JPWO2022223025A5 - - Google Patents
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- Publication number
- JPWO2022223025A5 JPWO2022223025A5 JP2023564007A JP2023564007A JPWO2022223025A5 JP WO2022223025 A5 JPWO2022223025 A5 JP WO2022223025A5 JP 2023564007 A JP2023564007 A JP 2023564007A JP 2023564007 A JP2023564007 A JP 2023564007A JP WO2022223025 A5 JPWO2022223025 A5 JP WO2022223025A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- cycloalkyl
- group
- halogen
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 212
- -1 nitro, hydroxy Chemical group 0.000 claims 138
- 125000000623 heterocyclic group Chemical group 0.000 claims 99
- 229910052736 halogen Inorganic materials 0.000 claims 93
- 150000002367 halogens Chemical group 0.000 claims 93
- 229910052739 hydrogen Inorganic materials 0.000 claims 88
- 239000001257 hydrogen Substances 0.000 claims 88
- 125000003545 alkoxy group Chemical group 0.000 claims 87
- 150000002431 hydrogen Chemical group 0.000 claims 86
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 83
- 229910052805 deuterium Inorganic materials 0.000 claims 83
- 125000001072 heteroaryl group Chemical group 0.000 claims 79
- 125000003118 aryl group Chemical group 0.000 claims 75
- 150000003573 thiols Chemical group 0.000 claims 66
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 44
- 125000000304 alkynyl group Chemical group 0.000 claims 41
- 125000003342 alkenyl group Chemical group 0.000 claims 40
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 40
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 40
- 125000000753 cycloalkyl group Chemical group 0.000 claims 37
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 36
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 34
- 125000004043 oxo group Chemical group O=* 0.000 claims 34
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 33
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 33
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 31
- 125000001188 haloalkyl group Chemical group 0.000 claims 31
- 125000001424 substituent group Chemical group 0.000 claims 24
- 125000004093 cyano group Chemical group *C#N 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 19
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical group [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- 101100240985 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) nrc-2 gene Proteins 0.000 claims 2
- 102100023712 Poly [ADP-ribose] polymerase 1 Human genes 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 239000003054 catalyst Substances 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 239000012661 PARP inhibitor Substances 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 108010064218 Poly (ADP-Ribose) Polymerase-1 Proteins 0.000 claims 1
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims 1
- 101710179684 Poly [ADP-ribose] polymerase Proteins 0.000 claims 1
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 208000023589 ischemic disease Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110443582.0 | 2021-04-23 | ||
| CN202110443582 | 2021-04-23 | ||
| CN202110653169.7 | 2021-06-11 | ||
| CN202110653169 | 2021-06-11 | ||
| CN202110808316.3 | 2021-07-16 | ||
| CN202110808316 | 2021-07-16 | ||
| CN202110926676.3 | 2021-08-12 | ||
| CN202110926676 | 2021-08-12 | ||
| CN202210072358 | 2022-01-21 | ||
| CN202210072358.X | 2022-01-21 | ||
| PCT/CN2022/088466 WO2022223025A1 (zh) | 2021-04-23 | 2022-04-22 | 杂环类衍生物抑制剂、其制备方法和应用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024514338A JP2024514338A (ja) | 2024-04-01 |
| JPWO2022223025A5 true JPWO2022223025A5 (https=) | 2025-05-01 |
| JP2024514338A5 JP2024514338A5 (https=) | 2025-05-01 |
Family
ID=83668197
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023564007A Pending JP2024514338A (ja) | 2021-04-23 | 2022-04-22 | 複素環式誘導体阻害剤及びその調製方法及びその用途 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20240228490A1 (https=) |
| EP (1) | EP4328225A4 (https=) |
| JP (1) | JP2024514338A (https=) |
| KR (1) | KR20240005756A (https=) |
| CN (2) | CN115232154A (https=) |
| AU (1) | AU2022261029A1 (https=) |
| BR (1) | BR112023019797A2 (https=) |
| CA (1) | CA3215823A1 (https=) |
| IL (1) | IL307824A (https=) |
| MX (1) | MX2023012054A (https=) |
| TW (1) | TW202309026A (https=) |
| WO (1) | WO2022223025A1 (https=) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202309025A (zh) | 2021-04-19 | 2023-03-01 | 美商辛瑟拉股份有限公司 | Parp1抑制劑及其用途 |
| WO2022222965A1 (zh) * | 2021-04-23 | 2022-10-27 | 成都百裕制药股份有限公司 | 吡啶衍生物及其在医药上的应用 |
| US20230159525A1 (en) | 2021-10-01 | 2023-05-25 | Xinthera, Inc. | Azetidine and pyrrolidine parp1 inhibitors and uses thereof |
| JP7762306B2 (ja) * | 2021-11-19 | 2025-10-29 | 康百達（四川）生物医薬科技有限公司 | 選択的ｐａｒｐ１阻害剤およびその用途 |
| CN116143776A (zh) * | 2021-11-22 | 2023-05-23 | 南京圣和药业股份有限公司 | Parp1抑制剂及其应用 |
| CA3241338A1 (en) * | 2021-12-17 | 2023-06-22 | Yongqi Deng | Parp inhibitor, pharmaceutical composition comprising same, and use thereof |
| WO2023138541A1 (zh) * | 2022-01-20 | 2023-07-27 | 微境生物医药科技(上海)有限公司 | 吡啶酰胺类parp抑制剂、及其制备方法和医药用途 |
| AU2023209820B2 (en) | 2022-01-21 | 2024-10-10 | Xinthera, Inc. | Parp1 inhibitors and uses thereof |
| US20260098024A1 (en) * | 2022-01-27 | 2026-04-09 | Xinthera, Inc. | Parp1 inhibitors and uses thereof |
| KR20240161147A (ko) | 2022-03-14 | 2024-11-12 | 슬랩 파마슈티컬스 엘엘씨 | 다중 사이클릭 화합물 |
| FI4497438T3 (fi) | 2022-04-28 | 2025-10-20 | Xinthera Inc | Trisyklisiä parp1:n estäjiä ja niiden käyttötapoja |
| WO2023207284A1 (en) * | 2022-04-28 | 2023-11-02 | Ningbo Newbay Technology Development Co., Ltd | Piperazine derivatives as parp1 inhibitiors |
| CN115919859B (zh) * | 2022-07-14 | 2024-01-05 | 四川海思科制药有限公司 | 一种杂芳基衍生物的药物组合物及其在医药上的应用 |
| WO2024041608A1 (zh) * | 2022-08-24 | 2024-02-29 | 四川海思科制药有限公司 | 一种杂芳基衍生物parp抑制剂的晶体形式及其用途 |
| WO2024041605A1 (zh) * | 2022-08-24 | 2024-02-29 | 四川海思科制药有限公司 | 一种杂芳基衍生物parp抑制剂药学上可接受的盐及其用途 |
| US20240132449A1 (en) * | 2022-08-30 | 2024-04-25 | 1Cbio, Inc. | Heterocyclic compounds and methods of use thereof |
| CN119365468A (zh) * | 2022-08-31 | 2025-01-24 | 江苏恒瑞医药股份有限公司 | 稠合二环类化合物、其制备方法及其在医药上的应用 |
| CN117658983A (zh) * | 2022-09-01 | 2024-03-08 | 浙江文达医药科技有限公司 | 选择性parp1抑制剂 |
| TW202415658A (zh) * | 2022-09-30 | 2024-04-16 | 大陸商中國醫藥研究開發中心有限公司 | 含氮雜環類化合物及其醫藥用途 |
| TW202416977A (zh) * | 2022-09-30 | 2024-05-01 | 大陸商中國醫藥研究開發中心有限公司 | 含氮雜環類化合物及其醫藥用途 |
| WO2024083218A1 (zh) * | 2022-10-20 | 2024-04-25 | 成都赜灵生物医药科技有限公司 | 取代四氢吡啶类化合物及其用途 |
| CN117946074A (zh) * | 2022-10-20 | 2024-04-30 | 上海海和药物研究开发股份有限公司 | 具有parp1抑制活性的化合物及其用途 |
| WO2024083201A1 (zh) * | 2022-10-20 | 2024-04-25 | 成都赜灵生物医药科技有限公司 | 并杂环类化合物及其用途 |
| JP2025535834A (ja) * | 2022-11-02 | 2025-10-28 | スアンズ バイオファーマシューティカル カンパニー，リミテッド | 多環式ポリ（ａｄｐリボース）ポリメラーゼ選択的阻害剤 |
| EP4615581A2 (en) * | 2022-11-09 | 2025-09-17 | Laekna Pharmaceutical Ningbo Co., Ltd. | Fused multicyclic compounds and their use as parp1 inhibitors |
| CN117903159A (zh) * | 2022-12-30 | 2024-04-19 | 成都硕德药业有限公司 | 一种内酰胺类衍生物、其制备方法及用途 |
| CN116375700B (zh) * | 2023-01-10 | 2024-12-17 | 中国科学院成都生物研究所 | 一种4-氮杂吲哚啉类化合物及其合成方法与应用 |
| EP4669633A1 (en) * | 2023-02-21 | 2025-12-31 | 1Cbio, Inc. | HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THEM |
| WO2024178125A1 (en) * | 2023-02-21 | 2024-08-29 | 1Cbio, Inc. | Heterocyclic compounds and methods of use thereof |
| EP4673448A1 (en) * | 2023-03-01 | 2026-01-07 | Impact Therapeutics (Shanghai), Inc. | Substituted nitrogen-containing tricyclic compounds as parp inhibitors and the use thereof |
| TW202502341A (zh) * | 2023-03-13 | 2025-01-16 | 大陸商江蘇豪森藥業集團有限公司 | 哌啶烯類化合物在製備治療癌症的藥物中的應用 |
| AU2024316921A1 (en) * | 2023-07-28 | 2026-02-05 | Sunshine Lake Pharma Co., Ltd. | Substituted nitrogen-containing bicyclic compound and use thereof |
| CN119462669A (zh) * | 2023-08-11 | 2025-02-18 | 上海海和药物研究开发股份有限公司 | 稠合三环类化合物、其药物组合物和用途 |
| CN121335891A (zh) * | 2023-08-17 | 2026-01-13 | Dic株式会社 | 化合物和使用该化合物的液晶组合物、液晶显示装置、传感器、液晶透镜、光通信装置和天线 |
| WO2025103407A1 (zh) * | 2023-11-16 | 2025-05-22 | 江苏豪森药业集团有限公司 | 抗体药物偶联物和多腺苷二磷酸核糖聚合酶抑制剂的联合应用 |
| WO2025168048A1 (zh) * | 2024-02-08 | 2025-08-14 | 上海璎黎药业有限公司 | 一种三键结构化合物、其药物组合物及其应用 |
| WO2025265123A1 (en) * | 2024-06-21 | 2025-12-26 | Protheragen Inc. | Parp1 inhibitors for the treatment of diseases |
| WO2026002281A1 (zh) * | 2024-06-28 | 2026-01-02 | 上海翰森生物医药科技有限公司 | 哌啶烯类化合物联合用药在制备治疗癌症的药物中的用途 |
| CN119039301B (zh) * | 2024-10-31 | 2025-09-02 | 江苏豪森药业集团有限公司 | 一种含氮杂环的多环化合物晶型ⅰ的制备方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1190466B (de) * | 1961-11-07 | 1965-04-08 | Cassella Farbwerke Mainkur Ag | Verfahren zur Herstellung von Piperazinderivaten |
| HUP9903758A3 (en) * | 1996-05-29 | 2000-07-28 | Warner Lambert Co | Benzoxazinone dopamine d4 receptor antagonists and pharmaceutical compositions containing the same |
| GB0227240D0 (en) * | 2002-11-21 | 2002-12-31 | Glaxo Group Ltd | Compounds |
| EA010592B1 (ru) * | 2003-12-10 | 2008-10-30 | Янссен Фармацевтика Н.В. | 6-замещённые циклогексилалкил 2-замещённые хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(adp-рибоза)полимеразы |
| RU2007101544A (ru) * | 2004-06-17 | 2008-08-10 | Уайт (Us) | Антагонисты рецепторов высвобождающего гонадотропин гормона |
| US8404713B2 (en) * | 2007-10-26 | 2013-03-26 | Janssen Pharmaceutica Nv | Quinolinone derivatives as PARP inhibitors |
| WO2010111626A2 (en) * | 2009-03-27 | 2010-09-30 | Takeda Pharmaceutical Company Limited | Poly (adp-ribose) polymerase (parp) inhibitors |
| EP3804336A4 (en) * | 2018-07-11 | 2021-08-11 | Huawei Technologies Co., Ltd. | FILTERING PROCESS AND APPARATUS DEPENDING ON THE ASPECT RATIO FOR INTRA-PREDICTION |
| MX2022000711A (es) * | 2019-07-19 | 2022-02-23 | Astrazeneca Ab | Inhibidores de parp1. |
| TW202309025A (zh) * | 2021-04-19 | 2023-03-01 | 美商辛瑟拉股份有限公司 | Parp1抑制劑及其用途 |
-
2022
- 2022-04-22 WO PCT/CN2022/088466 patent/WO2022223025A1/zh not_active Ceased
- 2022-04-22 TW TW111115479A patent/TW202309026A/zh unknown
- 2022-04-22 CA CA3215823A patent/CA3215823A1/en active Pending
- 2022-04-22 MX MX2023012054A patent/MX2023012054A/es unknown
- 2022-04-22 EP EP22791130.2A patent/EP4328225A4/en active Pending
- 2022-04-22 IL IL307824A patent/IL307824A/en unknown
- 2022-04-22 US US18/555,468 patent/US20240228490A1/en active Pending
- 2022-04-22 AU AU2022261029A patent/AU2022261029A1/en active Pending
- 2022-04-22 KR KR1020237039621A patent/KR20240005756A/ko active Pending
- 2022-04-22 BR BR112023019797A patent/BR112023019797A2/pt unknown
- 2022-04-22 CN CN202210431665.2A patent/CN115232154A/zh active Pending
- 2022-04-22 JP JP2023564007A patent/JP2024514338A/ja active Pending
- 2022-04-22 CN CN202280007892.0A patent/CN116601148A/zh active Pending
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