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

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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
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alkyl
compound
ethyl
hydrogen
imidazo
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TW105135436A
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Chinese (zh)
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TW201726673A (zh
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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
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美商施萬生物製藥研發Ｉｐ有限責任公司
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pulmonology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (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)

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US201562250113P 2015-11-03 2015-11-03
US62/250,113 2015-11-03

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

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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)
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Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3371185B1 (en) 2015-11-03 2020-09-30 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
US10100049B2 (en) 2015-11-03 2018-10-16 Theravance Biopharma R&D Ip, Llc JAK kinase inhibitor compounds for treatment of respiratory disease
CN110461839B (zh) 2017-03-09 2022-08-23 施万生物制药研发Ip有限责任公司 含有4元杂环酰胺的jak抑制剂
JP7096268B2 (ja) * 2017-05-01 2022-07-05 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阻害剤化合物の結晶形態
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
WO2019104225A1 (en) 2017-11-22 2019-05-31 Dauntless 2, 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
EA202190686A1 (ru) 2018-09-04 2021-07-23 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи 5-7-членные гетероциклические амиды в качестве ингибиторов jak
MX2021002273A (es) * 2018-09-04 2021-05-27 Theravance Biopharma R&D Ip Llc Proceso para preparar inhibidores de las jak y productos intermedios de estos.
PL3837258T3 (pl) * 2018-09-04 2024-09-16 Theravance Biopharma R&D Ip, Llc Amidy dimetyloaminoazetydyny jako inhibitory jak
AU2019373059A1 (en) 2018-10-29 2021-05-06 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
HRP20240994T1 (hr) 2019-02-25 2024-10-25 Henan Medinno Pharmaceutical Technology Co., Ltd. Spoj inhibitora jak i njegova uporaba
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
KR20210137087A (ko) 2019-03-05 2021-11-17 인사이트 코포레이션 만성 폐 동종이식 기능장애의 치료를 위한 jak1 경로 억제제
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) 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
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
US20220306626A1 (en) * 2021-03-26 2022-09-29 Theravance Biopharma R&D Ip, Llc Crystalline form of a dihydrochloride salt of a jak inhibitor compound
CA3223194A1 (en) * 2021-06-25 2022-12-29 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
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
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
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
JP5651681B2 (ja) 2009-04-03 2015-01-14 大日本住友製薬株式会社 代謝型グルタミン酸受容体５介在障害の治療のための化合物、およびその使用方法
WO2011017178A1 (en) 2009-07-28 2011-02-10 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN102821607B (zh) 2009-12-21 2014-12-17 萨穆梅德有限公司 1H-吡唑并[3，4-b]吡啶及其治疗应用
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
WO2012121764A1 (en) 2010-11-25 2012-09-13 Ratiopharm Gmbh Novel salts and polymorphic forms of afatinib
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
MA39092B1 (fr) 2013-12-05 2018-09-28 Pfizer Pyrrolo[2,3-d]pyrimidinyle, pyrrolo[2,3-b]pyrazinyle et pyrollo[2,3-d]pyridinyle acrylamides
SG11201609139WA (en) 2014-05-14 2016-11-29 Pfizer Pyrazolopyridines and pyrazolopyrimidines
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
EP3371185B1 (en) 2015-11-03 2020-09-30 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
US10100049B2 (en) 2015-11-03 2018-10-16 Theravance Biopharma R&D Ip, Llc JAK kinase inhibitor compounds for treatment of respiratory disease
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
CN110461839B (zh) 2017-03-09 2022-08-23 施万生物制药研发Ip有限责任公司 含有4元杂环酰胺的jak抑制剂
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
JP7096268B2 (ja) 2017-05-01 2022-07-05 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阻害剤化合物の結晶形態
PL3837258T3 (pl) 2018-09-04 2024-09-16 Theravance Biopharma R&D Ip, Llc Amidy dimetyloaminoazetydyny jako inhibitory jak
EA202190686A1 (ru) 2018-09-04 2021-07-23 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи 5-7-членные гетероциклические амиды в качестве ингибиторов jak
MX2021002273A (es) 2018-09-04 2021-05-27 Theravance Biopharma R&D Ip Llc Proceso para preparar inhibidores de las jak y productos intermedios de estos.
AU2019373059A1 (en) 2018-10-29 2021-05-06 Theravance Biopharma R&D Ip, Llc 2-azabicyclo hexane compound as JAK inhibitor
US20220306626A1 (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

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

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