Centrally active and orally bioavailable antidotes for organophosphate exposure and methods for making and using them
US-2015361060-A1 · Dec 17, 2015 · US
US9290491B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9290491-B2 |
| Application number | US-201414333003-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 16, 2014 |
| Priority date | Feb 28, 2007 |
| Publication date | Mar 22, 2016 |
| Grant date | Mar 22, 2016 |
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The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
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What is claimed is: 1. A crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide wherein a single crystal of the sulfate salt, analyzed at a temperature of −153±1° C., is characterized by an orthorhombic unit cell with dimensions a=6.824 Å, b=16.228 Å, c=24.202 Å, α=β=γ=90°; cell volume (V) of 2680.0 Å 3 , and a space group of P2 1 2 1 2 1 (#19). 2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and the crystalline sulfate salt of claim 1 .
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Centrally acting analgesics, e.g. opioids · CPC title
Drugs for disorders of the alimentary tract or the digestive system · CPC title
for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants · CPC title
Morphinan derivatives, e.g. morphine, codeine · CPC title
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