IP Library › Granted Patent US 11,912,727
Granted Patent B2
US 11,912,727 · App. 18/349,336 · Granted Feb 27, 2024

Arginase inhibitors and methods of use thereof

Inventors: Scott Nathan Mlynarski (Waltham, MA); Tyler Grebe (Waltham, MA); Sameer Kawatkar (Waltham, MA); Maurice Raymond Verschoyle Finlay (Cambridge, GB); Iain Simpson (Cambridge, GB); Jianyan Wang (Waltham, MA); Steve Cook (Waltham, MA); Dedong Wu (Waltham, MA)
Assignee: AstraZeneca AB
C07F5/025
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Quick Facts
Patent No.
US 11,912,727
App. No.
18/349,336
Granted
Feb 27, 2024
Kind
B2
Abstract

Disclosed are compounds of formula (Ia) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of formula (Ia) and methods of using the same for treating cancer or a respiratory inflammatory disease and inhibiting arginase: wherein R 1 is —NHR 1a ; R 1a is —H or —C(O)CH(R 1b )NHR 1c ; and R 1b is selected from —H, —(C 1 -C 4 ) alkyl and CH 2 OR 1d and R 1c is —H; or R 1b and R 1c , together with the atom to which they are attached, form a 5-membered heterocyclic ring; and R 1d is H or —CH 3 .

Claims (27)

1. A compound of formula (II), or a pharmaceutically acceptable salt thereof:

wherein

R 2 is —OH or —NHR 2a ;

R 2a is —H or —C(O)CH(R 2b )NH 2 ; and

R 2b is —CH 3 or —CH(CH 3 ) 2 .

2. The compound of claim 1 represented by formula (III), or a pharmaceutically acceptable salt thereof:

wherein R 3 is —CH 3 or —CH(CH 3 ) 2 .

3. A compound of formula (IIb), or a pharmaceutically acceptable salt thereof:

wherein

R 2 is —OH or —NHR 2a ;

R 2a is —H or —C(O)CH(R 2b )NH 2 ; and

R 2b is —CH 3 or —CH(CH 3 ) 2 .

4. The compound of claim 3 represented by formula (IIIb), or a pharmaceutically acceptable salt thereof:

wherein R 3 is —CH 3 or —CH(CH 3 ) 2 .

5. The compound of claim 1 selected from:

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 1 , having the following structure

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 1 , having the following structure

8. The compound of claim 1 , having the following structure

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 1 , having the following structure

10. The compound of claim 3 , having the following structure

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 3 , having the following structure

12. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

13. A pharmaceutical composition comprising a compound of claim 3 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignments (16)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: MLYNARSKI, SCOTT NATHAN; GREBE, TYLER; KAWATKAR, SAMEER
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 065593/0612 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA PHARMACEUTICALS LP
To: ASTRAZENECA UK LIMITED
Reel/Frame 065593/0720 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: SIMPSON, IAIN; VERSCHOYLE FINLAY, MAURICE RAYMOND
To: ASTRAZENECA UK LIMITED
Reel/Frame 065593/0888 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 065593/0962 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: MLYNARSKI, SCOTT NATHAN; GREBE, TYLER; KAWATKAR, SAMEER
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 065594/0172 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA PHARMACEUTICALS LP
To: ASTRAZENECA UK LIMITED
Reel/Frame 065594/0277 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: SIMPSON, IAIN; VERSCHOYLE-FINLAY, MAURICE RAYMOND
To: ASTRAZENECA UK LIMITED
Reel/Frame 065594/0436 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 065594/0498 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: MLYNARSKI, SCOTT NATHAN; GREBE, TYLER; KAWATKAR, SAMEER
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 065594/0690 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: WANG, JIANYAN; COOK, STEVE
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 065595/0014 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA PHARMACEUTICALS LP
To: ASTRAZENECA UK LIMITED
Reel/Frame 065595/0126 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: VERSCHOYLE FINLAY, MAURICE RAYMOND; SIMPSON, IAIN
To: ASTRAZENECA UK LIMITED
Reel/Frame 065595/0319 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 065595/0457 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: WU, DEDONG
To: ASTRAZENECA PHARMACEUTICALS LP
Reel/Frame 065595/0745 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA PHARMACEUTICALS LP
To: ASTRAZENECA UK LIMITED
Reel/Frame 065595/0939 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2023
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 065596/0120 →
Continuity (7)
Continuation 17812736 · Jul 15, 2022
Continuation 16969739
Provisional Application 62778002 · Dec 11, 2018
Provisional Application 62671576 · May 15, 2018
Provisional Application 62631659 · Feb 17, 2018
Provisional Application 62721113 · Aug 22, 2018
Related Publication 20230365599A1 · Nov 16, 2023
Cited By (2)
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