CO2022000118A2 - 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
CO2022000118A2
CO2022000118A2 CONC2022/0000118A CO2022000118A CO2022000118A2 CO 2022000118 A2 CO2022000118 A2 CO 2022000118A2 CO 2022000118 A CO2022000118 A CO 2022000118A CO 2022000118 A2 CO2022000118 A2 CO 2022000118A2
Authority
CO
Colombia
Prior art keywords
pyrazolopyrimidine
sulfone
kinase inhibitors
jak kinase
jak
Prior art date
Application number
CONC2022/0000118A
Other languages
English (en)
Inventor
Yun-Xing Cheng
Mark Edward Zak
Naomi S Rajapaksa
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 CO2022000118A2 publication Critical patent/CO2022000118A2/es

Links

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

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.
CONC2022/0000118A 2019-06-18 2022-01-12 Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos CO2022000118A2 (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
CO2022000118A2 true CO2022000118A2 (es) 2022-01-28

Family

ID=71575774

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0000118A CO2022000118A2 (es) 2019-06-18 2022-01-12 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
US6034057A (en) 1995-07-06 2000-03-07 Zeneca Limited Peptide inhibitors of fibronectine
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
CA2676658A1 (en) * 2007-01-30 2008-08-07 Biogen Idec Ma Inc. 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***激酶调节剂的用途
JP5512665B2 (ja) 2008-06-20 2014-06-04 ジェネンテック, インコーポレイテッド トリアゾロピリジンjak阻害剤化合物と方法
PE20131197A1 (es) 2008-10-31 2013-11-06 Genentech Inc Compuestos de pirazolopirimidina como inhibidores de jak y composiciones farmaceuticas que los contienen
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
SG11201503517WA (en) 2012-11-09 2015-06-29 Jacobus Pharmaceutical Company Inc Heteroaryl derivatives and uses thereof
SI3145929T1 (sl) 2014-05-23 2021-10-29 Hoffmann La Roche 5-kloro-2-difluorometoksifenil pirazolopirimidinove spojine, ki so zaviralci janusove kinaze
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
CN108473501B (zh) 2016-02-18 2021-07-16 豪夫迈·罗氏有限公司 治疗化合物、其组合物及使用方法
MX2019007339A (es) 2016-12-29 2019-09-06 Hoffmann La Roche Compuestos de pirazolopirimidina y metodos de uso de los mismos.
WO2018166993A2 (en) 2017-03-14 2018-09-20 F. Hoffmann-La Roche Ag Pyrazolochlorophenyl compounds, compositions and methods of use thereof
TW201902896A (zh) 2017-05-22 2019-01-16 瑞士商赫孚孟拉羅股份公司 治療化合物及組合物及其使用方法
JP7228318B6 (ja) 2017-05-22 2023-03-10 エフ. ホフマン-ラ ロシュ アーゲー 処置用化合物及び組成物、並びにその使用方法
EP3740488A1 (en) 2018-01-15 2020-11-25 F. Hoffmann-La Roche AG Pyrazolopyrimidine compounds as jak inhibitors
WO2020257142A1 (en) 2019-06-18 2020-12-24 Genentech, Inc. Tetrazole-substituted pyrazolopyrimidine inhibitors of jak kinases and uses thereof
WO2020257143A1 (en) 2019-06-18 2020-12-24 Genentech, Inc. Pyrazolopyrimidine aryl ether inhibitors of jak kinases and uses thereof

Also Published As

Publication number Publication date
EP3986901A1 (en) 2022-04-27
PE20220577A1 (es) 2022-04-20
IL288957A (en) 2022-02-01
CN114008051A (zh) 2022-02-01
BR112021025618A2 (pt) 2022-02-01
MA56518A (fr) 2022-04-27
US20200399275A1 (en) 2020-12-24
JP2022537964A (ja) 2022-08-31
KR20220024405A (ko) 2022-03-03
MX2021015319A (es) 2022-04-07
CA3140024A1 (en) 2020-12-24
US11453671B2 (en) 2022-09-27
AU2020297415A1 (en) 2022-01-06
CL2021003341A1 (es) 2022-07-22
CR20210661A (es) 2022-02-11
WO2020257145A1 (en) 2020-12-24
TW202115068A (zh) 2021-04-16
US20230016791A1 (en) 2023-01-19

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.
ECSP12011645A (es) Compuestos y métodos inhibidores de jak de pirazolopirimidina
CU20210015A7 (es) COMPUESTOS DE PIRAZOLO [3.4-b] PIRIDINA COMO INHIBIDORES DE CINASAS TAM Y MET
AR111233A1 (es) Inhibidores de tyk2, usos y métodos para la producción de los mismos
UY36371A (es) Compuestos de indolcarboxamida inhibidores de quinasas tipo btk y tipo tec
CO2019010559A2 (es) Composiciones y compuestos terapéuticos y métodos para utilizarlos
UY27234A1 (es) Inhibidores novedosos de tirosina cinasa
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.
AR066214A1 (es) Derivados de pirazolopirimidinas como inhibidores de quinasas dependientes de ciclinas. usos y composiciones farmaceuticas
EA201792116A1 (ru) Ингибитор янус-киназы
CR20110224A (es) Pirazolopirimidina inhibidor jak compuestos y metodos
DOP2010000064A (es) 2-anilinopurin 8-onas como inhibidores de ttk/mps1 para el tratamiento de trastornos proliferativos
ECSP088630A (es) Derivados de pirimidina utilizados como inhibidores de cinasa pi-3
UY28059A1 (es) Nuevos derivados de dihidropirimido (4,5-d) pirimidona sustituida por amino. fabricacion y uso de los mismos como agentes farmaceuticos.
CO2019012571A2 (es) Análogos de benzoazepina como agentes inhibidores de la tirosina cinasa de bruton
UY27714A1 (es) 2 - heteroaril - pirimidinas inhibidoras de cdk, su preparación y su uso como medicamentos.
WO2017089390A8 (en) Janus kinases inhibitors, compositions thereof and use thereof
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
CL2021003032A1 (es) Métodos de tratamiento de la urticaria crónica espontánea utilizando un inhibidor de la tirosina quinasa de bruton
CO2022000118A2 (es) Inhibidores de jak cinasas basados en pirazolopirimidina sulfona y usos de los mismos
CO2021000782A2 (es) Agentes inhibidores de ask1
BR112021019589A2 (pt) Derivados de isocromenos como inibidores de fosfoinositídeo 3-cinases
CO2024000572A2 (es) Compuestos pirimidínicos para usar como inhibidores de map4k1
ECSP23075535A (es) Compuestos cíclicos y métodos de uso