JP2020527588A5 - - Google Patents
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- JP2020527588A5 JP2020527588A5 JP2020502984A JP2020502984A JP2020527588A5 JP 2020527588 A5 JP2020527588 A5 JP 2020527588A5 JP 2020502984 A JP2020502984 A JP 2020502984A JP 2020502984 A JP2020502984 A JP 2020502984A JP 2020527588 A5 JP2020527588 A5 JP 2020527588A5
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- JP
- Japan
- Prior art keywords
- alkylene
- optionally
- alkyl
- halogen
- substituted
- 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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- 229910052736 halogen Inorganic materials 0.000 claims 63
- 150000002367 halogens Chemical class 0.000 claims 61
- 150000001875 compounds Chemical class 0.000 claims 51
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 43
- 150000003839 salts Chemical class 0.000 claims 42
- 125000000623 heterocyclic group Chemical group 0.000 claims 41
- 229910052739 hydrogen Inorganic materials 0.000 claims 30
- 239000001257 hydrogen Substances 0.000 claims 30
- 150000002431 hydrogen Chemical class 0.000 claims 28
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims 20
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 11
- 125000004429 atom Chemical group 0.000 claims 9
- -1 4-hydroxy-2-pyridyl Chemical group 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 5
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 102000009346 Adenosine receptors Human genes 0.000 claims 2
- 108050000203 Adenosine receptors Proteins 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000019491 signal transduction Effects 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims 1
- 125000004520 1,3,4-thiadiazolyl group Chemical group 0.000 claims 1
- WSPWLDRXZSCRNX-UHFFFAOYSA-N 2-[6-amino-3-(1-ethyl-2-methylbenzimidazol-5-yl)pyrazin-2-yl]-4-fluorophenol Chemical compound NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C1=CC2=C(N(C(=N2)C)CC)C=C1 WSPWLDRXZSCRNX-UHFFFAOYSA-N 0.000 claims 1
- GZSRKKZHGRCQSR-UHFFFAOYSA-N 5,6-bis(1-phenylbenzimidazol-2-yl)pyrazine-2,3-diamine Chemical compound N=1C2=CC=CC=C2N(C=2C=CC=CC=2)C=1C=1N=C(N)C(N)=NC=1C1=NC2=CC=CC=C2N1C1=CC=CC=C1 GZSRKKZHGRCQSR-UHFFFAOYSA-N 0.000 claims 1
- VATHFNVYAXGLOH-UHFFFAOYSA-N 5-(1-benzofuran-2-yl)-6-pyridin-4-ylpyrazine-2,3-diamine Chemical compound N1=C(N)C(N)=NC(C=2OC3=CC=CC=C3C=2)=C1C1=CC=NC=C1 VATHFNVYAXGLOH-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- XTCSOMYEISLLGM-UHFFFAOYSA-N C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C1=C(C=CC(=C1)F)OCC1=CC=CC=C1)N Chemical compound C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C1=C(C=CC(=C1)F)OCC1=CC=CC=C1)N XTCSOMYEISLLGM-UHFFFAOYSA-N 0.000 claims 1
- ULYJAQHOOLJROK-UHFFFAOYSA-N C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C1=CSC=C1)N Chemical compound C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C1=CSC=C1)N ULYJAQHOOLJROK-UHFFFAOYSA-N 0.000 claims 1
- GDAGEGPJSKKPKO-UHFFFAOYSA-N C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C1=NNC=C1)N Chemical compound C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C1=NNC=C1)N GDAGEGPJSKKPKO-UHFFFAOYSA-N 0.000 claims 1
- BDCSVEBCBFILPW-UHFFFAOYSA-N C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1C=NC=CC=1)N Chemical compound C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1C=NC=CC=1)N BDCSVEBCBFILPW-UHFFFAOYSA-N 0.000 claims 1
- KKZRWALWHDLSNI-UHFFFAOYSA-N C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1N=NNN=1)N Chemical compound C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1N=NNN=1)N KKZRWALWHDLSNI-UHFFFAOYSA-N 0.000 claims 1
- VUQVIEGJXVFQJL-UHFFFAOYSA-N C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1NC=CC=1)N Chemical compound C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1NC=CC=1)N VUQVIEGJXVFQJL-UHFFFAOYSA-N 0.000 claims 1
- XIFWKZBZIFTDNV-UHFFFAOYSA-N C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1SC=CC=1)N Chemical compound C(C)N1C=CC2=CC(=CC=C12)C=1N=CC(=NC=1C=1SC=CC=1)N XIFWKZBZIFTDNV-UHFFFAOYSA-N 0.000 claims 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 claims 1
- BZECPQWTJYCJJS-UHFFFAOYSA-N NC1=CN=C(C(=N1)C1=C(C(=CC=C1)F)O)C=1C=C2C=CN(C2=CC=1)CC Chemical compound NC1=CN=C(C(=N1)C1=C(C(=CC=C1)F)O)C=1C=C2C=CN(C2=CC=1)CC BZECPQWTJYCJJS-UHFFFAOYSA-N 0.000 claims 1
- HLVLCNODTJFDCE-UHFFFAOYSA-N NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C1=CC2=C(N(C=N2)CC)C=C1 Chemical compound NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C1=CC2=C(N(C=N2)CC)C=C1 HLVLCNODTJFDCE-UHFFFAOYSA-N 0.000 claims 1
- FCLPIEXRCIDCKO-UHFFFAOYSA-N NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C=1C=C2C=C(N(C2=CC=1)CC)C Chemical compound NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C=1C=C2C=C(N(C2=CC=1)CC)C FCLPIEXRCIDCKO-UHFFFAOYSA-N 0.000 claims 1
- OHHDJAVAPINJTO-UHFFFAOYSA-N NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C=1C=C2C=C(N(C2=CC=1)CC)F Chemical compound NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C=1C=C2C=C(N(C2=CC=1)CC)F OHHDJAVAPINJTO-UHFFFAOYSA-N 0.000 claims 1
- NSEWVNUFDDTVMQ-UHFFFAOYSA-N NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C=1C=C2C=CN(C2=CC=1)CC Chemical compound NC1=CN=C(C(=N1)C1=C(C=CC(=C1)F)O)C=1C=C2C=CN(C2=CC=1)CC NSEWVNUFDDTVMQ-UHFFFAOYSA-N 0.000 claims 1
- RPJXABBAMJZJHB-UHFFFAOYSA-N NC1=CN=C(C(=N1)C1=C(C=CC=C1)O)C=1C=C2C=CN(C2=CC=1)CC Chemical compound NC1=CN=C(C(=N1)C1=C(C=CC=C1)O)C=1C=C2C=CN(C2=CC=1)CC RPJXABBAMJZJHB-UHFFFAOYSA-N 0.000 claims 1
- HGLFIOCEQKDUOS-UHFFFAOYSA-N NC1=CN=C(C(=N1)C=1C(NC=CC=1)=O)C=1C=C2C=CN(C2=CC=1)CC Chemical compound NC1=CN=C(C(=N1)C=1C(NC=CC=1)=O)C=1C=C2C=CN(C2=CC=1)CC HGLFIOCEQKDUOS-UHFFFAOYSA-N 0.000 claims 1
- BOEVZQZKJSXIBZ-UHFFFAOYSA-N NC1=CN=C(C(=N1)C=1C(NC=NC=1)=O)C=1C=C2C=CN(C2=CC=1)CC Chemical compound NC1=CN=C(C(=N1)C=1C(NC=NC=1)=O)C=1C=C2C=CN(C2=CC=1)CC BOEVZQZKJSXIBZ-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229960005305 adenosine Drugs 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 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
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 0 Bc1c(*)nc(*)c(N*)n1 Chemical compound Bc1c(*)nc(*)c(N*)n1 0.000 description 2
- XJACKVVDISNTEQ-UHFFFAOYSA-N CC(C)c(cc1Cl)cc2c1nccc2 Chemical compound CC(C)c(cc1Cl)cc2c1nccc2 XJACKVVDISNTEQ-UHFFFAOYSA-N 0.000 description 1
- DWRZYRXRHJUAFM-UHFFFAOYSA-N CC(C)c1cc(Cl)c2[nH]cnc2c1 Chemical compound CC(C)c1cc(Cl)c2[nH]cnc2c1 DWRZYRXRHJUAFM-UHFFFAOYSA-N 0.000 description 1
- WBVWBHXCNQGIQO-UHFFFAOYSA-N CC(C)c1ccc2[nH]c(C)nc2c1 Chemical compound CC(C)c1ccc2[nH]c(C)nc2c1 WBVWBHXCNQGIQO-UHFFFAOYSA-N 0.000 description 1
- RFPOYGARIHBHDV-UHFFFAOYSA-N CC(C)c1ccc2[nH]cnc2c1 Chemical compound CC(C)c1ccc2[nH]cnc2c1 RFPOYGARIHBHDV-UHFFFAOYSA-N 0.000 description 1
- KDBNTZILRWFICA-UHFFFAOYSA-N CC(C)c1ccc2[o]cnc2c1 Chemical compound CC(C)c1ccc2[o]cnc2c1 KDBNTZILRWFICA-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762534176P | 2017-07-18 | 2017-07-18 | |
| US62/534,176 | 2017-07-18 | ||
| PCT/US2018/042777 WO2019018584A1 (en) | 2017-07-18 | 2018-07-18 | HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020527588A JP2020527588A (ja) | 2020-09-10 |
| JP2020527588A5 true JP2020527588A5 (enExample) | 2021-08-26 |
Family
ID=65014543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020502984A Pending JP2020527588A (ja) | 2017-07-18 | 2018-07-18 | アデノシンアンタゴニストとしてのヘテロ環式化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11028058B2 (enExample) |
| EP (1) | EP3654978A4 (enExample) |
| JP (1) | JP2020527588A (enExample) |
| KR (1) | KR20200041315A (enExample) |
| CN (1) | CN111163780A (enExample) |
| AU (1) | AU2018302179A1 (enExample) |
| CA (1) | CA3070273A1 (enExample) |
| IL (1) | IL272056A (enExample) |
| MX (1) | MX2020000690A (enExample) |
| SG (1) | SG11202000418XA (enExample) |
| WO (1) | WO2019018584A1 (enExample) |
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| US12030867B2 (en) | 2018-05-30 | 2024-07-09 | University Of Notre Dame Du Lac | Hsp90β selective inhibitors |
| CN110655509B (zh) * | 2018-06-29 | 2023-01-24 | 江苏恒瑞医药股份有限公司 | 2-胺基嘧啶类衍生物、其制备方法及其在医药上的应用 |
| CN111094254B (zh) * | 2018-07-12 | 2022-07-26 | 江苏恒瑞医药股份有限公司 | 杂芳基类衍生物、其制备方法及其在医药上的应用 |
| AU2019323035B2 (en) * | 2018-08-17 | 2024-11-07 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Pyrazine compounds and uses thereof |
| CN112279837B (zh) * | 2018-08-17 | 2022-08-09 | 迪哲(江苏)医药股份有限公司 | 吡嗪化合物和其用途 |
| CN113166119B (zh) * | 2018-12-28 | 2024-01-05 | 四川科伦博泰生物医药股份有限公司 | 取代芳基化合物及其制备方法和用途 |
| CN111377906B (zh) * | 2018-12-28 | 2022-09-02 | 四川科伦博泰生物医药股份有限公司 | 取代的吡嗪化合物及其制备方法和用途 |
| WO2020150674A1 (en) * | 2019-01-18 | 2020-07-23 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
| US11254670B2 (en) | 2019-01-18 | 2022-02-22 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| CA3126704A1 (en) * | 2019-01-18 | 2020-07-23 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
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| WO2022268520A1 (de) * | 2021-06-21 | 2022-12-29 | Bayer Aktiengesellschaft | Verwendung von substituierten pyrrolidinonen oder deren salzen zur steigerung der stresstoleranz in pflanzen. |
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| WO2023064585A1 (en) * | 2021-10-14 | 2023-04-20 | Vanderbilt University | 7,8-dihydro-5h-1,6-naphthyridine derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor m4 for treating neurological and psychiatric disorders |
| CN113968824B (zh) * | 2021-11-29 | 2024-01-19 | 郑州大学 | 一种2,3,5-三取代吡嗪类化合物及其制备方法和应用 |
| US11912680B2 (en) | 2021-12-28 | 2024-02-27 | Empathbio, Inc. | Nitric oxide releasing prodrugs of MDA and MDMA |
| AU2023397123A1 (en) * | 2022-12-12 | 2025-02-13 | Avelos Therapeutics Inc. | Substituted heterocyclic compound derivatives and their pharmaceutical use |
| CN121399112A (zh) * | 2023-04-27 | 2026-01-23 | 维泰瑞隆有限公司 | Sarm1调节剂、其制备和用途 |
| WO2025036840A1 (en) * | 2023-08-11 | 2025-02-20 | Almirall, S.A. | Pyridine or pyrazine derivatives as collagen vii (c7) inducers and their use in therapy |
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2018
- 2018-07-18 JP JP2020502984A patent/JP2020527588A/ja active Pending
- 2018-07-18 CN CN201880059365.8A patent/CN111163780A/zh active Pending
- 2018-07-18 SG SG11202000418XA patent/SG11202000418XA/en unknown
- 2018-07-18 CA CA3070273A patent/CA3070273A1/en active Pending
- 2018-07-18 US US16/039,307 patent/US11028058B2/en not_active Expired - Fee Related
- 2018-07-18 MX MX2020000690A patent/MX2020000690A/es unknown
- 2018-07-18 KR KR1020207004248A patent/KR20200041315A/ko not_active Ceased
- 2018-07-18 WO PCT/US2018/042777 patent/WO2019018584A1/en not_active Ceased
- 2018-07-18 EP EP18834623.3A patent/EP3654978A4/en not_active Withdrawn
- 2018-07-18 AU AU2018302179A patent/AU2018302179A1/en not_active Abandoned
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2020
- 2020-01-15 IL IL272056A patent/IL272056A/en unknown
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2021
- 2021-02-12 US US17/175,159 patent/US20210292285A1/en not_active Abandoned