CN104520296B - 作为ttx-s阻断剂的吡咯并吡啶酮衍生物 - Google Patents

作为ttx-s阻断剂的吡咯并吡啶酮衍生物 Download PDF

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CN104520296B
CN104520296B CN201380022248.1A CN201380022248A CN104520296B CN 104520296 B CN104520296 B CN 104520296B CN 201380022248 A CN201380022248 A CN 201380022248A CN 104520296 B CN104520296 B CN 104520296B
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pyridin
dihydro
oxygen
ethyl
methyl
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CN104520296A (zh
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川村清
森田干雄
山岸龙也
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Raqualia Pharma Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/535—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
    • A61K31/5355—Non-condensed oxazines 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
    • A61K31/535—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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
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    • A61P25/00—Drugs for disorders of the nervous system
    • 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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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
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    • A61P5/00—Drugs for disorders of the endocrine system
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics

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  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201380022248.1A 2012-04-25 2013-04-25 作为ttx-s阻断剂的吡咯并吡啶酮衍生物 Active CN104520296B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261638085P 2012-04-25 2012-04-25
US61/638,085 2012-04-25
JP2012260231 2012-11-28
JP2012-260231 2012-11-28
PCT/JP2013/002825 WO2013161312A1 (en) 2012-04-25 2013-04-25 Pyrrolopyridinone derivatives as ttx-s blockers

Publications (2)

Publication Number Publication Date
CN104520296A CN104520296A (zh) 2015-04-15
CN104520296B true CN104520296B (zh) 2016-11-16

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US (1) US9187475B2 (enExample)
EP (1) EP2841435B1 (enExample)
JP (1) JP6175672B2 (enExample)
KR (1) KR102090944B1 (enExample)
CN (1) CN104520296B (enExample)
BR (1) BR112014026283B1 (enExample)
CA (1) CA2871229C (enExample)
ES (1) ES2645984T3 (enExample)
IN (1) IN2014MN02056A (enExample)
MX (1) MX360323B (enExample)
RU (1) RU2646754C2 (enExample)
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WO (1) WO2013161312A1 (enExample)

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US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
CA3051054A1 (en) * 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
MA49014A (fr) * 2017-03-21 2020-02-05 Arbutus Biopharma Corp Dihydroindène-4-carboxamides substitués, leurs analogues et procédés d'utilisation correspondant
CN119285538A (zh) 2017-05-04 2025-01-10 发现号收购集团 作为例如用于保护植物的害虫防治剂的2-{[2-(苯氧基甲基)吡啶-5-基]氧基}乙胺衍生物及相关化合物
SG11202009681YA (en) 2018-04-03 2020-10-29 Blueprint Medicines Corp Ret inhibitor for use in treating cancer having a ret alteration
BR112021008995A2 (pt) 2018-12-26 2021-08-10 Raqualia Pharma Inc. derivados heterocíclicos como bloqueadores de nav1.7 e nav1.8
US12240855B2 (en) 2019-03-06 2025-03-04 Daiichi Sankyo Company, Limited Pyrrolopyrazole derivative
WO2021243192A1 (en) 2020-05-29 2021-12-02 Blueprint Medicines Corporation Solid forms of pralsetinib
CR20220666A (es) 2020-05-29 2023-05-05 Blueprint Medicines Corp Composiciones farmacéuticas de pralsetinib
CN117777011A (zh) * 2022-09-22 2024-03-29 顺毅宜昌化工有限公司 一种烷氧基取代的吡啶类化合物的制备方法
AU2024253757A1 (en) * 2023-04-07 2025-10-16 Biogen Ma Inc. 1h-pyrrolo[2,3-b]pyridin-4-yl]-2-oxopyrrolidine-3-carbonitrile derivatives as tyrosine kinase 2 (tyk2) inhibitors for the treatment of inflammatory diseases

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HK1203940A1 (en) 2015-11-06
MX2014012915A (es) 2014-11-25
US20150094306A1 (en) 2015-04-02
EP2841435A1 (en) 2015-03-04
RU2014147243A (ru) 2016-06-10
WO2013161312A1 (en) 2013-10-31
BR112014026283B1 (pt) 2022-08-02
ES2645984T3 (es) 2017-12-11
KR102090944B1 (ko) 2020-03-19
MX360323B (es) 2018-10-29
IN2014MN02056A (enExample) 2015-08-21
JP2015514679A (ja) 2015-05-21
CA2871229A1 (en) 2013-10-31
US9187475B2 (en) 2015-11-17
EP2841435B1 (en) 2017-09-06
TWI577677B (zh) 2017-04-11
KR20150006001A (ko) 2015-01-15
EP2841435A4 (en) 2015-11-11
CA2871229C (en) 2020-10-27
TW201350480A (zh) 2013-12-16
RU2646754C2 (ru) 2018-03-07
HK1207381A1 (en) 2016-01-29
CN104520296A (zh) 2015-04-15
BR112014026283A2 (pt) 2017-06-27

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