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AR127245A1 - Compuestos, composiciones farmacéuticas y métodos para el tratamiento, prevención o manejo de trastornos hiperproliferativos - Google Patents

Compuestos, composiciones farmacéuticas y métodos para el tratamiento, prevención o manejo de trastornos hiperproliferativos

Info

Publication number
AR127245A1
AR127245A1 ARP220102680A ARP220102680A AR127245A1 AR 127245 A1 AR127245 A1 AR 127245A1 AR P220102680 A ARP220102680 A AR P220102680A AR P220102680 A ARP220102680 A AR P220102680A AR 127245 A1 AR127245 A1 AR 127245A1
Authority
AR
Argentina
Prior art keywords
pharmaceutically acceptable
asn
ala
compound
acceptable salt
Prior art date
Application number
ARP220102680A
Other languages
English (en)
Inventor
Hans Lerchen
- Stelte-Ludwig Beatrix Georg
Mareike Wiedmann
Anne Rebstock
- Koebberling Johannes Sophie
Harvey Wong
Original Assignee
Vincerx Pharma Gmbh
Vincerx Pharma Inc
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 Vincerx Pharma Gmbh, Vincerx Pharma Inc filed Critical Vincerx Pharma Gmbh
Publication of AR127245A1 publication Critical patent/AR127245A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

En el presente documento, se divulgan compuestos, composiciones farmacéuticas y métodos para el tratamiento, prevención o manejo de enfermedades y afecciones que incluyen trastornos hiperproliferativos tales como el cáncer en humanos y otros mamíferos. Los compuestos divulgados en el presente documento son profármacos de inhibidores de topoisomerasa, conjugados a una porción de unión a integrinas mediante conectores de escisión y/o espaciadores funcionales. Reivindicación 1: Un compuesto, o una sal farmacéuticamente aceptable de este, caracterizado porque comprende un ligando hexacíclico citotóxico o citostático (CT) conjugado con uno o más aglutinantes de integrina (IN) a través de un conector. Reivindicación 22: Un compuesto, o una sal farmacéuticamente aceptable de este, o un estereoisómero o mezcla de estereoisómeros de este, de la fórmula (X) caracterizado porque: XC es un enlace, (-L-Asn-)-, (-L-Asp)-(L-Pro)-(L-Val-)-, (-L-Asn)-(L-Pro)-(L-Val-)-, (-L-Ala)-(L-Ala)-(L-Asn-)- o (-L-Ala)-(L-N-Me-Ala)-(L-Asn-)-. Reivindicación 26: Una composición farmacéutica caracterizado porque comprende el compuesto de una cualquiera de las reivindicaciones 1 - 25, o una de sus sales farmacéuticamente aceptables; o un estereoisómero o mezcla de estereoisómeros de este; y un excipiente farmacéuticamente aceptable. Reivindicación 50: Un método para tratar una enfermedad o trastorno en un sujeto, caracterizado porque comprende administrar al sujeto una cantidad terapéuticamente eficaz de un compuesto de cualquiera de las reivindicaciones 1 - 24, o una sal farmacéuticamente aceptable de este, o un estereoisómero o mezcla de estereoisómeros de este.
ARP220102680A 2021-10-04 2022-10-04 Compuestos, composiciones farmacéuticas y métodos para el tratamiento, prevención o manejo de trastornos hiperproliferativos AR127245A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202163252122P 2021-10-04 2021-10-04

Publications (1)

Publication Number Publication Date
AR127245A1 true AR127245A1 (es) 2024-01-03

Family

ID=84359901

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP220102680A AR127245A1 (es) 2021-10-04 2022-10-04 Compuestos, composiciones farmacéuticas y métodos para el tratamiento, prevención o manejo de trastornos hiperproliferativos

Country Status (8)

Country Link
US (1) US20250032477A1 (es)
EP (1) EP4412656A1 (es)
JP (1) JP2024536628A (es)
KR (1) KR20240089138A (es)
CN (1) CN118354796A (es)
AR (1) AR127245A1 (es)
TW (1) TW202330539A (es)
WO (1) WO2023057814A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202430150A (zh) * 2022-11-17 2024-08-01 德商溫瑟克斯製藥公司 在腫瘤微環境中可裂解之小分子藥物結合物
CN117417346B (zh) * 2023-09-11 2025-07-25 常州合全药业有限公司 喜树碱类衍生物的制备方法
CN117417347A (zh) * 2023-09-28 2024-01-19 杭州爱科瑞思生物医药有限公司 卤素取代的依沙替康的酰胺衍生物及其制备方法和应用

Family Cites Families (14)

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GB8705477D0 (en) 1987-03-09 1987-04-15 Carlton Med Prod Drug delivery systems
US4975278A (en) 1988-02-26 1990-12-04 Bristol-Myers Company Antibody-enzyme conjugates in combination with prodrugs for the delivery of cytotoxic agents to tumor cells
US4943579A (en) 1987-10-06 1990-07-24 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Water soluble prodrugs of camptothecin
FR2676058B1 (fr) 1991-04-30 1994-02-25 Hoechst Lab Prodrogues glycosylees, leur procede de preparation et leur utilisation dans le traitement des cancers.
DE4229903A1 (de) 1992-09-08 1994-03-10 Bayer Ag Neue Acetale von Ketophosphamid und Alkylglycosiden
DE4236237A1 (de) 1992-10-27 1994-04-28 Behringwerke Ag Prodrugs, ihre Herstellung und Verwendung als Arzneimittel
US5646159A (en) 1994-07-20 1997-07-08 Research Triangle Institute Water-soluble esters of camptothecin compounds
AU4412297A (en) 1996-09-10 1998-04-02 Burnham Institute, The Tumor homing molecules, conjugates derived therefrom, and methods of using sa me
WO2000069472A2 (en) 1999-05-14 2000-11-23 Boehringer Ingelheim Pharmaceuticals, Inc. Enzyme-activated anti-tumor prodrug compounds
DE60042700D1 (de) * 1999-09-08 2009-09-17 Markus Albers Integrin-vermittelte arzneimittel-zielrichtung
EP1238678A1 (en) 2001-03-08 2002-09-11 Bayer Aktiengesellschaft Enzyme-activated cytostatic conjugates with integrin ligands
EP4406606A3 (de) 2015-06-22 2024-10-09 Bayer Pharma Aktiengesellschaft Binder-wirkstoff-konjugate (adcs) und binder-prodrug-konjugate (apdcs) mit enzymatisch spaltbaren g
JP7509768B2 (ja) 2018-11-05 2024-07-02 バイエル ファーマ アクチェンゲゼルシャフト インテグリンリガンドを有する新規な細胞増殖抑制コンジュゲート
WO2021052402A1 (zh) * 2019-09-18 2021-03-25 四川百利药业有限责任公司 一种喜树碱衍生物及其偶联物

Also Published As

Publication number Publication date
KR20240089138A (ko) 2024-06-20
WO2023057814A1 (en) 2023-04-13
CN118354796A (zh) 2024-07-16
JP2024536628A (ja) 2024-10-04
EP4412656A1 (en) 2024-08-14
US20250032477A1 (en) 2025-01-30
TW202330539A (zh) 2023-08-01

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