IP Library Granted Patent US 8,772,483
Granted Patent B2
US 8,772,483 · App. 13/288,366 · Granted Jul 8, 2014

Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid

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Quick Facts
Patent No.
US 8,772,483
App. No.
13/288,366
Granted
Jul 8, 2014
Kind
B2
Abstract

Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. Pharmaceutical dosage forms and methods of their use are also disclosed.

Claims (12)

1. A crystalline compound, which is (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid besylate.

2. The crystalline compound of claim 1 , which is anhydrous.

3. The crystalline compound of claim 2 , which has a melting point of about 234° C. and/or a DSC peak at about 238° C.

4. The crystalline compound of claim 3 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 9.2, 15.9, 16.8, 18.4, 19.8, and/or 20.8 degrees 2θ.

5. The crystalline compound of claim 1 , which is a hydrate.

6. The crystalline compound of claim 5 , which has a melting point of about 218° C.

7. The compound of claim 5 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 8.7, 9.1, 13.4, 18.3, and/or 20.2 degrees 2θ.

8. The crystalline compound of claim 2 , which has a melting point of about 228° C. and/or a DSC peak at about 233° C.

9. The crystalline compound of claim 2 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 8.7, 9.5, 16.9, 17.5, 19.1, 19.7, 20.1, 20.4, 21.8, 22.1, and/or 26.4 degrees 2θ.

10. The crystalline compound of claim 2 , which has an X-ray powder diffraction pattern substantially the same as that shown in FIG. 1 .

11. The crystalline compound of claim 3 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 7.6, 8.6, 12.9, 15.0, 15.3, 17.3, 19.2, 19.5, 20.2, and/or 23.1 degrees 2θ.

12. A pharmaceutical dosage form comprising the crystalline compound of claim 1 .

Assignments (10)
RELEASE OF INTELLECTUAL PROPERTY SECURITY AGREEMENT RECORDED AT R/F 63227/0852 Recorded Jan 7, 2025
From: NEWSTONE CAPITAL PARTNERS, LLC
To: TERSERA THERAPEUTICS LLC
Reel/Frame 069835/0704 →
SECURITY INTEREST Recorded Apr 5, 2023
From: TERSERA THERAPEUTICS LLC
To: NEWSTONE CAPITAL PARTNERS, LLC
Reel/Frame 063227/0852 →
SECURITY INTEREST Recorded Apr 4, 2023
From: TERSERA THERAPEUTICS LLC
To: ANTARES CAPITAL LP, AS AGENT
Reel/Frame 063215/0724 →
RELEASE OF SECURITY INTEREST Recorded Apr 4, 2023
From: NEWSTONE CAPITAL PARTNERS, LLC
To: TERSERA THERAPEUTICS LLC; JDP THERAPEUTICS LLC
Reel/Frame 063221/0546 →
RELEASE OF SECURITY INTEREST Recorded Apr 4, 2023
From: MIDCAP FINANCIAL TRUST, AS AGENT
To: TERSERA THERAPEUTICS LLC
Reel/Frame 063253/0942 →
SECURITY INTEREST Recorded Sep 30, 2020
From: TERSERA THERAPEUTICS LLC
To: MIDCAP FINANCIAL TRUST, AS AGENT
Reel/Frame 053940/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 14, 2020
From: LEXICON PHARMACEUTICALS, INC.
To: TERSERA THERAPEUTICS LLC
Reel/Frame 053763/0754 →
RELEASE OF SECURITY INTEREST Recorded Sep 14, 2020
From: BIOPHARMA CREDIT PLC
To: LEXICON PHARMACEUTICALS, INC.
Reel/Frame 053767/0445 →
SECURITY INTEREST Recorded Sep 9, 2020
From: TERSERA THERAPEUTICS LLC
To: NEWSTONE CAPITAL PARTNERS, LLC
Reel/Frame 053721/0037 →
SECURITY INTEREST Recorded Dec 20, 2017
From: LEXICON PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 044958/0377 →