JP6033318B2 - 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
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- JP6033318B2 JP6033318B2 JP2014535916A JP2014535916A JP6033318B2 JP 6033318 B2 JP6033318 B2 JP 6033318B2 JP 2014535916 A JP2014535916 A JP 2014535916A JP 2014535916 A JP2014535916 A JP 2014535916A JP 6033318 B2 JP6033318 B2 JP 6033318B2
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- alkyl
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- alkylene
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- Expired - Fee Related
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- 0 C*(C(C(*(C(C)(C)C1)C(C=Cc2c(*)c(N)ccc2*2*=**=C2)=O)c2c1c(OCCC1CC*(C)CC1)ccc2)=O)c(cc1)ccc1C(OC)=O Chemical compound C*(C(C(*(C(C)(C)C1)C(C=Cc2c(*)c(N)ccc2*2*=**=C2)=O)c2c1c(OCCC1CC*(C)CC1)ccc2)=O)c(cc1)ccc1C(OC)=O 0.000 description 5
- VIOVOUIITBRXPV-SDNWHVSQSA-N CC(C)(C)OC(c(cc1)ccc1NC(C(c1c(CC2)c(OC3CCNCC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)=O)=O Chemical compound CC(C)(C)OC(c(cc1)ccc1NC(C(c1c(CC2)c(OC3CCNCC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)=O)=O VIOVOUIITBRXPV-SDNWHVSQSA-N 0.000 description 1
- DXEKUOPRXKPOFL-IRFPIXQFSA-N CC(C)(Cc(c([C@@H]1C(Nc(cc2)ccc2C(O)=O)=O)ccc2)c2-c(cc2)ccc2C(NC)=O)N1C(/C=C/c(c(-[n]1nnnc1)ccc1C)c1F)=O Chemical compound CC(C)(Cc(c([C@@H]1C(Nc(cc2)ccc2C(O)=O)=O)ccc2)c2-c(cc2)ccc2C(NC)=O)N1C(/C=C/c(c(-[n]1nnnc1)ccc1C)c1F)=O DXEKUOPRXKPOFL-IRFPIXQFSA-N 0.000 description 1
- AAGUCZQYYJDCSS-DTQAZKPQSA-N CCOC(c(cc1)ccc1NC(C(c1c(CC2(C)C)c(OCCC3CCN(C)CC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)=O)=O Chemical compound CCOC(c(cc1)ccc1NC(C(c1c(CC2(C)C)c(OCCC3CCN(C)CC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)=O)=O AAGUCZQYYJDCSS-DTQAZKPQSA-N 0.000 description 1
- RVFZCMYFXWGUAI-BZASRWHJSA-N CCOC(c(cc1)ccc1NC([C@@H](c1c(CC2)c(OCCC3CCNCC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)=O)=O Chemical compound CCOC(c(cc1)ccc1NC([C@@H](c1c(CC2)c(OCCC3CCNCC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)=O)=O RVFZCMYFXWGUAI-BZASRWHJSA-N 0.000 description 1
- MVQLGVFFPDIDOJ-FMIVXFBMSA-N COCCOc1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O Chemical compound COCCOc1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O MVQLGVFFPDIDOJ-FMIVXFBMSA-N 0.000 description 1
- CHQVZXAMVUFZTQ-FMIVXFBMSA-N CS(Nc1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)(=O)=O Chemical compound CS(Nc1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)(=O)=O CHQVZXAMVUFZTQ-FMIVXFBMSA-N 0.000 description 1
- IDOUIARWFOIWND-FMIVXFBMSA-N C[n]1ncc(-c2cccc(C3C(Nc(cc4)ccc4C(O)=O)=O)c2CCN3C(/C=C/c(c(-[n]2nnnc2)ccc2Cl)c2F)=O)c1 Chemical compound C[n]1ncc(-c2cccc(C3C(Nc(cc4)ccc4C(O)=O)=O)c2CCN3C(/C=C/c(c(-[n]2nnnc2)ccc2Cl)c2F)=O)c1 IDOUIARWFOIWND-FMIVXFBMSA-N 0.000 description 1
- QAIXYZBKMZTGRR-MHWRWJLKSA-N Cc(cc1)cc(CCC2)c1N2C(c1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O Chemical compound Cc(cc1)cc(CCC2)c1N2C(c1cccc(C2C(Nc(cc3)ccc3C(O)=O)=O)c1CCN2C(/C=C/c1cc(Cl)ccc1-[n]1nnnc1)=O)=O QAIXYZBKMZTGRR-MHWRWJLKSA-N 0.000 description 1
- WIGOOWKEZSCAOK-DHZHZOJOSA-N O=C(C(c1c(CC2)c(OCCC3CCNCC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)Nc(cc1)ccc1F Chemical compound O=C(C(c1c(CC2)c(OCCC3CCNCC3)ccc1)N2C(/C=C/c(c(-[n]1nnnc1)ccc1Cl)c1F)=O)Nc(cc1)ccc1F WIGOOWKEZSCAOK-DHZHZOJOSA-N 0.000 description 1
- HNFKHNIOGMFEJR-UHFFFAOYSA-N O=C(CCc1cc(Cl)ccc1-[n]1nnnc1)ON(C(CC1)=O)C1=O Chemical compound O=C(CCc1cc(Cl)ccc1-[n]1nnnc1)ON(C(CC1)=O)C1=O HNFKHNIOGMFEJR-UHFFFAOYSA-N 0.000 description 1
- CHRACTNYZGBMOH-DAFODLJHSA-N OC(/C=C/c1cc(Cl)ccc1OC(F)F)=O Chemical compound OC(/C=C/c1cc(Cl)ccc1OC(F)F)=O CHRACTNYZGBMOH-DAFODLJHSA-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
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- 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)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161547301P | 2011-10-14 | 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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2014530240A JP2014530240A (ja) | 2014-11-17 |
| JP2014530240A5 JP2014530240A5 (cg-RX-API-DMAC7.html) | 2015-12-03 |
| JP6033318B2 true JP6033318B2 (ja) | 2016-11-30 |
Family
ID=47116434
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014535916A Expired - Fee Related JP6033318B2 (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 (1) | US9079929B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2766347B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6033318B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN103987696B (cg-RX-API-DMAC7.html) |
| ES (1) | ES2579832T3 (cg-RX-API-DMAC7.html) |
| IN (1) | IN2014CN02805A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2013056034A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI577665B (zh) | 2010-02-11 | 2017-04-11 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之巨環類 |
| 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 |
| WO2013056034A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| RS56168B1 (sr) | 2011-10-14 | 2017-11-30 | Bristol Myers Squibb Co | Supstituisana jedinjenja tetrahidroizohinolina kao inhibitori xia faktora |
| EP2766345B1 (en) | 2011-10-14 | 2016-03-16 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| TW201416362A (zh) | 2012-07-19 | 2014-05-01 | Dainippon Sumitomo Pharma Co | １－（環烷基羰基）脯胺酸衍生物 |
| US9376444B2 (en) | 2012-08-03 | 2016-06-28 | Bristol-Myers Squibb Company | Dihydropyridone P1 as factor XIa inhibitors |
| BR112015002081A2 (pt) | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona p1 como inibidores de fator xia |
| WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| AU2013329125B2 (en) | 2012-10-12 | 2017-03-30 | Bristol-Myers Squibb Company | Crystalline forms of a factor XIa inhibitor |
| PL2964023T3 (pl) * | 2013-03-05 | 2020-01-31 | Bayer Cropscience Aktiengesellschaft | Zastosowanie n-(2-metoksybenzoilo)- 4-[(metyloaminokarbonylo)amino]benzenosulfonamidu w kombinacji ze środkiem owadobójczym lub fungicydem dla zwiększenia plonów roślin |
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| WO2015054087A1 (en) * | 2013-10-07 | 2015-04-16 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| SG10201908467RA (en) | 2014-01-31 | 2019-10-30 | Bristol Myers Squibb Co | Macrocycles with hetrocyclic p2' groups as factor xia inhibitors |
| NO2760821T3 (cg-RX-API-DMAC7.html) | 2014-01-31 | 2018-03-10 | ||
| WO2015123091A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| WO2015123093A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3134408B1 (en) | 2014-04-22 | 2020-08-12 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| GEP20196942B (en) | 2014-07-01 | 2019-02-11 | Pharmaceutical Company Limited Takeda | Heterocyclic compounds and their use as retinoidrelated orphan receptor (ror) gamma-t inhibitors |
| EP3180317B1 (en) | 2014-07-28 | 2021-04-14 | 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 |
| WO2016046166A1 (de) * | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| EP3197880B1 (de) | 2014-09-24 | 2018-10-24 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate mit anti-inflammatorischer und anti-thrombotischer wirkung |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| US10160750B2 (en) | 2015-06-19 | 2018-12-25 | Bristol-Myers Squibb Company | Diamide macrocycles as factor XIa inhibitors |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| KR102086934B1 (ko) | 2015-07-29 | 2020-03-09 | 브리스톨-마이어스 스큅 컴퍼니 | 알킬 또는 시클로알킬 P2' 모이어티를 갖는 인자 XIa 마크로시클릭 억제제 |
| EP3328852B1 (en) | 2015-07-29 | 2021-04-28 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group |
| US10336730B2 (en) | 2015-08-05 | 2019-07-02 | Bristol-Myers Squibb Company | Substituted glycine derived FXIA inhibitors |
| MX387515B (es) | 2015-10-29 | 2025-03-18 | Merck Sharp & Dohme Llc | Inhibidores de factor xia. |
| 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 |
| KR101894004B1 (ko) * | 2016-03-17 | 2018-08-31 | 연세대학교 산학협력단 | NamPT 억제용 신규 화합물 및 이를 포함하는 조성물 |
| TW201808908A (zh) | 2016-08-22 | 2018-03-16 | 美商默沙東藥廠 | 因子XIa抑制劑 |
| HUE057289T2 (hu) | 2016-08-31 | 2022-05-28 | Jiangsu Hengrui Medicine Co | Oxopikolinamid-származék, annak elõállítási módszere és gyógyszerészeti felhasználása |
| 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 |
| WO2019184744A1 (zh) * | 2018-03-28 | 2019-10-03 | 四川科伦博泰生物医药股份有限公司 | 四氢异喹啉类衍生物及其制备方法和用途 |
| EP3976027B1 (en) * | 2019-05-30 | 2025-11-05 | Merck Sharp & Dohme LLC | Quinoline derivatives as factor xi activation inhibitors |
| EP4125892A4 (en) * | 2020-04-01 | 2024-04-03 | Merck Sharp & Dohme LLC | Factor xi activation inhibitors |
| EP4149917B1 (en) * | 2020-05-12 | 2025-07-30 | Merck Sharp & Dohme LLC | 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 |
Family Cites Families (62)
| 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 |
| 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 |
| WO1996034010A2 (en) | 1995-03-29 | 1996-10-31 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5624936A (en) | 1995-03-29 | 1997-04-29 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| AU717298B2 (en) | 1996-04-03 | 2000-03-23 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5869682A (en) | 1996-04-03 | 1999-02-09 | 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. |
| RU2274642C2 (ru) | 1998-03-19 | 2006-04-20 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы каспаз |
| 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) |
| JP2002534420A (ja) | 1999-01-02 | 2002-10-15 | アベンティス・ファーマ・ドイチユラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 新規なマロン酸誘導体、その調製方法、その使用およびそれを含有する医薬組成物（Ｘａ因子活性阻害） |
| HK1045846A1 (zh) | 1999-04-09 | 2002-12-13 | 巴斯福股份公司 | 低分子量补体蛋白酶抑制剂 |
| 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 |
| EP1125925A1 (en) | 2000-02-15 | 2001-08-22 | Applied Research Systems ARS Holding N.V. | Amine derivatives for the treatment of apoptosis |
| ATE310728T1 (de) | 2000-05-11 | 2005-12-15 | Bristol Myers Squibb Co | Tetrahydroisochinolin-analoga als wachstumshormon-sekretagoga |
| 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 |
| KR100909141B1 (ko) | 2001-09-21 | 2009-07-23 | 브리스톨-마이어스스퀴브컴파니 | 인자 Ｘａ 억제제로서의 락탐-함유 화합물 및 그의 유도체 |
| AU2002357692A1 (en) * | 2001-11-09 | 2003-05-26 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity |
| 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 |
| US7208601B2 (en) * | 2003-08-08 | 2007-04-24 | Mjalli Adnan M M | Aryl and heteroaryl compounds, compositions, and methods of use |
| EP1660439A2 (en) * | 2003-08-08 | 2006-05-31 | 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 |
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered 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 |
| 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 |
| US20060183771A1 (en) | 2005-02-17 | 2006-08-17 | Seiffert Dietmar A | Novel combination of selective factor VIIa and/or factor XIa inhibitors and selective plasma kallikrein inhibitors |
| CN101198591B (zh) | 2005-06-17 | 2011-06-22 | 巴斯福股份公司 | 制备漂白促进剂的方法 |
| KR20080087817A (ko) | 2005-12-14 | 2008-10-01 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 ｘｉａ 억제제로서 아릴프로피온아미드,아릴아크릴아미드, 아릴프로핀아미드 또는 아릴메틸우레아유사체 |
| US8466295B2 (en) | 2005-12-14 | 2013-06-18 | Bristol-Myers Squibb Company | Thiophene derivatives as factor XIa inhibitors |
| WO2007070818A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| PL2061465T3 (pl) | 2006-08-23 | 2014-03-31 | Valeant Pharmaceuticals Int | Pochodne 4-(N-azacykloalkilo) anilidów jako modulatory kanałów potasowych |
| EP2102189B1 (en) | 2006-12-15 | 2015-07-29 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| CL2008001724A1 (es) | 2007-06-13 | 2008-08-08 | Bristol Myers Squibb Co | Compuestos derivados de analogos dipeptidos, inhibidores del factor de coagulacion; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de un trastorno tromboembolico, infarto de miocardio, trombosis, ate |
| CN102026996B (zh) | 2008-03-13 | 2015-01-07 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的哒嗪衍生物 |
| US8624040B2 (en) | 2009-06-22 | 2014-01-07 | 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 |
| TWI393716B (zh) | 2009-08-04 | 2013-04-21 | Merck Sharp & Dohme | 作為ｉｘａ因子抑制劑之雜環化合物 |
| TWI577665B (zh) | 2010-02-11 | 2017-04-11 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之巨環類 |
| EP2729150B1 (en) | 2011-07-08 | 2016-09-14 | 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 |
| EP2766345B1 (en) | 2011-10-14 | 2016-03-16 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2013056034A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| RS56168B1 (sr) | 2011-10-14 | 2017-11-30 | Bristol Myers Squibb Co | Supstituisana jedinjenja tetrahidroizohinolina kao inhibitori xia faktora |
| KR102011534B1 (ko) | 2011-12-21 | 2019-08-16 | 오노 야꾸힝 고교 가부시키가이샤 | 인자 ＸＩａ 억제제로서 피리디논 및 피리미디논 유도체 |
| EP2807156A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | Aminopyridine derivatives as plasma kallikrein inhibitors |
| WO2013111108A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | 5-membered heteroarylcarboxamide 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 |
| WO2013167669A1 (en) | 2012-05-10 | 2013-11-14 | Bayer Pharma Aktiengesellschaft | Antibodies capable of binding to the coagulation factor xi and/or its activated form factor xia and uses thereof |
| TW201416362A (zh) | 2012-07-19 | 2014-05-01 | Dainippon Sumitomo Pharma Co | １－（環烷基羰基）脯胺酸衍生物 |
| US9376444B2 (en) | 2012-08-03 | 2016-06-28 | Bristol-Myers Squibb Company | Dihydropyridone P1 as factor XIa inhibitors |
| BR112015002081A2 (pt) | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona p1 como inibidores de fator xia |
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- 2012-10-12 ES ES12780357.5T patent/ES2579832T3/es active Active
- 2012-10-12 US US14/350,411 patent/US9079929B2/en active Active
- 2012-10-12 JP JP2014535916A patent/JP6033318B2/ja not_active Expired - Fee Related
- 2012-10-12 EP EP12780357.5A patent/EP2766347B1/en not_active Not-in-force
- 2012-10-12 CN CN201280061628.1A patent/CN103987696B/zh not_active Expired - Fee Related
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|---|---|
| US9079929B2 (en) | 2015-07-14 |
| ES2579832T3 (es) | 2016-08-17 |
| CN103987696B (zh) | 2016-12-21 |
| IN2014CN02805A (cg-RX-API-DMAC7.html) | 2015-07-03 |
| JP2014530240A (ja) | 2014-11-17 |
| EP2766347A1 (en) | 2014-08-20 |
| EP2766347B1 (en) | 2016-05-04 |
| WO2013056034A1 (en) | 2013-04-18 |
| CN103987696A (zh) | 2014-08-13 |
| US20140274960A1 (en) | 2014-09-18 |
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