CL2021003341A1 - 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
CL2021003341A1
CL2021003341A1 CL2021003341A CL2021003341A CL2021003341A1 CL 2021003341 A1 CL2021003341 A1 CL 2021003341A1 CL 2021003341 A CL2021003341 A CL 2021003341A CL 2021003341 A CL2021003341 A CL 2021003341A CL 2021003341 A1 CL2021003341 A1 CL 2021003341A1
Authority
CL
Chile
Prior art keywords
pyrazolopyrimidine
sulfone
kinase inhibitors
jak kinase
jak
Prior art date
Application number
CL2021003341A
Other languages
English (en)
Inventor
Mark Edward Zak
Naomi S Rajapaksa
Yun-Xing Cheng
Jessica Marie Grandner
Daniel G M Shore
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 CL2021003341A1 publication Critical patent/CL2021003341A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)

Abstract

En el presente documento se describen compuestos de fórmula, 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.
CL2021003341A 2019-06-18 2021-12-14 Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos. CL2021003341A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2019091712 2019-06-18
US202063035381P 2020-06-05 2020-06-05

Publications (1)

Publication Number Publication Date
CL2021003341A1 true CL2021003341A1 (es) 2022-07-22

Family

ID=71575774

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2021003341A CL2021003341A1 (es) 2019-06-18 2021-12-14 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

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
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
DE60214428T2 (de) 2001-12-20 2007-09-20 Bayer Healthcare Ag 1, 4-dihydro-1, 4-diphenylpyridin-derivate
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
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
JP2010532312A (ja) * 2007-01-30 2010-10-07 バイオジェン・アイデック・エムエイ・インコーポレイテッド １−ｈ−ピラゾロ（３，４ｂ）ピリミジン誘導体および有糸分裂キナーゼの調節剤としてのその使用
RU2560153C2 (ru) 2008-06-20 2015-08-20 Дженентек, Инк. Триазолпиридиновые соединения, ингибирующие jak, и способы
MX2011004494A (es) 2008-10-31 2011-05-24 Genentech Inc Compuestos de pirazolopirimidina inhibidores de jak y metodos.
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
US8575336B2 (en) 2011-07-27 2013-11-05 Pfizer Limited Indazoles
KR20150079968A (ko) 2012-11-09 2015-07-08 자코버스 파마슈티컬 컴패니, 인코포레이티드 헤테로아릴 유도체 및 그의 용도
US9346815B2 (en) 2014-05-23 2016-05-24 Genentech, Inc. 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof
TW201720828A (zh) 2015-11-23 2017-06-16 赫孚孟拉羅股份公司 治療性化合物及組合物以及其使用方法
EP3416967B1 (en) * 2016-02-18 2022-02-09 F. Hoffmann-La Roche AG Therapeutic compounds, compositions and methods of use thereof
JP6900491B2 (ja) 2016-12-29 2021-07-07 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピラゾロピリミジン化合物及びその使用方法
JP2020510061A (ja) 2017-03-14 2020-04-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピラゾロクロロフェニル化合物、組成物及びその使用方法
US20180334465A1 (en) 2017-05-22 2018-11-22 Genentech, Inc. Therapeutic compounds and compositions, and methods of use thereof
WO2018215389A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
EP3740488A1 (en) 2018-01-15 2020-11-25 F. Hoffmann-La Roche AG Pyrazolopyrimidine compounds as jak inhibitors
TW202115069A (zh) 2019-06-18 2021-04-16 瑞士商赫孚孟拉羅股份公司 Ｊａｋ激酶之經四唑取代之吡唑并嘧啶抑制劑及其用途
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
CN114008051A (zh) 2022-02-01
KR20220024405A (ko) 2022-03-03
CA3140024A1 (en) 2020-12-24
JP2022537964A (ja) 2022-08-31
CR20210661A (es) 2022-02-11
CO2022000118A2 (es) 2022-01-28
PE20220577A1 (es) 2022-04-20
AU2020297415A1 (en) 2022-01-06
US11453671B2 (en) 2022-09-27
EP3986901A1 (en) 2022-04-27
MX2021015319A (es) 2022-04-07
US20200399275A1 (en) 2020-12-24
WO2020257145A1 (en) 2020-12-24
BR112021025618A2 (pt) 2022-02-01
TW202115068A (zh) 2021-04-16
US20230016791A1 (en) 2023-01-19
MA56518A (fr) 2022-04-27
IL288957A (en) 2022-02-01

Similar Documents

Publication Publication Date Title
CL2020002146A1 (es) Derivados de n-(fenil)-2-(fenil)pirimidina-4-carboxamida y compuestos relacionados como inhibidores hpki para tratar el cáncer.
CU20210015A7 (es) COMPUESTOS DE PIRAZOLO [3.4-b] PIRIDINA COMO INHIBIDORES DE CINASAS TAM Y MET
ECSP12011645A (es) Compuestos y métodos inhibidores de jak de pirazolopirimidina
UY36371A (es) Compuestos de indolcarboxamida inhibidores de quinasas tipo btk y tipo tec
AR111233A1 (es) Inhibidores de tyk2, usos y métodos para la producción de los mismos
CO2019010559A2 (es) Composiciones y compuestos terapéuticos y métodos para utilizarlos
CL2012000589A1 (es) Compuestos derivados de pirrolo piridin carboxamidas, inhibidores de jak2; composición farmacéutica que los comprende; uso en el tratamiento de enfermedades mieloproliferativas o cáncer, tales como policitemia vera, trombocitopenia esencial, mieloma múltiple, entre otras.
NI201600089A (es) Análogos de cortistatina y síntesis y usos de los mismos
EA201792116A1 (ru) Ингибитор янус-киназы
UY27234A1 (es) Inhibidores novedosos de tirosina cinasa
AR066214A1 (es) Derivados de pirazolopirimidinas como inhibidores de quinasas dependientes de ciclinas. usos y composiciones farmaceuticas
CO2019012571A2 (es) Análogos de benzoazepina como agentes inhibidores de la tirosina cinasa de bruton
WO2017089390A8 (en) Janus kinases inhibitors, compositions thereof and use thereof
CR20110224A (es) Pirazolopirimidina inhibidor jak compuestos y metodos
UY27714A1 (es) 2 - heteroaril - pirimidinas inhibidoras de cdk, su preparación y su uso como medicamentos.
CR20170092A (es) Compuestos y composiciones como inhibidores de quinasa raf
SA519402103B1 (ar) 1,6-naphthyridine مشتقات 1، 6 نفثيرايدين CDK4/6 على شكل مثبط
CL2021000844A1 (es) Compuestos de indolinona para uso como inhibidores de map4k1
ECSP099767A (es) Derivados de n' - (fenil) -n- (morfolin-4-il-piridin-2-il) -pirimidina-2, 4-diamina como inhibidores de quinasas ephb4 para el tratamiento de afecciones proliferativas
CL2021003032A1 (es) Métodos de tratamiento de la urticaria crónica espontánea utilizando un inhibidor de la tirosina quinasa de bruton
CL2021003341A1 (es) Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos.
CO2021001925A2 (es) Piridopirimidinas como inhibidores del receptor de histamina h4
PE20191715A1 (es) Derivados de pirrolotriazina como inhibidor de cinasas
CO2021000782A2 (es) Agentes inhibidores de ask1
BR112022021735A2 (pt) Compostos úteis para inibir cinase ret