힘멜스바흐 프랑크,랑코프 엘케,에크하르트 맛티아스,마르크 미하엘,마이어 롤란트,로츠 랄프 리하르트 헤르만,타다욘 모하매드
申请号：
KR1020097008185
公开号：
KR1011111010000B1
申请日:
2003.08.18
申请国别(地区):
KR
年份:
2012
代理人:
摘要：
8-(3-amino-piperidin-1-yl)-xanthine derivatives (I) are new. 8-(3-amino-piperidin-1-yl)-xanthine derivatives of formula (I) and their tautomers, enantiomers, diastereomers (or mixtures), prodrugs and salts are new. [Image] R 1>； : CH 2Q 1>；, CH 2CH 2OMe, CH 2CH 2OPh, CH 2CH 2CN, CH 2COPh or CHMeCOPh, phenylcarbonylmethyl mono-substituted in the ring by Q 2>； or phenylcarbonylmethyl substituted in the ring by two OMe groups or on two adjacent C-atoms by OCH 2O, OCH 2CH 2O or N(Me)COO； Q 1>； : CONMe 2, heterocycle or heteroaryl (optionally substituted)； Q 2>； : NH 2, NHCH 2CN, NHCOMe, NHCOEt, NHCOCHMe 2, NHCOOMe, NHCONHCOOEt, 2-oxo-imidazolin-1-yl, COOH, COMe, COOEt, CONH 2, CONHMe, CONMe 2, morpholinocarbonyl, SMe, SOMe, SO 2Me, OCH 2COOH, OCH 2COOEt, OCH 2COOCHMe 2, OCH 2CONH 2, OCH 2CONHMe, OCH 2CONHEt, OCH 2CONHCHMe 2, OCH 2CONMe 2, pyrrolidinocarbonyl-methoxy, morpholinocarbonyl-methoxy, OCHMeCOOEt, OCHMeCONH 2 or OCH 2SOMe； R 2>； : Me, CHMe 2 or Ph, and R 3>； : CH 2C(Me)=CH 2, CH 2C(Cl)=CH 2, CH 2CH=CHBr, CH 2CH=CHMe, CH 2C(Me)=CMe 2, CH 2CCMe, 1-cyclopenten-1-ylmethyl or 2-furanylmethyl. An independent claim is included for the preparation of (I). ACTIVITY : Antidiabetic； Antiarthritic； Anorectic； Immunosuppressive； Osteopathic； Ophthalmological； Nephrotropic； Neuroprotective； Antiarteriosclerosis； Tranquilizer； Cardiant； Diuretic； Hypotensive； Antiinflammatory； Antiulcer； Antiinfertility； Antirheumatic； Antithyroid； Virucide； Anti-HIV； Cytostatic； Nootropic； Cerebroprotective； Antiparkinsonian； Antimigraine； Antianemic； Dermatological； Antipsoriatic； Antidepressant. MECHANISM OF ACTION : Dipeptidylpeptidase-IV (DPP-IV) inhibitor； B-cell degeneration inhibitor； glucagon-like peptide (GLP) action modulator. 1-((Quinazolin-2-yl)-methyl)-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine (Ia) had an IC 50 value of 1 nM for inhibition of DPP-IV.본 발명은 화학식 1의 신규한 치환된 크산틴, 이의 호변이성체, 이의 입체이성체, 및 혼합물, 이의 전구약물 및 이의 염에 관한 것이며, 이는 매우 유용한 약리학적 특
