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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Oncology (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)

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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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CA2952025A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
MX2016016538A (es) 2014-06-13 2017-05-01 Gilead Sciences Inc Derivados de quinazolinona como inhibidores de fosfatidilinositol 3-cinasa.
MX2016016516A (es) 2014-06-13 2017-05-01 Gilead Sciences Inc Inhibidores de fosfatidilinositol 3-cinasa.
US11021467B2 (en) 2014-06-13 2021-06-01 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
EA201692557A1 (ru) 2014-07-04 2017-05-31 Люпин Лимитед Хинолизиноновые производные в качестве ингибиторов pi3k
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
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
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
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
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
WO2018237007A1 (en) * 2017-06-22 2018-12-27 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE AND HISTONE DEACETYLASE FOR THE TREATMENT OF CANCER
BR112020001949A2 (pt) * 2017-07-31 2020-07-28 The Trustees Of Columbia University In The City Of New York composto, composição farmacêutica, e, métodos para tratar um linfoma não hodgkin e para tratar um linfoma ou uma leucemia
EP3740468B1 (en) 2018-01-20 2025-12-31 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
TW202130643A (zh) * 2019-10-29 2021-08-16 美商百健Ma公司 螺環o-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃糖苷酶抑制劑
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
WO2022226052A1 (en) * 2021-04-20 2022-10-27 The Regents Of The University Of Michigan Pi3k inhibitors, nanoformulations, and uses thereof
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
DE60144277D1 (de) 2000-04-25 2011-05-05 Icos Corp Hemmer der menschlichen phosphatidyl-inositol-3-kinase delta
BRPI0906473A8 (pt) * 2008-01-04 2016-02-10 Intellikine Inc Certas entidades químicas, composições e métodos
US8193182B2 (en) * 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
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
UY35675A (es) * 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
WO2015081127A2 (en) 2013-11-26 2015-06-04 Gilead Sciences, Inc. Therapies for treating myeloproliferative disorders
WO2015168079A1 (en) * 2014-04-29 2015-11-05 Infinity Pharmaceuticals, Inc. Pyrimidine or pyridine derivatives useful as pi3k inhibitors
CA2952025A1 (en) * 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
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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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CN106459008A (zh) 2017-02-22
HK1231474A1 (zh) 2017-12-22
EP3160960B1 (en) 2021-10-13
JP2018090644A (ja) 2018-06-14
CA2953820A1 (en) 2015-12-30
EA201692487A1 (ru) 2017-06-30
IL249404A0 (en) 2017-02-28
AU2015280138A1 (en) 2016-12-22
MA40045A (fr) 2021-06-02
US9765060B2 (en) 2017-09-19
US20160024054A1 (en) 2016-01-28
BR112016029846A2 (pt) 2017-08-22
EP3160960A1 (en) 2017-05-03
JP2017519021A (ja) 2017-07-13
AU2015280138B2 (en) 2018-06-14
ES2900812T3 (es) 2022-03-18
AR100975A1 (es) 2016-11-16
WO2015200352A1 (en) 2015-12-30
SG11201610341PA (en) 2017-01-27
NZ727185A (en) 2018-04-27
KR20170015521A (ko) 2017-02-08
MX2016017110A (es) 2017-05-01
JP6391718B2 (ja) 2018-09-19
US20180065953A1 (en) 2018-03-08

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