3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVE AND USE THEREOF AS PHARMACEUTICAL

• Main Authors: WIRTH KLAUS, HERMAN SCHREUDER, CHRISTIAN BUNING, THORSTEN SADOWSKI, GEORGE HORSTICK, JOSEF PERNERSTORFER, SVEN RUF
• Format: Patent
• Language: English; Japanese
• Published: 09.02.2017
• 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 a compound which is an inhibitor of protease cathepsin A and useful for a treatment of atherosclerosis, cardiac failure, renal disease, hepatic failure, inflammation diseases or the like.SOLUTION: There is provided a 3-heteroaroylamino-propionic acid derivative represented by the formula I, where Ht is an imidazole ring binding to a substituent value at a specific position, an imidazole ring, an indazole ring, [1,2,4] oxadiazole ring, a pyrazole ring, a furan ring or the like, G is R-O-C(O)-, R-N(R)- or the like, Ris cycloalkyl, substituted/unsubstituted alkyl group or the like, Ris H or alkyl, Ris H, a hydroxyl group, alkyl or the like and Ris H or alkyl.SELECTED DRAWING: None 【課題】プロテアーゼカテプシンＡの阻害剤で、アテローム性動脈硬化症、心不全、腎疾患、肝疾患又は炎症性疾患等の処置に有用な化合物の提供。【解決手段】式Ｉで表される３−ヘテロアロイルアミノ−プロピオン酸誘導体。［Ｈｔは特定の位置に置いて置換基値と結合したイミダゾール環、インダゾール環、［１，２，４］オキサジアゾール環、ピラゾール環、フラン環等；ＧはＲ７１−Ｏ−Ｃ（Ｏ）−，Ｒ７２−Ｎ（Ｒ７３）−等；Ｒ３０はシクロアルキル、置換／非置のアルキル等；Ｒ４０はＨ又はアルキル；Ｒ５０はＨ、水酸基、アルキル等；Ｒ６はＨ又はアルキル］【選択図】なし