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 hiperproliferativosInfo
- 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
Links
Classifications
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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
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/54—Medicinal 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
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/54—Medicinal 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
- A61K47/55—Medicinal 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/62—Medicinal 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
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs 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.
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)
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
-
2022
- 2022-10-03 EP EP22805949.9A patent/EP4412656A1/en not_active Withdrawn
- 2022-10-03 CN CN202280079665.9A patent/CN118354796A/zh active Pending
- 2022-10-03 JP JP2024543593A patent/JP2024536628A/ja active Pending
- 2022-10-03 KR KR1020247014133A patent/KR20240089138A/ko active Pending
- 2022-10-03 WO PCT/IB2022/000566 patent/WO2023057814A1/en not_active Ceased
- 2022-10-03 US US18/698,341 patent/US20250032477A1/en not_active Abandoned
- 2022-10-04 AR ARP220102680A patent/AR127245A1/es not_active Application Discontinuation
- 2022-10-04 TW TW111137732A patent/TW202330539A/zh unknown
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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |