Discovery of 6-Phenylpyrimido[4,5-<i>b</i>][1,4]oxazines as Potent and Selective Acyl CoA:Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors with in Vivo Efficacy in Rodents
The discovery and optimization of a series of acyl CoA:diacylglycerol acyltransferase 1 (DGAT1) inhibitors based on a pyrimido[4,5-b][1,4]oxazine scaffold is described. The SAR of a moderately potent HTS hit was investigated resulting in the discovery of phenylcyclohexylacetic acid 1, which displayed good DGAT1 inhibitory activity, selectivity, and PK properties. During preclinical toxicity studies
描述和优化了一系列基于嘧啶[4,5- b ] [1,4]恶嗪骨架的酰基辅酶A:二酰基甘油酰基转移酶1(DGAT1)抑制剂。对中等强度HTS命中的SAR进行了研究,结果发现了苯基环己基乙酸1,该苯基环己基乙酸显示出良好的DGAT1抑制活性,选择性和PK性能。在临床前毒性研究过程中,观察到代谢物1升高了肝酶ALT和AST的水平。随后,合成类似物以排除有毒代谢物的形成。这项工作导致发现了螺螺茚满42,与1相比,螺螺茚满42显示出对DGAT1抑制作用的显着改善。。Spiroindane 42在啮齿动物体内具有良好的耐受性,在小鼠口服甘油三酸酯摄取研究中显示出功效,并且在临床前毒性研究中具有可接受的安全性。
RESIN COMPOSITION, LAMINATE, RESIN COMPOSITION LAYER-ATTACHED SEMICONDUCTOR WAFER, SUBSTRATE FOR MOUNTING RESIN COMPOSITION LAYER-ATTACHED SEMICONDUCTOR, AND SEMICONDUCTOR DEVICE
申请人:MITSUBISHI GAS CHEMICAL COMPANY, INC.
公开号:EP3786200A1
公开(公告)日:2021-03-03
A resin composition that has excellent flux activity, flexibility and storage stability and that is suitable for a pre-applied underfill material is provided. The resin composition of the present invention contains a compound (A) having a phenolic hydroxy group, a metal ion trapping agent (B) and a radical polymerizable compound (C).
RESIN COMPOSITION, LAMINATE, SEMICONDUCTOR WAFER WITH RESIN COMPOSITION LAYER, SUBSTRATE FOR MOUNTING SEMICONDUCTOR WITH RESIN COMPOSITION LAYER AND SEMICONDUCTOR DEVICE
申请人:MITSUBISHI GAS CHEMICAL COMPANY, INC.
公开号:US20210277221A1
公开(公告)日:2021-09-09
A resin composition that has excellent flux activity, flexibility and storage stability and that is suitable for a pre-applied underfill material is provided. The resin composition contains a compound (A) having a phenolic hydroxy group, a metal ion trapping agent (B) and a radical polymerizable compound (C).
[DE] MITTEL ZUM FÄRBEN VON KERATINHALTIGEN FASERN<br/>[EN] AGENTS FOR DYEING FIBRES CONTAINING KERATIN<br/>[FR] AGENT POUR LA COLORATION DE FIBRES KERATINIQUES
申请人:HENKEL KGAA
公开号:WO2001089587A2
公开(公告)日:2001-11-29
Es wird ein Mittel zum Färben von keratinhaltigen Fasern, insbesondere menschlichen Haaren, beansprucht, enthaltend mindestens ein Nitrosopyridin und/oder -pyrimidin mit der Formel (I), in der bedeuten Q ein Stickstoffatom oder die Gruppe CR?4 und R1, R2, R3 und R4¿, die gleich oder verschieden sein können, Wasserstoff, Halogen, eine C¿1?-C4-Alkylgruppe, C1-C4-Alkoxygruppe, C1-C4-Hydroxyalkylgruppe oder C1-C4-Hydroxyalkoxygruppe, eine Hydroxygruppe, eine Mercaptogruppe, eine Sulfogruppe, eine Carboxygruppe oder eine Aminogruppe, welche durch C1-C4-Alkyl-, C1-C4-Hydroxyalkyl- oder C1-C4-Acylgruppen substituiert sein kann, wobei auch zwei der Reste gemeinsam einen ankondensierten aromatischen beziehungsweise heteroaromatischen Ring bilden können.
Synthesis of 7-Aryl-2-dimethylamino-3,4,5,6-tetrahydropteridine-4,6-diones
作者:Masahiko Takahashi、Edward C. Taylor、Norio Kobayashi