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 |
|---|---|---|---|---|
| MY189453A (en) | 2015-06-03 | 2022-02-14 | Bristol Myers Squibb Co | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| CA3001974A1 (en) | 2015-10-14 | 2017-04-20 | Bristol-Myers Squibb Company | 2,4-dihydroxy-nicotinamides as apj agonists |
| WO2017096130A1 (en) | 2015-12-04 | 2017-06-08 | Bristol-Myers Squibb Company | Apelin receptor agonists and methods of use |
| PT3390395T (pt) | 2015-12-16 | 2020-11-03 | Loxo Oncology Inc | Compostos úteis como inibidores de quinase |
| MA43761A (fr) | 2016-03-24 | 2021-05-05 | Bristol Myers Squibb Co | 6-hydroxy-4-oxo-1,4-dihydropyrimidine-5-carboxamides comme inhibiteurs de la apj |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| KR102521955B1 (ko) | 2016-06-14 | 2023-04-13 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 수용체 효능제로서의 4-히드록시-3-술포닐피리딘-2(1h)-온 |
| US10508104B2 (en) | 2016-06-14 | 2019-12-17 | Bristol-Myers Squibb Company | 6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1H)-one as APJ agonists |
| EP3526198B1 (en) | 2016-10-14 | 2020-08-12 | Bristol-Myers Squibb Company | 3-sulfonyl-5-aminopyridine-2,4-diol apj agonists |
| US10906890B2 (en) | 2016-11-16 | 2021-02-02 | Amgen Inc. | Triazole phenyl compounds as agonists of the APJ receptor |
| MA46827A (fr) | 2016-11-16 | 2019-09-25 | Amgen Inc | Composés de triazole à substitution cycloalkyle en tant qu'agonistes du récepteur apj |
| EP3541792B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| WO2018097945A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Heteroaryl-substituted triazoles as apj receptor agonists |
| WO2018093580A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| US11191762B2 (en) | 2016-11-16 | 2021-12-07 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the APJ Receptor |
| WO2019213006A1 (en) | 2018-05-01 | 2019-11-07 | 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 |
| BR9711098B1 (pt) | 1996-07-01 | 2011-10-04 | compostos heterocìclicos, processo para sua preparação e composições farmacêuticas contendo os mesmos e seu uso no tratamento de diabetes e doenças relacionadas. | |
| 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 |
| NZ520752A (en) * | 2000-02-16 | 2004-03-26 | Smithkline Beecham P | Pyrimidine-4-one derivatives as LDL-PLA2 inhibitors |
| AU2001280590A1 (en) | 2000-07-18 | 2002-01-30 | 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 |
| EP1509507A4 (en) | 2002-05-23 | 2006-09-13 | Merck & Co Inc | INHIBITORS OF MITOTIC KINESINE |
| US20070167621A1 (en) | 2003-04-03 | 2007-07-19 | Pharmacia Corporation | Substituted pyrimidinones |
| WO2004094408A1 (en) | 2003-04-23 | 2004-11-04 | 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 |
| WO2005041888A2 (en) | 2003-11-03 | 2005-05-12 | Cytokinetics, Inc. | Pyrimidin-4-one compounds, compositions and methods |
| JP2007518711A (ja) | 2003-12-19 | 2007-07-12 | メルク エンド カムパニー インコーポレーテッド | 有糸分裂キネシン阻害剤 |
| 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 |
| KR20080080584A (ko) | 2005-11-30 | 2008-09-04 | 버텍스 파마슈티칼스 인코포레이티드 | ｃ-Ｍｅｔ의 억제제 및 이의 용도 |
| EP2016056A4 (en) | 2006-04-21 | 2010-11-10 | Univ Boston | IONIC VISCOELASTIC AND VISCOELASTIC SALTS |
| EP2079707B1 (de) | 2006-10-10 | 2014-12-03 | proionic GmbH & Co KG | Verfahren zur umsetzung von 1,3-hetero-aromatischen 2-carboxylaten mit wasser |
| 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 |
| EP2114898A2 (en) | 2007-02-16 | 2009-11-11 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors |
| EP2279192B1 (en) | 2008-05-28 | 2013-10-30 | 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 |
| US9040538B2 (en) | 2009-05-21 | 2015-05-26 | Universite Laval | Pyrimidines as novel therapeutic agents |
| US9212130B2 (en) | 2010-08-10 | 2015-12-15 | Shionogi & Co., Ltd. | Heterocyclic derivative and pharmaceutical composition comprising the same |
| KR20140039242A (ko) | 2011-05-31 | 2014-04-01 | 메르크 파텐트 게엠베하 | 전해질 제형 |
| 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 |
| CN110664816A (zh) | 2012-06-07 | 2020-01-10 | 佐治亚州立大学研究基金会公司 | Seca抑制剂以及其制备和使用方法 |
| HUE031733T2 (en) * | 2012-09-21 | 2017-07-28 | Sanofi Sa | Benzimidazole carboxylic acid amide derivatives for the treatment of metabolic or cardiovascular diseases |
| 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 |
| HK1212235A1 (en) | 2012-11-16 | 2016-06-10 | 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 |
| ES2906062T3 (es) | 2013-11-29 | 2022-04-13 | Proionic Gmbh | Procedimiento para la unión de un material termoplástico por medio de radiación de microondas |
| 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 |
| EP3152200A1 (en) * | 2014-06-06 | 2017-04-12 | Research Triangle Institute | Apelin receptor (apj) agonists and uses thereof |
| WO2016074757A1 (de) | 2014-11-11 | 2016-05-19 | Merck Patent Gmbh | Verfahren zur herstellung von mono- und bis(perfluoralkyl)fluorophosphatsalzen und deren säuren |
| MY189453A (en) * | 2015-06-03 | 2022-02-14 | Bristol Myers Squibb Co | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| CA3001974A1 (en) | 2015-10-14 | 2017-04-20 | Bristol-Myers Squibb Company | 2,4-dihydroxy-nicotinamides as apj agonists |
| WO2017096130A1 (en) | 2015-12-04 | 2017-06-08 | Bristol-Myers Squibb Company | Apelin receptor agonists and methods of use |
| MA43761A (fr) | 2016-03-24 | 2021-05-05 | Bristol Myers Squibb Co | 6-hydroxy-4-oxo-1,4-dihydropyrimidine-5-carboxamides comme inhibiteurs de la apj |
| KR102521955B1 (ko) | 2016-06-14 | 2023-04-13 | 브리스톨-마이어스 스큅 컴퍼니 | Apj 수용체 효능제로서의 4-히드록시-3-술포닐피리딘-2(1h)-온 |
| US10508104B2 (en) | 2016-06-14 | 2019-12-17 | Bristol-Myers Squibb Company | 6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1H)-one as APJ agonists |
| EP3526198B1 (en) | 2016-10-14 | 2020-08-12 | Bristol-Myers Squibb Company | 3-sulfonyl-5-aminopyridine-2,4-diol apj agonists |
-
2016
- 2016-12-15 TW TW105141572A patent/TW201725203A/zh unknown
- 2016-12-15 CA CA3008630A patent/CA3008630A1/en not_active Abandoned
- 2016-12-15 MX MX2018007155A patent/MX380669B/es unknown
- 2016-12-15 ES ES16820507T patent/ES2854733T3/es active Active
- 2016-12-15 KR KR1020187019799A patent/KR102742744B1/ko active Active
- 2016-12-15 SG SG11201804674UA patent/SG11201804674UA/en unknown
- 2016-12-15 UY UY0001037026A patent/UY37026A/es 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 EP EP16820507.8A patent/EP3390400B1/en active Active
- 2016-12-15 WO PCT/US2016/066750 patent/WO2017106396A1/en not_active Ceased
- 2016-12-15 PE PE2018001129A patent/PE20181487A1/es unknown
- 2016-12-15 AU AU2016372048A patent/AU2016372048B2/en not_active Ceased
- 2016-12-15 CN CN201680081704.3A patent/CN108602813B/zh active Active
- 2016-12-15 HK HK18114280.0A patent/HK1255163A1/zh unknown
- 2016-12-15 AR ARP160103867A patent/AR107061A1/es unknown
- 2016-12-15 US US16/061,365 patent/US10669261B2/en active Active
- 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