Pyridazinedione-based heterobicyclic covalent linkers and methods and applications thereof
US-2024425465-A1 · Dec 26, 2024 · US
DOT1L inhibitors
US9458165B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9458165-B2 |
| Application number | US-201514838142-A |
| Country | US |
| Kind code | B2 |
| Filing date | Aug 27, 2015 |
| Priority date | Aug 27, 2014 |
| Publication date | Oct 4, 2016 |
| Grant date | Oct 4, 2016 |
How to read this patent
A practical reading order for non-experts. Skip the full description unless you need deep technical detail.
- Title
What the patent document calls the invention.
- Abstract
A short plain-language summary of the technical disclosure.
- Assignees and inventors
Who owns or filed the patent and who is credited as inventor.
- Key dates
Filing, priority, publication, and grant dates set the timeline.
- First independent claim
The legal scope of protection — read this for what is actually claimed.
- CPC / IPC classifications
Technology tags used to group this patent with similar filings.
- Citations and related patents
Prior art links and similar publications in this corpus.
Abstract
Official abstract text for this publication.
Provided herein are inhibitors of DOT1L of formula (I) useful for treating diseases or disorders associated with DOT1L: in which R 1 is defined in the specification. An exemplary DOT1L inhibitor provided herein exhibits a biological half-life of 12.6 h. Methods for treating diseases associated with DOT1L are also provided.
First claim
Opening claim text (preview).
What is claimed is: 1. A compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from the group consisting of CN, halo, and C 1-4 haloalkyl. 2. The compound of claim 1 , wherein R 1 is halo. 3. The compound of claim 1 , wherein R 1 is chloro or bromo. 4. The compound of claim 1 , wherein R 1 is chloro. 5. The compound of claim 1 , wherein R 1 is bromo. 6. The compound of claim 1 , wherein R 1 is C 1-4 haloalkyl. 7. The compound of claim 1 , wherein R 1 is trifluoromethyl. 8. The compound of claim 1 , wherein R 1 is CN. 9. The compound of claim 1 , wherein the compound of Formula (I) is a compound of Formula (Ia): or a pharmaceutically acceptable salt thereof. 10. The compound of claim 1 , wherein the compound is selected from the group consisting of: or a pharmaceutically acceptable salt thereof. 11. The compound of claim 1 , wherein the compound is: or a pharmaceutically acceptable salt thereof. 12. The compound of claim 1 , wherein the compound has a biological half-life of from about 10 h to about 13 h. 13. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier. 14. A method of inhibiting an activity of DOT1L, comprising contacting DOT1L with a compound of claim 1 , or a pharmaceutically acceptable salt thereof. 15. A method of treating a disease in a patient, wherein said disease is selected from the group consisting of acute myeloid leukemia, acute lymphocytic leukemia, and mixed lineage leukemia, comprising administering to said patient a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.
Assignees
Inventors
Classifications
- C07D487/04Primary
Ortho-condensed systems · CPC title
Patent family
Related publications grouped by family.
External sources
Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US9458165B2 cover?
- Provided herein are inhibitors of DOT1L of formula (I) useful for treating diseases or disorders associated with DOT1L: in which R 1 is defined in the specification. An exemplary DOT1L inhibitor provided herein exhibits a biological half-life of 12.6 h. Methods for treating diseases associated with DOT1L are also provided.
- Who is the assignee on this patent?
- Dana Farber Cancer Inst Inc
- What technology area does this patent fall under?
- Primary CPC classification C07D487/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Oct 04 2016 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 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).