RU2664533C2 - Геминально-замещенные цианоэтилпиразолопиридоны в качестве ингибиторов janus киназ - Google Patents

Геминально-замещенные цианоэтилпиразолопиридоны в качестве ингибиторов janus киназ Download PDF

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RU2664533C2
RU2664533C2 RU2015144485A RU2015144485A RU2664533C2 RU 2664533 C2 RU2664533 C2 RU 2664533C2 RU 2015144485 A RU2015144485 A RU 2015144485A RU 2015144485 A RU2015144485 A RU 2015144485A RU 2664533 C2 RU2664533 C2 RU 2664533C2
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oxo
pyridin
dihydro
amino
pyrazolo
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RU2015144485A
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Russian (ru)
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RU2015144485A3 (enExample
RU2015144485A (ru
Inventor
Мэттью Ллойд ЧАЙЛДЕРС
Питер ФУЛЛЕР
Дэвид ГЕРИН
Джейсон Дэвид КАТЦ
Цинлинь ПУ
Марк Е. СКОТТ
Кристофер Ф. Томпсон
Мишель Мартинес
Дэниелл ФОЛКОН
Луис ТОРРЕС
Йонгки ДЕНГ
Рави КУРУКУЛАСУРИЯ
Хунбо ЦЗЭН
Юньфын БАЙ
Норман КУН
Юймэй ЛЮ
Чжисян ЧЖЭН
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Мерк Шарп И Доум Корп.
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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Transplantation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
RU2015144485A 2013-03-19 2014-03-19 Геминально-замещенные цианоэтилпиразолопиридоны в качестве ингибиторов janus киназ RU2664533C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2013/072873 WO2014146249A1 (en) 2013-03-19 2013-03-19 Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors
CNPCT/CN2013/072873 2013-03-19
PCT/CN2014/000297 WO2014146491A1 (en) 2013-03-19 2014-03-19 Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors

Publications (3)

Publication Number Publication Date
RU2015144485A RU2015144485A (ru) 2017-04-25
RU2015144485A3 RU2015144485A3 (enExample) 2018-02-13
RU2664533C2 true RU2664533C2 (ru) 2018-08-20

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RU2015144485A RU2664533C2 (ru) 2013-03-19 2014-03-19 Геминально-замещенные цианоэтилпиразолопиридоны в качестве ингибиторов janus киназ

Country Status (9)

Country Link
US (1) US9957264B2 (enExample)
EP (1) EP2976339B1 (enExample)
JP (1) JP2016514709A (enExample)
CN (1) CN105189498B (enExample)
AU (1) AU2014234907B2 (enExample)
BR (1) BR112015023858A2 (enExample)
CA (1) CA2901765A1 (enExample)
RU (1) RU2664533C2 (enExample)
WO (2) WO2014146249A1 (enExample)

Families Citing this family (8)

* 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
CN110291090A (zh) * 2017-01-20 2019-09-27 利奥制药有限公司 作为新型jak激酶抑制剂的双环胺
DK3915989T3 (da) 2019-01-30 2023-09-18 Felicamed Biotechnology Co Ltd Jak inhibitor and preparation method therefor
EP3982954A4 (en) * 2019-06-14 2024-01-03 The Trustees of Columbia University in the City of New York NT5C2 INHIBITORS FOR THE TREATMENT OF CHEMOTHERAPY-RESISTANT ACUTE LYMPHOBLASTIC LEUKEMIA
CN116322696A (zh) 2020-05-04 2023-06-23 安进公司 作为髓样细胞上表达的触发受体2激动剂的杂环化合物和使用方法
TW202208355A (zh) 2020-05-04 2022-03-01 美商安進公司 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法
JP7023026B1 (ja) 2021-05-18 2022-02-21 株式会社アイビー化粧品 Ｊａｋ阻害剤

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2340611C2 (ru) * 2000-09-15 2008-12-10 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразола, используемые в качестве ингибиторов протеинкиназы
US20100105661A1 (en) * 2007-01-12 2010-04-29 Astellas Pharma Inc. Condensed pyridine compound
WO2011130146A1 (en) * 2010-04-14 2011-10-20 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
WO2012030924A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Azolopyridine and azolopyrimidine compounds and methods of use thereof
WO2012066061A1 (en) * 2010-11-19 2012-05-24 F. Hoffmann-La Roche Ag Pyrazolopyridines and pyrazolopyridines and their use as tyk2 inhibitors
WO2012135799A1 (en) * 2011-04-01 2012-10-04 University Of Utah Research Foundation Substituted 3-(1h-benzo{d}imidazol-2-yl)-1h-indazole-analogs as inhibitors of the pdk1 kinase
WO2013036611A1 (en) * 2011-09-07 2013-03-14 Incyte Corporation Processes and intermediates for making a jak inhibitor
WO2013180265A1 (ja) * 2012-06-01 2013-12-05 武田薬品工業株式会社 複素環化合物
WO2013192125A1 (en) * 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA020777B1 (ru) * 2007-11-16 2015-01-30 Инсайт Корпорейшн 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus
MY165582A (en) * 2008-03-11 2018-04-05 Incyte Holdings Corp Azetidine and cyclobutane derivatives as jak inhibitors
TW201111385A (en) * 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
CA2792508C (en) * 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
AU2012312303B2 (en) * 2011-09-22 2016-09-15 Merck Sharp & Dohme Corp. Cyanomethylpyrazole carboxamides as janus kinase inhibitors

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2340611C2 (ru) * 2000-09-15 2008-12-10 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразола, используемые в качестве ингибиторов протеинкиназы
US20100105661A1 (en) * 2007-01-12 2010-04-29 Astellas Pharma Inc. Condensed pyridine compound
WO2011130146A1 (en) * 2010-04-14 2011-10-20 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
WO2012030924A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Azolopyridine and azolopyrimidine compounds and methods of use thereof
WO2012066061A1 (en) * 2010-11-19 2012-05-24 F. Hoffmann-La Roche Ag Pyrazolopyridines and pyrazolopyridines and their use as tyk2 inhibitors
WO2012135799A1 (en) * 2011-04-01 2012-10-04 University Of Utah Research Foundation Substituted 3-(1h-benzo{d}imidazol-2-yl)-1h-indazole-analogs as inhibitors of the pdk1 kinase
WO2013036611A1 (en) * 2011-09-07 2013-03-14 Incyte Corporation Processes and intermediates for making a jak inhibitor
WO2013180265A1 (ja) * 2012-06-01 2013-12-05 武田薬品工業株式会社 複素環化合物
EP2857400A4 (en) * 2012-06-01 2015-12-09 Takeda Pharmaceutical HETEROCYCLIC CONNECTION
WO2013192125A1 (en) * 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors

Also Published As

Publication number Publication date
WO2014146249A1 (en) 2014-09-25
US20160272632A1 (en) 2016-09-22
AU2014234907B2 (en) 2017-08-17
CN105189498A (zh) 2015-12-23
WO2014146491A1 (en) 2014-09-25
CA2901765A1 (en) 2014-09-25
BR112015023858A2 (pt) 2017-07-18
RU2015144485A (ru) 2017-04-25
CN105189498B (zh) 2017-06-27
EP2976339B1 (en) 2018-06-27
EP2976339A4 (en) 2016-08-31
AU2014234907A1 (en) 2015-08-13
EP2976339A1 (en) 2016-01-27
JP2016514709A (ja) 2016-05-23
US9957264B2 (en) 2018-05-01

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