JP6033317B2 - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP6033317B2 JP6033317B2 JP2014535894A JP2014535894A JP6033317B2 JP 6033317 B2 JP6033317 B2 JP 6033317B2 JP 2014535894 A JP2014535894 A JP 2014535894A JP 2014535894 A JP2014535894 A JP 2014535894A JP 6033317 B2 JP6033317 B2 JP 6033317B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- group
- chloro
- acryloyl
- 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.)
- Expired - Fee Related
Links
- 0 CCN(C(C(N*)=O)C1=S2(*)(CC2)CCCCCC1)C(C)=O Chemical compound CCN(C(C(N*)=O)C1=S2(*)(CC2)CCCCCC1)C(C)=O 0.000 description 5
- LWNZPXFPMLRKGK-UHFFFAOYSA-N CC(C)(C)OC(N(CCN1c2c(CCN=C3)c3ccc2)CC1=O)=O Chemical compound CC(C)(C)OC(N(CCN1c2c(CCN=C3)c3ccc2)CC1=O)=O LWNZPXFPMLRKGK-UHFFFAOYSA-N 0.000 description 1
- UUJNHTZCROBQHX-UHFFFAOYSA-N CC(C)C(NCCc1ccccc1)=O Chemical compound CC(C)C(NCCc1ccccc1)=O UUJNHTZCROBQHX-UHFFFAOYSA-N 0.000 description 1
- QHQKYJAIOSKSFL-UHFFFAOYSA-N CC(C)C(NCc1ccccc1)=O Chemical compound CC(C)C(NCc1ccccc1)=O QHQKYJAIOSKSFL-UHFFFAOYSA-N 0.000 description 1
- UIKJRDSCEYGECG-UHFFFAOYSA-N CC(C)C(OCc1ccccc1)=O Chemical compound CC(C)C(OCc1ccccc1)=O UIKJRDSCEYGECG-UHFFFAOYSA-N 0.000 description 1
- LMTGCJANOQOGPI-UHFFFAOYSA-N CC(N(C)c1ccccc1)=O Chemical compound CC(N(C)c1ccccc1)=O LMTGCJANOQOGPI-UHFFFAOYSA-N 0.000 description 1
- XVAIDCNLVLTVFM-UHFFFAOYSA-N CC(Nc(cc1)ccc1OC)=O Chemical compound CC(Nc(cc1)ccc1OC)=O XVAIDCNLVLTVFM-UHFFFAOYSA-N 0.000 description 1
- XWSRKIHDBLVVQU-UHFFFAOYSA-N CCC(Nc1ccc(C)cc1)=O Chemical compound CCC(Nc1ccc(C)cc1)=O XWSRKIHDBLVVQU-UHFFFAOYSA-N 0.000 description 1
- FVTFRNFJCGAMRS-MJZVOSTQSA-N COC(NCc(cc1)ccc1NC([C@H](c1c(CC2)cccc1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O Chemical compound COC(NCc(cc1)ccc1NC([C@H](c1c(CC2)cccc1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O FVTFRNFJCGAMRS-MJZVOSTQSA-N 0.000 description 1
- QYGIONMGVBWAHW-XNWCZRBMSA-N COC(Nc(cc1)ccc1NC(C(c1c(CC2)nc[nH]1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O Chemical compound COC(Nc(cc1)ccc1NC(C(c1c(CC2)nc[nH]1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O QYGIONMGVBWAHW-XNWCZRBMSA-N 0.000 description 1
- GVQIGVXVWBEQBR-NYYWCZLTSA-N COCCOc1cc(CCN(C2C(Nc(cc3)ccc3C(O)=O)=O)C(/C=C/c(cc(cc3)Cl)c3-[n]3nnnc3)=O)c2cc1 Chemical compound COCCOc1cc(CCN(C2C(Nc(cc3)ccc3C(O)=O)=O)C(/C=C/c(cc(cc3)Cl)c3-[n]3nnnc3)=O)c2cc1 GVQIGVXVWBEQBR-NYYWCZLTSA-N 0.000 description 1
- FNJYORJOJJSXMG-BJMVGYQFSA-N Cc1n[n](C)c(CC2)c1C(C(Nc(cc1)cc(CC3)c1NC3=O)=O)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O Chemical compound Cc1n[n](C)c(CC2)c1C(C(Nc(cc1)cc(CC3)c1NC3=O)=O)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O FNJYORJOJJSXMG-BJMVGYQFSA-N 0.000 description 1
- BOJKOKSDOYFFOO-KZLCEWNNSA-N OC(c(cc1)ccc1NC([C@H](c(cc1)c(CC2)cc1OCc1ccccc1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O Chemical compound OC(c(cc1)ccc1NC([C@H](c(cc1)c(CC2)cc1OCc1ccccc1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O BOJKOKSDOYFFOO-KZLCEWNNSA-N 0.000 description 1
- XLVCNINDJUKQNE-FRHHVXPKSA-N OC(c(cc1)ccc1NC([C@H](c1c(CC2)cccc1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O Chemical compound OC(c(cc1)ccc1NC([C@H](c1c(CC2)cccc1)N2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O)=O XLVCNINDJUKQNE-FRHHVXPKSA-N 0.000 description 1
Classifications
-
- 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
- C07D401/10—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 linked by a carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161547305P | 2011-10-14 | 2011-10-14 | |
| US61/547,305 | 2011-10-14 | ||
| PCT/US2012/059859 WO2013055984A1 (en) | 2011-10-14 | 2012-10-12 | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014528479A JP2014528479A (ja) | 2014-10-27 |
| JP2014528479A5 JP2014528479A5 (enExample) | 2015-12-03 |
| JP6033317B2 true JP6033317B2 (ja) | 2016-11-30 |
Family
ID=47080862
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014535894A Expired - Fee Related JP6033317B2 (ja) | 2011-10-14 | 2012-10-12 | 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 |
Country Status (7)
| Country | Link |
|---|---|
| US (5) | US9108951B2 (enExample) |
| EP (2) | EP2766345B1 (enExample) |
| JP (1) | JP6033317B2 (enExample) |
| CN (1) | CN103987697B (enExample) |
| ES (2) | ES2699226T3 (enExample) |
| IN (1) | IN2014CN02806A (enExample) |
| WO (1) | WO2013055984A1 (enExample) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2822130T3 (es) | 2010-02-11 | 2021-04-29 | Bristol Myers Squibb Co | Macrociclos como inhibidores del factor XIa |
| 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 |
| IN2014CN02806A (enExample) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| EA023649B1 (ru) | 2011-10-14 | 2016-06-30 | Бристол-Майерс Сквибб Кампани | ЗАМЕЩЕННЫЕ СОЕДИНЕНИЯ ТЕТРАГИДРОИЗОХИНОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa |
| ES2579832T3 (es) | 2011-10-14 | 2016-08-17 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa |
| HUE032622T2 (en) | 2012-08-03 | 2017-10-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| CA2880898A1 (en) | 2012-08-03 | 2014-02-06 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor xia inhibitors |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| NZ707990A (en) | 2012-10-12 | 2018-07-27 | Bristol Myers Squibb Co | Crystalline forms of a factor xia inhibitor |
| EP2906541B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| JP6280912B2 (ja) | 2013-03-14 | 2018-02-14 | 武田薬品工業株式会社 | 複素環化合物 |
| US9738655B2 (en) | 2013-03-25 | 2017-08-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors |
| US10053468B2 (en) | 2013-07-03 | 2018-08-21 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| ES2950424T3 (es) | 2013-07-03 | 2023-10-09 | Takeda Pharmaceuticals Co | Compuesto de amida |
| EP3049435A4 (en) * | 2013-09-27 | 2017-03-29 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| WO2015054087A1 (en) | 2013-10-07 | 2015-04-16 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| TWI859674B (zh) | 2014-01-31 | 2024-10-21 | 美商必治妥美雅史谷比公司 | 作為凝血因子xia抑制劑之具有雜環p2'基團之巨環化合物 |
| EP3104703B1 (en) | 2014-02-11 | 2020-11-18 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| WO2015123091A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| US10093683B2 (en) | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| ES2848348T3 (es) | 2014-05-16 | 2021-08-06 | Cumberland Pharmaceuticals Inc | Composiciones y métodos de tratamiento con ifetroban de la fibrosis cardíaca |
| MX2016016870A (es) * | 2014-07-01 | 2017-05-01 | Takeda Pharmaceuticals Co | Compuestos heterociclicos y su uso como inhibidores de receptor huerfano relacionado con retinoide (ror) gamma-t. |
| US9868727B2 (en) | 2014-07-28 | 2018-01-16 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| MX378273B (es) | 2014-08-01 | 2025-03-10 | Nuevolution As | Compuestos activos hacia bromodominios. |
| CN105461688B (zh) * | 2014-08-26 | 2017-12-29 | 上海医药工业研究院 | 苯并咪唑化合物k的合成方法 |
| US10081623B2 (en) | 2014-09-04 | 2018-09-25 | Bristol-Myers Squibb Company | Diamide macrocycles that are FXIa inhibitors |
| JP6799530B2 (ja) | 2014-10-01 | 2020-12-16 | メディミューン リミテッド | チカグレロルに対する抗体および使用方法 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| ES2762987T3 (es) | 2015-06-19 | 2020-05-26 | Bristol Myers Squibb Co | Macrociclos de diamida como inhibidores del factor XIA |
| CA2990880A1 (en) | 2015-06-30 | 2017-01-05 | Cumberland Pharmaceuticals, Inc. | Thromboxane receptor antagonists in aerd/asthma |
| ES2899906T3 (es) | 2015-07-06 | 2022-03-15 | Alkermes Inc | Inhibidores bicíclicos de histona desacetilasa |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| EP3868753B1 (en) | 2015-07-29 | 2022-12-21 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group |
| 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 |
| US10344039B2 (en) | 2015-10-29 | 2019-07-09 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use |
| CN108430471B (zh) | 2015-10-29 | 2021-07-09 | 默沙东公司 | 因子XIa抑制剂 |
| JP6964343B2 (ja) | 2015-11-20 | 2021-11-10 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的プロテアーゼ１阻害剤としてのプリノン |
| US11480559B2 (en) * | 2016-01-07 | 2022-10-25 | Fujimori Kogyo Co., Ltd. | Blood collection tube, reagent, and method for analyzing blood characteristics using same |
| CN107540659A (zh) * | 2016-06-29 | 2018-01-05 | 四川科伦博泰生物医药股份有限公司 | 四氢异喹啉类化合物、其制备方法、药物组合物及其用途 |
| TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
| ES2909086T3 (es) | 2017-01-11 | 2022-05-05 | Alkermes Inc | Inhibidores bicíclicos de histona desacetilasa |
| EA039417B1 (ru) | 2017-08-07 | 2022-01-25 | Родин Терапеутикс, Инк. | Бициклические ингибиторы гистондеацетилазы |
| CN109721539B (zh) * | 2017-10-27 | 2021-07-09 | 天津药物研究院有限公司 | 吡唑酰胺类衍生物及其制备方法和用途 |
| CN109867660A (zh) * | 2017-12-01 | 2019-06-11 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的四氢异喹啉酰胺化合物及其药物用途 |
| JP7458984B2 (ja) | 2018-03-28 | 2024-04-01 | 四川科倫博泰生物医薬股▲フン▼有限公司 | テトラヒドロイソキノリン系誘導体、その製造方法及び用途 |
| MA53721A (fr) * | 2018-09-28 | 2021-09-15 | Janssen Pharmaceutica Nv | Modulateurs de la monoacylglycérol lipase |
| US20200102311A1 (en) * | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol Lipase Modulators |
| HRP20231306T1 (hr) * | 2018-10-22 | 2024-02-02 | C4X Discovery Limited | Terapeutski spojevi |
| CN111727186B (zh) * | 2018-11-11 | 2022-11-08 | 上海海雁医药科技有限公司 | 双杂环取代的吡啶-2(1h)-酮衍生物、其制法与医药上的用途 |
| JP7697934B2 (ja) | 2019-09-30 | 2025-06-24 | ヤンセン ファーマシューティカ エヌ．ベー． | 放射線標識されたｍｇｌ ｐｅｔリガンド |
| US20230062486A1 (en) * | 2019-12-19 | 2023-03-02 | Betta Pharmaceuticals Co., Ltd | Kras g12c inhibitor and pharmaceutical use thereof |
| ES3048448T3 (en) * | 2020-07-22 | 2025-12-10 | Janssen Pharmaceutica Nv | Compounds useful as factor xia inhibitors |
Family Cites Families (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR1525186A (fr) | 1967-03-29 | 1968-05-17 | Roussel Uclaf | Nouvelles pénicillines et procédé de préparation |
| DE3065190D1 (en) | 1979-11-05 | 1983-11-10 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| US4843062A (en) | 1987-12-23 | 1989-06-27 | American Home Products Corporation | N-acyl-N-napthoylglycines as aldose reductase inhibitors |
| DE4034829A1 (de) | 1990-11-02 | 1992-05-07 | Merck Patent Gmbh | Cyclopeptide |
| JP3190431B2 (ja) | 1991-07-01 | 2001-07-23 | 三菱化学株式会社 | ケトン誘導体 |
| GB9206757D0 (en) | 1992-03-27 | 1992-05-13 | Ferring Bv | Novel peptide receptor ligands |
| US5624936A (en) | 1995-03-29 | 1997-04-29 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1996034010A2 (en) | 1995-03-29 | 1996-10-31 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5869682A (en) | 1996-04-03 | 1999-02-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| AU717298B2 (en) | 1996-04-03 | 2000-03-23 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| 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. |
| SK286736B6 (sk) | 1998-03-19 | 2009-04-06 | Vertex Pharmaceuticals Incorporated | Inhibítory kaspázy, farmaceutická kompozícia, ktorá ich obsahuje, a ich použitie |
| JP2002516327A (ja) | 1998-05-26 | 2002-06-04 | ワーナー−ランバート・カンパニー | 細胞増殖の阻害剤としての二環式ピリミジンおよび二環式３，４−ジヒドロピリミジン |
| US6307049B1 (en) | 1998-09-30 | 2001-10-23 | The Procter & Gamble Co. | Heterocyclic 2-substituted ketoamides |
| EP1016663A1 (en) | 1999-01-02 | 2000-07-05 | Aventis Pharma Deutschland GmbH | Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity) |
| TR200101903T2 (tr) | 1999-01-02 | 2001-11-21 | Aventis Pharma Deutschland Gmbh | Yeni malonik asit türevleri, bunların preparasyon işlemleri. |
| AU4111700A (en) | 1999-04-09 | 2000-11-14 | Basf Aktiengesellschaft | Low-molecular inhibitors of complement proteases |
| 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 |
| EP1125925A1 (en) | 2000-02-15 | 2001-08-22 | Applied Research Systems ARS Holding N.V. | Amine derivatives for the treatment of apoptosis |
| AU5959201A (en) * | 2000-05-11 | 2001-11-20 | Bristol Myers Squibb Co | Tetrahydroisoquinoline analogs useful as growth hormone secretagogues |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| 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 |
| WO2003016248A2 (en) | 2001-08-17 | 2003-02-27 | Bristol-Myers Squibb Company Patent Department | Bicyclic hydroxamates as inhibitors of matrix metalloproteinases and/or tnf-$g(a) converting enzyme (tace) |
| BRPI0212726B8 (pt) | 2001-09-21 | 2021-05-25 | Bristol Myers Squibb Co | compostos contendo lactamas, e derivados dos mesmos, composição farmacêutica que os compreende e seus usos |
| US6649606B1 (en) * | 2001-11-09 | 2003-11-18 | Bristol-Myers Squibb Co. | Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity |
| GB0206033D0 (en) | 2002-03-14 | 2002-04-24 | Pfizer Ltd | Compounds useful in therapy |
| 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 |
| AU2004263508A1 (en) * | 2003-08-08 | 2005-02-17 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions, and methods of use |
| 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 |
| EA200700225A1 (ru) | 2004-07-12 | 2008-02-28 | Айдан Фармасьютикалз, Инк. | Аналоги тетрапептида |
| US7459564B2 (en) | 2005-01-13 | 2008-12-02 | 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 |
| BRPI0612621B8 (pt) | 2005-06-17 | 2017-03-21 | Basf Ag | processo para produzir compostos químicos, e, composto |
| WO2007054453A2 (en) | 2005-11-11 | 2007-05-18 | F. Hoffmann-La Roche Ag | Carbocyclic fused cyclic amines as inhibitors of the coagulation factor xa |
| EP1966141A1 (en) | 2005-12-14 | 2008-09-10 | Brystol-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 |
| EP1981854B1 (en) | 2005-12-14 | 2011-06-01 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| AU2007288253B2 (en) | 2006-08-23 | 2013-05-02 | Xenon Pharmaceuticals Inc. | Derivatives of 4-(N-azacycloalkyl) anilides as potassium channel modulators |
| EP2102189B1 (en) | 2006-12-15 | 2015-07-29 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| AU2008266228A1 (en) | 2007-06-13 | 2008-12-24 | Bristol-Myers Squibb Company | Dipeptide analogs as coagulation factor inhibitors |
| KR20100027159A (ko) | 2007-06-28 | 2010-03-10 | 노파르티스 아게 | 칼리크레인 7 조절제 |
| JP5537442B2 (ja) | 2008-03-13 | 2014-07-02 | 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ピリダジン誘導体 |
| WO2010151317A1 (en) | 2009-06-22 | 2010-12-29 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| WO2011002520A2 (en) | 2009-07-02 | 2011-01-06 | Angion Biomedica Corp. | Small molecule inhibitors of parp activity |
| WO2011017296A1 (en) | 2009-08-04 | 2011-02-10 | Schering Corporation | 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
| ES2822130T3 (es) | 2010-02-11 | 2021-04-29 | Bristol Myers Squibb Co | Macrociclos como inhibidores del factor XIa |
| US9161924B2 (en) | 2011-07-08 | 2015-10-20 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
| 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 |
| IN2014CN02806A (enExample) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| EA023649B1 (ru) | 2011-10-14 | 2016-06-30 | Бристол-Майерс Сквибб Кампани | ЗАМЕЩЕННЫЕ СОЕДИНЕНИЯ ТЕТРАГИДРОИЗОХИНОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa |
| ES2579832T3 (es) | 2011-10-14 | 2016-08-17 | Bristol-Myers Squibb Company | Compuestos de tetrahidroisoquinolina sustituida como inhibidores del factor XIa |
| CN104136431B (zh) | 2011-12-21 | 2017-03-15 | 小野药品工业株式会社 | 作为凝血因子XIa抑制剂的吡啶酮和嘧啶酮衍生物 |
| US20140378474A1 (en) | 2012-01-27 | 2014-12-25 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| US20140350034A1 (en) | 2012-01-27 | 2014-11-27 | Novartis Ag | Aminopyridine derivatives as plasma kallikrein inhibitors |
| JP2015083542A (ja) | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | ３位置換プロリン誘導体 |
| NZ701121A (en) | 2012-05-10 | 2017-06-30 | Bayer Pharma AG | Antibodies capable of binding to the coagulation factor xi and/or its activated form factor xia and uses thereof |
| JP6220786B2 (ja) | 2012-07-19 | 2017-10-25 | 大日本住友製薬株式会社 | １−（シクロアルキルカルボニル）プロリン誘導体 |
| HUE032622T2 (en) | 2012-08-03 | 2017-10-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| CA2880898A1 (en) | 2012-08-03 | 2014-02-06 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor xia inhibitors |
-
2012
- 2012-10-12 IN IN2806CHN2014 patent/IN2014CN02806A/en unknown
- 2012-10-12 EP EP12778912.1A patent/EP2766345B1/en not_active Not-in-force
- 2012-10-12 EP EP14195397.6A patent/EP2899183B1/en not_active Not-in-force
- 2012-10-12 ES ES14195397T patent/ES2699226T3/es active Active
- 2012-10-12 WO PCT/US2012/059859 patent/WO2013055984A1/en not_active Ceased
- 2012-10-12 US US14/350,417 patent/US9108951B2/en active Active
- 2012-10-12 JP JP2014535894A patent/JP6033317B2/ja not_active Expired - Fee Related
- 2012-10-12 CN CN201280061670.3A patent/CN103987697B/zh not_active Expired - Fee Related
- 2012-10-12 ES ES12778912.1T patent/ES2572908T3/es active Active
-
2015
- 2015-07-15 US US14/799,681 patent/US9394276B2/en active Active
-
2016
- 2016-06-15 US US15/183,051 patent/US9725435B2/en active Active
-
2017
- 2017-07-07 US US15/643,891 patent/US10000466B2/en active Active
-
2018
- 2018-05-17 US US15/982,038 patent/US10906886B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US9725435B2 (en) | 2017-08-08 |
| US20180265494A1 (en) | 2018-09-20 |
| ES2699226T3 (es) | 2019-02-08 |
| EP2899183A1 (en) | 2015-07-29 |
| CN103987697B (zh) | 2017-04-26 |
| EP2766345A1 (en) | 2014-08-20 |
| US20140275061A1 (en) | 2014-09-18 |
| US9394276B2 (en) | 2016-07-19 |
| EP2766345B1 (en) | 2016-03-16 |
| US10000466B2 (en) | 2018-06-19 |
| US20170305880A1 (en) | 2017-10-26 |
| EP2899183B1 (en) | 2018-09-19 |
| IN2014CN02806A (enExample) | 2015-07-03 |
| WO2013055984A1 (en) | 2013-04-18 |
| US20150315200A1 (en) | 2015-11-05 |
| CN103987697A (zh) | 2014-08-13 |
| ES2572908T3 (es) | 2016-06-03 |
| US10906886B2 (en) | 2021-02-02 |
| JP2014528479A (ja) | 2014-10-27 |
| US9108951B2 (en) | 2015-08-18 |
| US20160289209A1 (en) | 2016-10-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6033317B2 (ja) | 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 | |
| JP6479763B2 (ja) | 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン | |
| JP6033319B2 (ja) | 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 | |
| EP3331872B1 (en) | Novel substituted glycine derived fxia inhibitors | |
| JP6082463B2 (ja) | 第ｘｉａ因子阻害剤としてのジヒドロピリドンｐ１ | |
| JP5537442B2 (ja) | 第ｘｉａ因子阻害剤としてのピリダジン誘導体 | |
| JP6742348B2 (ja) | 第ｘｉａ因子阻害剤としてのジアミド大員環 | |
| 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 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20151009 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20151009 |
|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7424 Effective date: 20160219 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20160524 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20160526 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160824 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20160927 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20161025 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6033317 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |