IP Library Granted Patent US 9,833,457
Granted Patent B2
US 9,833,457 · App. 15/600,942 · Granted Dec 5, 2017

Tricyclic compounds as modulators of TNF-α synthesis and as PDE4 inhibitors

Inventors: Adnan M. M. Mjalli (Oak Ridge, NC); Bapu Gaddam (Ellicott City, MD); Dharma Rao Polisetti (High Point, NC); Matthew J. Kostura (Hillsborough, NC); Mustafa Guzel (Jamestown, NC)
Assignee: vTv Therapeutics LLC
A61K31/519C07D471/04
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Quick Facts
Patent No.
US 9,833,457
App. No.
15/600,942
Granted
Dec 5, 2017
Kind
B2
Abstract

The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-α or by PDE4, including but not limited to psoriatic arthritis.

Claims (28)

1. A method of treating psoriatic arthritis comprising administering to a human a compound, wherein the compound is selected from the group consisting of

1-cyclopentyl-7-methoxy-3-(4-methyl-thiophen-2-yl)-1H-pyrimido[5,4-c]quinoline-2,4-dione,

1-cyclopentyl-7-methoxy-3-m-tolyl-1H-pyrimido[5,4-c]quinoline-2,4-dione,

3-(3-chloro-phenyl)-1-(1-methane-sulfonyl-piperidin-4-yl)-7-methoxy-1H-pyrimido[5,4-c]-quinoline-2,4-dione,

trans-4-[3-(3-chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido-[5,4-c]quinolin-1-yl]-cyclohexanecarboxylic acid methyl ester,

3-(3-chloro-phenyl)-1-((R)-1-methane-sulfonyl-pyrrolidin-3-yl)-7-methoxy-1H-pyrimido[5,4-c]quinoline-2,4-dione,

3-(3-chloro-phenyl)-1-((S)-1-methane-sulfonyl-pyrrolidin-3-yl)-7-methoxy-1H-pyrimido[5,4-c]quinoline-2,4-dione,

3-(3-chloro-phenyl)-1-(1-ethanesulfonyl-piperidin-4-yl)-7-methoxy-1H-pyrimido-[5,4-c]quinoline-2,4-dione, and

N-{4-[(S)-3-(3-chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido[5,4-c]quinolin-1-yl]-trans-cyclohexyl}-methanesulfonamide,

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is 1-cyclopentyl-7-methoxy-3-(4-methyl-thiophen-2-yl)-1H-pyrimido[5,4-c]quinoline-2,4-dione or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the compound is 1-cyclopentyl-7-methoxy-3-m-tolyl-1H-pyrimido[5,4-c]quinoline-2,4-dione or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein the compound is 3-(3-chloro-phenyl)-1-(1-methane-sulfonyl-piperidin-4-yl)-7-methoxy-1H-pyrimido[5,4-c]-quinoline-2,4-dione or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 , wherein the compound is trans-4-[3-(3-chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido-[5,4-c]quinolin-1-yl]-cyclohexanecarboxylic acid methyl ester or a pharmaceutically acceptable salt thereof.

6. The method of claim 1 , wherein the compound is 3-(3-chloro-phenyl)-1-((R)-1-methane-sulfonyl-pyrrolidin-3-yl)-7-methoxy-1H-pyrimido[5,4-c]quinoline-2,4-dione or a pharmaceutically acceptable salt thereof.

7. The method of claim 1 , wherein the compound is 3-(3-chloro-phenyl)-1-((S)-1-methane-sulfonyl-pyrrolidin-3-yl)-7-methoxy-1H-pyrimido[5,4-c]quinoline-2,4-dione or a pharmaceutically acceptable salt thereof.

8. The method of claim 1 , wherein the compound is 3-(3-chloro-phenyl)-1-(1-ethanesulfonyl-piperidin-4-yl)-7-methoxy-1H-pyrimido-[5,4-c]quinoline-2,4-dione or a pharmaceutically acceptable salt thereof.

9. The method of claim 1 , wherein the compound is N-{4-[(S)-3-(3-chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido[5,4-c]quinolin-1-yl]-trans-cyclohexyl}-methanesulfonamide or a pharmaceutically acceptable salt thereof.

10. The method of claim 1 , wherein the compound is administered topically.

11. The method of claim 1 , wherein the compound is administered orally.

12. A method of treating psoriatic arthritis comprising administering to a human a compound, wherein the compound is trans-4-[3-(3-chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido-[5,4-c]quinolin-1-yl]-cyclohexanecarboxylic acid or a pharmaceutically acceptable salt thereof.

13. The method of claim 12 , wherein the compound is trans-4-[3-(3-chloro-phenyl)-7-methoxy-2,4-dioxo-3,4-dihydro-2H-pyrimido-[5,4-c]quinolin-1-yl]-cyclohexanecarboxylic acid.

14. The method of claim 12 , wherein the compound is administered topically.

15. The method of claim 12 , wherein the compound is administered orally.

16. A method of treating psoriatic arthritis comprising administering to a human a compound, wherein the compound is 3-benzo[1,3]dioxol-5-yl-1-(1-methanesulfonyl-piperidin-4-yl)-7-methoxy-1H-pyrimido[5,4-c]quinoline-2,4-dione or a pharmaceutically acceptable salt thereof.

17. The method of claim 16 , wherein the compound is 3-benzo[1,3]dioxol-5-yl-1-(1-methanesulfonyl-piperidin-4-yl)-7-methoxy-1H-pyrimido[5,4-c]quinoline-2,4-dione.

18. The method of claim 16 , wherein the compound is administered topically.

19. The method of claim 16 , wherein the compound is administered orally.

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Jan 27, 2021
From: HORIZON TECHNOLOGY FINANCE CORPORATION, AS COLLATERAL AGENT
To: VTV THERAPEUTICS LLC
Reel/Frame 055133/0214 →
SECURITY INTEREST Recorded Apr 18, 2018
From: VTV THERAPEUTICS LLC
To: HORIZON TECHNOLOGY FINANCE CORPORATION, AS COLLATERAL AGENT
Reel/Frame 045969/0774 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 22, 2017
From: MJALLI, ADNAN M.M.; GADDAM, BAPU; POLISETTI, DHARMA RAO; KOSTURA, MATTHEW J.; GUZEL, MUSTAFA
To: TRANSTECH PHARMA, INC.
Reel/Frame 042456/0007 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 22, 2017
From: TRANSTECH PHARMA, INC.
To: HIGH POINT PHARMACEUTICALS, LLC
Reel/Frame 042456/0027 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 22, 2017
From: VTVX HOLDINGS II LLC
To: VTV THERAPEUTICS LLC
Reel/Frame 042456/0097 →
CHANGE OF NAME Recorded May 22, 2017
From: HIGH POINT PHARMACEUTICALS, LLC
To: VTVX HOLDINGS II LLC
Reel/Frame 042523/0968 →
Continuity (7)
Continuation 15184392 · Jun 16, 2016
Continuation 14850012 · Sep 10, 2015
Continuation 14477302 · Sep 4, 2014
Division 13040382 · Mar 4, 2011
Continuation 12532861
Provisional Application 61023617 · Jan 25, 2008
Related Publication 20170252343A1 · Sep 7, 2017