Title:
1- [([1, 5] Nauchi lysine 2- Il ) methyl] -3-methyl 7- (2- Butyne - 1- Il ) -8 - ((R) -3-amino piperidine 1- Il ) - Xanthine or its salt
Document Type and Number:
Japanese Patent JP6139004
Kind Code:
B2
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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Inventors:
Himmelsbach Frank
Rank Corp Elf
Eckhart Matthias
Marc michael
Mayer Laurent
Lots Ralph Richard Hermann
Tadaion Mohammad
Rank Corp Elf
Eckhart Matthias
Marc michael
Mayer Laurent
Lots Ralph Richard Hermann
Tadaion Mohammad
Application Number:
JP2016132807A
Publication Date:
May 31, 2017
Filing Date:
July 04, 2016
Export Citation:
Assignee:
Boehringer Ingelheim Pharma Gesellshaft Mitt Beschlenktel Haftung Und Company Comandito Gesellshaft
International Classes:
C07D519/00; A61K9/02; A61K9/20; A61K9/28; A61K9/48; A61K31/4375; A61K47/02; A61P3/10; A61P43/00; C07D473/04; C07D473/06; C07D473/08
Domestic Patent References:
| JP4395304B2 | ||||
| JP4233524B2 | ||||
| JP5351486B2 | ||||
| JP5623459B2 |
Attorney, Agent or Firm:
Takaki Nishijima
Disciple Maru Ken
Shinichiro Tanaka
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori
Disciple Maru Ken
Shinichiro Tanaka
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori