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 |
|---|---|---|---|---|
| MX2020000693A (es) | 2017-07-18 | 2020-07-29 | Nuvation Bio Inc | Compuestos de 1,8-naftiridinona, y usos de los mismos. |
| 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 |
| KR102816365B1 (ko) * | 2018-08-17 | 2025-06-02 | 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 | 피라진 화합물 및 이의 용도 |
| 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 |
| 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 |
| EP3904352A4 (en) * | 2018-12-28 | 2022-09-07 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | SUBSTITUTED ARYL COMPOUND, METHOD OF MANUFACTURE THEREOF AND USE THEREOF |
| AU2020208644A1 (en) * | 2019-01-18 | 2021-08-26 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
| AU2020207952A1 (en) * | 2019-01-18 | 2021-08-26 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
| WO2020150676A1 (en) | 2019-01-18 | 2020-07-23 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
| AU2019462140A1 (en) * | 2019-08-21 | 2022-02-24 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
| WO2021262596A1 (en) | 2020-06-22 | 2021-12-30 | Pmv Pharmaceuticals, Inc. | Methods and compounds for restoring mutant p53 function |
| 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 |
| CN118206499A (zh) * | 2021-11-29 | 2024-06-18 | 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 |
| WO2023129958A2 (en) | 2021-12-28 | 2023-07-06 | ATAI Life Sciences AG | 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 |
| EP4702017A1 (en) * | 2023-04-27 | 2026-03-04 | Sironax Ltd | Sarm1 modulators, preparations, and uses thereof |
| 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 |
| GEP20084341B (en) | 2003-02-26 | 2008-03-25 | Sugen Inc | Aminoheteroaryl compounds as protein kinase inhibitors |
| US20060293339A1 (en) | 2003-03-24 | 2006-12-28 | Chakravarty Prasun K | Biaryl substituted 6-membered heterocycles as sodium channel blockers |
| EP1678160A1 (en) | 2003-10-27 | 2006-07-12 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| DE602004024814D1 (de) | 2003-11-04 | 2010-02-04 | 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 |
| CA2713553A1 (en) | 2008-02-01 | 2009-08-06 | Akinion Pharmaceuticals Ab | Pyrazine derivatives and their use as protein kinase inhibitors |
| CL2009000780A1 (es) | 2008-03-31 | 2010-01-15 | Genentech Inc | Compuestos derivados de heterociclil-pirano-heterociclilo, heterociclil-oxepina-heterociclilo, benzopirano-heterociclilo y benzoxepina-heterociclilo sustituidos; composicion farmaceutica; procedimiento de preparacion de la composicion; kit farmaceutico; y su uso en el tratamiento del cancer, mediado por la inhibicion de pi3k. |
| WO2010088177A1 (en) | 2009-02-02 | 2010-08-05 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| RU2625791C2 (ru) * | 2010-02-05 | 2017-07-19 | Хептейрес Терапьютикс Лимитед | Производные 1,2,4-триазин-4-амина |
| MA34373B1 (fr) | 2010-07-14 | 2013-07-03 | Novartis Ag | Composés hétérocycliques agonistes du récepteur ip |
| WO2012168358A1 (en) | 2011-06-09 | 2012-12-13 | Novaled Ag | Compound for organic electronic device |
| ES2565826T3 (es) | 2012-01-13 | 2016-04-07 | Novartis Ag | Pirroles fusionados como agonistas del receptor IP para el tratamiento de hipertensión arterial pulmonar (PAH) y trastornos relacionados |
| 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 |
| EP2970312B1 (en) | 2013-03-11 | 2017-11-15 | The Regents of The University of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| 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 |
| SG11201510409QA (en) | 2013-06-21 | 2016-01-28 | Zenith Epigenetics Corp | Novel bicyclic bromodomain inhibitors |
| 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 |
| EP3027616B1 (en) | 2013-07-30 | 2018-01-10 | Boehringer Ingelheim International GmbH | Azaindole compounds as modulators of rorc |
| WO2015074064A2 (en) | 2013-11-18 | 2015-05-21 | Bair Kenneth W | Tetrahydroquinoline compositions as bet bromodomain inhibitors |
| US9422281B2 (en) | 2013-11-18 | 2016-08-23 | Forma Therapeutics, Inc. | Benzopiperazine compositions as BET bromodomain inhibitors |
| US9580430B2 (en) | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
| US10472347B2 (en) | 2014-11-18 | 2019-11-12 | Merck Sharp & Dohme Corp. | Aminopyrazine compounds with A2A antagonist properties |
| JP2017537946A (ja) | 2014-12-11 | 2017-12-21 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての置換複素環 |
| WO2016138332A1 (en) | 2015-02-27 | 2016-09-01 | The Regents Of The University Of Michigan | 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors |
| CA2988209A1 (en) | 2015-06-16 | 2016-12-22 | Orion Corporation | Spiro[cyclobutane-1,3'-indolin]-2'-one derivatives as bromodomain inhibitors |
| PH12018500284B1 (en) | 2015-08-11 | 2023-08-16 | Novartis Ag | 5-bromo-2,6-di-(1h-pyrazol-1-yl)pyrimidin-4-amine for use in the treatment of cancer |
| SG10201912386RA (en) | 2015-09-21 | 2020-02-27 | Plexxikon Inc | Heterocyclic compounds and uses thereof |
| AU2016326864A1 (en) | 2015-09-22 | 2018-03-22 | Glaxosmithkline Intellectual Property (No.2) Limited | Pyridinone dicarboxamide for use as bromodomain inhibitors |
| CA3009527C (en) | 2015-12-24 | 2024-01-09 | Stephen WILLINGHAM | Methods of treating cancer |
| CN109789142B (zh) | 2016-07-01 | 2022-08-23 | G1治疗公司 | N-(杂芳基)-吡咯并[3,2-d]嘧啶-2-胺的合成 |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| EA201990187A1 (ru) | 2016-07-01 | 2019-07-31 | Г1 Терапьютикс, Инк. | Антипролиферационные средства на основе пиримидина |
| 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 |
| TWI812494B (zh) | 2017-01-20 | 2023-08-11 | 美商阿克思生物科學有限公司 | 用於治療癌症相關病症之唑嘧啶 |
| 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 |
| CN115873022A (zh) | 2017-03-30 | 2023-03-31 | 伊忒欧斯比利时股份公司 | 作为a2a抑制剂的2-氧代噻唑衍生物和用于治疗癌症的化合物 |
| 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 |
| KR20200022027A (ko) | 2017-06-30 | 2020-03-02 | 리부 세라퓨틱스 에스.에이. | 아데노신 A2A 수용체의 이미다조[1,2,a]피라진 조절물질 |
| MX2020000693A (es) | 2017-07-18 | 2020-07-29 | Nuvation Bio Inc | Compuestos de 1,8-naftiridinona, y usos de los mismos. |
| CA3080976A1 (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 |
| EP3723754A4 (en) | 2017-12-13 | 2021-05-19 | Merck Sharp & Dohme Corp. | IMIDAZO [1,2-C] QUINAZOLINE-5-AMINE COMPOUNDS WITH PROPERTIES OF A2A ANTAGONIST |
| WO2019120234A2 (zh) | 2017-12-20 | 2019-06-27 | 贝达药业股份有限公司 | 作为溴结构域蛋白质抑制剂的化合物和组合物 |
| 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 |
| WO2019148161A1 (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 |
| MA51875A (fr) | 2018-02-13 | 2020-12-23 | Iovance Biotherapeutics Inc | Expansion de lymphocytes infiltrant les tumeurs (til) avec des antagonistes du récepteur a2a de l'adénosine et combinaisons thérapeutiques de til et d'antagonistes du récepteur a2a de l'adénosine |
| 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 |
| WO2019165204A1 (en) | 2018-02-23 | 2019-08-29 | Newave Pharmaceutical Inc. | 1,2-dihydro-3h-pyrazolo[3,4-d]pyrimidine-3-one compounds as inhibitors of wee-1 kinase |
| US20190292188A1 (en) | 2018-02-27 | 2019-09-26 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors |
| AU2019227823B2 (en) | 2018-02-28 | 2024-12-12 | The Regents Of The University Of Colorado, A Body Corporate | WEE1 kinase inhibitors and methods of treating cancer using the same |
| MX2020009372A (es) | 2018-03-09 | 2020-10-14 | Recurium Ip Holdings Llc | 1,2-dihidro-3h-pirazolo[3,4-d]pirimidin-3-onas sustituidas. |
| US11220510B2 (en) | 2018-04-09 | 2022-01-11 | Incyte Corporation | Pyrrole tricyclic compounds as A2A / A2B inhibitors |
| KR102816365B1 (ko) | 2018-08-17 | 2025-06-02 | 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 | 피라진 화합물 및 이의 용도 |
| 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 |
| AU2020208644A1 (en) | 2019-01-18 | 2021-08-26 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
| WO2020150676A1 (en) | 2019-01-18 | 2020-07-23 | Nuvation Bio Inc. | 1,8-naphthyridinone compounds and uses thereof |
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2018
- 2018-07-18 AU AU2018302179A patent/AU2018302179A1/en not_active Abandoned
- 2018-07-18 KR KR1020207004248A patent/KR20200041315A/ko not_active Ceased
- 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
- 2018-07-18 JP JP2020502984A patent/JP2020527588A/ja active Pending
- 2018-07-18 EP EP18834623.3A patent/EP3654978A4/en not_active Withdrawn
- 2018-07-18 SG SG11202000418XA patent/SG11202000418XA/en unknown
- 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 MX MX2020000690A patent/MX2020000690A/es unknown
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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