CN103260703A - 作为单酰甘油脂肪酶抑制剂的哌啶-4-基-氮杂环丁烷二酰胺 - Google Patents

作为单酰甘油脂肪酶抑制剂的哌啶-4-基-氮杂环丁烷二酰胺 Download PDF

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Publication number
CN103260703A
CN103260703A CN201180061809XA CN201180061809A CN103260703A CN 103260703 A CN103260703 A CN 103260703A CN 201180061809X A CN201180061809X A CN 201180061809XA CN 201180061809 A CN201180061809 A CN 201180061809A CN 103260703 A CN103260703 A CN 103260703A
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base
chemical compound
phenyl
trifluoromethyl
thiazol
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Chinese (zh)
Inventor
P.J.康诺利
H.卞
X.李
L.刘
M.J.马切拉
M.E.麦克唐奈
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C07ORGANIC CHEMISTRY
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    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
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  • Plural Heterocyclic Compounds (AREA)
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CN201180061809XA 2010-10-22 2011-10-20 作为单酰甘油脂肪酶抑制剂的哌啶-4-基-氮杂环丁烷二酰胺 Pending CN103260703A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40587610P 2010-10-22 2010-10-22
US61/405876 2010-10-22
PCT/US2011/057085 WO2012054716A1 (en) 2010-10-22 2011-10-20 Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors

Publications (1)

Publication Number Publication Date
CN103260703A true CN103260703A (zh) 2013-08-21

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Country Status (12)

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EP (1) EP2629851A1 (es)
JP (1) JP2013540159A (es)
KR (1) KR20130142137A (es)
CN (1) CN103260703A (es)
AR (1) AR083542A1 (es)
AU (1) AU2011316970A1 (es)
BR (1) BR112013009858A2 (es)
CA (1) CA2815350A1 (es)
IL (1) IL225769A0 (es)
RU (1) RU2013123275A (es)
TW (1) TW201305136A (es)
WO (1) WO2012054716A1 (es)

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CN109715613A (zh) * 2016-03-31 2019-05-03 武田药品工业株式会社 杂环化合物
CN109879797A (zh) * 2019-01-10 2019-06-14 安徽昊帆生物有限公司 N-苄基-四氢吡啶类化合物及其制备方法
CN111386269A (zh) * 2017-11-28 2020-07-07 豪夫迈·罗氏有限公司 新型杂环化合物

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CA2904393A1 (en) * 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
JP6454349B2 (ja) 2013-12-26 2019-01-16 武田薬品工業株式会社 モノアシルグリセロールリパーゼ(magl)阻害剤としての4−(ピペラジン−1−イル)−ピロリジン−2−オン化合物
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
ES2826443T3 (es) 2014-09-25 2021-05-18 Araxes Pharma Llc Inhibidores de proteínas mutantes KRAS G12C
US10106556B2 (en) 2015-03-30 2018-10-23 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Rasの阻害剤をスクリーニングするための方法
WO2017087528A1 (en) 2015-11-16 2017-05-26 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10463753B2 (en) 2016-02-19 2019-11-05 Lundbeck La Jolla Research Center, Inc. Radiolabeled monoacylglycerol lipase occupancy probe
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
US10610520B2 (en) 2016-03-31 2020-04-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
EP3630747A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Quinazoline derivatives as modulators of mutant kras, hras or nras
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
AU2018338855B2 (en) 2017-09-29 2022-04-28 Takeda Pharmaceutical Company Limited Heterocyclic compound
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109715613A (zh) * 2016-03-31 2019-05-03 武田药品工业株式会社 杂环化合物
CN109715613B (zh) * 2016-03-31 2021-07-30 武田药品工业株式会社 杂环化合物
CN111386269A (zh) * 2017-11-28 2020-07-07 豪夫迈·罗氏有限公司 新型杂环化合物
CN109879797A (zh) * 2019-01-10 2019-06-14 安徽昊帆生物有限公司 N-苄基-四氢吡啶类化合物及其制备方法

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AR083542A1 (es) 2013-03-06
CA2815350A1 (en) 2012-04-26
AU2011316970A1 (en) 2013-05-09
WO2012054716A1 (en) 2012-04-26
KR20130142137A (ko) 2013-12-27
RU2013123275A (ru) 2014-11-27
IL225769A0 (en) 2013-06-27
TW201305136A (zh) 2013-02-01
BR112013009858A2 (pt) 2016-07-26
JP2013540159A (ja) 2013-10-31
EP2629851A1 (en) 2013-08-28

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Application publication date: 20130821