MX2015005744A - Inhibidores de malti de molecula pequeña. - Google Patents

Inhibidores de malti de molecula pequeña.

Info

Publication number
MX2015005744A
MX2015005744A MX2015005744A MX2015005744A MX2015005744A MX 2015005744 A MX2015005744 A MX 2015005744A MX 2015005744 A MX2015005744 A MX 2015005744A MX 2015005744 A MX2015005744 A MX 2015005744A MX 2015005744 A MX2015005744 A MX 2015005744A
Authority
MX
Mexico
Prior art keywords
malt1
dlbcl
abc
activity
suppression
Prior art date
Application number
MX2015005744A
Other languages
English (en)
Inventor
Ari Melnick
Hao Wu
Original Assignee
Univ Cornell
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.)
Filing date
Publication date
Application filed by Univ Cornell filed Critical Univ Cornell
Publication of MX2015005744A publication Critical patent/MX2015005744A/es

Links

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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • 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)
    • G01N2333/948—Hydrolases (3) acting on peptide bonds (3.4)
    • G01N2333/95—Proteinases, i.e. endopeptidases (3.4.21-3.4.99)
    • G01N2333/964—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue
    • G01N2333/96425—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals
    • G01N2333/96427—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general
    • G01N2333/9643—Proteinases, i.e. endopeptidases (3.4.21-3.4.99) derived from animal tissue from mammals in general with EC number
    • G01N2333/96466—Cysteine endopeptidases (3.4.22)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/20—Screening for compounds of potential therapeutic value cell-free systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Analytical Chemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Microbiology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La actividad de escisión de MALT1 está enlazada a la patogénesis de linfoma difuso de célula B grande de tipo célula B activada (DLBCL ABC-), una forma quimio-resistente de DLBCL. Se han desarrollado un ensayo de actividad de MALT1 y se identificaron los inhibidores de MALT1 químicamente diversos. Un compuesto principal seleccionado Ml-2 caracteriza la unión directa a MALT1 y supresión de su función de proteasa. Ml-2 se concentra dentro de células DLBCL-ABC humanas e inhibe irreversiblemente la escisión de sustratos de MALT1. Esto va acompañado por la supresión de la actividad de NF-?B reportero, la inhibición de la ubicación nuclear de c-REL y sub-regulación de la firma génica de NF-?B objetivo. Más notablemente, Ml-2 no fue tóxico para los ratones, y desplegó una actividad potente y específica contra líneas celulares de DLBCL-ABC in vitro, y tumores DLBCL-ABC xeno-trasplantados in vivo. El compuesto también fue efectivo contra no DLBCL -GCB humanos primarios ex vivo.
MX2015005744A 2012-11-09 2013-11-08 Inhibidores de malti de molecula pequeña. MX2015005744A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261724650P 2012-11-09 2012-11-09
PCT/US2013/069141 WO2014074815A1 (en) 2012-11-09 2013-11-08 Small molecule inhibitors of malt1

Publications (1)

Publication Number Publication Date
MX2015005744A true MX2015005744A (es) 2016-02-10

Family

ID=50685175

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015005744A MX2015005744A (es) 2012-11-09 2013-11-08 Inhibidores de malti de molecula pequeña.

Country Status (14)

Country Link
US (1) US9592223B2 (es)
EP (1) EP2916656B1 (es)
JP (1) JP6159814B2 (es)
KR (1) KR20150093695A (es)
CN (1) CN105188376B (es)
AU (1) AU2013342267B2 (es)
BR (1) BR112015010504A2 (es)
CA (1) CA2890706A1 (es)
EA (1) EA201590916A1 (es)
IL (1) IL238719A0 (es)
MX (1) MX2015005744A (es)
PH (1) PH12015501035A1 (es)
SG (1) SG11201503642YA (es)
WO (1) WO2014074815A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2890706A1 (en) 2012-11-09 2014-05-15 Cornell University Small molecule inhibitors of malt1
JP6989505B2 (ja) 2015-08-28 2022-01-05 コーネル ユニヴァーシティー Ｍａｌｔ１阻害剤およびその使用
JPWO2017057695A1 (ja) * 2015-09-30 2018-07-19 東レ株式会社 ジフェニルピラゾール誘導体及びその医薬用途
CN107296807B (zh) * 2016-04-15 2020-03-20 中国科学院上海生命科学研究院 Malt1靶向抑制物在制备malt1依赖性肿瘤治疗药物中的应用
CN109476599A (zh) * 2016-07-29 2019-03-15 东丽株式会社 胍衍生物和其医药用途
RU2021113671A (ru) 2016-07-29 2021-07-08 Люпин Лимитед Замещенные тиазолопиридиновые соединения в качестве ингибиторов malt1
PE20190656A1 (es) 2016-07-29 2019-05-08 Lupin Ltd Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
JPWO2018159650A1 (ja) * 2017-02-28 2019-12-19 東レ株式会社 グアニジン誘導体及びその医薬用途
US11248007B2 (en) 2017-03-08 2022-02-15 Cornell University Inhibitors of MALT1 and uses thereof
CN107162978B (zh) * 2017-05-25 2019-06-07 福州大学 一种1,3,5-三取代吡唑化合物及其制备方法和应用
CN107698511B (zh) * 2017-11-07 2020-05-08 福州大学 一种1,3-二芳基-5-烷氧基吡唑化合物及其制备方法和应用
SG11202006200RA (en) 2017-12-28 2020-07-29 Massachusetts Gen Hospital Targeting the cbm signalosome complex induces regulatory t cells to inflame the tumor microenvironment
WO2021262969A1 (en) 2020-06-24 2021-12-30 The General Hospital Corporation Materials and methods of treating cancer
CN116710089A (zh) * 2020-11-12 2023-09-05 莫诺泰罗斯疗法公司 治疗癌症的材料和方法
CN113908279B (zh) * 2021-11-16 2022-12-06 四川大学华西医院 Malt1基因作为标志物在制备治疗结直肠癌药物中的应用
CA3240140A1 (en) * 2021-12-10 2023-06-15 Rarefied Biosciences, Inc. Methods for treating diseases using malt1 inhibitors
AU2022425324A1 (en) 2021-12-30 2024-05-30 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Tricyclic derivative inhibitor, preparation method therefor, and application thereof
CN114974441B (zh) * 2022-05-27 2024-07-12 煤炭科学研究总院有限公司 一种煤分子官能团生成方法

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PT1163208E (pt) 1999-08-06 2004-08-31 Vertex Pharma Inibidores de caspase e as suas utilizacoes
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AU2003300018A1 (en) * 2002-10-11 2004-05-04 Bristol-Myers Squibb Company Process for the preparation of tri-nitrogen containing heteroaryl-diamine derivatives useful as pharmaceutical agents and methods of producing pharmaceutical agents
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CA2890706A1 (en) 2012-11-09 2014-05-15 Cornell University Small molecule inhibitors of malt1

Also Published As

Publication number Publication date
EP2916656A4 (en) 2016-09-14
EP2916656A1 (en) 2015-09-16
CA2890706A1 (en) 2014-05-15
SG11201503642YA (en) 2015-06-29
EA201590916A1 (ru) 2016-02-29
JP6159814B2 (ja) 2017-07-05
CN105188376A (zh) 2015-12-23
US9592223B2 (en) 2017-03-14
BR112015010504A2 (pt) 2017-12-05
IL238719A0 (en) 2015-06-30
AU2013342267B2 (en) 2017-01-12
KR20150093695A (ko) 2015-08-18
CN105188376B (zh) 2017-12-01
WO2014074815A1 (en) 2014-05-15
JP2015536990A (ja) 2015-12-24
EP2916656B1 (en) 2017-10-25
US20150297570A1 (en) 2015-10-22
PH12015501035A1 (en) 2015-08-24

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