IP Library Granted Patent US 11,026,927
Granted Patent B2
US 11,026,927 · App. 16/277,829 · Granted Jun 8, 2021

Pharmaceutical combination comprising a selective S1P1 receptor agonist

Inventors: Martine Clozel (Allschwil, CH); Luca Piali (Basel, CH)
Assignee: ACTELION PHARMACEUTICALS LTD
A61K31/426A61K31/22A61K31/225A61K31/27A61K31/4015
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Quick Facts
Patent No.
US 11,026,927
App. No.
16/277,829
Granted
Jun 8, 2021
Kind
B2
Abstract

The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.

Claims (13)

1. A pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof, wherein the first agent and the second agent are in synergistically effective amounts for the treatment of multiple sclerosis.

2. A pharmaceutical combination according to claim 1 , wherein the first active ingredient is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one and the second active ingredient is methyl fumarate or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical combination according to claim 1 , wherein the first active ingredient is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one and the second active ingredient is dimethyl fumarate.

4. A pharmaceutical combination according to claim 1 , wherein the first active ingredient is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one and the second active ingredient is (N,N-diethylcarbamoyl)methyl methyl(2E)but-2-ene-1,4-dioate.

5. A pharmaceutical combination according to claim 1 , wherein the first active ingredient is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one and the second active ingredient is 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate.

6. A pharmaceutical combination according to claim 1 , wherein the first and the second active ingredient are comprised in a single pharmaceutical composition.

7. A pharmaceutical combination according to claim 1 , wherein the first and the second active ingredient are comprised in separated pharmaceutical compositions.

8. A pharmaceutical combination according to claim 1 for use in the treatment of relapsing multiple sclerosis.

9. A pharmaceutical combination according to claim 1 for use in the treatment of relapsing multiple sclerosis.

10. A pharmaceutical combination according to claim 1 for use in the prevention and/or treatment of relapsing-remitting multiple sclerosis.

11. A pharmaceutical composition containing, as active principle, (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one and at least one therapeutically inert excipient, wherein the pharmaceutical composition is to be administered in combination with a second pharmaceutical composition containing, as active principle, methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, or 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof and at least one therapeutically inert excipient, wherein the active principle from the pharmaceutical composition and the active principle from the second pharmaceutical composition are in synergistically effective amounts for the treatment of multiple sclerosis.

12. A pharmaceutical composition containing, as active principle, methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, or 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof, and at least one therapeutically inert excipient, wherein the pharmaceutical composition is to be administered in combination with a second pharmaceutical composition containing, as active principle, (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one and at least one therapeutically inert excipient, wherein the active principle from the pharmaceutical composition and the active principle from the second pharmaceutical composition are in synergistically effective amounts for the treatment of multiple sclerosis.

13. A pharmaceutical composition containing, as active principle, dimethyl fumarate and at least one therapeutically inert excipient, wherein the pharmaceutical composition is to be administered in combination with a second pharmaceutical composition containing, as active principle, (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one and at least one therapeutically inert excipient, wherein the active principle from the pharmaceutical composition and the active principle from the second pharmaceutical composition are in synergistically effective amounts for the treatment of multiple sclerosis.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 29, 2024
From: ACTELION PHARMACEUTICALS LTD
To: VANDA PHARMACEUTICALS INC.
Reel/Frame 066276/0577 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 27, 2019
From: CLOZEL, MARTINE; PIALI, LUCA
To: ACTELION PHARMACEUTICALS LTD
Reel/Frame 048715/0544 →
Priority Claims (1)
WO PCT/EP2014/077469 · Dec 11, 2014 · international
Continuity (2)
Division 15534951
Related Publication 20190175563A1 · Jun 13, 2019
Cited By (1)
US 12,409,167