TW202339730A - Gcn2及perk激酶抑制劑及其使用方法 - Google Patents
Gcn2及perk激酶抑制劑及其使用方法 Download PDFInfo
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Classifications
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
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- General Health & Medical Sciences (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US202163285833P | 2021-12-03 | 2021-12-03 | |
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| US202263348557P | 2022-06-03 | 2022-06-03 | |
| US63/348,557 | 2022-06-03 |
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| TW202339730A true TW202339730A (zh) | 2023-10-16 |
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| TW111146350A TW202339730A (zh) | 2021-12-03 | 2022-12-02 | Gcn2及perk激酶抑制劑及其使用方法 |
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| EP (1) | EP4440703A1 (https=) |
| JP (1) | JP2024544632A (https=) |
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| WO2024249493A2 (en) * | 2023-05-30 | 2024-12-05 | Deciphera Pharmaceuticals, Llc | Gcn2 and perk kinase modulators and methods of use thereof |
| WO2025043350A1 (en) * | 2023-08-30 | 2025-03-06 | Ontario Institute For Cancer Research (Oicr) | Triazolopyridopyrimidine and dihydroimidazopyridopyrimidine derivatives as inhibitors of the gcn2 kinase, compositions and uses thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4038932A1 (de) | 1990-12-06 | 1992-06-11 | Roehm Gmbh | Diuretische und antikaliuretisch wirksame pteridinderivate |
| US6060477A (en) | 1995-06-07 | 2000-05-09 | Cell Pathways, Inc. | Method of treating a patient having precancerous lesions with phenyl cycloamino pyrimidinone derivatives |
| TR199902301T2 (xx) | 1997-03-19 | 1999-12-21 | Basf Aktiengesellschaft | Pirilo $2,3D]pirimidinler ve onlar�n kullan�m�. |
| US7863444B2 (en) * | 1997-03-19 | 2011-01-04 | Abbott Laboratories | 4-aminopyrrolopyrimidines as kinase inhibitors |
| ES2253930T3 (es) | 1998-09-18 | 2006-06-01 | ABBOTT GMBH & CO. KG | 4-aminopirrolopirimidinas como inhibidores de quinasa. |
| US6713474B2 (en) | 1998-09-18 | 2004-03-30 | Abbott Gmbh & Co. Kg | Pyrrolopyrimidines as therapeutic agents |
| US7276506B2 (en) | 1998-12-28 | 2007-10-02 | 4 Aza Bioscience Nv | Immunosuppressive effects of pteridine derivatives |
| US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
| US7071199B1 (en) | 1999-09-17 | 2006-07-04 | Abbott Gmbh & Cco. Kg | Kinase inhibitors as therapeutic agents |
| JP2003509428A (ja) | 1999-09-17 | 2003-03-11 | アボツト・ゲー・エム・ベー・ハー・ウント・コンパニー・カーゲー | 治療薬としてのピラゾロピリミジン |
| AU2000240570A1 (en) | 2000-03-29 | 2001-10-08 | Knoll Gesellschaft Mit Beschraenkter Haftung | Pyrrolopyrimidines as tyrosine kinase inhibitors |
| US20030225098A1 (en) | 2002-03-21 | 2003-12-04 | Hirst Gavin C. | Kinase inhibitors |
| US20030199525A1 (en) | 2002-03-21 | 2003-10-23 | Hirst Gavin C. | Kinase inhibitors |
| US7202257B2 (en) | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| US7279576B2 (en) | 2002-12-31 | 2007-10-09 | Deciphera Pharmaceuticals, Llc | Anti-cancer medicaments |
| WO2004100868A2 (en) | 2003-04-23 | 2004-11-25 | Abbott Laboratories | Method of treating transplant rejection |
| WO2004100947A2 (en) | 2003-05-06 | 2004-11-25 | Smithkline Beecham Corporation | Novel chemical compounds |
| US7202363B2 (en) | 2003-07-24 | 2007-04-10 | Abbott Laboratories | Thienopyridine and furopyridine kinase inhibitors |
| US20050026944A1 (en) | 2003-07-24 | 2005-02-03 | Patrick Betschmann | Thienopyridine and furopyridine kinase inhibitors |
| DK1663244T3 (da) | 2003-09-12 | 2007-12-03 | 4 Aza Ip Nv | Pteridin-derivater til behandling af TNF-alpha-beslægtede sygdomme |
| AU2004279427B2 (en) | 2003-10-08 | 2008-07-03 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| CN1914204A (zh) | 2003-12-09 | 2007-02-14 | 弗特克斯药品有限公司 | 萘啶衍生物及其作为毒蕈碱性受体调节剂的用途 |
| CA2549641A1 (en) | 2003-12-19 | 2005-07-21 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| JP2007520559A (ja) | 2004-02-03 | 2007-07-26 | アボット・ラボラトリーズ | 治療薬としてのアミノベンゾオキサゾール類 |
| AU2005258266A1 (en) | 2004-06-23 | 2006-01-05 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| CA2592118C (en) | 2004-12-23 | 2015-11-17 | Deciphera Pharmaceuticals, Llc | Urea derivatives as enzyme modulators |
| EP1871773A1 (en) | 2005-03-17 | 2008-01-02 | Novartis AG | N-[3-(1-amino-5,6,7,8-tetrahydro-2,4,4b-triazafluoren-9-yl)-phenyl]benzamides as tyrosine/threonine kinase inhibitors, in particular b-raf kinase |
| WO2008003149A2 (en) | 2006-07-06 | 2008-01-10 | Gilead Sciences , Inc. | Substituted pteridines for the treatment and prevention of viral infections |
| US7897762B2 (en) | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| US8188113B2 (en) | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| PT2074122E (pt) | 2006-09-15 | 2011-08-24 | Pfizer Prod Inc | Compostos de pirido(2,3-d)-pirimidinona e sua utilização como inibidores de pi3 |
| US7893066B2 (en) | 2006-10-05 | 2011-02-22 | Gilead Palo Alto, Inc. | Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors |
| CA2665476A1 (en) | 2006-10-05 | 2008-04-10 | Cv Therapeutics, Inc. | Bicyclic nitrogen-containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors |
| US7790756B2 (en) | 2006-10-11 | 2010-09-07 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| WO2008051757A1 (en) | 2006-10-20 | 2008-05-02 | Irm Llc | Compositions and methods for modulating c-kit and pdgfr receptors |
| WO2008077649A1 (en) | 2006-12-26 | 2008-07-03 | Gilead Sciences, Inc. | Pyrido(3,2-d)pyrimidines useful for treating viral infectons |
| CA2681560A1 (en) | 2007-04-09 | 2008-10-16 | Cv Therapeutics, Inc. | Pteridinone derivatives for use as stearoyl coa desaturase inhibitors |
| WO2008131276A1 (en) | 2007-04-20 | 2008-10-30 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| WO2009111028A1 (en) | 2008-03-04 | 2009-09-11 | Vitae Pharmaceuticals, Inc. | Aurora kinase inhibitors |
| WO2009126123A1 (en) | 2008-04-10 | 2009-10-15 | Cv Therapeutics Inc. | Bicyclic nitrogen containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors |
| WO2010002998A1 (en) | 2008-07-03 | 2010-01-07 | Gilead Sciences, Inc. | 2,4,6-TRISUBSTITUTED PYRIDO (3,2-d) PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS |
| UY31982A (es) | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas |
| UY31984A (es) | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | DERIVADOS DE 1-(3,4-difluorobencil)-6-oxo-1,6-dihidropirimidin-5-carboxamidas N-sustituidas y de 2-(3,4-difluorobencil)-3-oxo-2,3-dihidro-1H-pirazol-4-carboxamidas N-sustituidas. |
| EP2358720B1 (en) | 2008-10-16 | 2016-03-02 | The Regents of The University of California | Fused ring heteroaryl kinase inhibitors |
| JP5444365B2 (ja) | 2008-10-29 | 2014-03-19 | デシフェラ ファーマシューティカルズ,エルエルシー | 抗癌活性および抗増殖活性を示すシクロプロパンアミドおよび類似物質 |
| WO2011047384A2 (en) | 2009-10-16 | 2011-04-21 | The Regents Of The University Of California | Methods of inhibiting ire1 |
| US9765037B2 (en) | 2010-01-28 | 2017-09-19 | University Of Washington Through Its Center For Commercialization | Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases |
| CA2800998A1 (en) | 2010-04-29 | 2011-11-10 | Deciphera Pharmaceuticals, Llc | Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities |
| SG185073A1 (en) | 2010-04-29 | 2012-12-28 | Deciphera Pharmaceuticals Llc | Cyclopropyl dicarboxamides and analogs exhibiting anti-cancer and anti-proliferative activites |
| MX2013007261A (es) | 2010-12-23 | 2013-11-04 | Amgen Inc | Compuestos heterociclicos y sus usos. |
| WO2013043232A2 (en) | 2011-04-08 | 2013-03-28 | Afraxis, Inc. | 8-ethyl-6-(aryl)pyrido [2,3-d]pyrimidin-7(8h) -ones for the treatment of nervous system disorders and cancer |
| WO2012158795A1 (en) | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| JP2015501786A (ja) | 2011-11-04 | 2015-01-19 | アフラクシス・ホールディングス・インコーポレイテッドAfraxis Holdings,Inc. | 脆弱x症候群を治療するためのpak阻害剤 |
| JP2015507606A (ja) | 2011-11-22 | 2015-03-12 | デシフェラ ファーマシューティカルズ,エルエルシー | 抗癌および抗増殖作用を示すピリドンアミドおよび類似体 |
| AR090151A1 (es) | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| WO2013134298A1 (en) | 2012-03-07 | 2013-09-12 | Deciphera Pharmaceuticals, Llc | Raf inhibitor compounds |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| WO2013191965A1 (en) | 2012-06-18 | 2013-12-27 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases |
| CN102746241B (zh) | 2012-07-02 | 2014-11-05 | 西安交通大学 | 2,3,5-三取代苯甲酰胺类化合物及其制备方法和用途 |
| US20140038991A1 (en) | 2012-08-06 | 2014-02-06 | Astar Biotech Llc | Protein Kinase Inhibitors |
| RU2015113597A (ru) | 2012-09-14 | 2016-11-10 | Итернити Байосайенс Инк. | Производные аминоизохинолина в качестве ингибиторов протеинкиназы |
| JP6495886B2 (ja) | 2013-03-15 | 2019-04-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Btk阻害剤としての複素環式芳香族化合物 |
| US9012635B2 (en) | 2013-03-15 | 2015-04-21 | Deciphera Pharmaceuticals, Llc | Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities |
| WO2014145015A2 (en) | 2013-03-15 | 2014-09-18 | Deciphera Pharmaceuticals, Llc | Imidazolidinones and analogs exhibiting anti-cancer and anti-proliferative activities |
| JP6364472B2 (ja) | 2013-03-15 | 2018-07-25 | デシフェラ ファーマシューティカルズ,エルエルシー | 抗がんおよび抗増殖活性を示すn−アシル−n’−(ピリジン−2−イル)尿素および類似体 |
| DK2968286T3 (en) | 2013-03-15 | 2018-01-02 | Deciphera Pharmaceuticals Llc | 2-AMINOPYRIMIDIN-6-ONES AND ANALOGS THAT HAVE ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES |
| WO2014145023A1 (en) | 2013-03-15 | 2014-09-18 | Deciphera Pharmaceuticals, Llc | 1,2,4-triazol-5-ones and analogs exhibiting anti-cancer and anti-proliferative activities |
| WO2014145029A2 (en) | 2013-03-15 | 2014-09-18 | Deciphera Pharmaceuticals, Llc | N-acyl-n'-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities |
| US9457019B2 (en) | 2013-11-07 | 2016-10-04 | Deciphera Pharmaceuticals, Llc | Methods for inhibiting tie-2 kinase useful in the treatment of cancer |
| CN105330699B (zh) | 2014-08-13 | 2018-12-04 | 山东汇睿迪生物技术有限公司 | 一种含磷吡啶并[2,3-d]嘧啶-7-酮类化合物或其药学上可接受的盐、药物组合物及其应用 |
| KR102562866B1 (ko) | 2014-11-14 | 2023-08-04 | 네르비아노 메디칼 사이언시스 에스.알.엘. | 단백질 키나아제 억제제로서의 6-아미노-7-바이사이클로-7-데아자-퓨린 유도체 |
| JP6867417B2 (ja) * | 2016-06-21 | 2021-04-28 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害剤としてのn−(置換フェニル)−スルホンアミド誘導体 |
| ES2965081T3 (es) | 2016-07-07 | 2024-04-11 | Daewoong Pharmaceutical Co Ltd | Derivados 4-aminopirazolo[3,4-d]pirimidinil-azabiciclo y composición farmacéutica que comprende dichos derivados |
| AU2017373758B2 (en) | 2016-12-07 | 2021-12-16 | Orimos Therapeutics Co., Ltd. | Compounds and pharmaceutical compositions for modulating SGK activity, and methods thereof |
| CA3174865A1 (en) | 2016-12-26 | 2018-07-05 | Institute Of Materia Medica, Chinese Academy Of Medical Sciences | Quinazoline compound and preparation method, application, and pharmaceutical composition thereof |
| MY205552A (en) | 2017-05-30 | 2024-10-25 | Deciphera Pharmaceuticals Inc | Use of 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl ]-3-phenylurea and analogs for the treatment of cancers associated with genetic abnormalities in platelet derived growth factor receptor alpha |
| JP7126084B2 (ja) | 2017-06-01 | 2022-08-26 | コーネル ユニバーシティー | Ire1小分子阻害薬 |
| CN109721531B (zh) | 2017-10-27 | 2022-07-29 | 中国科学院合肥物质科学研究院 | 一种新型的脂质体激酶抑制剂 |
| WO2019094641A1 (en) | 2017-11-10 | 2019-05-16 | Quentis Therapeutics, Inc. | Ire1 small molecule inhibitors |
| CN118416236A (zh) | 2018-01-31 | 2024-08-02 | 德西费拉制药有限责任公司 | 治疗胃肠道间质瘤的组合疗法 |
| IL276398B2 (en) | 2018-01-31 | 2026-03-01 | Deciphera Pharmaceuticals Llc | Combination therapy for mastocytosis |
| US12351576B2 (en) | 2018-09-14 | 2025-07-08 | Abbisko Therapeutics Co., Ltd. | FGFR inhibitor, preparation method therefor and application thereof |
| US11612606B2 (en) | 2018-10-03 | 2023-03-28 | Genentech, Inc. | 8-aminoisoquinoline compounds and uses thereof |
| US12071426B2 (en) | 2018-12-03 | 2024-08-27 | Cornell University | IRE1 small molecule inhibitors |
| BR112021012812A2 (pt) | 2018-12-28 | 2021-12-07 | Deciphera Pharmaceuticals Llc | Csf1r inhibitors para uso e tratamento de câncer |
| WO2020142612A1 (en) | 2019-01-03 | 2020-07-09 | Genentech, Inc. | Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases. |
| WO2020147097A1 (zh) | 2019-01-18 | 2020-07-23 | 中国科学院合肥物质科学研究院 | 一种新型的脂质体激酶抑制剂 |
| KR102747104B1 (ko) | 2019-02-18 | 2024-12-27 | 한국과학기술연구원 | 단백질 키나아제 저해 활성을 갖는 신규한 피리도[3,4-d]피리미딘-8-온 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물 |
| AR118119A1 (es) | 2019-02-18 | 2021-09-22 | Genentech Inc | Compuestos de pirido-pirimidinilo y métodos de uso |
| CN112955432B (zh) | 2019-03-06 | 2022-11-22 | 江苏恒瑞医药股份有限公司 | 稠合芳香环类衍生物、其制备方法及其在医药上的应用 |
| US20220388964A1 (en) | 2019-04-12 | 2022-12-08 | Hibercell, Inc. | (aza)indazolyl-aryl sulfonamide and related compounds and their use in treating medical conditions |
| US11518758B2 (en) | 2019-05-10 | 2022-12-06 | Deciphera Pharmaceuticals, Llc | Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof |
| PE20220597A1 (es) | 2019-05-10 | 2022-04-22 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de fenilaminopirimidina amida y metodos de uso de estos |
| WO2020232401A1 (en) | 2019-05-15 | 2020-11-19 | Cornell University | Combination therapies with ire1 small molecule inhibitors |
| WO2020232403A1 (en) | 2019-05-15 | 2020-11-19 | Cornell University | Treatment of fibrosis with ire1 small molecule inhibitors |
| SG11202112952SA (en) | 2019-05-31 | 2021-12-30 | Servier Lab | Heterobicyclic inhibitors of mat2a and methods of use for treating cancer |
| EP3983400B1 (en) | 2019-06-11 | 2025-05-28 | Genentech, Inc. | Quinazolinyl compounds and methods of use |
| PE20221083A1 (es) | 2019-06-17 | 2022-07-05 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| EP4013412B1 (en) | 2019-08-12 | 2026-01-28 | Deciphera Pharmaceuticals, LLC | Ripretinib for treating gastrointestinal stromal tumors |
| US20230277522A9 (en) | 2019-08-12 | 2023-09-07 | Deciphera Pharmaceuticals, Llc | Methods for treating vascular malformations |
| MX2022008103A (es) | 2019-12-30 | 2022-09-19 | Deciphera Pharmaceuticals Llc | Formulaciones de inhibidores de la cinasa amorfa y metodos de estas. |
| EP4084779B1 (en) | 2019-12-30 | 2024-10-09 | Deciphera Pharmaceuticals, LLC | Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea |
| KR102396930B1 (ko) | 2020-01-15 | 2022-05-12 | 한국과학기술연구원 | 피리도[3,4-d]피리미딘 유도체 및 이를 포함하는 치료용 약학 조성물 |
| JP2023514328A (ja) * | 2020-02-17 | 2023-04-05 | アレスタ・セラピューティクス・ベスローテン・フェンノートシャップ | Gcn2モジュレーター化合物 |
| IL302807A (en) | 2020-11-18 | 2023-07-01 | Deciphera Pharmaceuticals Llc | Gcn2 and perk kinase inhibitors and methods of use thereof |
| CN117241800A (zh) | 2020-11-25 | 2023-12-15 | 德西费拉制药有限责任公司 | Vps34抑制剂的抗病毒活性 |
| CN117136062A (zh) | 2020-11-25 | 2023-11-28 | 德西费拉制药有限责任公司 | Vps34抑制剂的抗病毒活性 |
| CA3200031A1 (en) | 2020-11-25 | 2022-06-02 | Deciphera Pharmaceuticals, Llc | Anti-viral activity of vps34 inhibitors |
| CA3199999A1 (en) | 2020-11-25 | 2022-06-02 | Deciphera Pharmaceuticals, Llc | Morpholino derivatives as vsp34 inhibitors for use in the treatment of a viral infection |
| US11801238B2 (en) | 2020-11-25 | 2023-10-31 | Deciphera Pharmaceuticals, Llc | Anti-viral activity of VPS34 inhibitors |
| CN117241829A (zh) | 2020-11-25 | 2023-12-15 | 德西费拉制药有限责任公司 | Vps34抑制剂的抗病毒活性 |
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