Reaction between (Z)-Arylchlorooximes and α-Isocyanoacetamides: A Procedure for the Synthesis of Aryl-α-ketoamide Amides
摘要:
(Z)-Arylchlorooximes and alpha-isocyanoacetamides undergo a smooth reaction to produce 1,3-oxazol-2-oxime derivatives in good yields. Opening of the oxazole ring and deoximation reaction give a facile access to aryl-alpha-ketoamide amides, a class of privileged scaffolds in medicinal chemistry and important synthetic intermediates in organic chemistry.
Reaction between (Z)-Arylchlorooximes and α-Isocyanoacetamides: A Procedure for the Synthesis of Aryl-α-ketoamide Amides
摘要:
(Z)-Arylchlorooximes and alpha-isocyanoacetamides undergo a smooth reaction to produce 1,3-oxazol-2-oxime derivatives in good yields. Opening of the oxazole ring and deoximation reaction give a facile access to aryl-alpha-ketoamide amides, a class of privileged scaffolds in medicinal chemistry and important synthetic intermediates in organic chemistry.
Oxadiazoline ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
申请人:——
公开号:US20040171651A1
公开(公告)日:2004-09-02
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
A compound represented by the formula (I)
1
wherein one of R
1
and R
2
is a hydrogen atom or a substituent and the other is an optionally substituted cyclic group;
W is a bond or a divalent aliphatic hydrocarbon group;
Y is a group of the formula: —OR
3
(wherein R
3
is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group) or an optionally esterified or amidated carboxyl group, or a salt thereof or a prodrug thereof has a superior insulin secretion promoting action and a hypoglycemic action and shows low toxicity. Therefore, the compound is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of diabetes and diabetic complications, and the like.
OXADIAZOLINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX
申请人:Hormann Robert Eugene
公开号:US20080255210A1
公开(公告)日:2008-10-16
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
A compound represented by the formula (I)
wherein one of R1 and R2 is a hydrogen atom or a substituent and the other is an optionally substituted cyclic group;
W is a bond or a divalent aliphatic hydrocarbon group;
Y is a group of the formula: -OR3 (wherein R3 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group) or an optionally esterified or amidated carboxyl group, or a salt thereof or a prodrug thereof has a superior insulin secretion promoting action and a hypoglycemic action and shows low toxicity. Therefore, the compound is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of diabetes and diabetic complications, and the like.
由式(I)代表的化合物
其中 R1 和 R2 中的一个是氢原子或取代基,另一个是任选取代的环状基团;
W 是键或二价脂族烃基;
Y 是式中的一个基团:-OR3(其中 R3 是氢原子、任选取代的烃基、任选取代的杂环基或任选取代的酰基)或任选酯化或酰胺化的羧基,或其盐或其原药具有优异的促进胰岛素分泌作用和降血糖作用,且毒性低。因此,该化合物可用作药物制剂,特别是用于预防或治疗糖尿病和糖尿病并发症等。