TWI710560B - 用於治療呼吸疾病之jak激酶抑制劑化合物 - Google Patents

用於治療呼吸疾病之jak激酶抑制劑化合物 Download PDF

Info

Publication number
TWI710560B
TWI710560B TW105135436A TW105135436A TWI710560B TW I710560 B TWI710560 B TW I710560B TW 105135436 A TW105135436 A TW 105135436A TW 105135436 A TW105135436 A TW 105135436A TW I710560 B TWI710560 B TW I710560B
Authority
TW
Taiwan
Prior art keywords
alkyl
compound
ethyl
hydrogen
imidazo
Prior art date
Application number
TW105135436A
Other languages
English (en)
Chinese (zh)
Other versions
TW201726673A (zh
Inventor
保羅 R 費瑟里
約翰 R 傑柯森
安－瑪莉 柏索里爾
蓋瑞 E L 布蘭德
梅莉沙 佛羅瑞
姜嵐
卡梅朗 史密斯
史蒂芬 D E 蘇利文
羅利 珍 凡歐丹
彼瑞 珍 寇森
吉尼 提摩西 法斯
麥洛史夫 瑞帕達
諾瓦 班傑明
瑪塔 代布洛斯
凡凱特 R 泰拉狄
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 TW201726673A publication Critical patent/TW201726673A/zh
Application granted granted Critical
Publication of TWI710560B publication Critical patent/TWI710560B/zh

Links

Images

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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW105135436A 2015-11-03 2016-11-02 用於治療呼吸疾病之jak激酶抑制劑化合物 TWI710560B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562250113P 2015-11-03 2015-11-03
US62/250,113 2015-11-03

Publications (2)

Publication Number Publication Date
TW201726673A TW201726673A (zh) 2017-08-01
TWI710560B true TWI710560B (zh) 2020-11-21

Family

ID=57442794

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105135436A TWI710560B (zh) 2015-11-03 2016-11-02 用於治療呼吸疾病之jak激酶抑制劑化合物

Country Status (22)

Country Link
US (6) US10100049B2 (enExample)
EP (1) EP3371186A1 (enExample)
JP (1) JP6800969B2 (enExample)
KR (1) KR20180073687A (enExample)
CN (1) CN108349972B (enExample)
AU (1) AU2016350816B2 (enExample)
BR (1) BR112018008966B1 (enExample)
CA (1) CA3001542C (enExample)
CL (1) CL2018001145A1 (enExample)
CO (1) CO2018005640A2 (enExample)
EA (1) EA034914B1 (enExample)
HK (1) HK1252685A1 (enExample)
IL (1) IL258772B (enExample)
MX (1) MX374605B (enExample)
MY (1) MY195427A (enExample)
NZ (1) NZ741737A (enExample)
PH (1) PH12018500828B1 (enExample)
SA (1) SA518391470B1 (enExample)
TW (1) TWI710560B (enExample)
UA (1) UA123633C2 (enExample)
WO (1) WO2017079205A1 (enExample)
ZA (1) ZA201802496B (enExample)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI710560B (zh) 2015-11-03 2020-11-21 美商施萬生物製藥研發Ｉｐ有限責任公司 用於治療呼吸疾病之jak激酶抑制劑化合物
EP3831830A1 (en) 2015-11-03 2021-06-09 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
DK3712152T3 (da) 2015-11-03 2021-03-22 Topivert Pharma Ltd 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridin og 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepinderivater som janus kinase-inhibitorer
TWI754019B (zh) * 2017-03-09 2022-02-01 美商施萬生物製藥研發 Ip有限責任公司 含有4員雜環醯胺之jak抑制劑
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
AU2018261588A1 (en) * 2017-05-01 2019-10-31 Theravance Biopharma R&D Ip, Llc Methods of treatment using a JAK inhibitor compound
EP3619208B1 (en) * 2017-05-01 2023-06-07 Theravance Biopharma R&D IP, LLC Crystalline forms of a jak inhibitor compound
US20200281857A1 (en) 2017-11-22 2020-09-10 Dauntless 1, Inc. Therapeutic compound formulations
US12171764B2 (en) 2018-06-20 2024-12-24 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with a JAK or other kinase inhibitor
BR112021004087A2 (pt) * 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc processo para preparar inibidores de jak e seus intermediários
DK3837258T3 (da) * 2018-09-04 2024-07-22 Theravance Biopharma R&D Ip Llc Dimethyl amino azetidine amides as jak inhibitors
BR112021004063A2 (pt) 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc amidas heterocíclicas com 5 a 7 membros como inibidores de jak
EP3853229A1 (en) 2018-10-29 2021-07-28 Theravance Biopharma R&D IP, LLC 2-azabicyclo hexane compound as jak inhibitor
WO2020106751A1 (en) * 2018-11-19 2020-05-28 New York University Inhinitors of gli1 as therapeutic agents
KR102873783B1 (ko) 2019-02-25 2025-10-21 메디노 파마슈티컬 테크놀로지 (주하이) 컴퍼니 리미티드 Jak 억제제 화합물 및 그 사용
US12698289B2 (en) 2019-02-25 2026-08-04 Henan Medinno Pharmaceutical Technology Co., Ltd. Solid forms of pharmaceutically acceptable salts of (S)-(2-ethyl-5-fluoro-4-hydroxyphenyl)-1H-indazol-3-yl)-4,6-dihydropyrrolo[3,4-d]imidazol-5(1H)-yl)(3-hydroxypyrrolidin-1-yl)methanone as JAK inhibitors
CN114075200A (zh) * 2020-08-14 2022-02-22 河南迈英诺医药科技有限公司 用于治疗重症肺炎的jak抑制剂化合物
UA130579C2 (uk) 2019-03-05 2026-03-25 Інсайт Корпорейшн Інгібітори шляхів jak1 для лікування хронічної дисфункції алотрансплантата легень
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
JP7580136B2 (ja) * 2019-12-30 2024-11-11 路良 Ｊａｋ阻害剤化合物及びその使用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR20220149585A (ko) 2020-03-02 2022-11-08 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 억제제 화합물의 결정성 수화물
TW202207934A (zh) * 2020-03-27 2022-03-01 瑞典商阿斯特捷利康公司 用於肺遞送的乾粉配製物及使用方法
WO2022178215A1 (en) * 2021-02-19 2022-08-25 Theravance Biopharma R&D Ip, Llc Amino amide tetrahydro imidazo pyridines as jak inhibitors
CA3212635A1 (en) 2021-03-26 2022-09-29 Theravance Biopharma R&D Ip, Llc Crystalline form of a dihydrochloride salt of a jak inhibitor compound
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
CN119403552A (zh) 2022-05-05 2025-02-07 施万生物制药研发Ip有限责任公司 用于通过雾化口腔吸入递送的奈珠西替尼

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013014567A1 (en) * 2011-07-27 2013-01-31 Pfizer Limited Indazoles

Family Cites Families (33)

* 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
US7872014B2 (en) 2003-07-23 2011-01-18 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
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
DK2089369T3 (da) 2006-10-19 2011-05-09 Rigel Pharmaceuticals Inc 2,4-pyrimidindiaminderivater som hæmmere af JAK-kinaser til behandling af autoimmune sygdomme
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
AU2009259853A1 (en) 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine JAK inhibitor compounds and methods
WO2010039825A2 (en) 2008-10-01 2010-04-08 Array Biopharma Inc. IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
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
CA2756989A1 (en) 2009-04-03 2010-10-07 Douglas Burdi Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
MX337849B (es) 2009-07-28 2016-03-09 Rigel Pharmaceuticals Inc Composiciones y metodos para inhibicion de la via jak.
SMT201700581T1 (it) * 2009-12-21 2018-01-11 Samumed Llc 1h-pirazolo[3,4-b]piridine e loro usi terapeutici
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
JP5808818B2 (ja) 2010-11-25 2015-11-10 ラツィオファーム・ゲーエムベーハー アファチニブの新規塩及び多形形態
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
TW201513861A (zh) * 2013-01-17 2015-04-16 Galapagos Nv 用於治療退化性及發炎疾病之新穎化合物
LT3077395T (lt) 2013-12-05 2018-02-12 Pfizer Inc. Pirolo[2,3-d]pirimidinilo, pirolo[2,3-b]pirazinilo ir pirolo[2,3-d]piridinilo akrilamidai
PE20161475A1 (es) 2014-05-14 2017-01-08 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
DK3712152T3 (da) 2015-11-03 2021-03-22 Topivert Pharma Ltd 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridin og 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepinderivater som janus kinase-inhibitorer
EP3831830A1 (en) 2015-11-03 2021-06-09 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
TWI710560B (zh) 2015-11-03 2020-11-21 美商施萬生物製藥研發Ｉｐ有限責任公司 用於治療呼吸疾病之jak激酶抑制劑化合物
TWI754019B (zh) 2017-03-09 2022-02-01 美商施萬生物製藥研發 Ip有限責任公司 含有4員雜環醯胺之jak抑制劑
EP3619208B1 (en) 2017-05-01 2023-06-07 Theravance Biopharma R&D IP, LLC Crystalline forms of a jak inhibitor compound
AU2018261588A1 (en) 2017-05-01 2019-10-31 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
DK3837258T3 (da) 2018-09-04 2024-07-22 Theravance Biopharma R&D Ip Llc Dimethyl amino azetidine amides as jak inhibitors
BR112021004087A2 (pt) 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc processo para preparar inibidores de jak e seus intermediários
BR112021004063A2 (pt) 2018-09-04 2021-05-25 Theravance Biopharma R&D Ip, Llc amidas heterocíclicas com 5 a 7 membros como inibidores de jak
EP3853229A1 (en) 2018-10-29 2021-07-28 Theravance Biopharma R&D IP, LLC 2-azabicyclo hexane compound as jak inhibitor
CA3212635A1 (en) 2021-03-26 2022-09-29 Theravance Biopharma R&D Ip, Llc Crystalline form of a dihydrochloride salt of a jak inhibitor compound

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013014567A1 (en) * 2011-07-27 2013-01-31 Pfizer Limited Indazoles

Also Published As

Publication number Publication date
CO2018005640A2 (es) 2018-05-31
JP6800969B2 (ja) 2020-12-16
US20190106420A1 (en) 2019-04-11
SA518391470B1 (ar) 2021-03-31
IL258772B (en) 2021-01-31
US10526330B2 (en) 2020-01-07
BR112018008966B1 (pt) 2023-05-02
US20170121327A1 (en) 2017-05-04
AU2016350816A1 (en) 2018-05-17
US20220306624A1 (en) 2022-09-29
BR112018008966A2 (pt) 2018-11-27
US20210130351A1 (en) 2021-05-06
CN108349972A (zh) 2018-07-31
US10100049B2 (en) 2018-10-16
IL258772A (en) 2018-06-28
US10913740B2 (en) 2021-02-09
NZ741737A (en) 2023-11-24
CA3001542C (en) 2021-02-16
US11718616B2 (en) 2023-08-08
CN108349972B (zh) 2021-06-08
JP2018531982A (ja) 2018-11-01
CL2018001145A1 (es) 2018-07-06
TW201726673A (zh) 2017-08-01
MX374605B (es) 2025-03-06
MY195427A (en) 2023-01-20
KR20180073687A (ko) 2018-07-02
US11299492B2 (en) 2022-04-12
WO2017079205A1 (en) 2017-05-11
US20180319796A1 (en) 2018-11-08
MX2018005446A (es) 2018-08-01
HK1252685A1 (zh) 2019-05-31
UA123633C2 (uk) 2021-05-05
US20200087303A1 (en) 2020-03-19
ZA201802496B (en) 2025-01-29
PH12018500828B1 (en) 2023-06-30
EA201891091A1 (ru) 2018-12-28
EA034914B1 (ru) 2020-04-06
CA3001542A1 (en) 2017-05-11
AU2016350816B2 (en) 2020-06-25
US10183942B2 (en) 2019-01-22
PH12018500828A1 (en) 2018-10-29
EP3371186A1 (en) 2018-09-12

Similar Documents

Publication Publication Date Title
US11718616B2 (en) JAK kinase inhibitor compounds for treatment of respiratory disease
US10370338B2 (en) Benzazepine dicarboxamide compounds with tertiary amide function
AU2019204244B2 (en) Cyclopropylamines as lsd1 inhibitors
US10323037B2 (en) Aminopyridazinone compounds as protein kinase inhibitors
TWI746178B (zh) 製備作為jak激酶抑制劑之萘啶化合物之方法
US10562891B2 (en) Quinazolinones as PARP14 inhibitors
JP7821812B2 (ja) ヤヌスキナーゼ阻害剤としてのヘテロ環誘導体
EP3768272B1 (en) Jak inhibitors
US8623877B2 (en) Substituted N-heteroaryl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof
CN117098765A (zh) 作为詹纳斯激酶抑制剂的杂环衍生物
HK40096740A (en) Heteroaryl carboxamide compound
HK40002463A (en) Benzazepine dicarboxamide compounds with tertiary amide function
HK40002463B (en) Benzazepine dicarboxamide compounds with tertiary amide function

Legal Events

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