EA201490554A1 - Пирролобензодиазепины - Google Patents
ПирролобензодиазепиныInfo
- Publication number
- EA201490554A1 EA201490554A1 EA201490554A EA201490554A EA201490554A1 EA 201490554 A1 EA201490554 A1 EA 201490554A1 EA 201490554 A EA201490554 A EA 201490554A EA 201490554 A EA201490554 A EA 201490554A EA 201490554 A1 EA201490554 A1 EA 201490554A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- group
- nitro
- halogen
- alkyl
- single bond
- Prior art date
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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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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P17/06—Antipsoriatics
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
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- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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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- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
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- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
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- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
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- Diabetes (AREA)
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- Orthopedic Medicine & Surgery (AREA)
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- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
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- Cardiology (AREA)
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Abstract
Соединение формулы Iгде Rимеет формулу IIгде А представляет собой Cарильную группу, X выбран из группы, включающей NHNH, CONHNH,и либо (i) Qпредставляет собой одинарную связь, Qвыбран из одинарной связи и -Z-(CH)-, где Z выбран из одинарной связи, О, S и NH, n составляет от 1 до 3; или (ii) Qпредставляет собой -СН=СН- и Qпредставляет собой одинарную связь; Rпредставляет собой Сарильную группу, необязательно замещенную одним или более заместителями, выбранными из группы, состоящей из галогена, нитро, циано, простого эфира, Cалкила, Сгетероциклила и бис-окси-Cалкилена; Rи Rнезависимо выбраны из Н, R, ОН, OR, SH, SR, NH, NHR, NRR', нитро, MeSn и галогена; где R и R' независимо выбраны из необязательно замещенной Cалкильной, Сгетероциклильной и Сарильной групп; Rвыбран из Н, R, ОН, OR, SH, SR, NH, NHR, NHRR', нитро, MeSn и галогена; либо (a) Rпредставляет собой Н, Rпредставляет собой ОН, OR, где Rпредставляет собой Cалкил; (b) Rи Rобразуют двойную связь азот-углерод между атомами азота и углерода, к которым они присоединены; или (c) Rпредставляет собой Н и Rпредставляет собой SOM, где z представляет собой 2 или 3 и М представляет собой одновалентный фармацевтически приемлемый катион; R" представляет собой Cалкиленовую группу, цепь которой может прерываться одним или более гетероатомами и/или ароматическими кольцами; Y и Y' выбраны из О, S или NH; R, R, Rвыбраны из тех же групп, как R, Rи Rсоответственно, и Rи Rпредставляют собой такие же группы, как Rи R, где если Rи Rпредставляют собой SOM, M может представлять собой двухвалентный фармацевтически приемлемый катион.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161547204P | 2011-10-14 | 2011-10-14 | |
PCT/EP2012/070231 WO2013053871A1 (en) | 2011-10-14 | 2012-10-12 | Pyrrolobenzodiazepines |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201490554A1 true EA201490554A1 (ru) | 2015-06-30 |
EA027386B1 EA027386B1 (ru) | 2017-07-31 |
Family
ID=47019018
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201490554A EA027386B1 (ru) | 2011-10-14 | 2012-10-12 | Пирролобензодиазепины |
Country Status (9)
Country | Link |
---|---|
US (1) | US9388187B2 (ru) |
EP (1) | EP2751110B1 (ru) |
JP (1) | JP6117801B2 (ru) |
CN (2) | CN110183470A (ru) |
AU (1) | AU2012322932B2 (ru) |
BR (1) | BR112014008981A2 (ru) |
CA (1) | CA2850264C (ru) |
EA (1) | EA027386B1 (ru) |
WO (1) | WO2013053871A1 (ru) |
Families Citing this family (58)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0819095D0 (en) | 2008-10-17 | 2008-11-26 | Spirogen Ltd | Pyrrolobenzodiazepines |
US9242013B2 (en) | 2010-04-15 | 2016-01-26 | Seattle Genetics Inc. | Targeted pyrrolobenzodiazapine conjugates |
EP2558475A1 (en) | 2010-04-15 | 2013-02-20 | Spirogen Sàrl | Pyrrolobenzodiazepines used to treat proliferative diseases |
KR101860174B1 (ko) | 2011-09-20 | 2018-05-21 | 메디뮨 리미티드 | 표적 접합체 내의 내포를 위한 비대칭 이량체 pbd 화합물로서 피롤로벤조디아제핀 |
CN110183470A (zh) | 2011-10-14 | 2019-08-30 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓 |
BR112014009055B1 (pt) | 2011-10-14 | 2021-12-14 | Seattle Genetics, Inc. | Compostos pirrolobenzodiazepinas, conjugados alvos, ligante de fármaco e uso dos ditos conjugados para tratar uma doença proliferativa |
US9399073B2 (en) | 2011-10-14 | 2016-07-26 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines |
US9526798B2 (en) | 2011-10-14 | 2016-12-27 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
AU2013328628B2 (en) | 2012-10-12 | 2016-12-15 | Adc Therapeutics Sa | Pyrrolobenzodiazepine-anti-CD22 antibody conjugates |
MX364329B (es) | 2012-10-12 | 2019-04-23 | Medimmune Ltd | Conjugados del anticuerpo pirrolobenzodiazepina. |
CN105102068B (zh) | 2012-10-12 | 2018-06-01 | Adc疗法责任有限公司 | 吡咯并苯并二氮杂卓-抗体结合物 |
ES2660029T3 (es) | 2012-10-12 | 2018-03-20 | Medimmune Limited | Conjugados de anticuerpo-pirrolobenzodiazepinas |
CA2885315C (en) | 2012-10-12 | 2020-06-23 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
WO2014057072A1 (en) | 2012-10-12 | 2014-04-17 | Spirogen Sàrl | Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation |
EP2906250B1 (en) | 2012-10-12 | 2018-05-30 | ADC Therapeutics SA | Pyrrolobenzodiazepine-anti-psma antibody conjugates |
KR101819404B1 (ko) | 2012-10-12 | 2018-02-28 | 메디뮨 리미티드 | 피롤로벤조디아제핀 및 그의 컨주게이트 |
PL2906253T3 (pl) | 2012-10-12 | 2019-02-28 | Adc Therapeutics Sa | Koniugaty pirolobenzodiazepina-przeciwciało anty-psma |
CN110452242A (zh) | 2012-12-21 | 2019-11-15 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓及其结合物 |
CA2894959C (en) | 2012-12-21 | 2022-01-11 | Spirogen Sarl | Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases |
BR112015023070B1 (pt) | 2013-03-13 | 2022-06-07 | Genentech, Inc. | Conjugados e compostos de pirrolobenzodiazepinas, composição farmacêutica que compreende os mesmo, bem como seus usos para o tratamento de uma doença proliferativa |
KR102066318B1 (ko) | 2013-03-13 | 2020-01-14 | 메디뮨 리미티드 | 피롤로벤조디아제핀 및 그의 컨쥬게이트 |
US10010624B2 (en) | 2013-10-11 | 2018-07-03 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
US9950078B2 (en) | 2013-10-11 | 2018-04-24 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
WO2015052535A1 (en) | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
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 |
CN106687141A (zh) | 2014-09-10 | 2017-05-17 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓及其缀合物 |
GB201416112D0 (en) | 2014-09-12 | 2014-10-29 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
GB201416960D0 (en) | 2014-09-25 | 2014-11-12 | Antikor Biopharma Ltd | Biological materials and uses thereof |
CN107148285B (zh) | 2014-11-25 | 2022-01-04 | Adc治疗股份有限公司 | 吡咯并苯并二氮杂䓬-抗体缀合物 |
CA2973354A1 (en) | 2015-01-14 | 2016-07-21 | Bristol-Myers Squibb Company | Benzodiazepine dimers, conjugates thereof, and methods of making and using |
CN107231804B (zh) | 2015-01-14 | 2019-11-26 | 百时美施贵宝公司 | 亚杂芳基桥连苯并二氮杂*二聚体、其缀合物及制备和使用方法 |
GB201506411D0 (en) | 2015-04-15 | 2015-05-27 | Bergenbio As | Humanized anti-axl antibodies |
GB201506402D0 (en) | 2015-04-15 | 2015-05-27 | Berkel Patricius H C Van And Howard Philip W | Site-specific antibody-drug conjugates |
EP3313854A1 (en) | 2015-06-23 | 2018-05-02 | Bristol-Myers Squibb Company | Macrocyclic benzodiazepine dimers, conjugates thereof, preparation and uses |
GB201601431D0 (en) | 2016-01-26 | 2016-03-09 | Medimmune Ltd | Pyrrolobenzodiazepines |
GB201602356D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
GB201602359D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
GB201607478D0 (en) | 2016-04-29 | 2016-06-15 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
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AU2012322932A1 (en) | 2014-05-29 |
EP2751110A1 (en) | 2014-07-09 |
BR112014008981A2 (pt) | 2017-05-02 |
CN103998449A (zh) | 2014-08-20 |
CN110183470A (zh) | 2019-08-30 |
CA2850264C (en) | 2019-11-05 |
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