4-(1-Methyl-1H-Pyrazol-4-yl)Benzoic Acid置于n,N-二甲基甲酰胺 草酰氯体系中,用 二氯甲烷 用作溶剂,化学反应 18.0H,反应生成4-氟-2-(三氟甲基)苯甲酰氯 参考文献:Vasopressin Agonist Formulation And Process 标题:Vasopressin Agonist Formulation And Process 摘要:该发明提供了用于加压素激动剂化合物的新型配方,或其药用盐,具有以下一般结构:并提供制备它们的方法,所述配方包括约1%至约20%的活性成分,约1%至约18%的表面活性剂成分,约50%至约80%的一种或多种聚乙二醇成分,约1%至约20%的一种或多种蔗糖脂肪酸酯和/或聚乙烯吡咯烷酮成分,以及可选地,一种或多种防腐剂或抗氧化剂.
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:US-2009099200-A1 优先权日:2005-06-09 标题 :Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS 权利人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS 摘要:Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
专利号:HU-E035391-T2 优先权日:2012-06-11 标 题 :Process for the preparation of 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound and intermediate of synthesis
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
参考文献:10.1007/s12272-017-0987-x 摘要:Jin G, Sivaraman A, Lee K. Development of taladegib as a sonic hedgehog signaling pathway inhibitor. Archives of Pharmacal Research. 2017 Nov 20;40(12):1390–3. doi: 10.1007/s12272-017-0987-x.