Co-Crystals Of A Triazolo [4,5-D] Pyrimide Platelet Aggregation Inhibitor

A technology of co-crystals and crystals, applied in the field of novel co-crystals, can solve problems such as vascular bed occlusion

Inactive Publication Date: 2014-12-24
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the process of platelet adhesion to the subendothelial surface may play an important role in the repair of damaged vessel walls, platelet aggregation thus induced can promote acute thrombotic occlusion of important vascular beds, leading to events with high morbidity such as Myocardial infarction and unstable angina

Method used

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  • Co-Crystals Of A Triazolo [4,5-D] Pyrimide Platelet Aggregation Inhibitor
  • Co-Crystals Of A Triazolo [4,5-D] Pyrimide Platelet Aggregation Inhibitor
  • Co-Crystals Of A Triazolo [4,5-D] Pyrimide Platelet Aggregation Inhibitor

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0089] For the preparation of soft gelatin capsules, the co-crystals of Compound A as defined herein may be mixed with eg vegetable oil or polyethylene glycol. Hard gelatine capsules may contain granules of the compound using the excipients mentioned above for tablets, such as lactose, sucrose, sorbitol, mannitol, starch, cellulose derivatives or gelatin. Liquid or semisolid formulations of the drug may also be filled into hard gelatin capsules.

[0090] Liquid preparations for oral administration may be in the form of syrups or suspensions, eg solutions containing the co-crystals of Compound A as defined herein, with the balance being sugar and a mixture of ethanol, water, glycerol and propylene glycol. Optionally, such liquid preparations may contain coloring agents, flavoring agents, saccharin and carboxymethylcellulose as a thickening agent, or other excipients known to those skilled in the art.

[0091] It is believed that the co-crystal of Compound A as defined herein r...

Embodiment 1

[0101] Example 1: Compound A co-crystal formation

[0102] The following coformers, which are readily available materials, were used to prepare using Compound A, which can be prepared as described in the PCT application mentioned herein, the relevant content of which is incorporated by reference and into the experiments in this paper).

[0103] Glycolic acid:

[0104] Salicylic Acid:

[0105] Capric acid (capric acid):

[0106] Gentisic acid (2,5-dihydroxybenzoic acid):

[0107] Glutaric acid:

[0108] Vanillic acid (4-hydroxy-3-methoxybenzoic acid)

[0109] Succinic acid:

[0110] Malonate:

[0111] Maltol (3-hydroxy-2-methyl-4-pyrone):

[0112] X-ray powder diffraction (XRPD) analysis was performed using an Inel XRG-3000 diffractometer equipped with a CPS (curved position sensitive) detector with a 2Θ range of 120°. Using Cu-Kα radiation (the wavelength of X-rays is ), to collect real-time data with a resolution of 0.03°2θ. The tube voltage an...

Embodiment l-A

[0113] Example 1-A: Compound A: Capric Acid Cocrystal Type A

[0114]10.3 mg capric acid in 500 μL methanol was added to 2 mL filtered solution of Compound A in acetone (15 mg / mL) with stirring. The vial was capped and wrapped with parafilm.

[0115] The resulting co-crystalline material gave the peaks listed in Example 2-C (see Figure 19 ) consistent diffraction pattern.

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Abstract

The present invention relates to novel co-crystal forms of the compound of formula (I) which is shown in the specification; wherein the co-former molecule is selected from glycolic acid, salicylic acid, decanoic (capric) acid, gentisic acid (2,5-dihydroxybenzoic acid), glutaric acid, vanillic acid (4-hydroxy-3-methoxybenzoic acid), succinic acid, malonic acid or maltol (3-hydroxy-2-methyl-4-pyrone); and to processes for their preparation, to pharmaceutical compositions containing such co-crystals, to the use of such co-crystals in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a co-crystal of the compound of formula (I).

Description

[0001] This application is an application number 201080063050.4 (international application number is PCT / GB2010 / 002222), the application date is December 3, 2010, and the invention name is "triazolo [4,5-D] pyrimidine platelet aggregation inhibitor. Crystal" is a divisional application of the Chinese patent application. technical field [0002] The present invention relates to novel co-crystals, more particularly to novel co-crystal forms of compounds of formula (I): [0003] [0004] The customary name of the compound of formula (I) is: {1S-[1α, 2α, 3β(1S ＊ , 2R ＊ ), 5β]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazole [4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol is hereinafter referred to as Compound A for convenience. [0005] More specifically, the present invention relates to several co-crystals of Compound A; their preparation; pharmaceutical compositions containing co-crystals of Compound A; Use in medicine for ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/519A61P7/02A61P9/10
CPCC07D487/04A61P7/02A61P9/00A61P9/10A61K31/519C07B2200/13
Inventor S. D. 科斯格罗夫M. J. 琼斯A. 波利亚科瓦-阿库斯V. N. 斯莫伦斯卡亚B. S. 沃尔费
Owner ASTRAZENECA AB
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