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)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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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Family Applications (1)

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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 (https=)
EP (1) EP3619208B1 (https=)
JP (1) JP7096268B2 (https=)
KR (1) KR20200003121A (https=)
CN (1) CN110603255B (https=)
AU (1) AU2018261591B2 (https=)
CA (1) CA3059790A1 (https=)
MX (1) MX389014B (https=)
MY (1) MY200348A (https=)
PH (1) PH12019502425A1 (https=)
SG (1) SG11201909376TA (https=)
TW (1) TWI808083B (https=)
WO (1) WO2018204236A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
MX2021004582A (es) 2018-10-29 2021-06-15 Theravance Biopharma R&D Ip Llc Compuesto 2-azabiciclo hexano inhibidor de jak.
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
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
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

Citations (2)

* 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
WO2017079205A1 (en) * 2015-11-03 2017-05-11 Theravance Biopharma R&D Ip, Llc Jak kinase inhibitor compounds for treatment of respiratory disease

Family Cites Families (14)

* 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
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
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
US10556901B2 (en) 2015-11-03 2020-02-11 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
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

Patent Citations (2)

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

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Granted publication date: 20230210