N6-substituted adenosine derivatives and N6-substituted adenine derivatives and uses thereof

Patent metadata

Field	Value
Publication number	US-10174033-B2
Application number	US-200913515152-A
Country	US
Kind code	B2
Filing date	Dec 10, 2009
Priority date	Dec 10, 2009
Publication date	Jan 8, 2019
Grant date	Jan 8, 2019

Abstract

The present invention provides N 6 -substituted adenosine derivatives and N 6 -substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.

First claim

The invention claimed is:

1. A compound that is an N 6 -substituted adenosine derivative or an N 6 -substituted adenine derivative, wherein said compound is selected from the group consisting of:
(72) N 6 -[(±)-1-(phenyl)-propyl]-adenosine
(75) N 6 -[(R)-1-(phenyl)-propyl]-adenosine
(76) N 6 -[(R)-1-(phenylpropyl)]-adenosine-2′,3′,5′-triacetate
(77) N 6 -[(R)-1-(phenylpropyl)]-adenosine-5′-acetate
(78) N 6 -[(S)-1-(phenylpropyl)]-adenosine
(79) N 6 -[(S)-1-(phenylpropyl)]-adenosine-2′,3′,5′-triacetate
(80) N 6 -[(S)-1-(phenylpropyl)]-adenosine-5′-acetate
(81) N 6 -[(S)-1-(phenyl)-propyl]-adenosine-5′-p-methyl-phenylpropionate
(82) N 6 -[(S)-1-(phenyl)-propyl]-adenosine-5′-methyl-cinnamate
(85) N 6 -[(R)-1-(phenyl)-propyl]-adenosine-5′-o-nitrophenyl ether
(86) N 6 -[(R)-1-(phenyl)-propyl]-adenosine-5′-propyl ether
(87) N 6 -[(±)-1-(phenyl)-butyl]-adenosine
(89) N 6 -[(R)-1-(phenyl)-butyl]-adenosine
(90) N 6 -[(S)-1-(phenyl)-butyl]-adenosine
and
(147) N 6 -[(S)-1-(phenyl)-propyl]-N 9 -(tetrahydrofuran-2-yl)-adenine.

2. A pharmaceutical composition comprising an effective dose of a compound according to claim 1 and pharmaceutically acceptable carrier(s).

3. A method of treating a subject having depression, insomnia, convulsion, epilepsy, Parkinson's disease, or dementia, the method comprising administering to the subject an effective dose of a compound according to claim 1 .

4. A compound selected from the group consisting of:
(72) N 6 -[(±)-1-(phenyl)-propyl]-adenosine,
(75) N 6 -[(R)-1-(phenylpropyl)]-adenosine, and
(78) N 6 -[(S)-1-(phenylpropyl)]-adenosine.

5. A pharmaceutical composition comprising an effective dose of a compound according to claim 4 and pharmaceutically acceptable carrier(s).

6. A method of treating a subject having depression, insomnia, convulsion, epilepsy, Parkinson's disease, or dementia, the method comprising administering to the subject an effective dose of a compound according to claim 4 .

Assignees

• Shi Jiangong
• Zhang Jianjun
• Yue Zhenggang
• Li Min
• Zhu Chenggen
• Zhang Ying
• Zi Jiachen
• Wang Yafang
• Fan Xiaona
• Xu Ruiming
• Lin Sheng
• Li Yan
• Yang Yongchun
• Sheng Li
• Inst Materia Medica Cams

Inventors

• Shi Jiangong
• Zhang Jianjun
• Yue Zhenggang
• Li Min
• Zhu Chenggen
• Zhang Ying
• Zi Jiachen
• Wang Yafang
• Fan Xiaona
• Xu Ruiming
• Lin Sheng
• Li Yan
• Yang Yongchun
• Sheng Li

Classifications

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61P25/20

  Hypnotics; Sedatives · CPC title

• A61P25/16

  Anti-Parkinson drugs · CPC title

• A61P25/08

  Antiepileptics; Anticonvulsants · CPC title

• C07D473/34 Primary

  attached in position 6, e.g. adenine · CPC title