US2016176912A1PendingUtilityA1
Novel Ticagrelor Co-Crystal
Est. expiryJun 1, 2031(~4.9 yrs left)· nominal 20-yr term from priority
A61K 31/7076A61K 31/616A61K 31/7042C07D 487/04A61P 43/00A61K 31/706C07H 19/16C07H 19/23A61K 31/7064A61K 31/7052A61P 9/00C07B 2200/13A61K 31/519C07H 19/167A61P 7/02
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Claims
Abstract
The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is acetyl salicylic acid, to processes for the preparation of the co-crystal, to the use of such a co-crystal 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 such a co-crystal.
Claims
exact text as granted — not AI-modified1 . A co-crystal of the compound {1S-[1α,2α,3β(1S*,2R*),5β]}-3-(7-{[2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol of formula (I) and a co-former molecule
wherein the co-former molecule is acetyl salicylic acid.
2 . A co-crystal of the compound of formula (I) and acetyl salicylic acid according to claim 1 , characterised in that it has an X-ray powder diffraction pattern with peaks as shown in the following Table
Angle (°2 Theta)
Measured at 1.5405 Å
d-spacing (Å)
2.73, 3.60, 7.28, 8.68, 8.98, 9.87
32.3, 24.5, 12.1, 10.2, 9.8, 9.0
wherein 2-theta values are +/−0.2°.
3 . A co-crystal of the compound of formula (I) and acetyl salicylic acid according to claim 2 , characterised in that it has an X-ray powder diffraction pattern with peaks in addition to those in claim 2 as shown in the following Table
Angle (°2 Theta)
Measured at 1.5405 Å
d-spacing (Å)
4.74, 6.12, 9.4, 11.31
18.6, 14.4, 9.4, 7.8
wherein 2-theta values are +/−0.2°.
4 . A co-crystal of the compound of formula (I) and acetyl salicylic acid according to claim 1 , characterised in that it has a stoichiometry of approximately 3:2 Compound A: acetyl salicylic acid.
5 . A method of preparing a co-crystal of the compound of formula (I) and acetyl salicylic acid as defined in claim 1 , said method comprising mixing a suspension of the compound of formula (I) and acetyl salicylic acid in a suitable solvent.
6 . A method of preparing a co-crystal of the compound of formula (I) and acetyl salicylic acid as defined in claim 5 , wherein the compound of formula (I) polymorph III is used.
7 . A pharmaceutical composition comprising a co-crystal of the compound of formula (I) and acetyl salicylic acid, as defined in claim 1 , and a pharmaceutically acceptable diluent or carrier.
8 - 10 . (canceled)
11 . A method of treating arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease by administering a therapeutically effective amount of a co-crystal of the compound of formula (I) and acetyl salicylic acid as defined in claim 1 .Cited by (0)
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