IP Library Granted Patent US 8,293,878
Granted Patent B2
US 8,293,878 · App. 13/207,576 · Granted Oct 23, 2012

Methods and compounds useful for the preparation of sodium glucose co-transporter 2 inhibitors

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Quick Facts
Patent No.
US 8,293,878
App. No.
13/207,576
Granted
Oct 23, 2012
Kind
B2
Abstract

Methods of synthesizing sodium glucose co-transporter 2 inhibitors, as well as compounds useful therein, are disclosed. Particular inhibitors are compounds of formula I.

Claims (14)

1. A compound of the formula:

2. The compound of claim 1 , which has an X-ray powder diffraction pattern with peaks at one or more of about 7.7, 11.9, 12.4, 16.9, 19.5, 19.9, 21.9, 23.2, 24.1, and/or 27.7 degrees 2θ.

3. The compound of claim 1 , which has a melting point of about 156° C.

4. A compound of the formula:

5. A compound of the formula:

6. A compound the formula:

7. A compound of the formula:

8. The compound of claim 7 , which is crystalline.

9. The compound of claim 8 , which has an X-ray powder diffraction pattern with peaks at one or more of about 7.6, 13.2, 17.0, 17.4, 18.6, 19.5, 20.5, 20.8 and/or 23.2 degrees 2θ.

10. The compound of claim 8 , which has a melting point of about 113° C.

11. A compound of the formula:

12. The compound of claim 11 , which is crystalline.

13. The compound of claim 12 , which has an X-ray powder diffraction pattern with peaks at one or more of about 9.0, 16.9, 17.6, 18.2, 18.4, 18.8 and/or 22.7 degrees 2θ.

14. The compound of claim 12 , which has a melting point of about 136° C.

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded May 5, 2026
From: OXFORD FINANCE LLC
To: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS
Reel/Frame 075545/0601 →
SECURITY INTEREST Recorded May 4, 2026
From: LEXICON PHARMACEUTICALS, INC.; LEXICON PHARMACEUTICALS (NEW JERSEY), INC.; LION ACQUISITION CORPORATION
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 075498/0899 →
SECURITY INTEREST Recorded Mar 17, 2022
From: LEXICON PHARMACEUTICALS, INC.
To: OXFORD FINANCE LLC, AS COLLATERAL AGENT
Reel/Frame 059432/0709 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 26, 2018
From: GOODWIN, NICOLE CATHLEEN; HARRISON, BRYCE ALDEN; IIMURA, SHINYA; MABON, ROSS; SONG, QIULING; WU, WENXUE; YAN, JIE; ZHANG, HAIMING; ZHAO, MATTHEW MANGZHU
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 045351/0473 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →