CYCLOALKYL-SUBSTITUTED IMIDAZOLE DERIVATIVE

• Main Authors: NAGATA TSUTOMU, ONO MAKOTO, NOGUCHI KENGO, INOUE MASAHIRO, ASHIDA YUKA
• Format: Patent
• Language: English; Japanese
• Published: 13.07.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide therapeutic drugs that exhibit a TAFIa-inhibiting activity and are useful for the treatment of myocardial infarction, angina, acute coronary syndrome, cerebral infarction, deep vein thrombosis, and pulmonary embolism.SOLUTION: This invention provides compounds represented by general formula (I) wherein A represents a C3-C12 cycloalkyl group optionally substituted by 1-3 substituents selected from among fluoro groups, hydroxide groups, a C1-C6 alkyl group and the like; R1, R2 and R3 each individually represent a hydrogen atom, a fluoro group or a C1-C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents -CH2-CHR5-CH2-NHR6, in which R5 represents a hydrogen atom, a C1-C6 alkyl group or a C1-C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group, and pharmacologically-acceptable salts thereof.SELECTED DRAWING: None 【課題】ＴＡＦＩａ酵素阻害活性を有する、心筋梗塞、狭心症、急性冠不全症候群、脳梗塞、深部静脈血栓症、肺塞栓症などの治療薬を提供する。【解決手段】下記の一般式（Ｉ）【化１】［式中、Ａはフルオロ基、水酸基、Ｃ１〜Ｃ６アルキル基等から選ばれる１〜３個で置換されていてもよいＣ３〜Ｃ１２シクロアルキル基を示し、Ｒ１、Ｒ２及びＲ３は各々独立して水素原子、フルオロ基又はＣ１〜Ｃ６アルキル基を示し、Ｒ４は水素原子又はプロドラッグ基を示し、Ｙは−ＣＨ２−ＣＨＲ５−ＣＨ２−ＮＨＲ６（ここで、Ｒ５は水素原子、Ｃ１〜Ｃ６アルキル基又はＣ１〜Ｃ６アルコキシ基を示し、Ｒ６は水素原子又はプロドラッグ基を示す。）等を示す。］で表される化合物、またはその薬理上許容される塩。【選択図】なし