JP2020515575A5 - - Google Patents
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- JP2020515575A5 JP2020515575A5 JP2019553090A JP2019553090A JP2020515575A5 JP 2020515575 A5 JP2020515575 A5 JP 2020515575A5 JP 2019553090 A JP2019553090 A JP 2019553090A JP 2019553090 A JP2019553090 A JP 2019553090A JP 2020515575 A5 JP2020515575 A5 JP 2020515575A5
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- JP
- Japan
- Prior art keywords
- group
- optionally substituted
- alkyl
- substituents selected
- groups
- 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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- 125000001424 substituent group Chemical group 0.000 claims 117
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 89
- 125000005843 halogen group Chemical group 0.000 claims 88
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 70
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 50
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 45
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 42
- 150000003839 salts Chemical class 0.000 claims 41
- -1 2-azaspiro [3.3] heptyl group Chemical group 0.000 claims 31
- 229910052799 carbon Inorganic materials 0.000 claims 30
- 125000004432 carbon atom Chemical group C* 0.000 claims 29
- 125000004093 cyano group Chemical group *C#N 0.000 claims 29
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 26
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 22
- 125000003118 aryl group Chemical group 0.000 claims 21
- 125000002950 monocyclic group Chemical group 0.000 claims 21
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 19
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 15
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 125000004043 oxo group Chemical group O=* 0.000 claims 12
- 125000003277 amino group Chemical group 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 10
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 9
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 8
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 7
- 125000003226 pyrazolyl group Chemical group 0.000 claims 7
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 6
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 6
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 125000002843 carboxylic acid group Chemical group 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 125000004431 deuterium atom Chemical group 0.000 claims 4
- 208000019622 heart disease Diseases 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 125000005974 C6-C14 arylcarbonyl group Chemical group 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- 206010003119 arrhythmia Diseases 0.000 claims 2
- 230000006793 arrhythmia Effects 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 150000003943 catecholamines Chemical group 0.000 claims 2
- 150000001925 cycloalkenes Chemical class 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 208000014321 polymorphic ventricular tachycardia Diseases 0.000 claims 2
- 230000002980 postoperative effect Effects 0.000 claims 2
- 125000003003 spiro group Chemical group 0.000 claims 2
- 206010047302 ventricular tachycardia Diseases 0.000 claims 2
- UGUHFDPGDQDVGX-UHFFFAOYSA-N 1,2,3-thiadiazole Chemical group C1=CSN=N1 UGUHFDPGDQDVGX-UHFFFAOYSA-N 0.000 claims 1
- GUEJTWUSAZVRKO-FQEVSTJZSA-N 1-[4-[[5-[4-chloro-3-[(2S)-1-(tetrazol-1-yl)propan-2-yl]oxyphenyl]pyrimidin-2-yl]amino]-1-[2-(oxan-4-yl)-2-azaspiro[3.3]heptan-6-yl]pyrazol-3-yl]propan-1-one Chemical compound N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)C1CC2(CN(C2)C2CCOCC2)C1)C(CC)=O GUEJTWUSAZVRKO-FQEVSTJZSA-N 0.000 claims 1
- 101710116137 Calcium/calmodulin-dependent protein kinase II Proteins 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- STHUJMGSNYMQSX-NYVOZVTQSA-N N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)C(F)(F)F Chemical compound N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)C(F)(F)F STHUJMGSNYMQSX-NYVOZVTQSA-N 0.000 claims 1
- NCCAWPHKRPSXIH-OYDLWJJNSA-N N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)OC1COC1 Chemical compound N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)OC1COC1 NCCAWPHKRPSXIH-OYDLWJJNSA-N 0.000 claims 1
- BTLDRKZWPPOTOY-VJBMBRPKSA-N N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)OCC(F)(F)F Chemical compound N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)OCC(F)(F)F BTLDRKZWPPOTOY-VJBMBRPKSA-N 0.000 claims 1
- MCLZGEHWQDRQER-VJBMBRPKSA-N N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)OCC(F)F Chemical compound N1(N=NN=C1)C[C@H](C)OC=1C=C(C=CC=1Cl)C=1C=NC(=NC=1)NC=1C(=NN(C=1)[C@@H]1CC[C@H](CC1)N1CCOCC1)OCC(F)F MCLZGEHWQDRQER-VJBMBRPKSA-N 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical group C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 231100000518 lethal Toxicity 0.000 claims 1
- 230000001665 lethal effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 1
- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 claims 1
- 125000005004 perfluoroethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 1
- 125000005936 piperidyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 150000003217 pyrazoles Chemical class 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- 0 CCCCC(C)=C([C@]1(*)CC(C2)(C3CC)C3C2CC1)C(C=CCCCCC1=C(CCC)CCC=C([C@@]2C=CC(CCC3C(C[C@](C)CC)C3)=C(C)C2)/C=C/CCCC1C)=CCC(CCC)C1CC(CC)(CC)C1 Chemical compound CCCCC(C)=C([C@]1(*)CC(C2)(C3CC)C3C2CC1)C(C=CCCCCC1=C(CCC)CCC=C([C@@]2C=CC(CCC3C(C[C@](C)CC)C3)=C(C)C2)/C=C/CCCC1C)=CCC(CCC)C1CC(CC)(CC)C1 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762476970P | 2017-03-27 | 2017-03-27 | |
| US62/476,970 | 2017-03-27 | ||
| PCT/US2018/024043 WO2018183112A1 (en) | 2017-03-27 | 2018-03-23 | Heterocyclic compound |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020515575A JP2020515575A (ja) | 2020-05-28 |
| JP2020515575A5 true JP2020515575A5 (enExample) | 2021-04-30 |
| JP7249950B2 JP7249950B2 (ja) | 2023-03-31 |
Family
ID=63671942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019553090A Active JP7249950B2 (ja) | 2017-03-27 | 2018-03-23 | ヘテロ環化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US10543212B2 (enExample) |
| EP (1) | EP3600327A4 (enExample) |
| JP (1) | JP7249950B2 (enExample) |
| KR (1) | KR102638678B1 (enExample) |
| CN (1) | CN110799190B (enExample) |
| AU (1) | AU2018243691B2 (enExample) |
| CA (1) | CA3058182A1 (enExample) |
| TW (1) | TWI789381B (enExample) |
| WO (1) | WO2018183112A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7249950B2 (ja) | 2017-03-27 | 2023-03-31 | カーデュリオン・ファーマシューティカルズ・リミテッド・ライアビリティ・カンパニー | ヘテロ環化合物 |
| JP7569688B2 (ja) | 2017-12-22 | 2024-10-18 | ハイバーセル，インコーポレイテッド | ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体 |
| WO2020068846A1 (en) * | 2018-09-25 | 2020-04-02 | Heterocyclic Compound | Heterocyclic compound |
| JP7447098B2 (ja) * | 2018-09-25 | 2024-03-11 | カーデュリオン・ファーマシューティカルズ・インコーポレイテッド | アミノピリミジン化合物 |
| WO2020140054A1 (en) | 2018-12-28 | 2020-07-02 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| EP4048664A1 (en) * | 2019-10-25 | 2022-08-31 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| SI4097097T1 (sl) | 2020-01-29 | 2025-04-30 | Gilead Sciences, Inc. | Spojine, ki modulirajo glp-1r |
| KR102563111B1 (ko) * | 2020-03-18 | 2023-08-04 | 주식회사 엘지화학 | Glp-1 수용체 효능제, 이를 포함하는 약학적 조성물 및 이의 제조방법 |
| WO2021187886A1 (ko) * | 2020-03-18 | 2021-09-23 | 주식회사 엘지화학 | Glp-1 수용체 효능제, 이를 포함하는 약학적 조성물 및 이의 제조방법 |
| JP2023543038A (ja) | 2020-09-28 | 2023-10-12 | カーデュリオン・ファーマシューティカルズ・インコーポレイテッド | 縮合ヘテロアリール化合物およびＣａＭＫＩＩ阻害剤としてのその使用 |
| EP4247804A1 (en) | 2020-11-20 | 2023-09-27 | Gilead Sciences, Inc. | Polyheterocyclic glp-1 r modulating compounds |
| WO2022192428A1 (en) | 2021-03-11 | 2022-09-15 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| EP4304712A1 (en) | 2021-03-11 | 2024-01-17 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| WO2022216094A1 (ko) * | 2021-04-08 | 2022-10-13 | 주식회사 엘지화학 | Glp-1 수용체 효능제, 이를 포함하는 약학적 조성물 및 이의 제조방법 |
| MX2023012418A (es) | 2021-04-21 | 2023-10-31 | Gilead Sciences Inc | Compuestos de modulacion de glp-1r de carboxi-bencimidazol. |
| US20250170101A1 (en) * | 2021-12-29 | 2025-05-29 | Psy Therapeutics, Inc. | Monoacylglycerol lipase inhibitors and use thereof for the treatment and management of pain and related conditions |
| EP4457213A4 (en) | 2021-12-29 | 2025-12-17 | Psy Therapeutics Inc | INHIBITION OF MONOACYLGLYCEROL LIPASE (MAGL) |
| CN114621312B (zh) * | 2022-03-24 | 2022-11-15 | 陕西师范大学 | 一种寡肽烷基侧链的选择性修饰方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020198219A1 (en) * | 2000-08-08 | 2002-12-26 | Grant Elfrida R. | 2-pyridinamine compositions and related methods |
| DE60136731D1 (de) | 2000-09-20 | 2009-01-08 | Ortho Mcneil Pharm Inc | Pyrazine derivate als tyrosin kinase modulatoren |
| AU2004261484A1 (en) | 2003-07-30 | 2005-02-10 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
| JP2007504229A (ja) | 2003-09-02 | 2007-03-01 | メルク エンド カムパニー インコーポレーテッド | 代謝調節型グルタミン酸受容体−５のモジュレーターとしてのビピリジルアミン類およびエーテル類 |
| AU2008236670B2 (en) * | 2007-04-05 | 2011-12-01 | Amgen Inc. | Aurora kinase modulators and method of use |
| WO2009032703A1 (en) | 2007-08-28 | 2009-03-12 | Irm Llc | 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors |
| WO2010038081A2 (en) * | 2008-10-03 | 2010-04-08 | Astrazeneca Ab | Heterocyclic derivatives and methods of use thereof |
| GB0821307D0 (en) * | 2008-11-21 | 2008-12-31 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| EP2638018A1 (en) * | 2010-11-09 | 2013-09-18 | Cellzome Limited | Pyridine compounds and aza analogues thereof as tyk2 inhibitors |
| EP2763976B1 (en) | 2011-10-05 | 2016-05-18 | Merck Sharp & Dohme Corp. | 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors |
| AU2013250378B2 (en) | 2012-04-17 | 2016-01-14 | Fujifilm Corporation | Nitrogen-containing heterocyclic compound or salt thereof |
| JP7249950B2 (ja) * | 2017-03-27 | 2023-03-31 | カーデュリオン・ファーマシューティカルズ・リミテッド・ライアビリティ・カンパニー | ヘテロ環化合物 |
-
2018
- 2018-03-23 JP JP2019553090A patent/JP7249950B2/ja active Active
- 2018-03-23 AU AU2018243691A patent/AU2018243691B2/en active Active
- 2018-03-23 CN CN201880021628.6A patent/CN110799190B/zh active Active
- 2018-03-23 WO PCT/US2018/024043 patent/WO2018183112A1/en not_active Ceased
- 2018-03-23 US US15/933,889 patent/US10543212B2/en active Active
- 2018-03-23 EP EP18777887.3A patent/EP3600327A4/en active Pending
- 2018-03-23 KR KR1020197031604A patent/KR102638678B1/ko active Active
- 2018-03-23 CA CA3058182A patent/CA3058182A1/en active Pending
- 2018-03-26 TW TW107110319A patent/TWI789381B/zh active
-
2020
- 2020-01-27 US US16/773,730 patent/US11197858B2/en active Active
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