CAS: 39931-77-6; Ethyl 2-(Pyridin-3-yl)Acetate

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3-iodopyridine bromo(2-ethoxy-2-oxoethyl)zinc formaldehyd diethyl 2-oxo-3-pyridylsuccinate sodium salt1-(2,4-Difluorophenyl)-2-(pyridin-3-yl)ethanone Di-p-tolylimino-oxalsaeurediethylester ethyl 2-methyl-2-(pyridin-3-yl)propionate coumarin 510

📜3-氯甲基吡啶盐酸盐置于盐酸,水体系中,用 二甲基亚砜 用作溶剂,化学反应 23.5H,反应生成3-吡啶乙酸乙酯
参考文献:四唑酰肼类化合物是jumonjic域含组蛋白去甲基化酶kdm4A的选择性片段样抑制剂
标题:四唑酰肼类化合物是jumonjic域含组蛋白去甲基化酶kdm4A的选择性片段样抑制剂
摘要:含有jumonjic域的组蛋白去甲基化酶2A(jmjd2A,Kdm4A)是基因表达的表观遗传调控中的关键角色.以前的出版物表明,升高和降低的酶水平均与某些类型的癌症有关,因此,Kdm4A在肿瘤发生中的明确作用仍然难以捉摸.为了鉴定具有非常好理化性质的新型分子起点来研究kdm4A的生理作用,我们通过使用两次独立的试验筛选了许多带有铁螯合部分的分子.通过这种方法,我们能够鉴定出2-(1 H-四唑-5-基)乙酰肼为新颖的类似片段的铅结构,相对分子质量低(m R = 142 Da),复杂度低,并且ic 5046.6μ值米在甲醛脱氢酶(fdh)-偶联测定法和2.4μ米在基于抗体的测定法.尽管它的体积很小,但是对于该化合物而言,可以证明它对另外两种脱甲基酶的相对选择性.这是四唑基团作为jmjd脱甲基酶中的战斗部的第一个例子.
Doi:10.1002/cmdc.201500335

专利信息

专利号:WO-2011147545-A1
优先权日:2010-05-24
标 题:Continuous process for preparing quantitatively terminally functionalized polymers using oxirane derivatives as termination reagents
发明人：FREY HOLGER; TONHAUSER CHRISTOPH; WILMS DANIEL; WURM FREDERIK; MASKOS MICHAEL
权利人:UNIV MAINZ JOHANNES GUTENBERG; FREY HOLGER; TONHAUSER CHRISTOPH; WILMS DANIEL; WURM FREDERIK; MASKOS MICHAEL
摘要:A process offers a time-saving and cost-effective method for the continuous synthesis of terminally functional polymers through the use of efficient termination reagents from the group encompassing oxiranes, sulphur-containing oxirane analogues and nitrogen-containing oxirane analogues. The continuous process allows the introduction of different functional groups. Within a relatively short time, the properties of the polymers, such as general chemical composition, molecular weight, polydispersity, chemical composition and functionalization of the chain end, and chemical composition of the end groups, can be varied within a wide range. The polymers obtained in accordance with the invention are particularly suitable as a dispersion reagent for the mixing or stabilization of two materials which differ in mixing behaviour. Coating materials are a further possible application, for the adjustment of surface properties or the adaptation of rheological properties of viscous materials.

专利号:US-6531477-B1
优先权日:1998-10-13
标 题:6-substituted pyrazolo [3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
发明人：MARKWALDER JAY A; SEITZ STEVEN P; SHERK SUSAN R
权利人:DU PONT PHARM CO
摘要:The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T.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-6559152-B2
优先权日:1998-10-13
标 题 :6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
发明人：MARKWALDER JAY A; SEITZ STEVEN P; SHERK SUSAN R
权利人:DU PONT PHARM CO
摘要:The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II):that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T.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:CN-105523986-A
优先权日:2015-12-30
标 题 :A kind of synthesis method of efflux pump inhibitor N-hydrogen-2-arylindole and its derivatives

专利号:US-6472403-B2
优先权日:2000-01-20
标 题 :αV integrin receptor antagonists
发明人：DUGGAN MARK E; HALCZENKO WASYL; HUTCHINSON JOHN H; LI AIWEN; MEISSNER ROBERT S; PERKINS JAMES J; STEELE THOMAS G; WANG JIABING; PATANE MICHAEL A
权利人:MERCK & CO INC
摘要:The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

专利号:US-7109191-B2
优先权日:2001-05-03
标题 :Benzazepinone alpha vintegrin receptor antagonists
发明人：MEISSNER ROBERT S; COLEMAN PAUL J; DUGGAN MARK E; HARTMAN GEORGE D; WANG JIABING; HUTCHINSON JOHN H
权利人:MERCK & CO INC
摘要:The present invention relates to novel benzazepinone derivatives, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and αvβ5 and are therefore useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.