Crystalline diacylhydrazine and the use thereof
US-8946294-B2 · Feb 3, 2015 · US
Crystalline diacylhydrazine and the use thereof
US9604913B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9604913-B2 |
| Application number | US-201414519408-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 21, 2014 |
| Priority date | Sep 8, 2011 |
| Publication date | Mar 28, 2017 |
| Grant date | Mar 28, 2017 |
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Abstract
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The present disclosure provides crystalline polymorphic and amorphous forms of (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 1) or (S)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 2). The present disclosure further provides compositions comprising crystalline polymorphic and amorphous forms of Compound 1 or Compound 2 and an excipient, methods of making crystalline polymorphic or amorphous forms of Compound 1 or Compound 2, and methods of using crystalline polymorphic or amorphous forms of Compound 1 or Compound 2 to regulate gene expression in a cell or in a subject.
First claim
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What is claimed is: 1. Crystalline (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide hydrate Form IV, characterized as having a powder x-ray diffraction pattern with peaks at 6.83, 10.31, 11.30, 12.18, 12.98, 13.69, 15.11, 16.23, 17.60, 17.99, 20.70, 21.15, 21.68, 22.71, 23.79, and 24.86 degrees 2Θ. 2. The (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide hydrate Form IV of claim 1 having an average particle size distribution of about 10 μm or less. 3. A composition comprising the (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide hydrate Form IV of claim 1 and one or more excipients. 4. The composition of claim 3 , wherein said one or more excipients comprise one or more pharmaceutically acceptable excipients. 5. The composition of claim 4 , wherein said one or more pharmaceutically acceptable excipients comprise Miglyol 812, phospholipon 90G, or tocopheryl polyethylene glycol 1000 succinate, or a mixture thereof. 6. A method of making a composition, the method comprising admixing the (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide hydrate Form IV of claim 1 and an excipient. 7. A kit comprising the (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide hydrate Form IV of claim 1 . 8. The crystalline (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide hydrate Form IV of claim 2 having an average particle size distribution of about 1 μm or less.
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- What does patent US9604913B2 cover?
- The present disclosure provides crystalline polymorphic and amorphous forms of (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 1) or (S)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N′-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 2). The present disclosure further provides compositions comprising crystalline polymorphic and amorphou…
- Who is the assignee on this patent?
- Intrexon Corp
- What technology area does this patent fall under?
- Primary CPC classification C07C243/38. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Mar 28 2017 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 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).