New 8-(3-amino-piperidin-1-yl)-xanthine derivatives, preparing method and uses thereof as a pharmaceutic preparation
By developing [3-amino-piperidin-1-yl]-xanthine compounds, the problem that existing drugs are difficult to inhibit the activity of DPP-IV has been solved, and effective treatment of type I and type II diabetes has been achieved.
CN105001222AInactive Publication Date: 2015-10-28BOEHRINGER INGELHEIM PHARMA GMBH & CO KG
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Patent Information
- Application Number
- CN201510299950.3
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2003-03-20
- Filing Date
- 2003-08-18
- Publication Date
- 2015-10-28
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Technical Problem
Existing drugs are difficult to effectively inhibit the activity of the enzyme dipeptidyl peptidase-IV (DPP-IV), resulting in the inability to effectively prevent or treat diseases related to DPP-IV activity, such as type I and type II diabetes.
Method used
A novel [3-amino-piperidin-1-yl]-xanthine compound was developed as DPP by preparing its tautomers, enantiomers, diastereomers and their salts -Inhibitors of IV, used to reduce DPP-IV activity to treat related diseases.
Benefits of technology
The compound can effectively inhibit DPP-IV activity, thereby playing a role in preventing or treating diseases such as type I and type II diabetes, and provides a new treatment method.
✦ Generated by Eureka AI based on patent content.
Abstract
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.
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