CAS: 852227-86-2; 5-(Chloromethyl)-1,3-Dimethyl-1H-Pyrazole

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84547-64-8 1072-91-9 1056598-95-8

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(1,3-二甲基-5-羟甲基-1H-吡唑 (1,3-Dimethyl-1H-Pyrazol-5-yl)Methanol 57012-20-1

📜(1,3-二甲基-5-羟甲基-1H-吡唑置于氯化亚砜体系中,化学反应 0.33H,反应生成 5-氯甲基-1,3-二甲基-1H-吡唑
参考文献:5-Lipoxygenase-Activating Protein (Flap) Inhibitors. Part 4: Development Of 3-[3-Tert-Butylsulfanyl-1-[4-(6-Ethoxypyridin-3-yl)Benzyl]-5-(5-Methylpyridin-2-Ylmethoxy)-1H-Indol-2-Yl]-2,2-Dimethylpropionic Acid (Am803),A Potent,Oral,Once Daily Flap Inhibitor
标题:5-Lipoxygenase-Activating Protein (Flap) Inhibitors. Part 4: Development Of 3-[3-Tert-Butylsulfanyl-1-[4-(6-Ethoxypyridin-3-yl)Benzyl]-5-(5-Methylpyridin-2-Ylmethoxy)-1H-Indol-2-Yl]-2,2-Dimethylpropionic Acid (Am803),A Potent,Oral,Once Daily Flap Inhibitor
摘要:The Potent 5-Lipoxygenase-Activating Protein (Flap) Inhibitor 3-[3-Tert-Butylsulfanyl-1-[4-(6-Ethoxypyridin-3-yl)Benzyl]-5-(5-Methylpyridin-2-Ylmethoxy)-1H-Indol-2-Yl]-2,2-Dimethylpropionic Acid 11Cc Is Described (Am803,Now Gsk2190915). Building Upon Am103 (1) (Hutchinson Et Al. J. Med Chem. 2009,52,5803-5815; Stock Et Al. Bioorg. Med. Chem. Lett. 2010,20,213-217; Stock Et Al. Bioorg. Med. Chem. Lett. 2010,20,4598-4601),Sar Studies Centering Around The Pyridine Moiety Led To The Discovery Of Compounds That Exhibit Significantly Increased Potency In A Human Whole Blood Assay Measuring Ltb4 Inhibition With Longer Drug Preincubation Times (15 Min Vs S H). Further Studies Identified 11Cc With A Potency Of 2.9 Nm In Flap Binding,An Ic50 Of 76 Nm For Inhibition Of Ltb4 In Human Blood (5 H Incubation) And Excellent Preclinical Toxicology And Pharmacoldnetics In Rat And Dog. 11Cc Also Demonstrated An Extended Pharmacodynamic Effect In A Rodent Bronchoalveolar Lavage (Bal) Model. This Compound Has Successfully Completed Phase 1 Clinical Studies In Healthy Volunteers And Is Currently Undergoing Phase 2 Trials In Asthmatic Patients.
DOI:10.1021/jm2008369

专利信息

专利号:US-8309540-B2
优先权日:2006-10-24
标 题:HCV NS3 protease inhibitors
发明人：LIVERTON NIGEL J; VACCA JOSEPH P; MCCAULEY JOHN A; ROMANO JOSEPH J; RUDD MICHAEL T
权利人:LIVERTON NIGEL J; VACCA JOSEPH P; MCCAULEY JOHN A; ROMANO JOSEPH J; RUDD MICHAEL T; MERCK SHARP & DOHME
摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. (I)