CN108349972B - 用于治疗呼吸疾病的jak激酶抑制剂化合物 - Google Patents

用于治疗呼吸疾病的jak激酶抑制剂化合物 Download PDF

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Publication number
CN108349972B
CN108349972B CN201680063886.1A CN201680063886A CN108349972B CN 108349972 B CN108349972 B CN 108349972B CN 201680063886 A CN201680063886 A CN 201680063886A CN 108349972 B CN108349972 B CN 108349972B
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alkyl
compound
ethyl
formula
hydrogen
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Chinese (zh)
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CN108349972A (zh
Inventor
保罗·R·法特里
约翰·R·雅各布森
安妮-玛丽·博索莱伊
加里·E·L·勃兰特
梅丽莎·弗勒里
姜岚
卡梅伦·史密斯
史蒂文·D·E·沙利文
洛里·琼·范奥登
皮埃尔-让·科尔松
吉恩·蒂莫西·法斯
米罗斯拉夫·拉普塔
诺亚·本杰明
马尔塔·达布罗斯
文卡特·R·萨兰迪
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • 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)
CN201680063886.1A 2015-11-03 2016-11-02 用于治疗呼吸疾病的jak激酶抑制剂化合物 Expired - Fee Related CN108349972B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562250113P 2015-11-03 2015-11-03
US62/250,113 2015-11-03
PCT/US2016/059999 WO2017079205A1 (en) 2015-11-03 2016-11-02 Jak kinase inhibitor compounds for treatment of respiratory disease

Publications (2)

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CN108349972A CN108349972A (zh) 2018-07-31
CN108349972B true CN108349972B (zh) 2021-06-08

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

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016350816B2 (en) 2015-11-03 2020-06-25 Theravance Biopharma R&D Ip, Llc JAK kinase inhibitor compounds for treatment of respiratory disease
PT3371185T (pt) 2015-11-03 2020-12-28 Topivert Pharma Ltd Derivados de 4,5,6,7-tetrahidro-1h-imidazo[4,5-c]piridina e 1,4,5,6,7,8-hexahidroimidazo[4,5-d]azepina como inibidores de janus quinase
US10851097B2 (en) 2015-11-03 2020-12-01 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
EA037261B1 (ru) * 2017-03-09 2021-03-01 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Ингибиторы jak, содержащие 4-членный гетероциклический амид
KR20200003121A (ko) 2017-05-01 2020-01-08 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 저해제 화합물의 결정형
CA3059785A1 (en) * 2017-05-01 2018-11-08 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
US20200281857A1 (en) 2017-11-22 2020-09-10 Dauntless 1, Inc. Therapeutic compound formulations
EP3810094A1 (en) 2018-06-20 2021-04-28 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with a jak or other kinase inhibitor
SI3837258T1 (sl) 2018-09-04 2024-09-30 Theravance Biopharma R&D Ip, Llc Dimetil amino azetidin amidi, ki se uporabljajo kot JAK zaviralci
CA3108848A1 (en) * 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc Process for preparing jak inhibitors and intermediates thereof
ES2955717T3 (es) 2018-09-04 2023-12-05 Theravance Biopharma R&D Ip Llc Amidas heterocíclicas de 5 a 7 elementos como inhibidores de JAK
EP3853229A1 (en) * 2018-10-29 2021-07-28 Theravance Biopharma R&D IP, LLC 2-azabicyclo hexane compound as jak inhibitor
JP2022509152A (ja) * 2018-11-19 2022-01-20 ニューヨーク ユニバーシティ 治療薬としてのGli1の阻害剤開示の背景
JP7514025B2 (ja) * 2019-02-25 2024-07-10 ホーナン メディノ ファーマシューティカル テクノロジー カンパニー リミテッド Jak阻害剤化合物及びその使用
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
MX2021010545A (es) 2019-03-05 2021-11-17 Incyte Corp Inhibidores de la vía de cinasa janus 1 (jak1) para el tratamiento de la disfunción crónica del aloinjerto pulmonar.
JP2022526713A (ja) 2019-03-21 2022-05-26 オンクセオ がんの処置のための、キナーゼ阻害剤と組み合わせたDbait分子
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
WO2021136345A1 (zh) * 2019-12-30 2021-07-08 路良 Jak抑制剂化合物及其用途
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
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
EP4359402A1 (en) * 2021-06-25 2024-05-01 Theravance Biopharma R&D IP, LLC Imidazolo indazole compounds as jak inhibitors
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
WO2023215478A1 (en) 2022-05-05 2023-11-09 Theravance Biopharma R&D Ip, Llc Nezulcitinib for delivery by nebulized oral inhalation

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010039939A1 (en) * 2008-10-02 2010-04-08 Incyte Corporation Janus kinase inhibitors for treatment of dry eye and other eye related diseases
WO2013014567A1 (en) * 2011-07-27 2013-01-31 Pfizer Limited Indazoles
WO2014111380A1 (en) * 2013-01-17 2014-07-24 Galapagos Nv Novel compound useful for the treatment of degenerative and inflammatory diseases

Family Cites Families (31)

* 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
AU2004259012C1 (en) 2003-07-23 2012-08-02 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
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
KR20110033223A (ko) 2008-06-20 2011-03-30 제넨테크, 인크. 트리아졸로피리딘 jak 억제제 화합물 및 방법
US20110184013A1 (en) 2008-10-01 2011-07-28 Shelley Allen Imidazo[1,2-a]Pyridine Compounds As Receptor Tyrosine 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
WO2010114971A1 (en) 2009-04-03 2010-10-07 Sepracor Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
CA2768543C (en) 2009-07-28 2017-06-20 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2011084486A1 (en) * 2009-12-21 2011-07-14 Epitherix, Llc 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
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
ME02883B (me) 2013-12-05 2018-04-20 Pfizer PIROLO[2,3-d]PIRIMIDINIL-, PIROLO[2,3-b]PIRAZINIL- I PIROLO[2,3-d] PIRIDINILAKRILAMIDI
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
US10851097B2 (en) 2015-11-03 2020-12-01 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
PT3371185T (pt) 2015-11-03 2020-12-28 Topivert Pharma Ltd Derivados de 4,5,6,7-tetrahidro-1h-imidazo[4,5-c]piridina e 1,4,5,6,7,8-hexahidroimidazo[4,5-d]azepina como inibidores de janus quinase
AU2016350816B2 (en) 2015-11-03 2020-06-25 Theravance Biopharma R&D Ip, Llc JAK kinase inhibitor compounds for treatment of respiratory disease
EA037261B1 (ru) 2017-03-09 2021-03-01 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Ингибиторы jak, содержащие 4-членный гетероциклический амид
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
CA3059785A1 (en) 2017-05-01 2018-11-08 Theravance Biopharma R&D Ip, Llc Methods of treatment using a jak inhibitor compound
KR20200003121A (ko) 2017-05-01 2020-01-08 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Jak 저해제 화합물의 결정형
CA3108848A1 (en) 2018-09-04 2020-03-12 Theravance Biopharma R&D Ip, Llc Process for preparing jak inhibitors and intermediates thereof
ES2955717T3 (es) 2018-09-04 2023-12-05 Theravance Biopharma R&D Ip Llc Amidas heterocíclicas de 5 a 7 elementos como inhibidores de JAK
SI3837258T1 (sl) 2018-09-04 2024-09-30 Theravance Biopharma R&D Ip, Llc Dimetil amino azetidin amidi, ki se uporabljajo kot JAK zaviralci
EP3853229A1 (en) 2018-10-29 2021-07-28 Theravance Biopharma R&D IP, LLC 2-azabicyclo hexane compound as jak inhibitor
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010039939A1 (en) * 2008-10-02 2010-04-08 Incyte Corporation Janus kinase inhibitors for treatment of dry eye and other eye related diseases
WO2013014567A1 (en) * 2011-07-27 2013-01-31 Pfizer Limited Indazoles
WO2014111380A1 (en) * 2013-01-17 2014-07-24 Galapagos Nv Novel compound useful for the treatment of degenerative and inflammatory diseases

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PH12018500828A1 (en) 2018-10-29
NZ741737A (en) 2023-11-24
US11718616B2 (en) 2023-08-08
US20170121327A1 (en) 2017-05-04
ZA201802496B (en) 2025-01-29
MX374605B (es) 2025-03-06
MX2018005446A (es) 2018-08-01
MY195427A (en) 2023-01-20
SA518391470B1 (ar) 2021-03-31
KR20180073687A (ko) 2018-07-02
CA3001542A1 (en) 2017-05-11
US20210130351A1 (en) 2021-05-06
IL258772A (en) 2018-06-28
US20200087303A1 (en) 2020-03-19
UA123633C2 (uk) 2021-05-05
CL2018001145A1 (es) 2018-07-06
TW201726673A (zh) 2017-08-01
IL258772B (en) 2021-01-31
US20220306624A1 (en) 2022-09-29
EA034914B1 (ru) 2020-04-06
EA201891091A1 (ru) 2018-12-28
WO2017079205A1 (en) 2017-05-11
EP3371186A1 (en) 2018-09-12
TWI710560B (zh) 2020-11-21
HK1252685A1 (zh) 2019-05-31
CO2018005640A2 (es) 2018-05-31
JP6800969B2 (ja) 2020-12-16
US20190106420A1 (en) 2019-04-11
US10100049B2 (en) 2018-10-16
JP2018531982A (ja) 2018-11-01
US10913740B2 (en) 2021-02-09
US20180319796A1 (en) 2018-11-08
PH12018500828B1 (en) 2023-06-30
AU2016350816A1 (en) 2018-05-17
BR112018008966A2 (pt) 2018-11-27
BR112018008966B1 (pt) 2023-05-02
US11299492B2 (en) 2022-04-12
AU2016350816B2 (en) 2020-06-25
US10183942B2 (en) 2019-01-22
CA3001542C (en) 2021-02-16
CN108349972A (zh) 2018-07-31
US10526330B2 (en) 2020-01-07

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