发明授权
- 专利标题: Glutaminyl cyclase inhibitors and the use thereof in treatment of various diseases
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申请号: US16472172申请日: 2018-05-24
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公开(公告)号: US11845740B2公开(公告)日: 2023-12-19
- 发明人: Vladimir Evgenievich Nebolsin , Anastasia Vladimirovna Rydlovskaya , Tatyana Alexandrovna Kromova
- 申请人: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
- 申请人地址: RU Moscow
- 专利权人: LTD “VALENTA-INTELLEKT”,Vladimir Evgenievich Nebolsin
- 当前专利权人: LTD “VALENTA-INTELLEKT”,Vladimir Evgenievich Nebolsin
- 当前专利权人地址: RU Moscow; RU Moscow
- 代理机构: BCF LLP
- 优先权: RU 17118350 2017.05.26 RU 17137615 2017.10.27
- 国际申请: PCT/RU2018/050058 2018.05.24
- 国际公布: WO2018/217139A 2018.11.29
- 进入国家日期: 2019-06-20
- 主分类号: C07D403/12
- IPC分类号: C07D403/12 ; A61P25/02 ; A61P37/00 ; A61P1/00 ; A61P29/00 ; A61K31/4178 ; A61P11/00 ; A61P13/12 ; A61P17/06 ; A61K47/00 ; A61K45/06 ; A61P3/04 ; A61P11/06 ; A61P17/00 ; C12N9/10
摘要:
The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A)
wherein
R1 is —C(O)—R2—(O)— or —R2—C(O)— group, where R2 is —(CH2)n-group optionally substituted with one or two C1-C6 alkyls, or phenyl,
n is an integer from 0 to 4;
wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system. This invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of the compounds of formula (A) as defined above.
wherein
R1 is —C(O)—R2—(O)— or —R2—C(O)— group, where R2 is —(CH2)n-group optionally substituted with one or two C1-C6 alkyls, or phenyl,
n is an integer from 0 to 4;
wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system. This invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of the compounds of formula (A) as defined above.
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