ES2762987T3 - Macrociclos de diamida como inhibidores del factor XIA - Google Patents
Macrociclos de diamida como inhibidores del factor XIA Download PDFInfo
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- ES2762987T3 ES2762987T3 ES16732191T ES16732191T ES2762987T3 ES 2762987 T3 ES2762987 T3 ES 2762987T3 ES 16732191 T ES16732191 T ES 16732191T ES 16732191 T ES16732191 T ES 16732191T ES 2762987 T3 ES2762987 T3 ES 2762987T3
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- 239000003112 inhibitor Substances 0.000 title description 59
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- 150000001875 compounds Chemical class 0.000 claims abstract description 181
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- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract description 71
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- 150000003839 salts Chemical class 0.000 claims abstract description 62
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- 229910052760 oxygen Inorganic materials 0.000 claims abstract description 54
- 229910052801 chlorine Inorganic materials 0.000 claims abstract description 48
- 229910052794 bromium Inorganic materials 0.000 claims abstract description 41
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 40
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract description 39
- 125000003118 aryl group Chemical group 0.000 claims abstract description 38
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- UWGYJXUZMHAURP-VFNWGFHPSA-N (4R,8S)-8-[4-[3-chloro-6-(4-chlorotriazol-1-yl)-2-fluorophenyl]-6-oxopyrimidin-1-yl]-4-methyl-2,10-diazabicyclo[10.4.0]hexadeca-1(16),12,14-triene-3,9-dione Chemical compound C[C@@H]1CCC[C@@H](C(=O)NCc2ccccc2NC1=O)n1cnc(cc1=O)-c1c(F)c(Cl)ccc1-n1cc(Cl)nn1 UWGYJXUZMHAURP-VFNWGFHPSA-N 0.000 claims 1
- FHJDPIAKYYOLAF-MWTRTKDXSA-N (4R,8S)-8-[4-[5-chloro-2-(4-chlorotriazol-1-yl)phenyl]-6-oxopyrimidin-1-yl]-4-methyl-2,10-diazabicyclo[10.4.0]hexadeca-1(16),12,14-triene-3,9-dione Chemical compound C[C@@H]1CCC[C@@H](C(=O)NCc2ccccc2NC1=O)n1cnc(cc1=O)-c1cc(Cl)ccc1-n1cc(Cl)nn1 FHJDPIAKYYOLAF-MWTRTKDXSA-N 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract description 22
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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
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562181875P | 2015-06-19 | 2015-06-19 | |
| PCT/US2016/037823 WO2016205482A1 (en) | 2015-06-19 | 2016-06-16 | Diamide macrocycles as factor xia inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2762987T3 true ES2762987T3 (es) | 2020-05-26 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES16732191T Active ES2762987T3 (es) | 2015-06-19 | 2016-06-16 | Macrociclos de diamida como inhibidores del factor XIA |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10160750B2 (https=) |
| EP (1) | EP3310777B1 (https=) |
| JP (1) | JP6742348B2 (https=) |
| CN (1) | CN108026083B (https=) |
| ES (1) | ES2762987T3 (https=) |
| WO (1) | WO2016205482A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
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| NO2760821T3 (https=) | 2014-01-31 | 2018-03-10 | ||
| CN116987080A (zh) | 2014-01-31 | 2023-11-03 | 百时美施贵宝公司 | 作为因子xia抑制剂的具有杂环p2′基团的大环化合物 |
| WO2016205482A1 (en) | 2015-06-19 | 2016-12-22 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| US10287288B2 (en) | 2015-07-29 | 2019-05-14 | Bristol-Myers Squibb | Factor XIa macrocyclic inhibitors bearing alkyl or cycloalkyl P2' moieties |
| ES2871111T3 (es) | 2015-07-29 | 2021-10-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático |
| KR20180117156A (ko) | 2016-03-02 | 2018-10-26 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 |
| JP2022513919A (ja) * | 2018-12-17 | 2022-02-09 | バイエル・アクチエンゲゼルシヤフト | 血栓性または血小板塞栓性疾患および／または血栓性または血小板塞栓性合併症の治療および／または予防のための置換オキソピリジン誘導体 |
| WO2021110076A1 (zh) * | 2019-12-04 | 2021-06-10 | 深圳信立泰药业股份有限公司 | 草酰胺类衍生物、其制备方法及其在医药上的应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| ZA985247B (en) | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
| EP1192135A2 (en) | 1999-06-14 | 2002-04-03 | Eli Lilly And Company | Serine protease inhibitors |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
| CA2461202C (en) | 2001-09-21 | 2011-07-12 | Donald Pinto | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
| US20040180855A1 (en) | 2003-02-19 | 2004-09-16 | Schumacher William A. | Methods of treating thrombosis with reduced risk of increased bleeding times |
| US7138412B2 (en) | 2003-03-11 | 2006-11-21 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives useful as serine protease inhibitors |
| US7129264B2 (en) | 2003-04-16 | 2006-10-31 | Bristol-Myers Squibb Company | Biarylmethyl indolines and indoles as antithromboembolic agents |
| US7417063B2 (en) | 2004-04-13 | 2008-08-26 | Bristol-Myers Squibb Company | Bicyclic heterocycles useful as serine protease inhibitors |
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| WO2006076575A2 (en) | 2005-01-13 | 2006-07-20 | Bristol-Myers Squibb Company | Substituted biaryl compounds as factor xia inhibitors |
| WO2006089005A2 (en) | 2005-02-17 | 2006-08-24 | Bristol-Myers Squibb Company | Combination of selective factor viia and/or xia and plasma kallikrein inhibitors |
| EP1981854B1 (en) | 2005-12-14 | 2011-06-01 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| AU2006325746A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| WO2007070816A2 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Thiophene derivatives as factor xia inhibitors |
| AR058380A1 (es) * | 2005-12-23 | 2008-01-30 | Bristol Myers Squibb Co | Inhibidores del factor viia macrociclicos utiles como anticoagulantes |
| CN101605779B (zh) | 2006-12-15 | 2013-11-20 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的芳基丙酰胺、芳基丙烯酰胺、芳基丙炔酰胺或芳基甲基脲类似物 |
| CA2676933C (en) | 2007-02-28 | 2015-09-29 | Leo Pharma A/S | Novel phosphodiesterase inhibitors |
| AR067329A1 (es) | 2007-06-13 | 2009-10-07 | Bristol Myers Squibb Co | Analogos dipeptidos como inhibidores del factor de coagulacion |
| US8324199B2 (en) | 2008-03-13 | 2012-12-04 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| FR2944014A1 (fr) | 2009-04-06 | 2010-10-08 | Univ Grenoble 1 | Peptides cycliques a activite antiparasitaire |
| ES2674745T3 (es) | 2010-02-11 | 2018-07-03 | Bristol-Myers Squibb Company | Macrociclos como inhibidores del factor XIa |
| EP2603080A4 (en) | 2010-08-12 | 2014-01-22 | Enanta Pharm Inc | HEPATITIS C-VIRUS HEMMER |
| TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之新穎巨環化合物 |
| TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑 |
| EP2766345B1 (en) | 2011-10-14 | 2016-03-16 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| ES2579832T3 (es) | 2011-10-14 | 2016-08-17 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa |
| KR101937514B1 (ko) | 2011-10-14 | 2019-01-10 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 xia 억제제로서의 치환된 테트라히드로이소퀴놀린 화합물 |
| KR20150038369A (ko) | 2012-08-03 | 2015-04-08 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 디히드로피리돈 P1 |
| MX361759B (es) * | 2012-08-03 | 2018-12-17 | Bristol Myers Squibb Co | Compuestos macrocíclicos de dihidropiridona como inhibidores del factor xia y el uso de los mismos en el tratamiento de un trastorno tromboembólico. |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| TR201807316T4 (tr) | 2012-10-12 | 2018-06-21 | Bristol Myers Squibb Co | Bir faktör XIa inhibitörünün kristalli formları. |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| WO2014160592A2 (en) * | 2013-03-27 | 2014-10-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| NO2760821T3 (https=) | 2014-01-31 | 2018-03-10 | ||
| CN116987080A (zh) | 2014-01-31 | 2023-11-03 | 百时美施贵宝公司 | 作为因子xia抑制剂的具有杂环p2′基团的大环化合物 |
| CN107074821B (zh) | 2014-09-04 | 2020-05-22 | 百时美施贵宝公司 | 为fxia抑制剂的二酰胺大环化合物 |
| NO2721243T3 (https=) | 2014-10-01 | 2018-10-20 | ||
| WO2016205482A1 (en) | 2015-06-19 | 2016-12-22 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| ES2871111T3 (es) | 2015-07-29 | 2021-10-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático |
| US10287288B2 (en) | 2015-07-29 | 2019-05-14 | Bristol-Myers Squibb | Factor XIa macrocyclic inhibitors bearing alkyl or cycloalkyl P2' moieties |
| ES2754599T3 (es) | 2015-08-05 | 2020-04-20 | Bristol Myers Squibb Co | Nuevos inhibidores de FXIa derivados de glicina sustituidos |
| KR20180117156A (ko) | 2016-03-02 | 2018-10-26 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 |
-
2016
- 2016-06-16 WO PCT/US2016/037823 patent/WO2016205482A1/en not_active Ceased
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- 2016-06-16 US US15/735,322 patent/US10160750B2/en active Active
- 2016-06-16 EP EP16732191.8A patent/EP3310777B1/en active Active
- 2016-06-16 CN CN201680048685.4A patent/CN108026083B/zh active Active
- 2016-06-16 JP JP2017565810A patent/JP6742348B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2016205482A1 (en) | 2016-12-22 |
| US10160750B2 (en) | 2018-12-25 |
| EP3310777A1 (en) | 2018-04-25 |
| JP6742348B2 (ja) | 2020-08-19 |
| JP2018517753A (ja) | 2018-07-05 |
| CN108026083A (zh) | 2018-05-11 |
| EP3310777B1 (en) | 2019-10-09 |
| US20180141932A1 (en) | 2018-05-24 |
| CN108026083B (zh) | 2021-08-27 |
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