IP Library Granted Patent US 9,758,539
Granted Patent B2
US 9,758,539 · App. 15/158,206 · Granted Sep 12, 2017

Alvocidib prodrugs having increased bioavailability

Inventors: Adam Siddiqui-Jain (South Jordan, UT); David J. Bearss (Alpine, UT)
Assignee: Tolero Pharmaceuticals, Inc.
C07F9/65586C07D311/22C07D311/30C07D405/04
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Quick Facts
Patent No.
US 9,758,539
App. No.
15/158,206
Granted
Sep 12, 2017
Kind
B2
Abstract

Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R 1 , R 2 or R 3 is —P(═O)(OH) 2 , and the other two of R 1 , R 2 and R 3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.

Claims (17)

1. A compound having the following structure (I):

or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein:

i) R 1 is —P(═O)(OH) 2 , and R 2 and R 3 are each H;

ii) R 2 is —P(═O)(OH) 2 , and R 1 and R 3 are each H; or

iii) R 3 is —P(═O)(OH) 2 , and R 1 and R 2 are each H.

2. The compound of claim 1 , having the following structure (I′):

3. The compound of claim 1 , having the following structure (IA):

4. The compound of claim 3 , having the following structure (IA′):

5. The compound of claim 1 , having the following structure (IB):

6. The compound of claim 5 , having the following structure (IB′):

7. The compound of claim 1 , having the following structure (IC):

8. The compound of claim 7 , having the following structure (IC′):

9. A pharmaceutically acceptable salt of a compound according to claim 1 .

10. The pharmaceutically acceptable salt of claim 9 , wherein the pharmaceutically acceptable salt is a base addition salt.

11. The pharmaceutically acceptable salt of claim 10 , wherein the pharmaceutically acceptable salt is a sodium salt.

12. The pharmaceutically acceptable salt of claim 9 , wherein the pharmaceutically acceptable salt is an acid addition salt.

13. The pharmaceutically acceptable salt of claim 12 , wherein the pharmaceutically acceptable salt is a hydrochloride salt.

Assignments (5)
CHANGE OF NAME Recorded Apr 27, 2022
From: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
To: SUMITOMO PHARMA ONCOLOGY, INC.
Reel/Frame 059809/0557 →
MERGER Recorded Jul 10, 2020
From: TOLERO PHARMACEUTICALS, INC.
To: BOSTON BIOMEDICAL, INC.
Reel/Frame 053172/0833 →
CHANGE OF NAME Recorded Jul 10, 2020
From: BOSTON BIOMEDICAL, INC.
To: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
Reel/Frame 053184/0705 →
SECURITY INTEREST Recorded Nov 17, 2016
From: TOLERO PHARMACEUTICALS, INC.
To: SUMITOMO DAINIPPON PHARMA CO., LTD.
Reel/Frame 040362/0884 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 5, 2016
From: SIDDIQUI-JAIN, ADAM; BEARSS, DAVID J.
To: TOLERO PHARMACEUTICALS, INC.
Reel/Frame 039358/0432 →
Continuity (2)
Provisional Application 62163188 · May 18, 2015
Related Publication 20160340376A1 · Nov 24, 2016