EA202191244A1 - Новые цитостатические конъюгаты с лигандами интегрина - Google Patents
Новые цитостатические конъюгаты с лигандами интегринаInfo
- Publication number
- EA202191244A1 EA202191244A1 EA202191244A EA202191244A EA202191244A1 EA 202191244 A1 EA202191244 A1 EA 202191244A1 EA 202191244 A EA202191244 A EA 202191244A EA 202191244 A EA202191244 A EA 202191244A EA 202191244 A1 EA202191244 A1 EA 202191244A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- conjugates
- integrin ligands
- new cytostatic
- new
- cytostatic
- Prior art date
Links
- 239000000824 cytostatic agent Substances 0.000 title 1
- 230000001085 cytostatic effect Effects 0.000 title 1
- 102000006495 integrins Human genes 0.000 title 1
- 108010044426 integrins Proteins 0.000 title 1
- 239000003446 ligand Substances 0.000 title 1
- 239000002202 Polyethylene glycol Substances 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229920001223 polyethylene glycol Polymers 0.000 abstract 2
- 229940123038 Integrin antagonist Drugs 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000016387 Pancreatic elastase Human genes 0.000 abstract 1
- 108010067372 Pancreatic elastase Proteins 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 231100000433 cytotoxic Toxicity 0.000 abstract 1
- 230000001472 cytotoxic effect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000006850 spacer group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61K47/62—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
- 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
- A61K47/56—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
- 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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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 (1)
| Publication Number | Publication Date |
|---|---|
| EA202191244A1 true EA202191244A1 (ru) | 2021-10-11 |
Family
ID=64453279
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202191244A EA202191244A1 (ru) | 2018-11-05 | 2019-10-30 | Новые цитостатические конъюгаты с лигандами интегрина |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20210386864A1 (https=) |
| EP (1) | EP3876993A1 (https=) |
| JP (1) | JP7509768B2 (https=) |
| KR (1) | KR20210100607A (https=) |
| CN (1) | CN113260382B (https=) |
| AR (1) | AR116999A1 (https=) |
| AU (1) | AU2019376293A1 (https=) |
| BR (1) | BR112021008232A2 (https=) |
| CA (1) | CA3118041A1 (https=) |
| CL (1) | CL2021001142A1 (https=) |
| EA (1) | EA202191244A1 (https=) |
| IL (1) | IL282748B2 (https=) |
| MX (1) | MX2021005134A (https=) |
| SG (1) | SG11202104491SA (https=) |
| TW (1) | TW202039005A (https=) |
| WO (1) | WO2020094471A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2018102358A (ru) | 2015-06-23 | 2019-07-25 | Байер Фарма Акциенгезельшафт | Нацеленные конъюгаты ksp ингибиторов |
| WO2017216028A1 (en) | 2016-06-15 | 2017-12-21 | Bayer Pharma Aktiengesellschaft | Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies |
| JP7030811B2 (ja) | 2016-12-21 | 2022-03-07 | バイエル・ファルマ・アクティエンゲゼルシャフト | Ｋｓｐ阻害剤を有する特異的抗体－薬物コンジュゲート（ａｄｃ） |
| CA3047491A1 (en) | 2016-12-21 | 2018-06-28 | Bayer Aktiengesellschaft | Prodrugs of cytotoxic active agents having enzymatically cleavable groups |
| JP7066714B2 (ja) | 2016-12-21 | 2022-05-13 | バイエル・ファルマ・アクティエンゲゼルシャフト | 酵素的に切断可能な基を有する抗体薬物コンジュゲート（ａｄｃ） |
| KR20210100607A (ko) * | 2018-11-05 | 2021-08-17 | 바이엘 파마 악티엔게젤샤프트 | 인테그린 리간드를 갖는 세포증식억제 콘쥬게이트 |
| CN118556062A (zh) | 2021-10-04 | 2024-08-27 | 文赛克斯制药有限责任公司 | 用于治疗、预防或管理过度增殖病症的化合物、药物组合物和方法 |
| 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 |
| CN118354796A (zh) | 2021-10-04 | 2024-07-16 | 文赛克斯制药有限责任公司 | 用于治疗、预防或管理过度增殖病症的化合物、药物组合物和方法 |
| TW202434305A (zh) | 2022-11-17 | 2024-09-01 | 德商溫瑟克斯製藥公司 | 於腫瘤微環境中可裂解之抗體-藥物結合物 |
| EP4619037A1 (en) | 2022-11-17 | 2025-09-24 | Hans-Georg Lerchen | Small molecule-drug-conjugates cleavable in a tumor microenvironment |
| US20240376212A1 (en) * | 2023-04-25 | 2024-11-14 | Targetthera Llc | Alpha v-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 |
| EP0927045B1 (en) | 1996-09-10 | 2005-12-14 | The Burnham Institute | Tumor homing molecules, conjugates derived therefrom, and methods of using same |
| CA2370245A1 (en) | 1999-05-14 | 2000-11-23 | Boehringer Ingelheim Pharmaceuticals, Inc. | Enzyme-activated anti-tumor prodrug compounds |
| 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 |
| KR20210100607A (ko) * | 2018-11-05 | 2021-08-17 | 바이엘 파마 악티엔게젤샤프트 | 인테그린 리간드를 갖는 세포증식억제 콘쥬게이트 |
-
2019
- 2019-10-30 KR KR1020217015569A patent/KR20210100607A/ko not_active Ceased
- 2019-10-30 JP JP2021523599A patent/JP7509768B2/ja active Active
- 2019-10-30 US US17/290,911 patent/US20210386864A1/en not_active Abandoned
- 2019-10-30 CN CN201980087910.9A patent/CN113260382B/zh active Active
- 2019-10-30 AU AU2019376293A patent/AU2019376293A1/en not_active Abandoned
- 2019-10-30 BR BR112021008232-8A patent/BR112021008232A2/pt not_active Application Discontinuation
- 2019-10-30 SG SG11202104491SA patent/SG11202104491SA/en unknown
- 2019-10-30 CA CA3118041A patent/CA3118041A1/en active Pending
- 2019-10-30 IL IL282748A patent/IL282748B2/en unknown
- 2019-10-30 WO PCT/EP2019/079601 patent/WO2020094471A1/en not_active Ceased
- 2019-10-30 EP EP19791285.0A patent/EP3876993A1/en active Pending
- 2019-10-30 MX MX2021005134A patent/MX2021005134A/es unknown
- 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 |
|---|---|
| US20240325553A1 (en) | 2024-10-03 |
| WO2020094471A1 (en) | 2020-05-14 |
| IL282748A (en) | 2021-06-30 |
| JP2022506299A (ja) | 2022-01-17 |
| CA3118041A1 (en) | 2020-05-14 |
| JP7509768B2 (ja) | 2024-07-02 |
| CN113260382A (zh) | 2021-08-13 |
| BR112021008232A2 (pt) | 2021-08-03 |
| SG11202104491SA (en) | 2021-05-28 |
| CN113260382B (zh) | 2024-09-13 |
| TW202039005A (zh) | 2020-11-01 |
| KR20210100607A (ko) | 2021-08-17 |
| US20210386864A1 (en) | 2021-12-16 |
| EP3876993A1 (en) | 2021-09-15 |
| CL2021001142A1 (es) | 2021-11-12 |
| AR116999A1 (es) | 2021-06-30 |
| IL282748B2 (en) | 2025-07-01 |
| IL282748B1 (en) | 2025-03-01 |
| AU2019376293A1 (en) | 2021-06-03 |
| MX2021005134A (es) | 2021-07-07 |
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