CN116687934A - 用于治疗纤维化的化合物和组合物 - Google Patents

用于治疗纤维化的化合物和组合物 Download PDF

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Publication number
CN116687934A
CN116687934A CN202310653335.2A CN202310653335A CN116687934A CN 116687934 A CN116687934 A CN 116687934A CN 202310653335 A CN202310653335 A CN 202310653335A CN 116687934 A CN116687934 A CN 116687934A
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China
Prior art keywords
mkp
compound
thio
alkyl
disease
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Pending
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CN202310653335.2A
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English (en)
Chinese (zh)
Inventor
A·班尼特
J·埃尔曼
H·贾马尔
K·S·安德森
E·洛丽丝
D·霍耶
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Yale University
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Yale University
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Publication of CN116687934A publication Critical patent/CN116687934A/zh
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/42—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving phosphatase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G01N2333/916—Hydrolases (3) acting on ester bonds (3.1), e.g. phosphatases (3.1.3), phospholipases C or phospholipases D (3.1.4)

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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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Analytical Chemistry (AREA)
  • Biophysics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
CN202310653335.2A 2017-12-18 2018-12-18 用于治疗纤维化的化合物和组合物 Pending CN116687934A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201762607110P 2017-12-18 2017-12-18
US62/607,110 2017-12-18
CN201880088382.4A CN111670188B (zh) 2017-12-18 2018-12-18 用于治疗纤维化的化合物和组合物
PCT/US2018/066191 WO2019126141A1 (en) 2017-12-18 2018-12-18 Compounds and compositions for treating fibrosis

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201880088382.4A Division CN111670188B (zh) 2017-12-18 2018-12-18 用于治疗纤维化的化合物和组合物

Publications (1)

Publication Number Publication Date
CN116687934A true CN116687934A (zh) 2023-09-05

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CN202310653335.2A Pending CN116687934A (zh) 2017-12-18 2018-12-18 用于治疗纤维化的化合物和组合物
CN201880088382.4A Active CN111670188B (zh) 2017-12-18 2018-12-18 用于治疗纤维化的化合物和组合物

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Country Status (9)

Country Link
US (3) US11504373B2 (https=)
EP (1) EP3732179B1 (https=)
JP (2) JP7317039B2 (https=)
KR (1) KR20200100726A (https=)
CN (2) CN116687934A (https=)
AU (3) AU2018388549B2 (https=)
CA (1) CA3085770A1 (https=)
MX (2) MX2020006398A (https=)
WO (1) WO2019126141A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2018388549B2 (en) * 2017-12-18 2023-06-01 Yale University Compounds and compositions for treating fibrosis
US12570670B2 (en) * 2019-01-30 2026-03-10 Yale University Compounds, compositions, and methods for treating fibrosis

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040086859A1 (en) 2000-04-10 2004-05-06 Klaus Ducker Identification of a dual specificity phosphate: dusp-10
DE60125783T2 (de) * 2000-08-11 2007-10-18 Evotec Ag Verfahren zum nachweis von acetylase oder deacetylase-aktivität in einem immunoassay
US20030162230A1 (en) * 2000-09-27 2003-08-28 Reagan Kevin J. Method for quantifying phosphokinase activity on proteins
JP2007518702A (ja) * 2003-11-25 2007-07-12 ノバルティス アクチエンゲゼルシャフト ソマトスタチン類似体処置の効力についてのバイオマーカー
US8546410B2 (en) 2008-05-05 2013-10-01 Abbvie Inc. Heteroaryl-fused macrocyclic pyrimidine derivatives
EP2351571A4 (en) * 2008-10-09 2012-08-01 Lsip Llc PROTEINPHOSPHATASEHEMMER
CA2944198C (en) 2013-04-26 2021-11-16 Indiana University Research & Technology Corporation Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2)
AU2018388549B2 (en) * 2017-12-18 2023-06-01 Yale University Compounds and compositions for treating fibrosis

Also Published As

Publication number Publication date
AU2018388549B2 (en) 2023-06-01
KR20200100726A (ko) 2020-08-26
JP2021506975A (ja) 2021-02-22
JP2023145544A (ja) 2023-10-11
EP3732179B1 (en) 2024-05-01
EP3732179A1 (en) 2020-11-04
EP3732179A4 (en) 2022-01-19
US20240335445A1 (en) 2024-10-10
CN111670188A (zh) 2020-09-15
AU2023204581A1 (en) 2023-10-05
AU2023204581B2 (en) 2025-06-26
JP7317039B2 (ja) 2023-07-28
US20200390770A1 (en) 2020-12-17
MX2020006398A (es) 2020-09-07
CA3085770A1 (en) 2019-06-27
MX2023009895A (es) 2023-09-04
CN111670188B (zh) 2023-06-23
AU2025234269A1 (en) 2025-10-16
US20230181588A1 (en) 2023-06-15
WO2019126141A1 (en) 2019-06-27
JP7676477B2 (ja) 2025-05-14
US11504373B2 (en) 2022-11-22
AU2018388549A1 (en) 2020-07-02

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