WO2024259310A3 - Composés antagonistes de pcsk9 perméables passifs - Google Patents

Composés antagonistes de pcsk9 perméables passifs Download PDF

Info

Publication number
WO2024259310A3
WO2024259310A3 PCT/US2024/034113 US2024034113W WO2024259310A3 WO 2024259310 A3 WO2024259310 A3 WO 2024259310A3 US 2024034113 W US2024034113 W US 2024034113W WO 2024259310 A3 WO2024259310 A3 WO 2024259310A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
passive
permeable
antagonist compounds
pcsk9
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
PCT/US2024/034113
Other languages
English (en)
Other versions
WO2024259310A2 (fr
Inventor
Abbas M. Walji
Harold B. Wood
Yuhua Huang
Thomas Joseph Tucker
Yi-Heng Chen
Mark W. Embrey
Fa-Xiang Ding
Jennifer HANISAK
Charles Lee Jayne
Chengwei WU
Jennifer Marie JOHNSTON
Shawn P. Walsh
Zhongxiang Sun
Danila Branca
Stefania Colarusso
Anilkumar G. Nair
Michael Man-Chu Lo
Peter Orth
Sookhee Nicole Ha
Liangqin Guo
Ling Tong
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of WO2024259310A2 publication Critical patent/WO2024259310A2/fr
Publication of WO2024259310A3 publication Critical patent/WO2024259310A3/fr
Anticipated expiration legal-status Critical
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • 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
    • A61P3/06—Antihyperlipidemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Des composés de formule (I), ou un sel pharmaceutiquement acceptable de ceux-ci (I), où A, B, R1, R2, R3, R4 et<sp />R5 sont tels que définis dans la description. Ces composés sont des antagonistes de PCSK9 et ont une perméabilité passive (ou intrinsèque) élevée de telle sorte qu'ils peuvent être utilisés sans agent d'amélioration de la perméabilité. L'invention concerne également des compositions pharmaceutiques comprenant les composés de formule I ou leurs sels, et des méthodes de traitement de maladies cardiovasculaires et d'états liés à l'activité du PCSK9, par exemple l'athérosclérose, l'hypercholestérolémie, la coronaropathie, le syndrome métabolique, le syndrome coronarien aigu ou les maladies cardiovasculaires et cardiométaboliques associées.
PCT/US2024/034113 2023-06-15 2024-06-14 Composés antagonistes de pcsk9 perméables passifs Pending WO2024259310A2 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202363508454P 2023-06-15 2023-06-15
US63/508,454 2023-06-15
US202363517742P 2023-08-04 2023-08-04
US63/517,742 2023-08-04

Publications (2)

Publication Number Publication Date
WO2024259310A2 WO2024259310A2 (fr) 2024-12-19
WO2024259310A3 true WO2024259310A3 (fr) 2025-01-16

Family

ID=93852845

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2024/034113 Pending WO2024259310A2 (fr) 2023-06-15 2024-06-14 Composés antagonistes de pcsk9 perméables passifs

Country Status (1)

Country Link
WO (1) WO2024259310A2 (fr)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019246349A1 (fr) * 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Composés antagonistes du pcsk9
WO2019246387A1 (fr) * 2018-06-21 2019-12-26 Ra Pharmaceuticals, Inc. Peptides cycliques pour l'inhibition de la pcsk9
WO2019246352A1 (fr) * 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Composés bicycliques antagonistes de pcsk9

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019246349A1 (fr) * 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Composés antagonistes du pcsk9
WO2019246387A1 (fr) * 2018-06-21 2019-12-26 Ra Pharmaceuticals, Inc. Peptides cycliques pour l'inhibition de la pcsk9
WO2019246352A1 (fr) * 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Composés bicycliques antagonistes de pcsk9

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ZHANG ET AL.: "Identification of a Small Peptide That Inhibits PCSK9 Protein Binding to the Low Density Lipoprotein Receptor", THE JOURNAL OF BIOLOGICAL CHEMISTRY ., vol. 289, no. 2, 2014, pages 942 - 955, XP055546006, DOI: 10.1074/jbc.M113.514067 *

Also Published As

Publication number Publication date
WO2024259310A2 (fr) 2024-12-19

Similar Documents

Publication Publication Date Title
EP4660303A3 (fr) Composés antagonistes de pcsk9
DE69815003T2 (de) Stabilisierte pharmazeutische Zusammensetzung
NO20041631L (no) Piperazinderivater med CCR1 reseptor antagonist
CA2694270A1 (fr) Aryloxazoles substitues et leur utilisation
IL314009B1 (en) Parp1 inhibitors and uses thereof
JP2017533930A5 (fr)
BR0215777A (pt) Composto, método para preparar o mesmo, composição farmacêutica para prevenir e tratar cardioisquemia, cerebroisquemia, oclusão arterial cerebral e para melhorar microcirculação do cérebro, e uso do composto
NO931921D0 (no) Fremgangsmaate for fremstilling av nye hydroksamsyre- og n-hydroksyurinstoff-derivater
MA46608B1 (fr) Formulation liposomale utile pour le traitement du cancer
CA2387134A1 (fr) Nouveaux cyclopropanes utilises comme antagonistes de cgrp, medicaments contenant lesdits composes et procedes permettant de les preparer
MX2024004438A (es) Inhibidores de integrinas y usos de los mismos en combinacion con otros agentes.
JOP20230249A1 (ar) مثبطات أروماتية غير متجانسة ثنائية الحلقات لـ klk5
JP2007522159A5 (fr)
EP4599892A3 (fr) Dérivés d&#39;acide boronique et leurs utilisations thérapeutiques
CA2378834A1 (fr) Pyrazinones, compositions contenant ces composes
WO2024155965A3 (fr) Biomarqueurs destinés à être utilisés en thérapie par inhibiteur d&#39;intégrine
JP2019510834A5 (fr)
WO2024259310A3 (fr) Composés antagonistes de pcsk9 perméables passifs
DE4124409B4 (de) Pharmazeutische Zubereitungen
FI95348C (fi) Menetelmä suun kautta annettavan nestemäisen koostumuksen valmistamiseksi
WO2020096916A3 (fr) Inhibiteurs de désacétylase d&#39;histone utiles pour traiter ou prévenir une infection par le vih
CA2382548A1 (fr) Traitement de la migraine par administration d&#39;acide alpha-lipoique ou de derives de cet acide
WO2021216450A8 (fr) Formulations d&#39;antagoniste opioïde
MX2024002146A (es) Compuestos para el tratamiento de afecciones relacionadas con la actividad de pcsk9.
WO2024249254A3 (fr) Procédés d&#39;utilisation d&#39;inhibiteurs d&#39;apol1

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 2024824271

Country of ref document: EP

NENP Non-entry into the national phase

Ref country code: DE

ENP Entry into the national phase

Ref document number: 2024824271

Country of ref document: EP

Effective date: 20260115

ENP Entry into the national phase

Ref document number: 2024824271

Country of ref document: EP

Effective date: 20260115

ENP Entry into the national phase

Ref document number: 2024824271

Country of ref document: EP

Effective date: 20260115

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 24824271

Country of ref document: EP

Kind code of ref document: A2