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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- 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) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018302178A1 (en) | 2017-07-18 | 2020-02-13 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| WO2019232223A1 (en) * | 2018-05-30 | 2019-12-05 | University Of Notre Dame Du Lac | Hsp90 beta 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 |
| CN115181092B (zh) * | 2018-08-17 | 2024-05-03 | 迪哲(江苏)医药股份有限公司 | 吡嗪化合物和其用途 |
| WO2020035052A1 (en) * | 2018-08-17 | 2020-02-20 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Pyrazine compounds and uses thereof |
| US20210395226A1 (en) * | 2018-12-28 | 2021-12-23 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Substituted aryl compound and preparation method therefor and use thereof |
| 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 |
| CA3126704A1 (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 |
| KR20210116550A (ko) | 2019-01-18 | 2021-09-27 | 누베이션 바이오 인크. | 아데노신 길항제로서의 헤테로시클릭 화합물 |
| CN114286820A (zh) * | 2019-08-21 | 2022-04-05 | 卡尔维斯塔制药有限公司 | 酶抑制剂 |
| EP4167982A4 (en) | 2020-06-22 | 2024-08-07 | PMV Pharmaceuticals, Inc. | METHODS AND COMPOUNDS FOR RESTORING FUNCTION OF P53 MUTANTS |
| KR102646627B1 (ko) * | 2021-03-24 | 2024-03-13 | 주식회사 스탠다임 | 아데노신 a2a 수용체 및 아데노신 a2b 수용체의 이중 길항제, 및 이의 용도 |
| WO2022268520A1 (de) * | 2021-06-21 | 2022-12-29 | Bayer Aktiengesellschaft | Verwendung von substituierten pyrrolidinonen oder deren salzen zur steigerung der stresstoleranz in pflanzen. |
| US12492178B2 (en) | 2021-09-01 | 2025-12-09 | Empathbio, Inc. | Stable polymorph of R-MDMA HCl |
| 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 |
| EP4634192A1 (en) * | 2022-12-12 | 2025-10-22 | Avelos Therapeutics Inc. | Substituted heterocyclic compound derivatives and their pharmaceutical use |
| TW202509019A (zh) * | 2023-04-27 | 2025-03-01 | 香港商維泰瑞隆（香港）生物科技有限公司 | Sarm1調節子、其製劑及用途 |
| 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 |
Family Cites Families (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| USRE47351E1 (en) | 1999-06-22 | 2019-04-16 | Gilead Sciences, Inc. | 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists |
| WO2003030909A1 (en) * | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| US6992087B2 (en) | 2001-11-21 | 2006-01-31 | Pfizer Inc | Substituted aryl 1,4-pyrazine derivatives |
| DK1603570T5 (da) | 2003-02-26 | 2013-12-09 | Sugen Inc | Aminoheteroarylforbindelser som proteinkinaseinhibitorer |
| CN1791580A (zh) * | 2003-03-24 | 2006-06-21 | 麦克公司 | 联芳基取代的6元杂环钠通道阻滞剂 |
| EP1678160A1 (en) * | 2003-10-27 | 2006-07-12 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| ATE452890T1 (de) | 2003-11-04 | 2010-01-15 | Merck & Co Inc | Substituierte naphthyridinonderivate |
| ES2270715B1 (es) | 2005-07-29 | 2008-04-01 | Laboratorios Almirall S.A. | Nuevos derivados de pirazina. |
| GB0800741D0 (en) * | 2008-01-16 | 2008-02-20 | Univ Greenwich | Cyclic triazo and diazo sodium channel blockers |
| AU2009209633C1 (en) | 2008-02-01 | 2014-01-23 | Akinion Pharmaceuticals Ab | Pyrazine derivatives and their use as protein kinase inhbitors |
| RU2506267C2 (ru) | 2008-03-31 | 2014-02-10 | Дженентек, Инк. | Бензопирановые и бензоксепиновые ингибиторы рi3k и их применение |
| WO2010088177A1 (en) | 2009-02-02 | 2010-08-05 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| US8809525B2 (en) * | 2010-02-05 | 2014-08-19 | Heptares Therapeutics Limited | 1,2,4-triazine-4-amine derivatives |
| SG186989A1 (en) | 2010-07-14 | 2013-02-28 | Novartis Ag | Ip receptor agonist heterocyclic compounds |
| WO2012168358A1 (en) | 2011-06-09 | 2012-12-13 | Novaled Ag | Compound for organic electronic device |
| JP6073923B2 (ja) | 2012-01-13 | 2017-02-01 | ノバルティス アーゲー | 肺動脈高血圧症（ｐａｈ）および関連障害の治療のためのｉｐ受容体アゴニストとしての縮合ピロール |
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| CN105377851B (zh) | 2013-03-11 | 2018-07-20 | 密执安州立大学董事会 | Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法 |
| EP3842424B1 (en) | 2013-03-15 | 2024-12-11 | The Trustees of Columbia University in the City of New York | Map kinase modulators and uses thereof in the tretament of tauopathies |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| CN104341386A (zh) * | 2013-07-23 | 2015-02-11 | 中国科学院上海药物研究所 | 一类芳基杂环小分子化合物、其衍生物及其制备方法和用途 |
| WO2015017335A1 (en) | 2013-07-30 | 2015-02-05 | Boehringer Ingelheim International Gmbh | Azaindole compounds as modulators of rorc |
| RU2720237C2 (ru) | 2013-11-18 | 2020-04-28 | Форма Терапеутикс, Инк. | Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет |
| DK3071203T3 (da) | 2013-11-18 | 2021-03-15 | Forma Therapeutics Inc | Tetrahydroquinolinsammensætninger som bet-bromdomæne-inhibitorer |
| WO2015131005A1 (en) | 2014-02-28 | 2015-09-03 | The Regents Of The University Of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| KR20170083136A (ko) | 2014-11-18 | 2017-07-17 | 머크 샤프 앤드 돔 코포레이션 | A2a 길항제 특성을 갖는 아미노피라진 화합물 |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| EP3262045A1 (en) | 2015-02-27 | 2018-01-03 | The Regents of The University of Michigan | 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors |
| WO2016203112A1 (en) | 2015-06-16 | 2016-12-22 | Orion Corporation | Spiro[cyclobutane-1,3'-indolin]-2'-one derivatives as bromodomain inhibitors |
| SG10202111808WA (en) | 2015-08-11 | 2021-11-29 | Novartis Ag | 5-bromo-2,6-di-(1h-pyrazol-1-yl)pyrimidin-4-amine for use in the treatment of cancer |
| CA3129180A1 (en) | 2015-09-21 | 2017-03-30 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| KR20180052762A (ko) | 2015-09-22 | 2018-05-18 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 브로모도메인 억제제로서 사용하기 위한 피리디논 디카르복스아미드 |
| CN108883107A (zh) | 2015-12-24 | 2018-11-23 | 科尔沃斯制药股份有限公司 | 治疗癌症的方法 |
| EA201990189A1 (ru) | 2016-07-01 | 2019-06-28 | Г1 Терапьютикс, Инк. | Синтез n-(гетероарил)пирроло[3,2-d]пиримидин-2-аминов |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| KR20190025943A (ko) | 2016-07-01 | 2019-03-12 | 쥐원 쎄라퓨틱스, 인크. | 피리미딘-기재 항증식제 |
| GB201612092D0 (en) | 2016-07-12 | 2016-08-24 | Almac Discovery Ltd | Pharmaceutical compounds |
| WO2018081863A1 (en) | 2016-11-04 | 2018-05-11 | University Of Wollongong | 6-SUBSTITUTED DERIVATIVES OF HEXAMETHYLENE AMILORIDE AS INHIBITORS OF uPA AND USES THEREOF |
| MX389798B (es) | 2017-01-20 | 2025-03-20 | Arcus Biosciences Inc | Azolopirimidina para el tratamiento de trastornos relacionados con el cáncer. |
| TWI801372B (zh) | 2017-03-30 | 2023-05-11 | 比利時商艾特歐斯比利時有限公司 | 作為a2a抑制劑的硫胺甲酸酯衍生物以及用於癌症治療的方法 |
| LT3601296T (lt) | 2017-03-30 | 2022-09-26 | iTeos Belgium SA | 2-okso-tiazolo derivatai kaip a2a inhibitoriai ir junginiai, skirti naudoti gydant vėžį |
| CN107221611B (zh) | 2017-06-15 | 2019-02-05 | 江西冠能光电材料有限公司 | 一种稳定易加工有机半导体材料及其有机发光器件应用 |
| JP2020525472A (ja) | 2017-06-30 | 2020-08-27 | ライブ・セラピューティクス・スプウカ・アクツィーナＲｙｖｕ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｓ．Ａ． | アデノシンａ２ａ受容体のイミダゾ［１，２−ａ］ピラジン調節剤 |
| AU2018302178A1 (en) | 2017-07-18 | 2020-02-13 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| WO2019090347A1 (en) | 2017-11-06 | 2019-05-09 | Corvus Pharmaceuticals Inc. | Adenosine pathway inhibitors for cancer treatment |
| CN109810111B (zh) | 2017-11-20 | 2023-10-27 | 上海医药集团股份有限公司 | 一种吡唑酮并嘧啶类化合物、其制备方法及应用 |
| US11498923B2 (en) | 2017-12-13 | 2022-11-15 | Merck Sharp & Dohme Llc | Substituted imidazo[1,2-c]quinazolines as A2A antagonists |
| IL275478B2 (en) | 2017-12-20 | 2024-06-01 | Betta Pharmaceuticals Co Ltd | A preparation that functions as a bromodomain protein inhibitor, and the composition |
| CN111315747B (zh) | 2018-01-05 | 2023-05-02 | 四川科伦博泰生物医药股份有限公司 | 二氢吡唑酮并嘧啶类化合物及其制备方法和用途 |
| EP3741758A1 (en) | 2018-01-16 | 2020-11-25 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences | Bromodomain inhibitor compound and use thereof |
| CA3088381A1 (en) | 2018-01-29 | 2019-08-01 | Beta Pharma, Inc. | 2h-indazole derivatives as cdk4 and cdk6 inhibitors and therapeutic uses thereof |
| CA3089159A1 (en) | 2018-02-06 | 2019-08-15 | Jiangsu Hengrui Medicine Co., Ltd. | Pyrazolo[1,5-a][1,3,5]triazine-2-amine derivative, preparation method therefor and medical use thereof |
| EP3752600A1 (en) | 2018-02-13 | 2020-12-23 | Iovance Biotherapeutics, Inc. | Expansion of tumor infiltrating lymphocytes (tils) with adenosine a2a receptor antagonists and therapeutic combinations of tils and adenosine a2a receptor antagonists |
| CN111989313A (zh) | 2018-02-15 | 2020-11-24 | 杭州阿诺生物医药科技有限公司 | A2a和/或a2b受体拮抗剂 |
| US11479555B2 (en) | 2018-02-23 | 2022-10-25 | Newave Pharmaceutical Inc. | Substituted 1,2-dihydro-3H-pyrazolo[3,4-D]pyrimidin-3-ones as inhibitors of WEE-1 kinase |
| MA52422A (fr) | 2018-02-27 | 2021-01-06 | Incyte Corp | Imidazopyrimidines et triazolopyrimidines en tant qu'inhibiteurs a2a/a2b |
| WO2019169065A2 (en) | 2018-02-28 | 2019-09-06 | The Regents Of The University Of Colorado, A Body Corporate | Wee1 kinase inhibitors and methods of treating cancer using the same |
| EP3762385B1 (en) | 2018-03-09 | 2025-02-12 | Recurium IP Holdings, LLC | Substituted 1,2-dihydro-3h-pyrazolo[3,4-d]pyrimidin-3-ones |
| US11220510B2 (en) | 2018-04-09 | 2022-01-11 | Incyte Corporation | Pyrrole tricyclic compounds as A2A / A2B inhibitors |
| WO2020035052A1 (en) | 2018-08-17 | 2020-02-20 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Pyrazine compounds and uses thereof |
| TWI820209B (zh) | 2018-09-12 | 2023-11-01 | 大陸商迪哲（江蘇）醫藥股份有限公司 | 三唑并－嘧啶化合物及其用途 |
| US11254670B2 (en) | 2019-01-18 | 2022-02-22 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| KR20210116550A (ko) | 2019-01-18 | 2021-09-27 | 누베이션 바이오 인크. | 아데노신 길항제로서의 헤테로시클릭 화합물 |
-
2018
- 2018-07-18 WO PCT/US2018/042777 patent/WO2019018584A1/en not_active Ceased
- 2018-07-18 CA CA3070273A patent/CA3070273A1/en active Pending
- 2018-07-18 SG SG11202000418XA patent/SG11202000418XA/en unknown
- 2018-07-18 AU AU2018302179A patent/AU2018302179A1/en not_active Abandoned
- 2018-07-18 JP JP2020502984A patent/JP2020527588A/ja active Pending
- 2018-07-18 KR KR1020207004248A patent/KR20200041315A/ko not_active Ceased
- 2018-07-18 MX MX2020000690A patent/MX2020000690A/es unknown
- 2018-07-18 EP EP18834623.3A patent/EP3654978A4/en not_active Withdrawn
- 2018-07-18 CN CN201880059365.8A patent/CN111163780A/zh active Pending
- 2018-07-18 US US16/039,307 patent/US11028058B2/en not_active Expired - Fee Related
-
2020
- 2020-01-15 IL IL272056A patent/IL272056A/en unknown
-
2021
- 2021-02-12 US US17/175,159 patent/US20210292285A1/en not_active Abandoned
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