CN110573508B - 稠合咪唑并-哌啶jak抑制剂化合物 - Google Patents
稠合咪唑并-哌啶jak抑制剂化合物 Download PDFInfo
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- CN110573508B CN110573508B CN201880028413.7A CN201880028413A CN110573508B CN 110573508 B CN110573508 B CN 110573508B CN 201880028413 A CN201880028413 A CN 201880028413A CN 110573508 B CN110573508 B CN 110573508B
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- Prior art keywords
- compound
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- Expired - Fee Related
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61K9/0048—Eye, e.g. artificial tears
-
- 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
- A61K9/10—Dispersions; Emulsions
-
- 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
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
-
- 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
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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]
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dispersion Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762492574P | 2017-05-01 | 2017-05-01 | |
| US62/492,574 | 2017-05-01 | ||
| PCT/US2018/030148 WO2018204238A1 (en) | 2017-05-01 | 2018-04-30 | Fused imidazo-piperidine jak inhibitor compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110573508A CN110573508A (zh) | 2019-12-13 |
| CN110573508B true CN110573508B (zh) | 2022-07-05 |
Family
ID=62165730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880028413.7A Expired - Fee Related CN110573508B (zh) | 2017-05-01 | 2018-04-30 | 稠合咪唑并-哌啶jak抑制剂化合物 |
Country Status (32)
| Country | Link |
|---|---|
| US (3) | US10493077B2 (https=) |
| EP (1) | EP3601283B1 (https=) |
| JP (1) | JP7098656B2 (https=) |
| KR (1) | KR102550225B1 (https=) |
| CN (1) | CN110573508B (https=) |
| AR (1) | AR111495A1 (https=) |
| AU (1) | AU2018261593B2 (https=) |
| BR (1) | BR112019022648A2 (https=) |
| CA (1) | CA3056283A1 (https=) |
| CL (1) | CL2019003086A1 (https=) |
| CO (1) | CO2019011809A2 (https=) |
| CY (1) | CY1125051T1 (https=) |
| DK (1) | DK3601283T3 (https=) |
| EA (1) | EA201992601A1 (https=) |
| ES (1) | ES2908756T3 (https=) |
| HR (1) | HRP20220330T1 (https=) |
| IL (1) | IL270231B2 (https=) |
| LT (1) | LT3601283T (https=) |
| MA (1) | MA47970B1 (https=) |
| MD (1) | MD3601283T2 (https=) |
| MX (1) | MX388751B (https=) |
| NZ (1) | NZ757570A (https=) |
| PH (1) | PH12019502264A1 (https=) |
| PL (1) | PL3601283T3 (https=) |
| PT (1) | PT3601283T (https=) |
| RS (1) | RS62995B1 (https=) |
| SG (1) | SG11201908604YA (https=) |
| SI (1) | SI3601283T1 (https=) |
| SM (1) | SMT202200079T1 (https=) |
| TW (1) | TWI760486B (https=) |
| UA (1) | UA124478C2 (https=) |
| WO (1) | WO2018204238A1 (https=) |
Families Citing this family (33)
| 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 |
| US10406148B2 (en) | 2017-05-01 | 2019-09-10 | Theravance Biopharma R&D Ip, Llc | Methods of treatment using a JAK inhibitor compound |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| WO2020051139A1 (en) | 2018-09-04 | 2020-03-12 | Theravance Biopharma R&D Ip, Llc | 5 to 7 membered heterocyclic amides as jak inhibitors |
| CA3108848A1 (en) | 2018-09-04 | 2020-03-12 | Theravance Biopharma R&D Ip, Llc | Process for preparing jak inhibitors and intermediates thereof |
| PT3837258T (pt) | 2018-09-04 | 2024-06-20 | Theravance Biopharma R&D Ip Llc | Amidas de dimetil amino azetidina como inibidores de jak |
| MX2021004582A (es) | 2018-10-29 | 2021-06-15 | Theravance Biopharma R&D Ip Llc | Compuesto 2-azabiciclo hexano inhibidor de jak. |
| EP3908278A4 (en) * | 2019-01-11 | 2022-09-28 | Naegis Pharmaceuticals Inc. | INHIBITORS OF LEUKOTRIEN SYNTHESIS |
| 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 |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| 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 |
| WO2021185305A1 (zh) * | 2020-03-18 | 2021-09-23 | 四川海思科制药有限公司 | 一种吲唑衍生物及其在医药上的应用 |
| CN111620868B (zh) * | 2020-05-28 | 2021-08-31 | 爱斯特（成都）生物制药股份有限公司 | 一种1H-吡唑并[3,4-b]吡啶-3-甲醛的制备方法 |
| 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 |
| CN114181055A (zh) * | 2021-12-21 | 2022-03-15 | 苏州楚凯药业有限公司 | 1-苄氧基-4-溴-5-乙基-2-氟苯的制备方法 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103717599A (zh) * | 2011-07-27 | 2014-04-09 | 辉瑞有限公司 | 吲唑 |
Family Cites Families (19)
| 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 |
| 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 |
| 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 |
| 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 |
| BR112019018648A2 (pt) | 2017-03-09 | 2020-06-16 | Theravance Biopharma R&D Ip, Llc | Inibidores de jak contendo uma amida heterocíclica com 4 membros |
| AR111495A1 (es) | 2017-05-01 | 2019-07-17 | Theravance Biopharma R&D Ip Llc | Compuestos de imidazo-piperidina fusionada como inhibidores de jak |
| 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 |
-
2018
- 2018-04-27 AR ARP180101103A patent/AR111495A1/es unknown
- 2018-04-30 SM SM20220079T patent/SMT202200079T1/it unknown
- 2018-04-30 SG SG11201908604Y patent/SG11201908604YA/en unknown
- 2018-04-30 JP JP2019559297A patent/JP7098656B2/ja not_active Expired - Fee Related
- 2018-04-30 HR HRP20220330TT patent/HRP20220330T1/hr unknown
- 2018-04-30 BR BR112019022648A patent/BR112019022648A2/pt not_active IP Right Cessation
- 2018-04-30 KR KR1020197035134A patent/KR102550225B1/ko active Active
- 2018-04-30 NZ NZ757570A patent/NZ757570A/en not_active IP Right Cessation
- 2018-04-30 CA CA3056283A patent/CA3056283A1/en active Pending
- 2018-04-30 DK DK18724754.9T patent/DK3601283T3/da active
- 2018-04-30 EP EP18724754.9A patent/EP3601283B1/en active Active
- 2018-04-30 MA MA47970A patent/MA47970B1/fr unknown
- 2018-04-30 PT PT187247549T patent/PT3601283T/pt unknown
- 2018-04-30 LT LTEPPCT/US2018/030148T patent/LT3601283T/lt unknown
- 2018-04-30 MX MX2019012942A patent/MX388751B/es unknown
- 2018-04-30 WO PCT/US2018/030148 patent/WO2018204238A1/en not_active Ceased
- 2018-04-30 MD MDE20200142T patent/MD3601283T2/ro not_active IP Right Cessation
- 2018-04-30 TW TW107114647A patent/TWI760486B/zh not_active IP Right Cessation
- 2018-04-30 CN CN201880028413.7A patent/CN110573508B/zh not_active Expired - Fee Related
- 2018-04-30 RS RS20220238A patent/RS62995B1/sr unknown
- 2018-04-30 AU AU2018261593A patent/AU2018261593B2/en not_active Ceased
- 2018-04-30 UA UAA201911546A patent/UA124478C2/uk unknown
- 2018-04-30 PL PL18724754T patent/PL3601283T3/pl unknown
- 2018-04-30 ES ES18724754T patent/ES2908756T3/es active Active
- 2018-04-30 EA EA201992601A patent/EA201992601A1/ru unknown
- 2018-04-30 SI SI201830589T patent/SI3601283T1/sl unknown
- 2018-04-30 US US15/966,467 patent/US10493077B2/en active Active
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2019
- 2019-09-30 PH PH12019502264A patent/PH12019502264A1/en unknown
- 2019-10-18 US US16/656,940 patent/US11160810B2/en not_active Expired - Fee Related
- 2019-10-24 CO CONC2019/0011809A patent/CO2019011809A2/es unknown
- 2019-10-28 CL CL2019003086A patent/CL2019003086A1/es unknown
- 2019-10-28 IL IL270231A patent/IL270231B2/en unknown
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2021
- 2021-09-28 US US17/449,131 patent/US20220008428A1/en not_active Abandoned
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2022
- 2022-03-09 CY CY20221100192T patent/CY1125051T1/el unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103717599A (zh) * | 2011-07-27 | 2014-04-09 | 辉瑞有限公司 | 吲唑 |
Non-Patent Citations (1)
| Title |
|---|
| Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin;Peter Jones等;《J. Med. Chem》;20161216;第60卷(第2期);767-789 * |
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