JP2018538304A5 - - Google Patents
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- Publication number
- JP2018538304A5 JP2018538304A5 JP2018531333A JP2018531333A JP2018538304A5 JP 2018538304 A5 JP2018538304 A5 JP 2018538304A5 JP 2018531333 A JP2018531333 A JP 2018531333A JP 2018531333 A JP2018531333 A JP 2018531333A JP 2018538304 A5 JP2018538304 A5 JP 2018538304A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- independently
- alkyl
- cycloalkyl
- heterocyclyl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 78
- 125000000623 heterocyclic group Chemical group 0.000 claims 46
- 229910052801 chlorine Inorganic materials 0.000 claims 41
- 229910052731 fluorine Inorganic materials 0.000 claims 41
- 229910052794 bromium Inorganic materials 0.000 claims 29
- 229910052799 carbon Inorganic materials 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 25
- -1 CN Inorganic materials 0.000 claims 23
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 16
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 229910004013 NO 2 Inorganic materials 0.000 claims 11
- 125000004452 carbocyclyl group Chemical group 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 8
- 150000001721 carbon Chemical group 0.000 claims 8
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000004975 3-butenyl group Chemical group C(CC=C)* 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 3
- 206010019280 Heart failures Diseases 0.000 claims 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010049694 Left Ventricular Dysfunction Diseases 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 230000002107 myocardial effect Effects 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 238000007634 remodeling Methods 0.000 claims 2
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000003037 Diastolic Heart Failure Diseases 0.000 claims 1
- 206010061216 Infarction Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000008253 Systolic Heart Failure Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 238000007675 cardiac surgery Methods 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000018578 heart valve disease Diseases 0.000 claims 1
- 230000007574 infarction Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000002459 sustained effect Effects 0.000 claims 1
- 0 CC(N(C(O)=C1c2nnc(*)[o]2)C2=C/C=C\C=CC=C(*)C2)=NC1=* Chemical compound CC(N(C(O)=C1c2nnc(*)[o]2)C2=C/C=C\C=CC=C(*)C2)=NC1=* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562267997P | 2015-12-16 | 2015-12-16 | |
| US62/267,997 | 2015-12-16 | ||
| PCT/US2016/066750 WO2017106396A1 (en) | 2015-12-16 | 2016-12-15 | Heteroarylhydroxypyrimidinones as agonists of the apj receptor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018538304A JP2018538304A (ja) | 2018-12-27 |
| JP2018538304A5 true JP2018538304A5 (enExample) | 2020-01-30 |
| JP6948322B2 JP6948322B2 (ja) | 2021-10-13 |
Family
ID=57708840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018531333A Active JP6948322B2 (ja) | 2015-12-16 | 2016-12-15 | Ａｐｊ受容体のａｐｊアゴニストとしてのヘテロアリールヒドロキシピリミジノン |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US10669261B2 (enExample) |
| EP (1) | EP3390400B1 (enExample) |
| JP (1) | JP6948322B2 (enExample) |
| KR (1) | KR102742744B1 (enExample) |
| CN (1) | CN108602813B (enExample) |
| AR (1) | AR107061A1 (enExample) |
| AU (1) | AU2016372048B2 (enExample) |
| BR (1) | BR112018012112A2 (enExample) |
| CA (1) | CA3008630A1 (enExample) |
| CL (1) | CL2018001621A1 (enExample) |
| CO (1) | CO2018007221A2 (enExample) |
| EA (1) | EA036736B1 (enExample) |
| ES (1) | ES2854733T3 (enExample) |
| HK (1) | HK1255163A1 (enExample) |
| IL (1) | IL259947B (enExample) |
| MX (1) | MX380669B (enExample) |
| PE (1) | PE20181487A1 (enExample) |
| SG (1) | SG11201804674UA (enExample) |
| TW (1) | TW201725203A (enExample) |
| UY (1) | UY37026A (enExample) |
| WO (1) | WO2017106396A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3303330T3 (pl) | 2015-06-03 | 2019-10-31 | Bristol Myers Squibb Co | Agoniści 4 - hydroksy - 3 - ( heteroarylo ) pirydyno - 2 - onowi receptora apj do stosowania w leczeniu zaburzeń sercowo-naczyniowych |
| UY36949A (es) | 2015-10-14 | 2017-04-28 | Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware | 2,4-dihidroxi-nicotinamidas como agonistas de apj |
| EA037257B1 (ru) | 2015-12-04 | 2021-02-26 | Бристол-Маерс Сквибб Компани | Новые агонисты рецептора апелина и способы применения |
| MA55064A (fr) | 2015-12-16 | 2021-09-29 | Loxo Oncology Inc | Composés utilisés comme inhibiteurs de kinase |
| CN109195963B (zh) | 2016-03-24 | 2021-04-23 | 百时美施贵宝公司 | 作为apj激动剂的6-羟基-4-氧代-1，4-二氢嘧啶-5-甲酰胺 |
| EP3452466B1 (en) | 2016-05-03 | 2020-08-12 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| US10889565B2 (en) | 2016-06-14 | 2021-01-12 | Bristol-Myers Squibb Company | 4-hydroxy-3-sulfonylpyridin-2(1H)-ones as APJ receptor agonists |
| CN109311821B (zh) | 2016-06-14 | 2022-10-14 | 百时美施贵宝公司 | 作为apj激动剂的6-羟基-5-(苯基/杂芳基磺酰基)嘧啶-4(1h)-酮 |
| CN110072850B (zh) | 2016-10-14 | 2023-07-21 | 百时美施贵宝公司 | 3-磺酰基-5-氨基吡啶-2,4-二醇apj激动剂 |
| US11020395B2 (en) | 2016-11-16 | 2021-06-01 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the APJ receptor |
| US10736883B2 (en) | 2016-11-16 | 2020-08-11 | Amgen Inc. | Triazole furan compounds as agonists of the APJ receptor |
| US10689367B2 (en) | 2016-11-16 | 2020-06-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the APJ receptor |
| WO2018093579A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole phenyl compounds as agonists of the apj receptor |
| US11046680B1 (en) | 2016-11-16 | 2021-06-29 | Amgen Inc. | Heteroaryl-substituted triazoles as APJ receptor agonists |
| US11191762B2 (en) | 2016-11-16 | 2021-12-07 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the APJ Receptor |
| US11807624B2 (en) | 2018-05-01 | 2023-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the APJ receptor |
Family Cites Families (52)
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|---|---|---|---|---|
| GB2263639A (en) | 1992-01-28 | 1993-08-04 | Merck & Co Inc | Substituted pyrimidinones as neurotensin antagonists |
| US6174998B1 (en) | 1996-03-12 | 2001-01-16 | Roche Diagnostics Gmbh | C-nucleoside derivatives and their use in the detection of nucleic acids |
| JPH08311041A (ja) | 1995-03-16 | 1996-11-26 | Takeda Chem Ind Ltd | 複素環化合物およびその剤 |
| KR100579765B1 (ko) | 1996-07-01 | 2006-12-28 | 닥터 레디스 레보러터리즈 리미티드 | 신규헤테로고리형화합물의제조방법,이를함유하는약제조성물및당뇨병및이와관련된질병의치료에있어서그의용도 |
| US6369067B1 (en) | 1997-10-27 | 2002-04-09 | Dr. Reddy's Research Foundation | Monocyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them |
| HU229479B1 (en) * | 2000-02-16 | 2014-01-28 | Glaxo Group Ltd | Pyrimidine-4-one derivatives |
| CA2416248A1 (en) | 2000-07-18 | 2002-01-24 | Neurogen Corporation | 5-substituted 2-aryl-4-pyrimidinones |
| WO2002081454A1 (en) | 2001-04-09 | 2002-10-17 | Dr. Reddy's Laboratories Ltd. | Derivatives of aryl acids, their use in medicine, process for their preparation and pharmaceutical compositions containing them |
| WO2003094839A2 (en) | 2002-05-09 | 2003-11-20 | Cytokinetics, Inc. | Pyrimidinone compounds, compositions and methods |
| WO2003099211A2 (en) | 2002-05-23 | 2003-12-04 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| US20070167621A1 (en) | 2003-04-03 | 2007-07-19 | Pharmacia Corporation | Substituted pyrimidinones |
| EP1620428A1 (en) | 2003-04-23 | 2006-02-01 | Pharmacia & Upjohn Company LLC | Substituted pyrimidinones and pyrimidinthiones as crf antagonists |
| WO2005026148A1 (en) | 2003-09-08 | 2005-03-24 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| US20050197327A1 (en) | 2003-11-03 | 2005-09-08 | Gustave Bergnes | Compounds, compositions, and methods |
| US7625912B2 (en) | 2003-12-19 | 2009-12-01 | Merck & Co. Inc | Mitotic kinesin inhibitors |
| JP4517349B2 (ja) | 2004-07-28 | 2010-08-04 | 宇部興産株式会社 | ピリミジン−４−オン化合物の製造方法 |
| DE102005025315A1 (de) | 2005-06-02 | 2006-12-14 | Merck Patent Gmbh | Ionische Flüssigkeiten mit niedriger Viskosität |
| WO2007037543A1 (ja) | 2005-09-29 | 2007-04-05 | Banyu Pharmaceutical Co., Ltd. | ビアリールアミド誘導体 |
| EP1963329B1 (en) | 2005-11-30 | 2013-01-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-met and uses thereof |
| US8367845B2 (en) | 2006-04-21 | 2013-02-05 | The Trustees Of Boston University | Ionic viscoelastics and viscoelastic salts |
| WO2008052861A2 (de) | 2006-10-10 | 2008-05-08 | Proionic Production Of Ionic Substances Gmbh & Co Keg | Verfahren zur herstellung von 1,3 -hetero-aromatischen carbonaten |
| ES2527722T3 (es) | 2006-10-10 | 2015-01-28 | Proionic Gmbh & Co Kg | Método para reaccionar 2-carboxilatos 1,3-heteroaromáticos con agua |
| JP2010519204A (ja) | 2007-02-16 | 2010-06-03 | アムジエン・インコーポレーテツド | 窒素含有複素環ケトン類およびそれらのｃ−Ｍｅｔ阻害薬としての使用 |
| WO2009152902A2 (en) | 2008-05-28 | 2009-12-23 | Merck Patent Gmbh, | Ionic liquids |
| DE102008031480A1 (de) | 2008-07-03 | 2010-01-07 | Merck Patent Gmbh | Salze enthaltend ein Pyrimidincarbonsäure-Derivat |
| WO2010072696A2 (de) | 2008-12-22 | 2010-07-01 | Basf Se | Mischungen hydrophober und hydrophiler ionischer flüssigkeiten und ihre verwendung in flüssigkeitsringverdichtern |
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| US9212130B2 (en) | 2010-08-10 | 2015-12-15 | Shionogi & Co., Ltd. | Heterocyclic derivative and pharmaceutical composition comprising the same |
| CN103597646A (zh) | 2011-05-31 | 2014-02-19 | 默克专利股份有限公司 | 电解质组合物 |
| TWI567084B (zh) | 2011-05-31 | 2017-01-21 | 麥克專利有限公司 | 含有氫－三氰－硼酸根陰離子之化合物 |
| CN102903954B (zh) | 2011-07-25 | 2015-06-03 | 微宏动力系统（湖州）有限公司 | 含有离子液体电解质的锂离子二次电池 |
| DE102012006896A1 (de) | 2012-04-05 | 2013-10-10 | Merck Patent Gmbh | Silikate mit organischen Kationen |
| EP3409666A3 (en) | 2012-06-07 | 2019-01-02 | Georgia State University Research Foundation, Inc. | Seca inhibitors and methods of making and using thereof |
| CA2885272A1 (en) * | 2012-09-21 | 2014-03-27 | Sanofi | Benzoimidazole-carboxylic acid amide derivatives as apj receptor modulators |
| WO2014056844A1 (en) | 2012-10-10 | 2014-04-17 | Basf Se | Ionic liquids based on oxalic acid mono esters |
| DE102012021452A1 (de) | 2012-10-31 | 2014-04-30 | Merck Patent Gmbh | Salze mit Trihydroperfluoralkoxybutansulfonat- oder Trihydroperfluoralkoxypropansulfonat-Anion |
| US20150291596A1 (en) | 2012-11-16 | 2015-10-15 | Biocryst Pharmaceuticals, Inc. | Antiviral azasugar-containing nucleosides |
| WO2014207100A1 (en) | 2013-06-27 | 2014-12-31 | Basf Se | A process for coating paper with cellulose using a solution containing cellulose |
| DE102013016324A1 (de) | 2013-10-04 | 2015-04-09 | Merck Patent Gmbh | Perfluoralkylfluor- oder Perfluoralkylchlorgermanate |
| CA2930343C (en) | 2013-11-29 | 2021-06-08 | Proionic Gmbh | Method for curing an adhesive using microwave irradiation |
| KR101550846B1 (ko) | 2014-01-29 | 2015-09-07 | 한국과학기술연구원 | 단일공정을 이용한 탄소소재의 다원소 도핑방법 및 그 용도 |
| KR101531023B1 (ko) | 2014-05-27 | 2015-06-23 | 한국과학기술연구원 | 열분해 가스 도핑에 의한 고강도 고전도성 탄소나노튜브섬유의 제조방법 및 이에 따라 제조된 탄소나노튜브섬유 |
| US10570128B2 (en) * | 2014-05-28 | 2020-02-25 | Sanford Burnham Prebys Medical Discovery Institute | Agonists of the apelin receptor and methods of use thereof |
| MX387055B (es) * | 2014-06-06 | 2025-03-19 | Res Triangle Inst | Agonistas del receptor de apelina (apj) y usos de los mismos. |
| WO2016074757A1 (de) | 2014-11-11 | 2016-05-19 | Merck Patent Gmbh | Verfahren zur herstellung von mono- und bis(perfluoralkyl)fluorophosphatsalzen und deren säuren |
| PL3303330T3 (pl) * | 2015-06-03 | 2019-10-31 | Bristol Myers Squibb Co | Agoniści 4 - hydroksy - 3 - ( heteroarylo ) pirydyno - 2 - onowi receptora apj do stosowania w leczeniu zaburzeń sercowo-naczyniowych |
| UY36949A (es) | 2015-10-14 | 2017-04-28 | Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware | 2,4-dihidroxi-nicotinamidas como agonistas de apj |
| EA037257B1 (ru) | 2015-12-04 | 2021-02-26 | Бристол-Маерс Сквибб Компани | Новые агонисты рецептора апелина и способы применения |
| CN109195963B (zh) | 2016-03-24 | 2021-04-23 | 百时美施贵宝公司 | 作为apj激动剂的6-羟基-4-氧代-1，4-二氢嘧啶-5-甲酰胺 |
| US10889565B2 (en) | 2016-06-14 | 2021-01-12 | Bristol-Myers Squibb Company | 4-hydroxy-3-sulfonylpyridin-2(1H)-ones as APJ receptor agonists |
| CN109311821B (zh) | 2016-06-14 | 2022-10-14 | 百时美施贵宝公司 | 作为apj激动剂的6-羟基-5-(苯基/杂芳基磺酰基)嘧啶-4(1h)-酮 |
| CN110072850B (zh) | 2016-10-14 | 2023-07-21 | 百时美施贵宝公司 | 3-磺酰基-5-氨基吡啶-2,4-二醇apj激动剂 |
-
2016
- 2016-12-15 ES ES16820507T patent/ES2854733T3/es active Active
- 2016-12-15 AR ARP160103867A patent/AR107061A1/es unknown
- 2016-12-15 AU AU2016372048A patent/AU2016372048B2/en not_active Ceased
- 2016-12-15 EP EP16820507.8A patent/EP3390400B1/en active Active
- 2016-12-15 KR KR1020187019799A patent/KR102742744B1/ko active Active
- 2016-12-15 CN CN201680081704.3A patent/CN108602813B/zh active Active
- 2016-12-15 PE PE2018001129A patent/PE20181487A1/es unknown
- 2016-12-15 WO PCT/US2016/066750 patent/WO2017106396A1/en not_active Ceased
- 2016-12-15 CA CA3008630A patent/CA3008630A1/en not_active Abandoned
- 2016-12-15 TW TW105141572A patent/TW201725203A/zh unknown
- 2016-12-15 HK HK18114280.0A patent/HK1255163A1/zh unknown
- 2016-12-15 MX MX2018007155A patent/MX380669B/es unknown
- 2016-12-15 US US16/061,365 patent/US10669261B2/en active Active
- 2016-12-15 UY UY0001037026A patent/UY37026A/es unknown
- 2016-12-15 SG SG11201804674UA patent/SG11201804674UA/en unknown
- 2016-12-15 JP JP2018531333A patent/JP6948322B2/ja active Active
- 2016-12-15 BR BR112018012112-6A patent/BR112018012112A2/pt not_active Application Discontinuation
- 2016-12-15 EA EA201891336A patent/EA036736B1/ru not_active IP Right Cessation
-
2018
- 2018-06-11 IL IL259947A patent/IL259947B/en active IP Right Grant
- 2018-06-15 CL CL2018001621A patent/CL2018001621A1/es unknown
- 2018-07-11 CO CONC2018/0007221A patent/CO2018007221A2/es unknown
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