CA2947987A1 - Factor xia inhibitors - Google Patents
Factor xia inhibitors Download PDFInfo
- Publication number
- CA2947987A1 CA2947987A1 CA2947987A CA2947987A CA2947987A1 CA 2947987 A1 CA2947987 A1 CA 2947987A1 CA 2947987 A CA2947987 A CA 2947987A CA 2947987 A CA2947987 A CA 2947987A CA 2947987 A1 CA2947987 A1 CA 2947987A1
- Authority
- CA
- Canada
- Prior art keywords
- mmol
- halo
- chloro
- heteroaryl
- optionally 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.)
- Abandoned
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
-
- 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
- C07D401/10—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 carbon chain containing 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462003693P | 2014-05-28 | 2014-05-28 | |
| US62/003,693 | 2014-05-28 | ||
| PCT/US2015/032091 WO2015183709A1 (en) | 2014-05-28 | 2015-05-22 | Factor xia inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2947987A1 true CA2947987A1 (en) | 2015-12-03 |
Family
ID=54699606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2947987A Abandoned CA2947987A1 (en) | 2014-05-28 | 2015-05-22 | Factor xia inhibitors |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9783530B2 (OSRAM) |
| EP (1) | EP3148542B1 (OSRAM) |
| JP (1) | JP2017517512A (OSRAM) |
| KR (1) | KR20170005871A (OSRAM) |
| CN (1) | CN106413710A (OSRAM) |
| AU (1) | AU2015267305A1 (OSRAM) |
| CA (1) | CA2947987A1 (OSRAM) |
| MX (1) | MX2016015484A (OSRAM) |
| RU (1) | RU2016150410A (OSRAM) |
| WO (1) | WO2015183709A1 (OSRAM) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9738655B2 (en) | 2013-03-25 | 2017-08-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors |
| BR112016015717B1 (pt) | 2014-01-31 | 2023-04-04 | Bristol-Myers Squibb Company | Compostos macrociclos com grupos p2' heterocíclicos como inibidores do fator xia, composição farmacêutica compreendendo os referidos compostos e uso dos mesmos |
| NO2760821T3 (OSRAM) | 2014-01-31 | 2018-03-10 | ||
| WO2016018702A1 (en) * | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| JP6526796B2 (ja) | 2014-09-04 | 2019-06-05 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｆｘｉａ阻害剤であるジアミドマクロ環 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| MX2017009445A (es) * | 2015-01-20 | 2017-11-08 | Merck Sharp & Dohme | Inhibidores del factor xia. |
| WO2017095760A1 (en) | 2015-12-02 | 2017-06-08 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
| CN111763171B (zh) * | 2019-04-02 | 2023-12-22 | 上海美悦生物科技发展有限公司 | 一种FXIa凝血因子抑制剂及其药物组合物、制备方法和医药用途 |
| AU2020355830B2 (en) * | 2019-09-27 | 2023-04-13 | Shenzhen Salubris Pharmaceuticals Co. Ltd | FXIa inhibitors and preparation method therefor and pharmaceutical use thereof |
| JP7700218B2 (ja) * | 2020-09-17 | 2025-06-30 | 浙江海正薬業股▲ふん▼有限公司 | ピペラジン誘導体、その製造方法、およびその使用 |
| US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as factor XIa inhibitors |
| US11845748B2 (en) | 2021-03-18 | 2023-12-19 | Janssen Pharmaceutica Nv | Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors |
| US11919881B2 (en) | 2021-03-18 | 2024-03-05 | Janssen Pharmaceutica Nv | Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7429604B2 (en) * | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| BRPI0610506A2 (pt) * | 2005-04-20 | 2010-06-29 | Johnson & Johnson | moduladores de trombina de n-óxidos de piridina fluorados e processo para n-oxidação de heteroarilas contendo nitrogênio |
| WO2007070818A1 (en) * | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US7829584B2 (en) | 2006-03-21 | 2010-11-09 | Janssen Pharmaceutica Nv | Pyridines and pyridine N-oxides as modulators of thrombin |
| MX2009012847A (es) * | 2007-06-13 | 2009-12-08 | Bristol Myers Squibb Co | Analogos dipeptidicos como inhibidores de factores de coagulacion. |
| EP2729150B1 (en) * | 2011-07-08 | 2016-09-14 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
| WO2016018701A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| WO2016018702A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| WO2016015593A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
-
2015
- 2015-05-22 KR KR1020167036089A patent/KR20170005871A/ko not_active Withdrawn
- 2015-05-22 US US15/312,839 patent/US9783530B2/en active Active
- 2015-05-22 EP EP15800524.9A patent/EP3148542B1/en active Active
- 2015-05-22 AU AU2015267305A patent/AU2015267305A1/en not_active Abandoned
- 2015-05-22 WO PCT/US2015/032091 patent/WO2015183709A1/en not_active Ceased
- 2015-05-22 JP JP2016569375A patent/JP2017517512A/ja active Pending
- 2015-05-22 CN CN201580028124.3A patent/CN106413710A/zh active Pending
- 2015-05-22 MX MX2016015484A patent/MX2016015484A/es unknown
- 2015-05-22 CA CA2947987A patent/CA2947987A1/en not_active Abandoned
- 2015-05-22 RU RU2016150410A patent/RU2016150410A/ru not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN106413710A (zh) | 2017-02-15 |
| US20170197953A1 (en) | 2017-07-13 |
| WO2015183709A1 (en) | 2015-12-03 |
| MX2016015484A (es) | 2017-03-23 |
| EP3148542A1 (en) | 2017-04-05 |
| AU2015267305A1 (en) | 2016-11-03 |
| KR20170005871A (ko) | 2017-01-16 |
| EP3148542A4 (en) | 2018-01-03 |
| RU2016150410A (ru) | 2018-06-28 |
| RU2016150410A3 (OSRAM) | 2018-11-30 |
| US9783530B2 (en) | 2017-10-10 |
| EP3148542B1 (en) | 2019-02-27 |
| JP2017517512A (ja) | 2017-06-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20211123 |
|
| FZDE | Discontinued |
Effective date: 20211123 |