JP2019507167A5 - - Google Patents
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- Publication number
- JP2019507167A5 JP2019507167A5 JP2018545880A JP2018545880A JP2019507167A5 JP 2019507167 A5 JP2019507167 A5 JP 2019507167A5 JP 2018545880 A JP2018545880 A JP 2018545880A JP 2018545880 A JP2018545880 A JP 2018545880A JP 2019507167 A5 JP2019507167 A5 JP 2019507167A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- nhco
- independently selected
- independently
- conh
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 82
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 229910052799 carbon Inorganic materials 0.000 claims 17
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 230000009424 thromboembolic effect Effects 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 200000000007 Arterial disease 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
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis 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
- 208000028922 artery disease Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 201000010849 intracranial embolism Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662302220P | 2016-03-02 | 2016-03-02 | |
| US62/302,220 | 2016-03-02 | ||
| PCT/US2017/020161 WO2017151746A1 (en) | 2016-03-02 | 2017-03-01 | Diamide macrocycles having factor xia inhibiting activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019507167A JP2019507167A (ja) | 2019-03-14 |
| JP2019507167A5 true JP2019507167A5 (enExample) | 2020-04-02 |
Family
ID=58361087
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018545880A Pending JP2019507167A (ja) | 2016-03-02 | 2017-03-01 | 第ｘｉａ因子阻害活性を有するジアミド大員環 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10752641B2 (enExample) |
| EP (1) | EP3423458A1 (enExample) |
| JP (1) | JP2019507167A (enExample) |
| KR (1) | KR20180117156A (enExample) |
| CN (1) | CN109195973A (enExample) |
| WO (1) | WO2017151746A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6742348B2 (ja) | 2015-06-19 | 2020-08-19 | 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ジアミド大員環 |
| US10676477B2 (en) | 2015-07-29 | 2020-06-09 | Bristol-Myers Squibb Company | Factor XIa macrocycle 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 |
| 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 |
| WO2022109161A1 (en) * | 2020-11-19 | 2022-05-27 | Merck Sharp & Dohme Corp. | Plasma kallikrein inhibitors |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | 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. |
| WO2000077027A2 (en) | 1999-06-14 | 2000-12-21 | Tularik Limited | 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 |
| EP1427415B1 (en) | 2001-09-21 | 2009-08-12 | Brystol-Myers Squibb Company | 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 |
| CA2789622C (en) * | 2010-02-11 | 2018-04-03 | Bristol-Myers Squibb Company | Macrocycles as factor xia inhibitors |
| 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 |
| PT2880026T (pt) | 2012-08-03 | 2017-05-03 | Bristol Myers Squibb Co | Dihidropiridona p1 como inibidores de fator xia |
| LT2882734T (lt) * | 2012-08-03 | 2016-12-12 | Bristol-Myers Squibb Company | Dihidropiridonai, kaip xia faktoriaus slopikliai |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| KR20240017118A (ko) | 2014-01-31 | 2024-02-06 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 헤테로시클릭 P2' 기를 갖는 마크로사이클 |
| US10093683B2 (en) * | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| EP3189047B1 (en) * | 2014-09-04 | 2018-12-26 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
| NO2721243T3 (enExample) | 2014-10-01 | 2018-10-20 | ||
| JP6742348B2 (ja) | 2015-06-19 | 2020-08-19 | 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ジアミド大員環 |
| 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 |
| US10676477B2 (en) | 2015-07-29 | 2020-06-09 | Bristol-Myers Squibb Company | Factor XIa macrocycle inhibitors bearing a non-aromatic P2' group |
-
2017
- 2017-03-01 WO PCT/US2017/020161 patent/WO2017151746A1/en not_active Ceased
- 2017-03-01 KR KR1020187027820A patent/KR20180117156A/ko not_active Ceased
- 2017-03-01 CN CN201780026984.2A patent/CN109195973A/zh active Pending
- 2017-03-01 EP EP17712282.7A patent/EP3423458A1/en not_active Withdrawn
- 2017-03-01 JP JP2018545880A patent/JP2019507167A/ja active Pending
- 2017-03-01 US US16/080,418 patent/US10752641B2/en active Active
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