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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
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    • 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
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    • 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
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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
    • C07D239/88—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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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Hematology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Rheumatology (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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CN102574816A true CN102574816A (zh) 2012-07-11

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US (1) US20120258975A1 (https=)
EP (1) EP2456761A2 (https=)
JP (1) JP2013500255A (https=)
KR (1) KR20120100886A (https=)
CN (1) CN102574816A (https=)
AU (1) AU2010276223A1 (https=)
BR (1) BR112012001316A2 (https=)
CA (1) CA2767772A1 (https=)
CL (1) CL2012000163A1 (https=)
IL (1) IL217502A0 (https=)
IN (1) IN2012DN01478A (https=)
MX (1) MX2012000940A (https=)
PE (1) PE20120798A1 (https=)
PH (1) PH12012500097A1 (https=)
RU (1) RU2012105914A (https=)
SG (1) SG177486A1 (https=)
WO (1) WO2011011522A2 (https=)
ZA (1) ZA201201224B (https=)

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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

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KR20180086187A (ko) * 2015-10-05 2018-07-30 더 트러스티이스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 자가포식 유동의 활성체 및 포스포리파제 d 및 타우를 포함하는 단백질 응집물의 클리어런스 및 단백질질환의 치료
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CN115485385A (zh) 2020-03-04 2022-12-16 瑞泽恩制药公司 用于使肿瘤细胞对免疫疗法敏感的方法和组合物
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KR20250004810A (ko) 2022-04-20 2025-01-08 컴쿼트 바이오사이언시즈 인크. 대환식 헤테로환 및 이의 용도
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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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