JP2018505207A5 - - Google Patents
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- Publication number
- JP2018505207A5 JP2018505207A5 JP2017542888A JP2017542888A JP2018505207A5 JP 2018505207 A5 JP2018505207 A5 JP 2018505207A5 JP 2017542888 A JP2017542888 A JP 2017542888A JP 2017542888 A JP2017542888 A JP 2017542888A JP 2018505207 A5 JP2018505207 A5 JP 2018505207A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- group
- pharmaceutically acceptable
- acceptable salt
- nitrogen
- 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.)
- Ceased
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 50
- 150000003839 salts Chemical class 0.000 claims 43
- 150000001875 compounds Chemical class 0.000 claims 41
- 229910052757 nitrogen Inorganic materials 0.000 claims 32
- 125000001424 substituent group Chemical group 0.000 claims 32
- 125000001072 heteroaryl group Chemical group 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 27
- 239000001257 hydrogen Substances 0.000 claims 27
- 125000003118 aryl group Chemical group 0.000 claims 22
- 125000002950 monocyclic group Chemical group 0.000 claims 21
- -1 N (R3) 2 Chemical class 0.000 claims 17
- 229910052760 oxygen Inorganic materials 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 150000002431 hydrogen Chemical group 0.000 claims 14
- 229910052717 sulfur Inorganic materials 0.000 claims 14
- 125000002619 bicyclic group Chemical group 0.000 claims 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 11
- 125000001188 haloalkyl group Chemical group 0.000 claims 10
- 229920006395 saturated elastomer Polymers 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 125000004438 haloalkoxy group Chemical group 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 241000282412 Homo Species 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 6
- 125000004244 benzofuran-2-yl group Chemical group [H]C1=C(*)OC2=C([H])C([H])=C([H])C([H])=C12 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 125000004430 oxygen atom Chemical group O* 0.000 claims 6
- 239000011593 sulfur Substances 0.000 claims 6
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 5
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 125000004434 sulfur atom Chemical group 0.000 claims 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 3
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- WFZCVZZPXZKOPL-UHFFFAOYSA-N 1h-pyrrolo[3,2-c]pyridine Chemical compound N1=CC=C2N[C]=CC2=C1 WFZCVZZPXZKOPL-UHFFFAOYSA-N 0.000 claims 1
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- IOVSATJFPJHKHE-UHFFFAOYSA-N 3h-pyrrolo[2,3-c]pyridine Chemical compound N1=CC=C2CC=NC2=C1 IOVSATJFPJHKHE-UHFFFAOYSA-N 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004190 benzothiazol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N=C(*)SC2=C1[H] 0.000 claims 1
- 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 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002249 indol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([*])=C([H])C2=C1[H] 0.000 claims 1
- 125000004531 indol-5-yl group Chemical group [H]N1C([H])=C([H])C2=C([H])C(*)=C([H])C([H])=C12 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000004497 pyrazol-5-yl group Chemical group N1N=CC=C1* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 125000006850 spacer group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15154685 | 2015-02-11 | ||
| EP15154685.0 | 2015-02-11 | ||
| EP15197976.2 | 2015-12-04 | ||
| EP15197976 | 2015-12-04 | ||
| PCT/EP2016/052828 WO2016128465A1 (en) | 2015-02-11 | 2016-02-10 | Substituted mono- and polyazanaphthalene derivatives and their use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018505207A JP2018505207A (ja) | 2018-02-22 |
| JP2018505207A5 true JP2018505207A5 (enExample) | 2019-03-14 |
Family
ID=55345828
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017542888A Ceased JP2018505207A (ja) | 2015-02-11 | 2016-02-10 | 置換モノおよびポリアザナフタレン誘導体およびその使用 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10487075B2 (enExample) |
| EP (1) | EP3256217A1 (enExample) |
| JP (1) | JP2018505207A (enExample) |
| KR (1) | KR20170117479A (enExample) |
| CN (1) | CN107428692A (enExample) |
| AU (1) | AU2016217874A1 (enExample) |
| BR (1) | BR112017017032A2 (enExample) |
| CA (1) | CA2974874A1 (enExample) |
| EA (1) | EA201791781A1 (enExample) |
| IL (1) | IL253656A0 (enExample) |
| MX (1) | MX2017010230A (enExample) |
| TW (1) | TW201636327A (enExample) |
| WO (1) | WO2016128465A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8993555B2 (en) | 2012-12-21 | 2015-03-31 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| CN106674085B (zh) * | 2016-12-20 | 2020-06-23 | 苏州汉德创宏生化科技有限公司 | N-1,3-二氟异丙基-4-氨基哌啶类化合物的合成方法 |
| CN108033909A (zh) * | 2017-12-20 | 2018-05-15 | 北京六合宁远科技有限公司 | 一种6-甲基-4-溴-异喹啉的制备方法 |
| CN108484489A (zh) * | 2018-05-25 | 2018-09-04 | 陈海鹏 | 一种含金刚烷取代基的吡啶类化合物及其在制备抗肿瘤药物中的用途 |
| CN108774167A (zh) * | 2018-05-25 | 2018-11-09 | 陈海鹏 | 一种含金刚烷取代基的吡啶类化合物及其在制备抗肿瘤药物中的用途 |
| CN108373443A (zh) * | 2018-05-25 | 2018-08-07 | 陈海鹏 | 一种含金刚烷取代基的吡啶类化合物及其在制备抗肿瘤药物中的用途 |
| CN110903286B (zh) * | 2019-12-16 | 2021-09-24 | 沈阳药科大学 | 4,6-双取代吡啶[3,2-d]嘧啶类化合物及其制备和应用 |
| WO2021257863A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Pyrrolotriazine compounds as jak2 v617f inhibitors |
| US11691971B2 (en) | 2020-06-19 | 2023-07-04 | Incyte Corporation | Naphthyridinone compounds as JAK2 V617F inhibitors |
| WO2022006456A1 (en) | 2020-07-02 | 2022-01-06 | Incyte Corporation | Tricyclic pyridone compounds as jak2 v617f inhibitors |
| BR112023000047A2 (pt) | 2020-07-02 | 2023-03-14 | Incyte Corp | Compostos de ureia tricíclicos como inibidores da v617f da jak2 |
| EP4186901A4 (en) * | 2020-07-23 | 2024-06-12 | Cytosinlab Therapeutics Co., Ltd. | COMPOUND HAVING KINASE INHIBITORY ACTIVITY |
| WO2022026380A1 (en) * | 2020-07-29 | 2022-02-03 | Board Of Regents, The University Of Texas System | Urea inhibitors of micro-rna |
| US11661422B2 (en) | 2020-08-27 | 2023-05-30 | Incyte Corporation | Tricyclic urea compounds as JAK2 V617F inhibitors |
| WO2022140231A1 (en) | 2020-12-21 | 2022-06-30 | Incyte Corporation | Deazaguaine compounds as jak2 v617f inhibitors |
| CN112876412B (zh) * | 2021-01-21 | 2022-05-24 | 温州大学 | 掺杂发光材料及其制备方法和应用 |
| AR125273A1 (es) | 2021-02-25 | 2023-07-05 | Incyte Corp | Lactamas espirocíclicas como inhibidores de jak2 v617f |
| WO2023143344A1 (zh) * | 2022-01-30 | 2023-08-03 | 微境生物医药科技(上海)有限公司 | 新型egfr抑制剂 |
| KR20240163688A (ko) | 2022-03-17 | 2024-11-19 | 인사이트 코포레이션 | Jak2 v617f 억제제로서의 삼환계 우레아 화합물 |
| AU2023247721A1 (en) * | 2022-03-31 | 2024-11-14 | Shanghai Shijiang Biotechnology Co., Ltd | Aromatic ring compound and use thereof |
| AR130742A1 (es) * | 2022-10-12 | 2025-01-15 | Adama Makhteshim Ltd | Proceso para la preparación de derivados de aminopiridazina |
| AR131541A1 (es) | 2023-01-07 | 2025-04-09 | Syngenta Crop Protection Ag | Compuestos de carboxamida novedosos |
| WO2025109114A1 (en) | 2023-11-24 | 2025-05-30 | Syngenta Crop Protection Ag | Novel carboxamide compounds |
| PY2501648A (es) | 2024-01-12 | 2025-10-31 | Syngenta Crop Protection Ag | Nuevos compuestos de carboxamida |
| WO2025149637A1 (en) | 2024-01-12 | 2025-07-17 | Syngenta Crop Protection Ag | Novel carboxamide compounds |
| WO2026008750A1 (en) | 2024-07-05 | 2026-01-08 | Syngenta Crop Protection Ag | Novel carboxamide compounds |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2102780C (en) | 1991-05-10 | 2007-01-09 | Alfred P. Spada | Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase |
| US5451596A (en) | 1992-12-29 | 1995-09-19 | Rhone Poulenc Rorer Pharmaceuticals Inc. | Cycloalkyl amine bis-aryl squalene synthase inhibitors |
| DE60040676D1 (de) | 1999-09-17 | 2008-12-11 | Millennium Pharm Inc | BENZAMIDE UND ÄHNLICHE INHIBITOREN VON FAKTOR Xa |
| EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| EP2258365B1 (en) | 2003-03-28 | 2013-05-29 | Novartis Vaccines and Diagnostics, Inc. | Use of organic compounds for immunopotentiation |
| AR045944A1 (es) * | 2003-09-24 | 2005-11-16 | Novartis Ag | Derivados de isoquinolina 1.4-disustituidas |
| EP1773834A2 (en) * | 2004-08-03 | 2007-04-18 | Serenex, Inc. | 2, 8-disubstituted naphthyridine derivatives |
| AU2007221049A1 (en) * | 2006-02-28 | 2007-09-07 | Amgen Inc. | Cinnoline and quinazoline derivates as phosphodiesterase 10 inhibitors |
| US20090099175A1 (en) * | 2006-03-01 | 2009-04-16 | Arrington Mark P | Phosphodiesterase 10 inhibitors |
| WO2007103554A1 (en) * | 2006-03-08 | 2007-09-13 | Amgen Inc. | Quinoline and isoquinoline derivatives as phosphodiesterase 10 inhibitors |
| WO2009025823A1 (en) * | 2007-08-21 | 2009-02-26 | Amgen Inc. | Phosphodiesterase 10 inhibitors |
| MX2011009213A (es) * | 2009-03-02 | 2011-12-14 | Sirtris Pharmaceuticals Inc | Quinolinas 8-sustituidas y analogos relacionados como moduladores de sirtuina. |
| GB0905441D0 (en) | 2009-03-30 | 2009-05-13 | Syngenta Ltd | Herbicidal compounds |
| CA2758144C (en) * | 2009-04-06 | 2014-05-13 | Daiichi Sankyo Company, Limited | Cyclic compound having substituted phenyl group |
| TW201116281A (en) * | 2009-08-06 | 2011-05-16 | Astellas Pharma Inc | N atom containing ring acylguanidine derivatives |
| TW201311149A (zh) * | 2011-06-24 | 2013-03-16 | Ishihara Sangyo Kaisha | 有害生物防治劑 |
| WO2013142390A1 (en) | 2012-03-21 | 2013-09-26 | Gtx, Inc. | Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors |
| EP2922540A1 (en) * | 2012-11-20 | 2015-09-30 | F. Hoffmann-La Roche AG | Substituted 1,6-naphthyridines |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| RU2673549C2 (ru) * | 2013-05-03 | 2018-11-28 | Ф. Хоффманн-Ля Рош Аг | Производные изохинолина, стимулирующие нейрогенез |
| EP3080085B1 (en) | 2013-12-09 | 2019-08-14 | UCB Biopharma SPRL | Fused bicyclic heteroaromatic derivatives as modulators of tnf activity |
| CN106817900A (zh) | 2014-07-17 | 2017-06-09 | 默克专利有限公司 | 新颖的萘啶和异喹啉及其作为cdk8/19抑制剂的用途 |
| US20180177784A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
-
2016
- 2016-02-10 AU AU2016217874A patent/AU2016217874A1/en not_active Abandoned
- 2016-02-10 MX MX2017010230A patent/MX2017010230A/es unknown
- 2016-02-10 CN CN201680009637.4A patent/CN107428692A/zh active Pending
- 2016-02-10 KR KR1020177025452A patent/KR20170117479A/ko not_active Withdrawn
- 2016-02-10 EP EP16703791.0A patent/EP3256217A1/en not_active Withdrawn
- 2016-02-10 EA EA201791781A patent/EA201791781A1/ru unknown
- 2016-02-10 BR BR112017017032A patent/BR112017017032A2/pt not_active Application Discontinuation
- 2016-02-10 US US15/545,149 patent/US10487075B2/en not_active Expired - Fee Related
- 2016-02-10 JP JP2017542888A patent/JP2018505207A/ja not_active Ceased
- 2016-02-10 WO PCT/EP2016/052828 patent/WO2016128465A1/en not_active Ceased
- 2016-02-10 CA CA2974874A patent/CA2974874A1/en not_active Abandoned
- 2016-02-15 TW TW105104357A patent/TW201636327A/zh unknown
-
2017
- 2017-07-25 IL IL253656A patent/IL253656A0/en unknown
-
2019
- 2019-10-04 US US16/593,231 patent/US20200031811A1/en not_active Abandoned
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