CR20210661A - Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos - Google Patents

Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos

Info

Publication number
CR20210661A
CR20210661A CR20210661A CR20210661A CR20210661A CR 20210661 A CR20210661 A CR 20210661A CR 20210661 A CR20210661 A CR 20210661A CR 20210661 A CR20210661 A CR 20210661A CR 20210661 A CR20210661 A CR 20210661A
Authority
CR
Costa Rica
Prior art keywords
pyrazolopyrimidine
jak kinases
inhibitors
jak
sulfone inhibitors
Prior art date
Application number
CR20210661A
Other languages
English (en)
Inventor
Yun-Xing Cheng
Jessica Marie Grandner
Mark Edward Zak
Daniel G M Shore
Naomi S Rajapaksa
Marian C Bryan
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CR20210661A publication Critical patent/CR20210661A/es

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Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Transplantation (AREA)

Abstract

En el presente documento se describen compuestos de fórmula (I) en los que R1 , R2 , R3 , R4 , R5 y R6 son como se definen en el presente documento, y sales de los mismos que son útiles como inhibidores de JAK cinasas. Además, se proporcionan composiciones farmacéuticas que incluyen dicho inhibidor de JAK y un portador, adyuvante o portador farmacéuticamente aceptable, y procedimientos para tratar o disminuir la gravedad de una enfermedad o afección sensible a la inhibición de la actividad de una Janus cinasa en un paciente.
CR20210661A 2019-06-18 2020-06-16 Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos CR20210661A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019091712 2019-06-18
US202063035381P 2020-06-05 2020-06-05
PCT/US2020/037853 WO2020257145A1 (en) 2019-06-18 2020-06-16 Pyrazolopyrimidine sulfone inhibitors of jak kinases and uses thereof

Publications (1)

Publication Number Publication Date
CR20210661A true CR20210661A (es) 2022-02-11

Family

ID=71575774

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20210661A CR20210661A (es) 2019-06-18 2020-06-16 Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos

Country Status (17)

Country Link
US (2) US11453671B2 (es)
EP (1) EP3986901A1 (es)
JP (1) JP2022537964A (es)
KR (1) KR20220024405A (es)
CN (1) CN114008051A (es)
AU (1) AU2020297415A1 (es)
BR (1) BR112021025618A2 (es)
CA (1) CA3140024A1 (es)
CL (1) CL2021003341A1 (es)
CO (1) CO2022000118A2 (es)
CR (1) CR20210661A (es)
IL (1) IL288957A (es)
MA (1) MA56518A (es)
MX (1) MX2021015319A (es)
PE (1) PE20220577A1 (es)
TW (1) TW202115068A (es)
WO (1) WO2020257145A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023218484A1 (en) 2022-05-11 2023-11-16 Pi Industries Ltd. Bicyclic compounds and their use as pest control agents

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US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
JPH11508583A (ja) 1995-07-06 1999-07-27 ゼネカ・リミテッド ペプチド系のフィブロネクチン阻害薬
US6248713B1 (en) 1995-07-11 2001-06-19 Biogen, Inc. Cell adhesion inhibitors
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
WO2003053930A1 (en) 2001-12-20 2003-07-03 Bayer Healthcare Ag 1,4-dihydro-1,4-diphenylpyridine derivatives
SE0302487D0 (sv) 2003-09-18 2003-09-18 Astrazeneca Ab Novel compounds
GB0502258D0 (en) 2005-02-03 2005-03-09 Argenta Discovery Ltd Compounds and their use
WO2008094575A2 (en) * 2007-01-30 2008-08-07 Biogen Idec Ma Inc. 1-h-pyrazolo(3,4b)pyrimidine derivatives and their use as modulators of mitotic kinases
CN101616921A (zh) * 2007-01-30 2009-12-30 比奥根艾迪克Ma公司 1-H-吡唑并(3,4b)嘧啶衍生物及其作为有丝分裂激酶调节剂的用途
KR20110033223A (ko) 2008-06-20 2011-03-30 제넨테크, 인크. 트리아졸로피리딘 jak 억제제 화합물 및 방법
KR101686685B1 (ko) 2008-10-31 2016-12-14 제넨테크, 인크. 피라졸로피리미딘 jak 억제제 화합물 및 방법
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
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CR20190310A (es) 2016-12-29 2019-08-21 Hoffmann La Roche Compuestos de pirazolopirimidina y métodos de uso de los mismos
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WO2018215390A1 (en) * 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
WO2019139714A1 (en) * 2018-01-15 2019-07-18 Genentech, Inc. Pyrazolopyrimidine compounds as jak inhibitors
US20200399274A1 (en) 2019-06-18 2020-12-24 Genentech, Inc. Tetrazole-substituted pyrazolopyrimidine inhibitors of jak kinases and uses thereof
JP2022537354A (ja) 2019-06-18 2022-08-25 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト Jakキナーゼのピラゾロピリミジンアリールエーテル阻害剤及びその使用

Also Published As

Publication number Publication date
KR20220024405A (ko) 2022-03-03
MX2021015319A (es) 2022-04-07
US20200399275A1 (en) 2020-12-24
CN114008051A (zh) 2022-02-01
US11453671B2 (en) 2022-09-27
TW202115068A (zh) 2021-04-16
US20230016791A1 (en) 2023-01-19
JP2022537964A (ja) 2022-08-31
IL288957A (en) 2022-02-01
WO2020257145A1 (en) 2020-12-24
CA3140024A1 (en) 2020-12-24
PE20220577A1 (es) 2022-04-20
EP3986901A1 (en) 2022-04-27
MA56518A (fr) 2022-04-27
BR112021025618A2 (pt) 2022-02-01
CL2021003341A1 (es) 2022-07-22
AU2020297415A1 (en) 2022-01-06
CO2022000118A2 (es) 2022-01-28

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