EA034950B1 - Производные майтанзиноида, их конъюгаты и способы использования - Google Patents
Производные майтанзиноида, их конъюгаты и способы использования Download PDFInfo
- Publication number
- EA034950B1 EA034950B1 EA201700464A EA201700464A EA034950B1 EA 034950 B1 EA034950 B1 EA 034950B1 EA 201700464 A EA201700464 A EA 201700464A EA 201700464 A EA201700464 A EA 201700464A EA 034950 B1 EA034950 B1 EA 034950B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compound
- antibody
- implementations
- formula
- integer
- Prior art date
Links
- 0 CCC(C)(*)C(CCCCC(N[C@@](C(C)C)C(NC1(C(CCNC(N)=O)C1)C(Nc1cc(O)ccc1C(N(C[C@@]1(C[C@](C[C@]([C@@](C=CC=C(C)Cc(cc2OC)cc(N(C)C(C3)=O)c2Cl)OC)(N2)O)OC2=O)O[C@@]1(C)[C@]3O1)[C@@](C)C1=O)=O)=O)=O)=O)=O Chemical compound CCC(C)(*)C(CCCCC(N[C@@](C(C)C)C(NC1(C(CCNC(N)=O)C1)C(Nc1cc(O)ccc1C(N(C[C@@]1(C[C@](C[C@]([C@@](C=CC=C(C)Cc(cc2OC)cc(N(C)C(C3)=O)c2Cl)OC)(N2)O)OC2=O)O[C@@]1(C)[C@]3O1)[C@@](C)C1=O)=O)=O)=O)=O)=O 0.000 description 3
- BYRGDWLRLNGTCP-HWQNMXLQSA-N CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(Nc(ccc(C(N(C)[C@@H](C)C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C1)(N2)O)OC)cc3OC)c3Cl)=O)[C@]3(C)O[C@H]3C[C@H]1OC2=O)=O)=O)c1)c1N1CCOCC1)=O)=O)NC(NCCCCN(C(C=C1)=O)C1=O)=S Chemical compound CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(Nc(ccc(C(N(C)[C@@H](C)C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C1)(N2)O)OC)cc3OC)c3Cl)=O)[C@]3(C)O[C@H]3C[C@H]1OC2=O)=O)=O)c1)c1N1CCOCC1)=O)=O)NC(NCCCCN(C(C=C1)=O)C1=O)=S BYRGDWLRLNGTCP-HWQNMXLQSA-N 0.000 description 1
- PTMNMZKKROUAPP-HHGNYWQVSA-N CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(Nc1ccccc1C(N(C)[C@@H](C)C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C1)(N2)O)OC)cc3OC)c3Cl)=O)[C@]3(C)O[C@H]3C[C@H]1OC2=O)=O)=O)=O)=O)NC(NCCOCCOCCC(ON(C(CC1)=O)C1=O)=O)=S Chemical compound CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(Nc1ccccc1C(N(C)[C@@H](C)C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C1)(N2)O)OC)cc3OC)c3Cl)=O)[C@]3(C)O[C@H]3C[C@H]1OC2=O)=O)=O)=O)=O)NC(NCCOCCOCCC(ON(C(CC1)=O)C1=O)=O)=S PTMNMZKKROUAPP-HHGNYWQVSA-N 0.000 description 1
- ORAIJESRWGDJHB-XLDUQJBBSA-N CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(Nc1ccccc1C(N(C)[C@@H](C)C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C[C@H](C)C1)(NC(O)=O)O)OC)cc2OC)c2Cl)=O)[C@@H](C)[C@H]1O)=O)=O)=O)=O)NC(NCCCCN(C(C=C1)=O)C1=O)=S Chemical compound CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(Nc1ccccc1C(N(C)[C@@H](C)C(O[C@@H](CC(N(C)c(cc(C/C(/C)=C/C=C/[C@H]([C@@](C[C@H](C)C1)(NC(O)=O)O)OC)cc2OC)c2Cl)=O)[C@@H](C)[C@H]1O)=O)=O)=O)=O)NC(NCCCCN(C(C=C1)=O)C1=O)=S ORAIJESRWGDJHB-XLDUQJBBSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- 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
- 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
- A61K47/68—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
- A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
-
- 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
- A61K47/68—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
- A61K47/6849—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 receptor, a cell surface antigen or a cell surface determinant
-
- 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
- A61K47/68—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
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Cell Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562139044P | 2015-03-27 | 2015-03-27 | |
| US201562252239P | 2015-11-06 | 2015-11-06 | |
| PCT/US2016/024343 WO2016160615A1 (en) | 2015-03-27 | 2016-03-25 | Maytansinoid derivatives, conjugates thereof, and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201700464A1 EA201700464A1 (ru) | 2018-11-30 |
| EA034950B1 true EA034950B1 (ru) | 2020-04-09 |
Family
ID=55650789
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201700464A EA034950B1 (ru) | 2015-03-27 | 2016-03-25 | Производные майтанзиноида, их конъюгаты и способы использования |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US20160375147A1 (enExample) |
| EP (1) | EP3273998B1 (enExample) |
| JP (2) | JP6948950B2 (enExample) |
| KR (2) | KR20240142591A (enExample) |
| CN (2) | CN107995912A (enExample) |
| AU (1) | AU2016243527B2 (enExample) |
| BR (1) | BR112017020149A8 (enExample) |
| CA (1) | CA2978340C (enExample) |
| CL (1) | CL2017002422A1 (enExample) |
| CO (1) | CO2017010890A2 (enExample) |
| EA (1) | EA034950B1 (enExample) |
| IL (1) | IL254267B (enExample) |
| MX (2) | MX386328B (enExample) |
| PH (1) | PH12017501780A1 (enExample) |
| SG (1) | SG11201707148PA (enExample) |
| WO (1) | WO2016160615A1 (enExample) |
| ZA (1) | ZA201706040B (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015022585B1 (pt) | 2013-03-15 | 2023-04-04 | Regeneron Pharmaceuticals, Inc | Composto, composição farmacêutica, conjugado droga-anticorpo, e, uso dos mesmos |
| JP6608823B2 (ja) | 2013-08-26 | 2019-11-20 | レゲネロン ファーマシューティカルス，インコーポレーテッド | マクロライドジアステレオマーを含む医薬組成物、その合成方法、及び治療上の使用 |
| KR20240142591A (ko) | 2015-03-27 | 2024-09-30 | 리제너론 파아마슈티컬스, 인크. | 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법 |
| EP3310800B1 (en) | 2015-06-19 | 2021-11-17 | Centurion BioPharma Corporation | Delivery systems for controlled drug release |
| JP6993958B2 (ja) | 2015-07-06 | 2022-02-04 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | 多重特異性抗原結合分子およびその使用 |
| AU2017211120C1 (en) | 2016-01-25 | 2021-10-07 | Regeneron Pharmaceuticals, Inc. | Maytansinoid derivatives, conjugates thereof, and methods of use |
| EP3448891A1 (en) | 2016-04-28 | 2019-03-06 | Regeneron Pharmaceuticals, Inc. | Methods of making multispecific antigen-binding molecules |
| MY199468A (en) | 2016-09-23 | 2023-10-31 | Regeneron Pharma | Anti-steap2 antibodies, antibody-drug conjugates, and bispecific antigen-binding molecules that bind steap2 and cd3, and uses thereof |
| PT3515946T (pt) | 2016-09-23 | 2022-08-04 | Regeneron Pharma | Anticorpos anti-muc16 (mucin 16) |
| TWI782930B (zh) | 2016-11-16 | 2022-11-11 | 美商再生元醫藥公司 | 抗ｍｅｔ抗體，結合ｍｅｔ之雙特異性抗原結合分子及其使用方法 |
| MX2019006131A (es) | 2016-11-29 | 2019-08-21 | Regeneron Pharma | Metodos para tratar cancer de mama positivo para prlr. |
| CN110944718A (zh) | 2017-05-18 | 2020-03-31 | 里珍纳龙药品有限公司 | 环糊精蛋白质药物偶联物 |
| MA50546A (fr) | 2017-06-07 | 2020-09-16 | Regeneron Pharma | Compositions et méthodes pour l'internalisation d'enzymes |
| CA3080857A1 (en) | 2017-11-07 | 2019-05-16 | Regeneron Pharmaceuticals, Inc. | Hydrophilic linkers for antibody drug conjugates |
| US11572373B2 (en) * | 2017-11-30 | 2023-02-07 | Ladrx Corporation | Maytansinoid-based drug delivery systems |
| KR102871690B1 (ko) | 2018-04-30 | 2025-10-16 | 리제너론 파마슈티칼스 인코포레이티드 | Her2 및/또는 aplp2에 결합하는 항체 및 이중특이적 항원-결합 분자 및 접합체 그리고 이들의 용도 |
| AU2019269685B2 (en) | 2018-05-17 | 2025-12-04 | Regeneron Pharmaceuticals, Inc. | Anti-CD63 antibodies, conjugates, and uses thereof |
| WO2020057543A1 (zh) * | 2018-09-21 | 2020-03-26 | 中国人民解放军军事科学院军事医学研究院 | 基于芳硝基的连接子、含连接子的抗体偶联药物及连接子的用途 |
| JP2022523360A (ja) | 2019-02-21 | 2022-04-22 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | Ｍｅｔに結合する抗ｍｅｔ抗体および二特異性抗原結合分子を使用した眼癌の治療方法 |
| KR20220063185A (ko) | 2019-09-16 | 2022-05-17 | 리제너론 파마슈티칼스 인코포레이티드 | 면역-pet 영상화를 위한 방사성 표지된 met 결합 단백질 |
| US11814428B2 (en) * | 2019-09-19 | 2023-11-14 | Regeneron Pharmaceuticals, Inc. | Anti-PTCRA antibody-drug conjugates and uses thereof |
| WO2021097220A1 (en) | 2019-11-15 | 2021-05-20 | Seagen Inc. | Methods of treating her2 positive breast cancer with tucatinib in combination with an anti-her2 antibody-drug conjugate |
| CN113292574B (zh) * | 2020-02-21 | 2022-05-03 | 四川大学 | 一类手性多环的托品烷化合物及其制备方法和用途 |
| AU2021228225A1 (en) | 2020-02-28 | 2022-09-01 | Regeneron Pharmaceuticals, Inc. | Bispecific antigen binding molecules that bind HER2, and methods of use thereof |
| IL297027B2 (en) | 2020-04-16 | 2025-08-01 | Regeneron Pharma | Antibody-drug conjugates prepared using diels-alder conjugation methods |
| JP7767411B2 (ja) | 2020-10-22 | 2025-11-11 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | 抗ｆｇｆｒ２抗体及びその使用方法 |
| CN116615257A (zh) | 2020-11-10 | 2023-08-18 | 瑞泽恩制药公司 | 硒抗体缀合物 |
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