JP2014527974A5 - - Google Patents
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- JP2014527974A5 JP2014527974A5 JP2014531224A JP2014531224A JP2014527974A5 JP 2014527974 A5 JP2014527974 A5 JP 2014527974A5 JP 2014531224 A JP2014531224 A JP 2014531224A JP 2014531224 A JP2014531224 A JP 2014531224A JP 2014527974 A5 JP2014527974 A5 JP 2014527974A5
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- Japan
- Prior art keywords
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- 150000001875 compounds Chemical class 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 239000003446 ligand Substances 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000005647 linker group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 2
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 2
- 125000005907 alkyl ester group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001768 cations Chemical class 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 239000004474 valine Substances 0.000 claims 2
- OMRPLUKQNWNZAV-CONSDPRKSA-N (6as)-3-[3-[[(6as)-2-methoxy-8-(4-methoxyphenyl)-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-8-(4-aminophenyl)-2-methoxy-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one Chemical group C1=CC(OC)=CC=C1C1=CN2C(=O)C3=CC(OC)=C(OCCCOC=4C(=CC=5C(=O)N6C=C(C[C@H]6C=NC=5C=4)C=4C=CC(N)=CC=4)OC)C=C3N=C[C@@H]2C1 OMRPLUKQNWNZAV-CONSDPRKSA-N 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 108010016626 Dipeptides Proteins 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- GDIHDSKOVXEJQQ-UHFFFAOYSA-N NC(O)=O.NC(O)=O.NC(O)=O.N Chemical group NC(O)=O.NC(O)=O.NC(O)=O.N GDIHDSKOVXEJQQ-UHFFFAOYSA-N 0.000 claims 1
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
- 150000001413 amino acids Chemical group 0.000 claims 1
- 235000013477 citrulline Nutrition 0.000 claims 1
- 229960002173 citrulline Drugs 0.000 claims 1
- IBAHLNWTOIHLKE-UHFFFAOYSA-N cyano cyanate Chemical group N#COC#N IBAHLNWTOIHLKE-UHFFFAOYSA-N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002825 nitriles Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 0 CC(C[C@@]1C(C)N(*)c2c3c(*)c(*)c(**(*c(c(*)c4N(*)C(*)[C@]5N6C=C(*)C5)c(*)c(*)c4C6=O)=C)c2*)[C@](C)N1C3=O Chemical compound CC(C[C@@]1C(C)N(*)c2c3c(*)c(*)c(**(*c(c(*)c4N(*)C(*)[C@]5N6C=C(*)C5)c(*)c(*)c4C6=O)=C)c2*)[C@](C)N1C3=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161536669P | 2011-09-20 | 2011-09-20 | |
| US61/536,669 | 2011-09-20 | ||
| PCT/EP2012/068506 WO2013041606A1 (en) | 2011-09-20 | 2012-09-20 | Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014527974A JP2014527974A (ja) | 2014-10-23 |
| JP2014527974A5 true JP2014527974A5 (enExample) | 2015-11-12 |
| JP6170494B2 JP6170494B2 (ja) | 2017-07-26 |
Family
ID=47137669
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014531224A Expired - Fee Related JP6170494B2 (ja) | 2011-09-20 | 2012-09-20 | ピロロベンゾジアゼピン |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9399641B2 (enExample) |
| EP (1) | EP2751120B1 (enExample) |
| JP (1) | JP6170494B2 (enExample) |
| KR (1) | KR101860174B1 (enExample) |
| CN (1) | CN103987718A (enExample) |
| AU (1) | AU2012311505B2 (enExample) |
| BR (1) | BR112014006703A8 (enExample) |
| CA (1) | CA2849039C (enExample) |
| EA (1) | EA027971B1 (enExample) |
| MX (1) | MX341524B (enExample) |
| SG (1) | SG11201400770SA (enExample) |
| WO (1) | WO2013041606A1 (enExample) |
Families Citing this family (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0819095D0 (en) | 2008-10-17 | 2008-11-26 | Spirogen Ltd | Pyrrolobenzodiazepines |
| CN103068405A (zh) | 2010-04-15 | 2013-04-24 | 西雅图基因公司 | 靶向吡咯并苯并二氮杂卓结合物 |
| MX368648B (es) | 2010-04-15 | 2019-10-09 | Seattle Genetics Inc | Pirrolobenzodiazepinas usadas para tratar enfermedades proliferativas. |
| US9399641B2 (en) | 2011-09-20 | 2016-07-26 | Medimmune Limited | Pyrrolobenzodiazepines as unsymmetrical dimeric PBD compounds for inclusion in targeted conjugates |
| CA2850373C (en) | 2011-10-14 | 2019-07-16 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
| CA2850375C (en) | 2011-10-14 | 2019-07-02 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
| AU2012322934B2 (en) | 2011-10-14 | 2016-09-08 | Medimmune Limited | Pyrrolobenzodiazepines |
| CA2850264C (en) | 2011-10-14 | 2019-11-05 | Medimmune Limited | Pyrrolobenzodiazepines |
| CN104520324A (zh) | 2012-02-24 | 2015-04-15 | 施特姆森特Rx股份有限公司 | Dll3调节剂及其使用方法 |
| PT2906248T (pt) | 2012-10-12 | 2019-03-04 | Medimmune Ltd | Pirrolobenzodiazepinas e conjugados das mesmas |
| KR101995620B1 (ko) | 2012-10-12 | 2019-07-03 | 에이디씨 테라퓨틱스 에스에이 | 피롤로벤조디아제핀-항체 컨주게이트 |
| EP2906297B1 (en) | 2012-10-12 | 2017-12-06 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
| DK2906298T3 (en) | 2012-10-12 | 2018-12-17 | Adc Therapeutics Sa | Pyrrolobenzodiazepine-antibody conjugates |
| BR112015008238A2 (pt) | 2012-10-12 | 2017-11-28 | Adc Therapeutics Sarl | conjugados de pirrolbenzodiazepina-anticorpo anti-cd22 |
| DK2839860T3 (da) | 2012-10-12 | 2019-06-17 | Medimmune Ltd | Pyrrolobenzodiazepiner og konjugater deraf |
| EP2906249B1 (en) | 2012-10-12 | 2018-06-27 | 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 |
| PT2906253T (pt) | 2012-10-12 | 2018-11-05 | Medimmune Ltd | Conjugados de anticorpo anti-psma de pirrolobenzodiazepina |
| AU2013366493B2 (en) | 2012-12-21 | 2017-08-24 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
| US9567340B2 (en) | 2012-12-21 | 2017-02-14 | Medimmune Limited | Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases |
| ES2731681T3 (es) | 2013-02-22 | 2019-11-18 | Abbvie Stemcentrx Llc | Conjugados de anticuerpo anti-DLL3 y PBD y usos de los mismos |
| KR102066318B1 (ko) | 2013-03-13 | 2020-01-14 | 메디뮨 리미티드 | 피롤로벤조디아제핀 및 그의 컨쥬게이트 |
| MX363787B (es) | 2013-03-13 | 2019-04-03 | Medimmune Ltd | Pirrolobenzodiazepinas y conjugados de los mismos. |
| JP2016531915A (ja) | 2013-08-28 | 2016-10-13 | ステムセントリックス, インコーポレイテッド | 部位特異的抗体コンジュゲーション方法および組成物 |
| WO2015028850A1 (en) * | 2013-09-02 | 2015-03-05 | Hangzhou Dac Biotech Co., Ltd | Novel cytotoxic agents for conjugation of drugs to cell binding molecule |
| 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 |
| WO2015052534A1 (en) * | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| US10010624B2 (en) | 2013-10-11 | 2018-07-03 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
| WO2015052535A1 (en) * | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| WO2015052533A1 (en) * | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| PT3057585T (pt) | 2013-10-15 | 2020-10-21 | Seagen Inc | Fármaco-ligadores peguilados para farmacocinética melhorada de conjugados de fármaco-ligando |
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| BR112016014126B1 (pt) * | 2013-12-16 | 2023-02-14 | Medimmune Limited | Composto não-peptídico, conjugados de anticorpo-fármaco do mesmo, uso dos ditos conjugados para o tratamento de câncer e composição farmacêutica que compreende os mesmos |
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-
2012
- 2012-09-20 US US14/346,006 patent/US9399641B2/en not_active Expired - Fee Related
- 2012-09-20 JP JP2014531224A patent/JP6170494B2/ja not_active Expired - Fee Related
- 2012-09-20 SG SG11201400770SA patent/SG11201400770SA/en unknown
- 2012-09-20 AU AU2012311505A patent/AU2012311505B2/en not_active Ceased
- 2012-09-20 EA EA201490518A patent/EA027971B1/ru unknown
- 2012-09-20 BR BR112014006703A patent/BR112014006703A8/pt not_active Application Discontinuation
- 2012-09-20 WO PCT/EP2012/068506 patent/WO2013041606A1/en not_active Ceased
- 2012-09-20 CN CN201280057069.7A patent/CN103987718A/zh active Pending
- 2012-09-20 MX MX2014003349A patent/MX341524B/es active IP Right Grant
- 2012-09-20 EP EP12781045.5A patent/EP2751120B1/en not_active Not-in-force
- 2012-09-20 KR KR1020147010023A patent/KR101860174B1/ko not_active Expired - Fee Related
- 2012-09-20 CA CA2849039A patent/CA2849039C/en not_active Expired - Fee Related
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