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
- conh
- compound
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- 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
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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
-
- 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)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Hematology (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 (enExample) | 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 (enExample) |
| EP (1) | EP2766347B1 (enExample) |
| JP (1) | JP6033318B2 (enExample) |
| CN (1) | CN103987696B (enExample) |
| ES (1) | ES2579832T3 (enExample) |
| IN (1) | IN2014CN02805A (enExample) |
| WO (1) | WO2013056034A1 (enExample) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2534152B1 (en) | 2010-02-11 | 2018-05-02 | 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 |
| ES2699226T3 (es) | 2011-10-14 | 2019-02-08 | Bristol Myers Squibb Co | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
| CN103974938B (zh) | 2011-10-14 | 2016-11-09 | 百时美施贵宝公司 | 作为因子xia抑制剂的经取代的四氢异喹啉化合物 |
| IN2014CN02805A (enExample) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| AU2013291098A1 (en) | 2012-07-19 | 2015-02-05 | Sumitomo Dainippon Pharma Co., Ltd. | 1-(cycloalkyl-carbonyl)proline derivative |
| SG11201500270RA (en) | 2012-08-03 | 2015-03-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| US9409908B2 (en) | 2012-08-03 | 2016-08-09 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor XIa inhibitors |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| JP6154473B2 (ja) | 2012-10-12 | 2017-06-28 | 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因子阻害剤の結晶形 |
| WO2014059214A1 (en) * | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| ES2748350T3 (es) * | 2013-03-05 | 2020-03-16 | Bayer Cropscience Ag | Uso de N-(2-metoxibenzoil)-4-[metilaminocarbonil)amino]bencenosulfonamida en combinación con un insecticida o fungicida para mejorar el rendimiento en plantas |
| ES2712699T3 (es) * | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| EP3054944B1 (en) | 2013-10-07 | 2019-12-04 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| TWI688564B (zh) | 2014-01-31 | 2020-03-21 | 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 |
| US9676723B2 (en) | 2014-02-11 | 2017-06-13 | Merck Sharp & Dohme Corp | Factor XIa inhibitors |
| US9944643B2 (en) | 2014-02-11 | 2018-04-17 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| EP3134408B1 (en) | 2014-04-22 | 2020-08-12 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| TN2016000567A1 (en) | 2014-07-01 | 2018-04-04 | Takeda Pharmaceuticals Co | Heterocyclic compounds and their use as retinoid-related orphan receptor (ror) gamma-t inhibitors |
| US9868727B2 (en) | 2014-07-28 | 2018-01-16 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| WO2016036893A1 (en) | 2014-09-04 | 2016-03-10 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
| EP3197872B1 (de) | 2014-09-24 | 2019-01-30 | Bayer Pharma Aktiengesellschaft | (2h)-2-oxopyridine als faktor xia-inhibitoren zur behandlung von thrombotischen erkrankungen |
| 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 |
| ES2762987T3 (es) | 2015-06-19 | 2020-05-26 | Bristol Myers Squibb Co | Macrociclos de diamida como inhibidores del factor XIA |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| ES2871111T3 (es) | 2015-07-29 | 2021-10-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático |
| KR102086934B1 (ko) | 2015-07-29 | 2020-03-09 | 브리스톨-마이어스 스큅 컴퍼니 | 알킬 또는 시클로알킬 P2' 모이어티를 갖는 인자 XIa 마크로시클릭 억제제 |
| JP6785838B2 (ja) * | 2015-08-05 | 2020-11-18 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 新規な置換グリシン誘導のｆｘｉａ阻害剤 |
| EP3371162B1 (en) | 2015-10-29 | 2022-01-26 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
| AU2016344476B2 (en) | 2015-10-29 | 2020-08-13 | Merck Sharp & Dohme Llc | Factor XIa inhibitors |
| WO2017123518A1 (en) * | 2016-01-11 | 2017-07-20 | The Rockefeller University | Aminotriazole immunomodulators for treating autoimmune diseases |
| CN108779104B (zh) * | 2016-03-17 | 2021-04-13 | 将军治疗有限公司 | 用于抑制烟酰胺磷酸核糖转移酶的新化合物和包含它的组合物 |
| WO2018039094A1 (en) | 2016-08-22 | 2018-03-01 | Merck Sharp & Dohme Corp. | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| 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 |
| US12304899B2 (en) | 2019-05-30 | 2025-05-20 | Merck Sharp & Dohme Llc | 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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| 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 |
| US5869682A (en) | 1996-04-03 | 1999-02-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| EP0891352A4 (en) | 1996-04-03 | 2001-08-16 | 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 |
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-
2012
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- 2012-10-12 JP JP2014535916A patent/JP6033318B2/ja not_active Expired - Fee Related
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- 2012-10-12 EP EP12780357.5A patent/EP2766347B1/en not_active Not-in-force
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- 2012-10-12 CN CN201280061628.1A patent/CN103987696B/zh not_active Expired - Fee Related
- 2012-10-12 WO PCT/US2012/059932 patent/WO2013056034A1/en not_active Ceased
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|---|---|
| EP2766347B1 (en) | 2016-05-04 |
| US20140274960A1 (en) | 2014-09-18 |
| ES2579832T3 (es) | 2016-08-17 |
| US9079929B2 (en) | 2015-07-14 |
| WO2013056034A1 (en) | 2013-04-18 |
| EP2766347A1 (en) | 2014-08-20 |
| CN103987696B (zh) | 2016-12-21 |
| JP2014530240A (ja) | 2014-11-17 |
| CN103987696A (zh) | 2014-08-13 |
| IN2014CN02805A (enExample) | 2015-07-03 |
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