CN110662747A - Janus激酶抑制剂的葡糖苷酸前药 - Google Patents

Janus激酶抑制剂的葡糖苷酸前药 Download PDF

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Publication number
CN110662747A
CN110662747A CN201880034623.7A CN201880034623A CN110662747A CN 110662747 A CN110662747 A CN 110662747A CN 201880034623 A CN201880034623 A CN 201880034623A CN 110662747 A CN110662747 A CN 110662747A
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CN
China
Prior art keywords
compound
methyl
formula
trifluoromethyl
hydrogen
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Pending
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CN201880034623.7A
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English (en)
Chinese (zh)
Inventor
丹尼尔·D·朗
唐娜·A·A·威尔顿
曼迪·洛
R·赫德森
P·J·布拉希尔
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Theravance Biopharma R&D IP LLC
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Theravance Biopharma R&D IP LLC
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Publication of CN110662747A publication Critical patent/CN110662747A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds 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
    • A61K31/7064Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/12Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)
CN201880034623.7A 2017-05-23 2018-05-22 Janus激酶抑制剂的葡糖苷酸前药 Pending CN110662747A (zh)

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 (1)

Publication Number Publication Date
CN110662747A true CN110662747A (zh) 2020-01-07

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Family Applications (1)

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CN201880034623.7A Pending CN110662747A (zh) 2017-05-23 2018-05-22 Janus激酶抑制剂的葡糖苷酸前药

Country Status (14)

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

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111196831A (zh) * 2020-01-20 2020-05-26 山西医科大学 一种呋喃酚葡萄糖醛酸结合物的制备方法
CN115073543A (zh) * 2022-07-20 2022-09-20 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
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

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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
WO2023018954A1 (en) * 2021-08-12 2023-02-16 Concert Pharmaceuticals, Inc. Treatment of jak-inhibition-responsive disorders with prodrugs of jak inhibitors
EP4507691A2 (en) * 2022-04-15 2025-02-19 The Regents Of The University Of Michigan Jak inhibitor analogs, formulations, and uses thereof
WO2024133631A1 (en) 2022-12-22 2024-06-27 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

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WO1993022334A1 (en) * 1992-05-04 1993-11-11 Sri International Pharmaceutical compositions and methods for colonic delivery of corticosteroids
CN102596960A (zh) * 2009-10-09 2012-07-18 因西特公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
CN106496233A (zh) * 2016-09-26 2017-03-15 东南大学 吡咯并嘧啶类化合物、其制备方法及其用途

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US5811388A (en) 1995-06-07 1998-09-22 Cibus Pharmaceutical, Inc. Delivery of drugs to the lower GI tract
AU777911B2 (en) 1999-12-10 2004-11-04 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
US7798257B2 (en) 2004-04-30 2010-09-21 Smith International, Inc. Shaped cutter surface
DK3184526T3 (en) 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
ES2602577T3 (es) 2008-03-11 2017-02-21 Incyte Holdings Corporation Derivados de azetidina y ciclobutano como inhibidores de JAK
RU2493157C2 (ru) 2008-08-20 2013-09-20 Пфайзер Инк. ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА
EP2515913A2 (en) 2009-12-23 2012-10-31 Glycomyr Inc. Use of vitamin d glycosides and sulfates for treatment of disease
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
CN102822177A (zh) 2010-02-05 2012-12-12 美国辉瑞有限公司 吡咯并[2,3-d]嘧啶脲化合物
CA2913752A1 (en) 2013-05-31 2014-12-04 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery
EA035816B1 (ru) 2015-11-24 2020-08-14 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта

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WO1993022334A1 (en) * 1992-05-04 1993-11-11 Sri International Pharmaceutical compositions and methods for colonic delivery of corticosteroids
CN102596960A (zh) * 2009-10-09 2012-07-18 因西特公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
CN106496233A (zh) * 2016-09-26 2017-03-15 东南大学 吡咯并嘧啶类化合物、其制备方法及其用途

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FRÉDÉRIC SCHMIDT等,: "In vitro fluorine-19 nuclear magnetic resonance study of the liberation of antitumor nitrogen mustard from prodrugs", 《J. CHEM. SOC.,PERKIN TRANS.1》 *
ISABELLETRANOY-OPALINSKI等: "β-Glucuronidase-responsive prodrugs for selective cancer chemotherapy: An update", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 *
S. PAPOT等: "Design of Selectively Activated Anticancer Prodrugs: Elimination and Cyclization Strategies", 《CURR. MED. CHEM. - ANTI-CANCER AGENTS》 *
STE´PHANE ANGENAULT等: "Cancer Chemotherapy: A SN-38 (7-Ethyl-10-hydroxycamptothecin)Glucuronide Prodrug for Treatment by a PMT (Prodrug MonoTherapy) Strategy", 《BIOORGANIC & MEDICINAL CHEMISTRY LETTERS》 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111196831A (zh) * 2020-01-20 2020-05-26 山西医科大学 一种呋喃酚葡萄糖醛酸结合物的制备方法
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
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
CN115073543A (zh) * 2022-07-20 2022-09-20 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

Also Published As

Publication number Publication date
PH12019502605A1 (en) 2020-10-26
AU2018273866A1 (en) 2019-12-19
RU2019142472A3 (enExample) 2021-09-23
WO2018217700A1 (en) 2018-11-29
BR112019024509A2 (pt) 2020-06-23
NZ759764A (en) 2022-07-01
RU2019142472A (ru) 2021-06-24
US20180339990A1 (en) 2018-11-29
IL270693A (en) 2020-01-30
CA3063963A1 (en) 2018-11-29
AU2018273866B2 (en) 2021-09-30
EP3609899A1 (en) 2020-02-19
KR20200010440A (ko) 2020-01-30
JP2020520955A (ja) 2020-07-16
MX2019014054A (es) 2020-02-05
US10745405B2 (en) 2020-08-18
US20210032250A1 (en) 2021-02-04

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