WO2010139180A8 - 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用 - Google Patents

作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用 Download PDF

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Publication number
WO2010139180A8
WO2010139180A8 PCT/CN2010/000272 CN2010000272W WO2010139180A8 WO 2010139180 A8 WO2010139180 A8 WO 2010139180A8 CN 2010000272 W CN2010000272 W CN 2010000272W WO 2010139180 A8 WO2010139180 A8 WO 2010139180A8
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WO
WIPO (PCT)
Prior art keywords
protein kinase
histone deacetylase
diseases
preparation methods
carboxamide derivatives
Prior art date
Application number
PCT/CN2010/000272
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English (en)
French (fr)
Other versions
WO2010139180A1 (zh
Inventor
鲁先平
李志斌
山松
余金迪
宁志强
Original Assignee
深圳微芯生物科技有限责任公司
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority to DK10782884.0T priority Critical patent/DK2439195T3/da
Priority to RU2011152113/04A priority patent/RU2497809C2/ru
Application filed by 深圳微芯生物科技有限责任公司 filed Critical 深圳微芯生物科技有限责任公司
Priority to JP2012513451A priority patent/JP5484568B2/ja
Priority to EP10782884.0A priority patent/EP2439195B1/en
Priority to SI201030695T priority patent/SI2439195T1/sl
Priority to UAA201115118A priority patent/UA103092C2/ru
Priority to KR1020147000095A priority patent/KR20140014313A/ko
Priority to MX2011012752A priority patent/MX2011012752A/es
Priority to CA2763822A priority patent/CA2763822C/en
Priority to AU2010256246A priority patent/AU2010256246B9/en
Priority to BRPI1011994A priority patent/BRPI1011994B8/pt
Priority to ES10782884.0T priority patent/ES2509615T3/es
Priority to PL10782884T priority patent/PL2439195T3/pl
Priority to KR1020117030659A priority patent/KR101421786B1/ko
Publication of WO2010139180A1 publication Critical patent/WO2010139180A1/zh
Priority to ZA2011/09030A priority patent/ZA201109030B/en
Publication of WO2010139180A8 publication Critical patent/WO2010139180A8/zh
Priority to HRP20140717AT priority patent/HRP20140717T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/90Oxygen atoms with acyclic radicals attached in position 2 or 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/233Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • C07D215/28Alcohols; Ethers thereof with halogen atoms or nitro radicals in positions 5, 6 or 7
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
PCT/CN2010/000272 2009-06-04 2010-03-05 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用 WO2010139180A1 (zh)

Priority Applications (16)

Application Number Priority Date Filing Date Title
PL10782884T PL2439195T3 (pl) 2009-06-04 2010-03-05 Pochodne naftalenokarboksyamidu jako inhibitory kinazy białkowej i deacetylazy histonowej, sposoby ich wytwarzania oraz ich zastosowania
MX2011012752A MX2011012752A (es) 2009-06-04 2010-03-05 Derivados de naftalenocarboxamida como inhibidores de proteina quinasa y de histona desacetilasa, procedimientos de preparacion y usos de los mismos.
JP2012513451A JP5484568B2 (ja) 2009-06-04 2010-03-05 プロテインキナーゼおよびヒストンデアセチラーゼの阻害剤としてのナフタレンカルボキサミド誘導体、その製造方法および用途
EP10782884.0A EP2439195B1 (en) 2009-06-04 2010-03-05 Naphthalene carboxamide derivatives as inhibitors of protein kinase and histone deacetylase, preparation methods and uses thereof
SI201030695T SI2439195T1 (sl) 2009-06-04 2010-03-05 Derivati naftalen karboksamida kot inhibitorji protein kinaze in histon deacetilaze, pripravljalni postopki in njihova uporaba
UAA201115118A UA103092C2 (ru) 2009-06-04 2010-03-05 Производные нафталинкарбоксамида как ингибиторы протеинкиназы и гистондеацетилазы, способ их получения и применения
KR1020147000095A KR20140014313A (ko) 2009-06-04 2010-03-05 단백질 키나제 및 히스톤 디아세틸라제의 억제제로서 나프탈렌 카르복스아미드 유도체, 그 제조 방법 및 용도
DK10782884.0T DK2439195T3 (da) 2009-06-04 2010-03-05 Naftalenkarboxamidderivater som proteinkinasehæmmere og histondeacetlylase, fremstillingsmetoder samt anvendelser deraf
CA2763822A CA2763822C (en) 2009-06-04 2010-03-05 Naphthalene carboxamide derivatives as inhibitors of protein kinase and histone deacetylase, preparation methods and uses thereof
BRPI1011994A BRPI1011994B8 (pt) 2009-06-04 2010-03-05 derivados de naftaleno carboxamida como inibidores de proteína quinase e histona desacetilase, métodos de preparação e usos
AU2010256246A AU2010256246B9 (en) 2009-06-04 2010-03-05 Naphthalene carboxamide derivatives as inhibitors of protein kinase and histone deacetylase, preparation methods and uses thereof
ES10782884.0T ES2509615T3 (es) 2009-06-04 2010-03-05 Derivados de naftaleno carboxamida como inhibidores de proteína cinasa e histona desacetilasa, procedimientos de preparación y usos de los mismos
RU2011152113/04A RU2497809C2 (ru) 2009-06-04 2010-03-05 Производные нафталинкарбоксамида в качестве ингибиторов протеинкиназы и гистондеацетилазы, способы их получения и применение
KR1020117030659A KR101421786B1 (ko) 2009-06-04 2010-03-05 단백질 키나제 및 히스톤 디아세틸라제의 억제제로서 나프탈렌 카르복스아미드 유도체, 그 제조 방법 및 용도
ZA2011/09030A ZA201109030B (en) 2009-06-04 2011-12-08 Naphthalene carboxamide derivatives as inhibitors of protein kinase and histone deacetylase,preparation methods and uses thereof
HRP20140717AT HRP20140717T1 (hr) 2009-06-04 2014-07-25 Derivati naftalen karboksamida kao inhibitori protein kinaze i histon deacetilaze, postupci njihove pripreme i njihove uporabe

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN200910143978 2009-06-04
CN200910143978.2 2009-06-04

Publications (2)

Publication Number Publication Date
WO2010139180A1 WO2010139180A1 (zh) 2010-12-09
WO2010139180A8 true WO2010139180A8 (zh) 2012-01-05

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PCT/CN2010/000272 WO2010139180A1 (zh) 2009-06-04 2010-03-05 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用

Country Status (18)

Country Link
EP (1) EP2439195B1 (zh)
JP (1) JP5484568B2 (zh)
KR (2) KR20140014313A (zh)
CN (1) CN101906076B (zh)
AU (1) AU2010256246B9 (zh)
BR (1) BRPI1011994B8 (zh)
CA (1) CA2763822C (zh)
DK (1) DK2439195T3 (zh)
ES (1) ES2509615T3 (zh)
HR (1) HRP20140717T1 (zh)
MX (1) MX2011012752A (zh)
PL (1) PL2439195T3 (zh)
PT (1) PT2439195E (zh)
RU (1) RU2497809C2 (zh)
SI (1) SI2439195T1 (zh)
UA (1) UA103092C2 (zh)
WO (1) WO2010139180A1 (zh)
ZA (1) ZA201109030B (zh)

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JP2011057661A (ja) * 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
CN102260210B (zh) * 2011-05-30 2012-06-27 王立强 蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物的制备方法
CN102603627B (zh) * 2011-05-31 2013-02-06 王立强 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物及其制备方法
CN102850236B (zh) * 2011-06-27 2016-05-18 国药一心制药有限公司 新型苯甲酰胺类组蛋白去乙酰化酶抑制剂及其应用
CN103420923B (zh) * 2012-05-18 2015-08-19 国药一心制药有限公司 4-氨基喹唑啉异羟肟酸类化合物及作为抗肿瘤药物应用
CN103288728A (zh) * 2013-05-17 2013-09-11 华侨大学 一种萘甲酰胺衍生物、其制备方法以及应用
CN103351336A (zh) * 2013-06-28 2013-10-16 华侨大学 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘甲酰胺衍生物及其制备方法
CN103432077A (zh) * 2013-08-21 2013-12-11 北京淦航医药科技有限公司 西达苯胺固体分散制剂
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CN103724260A (zh) * 2013-12-18 2014-04-16 华侨大学 一种苯甲酰胺衍生物及其制备方法和应用
CN104860885B (zh) * 2014-02-24 2017-11-17 中国科学院上海药物研究所 萘酰胺类化合物、其制备方法和用途
CN103896836A (zh) * 2014-03-20 2014-07-02 华侨大学 N-苯基-6-[(7-氯喹啉-4-氧基)酚醚]-2-萘甲酰胺及其制备方法
CN103923004A (zh) * 2014-04-04 2014-07-16 华侨大学 一种萘甲酰胺衍生物及其制备和应用
CN104030980A (zh) * 2014-06-10 2014-09-10 华侨大学 N-(3-甲氧基-4-氯苯基)-4-[(7-氯-4-喹啉)氨基]苯甲酰胺及其制备和应用
CN105399685B (zh) * 2014-09-16 2018-05-22 深圳微芯生物科技有限责任公司 作为选择性jak3和/或jak1激酶抑制剂的芳杂环化合物的制备方法及其应用
CN104447534A (zh) * 2014-12-04 2015-03-25 厦门大学 6-[(7-氯喹啉-4-氧基)酚醚]-2-萘甲酰胺类衍生物及其制备方法和用途
CN107868044B (zh) * 2016-09-27 2020-10-16 深圳微芯生物科技股份有限公司 一种非溶剂化晶体及其制备方法与应用
WO2018187894A1 (zh) * 2017-04-10 2018-10-18 师健友 一种用于治疗肿瘤疾病以及具有抗菌、抗病毒和抗炎作用的药物
CN109985039A (zh) * 2017-12-29 2019-07-09 深圳微芯生物科技股份有限公司 用于治疗白血病的联合用药物及其在制备用于治疗急性髓性白血病的药物中的用途
CN114681455A (zh) * 2018-08-17 2022-07-01 深圳微芯生物科技股份有限公司 组蛋白去乙酰化酶抑制剂与蛋白激酶抑制剂之组合及其制药用途
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CN113440615A (zh) * 2020-03-24 2021-09-28 深圳微芯生物科技股份有限公司 包含蛋白激酶抑制剂和化疗药物的药物组合物及其用途
CN114246864B (zh) * 2020-09-23 2024-06-21 上海润石医药科技有限公司 Csf1r激酶抑制剂及其用途
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