CAS: 79455-63-3; 2-Chloro-6-Fluorobenzoyl Chloride

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CAS号434-75-3 2-氯-6-氟苯甲酸 | CAS号66073-54-9 2-氯-6-氟苯甲酰胺

2-氯-6-氟苯甲酸置于氯化亚砜体系中,化学反应生成 2-氯-6-氟苯甲酰氯
参考文献:领先优化的4-氨基吡啶苯甲酰胺支架,以识别有力的,选择性的和口服生物利用性tyk2抑制剂.
标题:领先优化的4-氨基吡啶苯甲酰胺支架,以识别有力的,选择性的和口服生物利用性tyk2抑制剂.
摘要:在这里,我们从铅分子3开始,报告我们的铅优化工作,以鉴定有效的,选择性的和口服生物利用的tyk2抑制剂.我们使用基于结构的设计来发现2,6-二氯-4-氰基苯基和(1 R,2 R)-2-氟环丙基酰胺的修饰,相对于3,它们各自显示出更高的tyk2效力以及jak1和jak2选择性.进一步的优化最终导致化合物37在小鼠中表现出非常好的tyk2酶和白介素12(il-12)细胞效能,以及可接受的细胞jak1和jak2选择性以及出色的口服暴露.在小鼠il-12 Pk / Pd模型中测试时,化合物37 结果显示,细胞因子干扰素-γ(ifnγ)的抑制作用具有统计学意义,表明对tyk2激酶活性的选择性抑制可能足以阻断il-12体内途径.
DOI:10.1021/jm400266T

专利信息

专利号:US-8748459-B2
优先权日:2002-03-29
标 题 :Pyridinoylpiperidines as 5-HT1F agonists
发明人：COHEN MICHAEL PHILIP; KOHLMAN DANIEL TIMOTHY; LIANG SIDNEY XI; VICTOR FRANTZ; XU YAO-CHANG; YING BAI-PING; ZACHERL DEANNA PIATT; ZHANG DEYI
权利人:COHEN MICHAEL PHILIP; KOHLMAN DANIEL TIMOTHY; LIANG SIDNEY XI; VICTOR FRANTZ; XU YAO-CHANG; YING BAI-PING; ZACHERL DEANNA PIATT; ZHANG DEYI; LILLY CO ELI
摘要:The present invention relates to compounds of formula I: n nor pharmaceutically acceptable acid addition salts thereof, where;n R 1 is C 1 -C 6 alkyl, substituted C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, substituted C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkyl-C 1 -C 3 alkyl, substituted C 3 -C 7 cycloalkyl-C 1 -C 3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R 2 is hydrogen, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl-C 1 -C 3 alkyl, or a group of formula II nn n n n n n n n n n n n R 3 is hydrogen or C 1 -C 3 alkyl; n R 4 is hydrogen, halo, or C 1 -C 3 alkyl; n R 5 is hydrogen or C 1 -C 3 alkyl; n R 6 is hydrogen or C 1 -C 6 alkyl; and n n is an integer from 1 to 6 inclusively. n n n n n The compounds of the present invention are useful for activating 5-HT lF receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

专利号:PL-210019-B1
优先权日:2002-03-29
标题 :Pyridinoylpiperidine compounds, method of their preparation and use, and method of preparing intermediates for their synthesis