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PEPTIDE DEFORMYLASE INHIBITORS COMPRISING PYRIMIDINYL AND HYDRAZINO MOIETIES AND CRYSTALLINE FORMS THEREOF
专利权人:
GLAXOSMITHKLINE LLC
发明人:
QIN, DONGHUI,NORTON, BETH,LIAO, XIANGMIN,KNOX, ANDREW, NICHOLSON,FANG, YUHONG,LEE, JINHWA,DREABIT, JASON, CHRISTOPHER,CHRISTENSEN, SIEGFRIED, BENJAMIN, IV,BENOWITZ, ANDREW, B,AUBART, KELLY, M
申请号:
NZ58522108
公开号:
NZ585221A
申请日:
2008.11.06
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are compounds of Formula (I), crystalline forms thereof, and methods for their preparation. Specific compounds of formula (I) include: [(2R)-3-{ 2-[6-(1-Azetidinyl)-5-fluoro-2-methyl-4-pyrimidinyl]hydrazino} -2-(cyclopentylmethyl)-3-oxopropyl]hydroxyformamide, 6-[(4S)-4-hydroxy-3,3-dimethyl-1-pyrrolidinyl]-2-methyl-4-pyrimidinyl} hydrazino)-3-oxopropyl]hydroxyformamide, and [(2R)-2-(Cyclopentylmethyl)-3-(2-{ 5-fluoro-6-[(9aS)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-2-methyl-4-pyrimidinyl} hydrazino)-3-oxopropyl]hydroxyformamide. Compounds of formula (I) are useful for treating bacterial infections, particularly where the bacterial infection is caused by Streptococcus, Staphylococcus, Moraxella, Haemophilus, Neisseria, Mycoplasma, Legionella, Chlamydia, Bacteroides, Clostridium, Fusobacterium, Propionibacterium, or Peptostreptococcus. Also disclosed are three different crystalline forms of [(2R)-2-(cyciopentylmethyl)-3-(2-{ 5-fluoro-6-[(9aS)-hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)yl]-2-methyl-4-pyrimidinyl} hydrazino)-3-oxopropyl]hydroxyformamide. The crystalline polymorphs are characterised with infra-red spectroscopy, X-ray diffraction, thermogravimetric analysis and differential scanning calorimetry
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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