MX2017013892A - Inhibidores novedosos del factor xii activado por la enzima (fxiia). - Google Patents

Inhibidores novedosos del factor xii activado por la enzima (fxiia).

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Publication number
MX2017013892A
MX2017013892A MX2017013892A MX2017013892A MX2017013892A MX 2017013892 A MX2017013892 A MX 2017013892A MX 2017013892 A MX2017013892 A MX 2017013892A MX 2017013892 A MX2017013892 A MX 2017013892A MX 2017013892 A MX2017013892 A MX 2017013892A
Authority
MX
Mexico
Prior art keywords
amino acid
present
fxiia
factor xii
activated factor
Prior art date
Application number
MX2017013892A
Other languages
English (en)
Inventor
Heinis Christian
Middendorp Simon
Alfred Karl WILBS Jonas
BAERISWYL Vanessa
Original Assignee
Ecole Polytechnique Fed Lausanne Epfl
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 Ecole Polytechnique Fed Lausanne Epfl filed Critical Ecole Polytechnique Fed Lausanne Epfl
Publication of MX2017013892A publication Critical patent/MX2017013892A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/52—Cyclic peptides containing at least one abnormal peptide link with only normal peptide links in the ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6451—Coagulation factor XIIa (3.4.21.38)
    • 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
    • C12Q1/56—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving blood clotting factors, e.g. involving thrombin, thromboplastin, fibrinogen
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/86—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving blood coagulating time or factors, or their receptors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • G01N2333/81—Protease inhibitors
    • G01N2333/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • G01N2333/811—Serine protease (E.C. 3.4.21) inhibitors
    • 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
    • G01N2333/96433—Serine endopeptidases (3.4.21)
    • G01N2333/96441—Serine endopeptidases (3.4.21) with definite EC number
    • G01N2333/96458—Factor XII (3.4.21.38)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Engineering & Computer Science (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)

Abstract

La presente invención se refiere a un inhibidor bicíclico del factor XII activado por la enzima de coagulación (FXIIa) que comprende o que consiste del péptido (X1) (X2) (X3)n(X4)RL(X5) (X6)m(X7) (X9)l(X10) (X11) (X12) (X13) (X14)k(X15) (X16), en donde (X1) está presente o ausente y, si está presente, es un aminoácido; (X2) es un aminoácido con una cadena lateral; (X3) es un aminoácido y n está entre 0 y 3, preferiblemente 0 o 1 y lo más preferiblemente 0; (X4) es un aminoácido L alifático o un aminoácido L cíclico, preferiblemente L, P o un aminoácido L aromático, y lo más preferiblemente un aminoácido L aromático; (X5) es un aminoácido; (X6) es un aminoácido y m está entre 0 y 3, preferiblemente 0 o 1 y lo más preferiblemente 0; (X7) es un aminoácido con una cadena lateral; (X9) es un aminoácido y 1 está entre 0 y 3, preferiblemente 0 o 1 y lo más preferiblemente 0; (X10) es un aminoácido; (X11) es un aminoácido, preferiblemente Q; (X12) es un aminoácido L hidrofóbico, preferiblemente un aminoácido L alifático, y es más preferiblemente L; (X13) es un aminoácido; (X14) es un aminoácido y k está entre 0 y 3, preferiblemente 0 o 1 y lo más preferiblemente 0, (X15) es un aminoácido con una cadena lateral; y (X16) está presente o ausente y, si está presente, es un aminoácido; y en donde las cadenas laterales de (X2), (X7) y (X15) están conectadas por medio de una molécula de conexión, la molécula de conexión que tiene al menos tres grupos funcionales, cada grupo funcional que forma un enlace covalente con una de las cadenas laterales de (X2), (X7) y (X15).
MX2017013892A 2015-04-28 2016-04-27 Inhibidores novedosos del factor xii activado por la enzima (fxiia). MX2017013892A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15165508 2015-04-28
PCT/EP2016/059435 WO2016174103A1 (en) 2015-04-28 2016-04-27 Novel inhibitors of the enzyme activated factor xii (fxiia)

Publications (1)

Publication Number Publication Date
MX2017013892A true MX2017013892A (es) 2018-06-06

Family

ID=53052688

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017013892A MX2017013892A (es) 2015-04-28 2016-04-27 Inhibidores novedosos del factor xii activado por la enzima (fxiia).

Country Status (10)

Country Link
US (1) US20180118786A1 (es)
EP (1) EP3288962A1 (es)
JP (1) JP2018521960A (es)
KR (1) KR20170137929A (es)
CN (1) CN107810190A (es)
AU (1) AU2016256226A1 (es)
CA (1) CA2982413A1 (es)
IL (1) IL255154A0 (es)
MX (1) MX2017013892A (es)
WO (1) WO2016174103A1 (es)

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CN107148425B (zh) 2014-10-29 2021-08-03 拜斯科阿迪有限公司 对mt1-mmp特异性的双环肽配体
EP3645549A1 (en) 2017-06-26 2020-05-06 BicycleRD Limited Bicyclic peptide ligands with detectable moieties and uses thereof
JP7670481B2 (ja) 2017-08-04 2025-04-30 バイスクルテクス・リミテッド Ｃｄ１３７に対して特異的な二環式ペプチドリガンド
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
CN111902429A (zh) 2018-02-23 2020-11-06 拜斯科技术开发有限公司 多聚体双环肽配体
GB201810329D0 (en) * 2018-06-22 2018-08-08 Bicycletx Ltd Peptide ligands for binding to integrin avB3
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
GB201810320D0 (en) * 2018-06-22 2018-08-08 Bicycletx Ltd Peptide ligands for binding to CD38
GB201810327D0 (en) * 2018-06-22 2018-08-08 Bicycletx Ltd Peptide ligands for binding to IL-17
IL279489B2 (en) * 2018-06-22 2025-10-01 Bicycletx Ltd Bicyclic peptide ligands specific for nectin-4, a drug conjugate containing the peptide ligands and a pharmaceutical composition containing the drug conjugate
JP7135620B2 (ja) * 2018-09-07 2022-09-13 ソニーグループ株式会社 血液凝固系解析装置、血液凝固系解析方法及び血液凝固系解析プログラム
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for MT1-MMP
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
WO2020128527A1 (en) 2018-12-21 2020-06-25 Bicyclerd Limited Bicyclic peptide ligands specific for pd-l1
US12492224B2 (en) 2018-12-21 2025-12-09 Bicycletx Limited Bicyclic peptide ligands specific for PD-L1
GB201900530D0 (en) * 2019-01-15 2019-03-06 Bicyclerd Ltd Bicyclic peptide ligands specific for CD38
GB201900529D0 (en) * 2019-01-15 2019-03-06 Bicycletx Ltd Bicyclic peptide ligands specific for CD38
TWI860386B (zh) 2019-07-30 2024-11-01 英商拜西可泰克斯有限公司 異質雙環肽複合物
GB201918559D0 (en) * 2019-12-16 2020-01-29 Bicycle Tx Ltd Bicyclic peptide ligands specific for IL-17
GB201918558D0 (en) * 2019-12-16 2020-01-29 Bicycle Tx Ltd Bicyclic peptide ligands specific for IL-17
GB201918557D0 (en) * 2019-12-16 2020-01-29 Bicycle Tx Ltd Bicyclic peptide ligands specific for IL-17
WO2021123767A1 (en) * 2019-12-16 2021-06-24 Bicycletx Limited Bicyclic peptide ligands specific for il-17
EP4101929A4 (en) * 2019-12-27 2024-05-22 The University of Tokyo BANK CONSTRUCTION METHOD, CYCLIC PEPTIDE, FXIIA BINDER AND IFNGR1 BINDER
GB202002706D0 (en) * 2020-02-26 2020-04-08 Bicycletx Ltd Pbp3 binding bicyclic peptide ligands
AU2021322934A1 (en) 2020-08-03 2023-03-30 Bicycletx Limited Peptide-based linkers

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CA2591786C (en) * 2004-12-23 2013-07-16 Bernhard Nieswandt Prevention of thrombus formation and/or stabilization
CN101538317B (zh) * 2007-02-08 2012-02-29 深圳信立泰药业股份有限公司 凝血酶直接抑制剂多肽水合盐及合成方法
EP2371857A1 (en) * 2010-04-01 2011-10-05 CSL Behring GmbH Factor XII inhibitors for treating interstitial lung disease

Also Published As

Publication number Publication date
AU2016256226A1 (en) 2017-11-23
CN107810190A (zh) 2018-03-16
IL255154A0 (en) 2017-12-31
EP3288962A1 (en) 2018-03-07
JP2018521960A (ja) 2018-08-09
KR20170137929A (ko) 2017-12-13
US20180118786A1 (en) 2018-05-03
WO2016174103A1 (en) 2016-11-03
CA2982413A1 (en) 2016-11-03

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