Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

New crystal forms of trelagliptin, and preparation methods and application of crystal forms

A technology of crystal forms and uses, applied in the field of organic chemistry, can solve problems such as undisclosed solid forms

Inactive Publication Date: 2016-04-27
SICHUAN HAISCO PHARMA CO LTD
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] CN1926128A, CN101360723A etc. disclose the preparation method of Trexagliptin, but all do not disclose its solid form

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • New crystal forms of trelagliptin, and preparation methods and application of crystal forms
  • New crystal forms of trelagliptin, and preparation methods and application of crystal forms
  • New crystal forms of trelagliptin, and preparation methods and application of crystal forms

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] The preparation of embodiment 1 Trexagliptin crystal form F

[0101] Dissolve 7.0g of trexagliptin in 30ml of 1,2-propanediol at 95-100°C, stir and dissolve, cool to room temperature and let stand overnight, filter with suction, beat the filter cake with 20ml of ethyl acetate for about 0.5 hours Trexagliptin crystal form F was obtained.

[0102] The measured powder X-ray diffraction pattern is shown in figure 1 , its measured value is as follows (get the measured value corresponding to the diffraction peak whose relative intensity is greater than 1%):

[0103]

[0104]

Embodiment 2

[0105] The preparation of embodiment 2 Trexagliptin crystal form F

[0106] At 80-90°C, dissolve 2.0g of trexagliptin in a mixed solvent of 2.5ml of 1,2-propanediol and 2.5ml of ethyl acetate, stir and dissolve, cool to room temperature naturally, and filter with suction to obtain trexagliptin crystals Type F.

Embodiment 3

[0107] The preparation of embodiment 3 Trexagliptin crystal form F

[0108] At 80-90°C, dissolve 6.0g of Trexagliptin in a mixed solvent of 4ml of 1,2-propanediol and 8ml of ethyl acetate, stir and dissolve, cool to room temperature naturally, filter with suction, and beat the filter cake with 30ml of ethyl acetate After about 1 hour, dry under reduced pressure at 30-40° C. to obtain trexagliptin crystal form F.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to new crystal forms of trelagliptin, and preparation methods and application of the crystal forms. Specifically, the invention relates to two new crystal forms of trelagliptin as a dipeptidyl peptidase IV inhibitor and preparation methods of the two new crystal forms, a pharmaceutical composition containing the new crystal forms of trelagliptin, and application of the new crystal forms of trelagliptin in manufacturing drugs for treating dipeptidyl-peptidase-IV-mediated diseases.

Description

technical field [0001] The present invention relates to the fields of organic chemistry and pharmacy, in particular to new crystal forms of Trexagliptin and their preparation methods and uses, pharmaceutical compositions containing these new crystal forms, and the use of these new crystal forms for the preparation of dipeptide-based Use in medicine for peptidase IV (DPP-IV) mediated diseases. Background technique [0002] Trelagliptin, chemical name: 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4- Dioxy-1(2H)-pyrimidinyl]methyl]-4-fluoro-benzonitrile, the structure is shown in formula I: [0003] [0004] Trexagliptin is an inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine amino dipeptidase that removes XFF-Pro from the amino terminus (N-terminus) of polypeptides and proteins dipeptide. DPP-IV is constitutively expressed on epithelial and endothelial cells of a variety of different tissues (gut, liver, kidney and placenta), is also found in body flui...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61K31/513A61P3/10A61P3/00A61P3/04A61P1/00A61P29/00A61P17/06A61P19/02A61P35/00
Inventor 胡志鹏林志忠付李袁道义徐同利周仕川李方群罗杰向志祥
Owner SICHUAN HAISCO PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com