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 |
| ES2623057T3 (es) | 2010-04-15 | 2017-07-10 | Medimmune Limited | Pirrolobenzodiazepinas usadas para tratar enfermedades proliferativas |
| CN103987718A (zh) | 2011-09-20 | 2014-08-13 | 斯皮罗根有限公司 | 作为非对称二聚体pbd化合物用于内含在靶向结合物中的吡咯并苯并二氮杂卓 |
| CN103998450B (zh) | 2011-10-14 | 2017-03-08 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓 |
| 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 |
| CA2850375C (en) | 2011-10-14 | 2019-07-02 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
| CA2850373C (en) | 2011-10-14 | 2019-07-16 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
| PL2817338T3 (pl) | 2012-02-24 | 2017-12-29 | Abbvie Stemcentrx Llc | Modulatory DLL3 i sposoby zastosowania |
| HRP20180945T1 (hr) | 2012-10-12 | 2018-08-10 | Adc Therapeutics Sa | Konjugati protutijelo-pirolobenzodiazepin |
| CA2885305C (en) | 2012-10-12 | 2019-11-12 | Spirogen Sarl | Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation |
| CN104703630A (zh) | 2012-10-12 | 2015-06-10 | 斯皮罗根有限公司 | 吡咯并苯并二氮杂卓及其结合物 |
| ES2680153T3 (es) | 2012-10-12 | 2018-09-04 | Adc Therapeutics Sa | Conjugados de anticuerpos anti-PSMA-pirrolobenzodiazepinas |
| LT2906251T (lt) | 2012-10-12 | 2017-12-11 | Adc Therapeutics Sa | Pirolobenzodiazepino-anti-cd22 antikūno konjugatai |
| PT2906253T (pt) | 2012-10-12 | 2018-11-05 | Medimmune Ltd | Conjugados de anticorpo anti-psma de pirrolobenzodiazepina |
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| WO2014057120A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| RS58921B1 (sr) | 2012-10-12 | 2019-08-30 | Medimmune Ltd | Pirolobenzodiazepini i njihovi konjugati |
| WO2014096368A1 (en) | 2012-12-21 | 2014-06-26 | Spirogen Sàrl | Pyrrolobenzodiazepines and conjugates thereof |
| JP6527466B2 (ja) * | 2012-12-21 | 2019-06-05 | メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ | 増殖性疾患および自己免疫疾患の治療に使用するための非対称ピロロベンゾジアゼピンニ量体 |
| PL2958944T3 (pl) * | 2013-02-22 | 2019-09-30 | Abbvie Stemcentrx Llc | Koniugaty przeciwciało anty-DLL3-PBD i ich zastosowania |
| NZ710746A (en) | 2013-03-13 | 2018-11-30 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
| WO2014159981A2 (en) | 2013-03-13 | 2014-10-02 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| KR20160044042A (ko) | 2013-08-28 | 2016-04-22 | 스템센트알엑스 인코포레이티드 | 부위-특이적 항체 접합 방법 및 조성물 |
| CA2921982C (en) * | 2013-09-02 | 2020-08-25 | Hangzhou Dac Biotech Co., Ltd | Novel cytotoxic agents for conjugation of drugs to cell binding molecule |
| WO2015052535A1 (en) * | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| US20160256561A1 (en) * | 2013-10-11 | 2016-09-08 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
| WO2015052534A1 (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 |
| WO2015052532A1 (en) * | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
| JP6747971B2 (ja) | 2013-10-15 | 2020-08-26 | シアトル ジェネティックス， インコーポレイテッド | 改善されたリガンド−薬物コンジュゲート薬物動態のためのｐｅｇ化薬物−リンカー |
| JP6681838B2 (ja) * | 2013-12-16 | 2020-04-15 | ジェネンテック， インコーポレイテッド | ペプチド模倣薬化合物及びその抗体−薬剤複合体 |
| EA201691023A1 (ru) | 2013-12-16 | 2016-10-31 | Дженентек, Инк. | Пептидомиметические соединения и их конъюгаты антитела с лекарственным средством |
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- 2012-09-20 KR KR1020147010023A patent/KR101860174B1/ko not_active Expired - Fee Related
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- 2012-09-20 MX MX2014003349A patent/MX341524B/es active IP Right Grant
- 2012-09-20 BR BR112014006703A patent/BR112014006703A8/pt not_active Application Discontinuation
- 2012-09-20 JP JP2014531224A patent/JP6170494B2/ja not_active Expired - Fee Related
- 2012-09-20 WO PCT/EP2012/068506 patent/WO2013041606A1/en not_active Ceased
- 2012-09-20 US US14/346,006 patent/US9399641B2/en not_active Expired - Fee Related
- 2012-09-20 SG SG11201400770SA patent/SG11201400770SA/en unknown
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- 2012-09-20 EP EP12781045.5A patent/EP2751120B1/en not_active Not-in-force