IP Library Patent Application 15780212
Patent Application
App. No. 15/780,212

SOLID DISPERSIONS COMPRISING A SGC STIMULATOR

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Quick Facts
Patent No.
US None
App. No.
15/780,212
Abstract

The present invention relates to solid dispersions of amorphous 1,1,1,3,3,3-hexafluoro-2-(((5-fluoro-2-(1-(2-fluorobenzyl)-5-(isoxazol-3-yl)-1H-pyrazol-3-yl)pyrimidin-4-yl)amino)methyl)propan-2-ol (Compound I) or a pharmaceutically acceptable salt thereof. It also relates to pharmaceutical compositions and pharmaceutical oral dosage unit forms comprising them, and their uses thereof.

Claims (33)

1 . A solid dispersion of amorphous 1,1,1,3,3,3-hexafluoro-2-(((5-fluoro-2-(1-(2-fluorobenzyl)-5-(isoxazol-3-yl)-1H-pyrazol-3-yl)pyrimidin-4-yl)amino)methyl)propan-2-ol (Compound I) and a cellulosic polymer selected from hydroxypropylmethylcellulose acetate succinate (HPMCAS), hydroxypropylmethylcellulose phthalate (HPMCP), cellulose acetate phthalate (CAP), polyvinyl pyrrolidone (PVP), or a co-polymer of polyvinyl pyrrolidone.

2 - 5 . (canceled)

6 . The solid dispersion of claim 1 wherein the polymer carrier is HPMCAS.

7 - 10 . (canceled)

11 . The solid dispersion of claim 1 , wherein the polymer is present in an amount of between about 40% and about 95% of the total weight of the solid dispersion.

12 . The solid dispersion of claim 11 , wherein the polymer is present in an amount of between 50% and 90%, between about 60% and about 90%, between about 60% and about 95%, or between about 70% and about 90% of the total weight of the solid dispersion.

13 - 15 . (canceled)

16 . The solid dispersion of claim 12 , wherein the polymer is present in an amount of between about 75% and about 90% of the total weight of the solid dispersion.

17 - 18 . (canceled)

19 . The solid dispersion of claim 1 , wherein said solid dispersion is obtained by spray-drying.

20 - 21 . (canceled)

22 . The solid dispersion of claim 1 , wherein Compound I is present in an amount of from about 5% by weight to about 40% by weight, from about 10% by weight to about 30% by weight, from about 10% by weight to about 25% by weight, from about 15% by weight to about 40% by weight, or from about 20% by weight to about 30% by weight of the dispersion.

23 - 26 . (canceled)

27 . The solid dispersion of claim 1 , wherein said solid dispersion of Compound I comprises less than 20%, less than 10%, or less than 5% crystalline Compound I.

28 - 31 . (canceled)

32 . The solid dispersion of claim 1 , wherein the weight to weight ratio of Compound I to polymer is between 20:80 and 40:60.

33 . The solid dispersion of claim 32 , wherein the weight to weight ratio of Compound I to polymer is 25:75.

34 . (canceled)

35 . A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a solid dispersion according to claim 1 .

36 . (canceled)

37 . An oral dosage unit form, comprising a solid dispersion of claim 1 .

38 - 39 . (canceled)

40 . The oral dosage unit form according to claim 37 , wherein said dosage unit form is a tablet.

41 . A method of treating a disease, health condition or disorder in a subject in need of treatment, comprising administering a therapeutically effective amount of an amorphous solid dispersion of claim 1 , to the subject in need of treatment, wherein the disease, health condition or disorder is selected from: diabetic nephropathy, diabetic retinopathy, non-alcoholic steatohepatitis (NASH), hypertension, or heart failure.

42 . The method of claim 41 , wherein the disease is diabetic nephropathy.

43 . The method according to claim 41 , wherein the disease or disorder is diabetic retinopathy.

44 . The method according to claim 41 , wherein the disease or disorder is non-alcoholic steatohepatitis.

45 . The method according to claim 41 , wherein the disease or disorder is heart failure, wherein the heart failure is heart failure with preserved ejection fraction (HFpEF) or heart failure with reduced ejection fraction (HFrEF).

46 . (canceled)

47 . The method of claim 45 , wherein said heart failure is HFpEF.

48 . (canceled)

49 . The method according to claim 41 , wherein the disease or disorder is hypertension.

50 . The method according to claim 49 , wherein said hypertension is resistant hypertension.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 10, 2019
From: IRONWOOD PHARMACEUTICALS, INC.
To: CYCLERION THERAPEUTICS, INC.
Reel/Frame 048853/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 29, 2018
From: DUNBAR, CRAIG ANTONY; SETHURAMAN, VASU; HASHASH, AHMAD
To: IRONWOOD PHARMACEUTICALS, INC
Reel/Frame 047339/0542 →