Method for Preparing Largazole Analogs and Uses Thereof
US-2018044376-A1 · Feb 15, 2018 · US
Synthesis and utility of new capgroup largazole analogs
US10538534B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10538534-B2 |
| Application number | US-201615555792-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 4, 2016 |
| Priority date | Mar 6, 2015 |
| Publication date | Jan 21, 2020 |
| Grant date | Jan 21, 2020 |
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Abstract
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Analogs of largazole are described herein. Methods of treating cancer, blood disorders, autoimmune disease, and Alzheimer's Disease using largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.
First claim
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The invention claimed is: 1. A compound of Formula (B) wherein X═NH, or NR, wherein R is H or lower alkyl; wherein R 2 ═H, acyl, or cleavable SR 5 , wherein R 5 =folate, methotrexate, cytokines, peptide, carbohydrate, or another molecule of the same (i.e., resulting in a homodimer); or a pharmaceutically acceptable salt, solvate, clathrate, or stereoisomer thereof. 2. A compound of Formula (C) wherein X═NH, or NR, wherein R is H or lower alkyl; wherein R 2 ═H, acyl, or cleavable SR 5 , wherein R 5 =folate, methotrexate, cytokines, peptide, carbohydrate, or another molecule of the same (i.e., resulting in a homodimer); or a pharmaceutically acceptable salt, solvate, clathrate, or stereoisomer thereof. 3. A compound having a structure selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, clathrate, or stereoisomer thereof. 4. A method for alleviating symptoms of leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, renal cancer, prostate cancer, or breast cancer in a subject, comprising administering to the subject a therapeutically effective amount of the compound of claim 1 . 5. The method of claim 4 , wherein the symptoms are of leukemia. 6. The method of claim 4 , further comprising treating said subject with an additional form of therapy for cancer. 7. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 and at least one pharmaceutically acceptable excipient. 8. A composition comprising a radiolabelled compound of claim 1 . 9. A method for alleviating symptoms of leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, renal cancer, prostate cancer, or breast cancer in a subject, comprising administering to the subject a therapeutically effective amount of the compound of claim 2 . 10. The method of claim 9 , wherein the symptoms are of leukemia. 11. The method of claim 9 , further comprising treating said subject with an additional form of therapy for cancer. 12. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 2 and at least one pharmaceutically acceptable excipient. 13. A composition comprising a radiolabelled compound of claim 2 . 14. A method for alleviating symptoms of leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, renal cancer, prostate cancer, or breast cancer in a subject, comprising administering to the subject a therapeutically effective amount of the compound of claim 3 . 15. The method of claim 14 , wherein the symptoms are of leukemia. 16. The method of claim 14 , further comprising treating said subject with an additional form of therapy for cancer. 17. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 3 and at least one pharmaceutically acceptable excipient. 18. A composition comprising a radiolabelled compound of claim 3 .
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- What does patent US10538534B2 cover?
- Analogs of largazole are described herein. Methods of treating cancer, blood disorders, autoimmune disease, and Alzheimer's Disease using largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.
- Who is the assignee on this patent?
- Univ Colorado State Res Found, Dana Farber Cancer Inst Inc, Univ Notre Dame Du Lac
- What technology area does this patent fall under?
- Primary CPC classification C07D513/18. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Jan 21 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 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).