CN102574816A - 有效的小分子自噬抑制剂及其使用方法 - Google Patents

有效的小分子自噬抑制剂及其使用方法 Download PDF

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Publication number
CN102574816A
CN102574816A CN2010800332736A CN201080033273A CN102574816A CN 102574816 A CN102574816 A CN 102574816A CN 2010800332736 A CN2010800332736 A CN 2010800332736A CN 201080033273 A CN201080033273 A CN 201080033273A CN 102574816 A CN102574816 A CN 102574816A
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arbitrary described
compound
autophagy
described compound
cancer
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Chinese (zh)
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袁君英
马大伟
刘君丽
张丽红
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Shanghai Institute of Organic Chemistry of CAS
Harvard University
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Shanghai Institute of Organic Chemistry of CAS
Harvard University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/93—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN2010800332736A 2009-07-21 2010-07-21 有效的小分子自噬抑制剂及其使用方法 Pending CN102574816A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US22716409P 2009-07-21 2009-07-21
US61/227,164 2009-07-21
US29673510P 2010-01-20 2010-01-20
US61/296,735 2010-01-20
PCT/US2010/042759 WO2011011522A2 (en) 2009-07-21 2010-07-21 Potent small molecule inhibitors of autophagy, and methods of use thereof

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EP (1) EP2456761A2 (enExample)
JP (1) JP2013500255A (enExample)
KR (1) KR20120100886A (enExample)
CN (1) CN102574816A (enExample)
AU (1) AU2010276223A1 (enExample)
BR (1) BR112012001316A2 (enExample)
CA (1) CA2767772A1 (enExample)
CL (1) CL2012000163A1 (enExample)
IL (1) IL217502A0 (enExample)
IN (1) IN2012DN01478A (enExample)
MX (1) MX2012000940A (enExample)
PE (1) PE20120798A1 (enExample)
PH (1) PH12012500097A1 (enExample)
RU (1) RU2012105914A (enExample)
SG (1) SG177486A1 (enExample)
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ZA (1) ZA201201224B (enExample)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104164471A (zh) * 2013-11-04 2014-11-26 复旦大学 基于细胞自噬的抗肿瘤药物的筛选方法
CN107835688A (zh) * 2015-05-08 2018-03-23 得克萨斯州大学系统董事会 用于治疗阿尔茨海默病的神经元钙池操纵的钙进入途径的活化
WO2018214813A1 (zh) * 2017-05-22 2018-11-29 苏州偶领生物医药有限公司 一种共价键修饰哺乳动物atg8同源物的方法
CN109721554A (zh) * 2019-01-08 2019-05-07 贵州大学 一类4-氨基喹唑啉类化合物及其制备方法和应用
CN111304230A (zh) * 2013-07-26 2020-06-19 哈佛大学校长及研究员协会 基因组工程
CN112608302A (zh) * 2020-12-28 2021-04-06 郑州大学第一附属医院 低氧还原激活靶向泛素化降解egfr蛋白的喹唑啉类衍生物及其应用
CN114258318A (zh) * 2019-06-17 2022-03-29 德西费拉制药有限责任公司 氨基嘧啶酰胺自噬抑制剂及其使用方法
US12071432B2 (en) 2019-05-10 2024-08-27 Deciphera Pharmaceuticals, Llc Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof
US12479833B2 (en) 2019-05-10 2025-11-25 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2475378B1 (en) 2009-09-10 2019-07-24 Mayo Foundation For Medical Education And Research USP10 modulation for use in the treatment of cancer
US8598344B2 (en) * 2009-11-30 2013-12-03 Senex Biotechnology CDKI pathway inhibitors and uses thereof
ES2609578T3 (es) 2011-03-04 2017-04-21 Glaxosmithkline Intellectual Property Development Limited Amino-quinolinas como inhibidores de quinasa
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
SG11201401343YA (en) * 2011-09-13 2014-08-28 Igor Roninson TREATMENT OF DISEASE OR DISORDERS CAUSED BY INDUCED NFkB TRANSCRIPTIONAL ACTIVITY
TWI592417B (zh) 2012-09-13 2017-07-21 葛蘭素史克智慧財產發展有限公司 胺基喹唑啉激酶抑制劑之前藥
US9802904B2 (en) 2012-12-28 2017-10-31 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof
CA2898018C (en) 2013-02-01 2021-02-09 Wellstat Therapeutics Corporation Substituted quinolin-4-amine compounds and pharmaceutical compositions thereof having anti-inflammatory, antifungal, antiparasitic and anticancer activity
BR112015019624A2 (pt) 2013-02-21 2017-07-18 Glaxosmithkline Ip Dev Ltd quinazolinas como inibidores de quinase
WO2014134169A1 (en) * 2013-02-26 2014-09-04 Senex Biotechnology, Inc. Inhibitors of cdk8/19 for use in treating estrogen receptor positive breast cancer
WO2014145512A2 (en) * 2013-03-15 2014-09-18 President And Fellows Of Harvard College Potent small molecule inhibitors of autophagy, and methods of use thereof
WO2014144752A1 (en) * 2013-03-15 2014-09-18 The Board Of Trustees Of The Leland Stanford Junior University Targeting chromatin modifiers for the treatment of medical conditions
US9393244B2 (en) 2013-03-15 2016-07-19 Georgetown University Increasing parkin activity by administering a deubiquitinating enzyme inhibitor
JP6740354B2 (ja) * 2015-10-05 2020-08-12 ザ トラスティーズ オブ コロンビア ユニバーシティー イン ザ シティー オブ ニューヨーク オートファジーの流れ及びホスホリパーゼｄ及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法
EP3184514A1 (en) * 2015-12-23 2017-06-28 Deutsches Krebsforschungszentrum Autophagy inhibitors
GB201700814D0 (en) * 2017-01-17 2017-03-01 Liverpool School Tropical Medicine Compounds
JP7633676B2 (ja) 2018-07-26 2025-02-20 ドメイン・セラピューティクス 置換キナゾリノン誘導体、及びｍＧｌｕＲ４のポジティブアロステリック調節剤としてのその使用
US20210215710A1 (en) * 2019-12-23 2021-07-15 University Health Network Methods for use of cdx2 as a biomarker to guide use of autophagy inhibitors in ovarian cancer
WO2021178556A1 (en) 2020-03-04 2021-09-10 Regeneron Pharmaceuticals, Inc. Methods and compositions for sensitization of tumor cells to immune therapy
JP2024504587A (ja) * 2021-01-14 2024-02-01 ジョージタウン ユニバーシティ Ｕｓｐ１３阻害剤及びその使用方法
WO2022187411A1 (en) * 2021-03-02 2022-09-09 Kumquat Biosciences Inc. Heterocycles and uses thereof
US20240365736A1 (en) 2021-09-01 2024-11-07 Oerth Bio Llc Compositions and methods for targeted degradation of proteins in a plant cell
CN114224895B (zh) * 2022-01-06 2023-06-30 山东农业大学 3-甲基腺嘌呤在清除牛乳腺上皮细胞内无乳链球菌中的应用
CA3246750A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. MACROCYCLES AND HETEROCYCLES AND THEIR USES
CN116179494B (zh) * 2022-10-13 2024-01-26 武汉生物制品研究所有限责任公司 低成瘤性的mdck细胞株及其构建方法和应用
DE102022131212A1 (de) 2022-11-25 2024-05-29 Dr. Ing. H.C. F. Porsche Aktiengesellschaft Luftzufuhrvorrichtung einer Kraftfahrzeugkarosserie eines Kraftfahrzeugs

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS542325A (en) * 1977-06-07 1979-01-09 Sankyo Co Ltd Agricultural and horticultural pesticide
JPS542327A (en) * 1977-06-07 1979-01-09 Sankyo Co Ltd Agricultural and horticultural pesticide
GT198900008A (es) * 1988-01-29 1990-07-17 Derivados de quinolina, quinazolina y cinolina.
IL89027A (en) * 1988-01-29 1993-01-31 Lilly Co Eli Quinazoline derivatives, process for their preparation and fungicidal, insecticidal and miticidal compositions containing them
US5034393A (en) * 1989-07-27 1991-07-23 Dowelanco Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives
US5227387A (en) * 1991-09-03 1993-07-13 Dowelanco Quinoline nematicidal method
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
US6046206A (en) * 1995-06-07 2000-04-04 Cell Pathways, Inc. Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
US6262059B1 (en) * 1995-06-07 2001-07-17 Cell Pathways, Inc. Method of treating a patient having precancerous lesions with quinazoline derivatives
DE10042060A1 (de) * 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU2003207291A1 (en) * 2002-02-06 2003-09-02 Ube Industries, Ltd. Process for producing 4-aminoquinazoline compound
JP2004059454A (ja) * 2002-07-25 2004-02-26 Japan Energy Corp キナゾリン誘導体及びＮＦ−κＢ活性化阻害剤
EP1720841B1 (en) * 2004-02-19 2015-11-04 Rexahn Pharmaceuticals, Inc. Quinazoline derivatives and therapeutic use thereof
WO2006071095A1 (en) * 2004-12-31 2006-07-06 Sk Chemicals Co., Ltd. Quinazoline derivatives for the treatment and prevention of diabetes and obesity
US20080269259A1 (en) 2005-01-19 2008-10-30 The Trustees Of The University Of Pennsylvania Regulation of Autophagy and Cell Survival
WO2008122038A1 (en) * 2007-04-02 2008-10-09 President And Fellows Of Harvard College Regulating autophagy
US8039502B2 (en) 2007-07-24 2011-10-18 The Ohio State University Research Foundation Anti-infective agents against intracellular pathogens

Cited By (12)

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Publication number Priority date Publication date Assignee Title
CN111304230A (zh) * 2013-07-26 2020-06-19 哈佛大学校长及研究员协会 基因组工程
CN104164471A (zh) * 2013-11-04 2014-11-26 复旦大学 基于细胞自噬的抗肿瘤药物的筛选方法
CN107835688A (zh) * 2015-05-08 2018-03-23 得克萨斯州大学系统董事会 用于治疗阿尔茨海默病的神经元钙池操纵的钙进入途径的活化
WO2018214813A1 (zh) * 2017-05-22 2018-11-29 苏州偶领生物医药有限公司 一种共价键修饰哺乳动物atg8同源物的方法
US20200069609A1 (en) * 2017-05-22 2020-03-05 Wigen Biomedicine Technology (shanghai) Co., Ltd. Method for covalent bond modifying mammalian atg8 homologue
CN110933932A (zh) * 2017-05-22 2020-03-27 微境生物医药科技(上海)有限公司 一种共价键修饰哺乳动物atg8同源物的方法
CN109721554A (zh) * 2019-01-08 2019-05-07 贵州大学 一类4-氨基喹唑啉类化合物及其制备方法和应用
US12071432B2 (en) 2019-05-10 2024-08-27 Deciphera Pharmaceuticals, Llc Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof
US12479833B2 (en) 2019-05-10 2025-11-25 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
CN114258318A (zh) * 2019-06-17 2022-03-29 德西费拉制药有限责任公司 氨基嘧啶酰胺自噬抑制剂及其使用方法
US12377097B2 (en) 2019-06-17 2025-08-05 Deciphera Pharmaceuticals, Llc Aminopyrimidine amide autophagy inhibitors and methods of use thereof
CN112608302A (zh) * 2020-12-28 2021-04-06 郑州大学第一附属医院 低氧还原激活靶向泛素化降解egfr蛋白的喹唑啉类衍生物及其应用

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US20120258975A1 (en) 2012-10-11
BR112012001316A2 (pt) 2017-08-08
EP2456761A2 (en) 2012-05-30
MX2012000940A (es) 2012-05-08
JP2013500255A (ja) 2013-01-07
AU2010276223A1 (en) 2012-03-08
PH12012500097A1 (en) 2011-01-27
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RU2012105914A (ru) 2013-08-27
PE20120798A1 (es) 2012-07-27
IN2012DN01478A (enExample) 2015-06-05
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IL217502A0 (en) 2012-02-29
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