IP Library Granted Patent US 10,183,951
Granted Patent B2
US 10,183,951 · App. 15/446,873 · Granted Jan 22, 2019

Solid forms of a thienopyrimidinedione ACC inhibitor and methods for production thereof

Inventors: John C. Amedio, Jr. (Cambridge, MA); Sijun Hu (Cambridge, MA); Henry Morrison (Foster City, CA)
Assignee: Gilead Apollo, LLC
C07D495/04C07D309/12C12P41/001C12Y301/01003C07B2200/13
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Quick Facts
Patent No.
US 10,183,951
App. No.
15/446,873
Granted
Jan 22, 2019
Kind
B2
Abstract

The present invention provides solid forms of compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, methods of producing the same, and methods of using the same in the treatment of ACC-mediated diseases.

Claims (11)

1. A crystalline form of Compound 1:

(Compound 1 Form I) characterized by an X-ray powder diffractogram comprising the following peaks: 9.3, 15.0, and 19.8°2θ±0.2°2θ, as determined on a diffractometer using Cu—Kα radiation at a wavelength of 1.54 Å.

2. The crystalline form of claim 1 , wherein the diffractogram comprises one or more additional peaks at 16.0, 24.0, 25.8, and 27.3°2θ±0.2°2θ.

3. The crystalline form of claim 2 , wherein the diffractogram comprises peaks at 16.0 and 25.8°2θ±0.2°2θ.

4. The crystalline form of claim 1 , characterized by a differential scanning calorimetry (DSC) curve that comprises an endotherm between 189° C. to 193° C.

5. A pharmaceutical composition comprising the crystalline form of claim 3 and a pharmaceutically acceptable carrier, adjuvant or diluent.

6. A pharmaceutical composition comprising a therapeutically effective amount of the crystalline form of Compound 1 according to claim 1 , and a pharmaceutically acceptable carrier, adjuvant or diluent.

7. A method of inhibiting ACC in a patient in need thereof comprising administering to the patient the crystalline form of claim 1 .

8. The method according to claim 7 , wherein the patient is suffering from non-alcoholic fatty liver disease.

9. The method according to claim 8 , wherein the non-alcoholic fatty liver disease is non-alcoholic steatohepatitis.

10. The method of claim 7 , wherein the patient is suffering from acne vulgaris.

Assignments (20)
CORRECTIVE ASSIGNMENT TO CORRECT THE PROPERTY NUMBER PREVIOUSLY RECORDED AT REEL: 47626 FRAME: 965. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded May 16, 2019
From: LAWSON, JON P.
To: J.P. LAWSON CONSULTING LLC
Reel/Frame 049200/0799 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 8, 2019
From: NIMBUS DISCOVERY, INC.
To: NIMBUS APOLLO, INC.
Reel/Frame 048821/0394 →
CHANGE OF NAME Recorded Apr 8, 2019
From: NIMBUS APOLLO, INC.
To: GILEAD APOLLO, INC.
Reel/Frame 048825/0801 →
CHANGE OF NAME Recorded Apr 8, 2019
From: GILEAD APOLLO, INC.
To: GILEAD APOLLO, LLC
Reel/Frame 048825/0814 →
CORRECTIVE ASSIGNMENT TO CORRECT THE ADD ,LTD TO FIRST RECEIVING PARTY NAME PREVIOUSLY RECORDED AT REEL: 47626 FRAME: 828. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Feb 21, 2019
From: HU, SIJUN
To: PHARMARON BEIJING CO., LTD; PHARMARON, INC.
Reel/Frame 049257/0945 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 6, 2019
From: LAWSON, JON P.
To: J.P. LAWSON CONSULTING LLC
Reel/Frame 048251/0927 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 4, 2018
From: GILEAD SCIENCES, INC.
To: GILEAD APOLLO, LLC
Reel/Frame 047672/0935 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: PHARMARON BEIJING CO., LTD.; PHARMARON, INC.
To: PHARMARON, INC.
Reel/Frame 047628/0765 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: PHARMARON, INC.
To: NIMBUS APOLLO, INC.
Reel/Frame 047628/0816 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: ALEXANDER, KATY
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 047682/0970 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: AMEDIO CMC CONSULTING, LLC
To: NIMBUS DISCOVERY, INC.
Reel/Frame 047687/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: J.P. LAWSON CONSULTING LLC
To: PHARMACEUTICAL ADVISORS LLC
Reel/Frame 047694/0746 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: AMEDIO, JOHN C., JR.
To: AMEDIO CMC CONSULTING, LLC
Reel/Frame 047626/0588 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: HU, SIJUN
To: PHARMARON BEIJING LIMITED CO.; PHARMARON, INC.
Reel/Frame 047626/0828 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: YANG, XIAOWEI
To: PHARMARON BEIJING CO., LTD.; PHARMARON, INC.
Reel/Frame 047627/0313 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: HARRIMAN, GERALDINE C.
To: NIMBUS DISCOVERY, INC.
Reel/Frame 047628/0081 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: VARIA, KUNAL A.
To: SOLID FORM SOLUTIONS LIMITED
Reel/Frame 047628/0241 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: SOLID FORM SOLUTIONS LIMITED
To: NIMBUS APOLLO, INC.
Reel/Frame 047628/0557 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: PHARMACEUTICAL ADVISORS LLC
To: NIMBUS APOLLO, INC.
Reel/Frame 047628/0717 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2017
From: CALIMSIZ, SELCUK; GEIER, MICHAEL; MORRISON, HENRY; SABOURIN, KYLE; SCOTT, MARK E.; VARGHESE, VIMAL; WANG, XIAOTIAN
To: GILEAD SCIENCES, INC.
Reel/Frame 043538/0017 →
Continuity (3)
Provisional Application 62302755 · Mar 2, 2016
Provisional Application 62303237 · Mar 3, 2016
Related Publication 20170267690A1 · Sep 21, 2017