4位に置換基を有する2−シアノピロリジン誘導体及びその製造方法並びにそれを含有する薬剤

2-cyanopyrrolidine derivative having substituent at 4-position, method for producing the same, and medicament containing the same

Abstract

【課題】優れたジペプチジルペプチダーゼ(DPP-IV)阻害活性及び高い安定性を有し、糖尿病、肥満、HIV感染、癌転移、皮膚炎、前立腺肥大症、歯根膜炎又は自己免疫疾患の予防/治療に有用な4位に置換基を有する2-シアノピロリジン誘導体又はその塩を提供する。 【解決手段】次式の一般式(I): 【化1】 [式中、Aはフッ素原子、モノフルオロメチル基、ジフルオロメチル基又はトリフルオロメチル基、Bは-C(CH 3 ) 2 CH 2 -NH-D又は 【化2】 (式中、実線と点線を併記した結合は、単結合又は二重結合を示す。Dは置換基を有してもよい複素環を示す。)、Cは水素原子、低級アルキル基(C1-C8)を示す。] で表される4位に置換基を有する2−シアノピロリジン誘導体又はその医薬上許容される塩である。
PROBLEM TO BE SOLVED: To obtain a 2-cyanopyrrolidine derivative having a substituent at the 4-position or its salt, having excellent dipeptidylpeptidase (DPP-IV) inhibitory activity and high stability, and useful for preventing/treating diabetes, obesity, HIV infection, metastasis of cancer, dermatitis, prostatomegaly, periodontitis or autoimmune diseases. SOLUTION: The 2-cyanopyrrolidine derivative expressed by formula (I) [A is F, monofluoromethyl, difluoromethyl or trifluoromethyl; B is C-(CH 3 ) 2 CH 2 -NH-D or expressed by formula (2) (a bond expressed by a full line together with a dotted line is a single bond or a double bond; and D is a heterocyclic ring which may be substituted); and C is H or a 1-8C lower alkyl] and having the substituent at the 4-position, or its pharmaceutically acceptable salt, is provided in the specification. COPYRIGHT: (C)2004,JPO&NCIPI

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