CAS: 228867-86-5; 5-Hydroxy-3-Methylpicolinonitrile

相似化合物

1256792-12-7 61893-00-3 1256792-51-4

上下游产品

zinc(II) cyanide 2-chloro-5-hydroxy-3-methylpyridine 6-chloro-5-methylpyridin-3-amine 2-chloro-3-methyl-5-nitropyridine 5-methoxy-3-methylpicolinic acid (S)-N-(3-(5-amino-3-(fluoromethyl)-6,6-dimethyl-1,1-dioxido-3,6-dihydro-2H-1,4-thiazin-3-yl)-4-fluorophenyl)-5-(cyclobutylmethoxy)-3-methylpicolinamide 3-methyl-5-(2,2,2-trifluoroethoxy)picolinonitrile

📜3-甲基-5-硝基-2-吡啶甲腈置于硫酸,铁粉,Calcium Chloride,Sodium Nitrite体系中,用 乙醇,水 用作溶剂,化学反应 3.0H,反应生成2-氰基-3-甲基-5-羟基吡啶
参考文献:临床候选 Pf-06751979 的设计和合成:一种有效的,脑渗透性的,β 位点淀粉样前体蛋白裂解酶 1 (Bace1) 抑制剂,缺乏色素减退
标题:临床候选 Pf-06751979 的设计和合成:一种有效的,脑渗透性的,β 位点淀粉样前体蛋白裂解酶 1 (Bace1) 抑制剂,缺乏色素减退
摘要:开发用于治疗阿尔茨海默病的 β 位淀粉样前体蛋白裂解酶 1 (Bace1) 抑制剂的主要挑战是效力,类药物特性和对相关天冬氨酰蛋白酶(如组织蛋白酶 D (Catd))的比对和 Bace2.长期抑制 Bace2 的潜在负担直到最近才开始出现,因为 Bace2 影响前黑素体蛋白 (Pmel17) 的加工并破坏黑素体形态,导致色素脱失表型.在此,我们描述了临床候选 Pf-06751979 ( 64 )的鉴定,其表现出优异的脑渗透性,有效的体内功效以及对相关天冬氨酰蛋白酶(包括 Bace2)的广泛选择性.64 的慢性给药 在狗中长达 9 个月的时间未发现任何毛发颜色(色素沉着)变化的观察结果,并表明与当前在后期临床开发中对 Bace2 无选择性的 Bace1 抑制剂的关键区别.
Doi:10.1021/acs.Jmedchem.8B00246

专利信息

专利号:US-9771379-B2
优先权日:2015-09-24
标题:N-(2-(2-amino-6-substituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]OXAZIN-8a(8H)-yl)-thiazol-4-yl) amides
发明人：BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; ZHANG LEI; O'NEILL BRIAN THOMAS
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nwherein the variables R 1 , R 2 , R 3 , R 4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-9744173-B2
优先权日:2014-04-10
标题 :2-amino 6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides
发明人：BRODNEY MICHAEL AARON; BECK ELIZABETH MARY; BUTLER CHRISTOPHER RYAN; ZHANG LEI; O'NEILL BRIAN THOMAS; BARREIRO GABRIELA; LACHAPELLE ERIK ALPHIE; ROGERS BRUCE NELSEN
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nand the variable R 1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-9751895-B2
优先权日:2015-09-24
标 题:N-[2-(2-amino-6,6-disubstituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl)-1,3-thiazol-4-yl]amides
发明人：BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; ZHANG LEI; O'NEILL BRIAN THOMAS; VERHOEST PATRICK ROBERT; MIKOCHIK PETER JUSTIN; MURRAY JOHN CHARLES; HOU XINJUN
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nand the variables R 1 , R 2 and R 3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-9611264-B1
优先权日:2015-09-24
标 题:N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl] amides
发明人：BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; ZHANG LEI; O'NEILL BRIAN THOMAS; VERHOEST PATRICK ROBERT; SALOMON FERRER ROMELIA DEL CARMEN
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n n n n n n n n n n n n wherein the variables R 1 , R 2 and R 3 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.