CN103987696B - 作为因子xia抑制剂的取代的四氢异喹啉化合物 - Google Patents
作为因子xia抑制剂的取代的四氢异喹啉化合物 Download PDFInfo
- Publication number
- CN103987696B CN103987696B CN201280061628.1A CN201280061628A CN103987696B CN 103987696 B CN103987696 B CN 103987696B CN 201280061628 A CN201280061628 A CN 201280061628A CN 103987696 B CN103987696 B CN 103987696B
- Authority
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- China
- Prior art keywords
- alkyl
- occurrence
- substituted
- conh
- phenyl
- 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 CC(C([C@](C1F)C=CC(O)=O)=CC=C1Cl)=* Chemical compound CC(C([C@](C1F)C=CC(O)=O)=CC=C1Cl)=* 0.000 description 7
- JZDAEMFHMRJBET-SFQUDFHCSA-N CC(C)(C1)C(C(c(cc2)ccc2C(N)=O)=CCC2)=C2C(C(Nc(cc2)ccc2C(O)=O)=O)N1C(/C=C/C(C(C=C1)[n]2nnnc2)C=C1Cl)=O Chemical compound CC(C)(C1)C(C(c(cc2)ccc2C(N)=O)=CCC2)=C2C(C(Nc(cc2)ccc2C(O)=O)=O)N1C(/C=C/C(C(C=C1)[n]2nnnc2)C=C1Cl)=O JZDAEMFHMRJBET-SFQUDFHCSA-N 0.000 description 1
- JBGIHUBDSGFFHF-FBMGVBCBSA-N CC(c(c(/C=C/C(N(CC1)C(C(Nc(cc2)ccc2C(O)=O)=O)c2c1c(-c(cc1)ccc1C(NCCN(C)C)=O)ccc2)=O)c1F)ccc1Cl)=O Chemical compound CC(c(c(/C=C/C(N(CC1)C(C(Nc(cc2)ccc2C(O)=O)=O)c2c1c(-c(cc1)ccc1C(NCCN(C)C)=O)ccc2)=O)c1F)ccc1Cl)=O JBGIHUBDSGFFHF-FBMGVBCBSA-N 0.000 description 1
- JLSSWDFCYXSLQX-UHFFFAOYSA-N CCOC(c(cc1)ccc1C#N)=O Chemical compound CCOC(c(cc1)ccc1C#N)=O JLSSWDFCYXSLQX-UHFFFAOYSA-N 0.000 description 1
- WYSMEGUVKCVXQV-MDWZMJQESA-N CN(C)c1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c(cc(cc1)Cl)c1-[n]1nnnc1)=O Chemical compound CN(C)c1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c(cc(cc1)Cl)c1-[n]1nnnc1)=O WYSMEGUVKCVXQV-MDWZMJQESA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6524—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- C07D401/10—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
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161547301P | 2011-10-14 | 2011-10-14 | |
| US61/547301 | 2011-10-14 | ||
| US61/547,301 | 2011-10-14 | ||
| PCT/US2012/059932 WO2013056034A1 (en) | 2011-10-14 | 2012-10-12 | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103987696A CN103987696A (zh) | 2014-08-13 |
| CN103987696B true CN103987696B (zh) | 2016-12-21 |
Family
ID=47116434
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280061628.1A Expired - Fee Related CN103987696B (zh) | 2011-10-14 | 2012-10-12 | 作为因子xia抑制剂的取代的四氢异喹啉化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9079929B2 (OSRAM) |
| EP (1) | EP2766347B1 (OSRAM) |
| JP (1) | JP6033318B2 (OSRAM) |
| CN (1) | CN103987696B (OSRAM) |
| ES (1) | ES2579832T3 (OSRAM) |
| IN (1) | IN2014CN02805A (OSRAM) |
| WO (1) | WO2013056034A1 (OSRAM) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102753555B (zh) | 2010-02-11 | 2018-01-12 | 百时美施贵宝公司 | 作为因子xia抑制剂的大环类 |
| 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 |
| EP3309148A1 (en) | 2011-10-14 | 2018-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| 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 |
| EA028581B1 (ru) | 2012-08-03 | 2017-12-29 | Бристол-Маерс Сквибб Компани | ДИГИДРОПИРИДОН Р1 В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa |
| UY34959A (es) | 2012-08-03 | 2014-01-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Dihidropiridona p1 como inhibidores del factor xia |
| DK2906551T3 (en) | 2012-10-12 | 2018-05-22 | Bristol Myers Squibb Co | CRYSTALLIC FORMS OF A FACTOR XIA INHIBITOR |
| WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2906541B1 (en) * | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| HUE045111T2 (hu) * | 2013-03-05 | 2019-12-30 | Bayer Cropscience Ag | N-(2-metoxibenzil)-4-[(metilaminokarbonil)amino]benzolszulfonamid inszekticidekkel vagy fungicidekkel képzett kombinációjának alkalmazása növénytermesztés hatásfokának növelésére |
| US9738655B2 (en) | 2013-03-25 | 2017-08-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors |
| WO2015054087A1 (en) | 2013-10-07 | 2015-04-16 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| UY40230A (es) | 2014-01-31 | 2023-08-15 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Macrociclos con grupos P2’ heterocíclicos como inhibidores del factor XIa y composiciones farmacéuticas que los comprenden |
| NO2760821T3 (OSRAM) | 2014-01-31 | 2018-03-10 | ||
| WO2015123091A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3104703B1 (en) | 2014-02-11 | 2020-11-18 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| US10093683B2 (en) | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| 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. |
| WO2016015593A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| ES2714283T3 (es) | 2014-09-04 | 2019-05-28 | Bristol Myers Squibb Co | Macrociclos de diamida que son inhibidores de FXIa |
| US10167280B2 (en) | 2014-09-24 | 2019-01-01 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| WO2016046159A1 (de) * | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| EP3310777B1 (en) | 2015-06-19 | 2019-10-09 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| US10676477B2 (en) | 2015-07-29 | 2020-06-09 | Bristol-Myers Squibb Company | Factor XIa macrocycle 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 |
| WO2017023992A1 (en) | 2015-08-05 | 2017-02-09 | Bristol-Myers Squibb Company | Novel substituted glycine derived fxia inhibitors |
| US10214512B2 (en) | 2015-10-29 | 2019-02-26 | Merck Sharp & Dohme Corp. | Factor XIA inhibitors |
| 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 |
| WO2017123518A1 (en) * | 2016-01-11 | 2017-07-20 | The Rockefeller University | Aminotriazole immunomodulators for treating autoimmune diseases |
| KR102382188B1 (ko) * | 2016-03-17 | 2022-04-05 | 주식회사 체크메이트테라퓨틱스 | NamPT 억제용 신규 화합물 및 이를 포함하는 조성물 |
| EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| PT3486242T (pt) | 2016-08-31 | 2022-01-06 | Jiangsu Hengrui Medicine Co | Derivado de oxopicolinamida, método de preparação para esse fim e utilização farmacêutica do mesmo |
| 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 |
| US11541049B2 (en) | 2018-03-28 | 2023-01-03 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Tetrahydroisoquinoline derivatives, preparation process and use thereof |
| EP3976027B1 (en) * | 2019-05-30 | 2025-11-05 | Merck Sharp & Dohme LLC | Quinoline derivatives as factor xi activation inhibitors |
| US12492187B2 (en) | 2020-04-01 | 2025-12-09 | Merck Sharp & Dohme Llc | Factor XI activation inhibitors |
| WO2021231191A1 (en) * | 2020-05-12 | 2021-11-18 | Merck Sharp & Dohme Corp. | Factor xi activation inhibitors |
| EP3978487A1 (en) | 2020-09-30 | 2022-04-06 | Origo Biopharma, S.L. | 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 |
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| WO2003041641A2 (en) * | 2001-11-09 | 2003-05-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity |
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- 2012-10-12 IN IN2805CHN2014 patent/IN2014CN02805A/en unknown
- 2012-10-12 CN CN201280061628.1A patent/CN103987696B/zh not_active Expired - Fee Related
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Also Published As
| Publication number | Publication date |
|---|---|
| JP6033318B2 (ja) | 2016-11-30 |
| EP2766347A1 (en) | 2014-08-20 |
| ES2579832T3 (es) | 2016-08-17 |
| CN103987696A (zh) | 2014-08-13 |
| US20140274960A1 (en) | 2014-09-18 |
| US9079929B2 (en) | 2015-07-14 |
| IN2014CN02805A (OSRAM) | 2015-07-03 |
| JP2014530240A (ja) | 2014-11-17 |
| EP2766347B1 (en) | 2016-05-04 |
| WO2013056034A1 (en) | 2013-04-18 |
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