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New solid forms of trelagliptin and manufacturing method and purpose thereof

A solid and crystalline technology, applied in organic chemical methods, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the problems of undisclosed solid forms, etc.

Inactive Publication Date: 2014-08-27
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Patents CN1926128A, CN101360723A, etc. disclose the preparation method of Trexagliptin, but neither discloses its solid form

Method used

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  • New solid forms of trelagliptin and manufacturing method and purpose thereof
  • New solid forms of trelagliptin and manufacturing method and purpose thereof
  • New solid forms of trelagliptin and manufacturing method and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0137] The preparation of embodiment 1 Trexagliptin crystal form A

[0138] Dissolve 2.5g of Trexagliptin in 25ml of isopropanol at 75-78°C, cool to 5-10°C with stirring, filter with suction, and dry the resulting solid under reduced pressure at 45-50°C to obtain Quagliptin Gliptin crystal form A, white solid.

[0139] The measured powder X-ray diffraction pattern is shown in figure 1 , and its measured value is as follows (take the measured value corresponding to the diffraction peak whose relative intensity is greater than 1%):

[0140]

[0141]

Embodiment 2

[0142] The preparation of embodiment 2 Trexagliptin crystal form A

[0143] Dissolve 2.5 g of trexagliptin in 25 ml of tetrahydrofuran at 60-63°C, cool to 0-5°C while stirring, and filter with suction to obtain trexagliptin crystal form A as a white solid.

Embodiment 3

[0144] The preparation of embodiment 3 Trexagliptin crystal form A

[0145] Dissolve 2.5 g of Trexagliptin in 25 ml of ethyl acetate at 71-74°C, cool to 0-10°C while stirring, filter with suction, and dry the resulting solid under reduced pressure at 60-65°C to obtain Quagliptin Gliptin crystal form A, white solid.

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Abstract

The present invention relates to solid forms of trelagliptin, a preparation method therefor and applications thereof, and relates specifically to six new solid forms of the dipeptidyl peptidase-4 inhibitor trelagliptin and preparation methods therefor, as well as to pharmaceutical compositions comprising said solid forms of trelagliptin, and uses of same in the preparation of medicines for the treatment of diseases mediated by dipeptidyl peptidase-4.

Description

technical field [0001] The present invention relates to the fields of organic chemistry and pharmacy, in particular to six new solid forms of trelagliptin and their preparation methods, pharmaceutical compositions containing these new solid forms, and the use of these new solid forms for the preparation of Drug use in dipeptidyl 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 aminodipeptidase that removes Xaa-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 fluids, and is also expresse...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/513A61P3/10A61P3/04A61P1/00A61P25/00A61P17/06A61P19/02A61P29/00A61P31/18A61P35/00
CPCA61K31/513C07D401/04C07B2200/13A61P1/00A61P3/04A61P3/08A61P3/10A61P17/06A61P19/02A61P25/00A61P29/00A61P31/18A61P35/00A61P37/00
Inventor 付李袁道义罗杰赵雄徐同利向志祥
Owner SICHUAN HAISCO PHARMA CO LTD
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