CN111094268A - 一种凝血因子XIa抑制剂及其中间体的制备方法 - Google Patents
一种凝血因子XIa抑制剂及其中间体的制备方法 Download PDFInfo
- Publication number
- CN111094268A CN111094268A CN201980004506.0A CN201980004506A CN111094268A CN 111094268 A CN111094268 A CN 111094268A CN 201980004506 A CN201980004506 A CN 201980004506A CN 111094268 A CN111094268 A CN 111094268A
- Authority
- CN
- China
- Prior art keywords
- group
- compound
- groups
- alkyl
- substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/63—Esters of sulfonic acids
- C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
- C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
- C07C309/66—Methanesulfonates
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/63—Esters of sulfonic acids
- C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
本公开涉及一种凝血因子XIa抑制剂及其中间体的制备方法。具体而言,本公开涉及一种氧代吡啶酰胺类衍生物的制备方法,该方法收率高、产物纯度好、反应条件温和。
Description
PCT国内申请,说明书已公开。
Claims (26)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018107966463 | 2018-07-19 | ||
| CN201810796646 | 2018-07-19 | ||
| PCT/CN2019/096504 WO2020015698A1 (zh) | 2018-07-19 | 2019-07-18 | 一种凝血因子XIa抑制剂及其中间体的制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111094268A true CN111094268A (zh) | 2020-05-01 |
| CN111094268B CN111094268B (zh) | 2022-07-26 |
Family
ID=69163576
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980004506.0A Active CN111094268B (zh) | 2018-07-19 | 2019-07-18 | 一种凝血因子XIa抑制剂及其中间体的制备方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20210292279A1 (zh) |
| EP (1) | EP3825311A4 (zh) |
| JP (1) | JP2021530497A (zh) |
| KR (1) | KR20210033953A (zh) |
| CN (1) | CN111094268B (zh) |
| AU (1) | AU2019304392A1 (zh) |
| BR (1) | BR112021000439A2 (zh) |
| CA (1) | CA3106120A1 (zh) |
| MX (1) | MX2021000256A (zh) |
| TW (1) | TW202019904A (zh) |
| WO (1) | WO2020015698A1 (zh) |
| ZA (1) | ZA202007755B (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112010774A (zh) * | 2019-05-28 | 2020-12-01 | 上海美悦生物科技发展有限公司 | FXIa凝血因子抑制剂、其药物组合物和用途 |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3822264A4 (en) * | 2018-07-02 | 2021-11-10 | Jiangsu Hengrui Medicine Co., Ltd. | CRYSTALLINE FORMS OF AN OXYPYRIDINE AMIDE DERIVATIVE AND THEIR PREPARATION PROCESS |
| CN116262734B (zh) * | 2022-11-18 | 2025-05-13 | 成都施贝康生物医药科技有限公司 | 氧代吡啶类化合物及其制备方法和用途 |
| CN116262740A (zh) * | 2022-11-18 | 2023-06-16 | 成都施贝康生物医药科技有限公司 | 新型氧代吡啶类化合物及其制备方法和用途 |
| CN116621742B (zh) * | 2023-06-09 | 2025-05-06 | 成都施贝康生物医药科技有限公司 | 氧代吡啶类化合物的新型制备方法及关键中间体 |
| CN116751136B (zh) * | 2023-06-21 | 2025-08-29 | 成都施贝康生物医药科技有限公司 | 氧代吡啶类化合物的新型制备方法及关键中间体 |
| CN116621728B (zh) * | 2023-06-09 | 2025-07-29 | 成都施贝康生物医药科技有限公司 | 氧代吡啶类化合物的新型制备方法及关键中间体 |
| CN116874387B (zh) * | 2023-06-21 | 2025-08-26 | 成都施贝康生物医药科技有限公司 | 氧代吡啶类化合物的新型制备方法及关键中间体 |
| CN116730861A (zh) * | 2023-06-21 | 2023-09-12 | 成都施贝康生物医药科技有限公司 | 氧代吡啶类化合物的新型制备方法及关键中间体 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017037051A1 (de) * | 2015-09-04 | 2017-03-09 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| CN107428689A (zh) * | 2015-03-19 | 2017-12-01 | 拜耳制药股份公司 | 作为治疗血栓形成的因子xia抑制剂的氧代吡啶衍生物 |
| WO2018041122A1 (zh) * | 2016-08-31 | 2018-03-08 | 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 |
| 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 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7378409B2 (en) * | 2003-08-21 | 2008-05-27 | Bristol-Myers Squibb Company | Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity |
| CN1944398A (zh) * | 2005-01-11 | 2007-04-11 | 中国医学科学院药物研究所 | 新的苯甲酰胺类化合物及其制法和药物用途 |
| FR3005160B1 (fr) * | 2013-04-29 | 2016-02-12 | Sagem Defense Securite | Capteur angulaire inertiel de type mems equilibre et procede d'equilibrage d'un tel capteur |
| EP3104702B1 (en) * | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| EP3197889B1 (de) * | 2014-09-24 | 2018-08-01 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| AU2016301282B2 (en) * | 2015-08-03 | 2022-03-17 | Children's Medical Center Corporation | Charged ion channel blockers and methods for use |
| WO2017023992A1 (en) * | 2015-08-05 | 2017-02-09 | Bristol-Myers Squibb Company | Novel substituted glycine derived fxia inhibitors |
| CN107033043B (zh) * | 2016-02-04 | 2019-04-30 | 中国人民解放军第二军医大学 | N-取代苯磺酰基-取代苯甲酰胺类化合物及其制备药物的用途 |
| IT201600074606A1 (it) * | 2016-07-18 | 2018-01-18 | Italfarmaco Spa | New benzo-N-hydroxy amide compounds having antitumor activity |
| TWI592671B (zh) * | 2016-08-04 | 2017-07-21 | 台達電子工業股份有限公司 | 絕緣偵測電路、電源轉換裝置及絕緣阻抗值偵測方法 |
| EP3532469A1 (en) * | 2016-10-26 | 2019-09-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
-
2019
- 2019-07-18 JP JP2021500812A patent/JP2021530497A/ja not_active Withdrawn
- 2019-07-18 EP EP19837834.1A patent/EP3825311A4/en not_active Withdrawn
- 2019-07-18 AU AU2019304392A patent/AU2019304392A1/en not_active Abandoned
- 2019-07-18 WO PCT/CN2019/096504 patent/WO2020015698A1/zh not_active Ceased
- 2019-07-18 KR KR1020207037803A patent/KR20210033953A/ko not_active Withdrawn
- 2019-07-18 CN CN201980004506.0A patent/CN111094268B/zh active Active
- 2019-07-18 CA CA3106120A patent/CA3106120A1/en active Pending
- 2019-07-18 TW TW108125445A patent/TW202019904A/zh unknown
- 2019-07-18 US US17/259,917 patent/US20210292279A1/en not_active Abandoned
- 2019-07-18 BR BR112021000439-4A patent/BR112021000439A2/pt not_active IP Right Cessation
- 2019-07-18 MX MX2021000256A patent/MX2021000256A/es unknown
-
2020
- 2020-12-11 ZA ZA2020/07755A patent/ZA202007755B/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107428689A (zh) * | 2015-03-19 | 2017-12-01 | 拜耳制药股份公司 | 作为治疗血栓形成的因子xia抑制剂的氧代吡啶衍生物 |
| WO2017037051A1 (de) * | 2015-09-04 | 2017-03-09 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| WO2018041122A1 (zh) * | 2016-08-31 | 2018-03-08 | 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 |
| 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 |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112010774A (zh) * | 2019-05-28 | 2020-12-01 | 上海美悦生物科技发展有限公司 | FXIa凝血因子抑制剂、其药物组合物和用途 |
| CN112010774B (zh) * | 2019-05-28 | 2024-03-08 | 上海美悦生物科技发展有限公司 | FXIa凝血因子抑制剂、其药物组合物和用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112021000439A2 (pt) | 2021-04-06 |
| AU2019304392A1 (en) | 2021-01-28 |
| CA3106120A1 (en) | 2020-01-23 |
| WO2020015698A1 (zh) | 2020-01-23 |
| KR20210033953A (ko) | 2021-03-29 |
| CN111094268B (zh) | 2022-07-26 |
| US20210292279A1 (en) | 2021-09-23 |
| EP3825311A4 (en) | 2022-08-31 |
| EP3825311A1 (en) | 2021-05-26 |
| MX2021000256A (es) | 2021-03-25 |
| TW202019904A (zh) | 2020-06-01 |
| ZA202007755B (en) | 2022-06-29 |
| JP2021530497A (ja) | 2021-11-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN111094268B (zh) | 一种凝血因子XIa抑制剂及其中间体的制备方法 | |
| CN108047261B (zh) | 一种克立硼罗的制备方法 | |
| CA2862289A1 (en) | Modulators of methyl modifying enzymes, compositions and uses thereof | |
| TWI592418B (zh) | β-C-芳基葡萄糖苷之製造方法 | |
| WO2009011627A1 (en) | Pyridine compounds and their use as p2y12 antagonists | |
| KR102221087B1 (ko) | 항종양 약물 니라파립을 합성하기 위한 중간체의 제조방법 및 중간체 | |
| CN103360458A (zh) | 一种阿比特龙的合成方法 | |
| RU2779013C2 (ru) | Способ получения ингибитора фактора свертывания крови xia и его интермедиата | |
| CN102432642B (zh) | 1, 2, 3-o-三乙酰基-5-脱氧-d-呋喃核糖的合成方法 | |
| CN111393392A (zh) | 瑞德西韦关键中间体2,3,5-三苄氧基-d-核糖酸-1,4-内酯的合成 | |
| CN102796146A (zh) | 一种烟用保润剂及其制备方法 | |
| TW202330514A (zh) | 三並環衍生物及其製備方法和應用 | |
| JP2012507506A (ja) | (3s,4s)−4−((r)−2−(ベンジルオキシ)トリデシル)−3−ヘキシル−2−オキセタノンの製造方法及びそれに用いられる新規な中間体 | |
| TWI361191B (en) | Method of preparing (6r)-3-hexyl-4-hydroxy-6-undecyl-5,6-dihydropyran-2-one, and intermediate used in the method | |
| JP2022547113A (ja) | ピリミジニルビピリジン化合物の製造方法及びそのための中間体 | |
| CN112745350A (zh) | 一种4-膦酸烷基酯取代吲哚化合物的合成方法 | |
| CN116396272B (zh) | 一种2,5-二氢吡咯烷类衍生物及消旋尼古丁的制备方法 | |
| TW202021971A (zh) | 雙環雜芳香環衍生物 | |
| CN116462645B (zh) | 一种2-呋喃-2-基亚甲基-4-羟基丁酸酯及其制备方法和应用 | |
| CN104418707A (zh) | 一种天然产物补骨脂酚及其对映体的不对称合成方法 | |
| JPWO2011074675A1 (ja) | スピロケタール誘導体の製造方法 | |
| CN114057683A (zh) | 一种噻托溴铵中间体的制备方法 | |
| JP5776127B2 (ja) | 置換ピリジン−2−オンを製造する方法 | |
| CN112209872A (zh) | 一种2-溴-4-碘-3-甲基吡啶的合成工艺 | |
| CN117355513A (zh) | 一种btk抑制剂中间体的制备方法 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |