IP Library Granted Patent US 10,799,500
Granted Patent B2
US 10,799,500 · App. 16/276,331 · Granted Oct 13, 2020

Organic compounds

Inventors: Wei Yao (New Milford, NJ); Peng Li (New Milford, NJ); Robert Davis (San Diego, CA); Sharon Mates (New York, NY); Kimberly Vanover (New York, NY); Gretchen Snyder (New York, NY)
Assignee: INTRA-CELLULAR THERAPIES, INC.
A61K31/4985A61K9/0019A61K9/16A61K31/445A61K45/00A61K45/06A61P25/00C07D241/40C07D471/16
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Quick Facts
Patent No.
US 10,799,500
App. No.
16/276,331
Granted
Oct 13, 2020
Kind
B2
Abstract

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT 2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D 1 and D 2 receptor signaling system, and/or the μ-opioid receptor.

Claims (22)

1. A compound according to Formula I:

wherein:

X is NH;

L is O;

Z is —O— or —C(O)—;

in free form, salt form, or pharmaceutically acceptable salt form.

2. The compound according to claim 1 , wherein Z is —C(═O)—.

3. The compound according to claim 1 , wherein Z is O—.

4. The compound according to claim 3 in free form.

5. The compound according to claim 4 in solid form.

6. The compound according to claim 3 in pharmaceutically acceptable salt form.

7. The compound according to claim 6 , wherein the compound is in acid addition salt form with an acid selected from glutamic acid, tartaric acid, malic acid or ascorbic acid.

8. A pharmaceutical composition comprising the compound according to claim 1 in admixture with a pharmaceutically acceptable diluent or carrier.

9. The composition according to claim 8 , wherein the pharmaceutically acceptable diluent or carrier comprises a polymeric matrix.

10. The composition according to claim 9 , wherein the polymeric matrix comprises a biodegradable poly(d,l-lactide-co-glycolide) microsphere.

11. A pharmaceutical composition comprising the compound according to claim 3 in admixture with a pharmaceutically acceptable diluent or carrier.

12. A pharmaceutical composition comprising the compound according to claim 4 in admixture with a pharmaceutically acceptable diluent or carrier.

13. The composition according to claim 12 , wherein the pharmaceutically acceptable diluent or carrier comprises a polymeric matrix.

14. The composition according to claim 13 , wherein the polymeric matrix comprises a biodegradable poly(d,l-lactide-co-glycolide) microsphere.

15. A pharmaceutical composition comprising the compound according to claim 7 in admixture with a pharmaceutically acceptable diluent or carrier.

16. The composition according to claim 15 , wherein the pharmaceutically acceptable diluent or carrier comprises a polymeric matrix.

17. The composition according to claim 16 , wherein the polymeric matrix comprises a biodegradable poly(d,l-lactide-co-glycolide) microsphere.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 24, 2020
From: YAO, WEI; LI, PENG; DAVIS, ROBERT; MATES, SHARON; VANOVER, KIMBERLY; SNYDER, GRETCHEN
To: INTRA-CELLULAR THERAPIES, INC.
Reel/Frame 053308/0504 →
Continuity (5)
Continuation 15660615 · Jul 26, 2017
Continuation In Part PCTUS2017015178 · Jan 26, 2017
Provisional Application 62440130 · Dec 29, 2016
Provisional Application 62287264 · Jan 26, 2016
Related Publication 20190175590A1 · Jun 13, 2019
Cited By (16)
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