AU2018273866B2 - Glucuronide prodrugs of Janus kinase inhibitors - Google Patents

Glucuronide prodrugs of Janus kinase inhibitors Download PDF

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Publication number
AU2018273866B2
AU2018273866B2 AU2018273866A AU2018273866A AU2018273866B2 AU 2018273866 B2 AU2018273866 B2 AU 2018273866B2 AU 2018273866 A AU2018273866 A AU 2018273866A AU 2018273866 A AU2018273866 A AU 2018273866A AU 2018273866 B2 AU2018273866 B2 AU 2018273866B2
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AU
Australia
Prior art keywords
compound
methyl
formula
trifluoromethyl
hydrogen
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
AU2018273866A
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English (en)
Other versions
AU2018273866A1 (en
Inventor
Patrick J. Brassil
Ryan Hudson
Daniel D. Long
Mandy Loo
Donna A.A. Wilton
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Theravance Biopharma R&D IP LLC
Original Assignee
Theravance Biopharma R&D IP LLC
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.)
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Publication of AU2018273866A1 publication Critical patent/AU2018273866A1/en
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Publication of AU2018273866B2 publication Critical patent/AU2018273866B2/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/12—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group -X-C(=X)-X-, or halides thereof, in which each X means nitrogen, oxygen, sulfur, selenium or tellurium, e.g. carbonic acid, carbamic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
AU2018273866A 2017-05-23 2018-05-22 Glucuronide prodrugs of Janus kinase inhibitors Expired - Fee Related AU2018273866B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762509847P 2017-05-23 2017-05-23
US62/509,847 2017-05-23
PCT/US2018/033818 WO2018217700A1 (en) 2017-05-23 2018-05-22 Glucuronide prodrugs of janus kinase inhibitors

Publications (2)

Publication Number Publication Date
AU2018273866A1 AU2018273866A1 (en) 2019-12-19
AU2018273866B2 true AU2018273866B2 (en) 2021-09-30

Family

ID=62621001

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018273866A Expired - Fee Related AU2018273866B2 (en) 2017-05-23 2018-05-22 Glucuronide prodrugs of Janus kinase inhibitors

Country Status (14)

Country Link
US (2) US10745405B2 (https=)
EP (1) EP3609899A1 (https=)
JP (1) JP2020520955A (https=)
KR (1) KR20200010440A (https=)
CN (1) CN110662747A (https=)
AU (1) AU2018273866B2 (https=)
BR (1) BR112019024509A2 (https=)
CA (1) CA3063963A1 (https=)
IL (1) IL270693A (https=)
MX (1) MX2019014054A (https=)
NZ (1) NZ759764A (https=)
PH (1) PH12019502605A1 (https=)
RU (1) RU2019142472A (https=)
WO (1) WO2018217700A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111094314B (zh) * 2018-08-15 2022-08-12 江苏豪森药业集团有限公司 含有葡糖苷酸衍生物jak抑制剂的前药及其制备方法和应用
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
US12551564B2 (en) 2019-12-10 2026-02-17 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
WO2021127190A1 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN111196831B (zh) * 2020-01-20 2023-05-09 山西医科大学 一种呋喃酚葡萄糖醛酸结合物的制备方法
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
EP4384173A1 (en) * 2021-08-12 2024-06-19 Sun Pharmaceutical Industries, Inc. Treatment of jak-inhibition-responsive disorders with prodrugs of jak inhibitors
WO2023155905A1 (zh) * 2022-02-21 2023-08-24 上海岸阔医药科技有限公司 化合物及其用途
CN119923257A (zh) * 2022-04-15 2025-05-02 密歇根大学董事会 Jak抑制剂类似物、制剂及其用途
CN115073543B (zh) * 2022-07-20 2022-11-15 北京普祺医药科技股份有限公司 一种jak抑制剂的化合物前药及其制备与应用
EP4637724A1 (en) 2022-12-22 2025-10-29 KRKA, d.d., Novo mesto Veterinary composition comprising oclacitinib
WO2024148049A1 (en) * 2023-01-04 2024-07-11 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110086810A1 (en) * 2009-10-09 2011-04-14 Incyte Corporation HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d] PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993022334A1 (en) * 1992-05-04 1993-11-11 Sri International Pharmaceutical compositions and methods for colonic delivery of corticosteroids
US5811388A (en) 1995-06-07 1998-09-22 Cibus Pharmaceutical, Inc. Delivery of drugs to the lower GI tract
EP1382339B1 (en) 1999-12-10 2007-12-05 Pfizer Products Inc. Compositions containing pyrrolo ¬2,3-d pyrimidine derivatives
US7798257B2 (en) 2004-04-30 2010-09-21 Smith International, Inc. Shaped cutter surface
EP2455382B1 (en) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US8158616B2 (en) 2008-03-11 2012-04-17 Incyte Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
JP4884570B2 (ja) 2008-08-20 2012-02-29 ファイザー・インク ピロロ［２，３−ｄ］ピリミジン化合物
EP2695617B1 (en) 2009-12-23 2019-01-09 Glycomyr Inc. Vitamin D glycosides and sulfates for treating intestinal diseases
CN102724967A (zh) 2009-12-31 2012-10-10 安龙制药公司 包括可释放的脲连接体的含芳香胺化合物的聚合缀合物
JP2013518882A (ja) 2010-02-05 2013-05-23 ファイザー・インク ＪＡＫ阻害剤としてのピロロ［２，３−ｄ］ピリミジン尿素化合物
JP2016528174A (ja) 2013-05-31 2016-09-15 セルリアン・ファーマ・インコーポレイテッド 治療的送達用のシクロデキストリンベースのポリマー
ES2784523T3 (es) 2015-11-24 2020-09-28 Theravance Biopharma R&D Ip Llc Profármacos de un compuesto inhibidor de JAK para el tratamiento de enfermedades inflamatorias gastrointestinales
CN106496233B (zh) * 2016-09-26 2018-05-15 东南大学 吡咯并嘧啶类化合物、其制备方法及其用途

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110086810A1 (en) * 2009-10-09 2011-04-14 Incyte Corporation HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d] PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE

Also Published As

Publication number Publication date
WO2018217700A1 (en) 2018-11-29
US10745405B2 (en) 2020-08-18
MX2019014054A (es) 2020-02-05
US20180339990A1 (en) 2018-11-29
RU2019142472A3 (https=) 2021-09-23
NZ759764A (en) 2022-07-01
EP3609899A1 (en) 2020-02-19
CA3063963A1 (en) 2018-11-29
US20210032250A1 (en) 2021-02-04
JP2020520955A (ja) 2020-07-16
IL270693A (en) 2020-01-30
CN110662747A (zh) 2020-01-07
PH12019502605A1 (en) 2020-10-26
AU2018273866A1 (en) 2019-12-19
RU2019142472A (ru) 2021-06-24
KR20200010440A (ko) 2020-01-30
BR112019024509A2 (pt) 2020-06-23

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MK25 Application lapsed reg. 22.2i(2) - failure to pay acceptance fee