Process for the preparation of (2Z,5Z)-5-(3-chloro-4-((R)-2,3-dihydroxypropdxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one and intermediate used in said process
US-9340518-B2 · May 17, 2016 · US
Dosing regimen for a selective S1P1 receptor agonist
US10857134B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10857134-B2 |
| Application number | US-201916261327-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 29, 2019 |
| Priority date | Dec 11, 2014 |
| Publication date | Dec 8, 2020 |
| Grant date | Dec 8, 2020 |
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Abstract
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The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
First claim
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The invention claimed is: 1. A method of administering (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one (Compound 1), or a pharmaceutically acceptable salt thereof, to a subject in need thereof, for use in the treatment of a disease or disorder associated with an activated immune system, comprising the following steps: during initiation of treatment, or upon re-initiation of treatment after drug discontinuation, administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by (a) administering the maintenance dose of 10 mg of Compound 1 orally once daily from day 12 onwards; or (b) administering 10 mg of Compound 1 orally once daily for 2, 3 or 4 days, followed by the maintenance dose of 20 mg of Compound 1 to be administered orally once daily, wherein the disease is graft-versus-host disease. 2. A method as in claim 1 , comprising administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by administering 10 mg of Compound 1 orally once daily for 2, 3 or 4 days; followed by administering the maintenance dose of 20 mg of Compound 1 to orally once daily. 3. A method as in claim 1 , comprising administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by administering 10 mg of Compound 1 orally once daily on days 12, 13, and 14; followed by administering the maintenance dose of 20 mg of Compound 1 orally once daily from day 15 onwards. 4. A method as in claim 1 , comprising administering Compound 1, or a pharmaceutically acceptable salt thereof, orally once daily as follows: 2 mg of Compound 1 on days 1 and 2; 3 mg of Compound 1 on days 3 and 4; 4 mg of Compound 1 on days 5 and 6; 5 mg of Compound 1 on day 7; 6 mg of Compound 1 on day 8; 7 mg of Compound 1 on day 9; 8 mg of Compound 1 on day 10; and 9 mg of Compound 1 on day 11; followed by administering the maintenance dose of 10 mg of Compound 1 orally once daily from day 12 onwards. 5. A method as in claim 1 , wherein the disease or disorder to be treated is chronic graft-versus-host disease. 6. A method as in claim 2 , wherein the disease or disorder to be treated is chronic graft-versus-host disease. 7. A method as in claim 3 , wherein the disease or disorder to be treated is chronic graft-versus-host disease. 8. A method as in claim 4 , wherein the disease or disorder to be treated is chronic graft-versus-host disease.
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- What does patent US10857134B2 cover?
- The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
- Who is the assignee on this patent?
- Actelion Pharmaceuticals Ltd
- What technology area does this patent fall under?
- Primary CPC classification A61K31/426. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Dec 08 2020 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 4 related publications on this page (citations in our corpus or others sharing the same primary CPC).