IP Library Granted Patent US 11,584,775
Granted Patent B2
US 11,584,775 · App. 15/760,662 · Granted Feb 21, 2023

C4-modified oleanolic acid derivatives for inhibition of IL-17 and other uses

Inventors: Melean Visnick (Irving, TX); Xin Jiang (Coppell, TX); Martha R. Hotema (Hurst, TX); Chitase Lee (Ann Arbor, MI); Bradley William Caprathe (Livonia, MI); William H. Roark (Ann Arbor, MI); Gary L. Bolton (Ann Arbor, MI)
Assignee: REATA PHARMACEUTICALS, Inc.
C07J63/008A61P29/00C07J71/0005
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Quick Facts
Patent No.
US 11,584,775
App. No.
15/760,662
Granted
Feb 21, 2023
Kind
B2
Abstract

Disclosed herein are C4 modified oleanolic acid derivatives of the formula: Formula (X) or Formula (XII), as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17.

Claims (25)

1. A compound of the formula:

wherein:

R 1 is alkyl (C≤8) ;

R 3 is hydrogen or hydroxy, or R 3 is taken together with Y as described below;

Y is heteroaryl (C≤8) or substituted versions thereof;

—C(O)R c , wherein R c is hydroxy, alkoxy (C≤8) ; alkylamino (C≤8) , dialkyl-amino (C≤8) , or a substituted version of any of these groups;

—NR d C(O)R e , wherein: R d is hydrogen; and R e is alkyl (C≤8) , alkoxy (C≤8) , or a substituted version of any of these groups; or

Y is taken together with R 3 and is —C(O)O—;

wherein when the terms alkyl, alkoxy, alkylamino, dialkylamino, and heteroaryl are used with the substituted modifier, one or more hydrogen atom has been independently replaced by —F;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein R 1 is methyl.

3. The compound of claim 1 , wherein Y is heteroaryl (C≤8) or substituted heteroaryl (C≤8) .

4. The compound of claim 1 , wherein Y is taken together with R 3 and is —C(O)O—.

5. The compound of claim 1 , wherein Y is —C(O)R c , wherein R c is hydroxy or alkoxy (C ≤8) .

6. The compound of claim 1 , wherein R3 is hydrogen.

7. The compound of claim 1 , wherein the compound is further defined as:

or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition comprising:

(A) a compound of claim 1 ; and

(B) an excipient or a pharmaceutically acceptable carrier.

9. The compound of claim 1 , further defined as:

or a pharmaceutically acceptable salt thereof.

10. A pharmaceutical composition comprising:

(A) a compound of claim 9 ; and

(B) an excipient or a pharmaceutically acceptable carrier.

Assignments (9)
RELEASE OF SECURITY INTEREST Recorded Apr 9, 2025
From: BIOPHARMA CREDIT PLC
To: REATA PHARMACEUTICALS HOLDINGS, LLC; REATA PHARMACEUTICALS GLOBAL, INC.; REATA PHARMACEUTICALS, INC.
Reel/Frame 070793/0228 →
RELEASE OF SECURITY INTEREST Recorded Apr 9, 2025
From: BIOPHARMA CREDIT PLC
To: REATA PHARMACEUTICALS HOLDINGS, LLC; REATA PHARMACEUTICALS GLOBAL, INC.; REATA PHARMACEUTICALS, INC.
Reel/Frame 070793/0130 →
AMENDED AND RESTATED PATENT SECURITY AGREEMENT Recorded Jul 12, 2023
From: REATA PHARMACEUTICALS HOLDINGS, LLC; REATA PHARMACEUTICALS GLOBAL, INC.; REATA PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 064264/0557 →
PATENT SECURITY AGREEMENT Recorded May 18, 2023
From: REATA PHARMACEUTICALS HOLDINGS, LLC; REATA PHARMACEUTICALS GLOBAL, INC.; REATA PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 063697/0461 →
RELEASE OF SECURITY INTEREST Recorded Jun 24, 2020
From: OXFORD FINANCE LLC, AS COLLATERAL AGENT
To: REATA PHARMACEUTICALS, INC.
Reel/Frame 053034/0018 →
SECURITY INTEREST Recorded Jun 14, 2018
From: REATA PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 046357/0605 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2018
From: CAPRATHE, BRADLEY WILLIAM; BOLTON, GARY L.; LEE, CHITASE; ROARK, WILLIAM H.
To: AAPHARMASYN LLC
Reel/Frame 045715/0300 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2018
From: VISNICK, MELEAN; HOTEMA, MARTHA R.; JIANG, XIN
To: REATA PHARMACEUTICALS, INC.
Reel/Frame 045715/0461 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2018
From: AAPHARMASYN LLC
To: REATA PHARMACEUTICALS, INC.
Reel/Frame 045715/0363 →
Continuity (2)
Provisional Application 62222632 · Sep 23, 2015
Related Publication 20190153022A1 · May 23, 2019