JP2016504365A5 - - Google Patents
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- Publication number
- JP2016504365A5 JP2016504365A5 JP2015550767A JP2015550767A JP2016504365A5 JP 2016504365 A5 JP2016504365 A5 JP 2016504365A5 JP 2015550767 A JP2015550767 A JP 2015550767A JP 2015550767 A JP2015550767 A JP 2015550767A JP 2016504365 A5 JP2016504365 A5 JP 2016504365A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- compound
- heterocyclyl
- heteroaryl
- alkyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 17
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- -1 heteroaryl aryl Chemical group 0.000 claims 10
- 125000005843 halogen group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 102000001477 Deubiquitinating Enzymes Human genes 0.000 claims 1
- 108010093668 Deubiquitinating Enzymes Proteins 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940041181 antineoplastic drug Drugs 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 238000001308 synthesis method Methods 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261747052P | 2012-12-28 | 2012-12-28 | |
| US61/747,052 | 2012-12-28 | ||
| PCT/US2013/077804 WO2014105952A2 (en) | 2012-12-28 | 2013-12-26 | Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016504365A JP2016504365A (ja) | 2016-02-12 |
| JP2016504365A5 true JP2016504365A5 (OSRAM) | 2016-11-24 |
Family
ID=49958735
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015550767A Pending JP2016504365A (ja) | 2012-12-28 | 2013-12-26 | Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9802904B2 (OSRAM) |
| EP (1) | EP2938610A2 (OSRAM) |
| JP (1) | JP2016504365A (OSRAM) |
| AU (1) | AU2013370417A1 (OSRAM) |
| CA (1) | CA2896731A1 (OSRAM) |
| WO (1) | WO2014105952A2 (OSRAM) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016504365A (ja) | 2012-12-28 | 2016-02-12 | アメリカ合衆国 | Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用 |
| MA41291A (fr) * | 2014-12-30 | 2017-11-07 | Forma Therapeutics Inc | Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer |
| TWI698436B (zh) | 2014-12-30 | 2020-07-11 | 美商佛瑪治療公司 | 作為泛素特異性蛋白酶７抑制劑之吡咯并及吡唑并嘧啶 |
| WO2016126929A1 (en) | 2015-02-05 | 2016-08-11 | Forma Therapeutics, Inc. | Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors |
| JP2018504432A (ja) | 2015-02-05 | 2018-02-15 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的プロテアーゼ７阻害物質としてのイソチアゾロピリミジノン、ピラゾロピリミジノン及びピロロピリミジノン |
| JP2018504430A (ja) | 2015-02-05 | 2018-02-15 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的プロテアーゼ７阻害物質としてのキナゾリノン及びアザキナゾリノン |
| JP6964343B2 (ja) * | 2015-11-20 | 2021-11-10 | フォーマ セラピューティクス，インコーポレイテッド | ユビキチン特異的プロテアーゼ１阻害剤としてのプリノン |
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| CA3108676A1 (en) | 2018-08-09 | 2020-02-13 | David J. Guerin | Carboxamides as ubiquitin-specific protease inhibitors |
| JP2021534122A (ja) | 2018-08-09 | 2021-12-09 | ヴァロ アーリー ディスカバリー， インコーポレイテッド | 脱ユビキチン化酵素ｕｓｐ２５及びｕｓｐ２８の阻害 |
| JP7662519B2 (ja) | 2018-12-20 | 2025-04-15 | ケーエスキュー セラピューティクス， インコーポレイテッド | 置換されたピラゾロピリミジン及び置換されたプリンならびにユビキチン特異的プロセシングプロテアーゼ１（ｕｓｐ１）阻害剤としてのそれらの使用 |
| AU2020299526A1 (en) | 2019-05-31 | 2022-01-20 | Case Western Reserve University | Bax inhibitors and uses thereof |
| CN110699453B (zh) * | 2019-10-10 | 2020-09-01 | 山东大学第二医院 | 一种胆管癌检测、治疗和预后靶点及应用 |
| KR102481705B1 (ko) * | 2020-08-04 | 2022-12-27 | 연세대학교 산학협력단 | 트리아졸 유도체를 유효성분으로 포함하는 간 섬유증의 예방 또는 치료용 조성물 |
| IL302352A (en) | 2020-10-30 | 2023-06-01 | Ksq Therapeutics Inc | Solid state forms of substituted pyrazolopyrimidines and uses thereof |
| CN114436976B (zh) * | 2021-01-29 | 2023-07-11 | 石药集团中奇制药技术（石家庄）有限公司 | 一种新型喹唑啉类衍生物及其制备和应用 |
| WO2022199652A1 (en) * | 2021-03-24 | 2022-09-29 | Impact Therapeutics (Shanghai) , Inc | Five-membered heteroaryl-pyrimidine compounds as usp1 inhibitors and the use thereof |
| TN2023000250A1 (en) * | 2021-04-07 | 2025-07-02 | Forma Therapeutics Inc | Inhibiting ubiquitin-specific protease 1 (usp1) |
| CN113368112B (zh) * | 2021-05-10 | 2022-09-27 | 河南农业大学 | Usp1-uaf1抑制剂在制备药物中的应用，药物组合物 |
| EP4430050A4 (en) | 2021-11-12 | 2025-09-24 | Insilico Medicine Ip Ltd | SMALL MOLECULE INHIBITORS OF UBIQUITIN-SPECIFIC PROTEASE 1 AND THEIR USES |
| CN119365460A (zh) | 2022-04-08 | 2025-01-24 | 尚医治疗有限责任公司 | 与Ras超家族蛋白相互作用以用于治疗癌症、炎性疾病、RAS病和纤维化疾病的化合物 |
| IL316542A (en) * | 2022-04-29 | 2024-12-01 | Jiangsu Yahong Meditech Co Ltd | Pyrimidine compound, method for its preparation, and pharmaceutical use thereof |
| WO2024086790A1 (en) | 2022-10-21 | 2024-04-25 | Exelixis, Inc. | 4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[4,3-c]PYRIDINE COMPOUNDS AND DERIVATIVES AS USP1 INHIBITORS |
| CN120202201A (zh) * | 2022-11-04 | 2025-06-24 | 深圳晶泰科技有限公司 | 泛素特异性蛋白酶1的抑制剂及其应用 |
| WO2024153175A1 (en) * | 2023-01-19 | 2024-07-25 | Laekna Therapeutics Shanghai Co., Ltd. | Heteroaromatic compounds and their use as usp1 inhibitors |
| WO2024233605A1 (en) | 2023-05-08 | 2024-11-14 | Tango Therapeutics, Inc. | Compounds and their use against cancer |
| WO2024233665A1 (en) * | 2023-05-08 | 2024-11-14 | Tango Therapeutics, Inc. | Compounds and their use against cancer |
| WO2025005744A1 (ko) * | 2023-06-29 | 2025-01-02 | (주)아이젠사이언스 | 신규 피리미딘 유도체 |
| WO2025007840A1 (zh) * | 2023-07-05 | 2025-01-09 | 江苏亚虹医药科技股份有限公司 | 联嘧啶化合物的晶型及其制备方法和用途 |
| WO2025007777A1 (zh) * | 2023-07-05 | 2025-01-09 | 江苏亚虹医药科技股份有限公司 | 嘧啶类化合物、其制备方法及其医药用途 |
| WO2025010245A1 (en) | 2023-07-06 | 2025-01-09 | Exelixis, Inc. | Fused pyrazole derivatives as usp1 inhibitors |
| WO2025015905A1 (en) * | 2023-07-14 | 2025-01-23 | Laekna Therapeutics Shanghai Co., Ltd. | Pyrimidine compounds and their use as usp1 inhibitors |
| WO2025102016A1 (en) * | 2023-11-10 | 2025-05-15 | Vrise Therapeutics, Inc. | Novel molecules as inhibitors of dna damage repair pathway |
| WO2025129076A1 (en) * | 2023-12-15 | 2025-06-19 | Eikon Therapeutics, Inc. | Pyridopyrimidine and quinazoline derivatives as usp1 inhibitors, compositions comprising them and methods of using the same |
| WO2025129135A2 (en) * | 2023-12-15 | 2025-06-19 | Eikon Therapeutics, Inc. | Compositions comprising usp1 inhibitors and methods of using the same |
| WO2025151705A1 (en) | 2024-01-10 | 2025-07-17 | Vrise Therapeutics, Inc. | Novel inhibitors of dna damage repair pathway |
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| PT100905A (pt) * | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| JP2657760B2 (ja) * | 1992-07-15 | 1997-09-24 | 小野薬品工業株式会社 | ４−アミノキナゾリン誘導体およびそれを含有する医薬品 |
| DE19853278A1 (de) | 1998-11-19 | 2000-05-25 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
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| CN103261169A (zh) | 2010-09-24 | 2013-08-21 | 密歇根大学董事会 | 脱泛素酶抑制剂及其应用方法 |
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| EP2546684A1 (fr) | 2011-07-15 | 2013-01-16 | ETA SA Manufacture Horlogère Suisse | Guide de lumière pour l'éclairage d'un dispositif d'affichage d'informations |
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| JP2014237590A (ja) | 2011-09-30 | 2014-12-18 | アステラス製薬株式会社 | ２−（ピリジン−２−イル）ピリミジン−４−アミン化合物又はその塩 |
| KR102022575B1 (ko) | 2011-10-19 | 2019-09-18 | 비보룩스 아베 | 탈유비퀴틴화 활성의 저해 방법 |
| JP2015513317A (ja) | 2012-01-25 | 2015-05-07 | プロテオステイシス セラピューティクス，インコーポレイテッド | プロテアソーム活性を増強する化合物 |
| WO2013112651A2 (en) | 2012-01-25 | 2013-08-01 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating compounds |
| JP2016504365A (ja) | 2012-12-28 | 2016-02-12 | アメリカ合衆国 | Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用 |
-
2013
- 2013-12-26 JP JP2015550767A patent/JP2016504365A/ja active Pending
- 2013-12-26 AU AU2013370417A patent/AU2013370417A1/en not_active Abandoned
- 2013-12-26 WO PCT/US2013/077804 patent/WO2014105952A2/en not_active Ceased
- 2013-12-26 EP EP13821618.9A patent/EP2938610A2/en not_active Withdrawn
- 2013-12-26 CA CA2896731A patent/CA2896731A1/en not_active Abandoned
- 2013-12-26 US US14/655,538 patent/US9802904B2/en active Active
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