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 mismosInfo
- 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
- kinase inhibitors
- jak kinase
- sulphone based
- sulphone
- Prior art date
Links
- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical compound C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 2
- 108010024121 Janus Kinases Proteins 0.000 abstract 2
- 229940122245 Janus kinase inhibitor Drugs 0.000 abstract 1
- 239000002671 adjuvant Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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)
- 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.
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 (18)
| Country | Link |
|---|---|
| US (2) | US11453671B2 (es) |
| EP (1) | EP3986901A1 (es) |
| JP (1) | JP7657740B2 (es) |
| KR (1) | KR20220024405A (es) |
| CN (1) | CN114008051B (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) |
| PH (1) | PH12021552998A1 (es) |
| TW (1) | TW202115068A (es) |
| WO (1) | WO2020257145A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20200399274A1 (en) | 2019-06-18 | 2020-12-24 | Genentech, Inc. | Tetrazole-substituted pyrazolopyrimidine inhibitors of jak kinases and uses thereof |
| KR102767443B1 (ko) * | 2022-04-14 | 2025-02-12 | 한국화학연구원 | 퀴녹살린 카르복스아마이드 유도체 및 이를 유효성분으로 포함하는 교모세포종의 예방 또는 치료용 약학적 조성물 |
| EP4522598A1 (en) | 2022-05-11 | 2025-03-19 | PI Industries Ltd. | Bicyclic compounds and their use as pest control agents |
Family Cites Families (28)
| 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 |
| AU6311996A (en) | 1995-07-06 | 1997-02-05 | 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 |
| 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 |
| EP2108019A2 (en) * | 2007-01-30 | 2009-10-14 | Biogen Idec MA, Inc. | 1-h-pyrazolo[3,4b]pyrimidine derivatives and their use as modulators of mitotic kinases |
| EP2288260A4 (en) | 2008-06-20 | 2013-10-23 | Genentech Inc | TRIAZOLOPYRIDINE-JAK HEMMER COMPOUNDS AND METHOD |
| CN102271515B (zh) | 2008-10-31 | 2014-07-02 | 健泰科生物技术公司 | 吡唑并嘧啶jak抑制剂化合物和方法 |
| 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 |
| HRP20192020T1 (hr) | 2012-11-09 | 2020-02-07 | Mmv Medicines For Malaria Venture | Derivati heteroarila i njihova upotreba |
| PE20211782A1 (es) | 2014-05-23 | 2021-09-08 | Hoffmann La Roche | Compuestos de 5-cloro-2-difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos |
| 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 |
| EP3562809B1 (en) | 2016-12-29 | 2021-06-09 | F. Hoffmann-La Roche AG | Pyrazolopyrimidine compounds and methods of use thereof |
| CN110494434B (zh) | 2017-03-14 | 2022-05-24 | 豪夫迈·罗氏有限公司 | 吡唑并氯苯基化合物、其组合物及其使用方法 |
| CN110678467B (zh) * | 2017-05-22 | 2023-06-13 | 豪夫迈·罗氏有限公司 | 治疗化合物和组合物及其使用方法 |
| 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 |
| TWI724753B (zh) | 2019-01-25 | 2021-04-11 | 大陸商北京賽特明強醫藥科技有限公司 | 醯胺基橋連雜環類化合物、及其組合物與應用 |
| WO2020257143A1 (en) | 2019-06-18 | 2020-12-24 | Genentech, Inc. | Pyrazolopyrimidine aryl ether inhibitors of jak kinases and uses thereof |
| US20200399274A1 (en) | 2019-06-18 | 2020-12-24 | Genentech, Inc. | Tetrazole-substituted pyrazolopyrimidine inhibitors of jak kinases and uses thereof |
-
2020
- 2020-06-16 CA CA3140024A patent/CA3140024A1/en active Pending
- 2020-06-16 WO PCT/US2020/037853 patent/WO2020257145A1/en not_active Ceased
- 2020-06-16 TW TW109120272A patent/TW202115068A/zh unknown
- 2020-06-16 BR BR112021025618A patent/BR112021025618A2/pt not_active Application Discontinuation
- 2020-06-16 AU AU2020297415A patent/AU2020297415A1/en not_active Abandoned
- 2020-06-16 US US16/902,499 patent/US11453671B2/en active Active
- 2020-06-16 PE PE2021002182A patent/PE20220577A1/es unknown
- 2020-06-16 JP JP2021574283A patent/JP7657740B2/ja active Active
- 2020-06-16 EP EP20739492.5A patent/EP3986901A1/en active Pending
- 2020-06-16 MA MA056518A patent/MA56518A/fr unknown
- 2020-06-16 CR CR20210661A patent/CR20210661A/es unknown
- 2020-06-16 KR KR1020227000044A patent/KR20220024405A/ko not_active Ceased
- 2020-06-16 PH PH1/2021/552998A patent/PH12021552998A1/en unknown
- 2020-06-16 MX MX2021015319A patent/MX2021015319A/es unknown
- 2020-06-16 CN CN202080044750.2A patent/CN114008051B/zh active Active
-
2021
- 2021-12-13 IL IL288957A patent/IL288957A/en unknown
- 2021-12-14 CL CL2021003341A patent/CL2021003341A1/es unknown
-
2022
- 2022-01-12 CO CONC2022/0000118A patent/CO2022000118A2/es unknown
- 2022-08-24 US US17/821,851 patent/US20230016791A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| IL288957A (en) | 2022-02-01 |
| PE20220577A1 (es) | 2022-04-20 |
| JP2022537964A (ja) | 2022-08-31 |
| CN114008051B (zh) | 2024-08-13 |
| AU2020297415A1 (en) | 2022-01-06 |
| CL2021003341A1 (es) | 2022-07-22 |
| CA3140024A1 (en) | 2020-12-24 |
| EP3986901A1 (en) | 2022-04-27 |
| MA56518A (fr) | 2022-04-27 |
| US20200399275A1 (en) | 2020-12-24 |
| CO2022000118A2 (es) | 2022-01-28 |
| TW202115068A (zh) | 2021-04-16 |
| US20230016791A1 (en) | 2023-01-19 |
| WO2020257145A1 (en) | 2020-12-24 |
| JP7657740B2 (ja) | 2025-04-07 |
| BR112021025618A2 (pt) | 2022-02-01 |
| MX2021015319A (es) | 2022-04-07 |
| PH12021552998A1 (en) | 2023-08-14 |
| KR20220024405A (ko) | 2022-03-03 |
| US11453671B2 (en) | 2022-09-27 |
| CN114008051A (zh) | 2022-02-01 |
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