TW201625558A - 磷脂醯肌醇3-激酶抑制劑 - Google Patents

磷脂醯肌醇3-激酶抑制劑 Download PDF

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Publication number
TW201625558A
TW201625558A TW104120373A TW104120373A TW201625558A TW 201625558 A TW201625558 A TW 201625558A TW 104120373 A TW104120373 A TW 104120373A TW 104120373 A TW104120373 A TW 104120373A TW 201625558 A TW201625558 A TW 201625558A
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Taiwan
Prior art keywords
alkyl
dihydroquinazolin
amino
diamino
phenyl
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TW104120373A
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English (en)
Chinese (zh)
Inventor
傑瑞 伊瓦茲
約書亞 凱佩蘭
武成 金
廸凡 那都珊比
麗娜 珮托
史蒂芬 佩洛特
葛瑞 飛利浦
拉夫J 二世 珮維斯
柯克L 史蒂芬斯
珍妮佛A 崔柏
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基利科學股份有限公司
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Publication of TW201625558A publication Critical patent/TW201625558A/zh

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW104120373A 2014-06-24 2015-06-24 磷脂醯肌醇3-激酶抑制劑 TW201625558A (zh)

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US201462016194P 2014-06-24 2014-06-24

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US (2) US9765060B2 (enExample)
EP (1) EP3160960B1 (enExample)
JP (2) JP6391718B2 (enExample)
KR (1) KR20170015521A (enExample)
CN (1) CN106459008A (enExample)
AR (1) AR100975A1 (enExample)
AU (1) AU2015280138B2 (enExample)
BR (1) BR112016029846A2 (enExample)
CA (1) CA2953820A1 (enExample)
EA (1) EA201692487A1 (enExample)
ES (1) ES2900812T3 (enExample)
HK (1) HK1231474A1 (enExample)
IL (1) IL249404A0 (enExample)
MA (1) MA40045A (enExample)
MX (1) MX2016017110A (enExample)
NZ (1) NZ727185A (enExample)
SG (1) SG11201610341PA (enExample)
TW (1) TW201625558A (enExample)
WO (1) WO2015200352A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106632077A (zh) * 2016-10-10 2017-05-10 上海再启生物技术有限公司 一种2‑氨基‑4‑溴嘧啶的制备方法

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CA2952018A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors
CA2952037A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
JP6455995B2 (ja) 2014-06-13 2019-01-23 ギリアード サイエンシーズ, インコーポレイテッド ホスファチジルイノシトール3−キナーゼ阻害剤
CA2952025A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
PE20170640A1 (es) 2014-07-04 2017-05-26 Lupin Ltd Derivados de quinolizinona como inhibidores de pi3k
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) * 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
US10396145B2 (en) * 2017-01-12 2019-08-27 Micron Technology, Inc. Memory cells comprising ferroelectric material and including current leakage paths having different total resistances
US20200165257A1 (en) * 2017-06-22 2020-05-28 The United States Of America, As Represented By The Secretary, Department Of Health And Human Servic Inhibitors of phosphoinositide 3-kinase and histone deacetylase for treatment of cancer
US11459306B2 (en) 2017-07-31 2022-10-04 The Trustees Of Columbia University In The City Of New York Compounds, compositions, and methods for treating T-cell acute lymphoblastic leukemia
CA3083040A1 (en) 2018-01-20 2019-07-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
SG11202103118PA (en) * 2018-09-27 2021-04-29 Shanghai Yingli Pharmaceutical Co Ltd Crystal form of morpholino quinazoline compound, preparation method therefor and use thereof
US20220348558A1 (en) * 2019-09-05 2022-11-03 Wisconsin Alumni Research Foundation Inhibitors of encephalitic alphaviruses
CN110590681B (zh) * 2019-09-30 2021-06-01 中山大学 一种新型喹唑啉酮类化合物及其制备方法和应用
AR120324A1 (es) * 2019-10-29 2022-02-09 Biogen Ma Inc Inhibidores de o-glucoproteína-2-acetamido-2-deoxi-3-d-glucopiranosidasa espirocíclica
CN118373824A (zh) * 2020-04-09 2024-07-23 成都赜灵生物医药科技有限公司 取代喹唑啉-4-酮类化合物及其制备方法和用途
WO2024064024A1 (en) * 2022-09-19 2024-03-28 Onkure, Inc. ((4-oxo-3,4-dihydroquinazolin-8-yl)methyl)amine derivatives as p13k inhibitors for the treatment of cancer

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US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
MXPA02010618A (es) 2000-04-25 2004-05-05 Icos Corp Inhibidores de fosfatidilinositol 3-quinasa delta.
US8193182B2 (en) * 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
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JP5951600B2 (ja) 2010-05-21 2016-07-13 インフィニティー ファーマシューティカルズ, インコーポレイテッド キナーゼ調節のための、化合物、組成物および方法
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WO2014128612A1 (en) * 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
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US20150148345A1 (en) * 2013-11-26 2015-05-28 Gilead Sciences, Inc. Therapies for treating myeloproliferative disorders
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CA2952025A1 (en) * 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
JP6455995B2 (ja) * 2014-06-13 2019-01-23 ギリアード サイエンシーズ, インコーポレイテッド ホスファチジルイノシトール3−キナーゼ阻害剤

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106632077A (zh) * 2016-10-10 2017-05-10 上海再启生物技术有限公司 一种2‑氨基‑4‑溴嘧啶的制备方法
CN106632077B (zh) * 2016-10-10 2019-01-22 上海再启生物技术有限公司 一种2-氨基-4-溴嘧啶的制备方法

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JP2018090644A (ja) 2018-06-14
ES2900812T3 (es) 2022-03-18
EP3160960B1 (en) 2021-10-13
JP6391718B2 (ja) 2018-09-19
BR112016029846A2 (pt) 2017-08-22
NZ727185A (en) 2018-04-27
IL249404A0 (en) 2017-02-28
EA201692487A1 (ru) 2017-06-30
JP2017519021A (ja) 2017-07-13
WO2015200352A1 (en) 2015-12-30
KR20170015521A (ko) 2017-02-08
HK1231474A1 (zh) 2017-12-22
CN106459008A (zh) 2017-02-22
EP3160960A1 (en) 2017-05-03
US20160024054A1 (en) 2016-01-28
AU2015280138A1 (en) 2016-12-22
AU2015280138B2 (en) 2018-06-14
MA40045A (fr) 2021-06-02
AR100975A1 (es) 2016-11-16
US9765060B2 (en) 2017-09-19
CA2953820A1 (en) 2015-12-30
SG11201610341PA (en) 2017-01-27
MX2016017110A (es) 2017-05-01
US20180065953A1 (en) 2018-03-08

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