HRP20241002T1 - Dimetil amino azetidin amidi kao inhibitori jak - Google Patents
Dimetil amino azetidin amidi kao inhibitori jak Download PDFInfo
- Publication number
- HRP20241002T1 HRP20241002T1 HRP20241002TT HRP20241002T HRP20241002T1 HR P20241002 T1 HRP20241002 T1 HR P20241002T1 HR P20241002T T HRP20241002T T HR P20241002TT HR P20241002 T HRP20241002 T HR P20241002T HR P20241002 T1 HRP20241002 T1 HR P20241002T1
- Authority
- HR
- Croatia
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- formula
- image
- Prior art date
Links
- -1 DIMETHYL AMINO AZETIDINE AMIDES Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 23
- 210000004072 lung Anatomy 0.000 claims 5
- 208000023504 respiratory system disease Diseases 0.000 claims 5
- 206010051604 Lung transplant rejection Diseases 0.000 claims 4
- 206010035664 Pneumonia Diseases 0.000 claims 4
- 206010035742 Pneumonitis Diseases 0.000 claims 4
- 230000004064 dysfunction Effects 0.000 claims 4
- 208000023367 bronchiolitis obliterans with obstructive pulmonary disease Diseases 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000019693 Lung disease Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 206010029888 Obliterative bronchiolitis Diseases 0.000 claims 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000003848 bronchiolitis obliterans Diseases 0.000 claims 2
- 229940112141 dry powder inhaler Drugs 0.000 claims 2
- 208000013397 idiopathic acute eosinophilic pneumonia Diseases 0.000 claims 2
- 229940071648 metered dose inhaler Drugs 0.000 claims 2
- 206010006448 Bronchiolitis Diseases 0.000 claims 1
- 206010006474 Bronchopulmonary aspergillosis allergic Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 208000027004 Eosinophilic disease Diseases 0.000 claims 1
- 208000018428 Eosinophilic granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000034706 Graft dysfunction Diseases 0.000 claims 1
- 208000006968 Helminthiasis Diseases 0.000 claims 1
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 208000016300 Idiopathic chronic eosinophilic pneumonia Diseases 0.000 claims 1
- 102000037982 Immune checkpoint proteins Human genes 0.000 claims 1
- 108091008036 Immune checkpoint proteins Proteins 0.000 claims 1
- 208000004530 Primary Graft Dysfunction Diseases 0.000 claims 1
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 1
- 208000006778 allergic bronchopulmonary aspergillosis Diseases 0.000 claims 1
- 201000009267 bronchiectasis Diseases 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 201000009805 cryptogenic organizing pneumonia Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000001155 extrinsic allergic alveolitis Diseases 0.000 claims 1
- 230000002538 fungal effect Effects 0.000 claims 1
- 208000022098 hypersensitivity pneumonitis Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 230000000527 lymphocytic effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000006199 nebulizer Substances 0.000 claims 1
- 230000003448 neutrophilic effect Effects 0.000 claims 1
- 208000014837 parasitic helminthiasis infectious disease Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862726562P | 2018-09-04 | 2018-09-04 | |
| PCT/US2019/049276 WO2020051105A1 (en) | 2018-09-04 | 2019-09-03 | Dimethyl amino azetidine amides as jak inhibitors |
| EP19769674.3A EP3837258B1 (en) | 2018-09-04 | 2019-09-03 | Dimethyl amino azetidine amides as jak inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20241002T1 true HRP20241002T1 (hr) | 2024-10-25 |
Family
ID=67982186
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20241002TT HRP20241002T1 (hr) | 2018-09-04 | 2019-09-03 | Dimetil amino azetidin amidi kao inhibitori jak |
Country Status (27)
| Country | Link |
|---|---|
| US (4) | US10947229B2 (https=) |
| EP (1) | EP3837258B1 (https=) |
| JP (2) | JP7324836B2 (https=) |
| KR (1) | KR102826491B1 (https=) |
| CN (1) | CN112739697B (https=) |
| AR (1) | AR116115A1 (https=) |
| AU (1) | AU2019336167B2 (https=) |
| BR (1) | BR112021004052A2 (https=) |
| CL (1) | CL2021000514A1 (https=) |
| CO (1) | CO2021002977A2 (https=) |
| DK (1) | DK3837258T3 (https=) |
| EA (1) | EA202190681A1 (https=) |
| ES (1) | ES2982858T3 (https=) |
| FI (1) | FI3837258T3 (https=) |
| HR (1) | HRP20241002T1 (https=) |
| HU (1) | HUE068058T2 (https=) |
| IL (1) | IL281146B2 (https=) |
| LT (1) | LT3837258T (https=) |
| MA (1) | MA53229A (https=) |
| MX (1) | MX2021002521A (https=) |
| PH (1) | PH12021550368A1 (https=) |
| PL (1) | PL3837258T3 (https=) |
| PT (1) | PT3837258T (https=) |
| SG (1) | SG11202101734RA (https=) |
| SI (1) | SI3837258T1 (https=) |
| TW (1) | TWI791886B (https=) |
| WO (1) | WO2020051105A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HK1252685A1 (zh) | 2015-11-03 | 2019-05-31 | Theravance Biopharma R&D Ip, Llc | 用於治疗呼吸疾病的jak激酶抑制剂化合物 |
| BR112019018648A2 (pt) | 2017-03-09 | 2020-06-16 | Theravance Biopharma R&D Ip, Llc | Inibidores de jak contendo uma amida heterocíclica com 4 membros |
| PT3837258T (pt) | 2018-09-04 | 2024-06-20 | Theravance Biopharma R&D Ip Llc | Amidas de dimetil amino azetidina como inibidores de jak |
| CA3108848A1 (en) | 2018-09-04 | 2020-03-12 | Theravance Biopharma R&D Ip, Llc | Process for preparing jak inhibitors and intermediates thereof |
| WO2020051139A1 (en) | 2018-09-04 | 2020-03-12 | Theravance Biopharma R&D Ip, Llc | 5 to 7 membered heterocyclic amides as jak inhibitors |
| TW202144343A (zh) * | 2020-03-02 | 2021-12-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之結晶水合物 |
| WO2021226637A1 (en) * | 2020-05-08 | 2021-11-11 | Theravance Biopharma R&D Ip, Llc | Method of treating a patient infected with a coronavirus with nezulcitinib |
| US20230021647A1 (en) * | 2021-06-21 | 2023-01-26 | Theravance Biopharma R&D Ip, Llc | Method of treating a patient infected with a coronavirus and having a baseline level of crp below 150 mg/l |
| TW202317550A (zh) | 2021-06-25 | 2023-05-01 | 美商施萬生物製藥研發 Ip有限責任公司 | 作為jak抑制劑之咪唑吲唑化合物 |
| JP7644873B2 (ja) * | 2021-12-17 | 2025-03-12 | デウン ファーマシューティカル カンパニー リミテッド | （２Ｒ，３Ｓ）－２－（３－（４，５－ジクロロ－１Ｈ－ベンゾ［ｄ］イミダゾール－１－イル）プロピル）ピペリジン－３－オールの新規な酸付加塩および結晶形 |
| US20250288561A1 (en) | 2022-05-05 | 2025-09-18 | Theravance Biopharma R&D Ip, Llc | Nezulcitinib for delivery by nebulized oral inhalation |
| WO2023230236A1 (en) | 2022-05-26 | 2023-11-30 | Theravance Biopharma R&D Ip, Llc | Process for preparing jak inhibitors and intermediates thereof |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI262914B (en) | 1999-07-02 | 2006-10-01 | Agouron Pharma | Compounds and pharmaceutical compositions for inhibiting protein kinases |
| JP4836788B2 (ja) | 2003-07-23 | 2011-12-14 | エグゼリクシス， インコーポレイテッド | 未分化リンパ腫キナーゼ変調因子及びその使用法 |
| US20050090529A1 (en) | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| US7884109B2 (en) | 2005-04-05 | 2011-02-08 | Wyeth Llc | Purine and imidazopyridine derivatives for immunosuppression |
| US8648069B2 (en) | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| JP2010111624A (ja) | 2008-11-06 | 2010-05-20 | Shionogi & Co Ltd | Ｔｔｋ阻害作用を有するインダゾール誘導体 |
| EP2414340A1 (en) | 2009-04-03 | 2012-02-08 | Dainippon Sumitomo Pharma Co., Ltd. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| EP2515655B1 (en) | 2009-12-21 | 2015-08-05 | Samumed, LLC | 1h-pyrazolo[3,4-beta]pyridines and therapeutic uses thereof |
| US8575336B2 (en) | 2011-07-27 | 2013-11-05 | Pfizer Limited | Indazoles |
| MX368464B (es) | 2013-12-05 | 2019-10-02 | Pfizer | Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinil o y pirrolo[2,3-d]piridinilo. |
| CR20160525A (es) | 2014-05-14 | 2016-12-20 | Pfizer | Pirazolopiridinas y pirazolopirimidinas |
| WO2016026078A1 (en) | 2014-08-19 | 2016-02-25 | Changzhou Jiekai Pharmatech Co., Ltd. | Heterocyclic compounds as erk inhibitors |
| KR101663277B1 (ko) | 2015-03-30 | 2016-10-06 | 주식회사 녹십자 | TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물 |
| HK1252685A1 (zh) | 2015-11-03 | 2019-05-31 | Theravance Biopharma R&D Ip, Llc | 用於治疗呼吸疾病的jak激酶抑制剂化合物 |
| US10556901B2 (en) | 2015-11-03 | 2020-02-11 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as Janus kinase inhibitors |
| EP3712152B1 (en) | 2015-11-03 | 2021-01-13 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors |
| US20180258546A1 (en) * | 2017-03-09 | 2018-09-13 | Lam Research Corporation | Electroplating apparatus and methods utilizing independent control of impinging electrolyte |
| BR112019018648A2 (pt) | 2017-03-09 | 2020-06-16 | Theravance Biopharma R&D Ip, Llc | Inibidores de jak contendo uma amida heterocíclica com 4 membros |
| US10406148B2 (en) | 2017-05-01 | 2019-09-10 | Theravance Biopharma R&D Ip, Llc | Methods of treatment using a JAK inhibitor compound |
| CN110603255B (zh) | 2017-05-01 | 2023-02-10 | 施万生物制药研发Ip有限责任公司 | Jak抑制剂化合物的结晶型式 |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| AU2019306651B2 (en) | 2018-07-20 | 2025-03-20 | Porifera, Inc. | Osmosis modules having recirculation loops |
| PT3837258T (pt) | 2018-09-04 | 2024-06-20 | Theravance Biopharma R&D Ip Llc | Amidas de dimetil amino azetidina como inibidores de jak |
| CA3108848A1 (en) | 2018-09-04 | 2020-03-12 | Theravance Biopharma R&D Ip, Llc | Process for preparing jak inhibitors and intermediates thereof |
| WO2020051139A1 (en) | 2018-09-04 | 2020-03-12 | Theravance Biopharma R&D Ip, Llc | 5 to 7 membered heterocyclic amides as jak inhibitors |
| MX2021004582A (es) | 2018-10-29 | 2021-06-15 | Theravance Biopharma R&D Ip Llc | Compuesto 2-azabiciclo hexano inhibidor de jak. |
| FI3932919T3 (fi) | 2019-02-25 | 2024-08-30 | Henan Medinno Pharmaceutical Tech Co Ltd | Jak-inhibiittoriyhdiste ja sen käyttö |
| MA55201A (fr) | 2019-03-05 | 2022-01-12 | Incyte Corp | Inhibiteurs de la voie jak1 pour le traitement d'un dysfonctionnement chronique de l'allogreffe pulmonaire |
| CN112279848A (zh) | 2019-07-25 | 2021-01-29 | 四川海思科制药有限公司 | 一种泛JAKs抑制剂及其用途 |
| TW202144343A (zh) * | 2020-03-02 | 2021-12-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之結晶水合物 |
| WO2021226637A1 (en) | 2020-05-08 | 2021-11-11 | Theravance Biopharma R&D Ip, Llc | Method of treating a patient infected with a coronavirus with nezulcitinib |
| WO2022178215A1 (en) | 2021-02-19 | 2022-08-25 | Theravance Biopharma R&D Ip, Llc | Amino amide tetrahydro imidazo pyridines as jak inhibitors |
| TW202304902A (zh) | 2021-03-26 | 2023-02-01 | 美商施萬生物製藥研發 Ip有限責任公司 | Jak抑制劑化合物之二鹽酸鹽之結晶形式 |
| US20230021647A1 (en) * | 2021-06-21 | 2023-01-26 | Theravance Biopharma R&D Ip, Llc | Method of treating a patient infected with a coronavirus and having a baseline level of crp below 150 mg/l |
-
2019
- 2019-09-03 PT PT197696743T patent/PT3837258T/pt unknown
- 2019-09-03 BR BR112021004052-8A patent/BR112021004052A2/pt unknown
- 2019-09-03 US US16/559,077 patent/US10947229B2/en active Active
- 2019-09-03 SG SG11202101734RA patent/SG11202101734RA/en unknown
- 2019-09-03 PL PL19769674.3T patent/PL3837258T3/pl unknown
- 2019-09-03 DK DK19769674.3T patent/DK3837258T3/da active
- 2019-09-03 IL IL281146A patent/IL281146B2/en unknown
- 2019-09-03 HU HUE19769674A patent/HUE068058T2/hu unknown
- 2019-09-03 SI SI201930791T patent/SI3837258T1/sl unknown
- 2019-09-03 MA MA053229A patent/MA53229A/fr unknown
- 2019-09-03 WO PCT/US2019/049276 patent/WO2020051105A1/en not_active Ceased
- 2019-09-03 MX MX2021002521A patent/MX2021002521A/es unknown
- 2019-09-03 EA EA202190681A patent/EA202190681A1/ru unknown
- 2019-09-03 CN CN201980057577.7A patent/CN112739697B/zh active Active
- 2019-09-03 PH PH1/2021/550368A patent/PH12021550368A1/en unknown
- 2019-09-03 JP JP2021512257A patent/JP7324836B2/ja active Active
- 2019-09-03 FI FIEP19769674.3T patent/FI3837258T3/fi active
- 2019-09-03 AR ARP190102520A patent/AR116115A1/es not_active Application Discontinuation
- 2019-09-03 ES ES19769674T patent/ES2982858T3/es active Active
- 2019-09-03 EP EP19769674.3A patent/EP3837258B1/en active Active
- 2019-09-03 AU AU2019336167A patent/AU2019336167B2/en active Active
- 2019-09-03 KR KR1020217009936A patent/KR102826491B1/ko active Active
- 2019-09-03 TW TW108131679A patent/TWI791886B/zh active
- 2019-09-03 LT LTEPPCT/US2019/049276T patent/LT3837258T/lt unknown
- 2019-09-03 HR HRP20241002TT patent/HRP20241002T1/hr unknown
-
2021
- 2021-02-04 US US17/248,717 patent/US11634419B2/en active Active
- 2021-03-02 CL CL2021000514A patent/CL2021000514A1/es unknown
- 2021-03-04 CO CONC2021/0002977A patent/CO2021002977A2/es unknown
-
2022
- 2022-09-06 JP JP2022141182A patent/JP2022172299A/ja active Pending
-
2023
- 2023-03-09 US US18/181,138 patent/US20230322774A1/en not_active Abandoned
-
2024
- 2024-05-31 US US18/680,940 patent/US12398135B2/en active Active
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