CAS: 20173-24-4; 2-(Pyridin-3-yl)Ethanamine

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307496-23-7 3724-16-1 41038-69-1

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3-吡啶乙腈置于sodium Tetrahydroborate,Cobalt(II) Chloride体系中,用 甲醇 用作溶剂,化学反应 3.0H,反应生成3-(2-氨基乙基)吡啶
参考文献:苯乙基噻唑硫脲(pett)化合物,一类新的hiv-1逆转录酶抑制剂.1. Pett类似物的合成及其基本的构效关系研究.
标题:苯乙基噻唑硫脲(pett)化合物,一类新的hiv-1逆转录酶抑制剂.1. Pett类似物的合成及其基本的构效关系研究.
摘要:描述了一系列新的有效的特异性hiv-1抑制化合物.该系列中的主要化合物n-(2-苯乙基)-N'-(2-噻唑基)硫脲(1)使用rcdg作为模板抑制hiv-1 Rt,Ic50为0.9 Microm.在mt-4细胞中,化合物1抑制hiv-1的ed50为1.3 Microm.细胞培养物中50%的细胞毒性剂量> 380 Microm.通过将铅化合物概念上划分为四个象限来建立化学结构-活性关系(sar).搜救战略分为两个阶段.第一阶段涉及通过象限1-4的独立变化来优化抗病毒活性.第二阶段涉及制备结合了这些取代基中最好的杂化结构.进一步的sar研究和药代动力学考虑导致鉴定n-(2-吡啶基)-N'-(5-溴-2-吡啶基)-硫脲(62; Ly300046.Hcl)可作为临床评估的候选药物.Ly300046.Hcl抑制hiv-1 Rt的ic50为15 Nm,在细胞培养中的ed50为20 Nm.
Doi:10.1021/jm00025A010

专利信息

专利号:US-6413957-B1
优先权日:1998-04-21
标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones
发明人：NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W
权利人:BRISTOL MYERS SUIBB PHARMA COM
摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

专利号:US-9551018-B2
优先权日:2006-02-13
标 题 :Process for the preparation of optically active chiral amines
发明人：ROBINS KAREN; SCHEUER UWE; HOHNE MATTHIAS
权利人:LONZA AG
摘要:The present invention relates to the production of optically pure secondary amines, which can be used as intermediate products in a synthesis of for instance pharmaceutical products.

专利号:US-2023135239-A1
优先权日:2021-11-04
标 题 :Drug for treating severe acute respiratory syndrome caused by coronavirus and complications thereof and use of the drug
发明人：YU WENQIANG; LI ZHENYAN; XU JIANQING; LI WEI; LIAN CHENG
权利人:SHANGHAI PUBLIC HEALTH CLINICAL CT; SHANGHAI YIZHE BIOTECHNOLOGY CO LTD
摘要:The present invention discloses a drug for treating severe acute respiratory syndrome caused by coronavirus and the complications thereof and the use of the drug, and specifically the use of an agent in the preparation of a drug for treating severe acute respiratory syndrome caused by coronavirus and the complications thereof. The above-mentioned agent is at least one of hyaluronic acid synthesis inhibitor, hyaluronidase, hyaluronidase inhibitor, hyaluronic acid receptor inhibitor, and anticoagulant. The present invention is based on the discovery of an important pathogenic mechanism of severe acute respiratory syndrome-related coronavirus 2 that a sequence homologous to human in severe acute respiratory syndrome-related coronavirus 2, named HIS (Human Insert Sequence), can specifically activate hyaluronic acid synthase HAS and other inflammatory factors, and then it is found from clinical samples that the content of hyaluronic acid in the serum of a patient with severe COVID-19 is significantly higher than that in a patient with mild COVID-19. The above-mentioned agent is used for the first time for treating coronavirus and complications, and it is verified that a hyaluronic acid synthesis inhibitor can reduce the content of hyaluronic acid, thus the adjustment of hyaluronic acid level has good application value in the treatment and/or prevention of conditions caused by coronavirus.

专利号:US-7632972-B2
优先权日:2003-10-30
标 题 :Compounds and methods for treatment of cancer and modulation of programmed cell death for melanoma and other cancer cells
发明人：HERGENROTHER PAUL J; NESTERENKO VITALIY; PUTT KARSON; ALLEN BRITTANY JOY; DOTHAGER ROBIN SHANE; LESLIE BENJAMIN JAMES
权利人:UNIV ALABAMA
摘要:Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of synthetic combinatorial libraries and the evaluation of library member compounds regarding induction of apoptosis selectively in cancer cells are disclosed. Compounds, methods of making the compounds, and therapeutic methods with application against breast cancer cells, melanoma cancer cells, colon cancer cells, and other cancer cells are described.

专利号:US-7250435-B2
优先权日:1999-10-20
标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents
发明人：NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY
权利人:BRISTOL MYERS SQUIBB PHARMA CO
摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

专利号:US-6407103-B2
优先权日:1998-04-21
标 题:Indeno [1,2-c] pyrazol-4-ones and their uses
发明人：NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W
权利人:BRISTOL MYERS SQUIBB PHARMA CO
摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-9 and their regulatory subunits know as cyclins A-H.This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.