CA2894961C - Pyrrolobenzodiazepines and conjugates thereof - Google Patents
Pyrrolobenzodiazepines and conjugates thereof Download PDFInfo
- Publication number
- CA2894961C CA2894961C CA2894961A CA2894961A CA2894961C CA 2894961 C CA2894961 C CA 2894961C CA 2894961 A CA2894961 A CA 2894961A CA 2894961 A CA2894961 A CA 2894961A CA 2894961 C CA2894961 C CA 2894961C
- Authority
- CA
- Canada
- Prior art keywords
- group
- antibody
- alkyl
- genbank
- linker
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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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
- 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
- A61K31/55—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
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- 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
- A61K47/68035—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a pyrrolobenzodiazepine
-
- 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
- A61K47/6851—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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Cell Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261740592P | 2012-12-21 | 2012-12-21 | |
| US61/740,592 | 2012-12-21 | ||
| PCT/EP2013/077705 WO2014096368A1 (en) | 2012-12-21 | 2013-12-20 | Pyrrolobenzodiazepines and conjugates thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2894961A1 CA2894961A1 (en) | 2014-06-26 |
| CA2894961C true CA2894961C (en) | 2020-09-15 |
Family
ID=49886925
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2894961A Active CA2894961C (en) | 2012-12-21 | 2013-12-20 | Pyrrolobenzodiazepines and conjugates thereof |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9562049B2 (enExample) |
| EP (1) | EP2935268B2 (enExample) |
| JP (1) | JP6307519B2 (enExample) |
| CN (2) | CN105189507A (enExample) |
| AU (1) | AU2013366493B2 (enExample) |
| BR (1) | BR112015014669B1 (enExample) |
| CA (1) | CA2894961C (enExample) |
| EA (1) | EA031585B1 (enExample) |
| ES (1) | ES2658888T5 (enExample) |
| WO (1) | WO2014096368A1 (enExample) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0819095D0 (en) | 2008-10-17 | 2008-11-26 | Spirogen Ltd | Pyrrolobenzodiazepines |
| ES2623057T3 (es) | 2010-04-15 | 2017-07-10 | Medimmune Limited | Pirrolobenzodiazepinas usadas para tratar enfermedades proliferativas |
| JP5870400B2 (ja) | 2010-04-15 | 2016-03-01 | シアトル ジェネティクス，インコーポレーテッド | 標的化ピロロベンゾジアゼピンコンジュゲート |
| SG11201400770SA (en) | 2011-09-20 | 2014-04-28 | Spirogen Sarl | Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates |
| MX358757B (es) | 2011-10-14 | 2018-09-03 | Seattle Genetics Inc | Pirrolobenzodiazepinas y conjugados dirigidos. |
| SG11201401021TA (en) | 2011-10-14 | 2014-08-28 | Spirogen Sarl | Pyrrolobenzodiazepines |
| CN103998449A (zh) | 2011-10-14 | 2014-08-20 | 斯皮罗根有限公司 | 吡咯并苯并二氮杂卓 |
| US9526798B2 (en) | 2011-10-14 | 2016-12-27 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
| US9745303B2 (en) | 2012-10-12 | 2017-08-29 | Medimmune Limited | Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation |
| WO2014057114A1 (en) * | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sàrl | Pyrrolobenzodiazepine-anti-psma antibody conjugates |
| NZ707486A (en) * | 2012-10-12 | 2018-09-28 | Adc Therapeutics Sa | Pyrrolobenzodiazepine - anti-psma antibody conjugates |
| BR112015008251B1 (pt) | 2012-10-12 | 2023-09-26 | Medimmune Limited | Pirrolobenzodiazepinas, conjugados destas, composição e composição farmacêutica compreendendo os conjugados, uso dos conjugados para o tratamento de uma doença proliferativa e método para preparar os conjugados |
| WO2014057120A1 (en) * | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| ES2738310T3 (es) | 2012-10-12 | 2020-01-21 | Medimmune Ltd | Pirrolobenzodiazepinas y conjugados de las mismas |
| BR112015014669B1 (pt) | 2012-12-21 | 2023-09-26 | Medimmune Limited | Compostos pirrolobenzodiazepinas, conjugados compreendendo os mesmos e uso destes para tratar uma doença proliferativa |
| HK1216176A1 (zh) | 2012-12-21 | 2016-10-21 | Medlmmune Limited | 用於治疗增殖性和自身免疫疾病的非对称吡咯并苯并二氮杂卓二聚物 |
| CN105142674B (zh) | 2013-03-13 | 2018-11-13 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓和其结合物 |
| AU2014244245C1 (en) | 2013-03-13 | 2018-04-19 | Genentech, Inc. | Pyrrolobenzodiazepines and conjugates thereof |
| GB201317982D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| GB201317981D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| US10188746B2 (en) | 2014-09-10 | 2019-01-29 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
| MY186334A (en) | 2014-09-12 | 2021-07-12 | Genentech Inc | Anti-her2 antibodies and immunoconjugates |
| GB201416112D0 (en) | 2014-09-12 | 2014-10-29 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
| CN107124870A (zh) * | 2014-09-17 | 2017-09-01 | 基因泰克公司 | 包含抗her2抗体和吡咯并苯并二氮杂*的免疫缀合物 |
| EP3223854A1 (en) | 2014-11-25 | 2017-10-04 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
| KR20170102981A (ko) | 2015-01-14 | 2017-09-12 | 브리스톨-마이어스 스큅 컴퍼니 | 헤테로아릴렌-가교된 벤조디아제핀 이량체, 그의 접합체, 및 제조 및 사용 방법 |
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| KR102111338B1 (ko) | 2015-10-02 | 2020-05-15 | 제넨테크, 인크. | 피롤로벤조디아제핀 항체 약물 콘쥬게이트 및 이의 사용 방법 |
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| CN107847605B (zh) | 2015-11-25 | 2021-12-24 | 乐高化学生物科学股份有限公司 | 包含分支接头的抗体-药物缀合物及其相关方法 |
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| EP3612537B1 (en) | 2017-04-18 | 2022-07-13 | Medimmune Limited | Pyrrolobenzodiazepine conjugates |
| UA127900C2 (uk) * | 2017-06-14 | 2024-02-07 | Ейдісі Терапьютікс Са | Схема дозування для введення adc до cd19 |
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| SG11202001430SA (en) | 2017-09-29 | 2020-04-29 | Daiichi Sankyo Co Ltd | Antibody-pyrrolobenzodiazepine derivative conjugate |
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| IL278480B1 (en) | 2018-05-09 | 2026-04-01 | Ligachem Biosciences Inc | Compositions and methods related to anti-CD19 antibody drug conjugates |
| EP3801630A1 (en) * | 2018-05-25 | 2021-04-14 | Medimmune Limited | Pyrrolobenzodiazepine conjugates |
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| CN110452242A (zh) | 2019-11-15 |
| CA2894961A1 (en) | 2014-06-26 |
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| EP2935268A1 (en) | 2015-10-28 |
| JP2016508130A (ja) | 2016-03-17 |
| EA201590999A1 (ru) | 2016-01-29 |
| AU2013366493B2 (en) | 2017-08-24 |
| EA031585B1 (ru) | 2019-01-31 |
| AU2013366493A1 (en) | 2015-07-09 |
| US20150344482A1 (en) | 2015-12-03 |
| WO2014096368A1 (en) | 2014-06-26 |
| HK1216638A1 (en) | 2016-11-25 |
| CN105189507A (zh) | 2015-12-23 |
| JP6307519B2 (ja) | 2018-04-04 |
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