JP2022506111A - Ｊａｋ阻害剤としての２－アザビシクロヘキサン化合物 - Google Patents
Ｊａｋ阻害剤としての２－アザビシクロヘキサン化合物 Download PDFInfo
- Publication number
- JP2022506111A JP2022506111A JP2021523279A JP2021523279A JP2022506111A JP 2022506111 A JP2022506111 A JP 2022506111A JP 2021523279 A JP2021523279 A JP 2021523279A JP 2021523279 A JP2021523279 A JP 2021523279A JP 2022506111 A JP2022506111 A JP 2022506111A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- inhibitor
- pharmaceutically acceptable
- disease
- eye disease
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
- QQZWCCSFNDOGQA-RXAIFQJESA-N CCc(cc(c(F)c1)O)c1-c1cc(F)c2c(-c3nc(CN(CC4)C([C@@]56NCC[C@@H]5C6)=O)c4[nH]3)n[nH]c2c1 Chemical compound CCc(cc(c(F)c1)O)c1-c1cc(F)c2c(-c3nc(CN(CC4)C([C@@]56NCC[C@@H]5C6)=O)c4[nH]3)n[nH]c2c1 QQZWCCSFNDOGQA-RXAIFQJESA-N 0.000 description 2
- OOBPWIVRLKJRLT-UHFFFAOYSA-N CCOC(C(c(c(F)cc(Br)c1)c1F)=O)OCC Chemical compound CCOC(C(c(c(F)cc(Br)c1)c1F)=O)OCC OOBPWIVRLKJRLT-UHFFFAOYSA-N 0.000 description 1
- HMKKFNNTFKDYLF-UHFFFAOYSA-N CCc(cc(c(F)c1)OCc2ccccc2)c1-c(cc1)cc2c1c(-c1nc(CN(Cc3ccccc3)CC3)c3[nH]1)n[nH]2 Chemical compound CCc(cc(c(F)c1)OCc2ccccc2)c1-c(cc1)cc2c1c(-c1nc(CN(Cc3ccccc3)CC3)c3[nH]1)n[nH]2 HMKKFNNTFKDYLF-UHFFFAOYSA-N 0.000 description 1
- QVSBNSPQUVVCAC-UHFFFAOYSA-N CCc(cc(c(F)c1)OCc2ccccc2)c1-c1cc(F)c(C(C(OCC)OCC)=O)c(F)c1 Chemical compound CCc(cc(c(F)c1)OCc2ccccc2)c1-c1cc(F)c(C(C(OCC)OCC)=O)c(F)c1 QVSBNSPQUVVCAC-UHFFFAOYSA-N 0.000 description 1
- HSOCPYJXLCAOMS-UHFFFAOYSA-N CCc(cc(c(F)c1)OCc2ccccc2)c1-c1cc([nH]nc2C(OCC)OCC)c2c(F)c1 Chemical compound CCc(cc(c(F)c1)OCc2ccccc2)c1-c1cc([nH]nc2C(OCC)OCC)c2c(F)c1 HSOCPYJXLCAOMS-UHFFFAOYSA-N 0.000 description 1
- XKAPUCRFFCXCRY-UHFFFAOYSA-N CCc(cc(c(F)c1)OCc2ccccc2)c1-c1cc([nH]nc2C=O)c2c(F)c1 Chemical compound CCc(cc(c(F)c1)OCc2ccccc2)c1-c1cc([nH]nc2C=O)c2c(F)c1 XKAPUCRFFCXCRY-UHFFFAOYSA-N 0.000 description 1
- JXSIDYHFPVXHIZ-UHFFFAOYSA-N [BH+]c(cc1F)c(CC)cc1OCc1ccccc1 Chemical compound [BH+]c(cc1F)c(CC)cc1OCc1ccccc1 JXSIDYHFPVXHIZ-UHFFFAOYSA-N 0.000 description 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (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 |
|---|---|---|---|
| US201862751967P | 2018-10-29 | 2018-10-29 | |
| US62/751,967 | 2018-10-29 | ||
| PCT/US2019/056947 WO2020092019A1 (en) | 2018-10-29 | 2019-10-18 | 2-azabicyclo hexane compound as jak inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022506111A true JP2022506111A (ja) | 2022-01-17 |
| JP2022506111A5 JP2022506111A5 (https=) | 2022-09-01 |
| JPWO2020092019A5 JPWO2020092019A5 (https=) | 2022-09-01 |
Family
ID=68542755
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021523279A Withdrawn JP2022506111A (ja) | 2018-10-29 | 2019-10-18 | Ｊａｋ阻害剤としての２－アザビシクロヘキサン化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10968222B2 (https=) |
| EP (1) | EP3853229A1 (https=) |
| JP (1) | JP2022506111A (https=) |
| KR (1) | KR20210084512A (https=) |
| CN (1) | CN112955451A (https=) |
| AU (1) | AU2019373059A1 (https=) |
| BR (1) | BR112021007788A8 (https=) |
| CA (1) | CA3113667A1 (https=) |
| IL (1) | IL282460A (https=) |
| MX (1) | MX2021004582A (https=) |
| SG (1) | SG11202103042XA (https=) |
| WO (1) | WO2020092019A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024524214A (ja) * | 2021-06-25 | 2024-07-05 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤としてのイミダゾロインダゾール化合物 |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10029013B2 (en) | 2009-10-02 | 2018-07-24 | Foamix Pharmaceuticals Ltd. | Surfactant-free, water-free formable composition and breakable foams and their uses |
| 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 |
| MX377365B (es) | 2016-09-08 | 2025-03-10 | Journey Medical Corp | Composiciones y métodos para tratar rosácea y acné. |
| PT3837258T (pt) | 2018-09-04 | 2024-06-20 | Theravance Biopharma R&D Ip Llc | Amidas de dimetil amino azetidina como inibidores 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 |
| 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 |
| 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 |
| CN111973599A (zh) * | 2020-08-07 | 2020-11-24 | 杭州邦顺制药有限公司 | 用于眼部疾病治疗的化合物 |
| EP4196477A4 (en) * | 2020-08-17 | 2024-10-09 | Vyne Therapeutics Inc. | TOFACITINIB-CONTAINING ANHYDROUS ELASTOMER-BASED GEL FORMULATIONS |
| 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 |
| CN115969796B (zh) * | 2022-12-06 | 2024-07-09 | 苏州大学 | 一种jak抑制剂长效微球及其制备方法与应用 |
Family Cites Families (23)
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
-
2019
- 2019-10-18 MX MX2021004582A patent/MX2021004582A/es unknown
- 2019-10-18 US US16/656,946 patent/US10968222B2/en not_active Expired - Fee Related
- 2019-10-18 EP EP19802351.7A patent/EP3853229A1/en not_active Withdrawn
- 2019-10-18 KR KR1020217015109A patent/KR20210084512A/ko not_active Withdrawn
- 2019-10-18 WO PCT/US2019/056947 patent/WO2020092019A1/en not_active Ceased
- 2019-10-18 BR BR112021007788A patent/BR112021007788A8/pt not_active Application Discontinuation
- 2019-10-18 SG SG11202103042XA patent/SG11202103042XA/en unknown
- 2019-10-18 CN CN201980070126.7A patent/CN112955451A/zh active Pending
- 2019-10-18 JP JP2021523279A patent/JP2022506111A/ja not_active Withdrawn
- 2019-10-18 AU AU2019373059A patent/AU2019373059A1/en not_active Abandoned
- 2019-10-18 CA CA3113667A patent/CA3113667A1/en active Pending
-
2021
- 2021-03-01 US US17/249,373 patent/US20210206764A1/en not_active Abandoned
- 2021-04-20 IL IL282460A patent/IL282460A/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024524214A (ja) * | 2021-06-25 | 2024-07-05 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | Ｊａｋ阻害剤としてのイミダゾロインダゾール化合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3853229A1 (en) | 2021-07-28 |
| US10968222B2 (en) | 2021-04-06 |
| MX2021004582A (es) | 2021-06-15 |
| WO2020092019A1 (en) | 2020-05-07 |
| KR20210084512A (ko) | 2021-07-07 |
| BR112021007788A8 (pt) | 2022-04-26 |
| SG11202103042XA (en) | 2021-04-29 |
| CA3113667A1 (en) | 2020-05-07 |
| AU2019373059A1 (en) | 2021-05-06 |
| US20210206764A1 (en) | 2021-07-08 |
| BR112021007788A2 (pt) | 2021-07-27 |
| IL282460A (en) | 2021-06-30 |
| US20200131178A1 (en) | 2020-04-30 |
| CN112955451A (zh) | 2021-06-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20220823 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20220823 |
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| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20230727 |