WO2012136080A8 - Benzomorpholine derivatives, preparation method and use thereof - Google Patents

Benzomorpholine derivatives, preparation method and use thereof Download PDF

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Publication number
WO2012136080A8
WO2012136080A8 PCT/CN2012/000462 CN2012000462W WO2012136080A8 WO 2012136080 A8 WO2012136080 A8 WO 2012136080A8 CN 2012000462 W CN2012000462 W CN 2012000462W WO 2012136080 A8 WO2012136080 A8 WO 2012136080A8
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
derivatives
benzomorpholine derivatives
benzomorpholine
pi3k
Prior art date
Application number
PCT/CN2012/000462
Other languages
French (fr)
Chinese (zh)
Other versions
WO2012136080A1 (en
Inventor
匡荣仁
郭建辉
Original Assignee
上海艾力斯医药科技有限公司
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
Application filed by 上海艾力斯医药科技有限公司 filed Critical 上海艾力斯医药科技有限公司
Priority to CN201280012517.1A priority Critical patent/CN103534252B/en
Publication of WO2012136080A1 publication Critical patent/WO2012136080A1/en
Publication of WO2012136080A8 publication Critical patent/WO2012136080A8/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Disclosed are benzomorpholine derivatives as represented by the following formula (I) and pharmaceutical compositions comprising the derivatives as well as methods of preparation thereof, R1, R2 and R3 are as defined in the specification. The benzomorpholine derivatives of formula (I) are an inhibitor of phosphatidylinositol 3-kinases (PI3K), and have a good inhibitory effect on PI3K and on cancer cell proliferation, thereby serving as a therapeutic agent for the treatment of tumors.
PCT/CN2012/000462 2011-04-08 2012-04-09 Benzomorpholine derivatives, preparation method and use thereof WO2012136080A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201280012517.1A CN103534252B (en) 2011-04-08 2012-04-09 Benzomorpholine derivatives and its preparation method and application

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2011100872815A CN102731525A (en) 2011-04-08 2011-04-08 Benzomorpholine derivative
CN201110087281.5 2011-04-08

Publications (2)

Publication Number Publication Date
WO2012136080A1 WO2012136080A1 (en) 2012-10-11
WO2012136080A8 true WO2012136080A8 (en) 2013-10-24

Family

ID=46968575

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2012/000462 WO2012136080A1 (en) 2011-04-08 2012-04-09 Benzomorpholine derivatives, preparation method and use thereof

Country Status (2)

Country Link
CN (2) CN102731525A (en)
WO (1) WO2012136080A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2794600T3 (en) 2011-12-22 2018-06-29 Novartis Ag 2,3-Dihydro-benzo[1,4]oxazine derivatives and related compounds as phosphoinositide-3 kinase (PI3K) inhibitors for the treatment of e.g. rheumatoid arthritis
CN106146534B (en) * 2016-06-29 2017-12-08 福州大学 A kind of three ring Benzomorpholine derivatives and preparation method thereof
CN108239075B (en) * 2016-12-26 2021-07-02 中国医学科学院药物研究所 Quinazoline compound, preparation method, application and pharmaceutical composition thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL336580A1 (en) * 1997-03-03 2000-07-03 Boehringer Ingelheim Pharma Fine-molecular compounds useful in treating inflammatory diseases
US6087350A (en) * 1997-08-29 2000-07-11 University Of Pittsburgh Of The Commonwealth System Of Higher Education Use of pretreatment chemicals to enhance efficacy of cytotoxic agents
PT1939203E (en) * 2000-04-25 2015-02-04 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta isoform
DE60144322D1 (en) * 2000-04-27 2011-05-12 Astellas Pharma Inc CONDENSED HETEROARYL DERIVATIVES
AU2003303231A1 (en) * 2002-12-20 2004-07-14 Warner-Lambert Company Llc Benzoxazines and derivatives thereof as inhibitors of pi3ks
GB0524786D0 (en) * 2005-12-05 2006-01-11 Glaxo Group Ltd Compounds
US20100311736A1 (en) * 2007-10-22 2010-12-09 Glaxosmithkline Llc Pyridosulfonamide derivatives as p13 kinase inhibitors
WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase

Also Published As

Publication number Publication date
CN103534252B (en) 2016-08-24
CN102731525A (en) 2012-10-17
WO2012136080A1 (en) 2012-10-11
CN103534252A (en) 2014-01-22

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