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CN112074519A8 - 作为rip1激酶抑制剂用于治疗e.g.肠易激综合征（ibs）的n-[4-氧代-2,3-二氢-1,5-苯并氧氮杂䓬-3-基]-5,6-二氢-4h-吡咯并[1,2-b]吡唑-2-甲酰胺衍生物和有关化合物 - Google Patents

作为rip1激酶抑制剂用于治疗e.g.肠易激综合征（ibs）的n-[4-氧代-2,3-二氢-1,5-苯并氧氮杂䓬-3-基]-5,6-二氢-4h-吡咯并[1,2-b]吡唑-2-甲酰胺衍生物和有关化合物 Download PDF

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CN112074519A8
CN112074519A8 CN201980026880.0A CN201980026880A CN112074519A8 CN 112074519 A8 CN112074519 A8 CN 112074519A8 CN 201980026880 A CN201980026880 A CN 201980026880A CN 112074519 A8 CN112074519 A8 CN 112074519A8
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dihydro
pyrrolo
pyrazole
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irritable bowel
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S·帕特尔
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    • 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
    • C07D498/04—Ortho-condensed 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
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  • Psychiatry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

本发明提供具有通式(I)的化合物或其药学上可接受的盐，其中X、Y、R1、R2、R7a、R7b、X、RB1、RB2、n、p、q、A环和B环如本文所述，包括该化合物的药物组合物，以及化合物在治疗例如帕金森氏症或阿尔茨海默氏病、肠易激病症(IBD)、克罗恩病、呼吸窘迫综合征(ARDS)或慢性阻塞性肺病(COPD)的方法中用作受体相互作用蛋白-1(RIP1)激酶抑制剂的用途。示例性的化合物例如为(4S,6S)-4-氟-6-苯基-N-[(3S)-5-甲基-4-氧代-2,3-二氢-1,5-苯并氧氮杂
Figure DDA0002731674980000012
-3-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑-2-甲酰胺(实施例11)，其在RIP1测定中具有0.0044uM的Ki(uM)。
CN201980026880.0A 2018-04-20 2019-04-18 作为rip1激酶抑制剂用于治疗例如肠易激综合征(ibs)的化合物 Active CN112074519B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862660397P 2018-04-20 2018-04-20
US62/660,397 2018-04-20
PCT/US2019/028011 WO2019204537A1 (en) 2018-04-20 2019-04-18 N-[4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol e-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs)

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CN112074519A8 true CN112074519A8 (zh) 2021-05-11
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Correction item: Denomination of Invention

Correct: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza * - 3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

False: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza-3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

Number: 50-02

Page: The title page

Volume: 36

Correction item: Denomination of Invention

Correct: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza * - 3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

False: N - [4-oxo-2,3-dihydro-1,5-benzoxyaza-3-yl] - 5,6-dihydro-4h-pyrrolo [1,2-b] pyrazole-2-formamide derivatives and related compounds as rip1 kinase inhibitors for the treatment of e.g. irritable bowel syndrome (IBS)

Number: 50-02

Volume: 36

CI02 Correction of invention patent application
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