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
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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)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (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

Family

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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 (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=)

Cited By (3)

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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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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
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
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
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

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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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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
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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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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
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
AU2018273866B2 (en) 2021-09-30
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
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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