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Synthesis and biological activity of 2-methylene analogs of calcitriol and related compounds
US9688596B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9688596-B2 |
| Application number | US-201615220035-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 26, 2016 |
| Priority date | Aug 5, 2015 |
| Publication date | Jun 27, 2017 |
| Grant date | Jun 27, 2017 |
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- Title
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Abstract
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Disclosed are 2-methylene analogs of vitamin D 3 and related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1α-hydroxy-2-methylene-vitamin D 3 , (20S)-1α-hydroxy-2-methylene-vitamin D 3 , and (5E)-1α,25-dihydroxy-2-methylene-vitamin D 3 , their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders.
First claim
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We claim: 1. A compound having a formula: wherein: X 1 , and X 2 , which may be the same or different, are each selected from hydrogen or a hydroxy-protecting group. 2. The compound of claim 1 , wherein X 1 and X 2 are t-butyldimethylsilyl. 3. The compound of claim 1 , wherein X 1 and X 2 are hydrogen. 4. The compound of claim 1 having a formula: and called 1α-hydroxy-2-methylene-vitamin D 3 . 5. The compound of claim 1 having a formula: and called (20S)-1α-hydroxy-2-methylene-vitamin D 3 . 6. A pharmaceutical composition containing an effective amount of the compound of claim 1 and a pharmaceutically acceptable excipient. 7. A method for increasing bone strength in a patient in need thereof, the method comprising administering to the patient an effective amount of the compound of claim 1 .
Assignees
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Classifications
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Anorexiants; Antiobesity agents · CPC title
Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems · CPC title
the ring system containing nine carbon atoms, e.g. perhydroindane · CPC title
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- What does patent US9688596B2 cover?
- Disclosed are 2-methylene analogs of vitamin D 3 and related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1α-hydroxy-2-methylene-vitamin D 3 , (20S)-1α-hydroxy-2-methylene-vitamin D 3 , and (5E)-1α,25-dihydroxy-2-methylene-vitamin D 3 , their biological activities, and various pharmaceutical uses for these compounds inclu…
- Who is the assignee on this patent?
- Wisconsin Alumni Res Found
- What technology area does this patent fall under?
- Primary CPC classification A61K31/593. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Jun 27 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 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).