Invention Grant
US08524883B2 Monohydrate of (1-{9-[4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide
有权
（1- {9- [4S，2R，3R，5R）-3,4-二羟基-5-（羟甲基）氧杂环戊烷-2-基] -6-氨基嘌呤-2-基}吡唑-4-基） -N-甲基甲酰胺
![Monohydrate of (1-{9-[4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide](/docs/US/2013-09-03/US08524883B2/abs.jpg.600x600.jpg)
- Patent Title: Monohydrate of (1-{9-[4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide
- Patent Title (中): （1- {9- [4S，2R，3R，5R）-3,4-二羟基-5-（羟甲基）氧杂环戊烷-2-基] -6-氨基嘌呤-2-基}吡唑-4-基） -N-甲基甲酰胺
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Application No.: US13333872Application Date: 2011-12-21
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Publication No.: US08524883B2Publication Date: 2013-09-03
- Inventor: Jeff Zablocki , Elfatih Elzein , Robert Seemayer , Travis Lemons
- Applicant: Jeff Zablocki , Elfatih Elzein , Robert Seemayer , Travis Lemons
- Applicant Address: US CA Foster City
- Assignee: Gilead Sciences, Inc.
- Current Assignee: Gilead Sciences, Inc.
- Current Assignee Address: US CA Foster City
- Agency: Foley & Lardner LLP
- Main IPC: C07H19/00
- IPC: C07H19/00 ; C07H19/167 ; C07H19/173
![Monohydrate of (1-{9-[4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide](/abs-image/US/2013/09/03/US08524883B2/abs.jpg.150x150.jpg)
Abstract:
Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, namely, (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide. Also, disclosed are polymorphs of this compound and methods for isolating a specific polymorph. Also, disclosed are pharmaceutical compositions and methods for preparing pharmaceutical compositions.
Public/Granted literature
- US20120165350A1 PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS Public/Granted day:2012-06-28
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