IP Library Granted Patent US 12,180,219
Granted Patent B2
US 12,180,219 · App. 18/649,712 · Granted Dec 31, 2024

Process for preparing beta 3 agonists and intermediates

Inventors: Feng Xu (Staten Island, NY); Zhuqing Liu (Edison, NJ); Richard Desmond (Readington, NJ); Jeonghan Park (Whippany, NJ); Alexei Kalinin (Morganville, NJ); Birgit Kosjek (Westfield, NJ); Hallena Strotman (Somerset, NJ); Hongmei Li (Westfield, NJ); Johannah Moncecchi (Waltham, MA)
Assignee: MERCK SHARP & DOHME LLC
C07D487/04C07C215/30C07D207/08C07D207/12C12P17/10
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Quick Facts
Patent No.
US 12,180,219
App. No.
18/649,712
Granted
Dec 31, 2024
Kind
B2
Abstract

The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.

Claims (31)

1. A crystalline form of Compound I-7:

characterized by a powder X-ray diffraction (XRPD) pattern comprising °2θ peaks at about 5.5, 8.7, and 11.0.

2. The crystalline form of Compound I-7 of claim 1 , wherein the crystalline form is characterized by the XRPD pattern further comprising a °2θ peak at about 17.5.

3. The crystalline form of Compound I-7 of claim 1 , wherein the crystalline form is characterized by the XRPD pattern further comprising a °2θ peak at about 22.7.

4. The crystalline form of Compound I-7 of claim 1 , wherein the crystalline form is characterized by the XRPD pattern further comprising °2θ peaks at about 17.5 and 22.7.

5. The crystalline form of Compound I-7 of claim 1 , characterized by an XRPD pattern as shown in FIG. 2 .

6. The crystalline form of Compound I-7 of claim 1 which is anhydrous.

7. The crystalline form of Compound I-7 of claim 1 , wherein the crystalline form is characterized by an XRPD pattern comprising the following reflections with d-spacing:

Position [°2 Theta]

d-spacing [Å]

5.4897

16.09873

8.7494

10.10683

11.0426

8.01261

16.4521

5.38818

16.6518

5.32402

17.4975

5.06857

18.853

4.7071

21.2176

4.18756

21.7532

4.08564

22.7425

3.9101

8. A composition comprising the crystalline form of Compound I-7 of claim 1 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 7, 2024
From: XU, FENG; LIU, ZHUQING; DESMOND, RICHARD; PARK, JEONGHAN; KALININ, ALEXEI; KOSJEK, BIRGIT; STROTMAN, HALLENA; LI, HONGMEI; MONCECCHI, JOHANNAH
To: MERCK SHARP & DOHME CORP.
Reel/Frame 069188/0696 →
MERGER Recorded Nov 7, 2024
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 069189/0030 →
Continuity (8)
Continuation 18508594 · Nov 14, 2023
Continuation 18317417 · May 15, 2023
Continuation 17399274 · Aug 11, 2021
Continuation 16914138 · Jun 26, 2020
Continuation 16298467 · Mar 11, 2019
Division 14776366
Provisional Application 61791247 · Mar 15, 2013
Related Publication 20240300960A1 · Sep 12, 2024
Cited By (1)
US 12,357,636