IP Library Granted Patent US 10,533,001
Granted Patent B2
US 10,533,001 · App. 15/828,154 · Granted Jan 14, 2020

Inhibitors of protein kinases

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Quick Facts
Patent No.
US 10,533,001
App. No.
15/828,154
Granted
Jan 14, 2020
Kind
B2
Abstract

The present invention is directed to topical pharmaceutical compositions of Formula (If) or pharmaceutically acceptable salt thereof, which act as inhibitors of syk and/or JAK kinase activity. The described topical pharmaceutical compositions are useful in preventing or treating a number of conditions mediated at least in part by syk and/or JAK kinase activity.

Claims (24)

1. A topical pharmaceutical composition comprising a compound of

Formula If

or pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers,

wherein

D 1b is C 3-8 cycloalkyl;

R 1b is selected from the group consisting of

each of which is substituted with from 1 to 2 substituents independently selected from the group consisting of hydroxyl, hydroxyC 1-8 alkylene, C 1-8 alkoxyC 1-8 alkylene, C 1-8 alkylcarbonyl, carboxy and C 1-8 alkylsulfonyl;

R 2b is H or halo; and

the wavy line in the substituents of R 1b indicates the point of attachment to the rest of the molecule.

2. The topical pharmaceutical composition of claim 1 , wherein

R 1b is

3. The topical pharmaceutical composition of claim 1 , wherein R 1b is substituted with from 1 to 2 substituents independently selected from the group consisting of C 1-8 alkylcarbonyl and C 1-8 alkylsulfonyl.

4. The topical pharmaceutical composition of claim 3 , wherein R 1b is substituted with a C 1-8 alkylsulfonyl substituent.

5. The topical pharmaceutical composition of claim 3 , wherein R 1b is substituted with a C 1-8 alkylcarbonyl substituent.

6. The topical pharmaceutical composition of claim 1 , wherein R 2b is H.

7. The topical pharmaceutical composition of claim 1 , wherein said compound of Formula If has the formula

or a pharmaceutically acceptable salt thereof.

8. The topical pharmaceutical composition of claim 1 , wherein said compound of Formula If has the formula

or a pharmaceutically acceptable salt thereof.

9. The topical pharmaceutical composition of claim 1 , wherein said topical pharmaceutical composition is in the form of an emulsion, a lotion, a gel, a foam, a cream, a jelly, a solution, a suspension, an ointment, or a transdermal patch.

10. The topical pharmaceutical composition of claim 9 , wherein said topical pharmaceutical composition is in the form of an ointment.

11. The topical pharmaceutical composition of claim 9 , wherein said topical pharmaceutical composition is in the form of a lotion or a cream.

12. The topical pharmaceutical composition of claim 1 , wherein said topical pharmaceutical composition is suspended or dissolved in said one or more carriers.

13. The topical pharmaceutical composition of claim 12 , wherein said one or more carriers is selected from the group consisting of mineral oil, liquid petrolatum, white petrolatum, propylene glycol, polyoxyethylene, polyoxypropylene compound, emulsifying wax, sorbitan monostearate, polysorbate 60, cetyl esters, wax, cetyl alcohol, 2-octyldodecanol, benzyl alcohol and water.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 14, 2021
From: PORTOLA PHARMACEUTICALS, LLC
To: ALEXION PHARMACEUTICALS, INC.
Reel/Frame 054999/0218 →
CHANGE OF NAME Recorded Jan 12, 2021
From: PORTOLA PHARMACEUTICALS, INC.
To: PORTOLA PHARMACEUTICALS, LLC
Reel/Frame 054975/0183 →
RELEASE OF SECURITY INTEREST Recorded Jul 2, 2020
From: HCR COLLATERAL MANAGEMENT, LLC
To: PORTOLA PHARMACEUTICALS, INC.
Reel/Frame 053120/0925 →
SECURITY INTEREST Recorded Mar 18, 2019
From: PORTOLA PHARMACEUTICALS, INC.
To: HCR COLLATERAL MANAGEMENT, LLC
Reel/Frame 048633/0673 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 25, 2018
From: BAUER, SHAWN M.; JIA, ZHAOZHONG J.; SONG, YONGHONG; XU, QING; MEHROTRA, MUKUND; ROSE, JACK W.; HUANG, WOLIN; VENKATARAMANI, CHANDRASEKAR; PANDEY, ANJALI
To: PORTOLA PHARMACEUTICALS, INC.
Reel/Frame 044732/0519 →