CN110603255B - Jak抑制剂化合物的结晶型式 - Google Patents

Jak抑制剂化合物的结晶型式 Download PDF

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Publication number
CN110603255B
CN110603255B CN201880029410.5A CN201880029410A CN110603255B CN 110603255 B CN110603255 B CN 110603255B CN 201880029410 A CN201880029410 A CN 201880029410A CN 110603255 B CN110603255 B CN 110603255B
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China
Prior art keywords
crystalline
hydrate salt
compound
succinic acid
imidazo
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Expired - Fee Related
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CN201880029410.5A
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English (en)
Chinese (zh)
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CN110603255A (zh
Inventor
M·达布罗斯
V·R·萨兰迪
J·恩泽雷姆
M·A·克莱因舍尔克
G·D·克拉泰尔
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880029410.5A 2017-05-01 2018-04-30 Jak抑制剂化合物的结晶型式 Expired - Fee Related CN110603255B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762492571P 2017-05-01 2017-05-01
US62/492,571 2017-05-01
PCT/US2018/030144 WO2018204236A1 (en) 2017-05-01 2018-04-30 Crystalline forms of a jak inhibitor compound

Publications (2)

Publication Number Publication Date
CN110603255A CN110603255A (zh) 2019-12-20
CN110603255B true CN110603255B (zh) 2023-02-10

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CN201880029410.5A Expired - Fee Related CN110603255B (zh) 2017-05-01 2018-04-30 Jak抑制剂化合物的结晶型式

Country Status (13)

Country Link
US (1) US10251874B2 (enExample)
EP (1) EP3619208B1 (enExample)
JP (1) JP7096268B2 (enExample)
KR (1) KR20200003121A (enExample)
CN (1) CN110603255B (enExample)
AU (1) AU2018261591B2 (enExample)
CA (1) CA3059790A1 (enExample)
MX (1) MX389014B (enExample)
MY (1) MY200348A (enExample)
PH (1) PH12019502425A1 (enExample)
SG (1) SG11201909376TA (enExample)
TW (1) TWI808083B (enExample)
WO (1) WO2018204236A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX374605B (es) 2015-11-03 2025-03-06 Theravance Biopharma R&D Ip Llc Compuestos inhibidores de jak quinasa para el tratamiento de enfermedad respiratoria.
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
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
JP2021535176A (ja) 2018-09-04 2021-12-16 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阻害剤およびその中間体を調製するためのプロセス
EA202190686A1 (ru) 2018-09-04 2021-07-23 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи 5-7-членные гетероциклические амиды в качестве ингибиторов jak
EP3837258B1 (en) 2018-09-04 2024-04-24 Theravance Biopharma R&D IP, LLC Dimethyl amino azetidine amides as jak inhibitors
JP2022506111A (ja) 2018-10-29 2022-01-17 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２－アザビシクロヘキサン化合物
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
WO2022204473A1 (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
CN118401508A (zh) * 2021-12-17 2024-07-26 株式会社大熊制药 (2R,3S)-2-(3-(4,5-二氯-1H-苯并[d]咪唑-1-基)丙基)哌啶-3-醇的新酸加成盐及晶形

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2013014567A1 (en) * 2011-07-27 2013-01-31 Pfizer Limited Indazoles
WO2017079205A1 (en) * 2015-11-03 2017-05-11 Theravance Biopharma R&D Ip, Llc Jak kinase inhibitor compounds for treatment of respiratory disease

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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
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
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
US8450340B2 (en) 2009-12-21 2013-05-28 Samumed, Llc 1H-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
NZ720092A (en) 2013-12-05 2019-05-31 Pfizer Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
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
EP3865481A1 (en) 2015-11-03 2021-08-18 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
PL3371185T3 (pl) 2015-11-03 2021-04-06 Topivert Pharma Limited Pochodne 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pirydyny i 1,4,5,6,7,8-heksahydroimidazo[4,5-d]azepiny jako inhibitory kinaz janusowych

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WO2013014567A1 (en) * 2011-07-27 2013-01-31 Pfizer Limited Indazoles
WO2017079205A1 (en) * 2015-11-03 2017-05-11 Theravance Biopharma R&D Ip, Llc Jak kinase inhibitor compounds for treatment of respiratory disease

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Sorting Out the Stats from the Jaks;Mark B. Abelson 等;《Review of Ophthalmology》;20130405;第84-88页 *

Also Published As

Publication number Publication date
SG11201909376TA (en) 2019-11-28
US10251874B2 (en) 2019-04-09
JP7096268B2 (ja) 2022-07-05
AU2018261591A1 (en) 2019-11-07
RU2019138700A3 (enExample) 2022-01-26
WO2018204236A1 (en) 2018-11-08
EP3619208B1 (en) 2023-06-07
EP3619208C0 (en) 2023-06-07
TW201900643A (zh) 2019-01-01
AU2018261591B2 (en) 2021-09-02
RU2019138700A (ru) 2021-06-02
PH12019502425A1 (en) 2020-06-29
JP2020518582A (ja) 2020-06-25
TWI808083B (zh) 2023-07-11
US20180311223A1 (en) 2018-11-01
MY200348A (en) 2023-12-21
CA3059790A1 (en) 2018-11-08
CN110603255A (zh) 2019-12-20
MX389014B (es) 2025-03-20
EP3619208A1 (en) 2020-03-11
KR20200003121A (ko) 2020-01-08
MX2019012945A (es) 2019-12-16

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Granted publication date: 20230210