JP2021100934A5 - - Google Patents
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- 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.)
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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 |
|---|---|---|---|
| US201562265168P | 2015-12-09 | 2015-12-09 | |
| US201562265177P | 2015-12-09 | 2015-12-09 | |
| US62/265,177 | 2015-12-09 | ||
| US62/265,168 | 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 (https=) | 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 (https=) |
| EP (1) | EP3386976A1 (https=) |
| JP (2) | JP2019501899A (https=) |
| KR (1) | KR20180090852A (https=) |
| CN (1) | CN108602806B (https=) |
| AU (1) | AU2016366310C1 (https=) |
| BR (1) | BR112018011784A2 (https=) |
| CO (1) | CO2018005871A2 (https=) |
| HK (1) | HK1255452A1 (https=) |
| IL (1) | IL259634A (https=) |
| MA (1) | MA43417A (https=) |
| MX (2) | MX391898B (https=) |
| PE (1) | PE20190258A1 (https=) |
| RU (2) | RU2766148C1 (https=) |
| WO (1) | WO2017100558A1 (https=) |
| ZA (1) | ZA201803301B (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX387055B (es) | 2014-06-06 | 2025-03-19 | Res Triangle Inst | Agonistas del receptor de apelina (apj) y usos de los mismos. |
| HUE050317T2 (hu) | 2015-05-20 | 2020-11-30 | Amgen Inc | APJ receptor triazol agonistái |
| 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 |
| WO2017100558A1 (en) | 2015-12-09 | 2017-06-15 | Research Triangle Institute | Improved apelin receptor (apj) agonists and uses thereof |
| US9988369B2 (en) | 2016-05-03 | 2018-06-05 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the APJ receptor |
| MX394907B (es) * | 2016-10-12 | 2025-03-24 | Res Triangle Inst | Agonistas heterociclicos del receptor de apelina (apj) y usos de los mismos |
| US10736883B2 (en) | 2016-11-16 | 2020-08-11 | Amgen Inc. | Triazole furan compounds as agonists of the APJ receptor |
| EP3541803B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| WO2018093577A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the apj receptor |
| WO2018093576A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Alkyl substituted triazole 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 |
| AU2018346597B2 (en) | 2017-10-06 | 2023-07-13 | 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 |
| MA50509A (fr) | 2017-11-03 | 2021-06-02 | Amgen Inc | Agonistes de triazole fusionnés du récepteur apj |
| US11807624B2 (en) | 2018-05-01 | 2023-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the APJ receptor |
| JP7449242B2 (ja) | 2018-05-17 | 2024-03-13 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的ペプチダーゼ３０（ｕｓｐ３０）阻害剤として有用な縮合二環化合物 |
| JP7530889B2 (ja) | 2018-10-05 | 2024-08-08 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的プロテアーゼ３０（ｕｓｐ３０）阻害剤として作用する縮合ピロリン |
| KR20220054391A (ko) * | 2019-08-29 | 2022-05-02 | 리서치 트라이앵글 인스티튜트 | 아펠린 수용체 작용제에 대한 방법 및 용도 |
| 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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| MX387055B (es) * | 2014-06-06 | 2025-03-19 | Res Triangle Inst | Agonistas del receptor de apelina (apj) y usos de los mismos. |
| WO2017100558A1 (en) * | 2015-12-09 | 2017-06-15 | Research Triangle Institute | Improved apelin receptor (apj) agonists and uses thereof |
| MX394907B (es) | 2016-10-12 | 2025-03-24 | Res Triangle Inst | Agonistas heterociclicos del receptor de apelina (apj) y usos de los mismos |
| KR20220054391A (ko) | 2019-08-29 | 2022-05-02 | 리서치 트라이앵글 인스티튜트 | 아펠린 수용체 작용제에 대한 방법 및 용도 |
-
2016
- 2016-12-09 WO PCT/US2016/065808 patent/WO2017100558A1/en not_active Ceased
- 2016-12-09 MA MA043417A patent/MA43417A/fr unknown
- 2016-12-09 EP EP16826220.2A patent/EP3386976A1/en active Pending
- 2016-12-09 MX MX2018006979A patent/MX391898B/es unknown
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- 2016-12-09 AU AU2016366310A patent/AU2016366310C1/en active Active
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