CA2901765A1 - Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors - Google Patents

Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors Download PDF

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Publication number
CA2901765A1
CA2901765A1 CA2901765A CA2901765A CA2901765A1 CA 2901765 A1 CA2901765 A1 CA 2901765A1 CA 2901765 A CA2901765 A CA 2901765A CA 2901765 A CA2901765 A CA 2901765A CA 2901765 A1 CA2901765 A1 CA 2901765A1
Authority
CA
Canada
Prior art keywords
oxo
pyridin
dihydro
amino
pyrazolo
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2901765A
Other languages
English (en)
French (fr)
Inventor
Matthew Lloyd CHILDERS
Peter Fuller
David Guerin
Jason David KATZ
Qinglin PU
Mark E. Scott
Christopher F. Thompson
Michelle Martinez
Danielle Falcone
Luis Torres
Yongqi Deng
Ravi Kurukulasuriya
Hongbo Zeng
Yunfeng BAI
Norman Kong
Yumei Liu
Zhixiang Zheng
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of CA2901765A1 publication Critical patent/CA2901765A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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)
CA2901765A 2013-03-19 2014-03-19 Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors Abandoned CA2901765A1 (en)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
CA2901765A1 true CA2901765A1 (en) 2014-09-25

Family

ID=51579271

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2901765A Abandoned CA2901765A1 (en) 2013-03-19 2014-03-19 Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors

Country Status (8)

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

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
WO2020155931A1 (zh) 2019-01-30 2020-08-06 格格巫（珠海）生物科技有限公司 一种jak抑制剂及其制备方法
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
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
PE20230609A1 (es) 2020-05-04 2023-04-13 Amgen Inc Compuestos heterociclicos como agonistas del receptor de activacion expresado en las celulas mieloides 2 y metodos de uso
JP7023026B1 (ja) 2021-05-18 2022-02-21 株式会社アイビー化粧品 Ｊａｋ阻害剤

Family Cites Families (14)

* 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
EP2123651A4 (en) * 2007-01-12 2011-05-04 Astellas Pharma Inc CONDENSED PYRIDINE COMPOUND
WO2009064835A1 (en) * 2007-11-16 2009-05-22 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
US8158616B2 (en) * 2008-03-11 2012-04-17 Incyte Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
TW201111385A (en) * 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
PT3354652T (pt) * 2010-03-10 2020-07-20 Incyte Holdings Corp Derivados de piperidin-4-ilazetidina como inibidores de jak1
KR20130094710A (ko) 2010-04-14 2013-08-26 어레이 바이오파마 인크. Ｊａｋ 키나아제의 억제제로서 5,7-치환된-이미다조［1,2-ｃ］피리미딘
WO2012030924A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Azolopyridine and azolopyrimidine compounds and methods of use thereof
MX2013005445A (es) * 2010-11-19 2013-07-29 Hoffmann La Roche Pirazolopiridinas y el uso de pirazolopiridinas como inhibidores de tirosina cinasa 2 (tyk2).
BR112013025142A2 (pt) * 2011-04-01 2019-09-24 Univ Utah Res Found análogos de 3-(1h-benzo{d}imidazol-2-il)-1h-indazol substituído como inibidores da cinase pdk1
UA111854C2 (uk) * 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013041042A1 (en) * 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Pyrazole carboxamides as janus kinase inhibitors
WO2013180265A1 (ja) 2012-06-01 2013-12-05 武田薬品工業株式会社 複素環化合物
EP2863914B1 (en) * 2012-06-20 2018-10-03 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
US9957264B2 (en) 2018-05-01
RU2015144485A (ru) 2017-04-25
EP2976339A4 (en) 2016-08-31
EP2976339A1 (en) 2016-01-27
EP2976339B1 (en) 2018-06-27
AU2014234907B2 (en) 2017-08-17
RU2664533C2 (ru) 2018-08-20
JP2016514709A (ja) 2016-05-23
WO2014146491A1 (en) 2014-09-25
AU2014234907A1 (en) 2015-08-13
BR112015023858A2 (pt) 2017-07-18

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Date Code Title Description
FZDE Discontinued

Effective date: 20200831