JP2020533347A5 - - Google Patents
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- Publication number
- JP2020533347A5 JP2020533347A5 JP2020514579A JP2020514579A JP2020533347A5 JP 2020533347 A5 JP2020533347 A5 JP 2020533347A5 JP 2020514579 A JP2020514579 A JP 2020514579A JP 2020514579 A JP2020514579 A JP 2020514579A JP 2020533347 A5 JP2020533347 A5 JP 2020533347A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halogen
- hydrogen
- cycloalkyl
- halo
- 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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- 229910052739 hydrogen Inorganic materials 0.000 claims description 139
- 239000001257 hydrogen Substances 0.000 claims description 131
- 229910052736 halogen Inorganic materials 0.000 claims description 128
- 150000002367 halogens Chemical class 0.000 claims description 128
- 125000005843 halogen group Chemical group 0.000 claims description 95
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 91
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 80
- 150000002431 hydrogen Chemical class 0.000 claims description 75
- 150000001875 compounds Chemical class 0.000 claims description 56
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 54
- 229910052760 oxygen Inorganic materials 0.000 claims description 52
- 125000005842 heteroatom Chemical group 0.000 claims description 46
- -1 C 2 to C 6 alkynyl Chemical group 0.000 claims description 45
- 229910052717 sulfur Inorganic materials 0.000 claims description 41
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 35
- 125000000623 heterocyclic group Chemical group 0.000 claims description 33
- 125000000217 alkyl group Chemical group 0.000 claims description 32
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- 125000004043 oxo group Chemical group O=* 0.000 claims description 24
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 22
- 229910052799 carbon Inorganic materials 0.000 claims description 21
- 239000008194 pharmaceutical composition Substances 0.000 claims description 19
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 16
- 125000004432 carbon atom Chemical group C* 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 12
- 206010019280 Heart failures Diseases 0.000 claims description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
- 125000006413 ring segment Chemical group 0.000 claims description 12
- 229920006395 saturated elastomer Polymers 0.000 claims description 12
- 241000124008 Mammalia Species 0.000 claims description 11
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 239000001301 oxygen Substances 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 125000003003 spiro group Chemical group 0.000 claims description 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 8
- 208000019622 heart disease Diseases 0.000 claims description 8
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 7
- 125000004981 cycloalkylmethyl group Chemical group 0.000 claims description 7
- 125000001188 haloalkyl group Chemical group 0.000 claims description 6
- 230000002107 myocardial effect Effects 0.000 claims description 6
- 125000003566 oxetanyl group Chemical group 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 125000002393 azetidinyl group Chemical group 0.000 claims description 5
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims description 4
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 4
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 4
- 229940127557 pharmaceutical product Drugs 0.000 claims description 4
- 102000003505 Myosin Human genes 0.000 claims description 3
- 108060008487 Myosin Proteins 0.000 claims description 3
- 230000002708 enhancing effect Effects 0.000 claims description 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 3
- 230000001105 regulatory effect Effects 0.000 claims description 3
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 2
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical group C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 claims description 2
- RQMWVVBHJMUJNZ-UHFFFAOYSA-N 4-chloropyridin-2-amine Chemical group NC1=CC(Cl)=CC=N1 RQMWVVBHJMUJNZ-UHFFFAOYSA-N 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 2
- 208000008253 Systolic Heart Failure Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000005605 benzo group Chemical group 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- 239000006071 cream Substances 0.000 claims description 2
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims description 2
- 239000000499 gel Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 2
- 239000006187 pill Substances 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- 239000006188 syrup Substances 0.000 claims description 2
- 235000020357 syrup Nutrition 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 2
- 238000000034 method Methods 0.000 description 17
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 239000007858 starting material Substances 0.000 description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762557846P | 2017-09-13 | 2017-09-13 | |
| US62/557,846 | 2017-09-13 | ||
| PCT/US2018/050793 WO2019055590A1 (en) | 2017-09-13 | 2018-09-13 | SARCOMERIC BISAMIDE ACTIVATOR COMPOUNDS AND USES THEREOF |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020533347A JP2020533347A (ja) | 2020-11-19 |
| JP2020533347A5 true JP2020533347A5 (https=) | 2021-10-21 |
| JP7308816B2 JP7308816B2 (ja) | 2023-07-14 |
Family
ID=63794635
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020514579A Active JP7308816B2 (ja) | 2017-09-13 | 2018-09-13 | ビスアミド筋節活性化化合物及びその使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (6) | US10723720B2 (https=) |
| EP (1) | EP3681882A1 (https=) |
| JP (1) | JP7308816B2 (https=) |
| KR (1) | KR20200054237A (https=) |
| CN (1) | CN111601798B (https=) |
| AR (1) | AR112804A1 (https=) |
| AU (1) | AU2018332887B2 (https=) |
| BR (1) | BR112020004800A2 (https=) |
| CA (1) | CA3075669A1 (https=) |
| CL (1) | CL2020000610A1 (https=) |
| CO (1) | CO2020002745A2 (https=) |
| CR (1) | CR20200116A (https=) |
| EA (1) | EA202090688A1 (https=) |
| IL (1) | IL272573B2 (https=) |
| JO (1) | JOP20200059A1 (https=) |
| MA (1) | MA50173A (https=) |
| MX (2) | MX2020002696A (https=) |
| PE (1) | PE20200924A1 (https=) |
| PH (1) | PH12020500446A1 (https=) |
| SA (1) | SA520411524B1 (https=) |
| SG (1) | SG11202001377PA (https=) |
| TW (1) | TWI790281B (https=) |
| UY (1) | UY37879A (https=) |
| WO (1) | WO2019055590A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20200924A1 (es) | 2017-09-13 | 2020-09-14 | Amgen Inc | Compuestos de bisamida sustituida que activan el sarcomero cardiaco |
| US11584714B2 (en) | 2018-05-29 | 2023-02-21 | Omeros Corporation | MASP-2 inhibitors and methods of use |
| IL311042B1 (en) * | 2018-05-29 | 2026-04-01 | Omeros Corp | MASP-2 inhibitors and methods of use |
| US20220185791A1 (en) * | 2019-03-12 | 2022-06-16 | Amgen Inc. | Polymorphs of a cardiac troponin activator |
| SG11202109891WA (en) * | 2019-03-12 | 2021-10-28 | Amgen Inc | Polymorphs and cocrystals of a cardiac troponin activator |
| CN118561817A (zh) * | 2019-07-23 | 2024-08-30 | 拜耳公司 | 作为农药的新的杂芳基-三唑化合物 |
| EP4069676A1 (en) | 2019-12-04 | 2022-10-12 | Omeros Corporation | Masp-2 inhibitors and methods of use |
| IL293588B1 (en) | 2019-12-04 | 2026-04-01 | Omeros Corp | 3-Amino-1-methylpyrazin-2(H1)-one derivatives as MASP-2 inhibitors, compositions containing them and uses thereof |
| BR112022010895A2 (pt) | 2019-12-04 | 2022-09-06 | Omeros Corp | Composto, composição farmacêutica, e, método para tratar uma doença ou distúrbio associado à serina protease-2 associada à lectina de ligação ao manan |
| EP4069678A1 (en) | 2019-12-04 | 2022-10-12 | Omeros Corporation | Masp-2 inhibitors and methods of use |
| US11802122B2 (en) * | 2020-06-17 | 2023-10-31 | Merck Sharp & Dohme Llc | 2-oxoimidazolidine-4-carboxamides as NAv1.8 inhibitors |
| AU2022239717A1 (en) | 2021-03-15 | 2023-11-02 | Maze Therapeutics, Inc. | Inhibitors of glycogen synthase 1 (gys1) and methods of use thereof |
| WO2023122325A2 (en) * | 2021-12-23 | 2023-06-29 | Regents Of The University Of Michigan | Meta anilide compounds and methods for use of the same to treat diseases and disorders |
| JP2025534288A (ja) | 2022-09-26 | 2025-10-15 | エッジワイズ セラピューティクス， インコーポレイテッド | １，４－ジヒドロキナゾリノン化合物およびその使用 |
| WO2024206339A1 (en) | 2023-03-27 | 2024-10-03 | Edgewise Therapeutics, Inc. | Quinolinone amide compounds and uses thereof |
| EP4688756A1 (en) | 2023-03-27 | 2026-02-11 | Edgewise Therapeutics, Inc. | Quinazoline dione compounds and uses thereof |
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| AU2018294254C1 (en) | 2017-06-30 | 2022-10-13 | Amgen Inc. | Synthesis of omecamtiv mecarbil |
| PE20200924A1 (es) | 2017-09-13 | 2020-09-14 | Amgen Inc | Compuestos de bisamida sustituida que activan el sarcomero cardiaco |
| PT3594199T (pt) | 2018-07-09 | 2020-09-04 | Amgen Inc | 2-fluoro-3-nitrotolueno cristalino e processo para a sua preparação |
| MA53226A (fr) | 2018-08-17 | 2021-11-24 | Amgen Inc | Sel et formes cristallines d'omecamtiv mecarbil |
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| US20220185791A1 (en) | 2019-03-12 | 2022-06-16 | Amgen Inc. | Polymorphs of a cardiac troponin activator |
| SG11202109891WA (en) | 2019-03-12 | 2021-10-28 | Amgen Inc | Polymorphs and cocrystals of a cardiac troponin activator |
-
2018
- 2018-09-13 PE PE2020000339A patent/PE20200924A1/es unknown
- 2018-09-13 MA MA050173A patent/MA50173A/fr unknown
- 2018-09-13 CA CA3075669A patent/CA3075669A1/en active Pending
- 2018-09-13 US US16/129,862 patent/US10723720B2/en active Active
- 2018-09-13 AR ARP180102603A patent/AR112804A1/es unknown
- 2018-09-13 IL IL272573A patent/IL272573B2/en unknown
- 2018-09-13 CR CR20200116A patent/CR20200116A/es unknown
- 2018-09-13 BR BR112020004800-3A patent/BR112020004800A2/pt not_active Application Discontinuation
- 2018-09-13 EA EA202090688A patent/EA202090688A1/ru unknown
- 2018-09-13 CN CN201880072907.5A patent/CN111601798B/zh active Active
- 2018-09-13 UY UY0001037879A patent/UY37879A/es not_active Application Discontinuation
- 2018-09-13 TW TW107132171A patent/TWI790281B/zh active
- 2018-09-13 JO JOP/2020/0059A patent/JOP20200059A1/ar unknown
- 2018-09-13 MX MX2020002696A patent/MX2020002696A/es unknown
- 2018-09-13 WO PCT/US2018/050793 patent/WO2019055590A1/en not_active Ceased
- 2018-09-13 JP JP2020514579A patent/JP7308816B2/ja active Active
- 2018-09-13 KR KR1020207010115A patent/KR20200054237A/ko not_active Abandoned
- 2018-09-13 SG SG11202001377PA patent/SG11202001377PA/en unknown
- 2018-09-13 AU AU2018332887A patent/AU2018332887B2/en not_active Ceased
- 2018-09-13 EP EP18783202.7A patent/EP3681882A1/en not_active Withdrawn
-
2020
- 2020-03-05 PH PH12020500446A patent/PH12020500446A1/en unknown
- 2020-03-10 CO CONC2020/0002745A patent/CO2020002745A2/es unknown
- 2020-03-10 CL CL2020000610A patent/CL2020000610A1/es unknown
- 2020-03-10 MX MX2022014864A patent/MX2022014864A/es unknown
- 2020-03-12 SA SA520411524A patent/SA520411524B1/ar unknown
- 2020-03-27 US US16/833,321 patent/US11254658B2/en not_active Expired - Fee Related
- 2020-03-27 US US16/833,336 patent/US10899746B2/en active Active
- 2020-10-12 US US17/068,518 patent/US11299479B1/en active Active
-
2022
- 2022-02-15 US US17/672,594 patent/US11780826B2/en active Active
-
2023
- 2023-08-17 US US18/451,757 patent/US20240158372A1/en not_active Abandoned
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