RU2016150410A - Ингибиторы фактора xia - Google Patents
Ингибиторы фактора xia Download PDFInfo
- Publication number
- RU2016150410A RU2016150410A RU2016150410A RU2016150410A RU2016150410A RU 2016150410 A RU2016150410 A RU 2016150410A RU 2016150410 A RU2016150410 A RU 2016150410A RU 2016150410 A RU2016150410 A RU 2016150410A RU 2016150410 A RU2016150410 A RU 2016150410A
- Authority
- RU
- Russia
- Prior art keywords
- halo
- optionally substituted
- heteroaryl
- group
- independently selected
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000001424 substituent group Chemical group 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 241000124008 Mammalia Species 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 208000007536 Thrombosis Diseases 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014498 Embolic stroke Diseases 0.000 claims 1
- 206010014522 Embolism venous Diseases 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 208000004043 venous thromboembolism Diseases 0.000 claims 1
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)
- Pyridine Compounds (AREA)
- Plural Heterocyclic 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 (2)
| Publication Number | Publication Date |
|---|---|
| RU2016150410A true RU2016150410A (ru) | 2018-06-28 |
| RU2016150410A3 RU2016150410A3 (https=) | 2018-11-30 |
Family
ID=54699606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016150410A RU2016150410A (ru) | 2014-05-28 | 2015-05-22 | Ингибиторы фактора xia |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9783530B2 (https=) |
| EP (1) | EP3148542B1 (https=) |
| JP (1) | JP2017517512A (https=) |
| KR (1) | KR20170005871A (https=) |
| CN (1) | CN106413710A (https=) |
| AU (1) | AU2015267305A1 (https=) |
| CA (1) | CA2947987A1 (https=) |
| MX (1) | MX2016015484A (https=) |
| RU (1) | RU2016150410A (https=) |
| WO (1) | WO2015183709A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014160668A1 (en) | 2013-03-25 | 2014-10-02 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
| SG10201908467RA (en) | 2014-01-31 | 2019-10-30 | Bristol Myers Squibb Co | Macrocycles with hetrocyclic p2' groups as factor xia inhibitors |
| NO2760821T3 (https=) | 2014-01-31 | 2018-03-10 | ||
| US9975874B2 (en) | 2014-07-28 | 2018-05-22 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| ES2714283T3 (es) | 2014-09-04 | 2019-05-28 | Bristol Myers Squibb Co | Macrociclos de diamida que son inhibidores de FXIa |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| KR20170103962A (ko) * | 2015-01-20 | 2017-09-13 | 머크 샤프 앤드 돔 코포레이션 | 인자 xia 억제제 |
| US10472344B2 (en) | 2015-12-02 | 2019-11-12 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| WO2018039094A1 (en) | 2016-08-22 | 2018-03-01 | Merck Sharp & Dohme Corp. | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| 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 |
| MX2022003649A (es) * | 2019-09-27 | 2022-06-08 | Shenzhen Salubris Pharm Co Ltd | Inhibidores del fxia y metodo de preparacion de los mismos y uso farmaceutico de los mismos. |
| 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 |
| 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 |
| US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as 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 |
| EP1966141A1 (en) * | 2005-12-14 | 2008-09-10 | Brystol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| WO2007109459A2 (en) * | 2006-03-21 | 2007-09-27 | Janssen Pharmaceutica, Nv | Pyridines and pyridine n-oxides as modulators of thrombin |
| CN101784516B (zh) * | 2007-06-13 | 2014-07-02 | 百时美施贵宝公司 | 作为凝血因子抑制剂的二肽类似物 |
| US9161924B2 (en) * | 2011-07-08 | 2015-10-20 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
| US10011585B2 (en) | 2014-07-28 | 2018-07-03 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| US9975874B2 (en) | 2014-07-28 | 2018-05-22 | 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 CA CA2947987A patent/CA2947987A1/en not_active Abandoned
- 2015-05-22 EP EP15800524.9A patent/EP3148542B1/en active Active
- 2015-05-22 MX MX2016015484A patent/MX2016015484A/es unknown
- 2015-05-22 AU AU2015267305A patent/AU2015267305A1/en not_active Abandoned
- 2015-05-22 RU RU2016150410A patent/RU2016150410A/ru not_active Application Discontinuation
- 2015-05-22 KR KR1020167036089A patent/KR20170005871A/ko not_active Withdrawn
- 2015-05-22 JP JP2016569375A patent/JP2017517512A/ja active Pending
- 2015-05-22 WO PCT/US2015/032091 patent/WO2015183709A1/en not_active Ceased
- 2015-05-22 CN CN201580028124.3A patent/CN106413710A/zh active Pending
- 2015-05-22 US US15/312,839 patent/US9783530B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US9783530B2 (en) | 2017-10-10 |
| EP3148542A4 (en) | 2018-01-03 |
| EP3148542A1 (en) | 2017-04-05 |
| US20170197953A1 (en) | 2017-07-13 |
| CN106413710A (zh) | 2017-02-15 |
| CA2947987A1 (en) | 2015-12-03 |
| JP2017517512A (ja) | 2017-06-29 |
| KR20170005871A (ko) | 2017-01-16 |
| MX2016015484A (es) | 2017-03-23 |
| AU2015267305A1 (en) | 2016-11-03 |
| EP3148542B1 (en) | 2019-02-27 |
| WO2015183709A1 (en) | 2015-12-03 |
| RU2016150410A3 (https=) | 2018-11-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20190416 |