KR20150132170A - 야누스 키나제 억제제로서의 비-시클릭 시아노에틸피라졸로 피리돈 - Google Patents

야누스 키나제 억제제로서의 비-시클릭 시아노에틸피라졸로 피리돈 Download PDF

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KR20150132170A
KR20150132170A KR1020157025520A KR20157025520A KR20150132170A KR 20150132170 A KR20150132170 A KR 20150132170A KR 1020157025520 A KR1020157025520 A KR 1020157025520A KR 20157025520 A KR20157025520 A KR 20157025520A KR 20150132170 A KR20150132170 A KR 20150132170A
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South Korea
Prior art keywords
dihydro
pyridin
amino
oxo
pyrazolo
Prior art date
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Withdrawn
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KR1020157025520A
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Korean (ko)
Inventor
크리스토퍼 딘스모어
피터 풀러
데이비드 게린
제이슨 데이비드 카츠
크리스토퍼 에프. 톰슨
다니엘 팔콘
웨이 덩
루이스 토레스
훙보 정
윈펑 바이
지안민 푸
노르만 콩
유메이 리우
지시앙 정
마크 이. 스콧
Original Assignee
머크 샤프 앤드 돔 코포레이션
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Publication of KR20150132170A publication Critical patent/KR20150132170A/ko
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
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    • AHUMAN NECESSITIES
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    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020157025520A 2013-03-19 2014-03-19 야누스 키나제 억제제로서의 비-시클릭 시아노에틸피라졸로 피리돈 Withdrawn KR20150132170A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361803241P 2013-03-19 2013-03-19
US61/803,241 2013-03-19
PCT/CN2014/000299 WO2014146493A1 (en) 2013-03-19 2014-03-19 Acyclic cyanoethylpyrazolo pyridones as janus kinase inhibitors

Publications (1)

Publication Number Publication Date
KR20150132170A true KR20150132170A (ko) 2015-11-25

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KR1020157025520A Withdrawn KR20150132170A (ko) 2013-03-19 2014-03-19 야누스 키나제 억제제로서의 비-시클릭 시아노에틸피라졸로 피리돈

Country Status (11)

Country Link
US (1) US10059705B2 (OSRAM)
EP (1) EP2976341B1 (OSRAM)
JP (1) JP6305510B2 (OSRAM)
KR (1) KR20150132170A (OSRAM)
CN (1) CN105121444B (OSRAM)
AU (1) AU2014234909B2 (OSRAM)
BR (1) BR112015024050A2 (OSRAM)
CA (1) CA2901770A1 (OSRAM)
MX (1) MX2015013419A (OSRAM)
RU (1) RU2015144385A (OSRAM)
WO (1) WO2014146493A1 (OSRAM)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014146246A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
WO2016061751A1 (en) * 2014-10-22 2016-04-28 Merck Sharp & Dohme Corp. Ethyl n-boc piperidinyl pyrazolo pyridones as janus kinase inhibitors
CN105327207A (zh) * 2015-12-07 2016-02-17 雷文金 一种治疗风湿热痹的中药组合物
CN105435170A (zh) * 2015-12-11 2016-03-30 张量才 一种食药同源的中药保健食品
TWI804498B (zh) 2017-06-23 2023-06-11 日商協和麒麟股份有限公司 α、β不飽和醯胺化合物
US11098216B2 (en) 2017-09-28 2021-08-24 Ricoh Company, Ltd. Image forming method, image forming apparatus, and method for manufacturing printed matter
EP3650447A1 (en) * 2018-11-08 2020-05-13 Universite de Nantes New selective modulators of insect nicotinic acetylcholine receptors
CN111499592B (zh) * 2020-03-14 2023-06-23 江苏省农用激素工程技术研究中心有限公司 5-氨甲基糖精的合成方法
CN116157124A (zh) * 2020-05-29 2023-05-23 大邱庆北尖端医疗产业振兴财团 磺胺衍生物和含其作为活性成分的用于预防或治疗精神疾病的药物组合物
CN112694497A (zh) * 2020-12-25 2021-04-23 蚌埠中实化学技术有限公司 一种4-异丙基磺酰基苯硼酸的制备方法
EP4540230A1 (en) * 2022-06-16 2025-04-23 Ensem Therapeutics, Inc. Anilino-pyrazole derivatives, compositions and methods thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090106604A (ko) 2007-01-12 2009-10-09 아스텔라스세이야쿠 가부시키가이샤 축합 피리딘 화합물
EP2451813B1 (en) 2009-07-08 2014-10-01 Leo Pharma A/S Heterocyclic compounds as jak receptor and protein tyrosine kinase inhibitors
BR112012005382A2 (pt) * 2009-09-10 2016-03-29 Hoffmann La Roche inibidores de jak
AU2011224484A1 (en) 2010-03-10 2012-09-27 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
CA2830882C (en) * 2011-03-22 2021-03-16 Dinesh Barawkar Substituted fused tricyclic compounds, compositions and medicinal applications thereof
WO2013017480A1 (en) 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
WO2013017479A1 (en) * 2011-07-29 2013-02-07 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
BR112014029705A2 (pt) * 2012-06-01 2017-06-27 Takeda Pharmaceuticals Co composto ou sal, medicamento, métodos para inibir quinase de janus em um mamífero, e para a profilaxia ou tratamento de doenças autoimunes, e, uso de um composto ou sal

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Publication number Publication date
EP2976341B1 (en) 2018-02-28
EP2976341A4 (en) 2016-10-12
MX2015013419A (es) 2016-07-19
RU2015144385A (ru) 2017-04-26
AU2014234909A1 (en) 2015-08-13
CA2901770A1 (en) 2014-09-25
CN105121444B (zh) 2018-02-16
WO2014146493A1 (en) 2014-09-25
JP6305510B2 (ja) 2018-04-04
US20160272634A1 (en) 2016-09-22
JP2016514711A (ja) 2016-05-23
EP2976341A1 (en) 2016-01-27
CN105121444A (zh) 2015-12-02
BR112015024050A2 (pt) 2017-07-18
US10059705B2 (en) 2018-08-28
AU2014234909B2 (en) 2017-10-05

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PA0105 International application

Patent event date: 20150916

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
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WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid