides as TRPV3 modulators
发明人：CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
权利人:CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI; GLENMARK PHARMACEUTICALS SA
摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.