WO2020141923A3 - 안전성이 향상된 피롤로벤조디아제핀 이량체 화합물 및 이의 용도 - Google Patents
안전성이 향상된 피롤로벤조디아제핀 이량체 화합물 및 이의 용도 Download PDFInfo
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- WO2020141923A3 WO2020141923A3 PCT/KR2020/000091 KR2020000091W WO2020141923A3 WO 2020141923 A3 WO2020141923 A3 WO 2020141923A3 KR 2020000091 W KR2020000091 W KR 2020000091W WO 2020141923 A3 WO2020141923 A3 WO 2020141923A3
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- WIPO (PCT)
- Prior art keywords
- dimer compound
- pyrrolobenzodiazepine dimer
- present
- drug
- ligand
- Prior art date
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- -1 Pyrrolobenzodiazepine dimer compound Chemical class 0.000 title abstract 4
- 239000003814 drug Substances 0.000 abstract 4
- 229940079593 drug Drugs 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 4
- 239000002246 antineoplastic agent Substances 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000001093 anti-cancer Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000008685 targeting Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 231100001274 therapeutic index Toxicity 0.000 abstract 1
- 230000001988 toxicity Effects 0.000 abstract 1
- 231100000419 toxicity Toxicity 0.000 abstract 1
- 239000003053 toxin Substances 0.000 abstract 1
- 231100000765 toxin Toxicity 0.000 abstract 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
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- 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
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- 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
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- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
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- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68035—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a pyrrolobenzodiazepine
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- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- A61K47/6855—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
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Abstract
본 발명은 신규한 피롤로벤조디아제핀 이량체 화합물 또는 이의 약학적으로 허용되는 염, 이의 리간드-약물 접합체 화합물, 이를 함유하는 조성물, 및 항암제로서의 이의 치료용도에 관한 것으로서, 본 발명에 따른 피롤로벤조디아제핀 이량체 화합물은 프리 톡신(free toxin) 형태에서는 활성이 떨어져 독성이 크게 감소하는 효과를 나타내면서도 리간드-약물 접합체에 약물로 적용되어 투여되는 경우 항암 활성이 기존 항암제 대비 동등 내지 우수한 것으로 나타났는바 치료지수(therapeutic index)가 현저히 향상되는 효과를 나타내며, 따라서 암과 같은 증식성 질환의 표적화, 특이적 치료, 약효의 극대화 및 부작용 발현의 최소화가 가능하다는 점에서 산업상 매우 유용하다.
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN202080008057.XA CN113260621A (zh) | 2019-01-03 | 2020-01-03 | 安全性得到提高的吡咯并苯并二氮杂二聚体化合物及其用途 |
JP2021538804A JP7542266B2 (ja) | 2019-01-03 | 2020-01-03 | 安定性が向上したピロロベンゾジアゼピン二量体化合物及びその用途 |
US17/420,007 US20220096641A1 (en) | 2019-01-03 | 2020-01-03 | Pyrrolobenzodiazepine dimer compound with improved safety and use thereof |
EP20735878.9A EP3907226A4 (en) | 2019-01-03 | 2020-01-03 | PYRROLOBENZODIAZEPINE DIMER COMPOUND WITH IMPROVED SAFETY AND USE THEREOF |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
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KR20190000514 | 2019-01-03 | ||
KR10-2019-0000514 | 2019-01-03 | ||
KR1020200000270A KR20200084802A (ko) | 2019-01-03 | 2020-01-02 | 안전성이 향상된 피롤로벤조디아제핀 이량체 화합물 및 이의 용도 |
KR10-2020-0000270 | 2020-01-02 |
Publications (3)
Publication Number | Publication Date |
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WO2020141923A2 WO2020141923A2 (ko) | 2020-07-09 |
WO2020141923A3 true WO2020141923A3 (ko) | 2020-10-29 |
WO2020141923A9 WO2020141923A9 (ko) | 2020-12-10 |
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PCT/KR2020/000091 WO2020141923A2 (ko) | 2019-01-03 | 2020-01-03 | 안전성이 향상된 피롤로벤조디아제핀 이량체 화합물 및 이의 용도 |
Country Status (4)
Country | Link |
---|---|
US (1) | US20220096641A1 (ko) |
JP (1) | JP7542266B2 (ko) |
KR (1) | KR102591073B1 (ko) |
WO (1) | WO2020141923A2 (ko) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2022187591A1 (en) | 2021-03-05 | 2022-09-09 | Go Therapeutics, Inc. | Anti-glyco-cd44 antibodies and their uses |
KR20240107093A (ko) | 2021-08-05 | 2024-07-08 | 고 테라퓨틱스, 인크. | 항-글리코-muc4 항체 및 그의 용도 |
EP4389152A1 (en) | 2022-12-23 | 2024-06-26 | Synaffix B.V. | Conjugates of pbd prodrugs |
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2020
- 2020-01-03 JP JP2021538804A patent/JP7542266B2/ja active Active
- 2020-01-03 US US17/420,007 patent/US20220096641A1/en active Pending
- 2020-01-03 WO PCT/KR2020/000091 patent/WO2020141923A2/ko unknown
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2022
- 2022-08-23 KR KR1020220105670A patent/KR102591073B1/ko active IP Right Grant
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WO2018069490A1 (en) * | 2016-10-14 | 2018-04-19 | Medimmune Limited | Pyrrolobenzodiazepine conjugates |
KR20180110645A (ko) * | 2017-03-29 | 2018-10-10 | 주식회사 레고켐 바이오사이언스 | 피롤로벤조디아제핀 이량체 전구체 및 이의 리간드-링커 접합체 화합물 |
WO2018192944A1 (en) * | 2017-04-18 | 2018-10-25 | Medimmune Limited | Pyrrolobenzodiazepine conjugates |
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US20220096641A1 (en) | 2022-03-31 |
KR20220122590A (ko) | 2022-09-02 |
JP2022516911A (ja) | 2022-03-03 |
WO2020141923A2 (ko) | 2020-07-09 |
KR102591073B1 (ko) | 2023-10-19 |
WO2020141923A9 (ko) | 2020-12-10 |
JP7542266B2 (ja) | 2024-08-30 |
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