IL282748B2 - Cytostatic conjugates with integrin ligands - Google Patents
Cytostatic conjugates with integrin ligandsInfo
- Publication number
- IL282748B2 IL282748B2 IL282748A IL28274821A IL282748B2 IL 282748 B2 IL282748 B2 IL 282748B2 IL 282748 A IL282748 A IL 282748A IL 28274821 A IL28274821 A IL 28274821A IL 282748 B2 IL282748 B2 IL 282748B2
- Authority
- IL
- Israel
- Prior art keywords
- compound
- solvate
- salt
- acid
- pharmaceutically acceptable
- Prior art date
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
- A61K31/435—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
-
- 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
- A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18204423 | 2018-11-05 | ||
| PCT/EP2019/079601 WO2020094471A1 (en) | 2018-11-05 | 2019-10-30 | Cytostatic conjugates with integrin ligands |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| IL282748A IL282748A (en) | 2021-06-30 |
| IL282748B1 IL282748B1 (en) | 2025-03-01 |
| IL282748B2 true IL282748B2 (en) | 2025-07-01 |
Family
ID=64453279
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL282748A IL282748B2 (en) | 2018-11-05 | 2019-10-30 | Cytostatic conjugates with integrin ligands |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20210386864A1 (enExample) |
| EP (1) | EP3876993A1 (enExample) |
| JP (1) | JP7509768B2 (enExample) |
| KR (1) | KR20210100607A (enExample) |
| CN (1) | CN113260382B (enExample) |
| AR (1) | AR116999A1 (enExample) |
| AU (1) | AU2019376293A1 (enExample) |
| BR (1) | BR112021008232A2 (enExample) |
| CA (1) | CA3118041A1 (enExample) |
| CL (1) | CL2021001142A1 (enExample) |
| EA (1) | EA202191244A1 (enExample) |
| IL (1) | IL282748B2 (enExample) |
| MX (1) | MX2021005134A (enExample) |
| SG (1) | SG11202104491SA (enExample) |
| TW (1) | TW202039005A (enExample) |
| WO (1) | WO2020094471A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2017017138A (es) | 2015-06-23 | 2018-04-30 | Bayer Pharma AG | Conjugados homogeneos especificos de sitio con inhibidores de ksp. |
| WO2017216028A1 (en) | 2016-06-15 | 2017-12-21 | Bayer Pharma Aktiengesellschaft | Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies |
| AU2017380871C1 (en) | 2016-12-21 | 2025-05-15 | Bayer Aktiengesellschaft | Antibody drug conjugates (ADCs) having enzymatically cleavable groups |
| US12059472B2 (en) | 2016-12-21 | 2024-08-13 | Bayer Aktiengesellschaft | Prodrugs of cytotoxic active agents having enzymatically cleavable groups |
| US11433140B2 (en) | 2016-12-21 | 2022-09-06 | Bayer Pharma Aktiengesellschaft | Specific antibody drug conjugates (ADCs) having KSP inhibitors |
| MX2021005134A (es) * | 2018-11-05 | 2021-07-07 | Bayer Pharma AG | Nuevos conjugados citostaticos con ligandos de integrina. |
| EP4413006A1 (en) | 2021-10-04 | 2024-08-14 | Vincerx Pharma GmbH | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders |
| EP4412656A1 (en) | 2021-10-04 | 2024-08-14 | Vincerx Pharma GmbH | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorders |
| US20240408222A1 (en) | 2021-10-04 | 2024-12-12 | Vincerx Pharma Gmbh | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorder |
| WO2024105206A1 (en) | 2022-11-17 | 2024-05-23 | Vincerx Pharma Gmbh | Antibody-drug-conjugates cleavable in a tumor microenvironment |
| 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 |
| US12624109B2 (en) * | 2023-04-25 | 2026-05-12 | Targetthera Llc | αv-integrin targeted small molecule drug conjugates |
| CN119143798B (zh) * | 2024-08-01 | 2025-09-30 | 河北医科大学 | 一种骨靶向阿仑膦酸-普萘洛尔及其制备方法与应用 |
Family Cites Families (12)
| 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 |
| WO1998010795A2 (en) | 1996-09-10 | 1998-03-19 | The Burnham Institute | Tumor homing molecules, conjugates derived therefrom, and methods of using same |
| MXPA01011502A (es) | 1999-05-14 | 2003-08-20 | Boehringer Ingelheim Pharma | Compuestos de tipo profarmaco anti-tumorigenos, activados por enzimas. |
| EP1238678A1 (en) | 2001-03-08 | 2002-09-11 | Bayer Aktiengesellschaft | Enzyme-activated cytostatic conjugates with integrin ligands |
| TW201004647A (en) | 2008-05-20 | 2010-02-01 | Sigma Tau Ind Farmaceuti | Novel dual targeting antitumoural conjugates |
| MX2021005134A (es) * | 2018-11-05 | 2021-07-07 | Bayer Pharma AG | Nuevos conjugados citostaticos con ligandos de integrina. |
-
2019
- 2019-10-30 MX MX2021005134A patent/MX2021005134A/es unknown
- 2019-10-30 CN CN201980087910.9A patent/CN113260382B/zh active Active
- 2019-10-30 KR KR1020217015569A patent/KR20210100607A/ko not_active Ceased
- 2019-10-30 US US17/290,911 patent/US20210386864A1/en not_active Abandoned
- 2019-10-30 BR BR112021008232-8A patent/BR112021008232A2/pt not_active Application Discontinuation
- 2019-10-30 JP JP2021523599A patent/JP7509768B2/ja active Active
- 2019-10-30 AU AU2019376293A patent/AU2019376293A1/en not_active Abandoned
- 2019-10-30 IL IL282748A patent/IL282748B2/en unknown
- 2019-10-30 CA CA3118041A patent/CA3118041A1/en active Pending
- 2019-10-30 SG SG11202104491SA patent/SG11202104491SA/en unknown
- 2019-10-30 EP EP19791285.0A patent/EP3876993A1/en active Pending
- 2019-10-30 WO PCT/EP2019/079601 patent/WO2020094471A1/en not_active Ceased
- 2019-10-30 EA EA202191244A patent/EA202191244A1/ru unknown
- 2019-11-01 TW TW108139645A patent/TW202039005A/zh unknown
- 2019-11-06 AR ARP190103243A patent/AR116999A1/es not_active Application Discontinuation
-
2021
- 2021-04-30 CL CL2021001142A patent/CL2021001142A1/es unknown
-
2024
- 2024-06-14 US US18/744,084 patent/US20240325553A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020094471A1 (en) | 2020-05-14 |
| CN113260382B (zh) | 2024-09-13 |
| BR112021008232A2 (pt) | 2021-08-03 |
| TW202039005A (zh) | 2020-11-01 |
| EP3876993A1 (en) | 2021-09-15 |
| EA202191244A1 (ru) | 2021-10-11 |
| KR20210100607A (ko) | 2021-08-17 |
| AU2019376293A1 (en) | 2021-06-03 |
| US20210386864A1 (en) | 2021-12-16 |
| IL282748A (en) | 2021-06-30 |
| IL282748B1 (en) | 2025-03-01 |
| SG11202104491SA (en) | 2021-05-28 |
| JP7509768B2 (ja) | 2024-07-02 |
| MX2021005134A (es) | 2021-07-07 |
| JP2022506299A (ja) | 2022-01-17 |
| AR116999A1 (es) | 2021-06-30 |
| CA3118041A1 (en) | 2020-05-14 |
| CN113260382A (zh) | 2021-08-13 |
| US20240325553A1 (en) | 2024-10-03 |
| CL2021001142A1 (es) | 2021-11-12 |
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