CN115515938A - FXIa抑制剂化合物的盐及其制备方法和医药用途 - Google Patents
FXIa抑制剂化合物的盐及其制备方法和医药用途 Download PDFInfo
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- CN115515938A CN115515938A CN202180030803.XA CN202180030803A CN115515938A CN 115515938 A CN115515938 A CN 115515938A CN 202180030803 A CN202180030803 A CN 202180030803A CN 115515938 A CN115515938 A CN 115515938A
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- Prior art keywords
- salt
- inhibitor compound
- fxia inhibitor
- fxia
- amorphous
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
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- BBFCIBZLAVOLCF-UHFFFAOYSA-N pyridin-1-ium;bromide Chemical compound Br.C1=CC=NC=C1 BBFCIBZLAVOLCF-UHFFFAOYSA-N 0.000 description 1
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- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
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- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 239000003868 thrombin inhibitor Substances 0.000 description 1
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- SEDZOYHHAIAQIW-UHFFFAOYSA-N trimethylsilyl azide Chemical compound C[Si](C)(C)N=[N+]=[N-] SEDZOYHHAIAQIW-UHFFFAOYSA-N 0.000 description 1
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/14—Oxygen atoms
- C07D237/16—Two oxygen atoms
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Abstract
提供了一系列的FXIa抑制剂化合物的盐，包含这些化合物的盐的药物组合物，以及使用该化合物治疗血栓栓塞等疾病的药物中的用途。
Description
PCT国内申请，说明书已公开。
Claims (17)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2020111527428 | 2020-10-23 | ||
| CN202011152742 | 2020-10-23 | ||
| CN202110258902 | 2021-03-09 | ||
| CN2021102589025 | 2021-03-09 | ||
| PCT/CN2021/125449 WO2022083706A1 (zh) | 2020-10-23 | 2021-10-22 | FXIa抑制剂化合物的盐及其制备方法和医药用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN115515938A true CN115515938A (zh) | 2022-12-23 |
| CN115515938B CN115515938B (zh) | 2024-05-10 |
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| CN202180030803.XA Active CN115515938B (zh) | 2020-10-23 | 2021-10-22 | FXIa抑制剂化合物的盐及其制备方法和医药用途 |
Country Status (3)
| Country | Link |
|---|---|
| CN (1) | CN115515938B (zh) |
| TW (1) | TW202222315A (zh) |
| WO (1) | WO2022083706A1 (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115461330A (zh) * | 2021-03-18 | 2022-12-09 | 深圳信立泰药业股份有限公司 | FXIa抑制剂化合物杂质及其制备方法和用途 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201122139D0 (en) * | 2011-12-21 | 2012-02-01 | Ono Pharmaceutical Co | Compounds |
| CN107793396A (zh) * | 2016-08-31 | 2018-03-13 | 江苏恒瑞医药股份有限公司 | 环氧基取代的氧代吡啶类衍生物、其制备方法及其在医药上的应用 |
| CN108137549A (zh) * | 2015-08-05 | 2018-06-08 | 百时美施贵宝公司 | 新颖的取代的甘氨酸衍生的fxia抑制剂 |
| CN108495850A (zh) * | 2016-08-31 | 2018-09-04 | 江苏恒瑞医药股份有限公司 | 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用 |
| CN115427043A (zh) * | 2020-10-23 | 2022-12-02 | 深圳信立泰药业股份有限公司 | FXIa抑制剂化合物或其盐的医药用途 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20230027295A1 (en) * | 2019-09-27 | 2023-01-26 | Shenzhen Salubris Pharmaceuticals Co., Ltd. | Fxia inhibitors and preparation method therefor and pharmaceutical use thereof |
| CN112675173B (zh) * | 2020-12-25 | 2022-04-05 | 华南理工大学 | FXIa抑制剂化合物或其盐的医药用途 |
-
2021
- 2021-10-22 CN CN202180030803.XA patent/CN115515938B/zh active Active
- 2021-10-22 TW TW110139275A patent/TW202222315A/zh unknown
- 2021-10-22 WO PCT/CN2021/125449 patent/WO2022083706A1/zh active Application Filing
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201122139D0 (en) * | 2011-12-21 | 2012-02-01 | Ono Pharmaceutical Co | Compounds |
| CN108137549A (zh) * | 2015-08-05 | 2018-06-08 | 百时美施贵宝公司 | 新颖的取代的甘氨酸衍生的fxia抑制剂 |
| CN107793396A (zh) * | 2016-08-31 | 2018-03-13 | 江苏恒瑞医药股份有限公司 | 环氧基取代的氧代吡啶类衍生物、其制备方法及其在医药上的应用 |
| CN108495850A (zh) * | 2016-08-31 | 2018-09-04 | 江苏恒瑞医药股份有限公司 | 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用 |
| CN115427043A (zh) * | 2020-10-23 | 2022-12-02 | 深圳信立泰药业股份有限公司 | FXIa抑制剂化合物或其盐的医药用途 |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115461330A (zh) * | 2021-03-18 | 2022-12-09 | 深圳信立泰药业股份有限公司 | FXIa抑制剂化合物杂质及其制备方法和用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN115515938B (zh) | 2024-05-10 |
| TW202222315A (zh) | 2022-06-16 |
| WO2022083706A1 (zh) | 2022-04-28 |
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