Combination therapy
US-9186392-B2 · Nov 17, 2015 · US
Process for the preparation of chiral 8-(3-aminopiperidin-1-yl)-xanthines
US9499546B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9499546-B2 |
| Application number | US-201414507190-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 6, 2014 |
| Priority date | Nov 5, 2004 |
| Publication date | Nov 22, 2016 |
| Grant date | Nov 22, 2016 |
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- Title
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Abstract
Official abstract text for this publication.
The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
First claim
Opening claim text (preview).
What is claimed is: 1. A process for preparing a medicament comprising a first compound of formula or a physiologically acceptable salt thereof, the process comprising deprotecting a second compound of formula by detaching the phthalyl protecting group to provide the first compound, wherein R 1 is a (4-methylquinazolin-2-yl)methyl, (3-methylisoquinolin-1-yl)methyl or (3-cyanopyridin-2-yl)methyl group, R 2 is a methyl group, and R 3 is a 2-butyn-1-yl group; and combining the first compound with one or more inert carriers and/or diluents. 2. The process according to claim 1 wherein R 1 is a (4-methylquinazolin-2-yl)methyl. 3. The process according to claim 2 , wherein the phthalyl protecting group of the second compound is detached in the presence of ethanolamine. 4. The process according to claim 2 , wherein the phthalyl protecting group of the second compound is detached in the presence of (a) ethanolamine and toluene or (b) ethanolamine and a mixture of tetrahydrofuran and water. 5. The process according to claim 2 , further comprising crystallizing the first compound from ethanol or methanol. 6. The process according to claim 2 , further comprising crystallizing the first compound from ethanol. 7. The process according to claim 2 , wherein the step of detaching the phthalyl protecting group of the second compound is carried out the presence of (a) ethanolamine and toluene or (b) ethanolamine and a mixture of tetrahydrofuran and water, to provide the first compound, and the process further comprises crystallizing the first compound from ethanol or methanol. 8. The process according to claim 7 , wherein the first compound is crystallized from ethanol.
Assignees
Inventors
Classifications
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Immunosuppressants, e.g. drugs for graft rejection · CPC title
for glucose homeostasis (pancreatic hormones A61P5/48) · CPC title
Anorexiants; Antiobesity agents · CPC title
for hyperglycaemia, e.g. antidiabetics · CPC title
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Frequently asked questions
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- What does patent US9499546B2 cover?
- The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
- Who is the assignee on this patent?
- Pfrengle Waldemar, Pachur Thorsten, Nicola Thomas, and 2 more
- What technology area does this patent fall under?
- Primary CPC classification C07D473/06. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Nov 22 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 6 related publications on this page (citations in our corpus or others sharing the same primary CPC).