JP2016504365A5 - - Google Patents
Download PDFInfo
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP2938610A2 (enExample) |
| JP (1) | JP2016504365A (enExample) |
| AU (1) | AU2013370417A1 (enExample) |
| CA (1) | CA2896731A1 (enExample) |
| WO (1) | WO2014105952A2 (enExample) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2938610A2 (en) | 2012-12-28 | 2015-11-04 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof |
| 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 |
| 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 |
| EP3253759A1 (en) | 2015-02-05 | 2017-12-13 | Forma Therapeutics, Inc. | Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors |
| JP2018504431A (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阻害物質としてのチエノピリミジノン |
| 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 |
| RU2750151C2 (ru) | 2015-11-20 | 2021-06-22 | Форма Терапьютикс, Инк. | Гипоксантины в качестве ингибиторов убиквитин-специфической протеазы 1 |
| US10913753B2 (en) | 2016-02-12 | 2021-02-09 | Valo Early Discovery, Inc. | Thienopyridine carboxamides as ubiquitin-specific protease inhibitors |
| EP3414251B1 (en) | 2016-02-12 | 2019-10-16 | Forma Therapeutics, Inc. | Thienopyrazine carboxamides as ubiquitin-specific protease inhibitors |
| GB201604647D0 (en) * | 2016-03-18 | 2016-05-04 | Mission Therapeutics Ltd | Novel compounds |
| GB201604638D0 (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 |
| ES3040707T3 (en) | 2017-11-01 | 2025-11-04 | Dana Farber Cancer Inst Inc | Usp1 or uaf1 inhibitors for use in treating cancer |
| WO2020033709A1 (en) | 2018-08-09 | 2020-02-13 | Forma Therapeutics, Inc. | Inhibiting deubiquitinase usp25 and usp28 |
| CA3108676A1 (en) | 2018-08-09 | 2020-02-13 | David J. Guerin | Carboxamides as ubiquitin-specific protease inhibitors |
| IL284050B2 (en) | 2018-12-20 | 2026-01-01 | Ksq Therapeutics Inc | Modified pyrazolopyrimidines and modified purines and their use as 1 uso inhibitors |
| EP3976009A4 (en) | 2019-05-31 | 2023-07-05 | 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 |
| KR20230098186A (ko) | 2020-10-30 | 2023-07-03 | 케이에스큐 세러퓨틱스 인코포레이티드 | 치환된 피라졸로피리미딘의 고체 상태 형태 및 이의 용도 |
| 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 |
| MX2023011709A (es) * | 2021-04-07 | 2023-10-12 | Forma Therapeutics Inc | Inhibidor de la proteasa 1 especifica de ubiquitina (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 |
| WO2023083286A1 (en) | 2021-11-12 | 2023-05-19 | Insilico Medicine Ip Limited | Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof |
| JP2025512935A (ja) | 2022-04-08 | 2025-04-22 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリータンパク質と相互作用する化合物 |
| WO2023208130A1 (zh) * | 2022-04-29 | 2023-11-02 | 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 |
| EP4605391A1 (en) | 2022-10-21 | 2025-08-27 | Exelixis, Inc. | 4,5,6,7-tetrahydro-1-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 |
| TW202509030A (zh) * | 2023-05-08 | 2025-03-01 | 美商譚格醫療公司 | 化合物及使用方法 |
| 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 |
| CN121511238A (zh) * | 2023-07-05 | 2026-02-10 | 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 |
| CN121219283A (zh) * | 2023-07-05 | 2025-12-26 | 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 |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| ES2242839T3 (es) | 2001-04-20 | 2005-11-16 | Ciba Specialty Chemicals Holding Inc. | 4-amino-2- (piridin-2-il)pirimidina como sustancias activas microbicidas. |
| EP1254903B1 (en) * | 2001-04-20 | 2005-06-08 | Ciba SC Holding AG | 4-Amino-2-(pyridin-2-yl)pyrimidine as microbicidal active substances |
| JPWO2003026661A1 (ja) * | 2001-09-14 | 2005-01-06 | 山之内製薬株式会社 | インスリン分泌促進剤及び新規なピリミジン誘導体 |
| JP2005516005A (ja) | 2001-12-07 | 2005-06-02 | バーテクス ファーマスーティカルズ インコーポレイテッド | Ｇｓｋ−３阻害剤として有用なピリミジンベースの化合物 |
| ATE366045T1 (de) | 2002-03-15 | 2007-07-15 | Ciba Sc Holding Ag | Verwendung von 4-aminopyrimidinen zur antimikrobiellen behandlung von oberflächen |
| EP1537116B1 (en) * | 2002-09-04 | 2010-06-02 | Schering Corporation | Pyrazolopyrimidines suitable for the treatment of cancer diseases |
| WO2005103022A1 (en) * | 2004-04-20 | 2005-11-03 | Transtech Pharma, Inc. | Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators |
| US8338591B2 (en) | 2004-05-08 | 2012-12-25 | Novartis International Pharmaceutical Ltd. | 3-aryl-5,6-disubstituted pyridazines |
| JP2008526734A (ja) | 2004-12-31 | 2008-07-24 | エスケー ケミカルズ カンパニー リミテッド | 糖尿及び肥満治療予防に有効なキナゾリン誘導体 |
| US20070032499A1 (en) | 2005-08-05 | 2007-02-08 | Philippe Guedat | Novel cysteine protease inhibitors and their therapeutic applications |
| WO2008040753A1 (en) | 2006-10-03 | 2008-04-10 | Neurosearch A/S | Indazolyl derivatives useful as potassium channel modulating agents |
| 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 |
| US20130045992A1 (en) | 2010-01-28 | 2013-02-21 | President And Fellows Of Harvard College | Compositions and Methods for Enhancing Proteasome Activity |
| 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 |
| WO2011140527A2 (en) | 2010-05-07 | 2011-11-10 | California Institute Of Technology And The University Of Kansas | Methods and compositions for inhibition of the transitional endoplasmic reticulum atpase |
| JP6042331B2 (ja) | 2010-07-23 | 2016-12-14 | プレジデント アンド フェローズ オブ ハーバード カレッジ | プロテアソーム活性を向上させる三環系化合物 |
| WO2012040527A2 (en) | 2010-09-24 | 2012-03-29 | 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 |
| AU2012280725B2 (en) * | 2011-07-07 | 2017-02-02 | Merck Patent Gmbh | Substituted azaheterocycles for the treatment of cancer |
| 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 |
| CA2852518C (en) | 2011-10-19 | 2019-09-24 | Vivolux Ab | Azepanone compounds and their use for the inhibition of deubiquitinating activity and the treatment of cancer |
| CA2861462A1 (en) | 2012-01-25 | 2013-08-01 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating tricyclic compounds |
| EP2806875B1 (en) | 2012-01-25 | 2017-07-19 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating compounds |
| EP2938610A2 (en) | 2012-12-28 | 2015-11-04 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof |
-
2013
- 2013-12-26 EP EP13821618.9A patent/EP2938610A2/en not_active Withdrawn
- 2013-12-26 WO PCT/US2013/077804 patent/WO2014105952A2/en not_active Ceased
- 2013-12-26 CA CA2896731A patent/CA2896731A1/en not_active Abandoned
- 2013-12-26 US US14/655,538 patent/US9802904B2/en active Active
- 2013-12-26 AU AU2013370417A patent/AU2013370417A1/en not_active Abandoned
- 2013-12-26 JP JP2015550767A patent/JP2016504365A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016504365A5 (enExample) | ||
| JP2017531041A5 (enExample) | ||
| EA201201677A1 (ru) | Производные гетероарилимидазолона в качестве ингибиторов jak | |
| EA201200938A1 (ru) | Производные имидазопиридина в качестве ингибиторов jak | |
| NZ718487A (en) | Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof | |
| RU2020102453A (ru) | Фармацевтические композиции | |
| EA201201143A1 (ru) | Производные пиразола в качестве ингибиторов jak | |
| PE20081888A1 (es) | ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3 | |
| JP2014500870A5 (enExample) | ||
| EA201301319A1 (ru) | Производные пиридин-2(1н)-она, применимые в качестве лекарственных средств для лечения миелопролиферативных нарушений, отторжения трансплантата, иммунологически обусловленных и воспалительных заболеваний | |
| JP2014508811A5 (enExample) | ||
| SV2010003463A (es) | Compuestos organicos | |
| EA201400182A1 (ru) | Производные пиридин-2(1н)-она в качестве ингибиторов jak | |
| MX2013005008A (es) | Derivados de carboxamida y urea heteroaromaticos sustituidos como ligandos del receptor vanilloide. | |
| CL2008001230A1 (es) | Compuestos derivados de pirrol (2.3-d)pirimidina. purin-6-ilo o pirazol(3,4-d)pirimldina, inhibidores de quinasa p70 s6; composición farmaceutica; y uso para la preparación de medicamentos utiles en el tratamiento de adenocarcinomas del colon e inhibición de angiogénesis. | |
| TN2016000014A1 (fr) | Nouveaux dérivés d'indolizine, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent | |
| EA201000614A1 (ru) | Производные пурина как лиганды аденозинового рецептора а | |
| NZ590650A (en) | Buprenorphine analogs | |
| EA201200471A1 (ru) | Простые эфирные производные бициклических гетероарилов | |
| RU2015135722A (ru) | Дейтерированный фениламинопиримидин и фармацевтическая композиция, содержащая такое соединение | |
| MX2012013274A (es) | Novedosos derivados de la pirimidina. | |
| EA201591301A1 (ru) | Новые пиримидиновые и пиридиновые соединения и их применение | |
| RU2013141559A (ru) | Способ ингибирования клеток опухоли гамартомы | |
| JP2016537382A5 (enExample) | ||
| JP2015502367A5 (enExample) |