CN112153978A - Ws-635其在医学中用途 - Google Patents
Ws-635其在医学中用途 Download PDFInfo
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- CN112153978A CN112153978A CN201980033730.2A CN201980033730A CN112153978A CN 112153978 A CN112153978 A CN 112153978A CN 201980033730 A CN201980033730 A CN 201980033730A CN 112153978 A CN112153978 A CN 112153978A
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- A61P25/28—Drugs for disorders of the nervous system 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
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- A—HUMAN NECESSITIES
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- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
- A61K38/13—Cyclosporins
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract
Description
Claims (52)
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CN (1) | CN112153978B (zh) |
CA (1) | CA3128410A1 (zh) |
WO (1) | WO2021068188A1 (zh) |
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Publication number | Priority date | Publication date | Assignee | Title |
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WO2021243658A1 (en) * | 2020-06-04 | 2021-12-09 | Waterstone Pharmaceuticals (Wuhan) Co., Ltd. | Treatment or prevention of coronaviridae infection |
WO2022213354A1 (en) * | 2021-04-09 | 2022-10-13 | Waterstone Pharmaceuticals (Wuhan) Co., Ltd. | Ws635 uses thereof in medicine |
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WO2023102847A1 (en) * | 2021-12-09 | 2023-06-15 | Waterstone Pharmaceuticals (Wuhan) Co., Ltd. | Ws635 uses thereof in medicine |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20120316247A1 (en) * | 2009-10-20 | 2012-12-13 | The General Hospital Corporation | Prevention and treatment of post-operative cognitive dysfunction (pocd) |
US20160039879A1 (en) * | 2013-03-15 | 2016-02-11 | S&T Global Inc. | Novel cyclosporin derivatives and uses thereof |
CN106902347A (zh) * | 2015-12-23 | 2017-06-30 | 中美华世通生物医药科技(武汉)有限公司 | 亲环孢素抑制剂的用途 |
CN106902346A (zh) * | 2015-12-23 | 2017-06-30 | 中美华世通生物医药科技(武汉)有限公司 | 药物组合物及其制药用途 |
Family Cites Families (7)
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---|---|---|---|---|
US4328245A (en) | 1981-02-13 | 1982-05-04 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
US4410545A (en) | 1981-02-13 | 1983-10-18 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
US4409239A (en) | 1982-01-21 | 1983-10-11 | Syntex (U.S.A.) Inc. | Propylene glycol diester solutions of PGE-type compounds |
RU2011127079A (ru) | 2009-01-07 | 2013-02-20 | Сайнексис, Инк. | Комбинация производного циклоспорина и нуклеозидов для лечения инфекции вирусом гепатита с |
AU2010203656A1 (en) | 2009-01-07 | 2011-07-21 | Scynexis, Inc. | Cyclosporine derivative for use in the treatment of HCV and HIV infection |
DK2646043T3 (da) * | 2010-12-03 | 2017-05-22 | S&T Global Inc | Hidtil ukendte cyclosporinderivater til behandling og forebyggelse af en virusinfektion |
EP3831841A1 (en) | 2016-05-17 | 2021-06-09 | S&T Global Inc. | Novel cyclosporin derivatives and uses thereof |
-
2019
- 2019-10-11 CA CA3128410A patent/CA3128410A1/en active Pending
- 2019-10-11 WO PCT/CN2019/110576 patent/WO2021068188A1/en unknown
- 2019-10-11 EP EP19948286.0A patent/EP4041274B1/en active Active
- 2019-10-11 JP JP2021551528A patent/JP7232932B2/ja active Active
- 2019-10-11 US US17/429,667 patent/US20220105149A1/en active Pending
- 2019-10-11 CN CN201980033730.2A patent/CN112153978B/zh active Active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20120316247A1 (en) * | 2009-10-20 | 2012-12-13 | The General Hospital Corporation | Prevention and treatment of post-operative cognitive dysfunction (pocd) |
US20160039879A1 (en) * | 2013-03-15 | 2016-02-11 | S&T Global Inc. | Novel cyclosporin derivatives and uses thereof |
CN106902347A (zh) * | 2015-12-23 | 2017-06-30 | 中美华世通生物医药科技(武汉)有限公司 | 亲环孢素抑制剂的用途 |
CN106902346A (zh) * | 2015-12-23 | 2017-06-30 | 中美华世通生物医药科技(武汉)有限公司 | 药物组合物及其制药用途 |
Non-Patent Citations (1)
Title |
---|
MIAN PENG等: "Battery of behavioral tests in mice to study postoperative delirium", SCIENTIFIC REPORTS, pages 1 - 3 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2021243658A1 (en) * | 2020-06-04 | 2021-12-09 | Waterstone Pharmaceuticals (Wuhan) Co., Ltd. | Treatment or prevention of coronaviridae infection |
WO2022213354A1 (en) * | 2021-04-09 | 2022-10-13 | Waterstone Pharmaceuticals (Wuhan) Co., Ltd. | Ws635 uses thereof in medicine |
Also Published As
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JP2022532821A (ja) | 2022-07-20 |
EP4041274B1 (en) | 2024-05-08 |
CA3128410A1 (en) | 2021-04-15 |
CN112153978B (zh) | 2024-04-19 |
JP7232932B2 (ja) | 2023-03-03 |
EP4041274A4 (en) | 2023-05-17 |
US20220105149A1 (en) | 2022-04-07 |
WO2021068188A1 (en) | 2021-04-15 |
EP4041274A1 (en) | 2022-08-17 |
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