JP2018522024A5 - - Google Patents
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- Publication number
- JP2018522024A5 JP2018522024A5 JP2018504188A JP2018504188A JP2018522024A5 JP 2018522024 A5 JP2018522024 A5 JP 2018522024A5 JP 2018504188 A JP2018504188 A JP 2018504188A JP 2018504188 A JP2018504188 A JP 2018504188A JP 2018522024 A5 JP2018522024 A5 JP 2018522024A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- independently
- heterocyclyl
- independently selected
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 81
- 125000000623 heterocyclic group Chemical group 0.000 claims 51
- 229910052739 hydrogen Inorganic materials 0.000 claims 38
- 229910052799 carbon Inorganic materials 0.000 claims 34
- 125000004452 carbocyclyl group Chemical group 0.000 claims 20
- 229910052731 fluorine Inorganic materials 0.000 claims 19
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 18
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 229910052801 chlorine Inorganic materials 0.000 claims 17
- 229910052794 bromium Inorganic materials 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 208000001435 Thromboembolism Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 230000009424 thromboembolic effect Effects 0.000 claims 4
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 2
- -1 = O Inorganic materials 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010003178 Arterial thrombosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 206010008088 Cerebral artery embolism Diseases 0.000 claims 1
- 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 208000005189 Embolism Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000001746 atrial effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 201000010849 intracranial embolism Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 1
- 230000002861 ventricular Effects 0.000 claims 1
- 0 CC1N(C)CCN(*)C1 Chemical compound CC1N(C)CCN(*)C1 0.000 description 1
- JVZPMYMWYNQLKR-FZPRHHONSA-N CN(c(cccc1I)c1I)/N=C\C(C(NC(CCCCCNC(C(C1)N2CCN1I)=O)c1cc2ccc1)=O)=C Chemical compound CN(c(cccc1I)c1I)/N=C\C(C(NC(CCCCCNC(C(C1)N2CCN1I)=O)c1cc2ccc1)=O)=C JVZPMYMWYNQLKR-FZPRHHONSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562198188P | 2015-07-29 | 2015-07-29 | |
| US62/198,188 | 2015-07-29 | ||
| PCT/US2016/044363 WO2017019821A1 (en) | 2015-07-29 | 2016-07-28 | Factor xia new macrocycle bearing a non-aromatic p2' group |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018522024A JP2018522024A (ja) | 2018-08-09 |
| JP2018522024A5 true JP2018522024A5 (enExample) | 2019-08-29 |
| JP6816103B2 JP6816103B2 (ja) | 2021-01-20 |
Family
ID=56609993
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018504188A Active JP6816103B2 (ja) | 2015-07-29 | 2016-07-28 | 非芳香族性Ｐ２’基を担持する新規大員環の第ＸＩａ因子阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10676477B2 (enExample) |
| EP (2) | EP3868753B1 (enExample) |
| JP (1) | JP6816103B2 (enExample) |
| KR (1) | KR102729666B1 (enExample) |
| CN (3) | CN114805365B (enExample) |
| ES (2) | ES2937156T3 (enExample) |
| WO (1) | WO2017019821A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9453018B2 (en) * | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| 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 |
| US10752641B2 (en) | 2016-03-02 | 2020-08-25 | Bristol-Myers Squibb Company | Diamide macrocycles having factor XIa inhibiting activity |
| EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3065190D1 (en) | 1979-11-05 | 1983-11-10 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| 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 |
| 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 |
| US8163749B2 (en) | 2005-12-14 | 2012-04-24 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| NZ568595A (en) | 2005-12-14 | 2010-04-30 | Bristol Myers Squibb Co | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor Xla inhibitors |
| US8466295B2 (en) | 2005-12-14 | 2013-06-18 | Bristol-Myers Squibb Company | Thiophene derivatives as factor XIa inhibitors |
| US8410155B2 (en) | 2006-12-15 | 2013-04-02 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIA inhibitors |
| PE20081775A1 (es) * | 2006-12-20 | 2008-12-18 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| 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 |
| KR101843542B1 (ko) | 2010-02-11 | 2018-03-30 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 ＸＩａ 억제제로서의 마크로사이클 |
| 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 |
| EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| 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 |
| 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 |
| EA032092B1 (ru) | 2012-10-12 | 2019-04-30 | Бристол-Майерс Сквибб Компани | Кристаллические формы ингибитора 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 |
| EP2978751B1 (en) | 2013-03-25 | 2018-12-05 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
| 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 | ||
| 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 |
| 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
- 2016-07-28 EP EP21164321.8A patent/EP3868753B1/en active Active
- 2016-07-28 EP EP16747990.6A patent/EP3328852B1/en active Active
- 2016-07-28 ES ES21164321T patent/ES2937156T3/es active Active
- 2016-07-28 WO PCT/US2016/044363 patent/WO2017019821A1/en not_active Ceased
- 2016-07-28 CN CN202210443120.3A patent/CN114805365B/zh active Active
- 2016-07-28 JP JP2018504188A patent/JP6816103B2/ja active Active
- 2016-07-28 CN CN201680044102.0A patent/CN107922393A/zh active Pending
- 2016-07-28 ES ES16747990T patent/ES2871111T3/es active Active
- 2016-07-28 US US15/747,867 patent/US10676477B2/en active Active
- 2016-07-28 KR KR1020187005398A patent/KR102729666B1/ko active Active
- 2016-07-28 CN CN202210447302.8A patent/CN114874222B/zh active Active
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