US2015366870A1PendingUtilityA1
Novel compounds
Est. expiryDec 8, 2028(~2.3 yrs left)· nominal 20-yr term from priority
A61P 9/10A61P 9/14A61P 7/02A61P 9/00A61P 3/10A61P 3/06A61P 9/04A61P 3/04A61P 3/00A61P 1/14A61P 13/12C07D 473/06A61K 31/133C07D 473/04A61K 31/522
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Claims
Abstract
The present invention relates to a tris salt of 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione of Formula (A): corresponding manufacture processes, pharmaceutical formulations containing and uses of the aforementioned compound in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A method for treating stroke in a human subject in need thereof, comprising administering to said subject a therapeutically effective amount of a compound which is 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxymethyl)aminomethane (Formula (IA):
2 . The method according to claim 1 wherein the compound is 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxymethyl)aminomethane anhydrate
3 . The method according to claim 2 wherein the compound is crystalline.
4 . The method according to claim 3 wherein the crystalline form of the compound is characterised by an XRPD pattern comprising the following peaks:
Position
d-spacing
(±0.2° 2-theta)
((Å))
10.1
8.7
10.5
8.4
12.2
7.3
13.0
6.8
13.5
6.5
17.3
5.1
17.5
5.1
17.9
5.0
18.3
4.8
19.2
4.6
19.8
4.5
20.2
4.4
20.6
4.3
20.9
4.2
21.7
4.1
22.1
4.0
23.3
3.8
23.9
3.7
24.6
3.6
26.3
3.4
27.1
3.3
27.9
3.2
28.2
3.2
28.6
3.1
29.6
3.0.
5 . The method according to claim 3 wherein the crystalline form of the compound is characterised by an XRPD pattern that is substantially as shown in FIG. 2 .
6 . The method according to claim 3 wherein the crystalline form of the compound is characterised by a melting endotherm with an onset melting temperature of 212±2° C. in a DSC thermogram.
7 . The method according to claim 3 wherein the crystalline form of the compound is characterised by the following absorption peaks in an ATR-IR spectrum of the solid product: 3370, 3041, 2946, 2858, 1680, 1656, 1528, 1266, 1243, 1078, 1068, 1049±1 cm-1.
8 . The method according to claim 3 wherein the crystalline form of the compound is characterised in that it has an ATR infra red spectrum that is substantially as shown in FIG. 6 .
9 . A method for treating multiple sclerosis in a human subject in need thereof, comprising administering to said subject a therapeutically effective amount of a compound which is 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxymethyl)aminomethane (Formula (IA):
10 . The method according to claim 9 wherein the compound is 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxymethyl)aminomethane anhydrate.
11 . The method according to claim 10 wherein the compound is crystalline.
12 . The method according to claim 10 wherein the crystalline form of the compound is characterised by an XRPD pattern comprising the following peaks:
Position
d-spacing
(±0.2° 2-theta)
((Å))
10.1
8.7
10.5
8.4
12.2
7.3
13.0
6.8
13.5
6.5
17.3
5.1
17.5
5.1
17.9
5.0
18.3
4.8
19.2
4.6
19.8
4.5
20.2
4.4
20.6
4.3
20.9
4.2
21.7
4.1
22.1
4.0
23.3
3.8
23.9
3.7
24.6
3.6
26.3
3.4
27.1
3.3
27.9
3.2
28.2
3.2
28.6
3.1
29.6
3.0.
13 . The method according to claim 10 wherein the crystalline form of the compound is characterised by an XRPD pattern that is substantially as shown in FIG. 2 .
14 . The method according to claim 10 wherein the crystalline form of the compound is characterised by a melting endotherm with an onset melting temperature of 212±2° C. in a DSC thermogram.
15 . The method according to claim 10 wherein the crystalline form of the compound is characterised by the following absorption peaks in an ATR-IR spectrum of the solid product: 3370, 3041, 2946, 2858, 1680, 1656, 1528, 1266, 1243, 1078, 1068, 1049±1 cm-1.
16 . The method according to claim 10 wherein the crystalline form of the compound is characterised in that it has an ATR infra red spectrum that is substantially as shown in FIG. 6 .
17 . A method for treating inflammatory sequelae of viral or bacterial infection in a human subject in need thereof, comprising administering to said subject a therapeutically effective amount of a compound which is 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxymethyl)aminomethane anyhydrate (Formula (IA):
18 . The method according to claim 17 wherein the compound is 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxymethyl)aminomethane anhydrate.
19 . The method according to claim 18 wherein the compound is crystalline.
20 . The method according to claim 18 wherein the crystalline form of the compound is characterised by an XRPD pattern comprising the following peaks:
Position
d-spacing
(±0.2° 2-theta)
((Å))
10.1
8.7
10.5
8.4
12.2
7.3
13.0
6.8
13.5
6.5
17.3
5.1
17.5
5.1
17.9
5.0
18.3
4.8
19.2
4.6
19.8
4.5
20.2
4.4
20.6
4.3
20.9
4.2
21.7
4.1
22.1
4.0
23.3
3.8
23.9
3.7
24.6
3.6
26.3
3.4
27.1
3.3
27.9
3.2
28.2
3.2
28.6
3.1
29.6
3.0.
21 . The method according to claim 18 wherein the crystalline form of the compound is characterised by an XRPD pattern that is substantially as shown in FIG. 2 .
22 . The method according to claim 18 wherein the crystalline form of the compound is characterised by a melting endotherm with an onset melting temperature of 212±2° C. in a DSC thermogram.
23 . The method according to claim 18 wherein the crystalline form of the compound is characterised by the following absorption peaks in an ATR-IR spectrum of the solid product: 3370, 3041, 2946, 2858, 1680, 1656, 1528, 1266, 1243, 1078, 1068, 1049±1 cm-1.
24 . The method according to claim 18 wherein the crystalline form of the compound is characterised in that it has an ATR infra red spectrum that is substantially as shown in FIG. 6 .Join the waitlist — get patent alerts
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