CAS: 1810-66-8; 6-Bromoquinolin-2(1H)-One

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99465-10-8 67805-67-8 939-16-2

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📜4-溴-2-碘苯甲胺置于n-甲基吡咯烷酮,Palladium Diacetate,三正丁胺体系中,用 乙二醇 用作溶剂,化学反应 0.33H,反应生成6-溴喹啉-2-酮
参考文献:Development Of 6-Substituted Indolylquinolinones As Potent Chek1 Kinase Inhibitors
标题:Development Of 6-Substituted Indolylquinolinones As Potent Chek1 Kinase Inhibitors
摘要:Through A Comparison Of X-Ray Co-Crystallographic Data For 1 And 2 In The Chek1 Active Site,It Was Hypothesized That The Affinity Of The Indolylquinolinone Series (2) For Chek1 Kinase Would Be Improved Via C6 Substitution Into The Hydrophobic Region I (Hi) Pocket. An Efficient Route To 6-Bromo-3-Indolyl-Quinolinone (9) Was Developed,And This Series Was Rapidly Optimized For Potency By Modification At C6. A General Trend Was Observed Among These Low Nanomolar Chek1 Inhibitors That Compounds With Multiple Basic Amines,Or Elevated Polar Surface Area (Psa) Exhibited Poor Cell Potency. Minimization Of These Parameters (Basic Amines,Psa) Resulted In Chek1 Inhibitors With Improved Cell Potency,And Preliminary Pharmacokinetic Data Are Presented For Several Of These Compounds.
Doi:10.1016/j.Bmcl.2006.08.053

专利信息

专利号:CN-108503582-A
优先权日:2018-01-19
标 题:Microwave Assisted Synthesis of 2-(1H)-Quinolinones

专利号:WO-9531458-A1
优先权日:1992-10-13
标 题:3-hydroxyquinuclidin-3-ylphenylquinolines as squalene synthase inhibitors
发明人：NEUENSCHWANDER KENT W; GRONEBERG ROBERT D; MORRIS ROBERT L; SCOTESE ANTHONY C; MAGUIRE MARTIN P
权利人:RHONE POULENC RORER PHARMA; NEUENSCHWANDER KENT W; GRONEBERG ROBERT D; MORRIS ROBERT L; SCOTESE ANTHONY C; MAGUIRE MARTIN P
摘要:This invention relates to a class of novel compounds useful in the treatment of diseases associated with undesirable cholesterol levels in the body, and particularly diseases of the cardiovascular system, such as atherosclerosis. The compounds of this invention are novel quinolinyl phenyl 3-hydroxyquinuclidines which may be linked directly or through a chain linking the quinolinyl to the phenyl and/or the phenyl to the quinuclidine. Compounds of this invention exhibit squalene synthase inhibition properties and reduce levels of serum cholesterol without significantly reducing mevalonic metabolite synthesis and thus provide a therapeutic agent having fewer side effects than agents which act by inhibiting the HMG-CoA reductase enzyme. Compounds of the present invention may also be useful in treating fungal infections. This invention further relates to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

专利号:US-7696246-B2
优先权日:1999-08-27
标题:Bicyclic androgen and progesterone receptor modulator compounds and methods
发明人：ZHI LIN; VAN OEVEREN CORNELIS ARJAN; MARTINBOROUGH ESTHER
权利人:LIGAND PHARM INC
摘要:The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.

专利号:CN-108503582-B
优先权日:2018-01-19
标 题:Microwave-assisted synthesis method of 2- (1H) -quinolinone compounds