JP2019507167A - 第xia因子阻害活性を有するジアミド大員環 - Google Patents
第xia因子阻害活性を有するジアミド大員環 Download PDFInfo
- Publication number
- JP2019507167A JP2019507167A JP2018545880A JP2018545880A JP2019507167A JP 2019507167 A JP2019507167 A JP 2019507167A JP 2018545880 A JP2018545880 A JP 2018545880A JP 2018545880 A JP2018545880 A JP 2018545880A JP 2019507167 A JP2019507167 A JP 2019507167A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- nhco
- independently selected
- pharmaceutically acceptable
- independently
- 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
Links
- 0 CC(c1ccc(*)cc1C)=C Chemical compound CC(c1ccc(*)cc1C)=C 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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 true JP2019507167A (ja) | 2019-03-14 |
| JP2019507167A5 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) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023551150A (ja) * | 2020-11-19 | 2023-12-07 | メルク・シャープ・アンド・ドーム・エルエルシー | 血漿カリクレイン阻害剤 |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10160750B2 (en) | 2015-06-19 | 2018-12-25 | Bristol-Myers Squibb Company | Diamide macrocycles as factor XIa inhibitors |
| CN107922393A (zh) | 2015-07-29 | 2018-04-17 | 百时美施贵宝公司 | 携带非芳族p2,基团的因子xia新大环 |
| CN107849026B (zh) | 2015-07-29 | 2021-01-01 | 百时美施贵宝公司 | 携带烷基或环烷基p2′部分的因子xia大环抑制剂 |
| US20230373972A1 (en) | 2020-09-17 | 2023-11-23 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Piperazine derivative, preparation method therefor and use thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013519678A (ja) * | 2010-02-11 | 2013-05-30 | ブリストル−マイヤーズ スクイブ カンパニー | 第xia因子阻害剤としてのマクロ環 |
| JP2015524443A (ja) * | 2012-08-03 | 2015-08-24 | 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ヒドロピリドンp1 |
| WO2015164308A1 (en) * | 2014-04-22 | 2015-10-29 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
Family Cites Families (18)
| 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. |
| WO2000076970A2 (en) | 1999-06-14 | 2000-12-21 | 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 |
| GEP20074098B (en) | 2001-09-21 | 2007-05-10 | Bristol Myers Squibb Co | 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 |
| 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 |
| US9409908B2 (en) | 2012-08-03 | 2016-08-09 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor XIa inhibitors |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| ES2687498T3 (es) | 2014-01-31 | 2018-10-25 | Bristol-Myers Squibb Company | Macrociclos con grupos P2¿ heterocíclicos como inhibidores del factor XIa |
| ES2714283T3 (es) * | 2014-09-04 | 2019-05-28 | Bristol Myers Squibb Co | Macrociclos de diamida que son inhibidores de FXIa |
| NO2721243T3 (enExample) | 2014-10-01 | 2018-10-20 | ||
| US10160750B2 (en) | 2015-06-19 | 2018-12-25 | Bristol-Myers Squibb Company | Diamide macrocycles as factor XIa inhibitors |
| CN107922393A (zh) | 2015-07-29 | 2018-04-17 | 百时美施贵宝公司 | 携带非芳族p2,基团的因子xia新大环 |
| CN107849026B (zh) | 2015-07-29 | 2021-01-01 | 百时美施贵宝公司 | 携带烷基或环烷基p2′部分的因子xia大环抑制剂 |
-
2017
- 2017-03-01 WO PCT/US2017/020161 patent/WO2017151746A1/en not_active Ceased
- 2017-03-01 CN CN201780026984.2A patent/CN109195973A/zh active Pending
- 2017-03-01 KR KR1020187027820A patent/KR20180117156A/ko not_active Ceased
- 2017-03-01 JP JP2018545880A patent/JP2019507167A/ja active Pending
- 2017-03-01 US US16/080,418 patent/US10752641B2/en active Active
- 2017-03-01 EP EP17712282.7A patent/EP3423458A1/en not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013519678A (ja) * | 2010-02-11 | 2013-05-30 | ブリストル−マイヤーズ スクイブ カンパニー | 第xia因子阻害剤としてのマクロ環 |
| JP2015524443A (ja) * | 2012-08-03 | 2015-08-24 | 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ヒドロピリドンp1 |
| WO2015164308A1 (en) * | 2014-04-22 | 2015-10-29 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023551150A (ja) * | 2020-11-19 | 2023-12-07 | メルク・シャープ・アンド・ドーム・エルエルシー | 血漿カリクレイン阻害剤 |
| JP7787890B2 (ja) | 2020-11-19 | 2025-12-17 | メルク・シャープ・アンド・ドーム・エルエルシー | 血漿カリクレイン阻害剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017151746A1 (en) | 2017-09-08 |
| US10752641B2 (en) | 2020-08-25 |
| US20190062343A1 (en) | 2019-02-28 |
| CN109195973A (zh) | 2019-01-11 |
| KR20180117156A (ko) | 2018-10-26 |
| EP3423458A1 (en) | 2019-01-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7317905B2 (ja) | 第xia因子阻害剤としてのピリミジノン | |
| JP6526796B2 (ja) | Fxia阻害剤であるジアミドマクロ環 | |
| JP6082462B2 (ja) | 第xia因子阻害剤としてのジヒドロピリドンp1 | |
| JP5841547B2 (ja) | 第xia因子阻害剤としてのマクロ環 | |
| US9403774B2 (en) | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors | |
| US9315519B2 (en) | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors | |
| JP2018522046A (ja) | 新規な置換グリシン誘導のfxia阻害剤 | |
| JP6629958B2 (ja) | 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 | |
| JP6742348B2 (ja) | 第xia因子阻害剤としてのジアミド大員環 | |
| JP2019507167A (ja) | 第xia因子阻害活性を有するジアミド大員環 | |
| JP6816103B2 (ja) | 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 | |
| US20190144393A1 (en) | Factor xia macrocycles with novel p1 groups | |
| BR112017006702B1 (pt) | Pirimidinonas inibidoras de fator xia, composição farmacêutica e seu uso |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200221 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20200221 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20210128 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20210202 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20210430 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20210701 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20211124 |