FI3727461T3 - EPHA2:lle spesifisiä bisyklisiä peptidiligandeja - Google Patents
EPHA2:lle spesifisiä bisyklisiä peptidiligandejaInfo
- Publication number
- FI3727461T3 FI3727461T3 FIEP18829926.7T FI18829926T FI3727461T3 FI 3727461 T3 FI3727461 T3 FI 3727461T3 FI 18829926 T FI18829926 T FI 18829926T FI 3727461 T3 FI3727461 T3 FI 3727461T3
- Authority
- FI
- Finland
- Prior art keywords
- compound
- cancer
- pharmaceutical composition
- seq
- harg
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/10—Peptides having 12 to 20 amino acids
-
- 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
-
- 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
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
-
- 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
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
- A61K47/6415—Toxins or lectins, e.g. clostridial toxins or Pseudomonas exotoxins
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (10)
1. Yhdiste, joka yhdiste on BCY6136 tai sen farmaseuttisesti hyväksyttävä suola, jolloin mainitulla yhdisteellä BCY6136 on rakenne: DN Oa N ; NOT Lb aN 02 0E meveom o Y ux SNE AN ON SÅN BOYSOGG vo Hoi o + H AN BDCYS136 HN YO — jolloin BCY6099 on sekvenssin SEQ ID NO: 2 mukainen polypeptidi (B-Ala)-Sari0-A(HArg)D-Ci(HyP)LVNPLCiiLHP(D-Asp)W(HArg)Cii (SEQ ID NO: 2) jolloin Sar on sarkosiini, HArg on homoarginiini ja HyP on hydroksiproliini; jolloin sekvenssin SEQ ID NO: 2 mukainen polypeptidi on syklisoitu Ci:ssä, Cii:ssä ja Cii:ssä 1,1’,1”-(1,3,5-triatsinaani-1,3,5-triyyli)triprop-2-en-1-onilla (TATA).
2. Patenttivaatimuksen 1 mukainen yhdiste, jolloin sekvenssi SEO ID NO: 2 on amidoitu C-terminuksessa.
3. Patenttivaatimuksen 1 tai 2 mukainen yhdiste, jolloin farmaseuttisesti hyväksyttävä suola on valittu vapaasta haposta tai natrium-, kalium-, kalsium- tai ammoniumsuolasta.
4. Farmaseuttinen koostumus, joka käsittää jonkin patenttivaatimuksista 1-3 mukaista yhdistettä yhdessä yhden tai useamman farmaseuttisesti hyväksyttävän apuaineen kanssa.
5. Jonkin patenttivaatimuksista 1-3 mukainen yhdiste tai patenttivaatimuksen 4 mukainen farmaseuttinen koostumus käytettäväksi sellaisen sairauden tai häiriön — ehkäisyyn, tukahduttamiseen tai hoitoon, jolle on ominaista EphAZ2:n likailmentyminen sairaassa kudoksessa.
6. Jonkin patenttivaatimuksista 1-3 mukainen yhdiste tai patenttivaatimuksen 4 mukainen farmaseuttinen koostumus käytettäväksi menetelmässä syövän ehkäisemiseksi, tukahduttamiseksi tai hoitamiseksi.
7. Yhdiste — käytettäväksi tai farmaseuttinen koostumus käytettäväksi patenttivaatimuksen 5 mukaisesti, jolloin sairaus tai häiriö on syöpä.
8. Patenttivaatimuksen 6 tai / mukainen yhdiste tai farmaseuttinen koostumus, jossa syöpä on valittu eturauhassyövän, keuhkosyövän, rintasyövän, mahasyövän, —munasarjasyövän, ruokatorven syövän, multippeli myelooman ja fibrosarkooman joukosta.
9. Yhdiste — käytettäväksi tai farmaseuttinen koostumus käytettäväksi patenttivaatimuksen 8 mukaisesti, jolloin keuhkosyöpä on ei-pienisoluinen keuhkokarsinooma (NSCLC) ja/tai jolloin rintasyöpä on kolmoisnegatiivinen — rintasyöpä
10. — Jonkin patenttivaatimuksista 1-3 mukainen yhdiste tai patenttivaatimuksen 4 mukainen farmaseuttinen koostumus käytettäväksi menetelmässä syövän ehkäisemiseksi, tukahduttamiseksi tai hoitamiseksi sitä tarvitsevalla potilaalla, jolloin mainitulla potilaalla on tunnistettu EphA2:n lisääntynyt kopiomäärän variaatio (CNV).
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1721259.8A GB201721259D0 (en) | 2017-12-19 | 2017-12-19 | Bicyclic peptide ligands specific for EphA2 |
| GBGB1804102.0A GB201804102D0 (en) | 2018-03-14 | 2018-03-14 | Bicycle peptide ligands specific for EphA2 |
| GBGB1818603.1A GB201818603D0 (en) | 2018-11-14 | 2018-11-14 | Bicyclic peptide ligands specific for epha2 |
| PCT/GB2018/053678 WO2019122863A1 (en) | 2017-12-19 | 2018-12-19 | Bicyclic peptide ligands specific for epha2 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI3727461T3 true FI3727461T3 (fi) | 2025-08-15 |
Family
ID=64902125
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP22161978.6T FI4053145T3 (fi) | 2017-12-19 | 2018-12-19 | EphA2:lle spesifisiä peptidiligandeja |
| FIEP18829926.7T FI3727461T3 (fi) | 2017-12-19 | 2018-12-19 | EPHA2:lle spesifisiä bisyklisiä peptidiligandeja |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP22161978.6T FI4053145T3 (fi) | 2017-12-19 | 2018-12-19 | EphA2:lle spesifisiä peptidiligandeja |
Country Status (27)
| Country | Link |
|---|---|
| US (5) | US11484602B2 (fi) |
| EP (4) | EP3727460B1 (fi) |
| JP (4) | JP7293231B2 (fi) |
| KR (2) | KR102791088B1 (fi) |
| CN (4) | CN111741771B (fi) |
| AU (3) | AU2018387417C9 (fi) |
| BR (2) | BR112020012349A2 (fi) |
| CA (2) | CA3085253A1 (fi) |
| CY (1) | CY1125367T1 (fi) |
| DK (3) | DK4053145T3 (fi) |
| ES (3) | ES2922632T3 (fi) |
| FI (2) | FI4053145T3 (fi) |
| HR (2) | HRP20220871T1 (fi) |
| HU (1) | HUE059126T2 (fi) |
| IL (3) | IL321490A (fi) |
| LT (2) | LT3727460T (fi) |
| MX (2) | MX2020006474A (fi) |
| PH (1) | PH12020550929A1 (fi) |
| PL (3) | PL3727461T3 (fi) |
| PT (3) | PT4053145T (fi) |
| RS (1) | RS67248B1 (fi) |
| SA (1) | SA520412268B1 (fi) |
| SG (2) | SG11202005494QA (fi) |
| SI (2) | SI3727461T1 (fi) |
| SM (1) | SMT202500312T1 (fi) |
| TW (1) | TWI825046B (fi) |
| WO (2) | WO2019122860A1 (fi) |
Families Citing this family (35)
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|---|---|---|---|---|
| US10532106B2 (en) | 2014-10-29 | 2020-01-14 | Bicyclerd Limited | Bicyclic peptide ligands specific for MT1-MMP |
| GB201607827D0 (en) | 2016-05-04 | 2016-06-15 | Bicycle Therapeutics Ltd | Bicyclic peptide-toxin conjugates specific for MT1-MMP |
| JP2020502238A (ja) | 2016-12-23 | 2020-01-23 | バイスクルアールディー・リミテッド | 新規連結構造を有するペプチド誘導体 |
| WO2019002842A1 (en) | 2017-06-26 | 2019-01-03 | Bicyclerd Limited | BICYCLIC PEPTIDE LIGANDS WITH DETECTABLE FRACTIONS AND USES THEREOF |
| CN111183147B (zh) | 2017-08-04 | 2024-07-05 | 拜斯科技术开发有限公司 | Cd137特异性的双环肽配体 |
| GB201721265D0 (en) | 2017-12-19 | 2018-01-31 | Bicyclerd Ltd | Bicyclic peptide ligands specific for EphA2 |
| TWI825046B (zh) | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
| JP2021514953A (ja) | 2018-02-23 | 2021-06-17 | バイスクルテクス・リミテッド | 多量体二環式ペプチドリガンド |
| KR20200139236A (ko) | 2018-04-04 | 2020-12-11 | 바이사이클티엑스 리미티드 | 헤테로탠덤 비사이클릭 펩티드 복합체 |
| US11180531B2 (en) | 2018-06-22 | 2021-11-23 | Bicycletx Limited | Bicyclic peptide ligands specific for Nectin-4 |
| GB201810316D0 (en) | 2018-06-22 | 2018-08-08 | Bicyclerd Ltd | Peptide ligands for binding to EphA2 |
| GB201820288D0 (en) | 2018-12-13 | 2019-01-30 | Bicycle Tx Ltd | Bicycle peptide ligaands specific for MT1-MMP |
| GB201820325D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for psma |
| GB201820295D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for MT1-MMP |
| WO2020128526A1 (en) | 2018-12-21 | 2020-06-25 | Bicycletx Limited | Bicyclic peptide ligands specific for pd-l1 |
| JP2022528887A (ja) * | 2019-04-02 | 2022-06-16 | バイスクルテクス・リミテッド | バイシクルトキシンコンジュゲートおよびその使用 |
| CN113811541A (zh) | 2019-05-09 | 2021-12-17 | 拜斯科技术开发有限公司 | Ox40特异性的双环肽配体 |
| TWI862640B (zh) * | 2019-07-30 | 2024-11-21 | 英商拜西可泰克斯有限公司 | 異質雙環肽複合物 |
| JP2022544246A (ja) * | 2019-08-13 | 2022-10-17 | バイスクルテクス・リミテッド | 修飾された多量体二環式ペプチドリガンド |
| PL4464721T3 (pl) * | 2019-10-03 | 2025-08-25 | Bicycletx Limited | Heterotandemowe kompleksy peptydów bicyklicznych |
| IL293200A (en) * | 2019-11-27 | 2022-07-01 | Bicycletx Ltd | Bicyclic peptide ligands specific for epha2 and uses thereof |
| IL298382A (en) * | 2020-05-20 | 2023-01-01 | Bicycletx Ltd | Nectin-4-specific bicyclic peptide ligands and their uses |
| IL298868A (en) | 2020-06-12 | 2023-02-01 | Bicycletx Ltd | Treatment of diseases characterized by overexpression of erythropoietin-producing hepatocellular receptor a2 (epha2) |
| US20220031858A1 (en) * | 2020-08-03 | 2022-02-03 | Bicycle TX Limited | Novel linkers |
| US20240197897A1 (en) | 2021-01-08 | 2024-06-20 | Bicycle TX Limited | Heterotandem bicyclic peptide complexes |
| US20250186539A2 (en) | 2021-01-11 | 2025-06-12 | Bicycletx Limited | Methods for treating cancer |
| EP4349857A4 (en) | 2021-05-25 | 2025-06-11 | Vaxcell-Bio | Monobody-based chimeric antigen receptor and immune cell including same |
| US20250121076A1 (en) * | 2021-08-17 | 2025-04-17 | Medshine Discovery Inc. | Polypeptide drug conjugate having novel structure and application thereof |
| JP2024537396A (ja) * | 2021-10-14 | 2024-10-10 | シーザン ハイスーク ファーマシューティカル カンパニー リミテッド | EphA2の二環式ペプチドリガンド及びそのコンジュゲート |
| KR20230140746A (ko) * | 2022-03-30 | 2023-10-10 | 연세대학교 산학협력단 | 암전이의 검출용 신규 바이오마커 |
| CN116063379B (zh) * | 2022-08-23 | 2025-05-02 | 中国药科大学 | EphA2靶向多肽及其应用 |
| CN120835795A (zh) | 2023-03-09 | 2025-10-24 | 拜斯科技术开发有限公司 | 双环毒素偶联物及其中间体的合成 |
| WO2024261490A1 (en) | 2023-06-23 | 2024-12-26 | Bicycletx Limited | Bicyclic peptide ligands specific for nk cells |
| WO2025191096A1 (en) * | 2024-03-14 | 2025-09-18 | Bicycletx Limited | Bicyclic peptide |
| CN119874840B (zh) * | 2025-03-31 | 2025-08-08 | 晶核生物医药科技(上海)有限公司 | 一种双环肽及其应用 |
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