JP2018517753A5 - - Google Patents
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- Publication number
- JP2018517753A5 JP2018517753A5 JP2017565810A JP2017565810A JP2018517753A5 JP 2018517753 A5 JP2018517753 A5 JP 2018517753A5 JP 2017565810 A JP2017565810 A JP 2017565810A JP 2017565810 A JP2017565810 A JP 2017565810A JP 2018517753 A5 JP2018517753 A5 JP 2018517753A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- independently
- alkyl
- heterocyclyl
- carbocyclyl
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 111
- 125000000623 heterocyclic group Chemical group 0.000 claims 62
- 229910052739 hydrogen Inorganic materials 0.000 claims 38
- 229910052736 halogen Inorganic materials 0.000 claims 37
- 150000002367 halogens Chemical class 0.000 claims 37
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 33
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 33
- 125000004452 carbocyclyl group Chemical group 0.000 claims 31
- 229910052731 fluorine Inorganic materials 0.000 claims 28
- 229910052757 nitrogen Inorganic materials 0.000 claims 24
- 229910052801 chlorine Inorganic materials 0.000 claims 21
- 229910052794 bromium Inorganic materials 0.000 claims 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 229910052799 carbon Inorganic materials 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 7
- -1 = O Inorganic materials 0.000 claims 6
- 230000009424 thromboembolic effect Effects 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 0 C**1C(**)=C(C(NC)=O)N=C1 Chemical compound C**1C(**)=C(C(NC)=O)N=C1 0.000 description 157
- DRKFJWVVTIJFBT-UHFFFAOYSA-N Cc(c(-[n]1nnc(-c2ccccc2)c1)ccc1Cl)c1F Chemical compound Cc(c(-[n]1nnc(-c2ccccc2)c1)ccc1Cl)c1F DRKFJWVVTIJFBT-UHFFFAOYSA-N 0.000 description 4
- WJQYPAVCHUGBGU-UHFFFAOYSA-N Cc(cc(cc1)Cl)c1-[n]1nnc(-c2ccccc2)c1 Chemical compound Cc(cc(cc1)Cl)c1-[n]1nnc(-c2ccccc2)c1 WJQYPAVCHUGBGU-UHFFFAOYSA-N 0.000 description 4
- TYWQEYPAQNUPOX-UHFFFAOYSA-N Cc(c(-[n]1nnc(Cl)c1)ccc1Cl)c1F Chemical compound Cc(c(-[n]1nnc(Cl)c1)ccc1Cl)c1F TYWQEYPAQNUPOX-UHFFFAOYSA-N 0.000 description 3
- UKRDVXIHHFIBSZ-UHFFFAOYSA-N Cc(c(F)c(cc1)Cl)c1-[n]1nnc(C#N)c1 Chemical compound Cc(c(F)c(cc1)Cl)c1-[n]1nnc(C#N)c1 UKRDVXIHHFIBSZ-UHFFFAOYSA-N 0.000 description 3
- QRLDOZMPJNWVLC-UHFFFAOYSA-N Cc1cc(Cl)ccc1-[n]1nnc(O)c1 Chemical compound Cc1cc(Cl)ccc1-[n]1nnc(O)c1 QRLDOZMPJNWVLC-UHFFFAOYSA-N 0.000 description 3
- FUIAHKMPLJXXGO-UHFFFAOYSA-N Cc(c(-[n]1nnc(Br)c1)ccc1Cl)c1F Chemical compound Cc(c(-[n]1nnc(Br)c1)ccc1Cl)c1F FUIAHKMPLJXXGO-UHFFFAOYSA-N 0.000 description 2
- UPCDFPFOPGIKBT-UHFFFAOYSA-N Cc(c(-[n]1nncc1)ccc1Cl)c1F Chemical compound Cc(c(-[n]1nncc1)ccc1Cl)c1F UPCDFPFOPGIKBT-UHFFFAOYSA-N 0.000 description 2
- YXYNNFWXQVBZEN-UHFFFAOYSA-N Cc(c(F)c(cc1)Cl)c1-[n]1nnnc1 Chemical compound Cc(c(F)c(cc1)Cl)c1-[n]1nnnc1 YXYNNFWXQVBZEN-UHFFFAOYSA-N 0.000 description 2
- UGIMVWNCXGIZFG-UHFFFAOYSA-N Cc(cc(cc1)Cl)c1-[n]1ncc(C(F)(F)F)c1 Chemical compound Cc(cc(cc1)Cl)c1-[n]1ncc(C(F)(F)F)c1 UGIMVWNCXGIZFG-UHFFFAOYSA-N 0.000 description 2
- SIOHAFYQOWMGEV-UHFFFAOYSA-N Cc(cc1)cc(C)c1-[n]1nncc1 Chemical compound Cc(cc1)cc(C)c1-[n]1nncc1 SIOHAFYQOWMGEV-UHFFFAOYSA-N 0.000 description 2
- PXHHIBMOFPCBJQ-UHFFFAOYSA-N CC1N(C)CCC1 Chemical compound CC1N(C)CCC1 PXHHIBMOFPCBJQ-UHFFFAOYSA-N 0.000 description 1
- YFHWLEBTFZOVAI-UHFFFAOYSA-N CCCc1cc(Cl)ccc1-[n]1nnc(C(F)(F)F)c1 Chemical compound CCCc1cc(Cl)ccc1-[n]1nnc(C(F)(F)F)c1 YFHWLEBTFZOVAI-UHFFFAOYSA-N 0.000 description 1
- ARKHVLKOCPDMKY-UHFFFAOYSA-N CNc1cc(Cl)ccc1-[n]1nnc(C2CC2)c1 Chemical compound CNc1cc(Cl)ccc1-[n]1nnc(C2CC2)c1 ARKHVLKOCPDMKY-UHFFFAOYSA-N 0.000 description 1
- QUSXOOXCTYHDOT-UHFFFAOYSA-N Cc(c(-[n]1ncc(Cl)c1)ccc1Cl)c1F Chemical compound Cc(c(-[n]1ncc(Cl)c1)ccc1Cl)c1F QUSXOOXCTYHDOT-UHFFFAOYSA-N 0.000 description 1
- OGYWUDULVQLNLI-UHFFFAOYSA-N Cc(c(-[n]1ncnc1)ccc1Cl)c1F Chemical compound Cc(c(-[n]1ncnc1)ccc1Cl)c1F OGYWUDULVQLNLI-UHFFFAOYSA-N 0.000 description 1
- ATSVYCAQSPYJPC-UHFFFAOYSA-N Cc(c(-[n]1nnc(C(F)(F)F)c1)ccc1Cl)c1F Chemical compound Cc(c(-[n]1nnc(C(F)(F)F)c1)ccc1Cl)c1F ATSVYCAQSPYJPC-UHFFFAOYSA-N 0.000 description 1
- NYIWHEOSICMABJ-UNGZJSBBSA-N Cc(c(F)c(cc1)Cl)c1N/C=C(/C#N)\N=N Chemical compound Cc(c(F)c(cc1)Cl)c1N/C=C(/C#N)\N=N NYIWHEOSICMABJ-UNGZJSBBSA-N 0.000 description 1
- HINGMCLPXWSDQB-UHFFFAOYSA-N Cc(c(F)c1C)ccc1-[n]1nnc(C#N)c1 Chemical compound Cc(c(F)c1C)ccc1-[n]1nnc(C#N)c1 HINGMCLPXWSDQB-UHFFFAOYSA-N 0.000 description 1
- LEMJRRYQOXVXKP-UHFFFAOYSA-N Cc(c([Br]=C)ccc1Cl)c1F Chemical compound Cc(c([Br]=C)ccc1Cl)c1F LEMJRRYQOXVXKP-UHFFFAOYSA-N 0.000 description 1
- SBAKFPOOEWGIMM-UHFFFAOYSA-N Cc(cc(cc1)Cl)c1-[n]1nnc(C2CC2)c1 Chemical compound Cc(cc(cc1)Cl)c1-[n]1nnc(C2CC2)c1 SBAKFPOOEWGIMM-UHFFFAOYSA-N 0.000 description 1
- ZGRHBEFXFOAXIV-UHFFFAOYSA-N Cc(cc1C)ccc1-[n]1nnc(Br)c1 Chemical compound Cc(cc1C)ccc1-[n]1nnc(Br)c1 ZGRHBEFXFOAXIV-UHFFFAOYSA-N 0.000 description 1
- DSOORFAOGONVAF-UHFFFAOYSA-N Cc1c[n](-c(cc2)c(C)c(F)c2Cl)nn1 Chemical compound Cc1c[n](-c(cc2)c(C)c(F)c2Cl)nn1 DSOORFAOGONVAF-UHFFFAOYSA-N 0.000 description 1
- JWWYZBDKYVFFCQ-UHFFFAOYSA-N Cc1c[n](-c(cc2)c(C)cc2Cl)nn1 Chemical compound Cc1c[n](-c(cc2)c(C)cc2Cl)nn1 JWWYZBDKYVFFCQ-UHFFFAOYSA-N 0.000 description 1
- PPZQUDSVSGGEQB-UHFFFAOYSA-N Cc1c[n](-c2c(C)c(F)c(C)cc2)nn1 Chemical compound Cc1c[n](-c2c(C)c(F)c(C)cc2)nn1 PPZQUDSVSGGEQB-UHFFFAOYSA-N 0.000 description 1
- YVOWGFBOBOZORT-UHFFFAOYSA-N Cc1cc(Cl)ccc1-[n]1ncc(Cl)c1 Chemical compound Cc1cc(Cl)ccc1-[n]1ncc(Cl)c1 YVOWGFBOBOZORT-UHFFFAOYSA-N 0.000 description 1
- DQMFBHFMMBHHNX-UHFFFAOYSA-N Cc1cc(Cl)ccc1-[n]1nnc(Br)c1 Chemical compound Cc1cc(Cl)ccc1-[n]1nnc(Br)c1 DQMFBHFMMBHHNX-UHFFFAOYSA-N 0.000 description 1
- GFDGCPAHWMLSEI-UHFFFAOYSA-N Cc1cc(Cl)ccc1-[n]1nnc(C#N)c1 Chemical compound Cc1cc(Cl)ccc1-[n]1nnc(C#N)c1 GFDGCPAHWMLSEI-UHFFFAOYSA-N 0.000 description 1
- KRYQSDCIOZEBRL-UHFFFAOYSA-N Cc1cc(Cl)ccc1-[n]1nnc(Cl)c1 Chemical compound Cc1cc(Cl)ccc1-[n]1nnc(Cl)c1 KRYQSDCIOZEBRL-UHFFFAOYSA-N 0.000 description 1
- ZAGDBLVKXMLMGP-UHFFFAOYSA-N Cc1cc(Cl)ccc1-[n]1nncc1 Chemical compound Cc1cc(Cl)ccc1-[n]1nncc1 ZAGDBLVKXMLMGP-UHFFFAOYSA-N 0.000 description 1
- VJRMGOBYEDCHHJ-UHFFFAOYSA-N Cc1cc(Cl)ccc1-c1cncnc1 Chemical compound Cc1cc(Cl)ccc1-c1cncnc1 VJRMGOBYEDCHHJ-UHFFFAOYSA-N 0.000 description 1
- ZZAJFWXXFZTTLH-UHFFFAOYSA-N Cc1cc(Cl)ccc1C#N Chemical compound Cc1cc(Cl)ccc1C#N ZZAJFWXXFZTTLH-UHFFFAOYSA-N 0.000 description 1
- RWXLVNJPMZXECS-UHFFFAOYSA-N Cc1cc(Cl)ccc1C(F)(F)F Chemical compound Cc1cc(Cl)ccc1C(F)(F)F RWXLVNJPMZXECS-UHFFFAOYSA-N 0.000 description 1
- OSOUNOBYRMOXQQ-UHFFFAOYSA-N Cc1cccc(Cl)c1 Chemical compound Cc1cccc(Cl)c1 OSOUNOBYRMOXQQ-UHFFFAOYSA-N 0.000 description 1
- XWNCXZSWLVMDOJ-UHFFFAOYSA-N Nc(c(-[n]1ncnc1)ccc1Cl)c1F Chemical compound Nc(c(-[n]1ncnc1)ccc1Cl)c1F XWNCXZSWLVMDOJ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562181875P | 2015-06-19 | 2015-06-19 | |
| US62/181,875 | 2015-06-19 | ||
| PCT/US2016/037823 WO2016205482A1 (en) | 2015-06-19 | 2016-06-16 | Diamide macrocycles as factor xia inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018517753A JP2018517753A (ja) | 2018-07-05 |
| JP2018517753A5 true JP2018517753A5 (enExample) | 2019-06-20 |
| JP6742348B2 JP6742348B2 (ja) | 2020-08-19 |
Family
ID=56204067
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017565810A Active JP6742348B2 (ja) | 2015-06-19 | 2016-06-16 | 第ｘｉａ因子阻害剤としてのジアミド大員環 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10160750B2 (enExample) |
| EP (1) | EP3310777B1 (enExample) |
| JP (1) | JP6742348B2 (enExample) |
| CN (1) | CN108026083B (enExample) |
| ES (1) | ES2762987T3 (enExample) |
| WO (1) | WO2016205482A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY35971A (es) | 2014-01-31 | 2015-07-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| CN108026083B (zh) | 2015-06-19 | 2021-08-27 | 百时美施贵宝公司 | 作为因子xia抑制剂的二酰胺大环 |
| JP6629958B2 (ja) | 2015-07-29 | 2020-01-15 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤 |
| EP3868753B1 (en) | 2015-07-29 | 2022-12-21 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group |
| US10752641B2 (en) | 2016-03-02 | 2020-08-25 | Bristol-Myers Squibb Company | Diamide macrocycles having factor XIa inhibiting activity |
| CN113166099A (zh) * | 2018-12-17 | 2021-07-23 | 拜耳公司 | 用于治疗和/或预防血栓形成性或血栓栓塞性疾病和/或血栓形成性或血栓栓塞性并发症的取代的氧代吡啶衍生物 |
| 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 |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| AU5546000A (en) | 1999-06-14 | 2001-01-02 | Protherics Molecular Design Limited | Compounds |
| 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 |
| HRP20080382A2 (en) | 2001-09-21 | 2008-12-31 | Bristol-Myers Squibb Company A Delaware (Usa) Corporation | 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 |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered 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 |
| CN101137412B (zh) | 2005-01-13 | 2012-11-07 | 布里斯托尔-迈尔斯·斯奎布公司 | 用作凝血因子XIa抑制剂的取代的二芳基化合物 |
| WO2006089005A2 (en) | 2005-02-17 | 2006-08-24 | Bristol-Myers Squibb Company | Combination of selective factor viia and/or xia and plasma kallikrein inhibitors |
| US8466295B2 (en) | 2005-12-14 | 2013-06-18 | Bristol-Myers Squibb Company | Thiophene derivatives as factor XIa inhibitors |
| NZ568595A (en) | 2005-12-14 | 2010-04-30 | Bristol Myers Squibb Co | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor Xla inhibitors |
| US8163749B2 (en) | 2005-12-14 | 2012-04-24 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| PE20071132A1 (es) * | 2005-12-23 | 2007-12-14 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| US8410155B2 (en) | 2006-12-15 | 2013-04-02 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIA inhibitors |
| CA2676933C (en) | 2007-02-28 | 2015-09-29 | Leo Pharma A/S | Novel phosphodiesterase inhibitors |
| MX2009012847A (es) | 2007-06-13 | 2009-12-08 | Bristol Myers Squibb Co | Analogos dipeptidicos como inhibidores de factores de coagulacion. |
| ATE543811T1 (de) | 2008-03-13 | 2012-02-15 | Bristol Myers Squibb Co | Pyridazinderivate als faktor-xia-inhibitoren |
| FR2944014A1 (fr) | 2009-04-06 | 2010-10-08 | Univ Grenoble 1 | Peptides cycliques a activite antiparasitaire |
| KR101843542B1 (ko) | 2010-02-11 | 2018-03-30 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 ＸＩａ 억제제로서의 마크로사이클 |
| EP2603080A4 (en) | 2010-08-12 | 2014-01-22 | Enanta Pharm Inc | HEPATITIS C-VIRUS HEMMER |
| 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 |
| 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 |
| UY34393A (es) | 2011-10-14 | 2013-04-30 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor xia |
| JP6033317B2 (ja) | 2011-10-14 | 2016-11-30 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害剤としての置換テトラヒドロイソキノリン化合物 |
| EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| BR112015002081A2 (pt) * | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona p1 como inibidores de fator xia |
| EA025392B1 (ru) | 2012-08-03 | 2016-12-30 | Бристол-Маерс Сквибб Компани | Дигидропиридон р1 в качестве ингибиторов фактора xia |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EA032092B1 (ru) | 2012-10-12 | 2019-04-30 | Бристол-Майерс Сквибб Компани | Кристаллические формы ингибитора фактора xia |
| EP2978751B1 (en) | 2013-03-25 | 2018-12-05 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
| WO2014160592A2 (en) * | 2013-03-27 | 2014-10-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| UY35971A (es) | 2014-01-31 | 2015-07-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia |
| 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 (enExample) | 2014-10-01 | 2018-10-20 | ||
| CN108026083B (zh) | 2015-06-19 | 2021-08-27 | 百时美施贵宝公司 | 作为因子xia抑制剂的二酰胺大环 |
| EP3868753B1 (en) | 2015-07-29 | 2022-12-21 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group |
| JP6629958B2 (ja) | 2015-07-29 | 2020-01-15 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤 |
| KR102697816B1 (ko) | 2015-08-05 | 2024-08-21 | 브리스톨-마이어스 스큅 컴퍼니 | 신규 치환된 글리신 유도된 fxia 억제제 |
| US10752641B2 (en) | 2016-03-02 | 2020-08-25 | Bristol-Myers Squibb Company | Diamide macrocycles having factor XIa inhibiting activity |
-
2016
- 2016-06-16 CN CN201680048685.4A patent/CN108026083B/zh active Active
- 2016-06-16 ES ES16732191T patent/ES2762987T3/es active Active
- 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 JP JP2017565810A patent/JP6742348B2/ja active Active
- 2016-06-16 WO PCT/US2016/037823 patent/WO2016205482A1/en not_active Ceased
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