IP Library › Granted Patent US 12,642,803
Granted Patent B2
US 12,642,803 · App. 18/072,246 · Granted Jun 2, 2026

Pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyljurea

Inventors: James Joseph Hussey (Sandwich, GB); Andrew Gilbert Bright (Winchester, GB)
Assignee: PFIZER INC.
A61K31/5377A61K9/0019A61K9/08A61K9/19A61K47/20A61K47/26A61K47/40
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Quick Facts
Patent No.
US 12,642,803
App. No.
18/072,246
Granted
Jun 2, 2026
Kind
B2
Abstract

The present invention relates to a pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable alkanesulphonate salt thereof, that is a clear solution. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.

Claims (10)

1 . A method of treating cancer in a mammal comprising administering to the mammal in need thereof an effective amount of a clear pharmaceutical aqueous solution formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea or an alkanesulphonate salt thereof.

2 . The method of claim 1 , wherein the solution formulation comprises 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or a methanesulphonate salt thereof, methanesulphonic acid and water, wherein 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea at a solution concentration of from 6 to 30 mg/ml.

3 . The method of claim 1 , wherein the solution formulation comprises 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or an ethanesulphonate salt thereof, ethanesulphonic acid and water, wherein 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea at a solution concentration of from 6 to 30 mg/ml.

4 . The method of claim 1 , wherein the solution formulation further comprises one or more cyclodextrins selected from the group consisting of beta-cyclodextrins, gamma-cyclodextrins, or a mixture thereof.

5 . The method of claim 4 , wherein the one or more cyclodextrins comprise hydroxypropyl-beta-cyclodextrin.

6 . The method of claim 4 , wherein the one or more cyclodextrins comprise sulphobutylether-beta-cyclodextrin.

7 . The method of claim 4 , wherein the one or more cyclodextrins comprise gamma-cyclodextrin.

8 . The method of claim 1 , wherein the pH of the solution formulation is from 3 to 8.

9 . The method of claim 1 , wherein the solution formulation is administered at a weekly dose in a range from 100 to 400 mg per week.

10 . A method of claim 1 , wherein the cancer is selected from the group consisting of leukemia, skin cancer, bladder cancer, breast cancer, uterus cancer, ovary cancer, prostate cancer, lung cancer, colon cancer, pancreas cancer, renal cancer, gastric cancer and brain cancer.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2022
From: PFIZER LIMITED
To: PFIZER INC.
Reel/Frame 062016/0172 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2022
From: BRIGHT, ANDREW GILBERT
To: PFIZER LIMITED
Reel/Frame 062016/0239 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2022
From: HUSSEY, JAMES JOSEPH
To: PFIZER LIMITED
Reel/Frame 062016/0322 →
Continuity (5)
Continuation 16641045
Provisional Application 62703022 · Jul 25, 2018
Provisional Application 62681720 · Jun 7, 2018
Provisional Application 62550007 · Aug 25, 2017
Related Publication 20230218628A1 · Jul 13, 2023
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