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 (Direct) | 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 (Direct) |
| EP (1) | EP2938610A2 (Direct) |
| JP (1) | JP2016504365A (Direct) |
| AU (1) | AU2013370417A1 (Direct) |
| CA (1) | CA2896731A1 (Direct) |
| WO (1) | WO2014105952A2 (Direct) |
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 |
| AR103297A1 (es) | 2014-12-30 | 2017-05-03 | Forma Therapeutics Inc | Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina |
| 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 |
| 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 |
| WO2016126929A1 (en) | 2015-02-05 | 2016-08-11 | Forma Therapeutics, Inc. | Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors |
| US9938300B2 (en) | 2015-02-05 | 2018-04-10 | Forma Therapeutics, Inc. | Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors |
| SG11201804098TA (en) | 2015-11-20 | 2018-06-28 | Forma Therapeutics Inc | Purinones as ubiquitin-specific protease 1 inhibitors |
| CN109071560B (zh) * | 2016-02-12 | 2022-01-14 | 瓦洛健康公司 | 用作泛素特异性蛋白酶抑制剂的噻吩并吡啶甲酰胺 |
| ES2763274T3 (es) | 2016-02-12 | 2020-05-27 | Forma Therapeutics Inc | Carboxamidas de tienopirazina como inhibidores de la proteasa específica de la ubiquitina |
| GB201604638D0 (en) * | 2016-03-18 | 2016-05-04 | Mission Therapeutics Ltd | Novel compounds |
| GB201604647D0 (en) * | 2016-03-18 | 2016-05-04 | Mission Therapeutics Ltd | Novel compounds |
| KR102327053B1 (ko) * | 2017-03-16 | 2021-11-17 | 기초과학연구원 | 퀴나졸린, 퀴놀린 유도체 및 egfr 키나제 억제제로서의 용도 |
| KR101986013B1 (ko) * | 2017-08-04 | 2019-06-04 | 연세대학교 산학협력단 | Ml323을 유효성분으로 포함하는 비만 예방 또는 치료용 조성물 |
| TW201920157A (zh) | 2017-08-11 | 2019-06-01 | 美商弗瑪治療公司 | 作為泛素–特異性蛋白酶抑制劑之甲醯胺 |
| WO2019089216A1 (en) | 2017-11-01 | 2019-05-09 | Dana-Farber Cancer Institute, Inc. | Methods of treating cancers |
| EP3833661A1 (en) | 2018-08-09 | 2021-06-16 | Valo Early Discovery, Inc. | Carboxamides as ubiquitin-specific protease inhibitors |
| EP3833441A1 (en) | 2018-08-09 | 2021-06-16 | Valo Early Discovery, Inc. | Inhibiting deubiquitinase usp25 and usp28 |
| TWI895986B (zh) | 2018-12-20 | 2025-09-01 | 美商Ｋｓｑ治療公司 | 經取代之吡唑并嘧啶及經取代之嘌呤以及其作為泛素特異性加工蛋白酶１（ｕｓｐ１）抑制劑的用途 |
| 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 |
| JP2023548148A (ja) | 2020-10-30 | 2023-11-15 | 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 | 置換ピラゾロピリミジンの固体形態及びその使用 |
| 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 |
| CN117241801A (zh) * | 2021-04-07 | 2023-12-15 | 福马治疗有限公司 | 抑制泛素特异性蛋白酶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 |
| GEAP202416532A (en) | 2021-11-12 | 2024-08-12 | Insilico Medicine Ip Ltd | Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof |
| KR20250007533A (ko) | 2022-04-08 | 2025-01-14 | 샤이 테라퓨틱스 엘엘씨 | 암, 염증성 질환, ras질환 및 섬유성 질환의 치료를 위한 ras 슈퍼패밀리 단백질과 상호작용하는 화합물 |
| JP2025515319A (ja) * | 2022-04-29 | 2025-05-14 | 江▲蘇▼▲亞▼虹医▲薬▼科技股▲フン▼有限公司 | ピリミジン化合物、それを調製するための方法、及びその薬学的使用 |
| 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 |
Family Cites Families (36)
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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 |
| ATE297390T1 (de) | 2001-04-20 | 2005-06-15 | Ciba Sc Holding Ag | 4-amino-2-(2-pyridinyl)pyrimidine als mikrobizide wirksubstanzen |
| EP1254903B1 (en) | 2001-04-20 | 2005-06-08 | Ciba SC Holding AG | 4-Amino-2-(pyridin-2-yl)pyrimidine as microbicidal active substances |
| WO2003026661A1 (fr) * | 2001-09-14 | 2003-04-03 | Yamanouchi Pharmaceutical Co., Ltd. | Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine |
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| CN1642422A (zh) | 2002-03-15 | 2005-07-20 | 西巴特殊化学品控股有限公司 | 4－氨基嘧啶及其在表面抗菌处理中的应用 |
| ATE469903T1 (de) | 2002-09-04 | 2010-06-15 | Schering Corp | Zur behandlung von krebserkrankungen geeignete pyrazolopyrimidine |
| MXPA06012130A (es) * | 2004-04-20 | 2007-01-31 | Transtech Pharma Inc | Derivados de tiazol y pirimidina substituidos como moduladores del receptor de melanocortina. |
| WO2006004589A2 (en) * | 2004-05-08 | 2006-01-12 | Neurogen Corporation | 3-aryl-5,6-disubstituted pyridazines |
| KR20060079121A (ko) | 2004-12-31 | 2006-07-05 | 에스케이케미칼주식회사 | 당뇨 및 비만 치료예방에 유효한 퀴나졸린 유도체 |
| US20070032499A1 (en) | 2005-08-05 | 2007-02-08 | Philippe Guedat | Novel cysteine protease inhibitors and their therapeutic applications |
| JP2010505794A (ja) | 2006-10-03 | 2010-02-25 | ノイロサーチ アクティーゼルスカブ | カリウムチャネル調節剤として有用なインダゾリル誘導体 |
| JP2010208945A (ja) * | 2007-06-01 | 2010-09-24 | Mitsubishi Tanabe Pharma Corp | 複素環化合物 |
| US8637560B2 (en) | 2007-07-18 | 2014-01-28 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Imidazolidinone compounds, methods to inhibit deubiquitination and methods of treatment |
| JP2011032169A (ja) * | 2007-12-11 | 2011-02-17 | Genecare Research Institute Co Ltd | ４−アミノピリミジン誘導体および該化合物を含有する医薬組成物 |
| PH12012500097A1 (en) | 2009-07-21 | 2011-01-27 | Shanghai Inst Organic Chem | Potent small molecule inhibitors of autophagy, and methods of use thereof |
| AR077999A1 (es) * | 2009-09-02 | 2011-10-05 | Vifor Int Ag | Antagonistas de pirimidin y triazin-hepcidina |
| BR112012018631A8 (pt) | 2010-01-28 | 2017-12-19 | President And Fellows Of Harvard Colege | composições e métodos para intensificação da atividade do proteassoma |
| EP2360158A1 (en) * | 2010-02-18 | 2011-08-24 | Almirall, S.A. | Pyrazole derivatives as jak inhibitors |
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| WO2011137320A2 (en) | 2010-04-30 | 2011-11-03 | Dana-Farber Cancer Institute, Inc. | Small molecule inhibitors of usp1 deubiquitinating enzyme activity |
| EP2566480A4 (en) | 2010-05-07 | 2014-03-19 | California Inst Of Techn | METHOD AND COMPOSITIONS FOR INHIBITING THE VALOSIN-CONTAINING PROTEIN |
| CA2808432C (en) | 2010-07-23 | 2019-06-04 | President And Fellows Of Harvard College | Tricyclic proteasome activity enhancing compounds with thieno[2,3-d]pyrimidine core |
| EP2619184B1 (en) | 2010-09-24 | 2018-05-23 | The Regents of the University of Michigan | Deubiquitinase inhibitors and methods for use of the same |
| WO2012061754A2 (en) | 2010-11-05 | 2012-05-10 | The Broad Institute, Inc. | Compounds and methods for treating autoimmune diseases |
| WO2012172043A1 (en) | 2011-06-15 | 2012-12-20 | Laboratoire Biodim | Purine derivatives and their use as pharmaceuticals for prevention or treatment of bacterial infections |
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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 |
| EP2565186A1 (en) | 2011-09-02 | 2013-03-06 | Hybrigenics S.A. | Selective and reversible inhibitors of ubiquitin specific protease 7 |
| 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 |
| WO2013058691A1 (en) | 2011-10-19 | 2013-04-25 | Vivolux Ab | Method for inhibition of deubiquitinating activity |
| CA2861462A1 (en) | 2012-01-25 | 2013-08-01 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating tricyclic compounds |
| JP2015504919A (ja) | 2012-01-25 | 2015-02-16 | 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調節する化合物 |
| 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 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 AU AU2013370417A patent/AU2013370417A1/en not_active Abandoned
- 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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