JP2021100934A5 - - Google Patents
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- Publication number
- JP2021100934A5 JP2021100934A5 JP2021029791A JP2021029791A JP2021100934A5 JP 2021100934 A5 JP2021100934 A5 JP 2021100934A5 JP 2021029791 A JP2021029791 A JP 2021029791A JP 2021029791 A JP2021029791 A JP 2021029791A JP 2021100934 A5 JP2021100934 A5 JP 2021100934A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- conr
- receptor
- apj
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000006552 (C3-C8) cycloalkyl group Chemical class 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 16
- 208000035475 disorder Diseases 0.000 claims 16
- 102000005962 receptors Human genes 0.000 claims 16
- 108020003175 receptors Proteins 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 13
- -1 adamantanyl Chemical group 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 claims 8
- 208000031229 Cardiomyopathies Diseases 0.000 claims 8
- 208000032928 Dyslipidaemia Diseases 0.000 claims 8
- 206010020772 Hypertension Diseases 0.000 claims 8
- 206010061218 Inflammation Diseases 0.000 claims 8
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 8
- 208000008589 Obesity Diseases 0.000 claims 8
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 8
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 8
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 8
- 229940125364 angiotensin receptor blocker Drugs 0.000 claims 8
- 208000006673 asthma Diseases 0.000 claims 8
- 206010012601 diabetes mellitus Diseases 0.000 claims 8
- 230000004054 inflammatory process Effects 0.000 claims 8
- 208000019423 liver disease Diseases 0.000 claims 8
- 208000030159 metabolic disease Diseases 0.000 claims 8
- 230000004770 neurodegeneration Effects 0.000 claims 8
- 208000015122 neurodegenerative disease Diseases 0.000 claims 8
- 235000020824 obesity Nutrition 0.000 claims 8
- 230000008085 renal dysfunction Effects 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 5
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 4
- 208000021908 Myocardial disease Diseases 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000005233 alkylalcohol group Chemical group 0.000 claims 4
- 239000002160 alpha blocker Substances 0.000 claims 4
- 229940124308 alpha-adrenoreceptor antagonist Drugs 0.000 claims 4
- 239000002876 beta blocker Substances 0.000 claims 4
- 229940097320 beta blocking agent Drugs 0.000 claims 4
- 239000000480 calcium channel blocker Substances 0.000 claims 4
- 239000002934 diuretic Substances 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 201000011461 pre-eclampsia Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000005012 alkyl thioether group Chemical group 0.000 claims 3
- 150000001356 alkyl thiols Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 230000001882 diuretic effect Effects 0.000 claims 2
- 229940030606 diuretics Drugs 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- OUOJIFQQBPKAMU-UHFFFAOYSA-N tetrazol-5-one Chemical compound O=C1N=NN=N1 OUOJIFQQBPKAMU-UHFFFAOYSA-N 0.000 claims 1
- 150000003568 thioethers Chemical class 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 0 *C(*)(*)NC(c1n[n](*)c(I)c1)=O Chemical compound *C(*)(*)NC(c1n[n](*)c(I)c1)=O 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562265177P | 2015-12-09 | 2015-12-09 | |
| US201562265168P | 2015-12-09 | 2015-12-09 | |
| US62/265,168 | 2015-12-09 | ||
| US62/265,177 | 2015-12-09 | ||
| JP2018530026A JP2019501899A (ja) | 2015-12-09 | 2016-12-09 | 改良アペリンレセプター（ａｐｊ）アゴニストおよびその使用 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018530026A Division JP2019501899A (ja) | 2015-12-09 | 2016-12-09 | 改良アペリンレセプター（ａｐｊ）アゴニストおよびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021100934A JP2021100934A (ja) | 2021-07-08 |
| JP2021100934A5 true JP2021100934A5 (enExample) | 2021-08-19 |
| JP7195356B2 JP7195356B2 (ja) | 2022-12-23 |
Family
ID=57796972
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018530026A Pending JP2019501899A (ja) | 2015-12-09 | 2016-12-09 | 改良アペリンレセプター（ａｐｊ）アゴニストおよびその使用 |
| JP2021029791A Active JP7195356B2 (ja) | 2015-12-09 | 2021-02-26 | 改良アペリンレセプター（ａｐｊ）アゴニストおよびその使用 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018530026A Pending JP2019501899A (ja) | 2015-12-09 | 2016-12-09 | 改良アペリンレセプター（ａｐｊ）アゴニストおよびその使用 |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US10100059B2 (enExample) |
| EP (1) | EP3386976A1 (enExample) |
| JP (2) | JP2019501899A (enExample) |
| KR (1) | KR20180090852A (enExample) |
| CN (1) | CN108602806B (enExample) |
| AU (1) | AU2016366310C1 (enExample) |
| BR (1) | BR112018011784A2 (enExample) |
| CO (1) | CO2018005871A2 (enExample) |
| HK (1) | HK1255452A1 (enExample) |
| IL (1) | IL259634A (enExample) |
| MA (1) | MA43417A (enExample) |
| MX (2) | MX391898B (enExample) |
| PE (1) | PE20190258A1 (enExample) |
| RU (2) | RU2021133849A (enExample) |
| WO (1) | WO2017100558A1 (enExample) |
| ZA (1) | ZA201803301B (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA39999A (fr) | 2014-06-06 | 2015-12-10 | Res Triangle Inst | Agonistes du récepteur de l'apeline (apj) et leurs utilisations |
| JP6356364B1 (ja) | 2015-05-20 | 2018-07-11 | アムジエン・インコーポレーテツド | Ａｐｊ受容体のトリアゾールアゴニスト |
| PH12017502158B1 (en) | 2015-06-03 | 2022-04-27 | Bristol Meyers Squibb Co | 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders |
| EP3386976A1 (en) | 2015-12-09 | 2018-10-17 | Research Triangle Institute, International | Improved apelin receptor (apj) agonists and uses thereof |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| RU2764039C2 (ru) | 2016-10-12 | 2022-01-14 | Рисерч Трайэнгл Инститьют | Гетероциклические агонисты рецептора апелина (apj) и их применение |
| US11046680B1 (en) | 2016-11-16 | 2021-06-29 | Amgen Inc. | Heteroaryl-substituted triazoles as APJ receptor agonists |
| MA46824A (fr) | 2016-11-16 | 2019-09-25 | Amgen Inc | Composés de triazole substitués par alkyle en tant qu'agonistes du récepteur apj |
| EP3541803B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole pyridyl 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 |
| EP3541810B1 (en) | 2016-11-16 | 2020-12-23 | 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 |
| US11247987B2 (en) | 2017-10-06 | 2022-02-15 | Forma Therapeutics, Inc. | Inhibiting ubiquitin specific peptidase 30 |
| EP3692015B1 (en) | 2017-10-06 | 2022-08-24 | The John Hopkins University | Novel glutamine antagonists and uses thereof |
| US11149040B2 (en) | 2017-11-03 | 2021-10-19 | Amgen Inc. | Fused triazole agonists of the APJ receptor |
| WO2019213006A1 (en) | 2018-05-01 | 2019-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the apj receptor |
| ES2988920T3 (es) | 2018-05-17 | 2024-11-22 | Forma Therapeutics Inc | Compuestos bicíclicos fusionados útiles como inhibidores de la peptidasa 30 específica de ubiquitina |
| MX2021002981A (es) | 2018-10-05 | 2021-05-14 | Forma Therapeutics Inc | Pirrolinas fusionadas que actuan como inhibidores de la proteasa 30 especifica de la ubiquitina (usp30). |
| CA3145074A1 (en) * | 2019-08-29 | 2021-03-04 | Research Triangle Institute | Methods and uses for apelin receptor agonists |
| WO2022182547A1 (en) * | 2021-02-25 | 2022-09-01 | Research Triangle Institute | Heteroaryl derivatives as apelin receptor agonists |
| WO2024148104A1 (en) * | 2023-01-03 | 2024-07-11 | BioAge Labs, Inc. | Combination therapy of apelin receptor agonist and glp-1 receptor agonist for treating a disease or condition associated with weight gain |
| WO2025213190A1 (en) | 2024-04-05 | 2025-10-09 | BioAge Labs, Inc. | Methods of treating a disease or condition associated with weight gain |
| WO2025251084A1 (en) | 2024-05-31 | 2025-12-04 | BioAge Labs, Inc. | Methods of treating a disease or condition associated with weight gain |
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| US20170174633A1 (en) * | 2014-03-25 | 2017-06-22 | Research Triangle Institute | Pyrazole compounds selective for neurotensin 2 receptor |
| US10570128B2 (en) | 2014-05-28 | 2020-02-25 | Sanford Burnham Prebys Medical Discovery Institute | Agonists of the apelin receptor and methods of use thereof |
| MA39999A (fr) | 2014-06-06 | 2015-12-10 | Res Triangle Inst | Agonistes du récepteur de l'apeline (apj) et leurs utilisations |
| EP3386976A1 (en) | 2015-12-09 | 2018-10-17 | Research Triangle Institute, International | Improved apelin receptor (apj) agonists and uses thereof |
| RU2764039C2 (ru) | 2016-10-12 | 2022-01-14 | Рисерч Трайэнгл Инститьют | Гетероциклические агонисты рецептора апелина (apj) и их применение |
| CA3145074A1 (en) | 2019-08-29 | 2021-03-04 | Research Triangle Institute | Methods and uses for apelin receptor agonists |
-
2016
- 2016-12-09 EP EP16826220.2A patent/EP3386976A1/en active Pending
- 2016-12-09 PE PE2018001082A patent/PE20190258A1/es unknown
- 2016-12-09 RU RU2021133849A patent/RU2021133849A/ru unknown
- 2016-12-09 US US15/374,386 patent/US10100059B2/en not_active Ceased
- 2016-12-09 RU RU2018118568A patent/RU2766148C1/ru active
- 2016-12-09 JP JP2018530026A patent/JP2019501899A/ja active Pending
- 2016-12-09 HK HK18114625.4A patent/HK1255452A1/zh unknown
- 2016-12-09 BR BR112018011784A patent/BR112018011784A2/pt not_active Application Discontinuation
- 2016-12-09 MA MA043417A patent/MA43417A/fr unknown
- 2016-12-09 AU AU2016366310A patent/AU2016366310C1/en active Active
- 2016-12-09 CN CN201680081397.9A patent/CN108602806B/zh not_active Expired - Fee Related
- 2016-12-09 KR KR1020187018896A patent/KR20180090852A/ko not_active Ceased
- 2016-12-09 MX MX2018006979A patent/MX391898B/es unknown
- 2016-12-09 WO PCT/US2016/065808 patent/WO2017100558A1/en not_active Ceased
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2018
- 2018-05-17 ZA ZA2018/03301A patent/ZA201803301B/en unknown
- 2018-05-18 US US15/983,519 patent/US10954247B2/en active Active
- 2018-05-27 IL IL259634A patent/IL259634A/en unknown
- 2018-06-07 MX MX2022002026A patent/MX2022002026A/es unknown
- 2018-06-07 CO CONC2018/0005871A patent/CO2018005871A2/es unknown
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2020
- 2020-05-04 US US16/974,363 patent/USRE49594E1/en active Active
- 2020-10-28 US US17/082,650 patent/US11535630B2/en active Active
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2021
- 2021-02-26 JP JP2021029791A patent/JP7195356B2/ja active Active