UA124246C2 - Селективні інгібітори jak1 - Google Patents
Селективні інгібітори jak1 Download PDFInfo
- Publication number
- UA124246C2 UA124246C2 UAA201909176A UAA201909176A UA124246C2 UA 124246 C2 UA124246 C2 UA 124246C2 UA A201909176 A UAA201909176 A UA A201909176A UA A201909176 A UAA201909176 A UA A201909176A UA 124246 C2 UA124246 C2 UA 124246C2
- Authority
- UA
- Ukraine
- Prior art keywords
- fluoro
- methylsulfonyl
- indol
- phenyl
- amino
- Prior art date
Links
- 229940124639 Selective inhibitor Drugs 0.000 title description 3
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 title 1
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 207
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- -1 4-methyl-1,4-diazepan-1-yl Chemical group 0.000 claims description 139
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 99
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 84
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 70
- DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims description 63
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims description 31
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 28
- 238000011282 treatment Methods 0.000 claims description 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 23
- 208000035475 disorder Diseases 0.000 claims description 22
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 22
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- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 7
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 7
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- A61P37/00—Drugs for immunological or allergic disorders
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Immunology (AREA)
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- Diabetes (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
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- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762447057P | 2017-01-17 | 2017-01-17 | |
| PCT/EP2018/051038 WO2018134213A1 (en) | 2017-01-17 | 2018-01-16 | Jak1 selective inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA124246C2 true UA124246C2 (uk) | 2021-08-11 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA201909176A UA124246C2 (uk) | 2017-01-17 | 2018-01-16 | Селективні інгібітори jak1 |
Country Status (38)
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20191108A1 (es) * | 2017-01-17 | 2019-08-26 | Astrazeneca Ab | Inhibidores selectivos de jak1 |
| TWI810172B (zh) | 2017-01-26 | 2023-08-01 | 南韓商韓美藥品股份有限公司 | 嘧啶化合物及包括其的藥學組成物 |
| US11149029B2 (en) * | 2018-07-18 | 2021-10-19 | Astrazeneca Ab | Salts of IJAK inhibitors and methods of using the same |
| KR101954370B1 (ko) | 2018-07-25 | 2019-03-05 | 한미약품 주식회사 | 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 |
| EP3854793A4 (en) * | 2018-09-21 | 2022-06-01 | Shanghai Ennovabio Pharmaceuticals Co., Ltd. | AROMATIC HETEROCYCLIC COMPOUND WITH KINASE INHIBITORY ACTIVITY |
| BR112021016522A2 (pt) | 2019-02-22 | 2021-10-26 | Hanmi Pharm. Co., Ltd. | Composição farmacêutica para o tratamento da leucemia mieloide aguda |
| AU2020258619C1 (en) * | 2019-04-19 | 2026-01-29 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | JAK1 selective kinase inhibitor |
| EP3991733A4 (en) | 2019-06-27 | 2023-07-05 | Hanmi Pharm. Co., Ltd. | Pharmaceutical composition for treating acute myeloid leukemia, containing flt3 inhibitor and chemotherapeutic agents |
| CA3174321A1 (en) | 2020-04-09 | 2021-10-14 | Disarm Therapeutics, Inc. | Indazole derivatives as inhibitors of sarm1 |
| WO2022111499A1 (zh) | 2020-11-26 | 2022-06-02 | 深圳铂立健医药有限公司 | 一种酰胺化合物、药物组合物及其应用 |
| EP4297873A1 (en) * | 2021-02-26 | 2024-01-03 | Tyra Biosciences, Inc. | Aminopyrimidine compounds and methods of their use |
| US12240836B2 (en) | 2022-07-05 | 2025-03-04 | Dong-A St Co., Ltd. | Compounds as GCN2 inhibitors, pharmaceutical compositions and uses thereof |
| CN115260128B (zh) * | 2022-09-21 | 2022-12-09 | 苏州凯瑞医药科技有限公司 | 一种新型jak抑制剂关键中间体的制备方法 |
| WO2024150110A1 (en) * | 2023-01-11 | 2024-07-18 | Pfizer Inc. | Compositions and methods for the treatment and/or prevention of type 1 diabetes |
| CN115974845B (zh) * | 2023-01-19 | 2024-09-20 | 奥锐特药业股份有限公司 | 奥希替尼中间体的制备方法 |
| KR20250174908A (ko) * | 2023-03-16 | 2025-12-15 | 인사이트 코포레이션 | 천식의 치료를 위한 jak1 경로 저해제 |
| GB202316063D0 (en) | 2023-10-20 | 2023-12-06 | Astrazeneca Ab | Dosing regime |
| GB202403369D0 (en) | 2024-03-08 | 2024-04-24 | Astrazeneca Ab | Process and intermediates for the production of a jak1 inhibitor |
| WO2026132265A1 (en) | 2024-12-19 | 2026-06-25 | Astrazeneca Ab | Dry powder inhaler |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7799915B2 (en) | 2004-10-13 | 2010-09-21 | Wyeth Llc | Anilino-pyrimidine analogs |
| GB2431927B (en) | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| CN101421250A (zh) * | 2006-01-30 | 2009-04-29 | 埃克塞里艾克西斯公司 | 作为jak-2调节剂的4-芳基-2-氨基-嘧啶或4-芳基-2-氨基烷基-嘧啶及包含它们的药物组合物 |
| WO2008097930A1 (en) | 2007-02-05 | 2008-08-14 | Amira Pharmaceuticals, Inc. | Reverse indoles as 5-lipoxygenase-activating protein (flap) inhibitors |
| EP2207547A4 (en) | 2007-10-05 | 2010-11-17 | Amira Pharmaceuticals Inc | PROTEIN INHIBITORS THAT ACTIVATE 5-LIPOXYGENASE |
| WO2009046416A1 (en) * | 2007-10-05 | 2009-04-09 | Targegen Inc. | Anilinopyrimidines as jak kinase inhibitors |
| GB0805477D0 (en) * | 2008-03-26 | 2008-04-30 | Univ Nottingham | Pyrimidines triazines and their use as pharmaceutical agents |
| UA110324C2 (en) * | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| CA2792508C (en) | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| RU2013114352A (ru) * | 2010-09-15 | 2014-10-20 | Ф. Хоффманн-Ля Рош Аг | Азабензотиазолы, композиции и способы применения |
| EP3060234A1 (en) | 2013-10-24 | 2016-08-31 | AbbVie Inc. | Jak1 selective inhibitor and uses thereof |
| KR102774784B1 (ko) * | 2015-09-25 | 2025-02-27 | 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 | Jak를 억제하기 위한 화합물 및 방법 |
| PE20191108A1 (es) * | 2017-01-17 | 2019-08-26 | Astrazeneca Ab | Inhibidores selectivos de jak1 |
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