CN103946222B - 作为mtor抑制剂的吗啉代取代的双环嘧啶脲或氨基甲酸衍生物 - Google Patents

作为mtor抑制剂的吗啉代取代的双环嘧啶脲或氨基甲酸衍生物 Download PDF

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CN103946222B
CN103946222B CN201280057967.2A CN201280057967A CN103946222B CN 103946222 B CN103946222 B CN 103946222B CN 201280057967 A CN201280057967 A CN 201280057967A CN 103946222 B CN103946222 B CN 103946222B
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dioxo
pyrimidin
phenyl
urea
methylmorpholino
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CN103946222A (zh
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R.林克
A.D.坎斯菲尔德
D.P.哈迪
J.T.福伊特里尔
R.阿德雷戈
K.埃拉尔德
T.拉杜瓦赫蒂
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Cellzome Ltd
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Cellzome Ltd
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    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • A61P25/28—Drugs 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
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    • 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
    • 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
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Hospice & Palliative Care (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201280057967.2A 2011-10-07 2012-10-05 作为mtor抑制剂的吗啉代取代的双环嘧啶脲或氨基甲酸衍生物 Expired - Fee Related CN103946222B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
EP11184358 2011-10-07
EP11184358.7 2011-10-07
US201261649995P 2012-05-22 2012-05-22
US61/649995 2012-05-22
US61/649,995 2012-05-22
PCT/EP2012/069676 WO2013050508A1 (en) 2011-10-07 2012-10-05 Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mtor inhibitors

Publications (2)

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CN103946222A CN103946222A (zh) 2014-07-23
CN103946222B true CN103946222B (zh) 2016-12-28

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Country Link
US (1) US9242993B2 (https=)
EP (1) EP2763985B1 (https=)
JP (1) JP5995977B2 (https=)
KR (1) KR20140084130A (https=)
CN (1) CN103946222B (https=)
AU (1) AU2012320465B2 (https=)
BR (1) BR112014008241A2 (https=)
CA (1) CA2850852A1 (https=)
ES (1) ES2592219T3 (https=)
MX (1) MX341577B (https=)
RU (1) RU2609208C2 (https=)
WO (1) WO2013050508A1 (https=)

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US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
CN106117242B (zh) * 2016-06-27 2018-08-03 山东大学 四氢噻喃并嘧啶类衍生物及其制备方法与应用
FR3075795A1 (fr) * 2017-12-21 2019-06-28 Galderma Research & Development Nouveaux composes inhibiteurs de mtor
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020103897A1 (zh) * 2018-11-22 2020-05-28 上海迪诺医药科技有限公司 杂环稠合嘧啶衍生物、其药物组合物及应用
TW202140474A (zh) * 2020-01-17 2021-11-01 大陸商江蘇恆瑞醫藥股份有限公司 稠合雜芳基類衍生物、其製備方法及其在醫藥上的應用
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EP2763985B1 (en) 2016-06-22
JP2014528436A (ja) 2014-10-27
MX2014004161A (es) 2014-11-26
MX341577B (es) 2016-08-25
CA2850852A1 (en) 2013-04-11
WO2013050508A1 (en) 2013-04-11
JP5995977B2 (ja) 2016-09-21
AU2012320465B2 (en) 2016-03-03
EP2763985A1 (en) 2014-08-13
US9242993B2 (en) 2016-01-26
CN103946222A (zh) 2014-07-23
RU2014109748A (ru) 2015-11-20
AU2012320465A1 (en) 2014-05-08
ES2592219T3 (es) 2016-11-28
BR112014008241A2 (pt) 2017-04-18
US20140288066A1 (en) 2014-09-25
RU2609208C2 (ru) 2017-01-31
KR20140084130A (ko) 2014-07-04

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