TWI793365B - 作為jak抑制劑之5至7員雜環醯胺 - Google Patents

作為jak抑制劑之5至7員雜環醯胺 Download PDF

Info

Publication number
TWI793365B
TWI793365B TW108131710A TW108131710A TWI793365B TW I793365 B TWI793365 B TW I793365B TW 108131710 A TW108131710 A TW 108131710A TW 108131710 A TW108131710 A TW 108131710A TW I793365 B TWI793365 B TW I793365B
Authority
TW
Taiwan
Prior art keywords
compound
pharmaceutically acceptable
lung
acceptable salt
mmol
Prior art date
Application number
TW108131710A
Other languages
English (en)
Chinese (zh)
Other versions
TW202024075A (zh
Inventor
丹尼爾 D 羅恩
卡梅朗 史密斯
柯賓 湯普森
Original Assignee
美商施萬生物製藥研發 Ip有限責任公司
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 美商施萬生物製藥研發 Ip有限責任公司 filed Critical 美商施萬生物製藥研發 Ip有限責任公司
Publication of TW202024075A publication Critical patent/TW202024075A/zh
Application granted granted Critical
Publication of TWI793365B publication Critical patent/TWI793365B/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW108131710A 2018-09-04 2019-09-03 作為jak抑制劑之5至7員雜環醯胺 TWI793365B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862726583P 2018-09-04 2018-09-04
US62/726,583 2018-09-04

Publications (2)

Publication Number Publication Date
TW202024075A TW202024075A (zh) 2020-07-01
TWI793365B true TWI793365B (zh) 2023-02-21

Family

ID=68051893

Family Applications (1)

Application Number Title Priority Date Filing Date
TW108131710A TWI793365B (zh) 2018-09-04 2019-09-03 作為jak抑制劑之5至7員雜環醯胺

Country Status (20)

Country Link
US (2) US10836763B2 (https=)
EP (1) EP3837010B1 (https=)
JP (1) JP7383696B2 (https=)
KR (1) KR20210056380A (https=)
CN (1) CN112703037B (https=)
AR (1) AR116114A1 (https=)
AU (1) AU2019335200A1 (https=)
BR (1) BR112021004063A2 (https=)
CL (1) CL2021000515A1 (https=)
CO (1) CO2021002976A2 (https=)
EA (1) EA202190686A1 (https=)
ES (1) ES2955717T3 (https=)
IL (1) IL281150B2 (https=)
MX (1) MX2021002484A (https=)
PH (1) PH12021550324A1 (https=)
SG (1) SG11202101751XA (https=)
TW (1) TWI793365B (https=)
UA (1) UA127328C2 (https=)
WO (1) WO2020051139A1 (https=)
ZA (1) ZA202100990B (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016004079A1 (en) 2014-06-30 2016-01-07 Black & Decker Inc. Battery pack for a cordless power tools
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
WO2022081872A1 (en) * 2020-10-16 2022-04-21 Gb008, Inc. Janus kinase inhibitors
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
WO2025172431A1 (en) * 2024-02-14 2025-08-21 Almirall, S.A. Stat6 inhibitors and methods of use thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017077288A1 (en) * 2015-11-03 2017-05-11 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

Family Cites Families (29)

* Cited by examiner, † Cited by third party
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
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
BRPI0909945A2 (pt) 2008-06-20 2015-07-28 Genentech Inc "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase"
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
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
EP3484876A1 (en) * 2016-07-14 2019-05-22 Pfizer Inc Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme
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
WO2020051139A1 (en) * 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc 5 to 7 membered heterocyclic amides as jak inhibitors
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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017077288A1 (en) * 2015-11-03 2017-05-11 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

Also Published As

Publication number Publication date
WO2020051139A1 (en) 2020-03-12
KR20210056380A (ko) 2021-05-18
UA127328C2 (uk) 2023-07-19
ZA202100990B (en) 2024-09-25
JP2021535174A (ja) 2021-12-16
EA202190686A1 (ru) 2021-07-23
EP3837010A1 (en) 2021-06-23
CN112703037A (zh) 2021-04-23
EP3837010B1 (en) 2023-07-05
SG11202101751XA (en) 2021-03-30
CO2021002976A2 (es) 2021-05-31
CN112703037B (zh) 2023-10-20
IL281150B2 (en) 2024-03-01
ES2955717T3 (es) 2023-12-05
MX2021002484A (es) 2021-05-12
PH12021550324A1 (en) 2021-10-04
TW202024075A (zh) 2020-07-01
BR112021004063A2 (pt) 2021-05-25
US11713315B2 (en) 2023-08-01
US10836763B2 (en) 2020-11-17
JP7383696B2 (ja) 2023-11-20
IL281150B1 (en) 2023-11-01
IL281150A (en) 2021-04-29
US20200071325A1 (en) 2020-03-05
US20210024517A1 (en) 2021-01-28
AR116114A1 (es) 2021-03-31
AU2019335200A1 (en) 2021-03-11
EP3837010C0 (en) 2023-07-05
CL2021000515A1 (es) 2021-07-23

Similar Documents

Publication Publication Date Title
TWI793365B (zh) 作為jak抑制劑之5至7員雜環醯胺
TWI791886B (zh) 作為jak抑制劑之二甲基胺基氮雜環丁烷醯胺
TWI754019B (zh) 含有4員雜環醯胺之jak抑制劑
TW202144343A (zh) Jak抑制劑化合物之結晶水合物
CA3053853C (en) Dimethyl amino azetidine amides and 5 to 7 membered heterocyclic amides as jak inhibitors
EA040464B1 (ru) Амиды диметиламиноазетидина в качестве jak ингибиторов
EA040902B1 (ru) 5-7-членные гетероциклические амиды в качестве ингибиторов jak

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees