JP2014534200A5 - - Google Patents
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- JP2014534200A5 JP2014534200A5 JP2014535898A JP2014535898A JP2014534200A5 JP 2014534200 A5 JP2014534200 A5 JP 2014534200A5 JP 2014535898 A JP2014535898 A JP 2014535898A JP 2014535898 A JP2014535898 A JP 2014535898A JP 2014534200 A5 JP2014534200 A5 JP 2014534200A5
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- 150000001875 compounds Chemical class 0.000 claims 18
- 239000003446 ligand Substances 0.000 claims 8
- 125000005647 linker group Chemical group 0.000 claims 7
- -1 4-carboxy - phenyl Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 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 compound 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 2
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-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
- 150000001413 amino acids Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001768 cations Chemical class 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- 239000004474 valine Substances 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- LJCZNYWLQZZIOS-UHFFFAOYSA-N 2,2,2-trichlorethoxycarbonyl chloride Chemical compound ClC(=O)OCC(Cl)(Cl)Cl LJCZNYWLQZZIOS-UHFFFAOYSA-N 0.000 claims 1
- 125000004208 3-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(*)=C1[H] 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 108010016626 Dipeptides Proteins 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 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
- 206010025323 Lymphomas Diseases 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
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 210000001744 T-lymphocyte Anatomy 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 201000008275 breast carcinoma Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 1
- 235000013477 citrulline Nutrition 0.000 claims 1
- 229960002173 citrulline Drugs 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 230000002197 limbic effect Effects 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 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
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161547195P | 2011-10-14 | 2011-10-14 | |
| US61/547,195 | 2011-10-14 | ||
| PCT/US2012/059870 WO2013055993A1 (en) | 2011-10-14 | 2012-10-12 | Pyrrolobenzodiazepines and targeted conjugates |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018095724A Division JP6599509B2 (ja) | 2011-10-14 | 2018-05-17 | ピロロベンゾジアゼピンおよび標的コンジュゲート |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014534200A JP2014534200A (ja) | 2014-12-18 |
| JP2014534200A5 true JP2014534200A5 (enExample) | 2015-12-03 |
| JP6399930B2 JP6399930B2 (ja) | 2018-10-03 |
Family
ID=48082466
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014535898A Active JP6399930B2 (ja) | 2011-10-14 | 2012-10-12 | ピロロベンゾジアゼピンおよび標的コンジュゲート |
| JP2018095724A Active JP6599509B2 (ja) | 2011-10-14 | 2018-05-17 | ピロロベンゾジアゼピンおよび標的コンジュゲート |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018095724A Active JP6599509B2 (ja) | 2011-10-14 | 2018-05-17 | ピロロベンゾジアゼピンおよび標的コンジュゲート |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US9387259B2 (enExample) |
| EP (2) | EP3309162A1 (enExample) |
| JP (2) | JP6399930B2 (enExample) |
| KR (1) | KR101961976B1 (enExample) |
| CN (1) | CN103997893B (enExample) |
| AU (1) | AU2012322613B2 (enExample) |
| BR (2) | BR112014009055B1 (enExample) |
| CA (1) | CA2850375C (enExample) |
| EA (2) | EA026643B1 (enExample) |
| ES (1) | ES2660233T3 (enExample) |
| HK (1) | HK1253715A1 (enExample) |
| IL (1) | IL231797A (enExample) |
| MX (3) | MX375987B (enExample) |
| WO (1) | WO2013055993A1 (enExample) |
| ZA (1) | ZA201402404B (enExample) |
Families Citing this family (135)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0819095D0 (en) | 2008-10-17 | 2008-11-26 | Spirogen Ltd | Pyrrolobenzodiazepines |
| EP2558127B1 (en) | 2010-04-15 | 2022-01-19 | Seagen Inc. | Targeted pyrrolobenzodiazepine conjugates |
| JP5875083B2 (ja) | 2010-04-15 | 2016-03-02 | メディミューン リミテッド | 増殖性疾患治療用ピロロベンゾジアゼピン |
| KR101860174B1 (ko) | 2011-09-20 | 2018-05-21 | 메디뮨 리미티드 | 표적 접합체 내의 내포를 위한 비대칭 이량체 pbd 화합물로서 피롤로벤조디아제핀 |
| EP2751111B1 (en) | 2011-10-14 | 2017-04-26 | MedImmune Limited | Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases |
| ES2945932T3 (es) | 2011-10-14 | 2023-07-10 | Seagen Inc | Pirrolobenzodiazepinas y conjugados dirigidos |
| EA027386B1 (ru) * | 2011-10-14 | 2017-07-31 | Медимьюн Лимитед | Пирролобензодиазепины |
| US9387259B2 (en) | 2011-10-14 | 2016-07-12 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
| CA2887895C (en) | 2012-10-12 | 2019-10-29 | Adc Therapeutics Sarl | Pyrrolobenzodiazepine-anti-cd19 antibody conjugates |
| CN105102004B (zh) | 2012-10-12 | 2019-01-25 | Adc疗法责任有限公司 | 吡咯并苯并二氮杂卓-抗cd22抗体结合物 |
| SI2766048T1 (sl) | 2012-10-12 | 2015-03-31 | Spirogen Sarl | Pirolobenzodiazepini in njihovi konjugati |
| LT2906248T (lt) | 2012-10-12 | 2019-02-11 | Medimmune Limited | Pirolobenzodiazepinai ir jų konjugatai |
| TR201808051T4 (tr) | 2012-10-12 | 2018-06-21 | Adc Therapeutics Sa | Pirrolobenzodiazepin antikor konjugatları. |
| EP2906297B1 (en) | 2012-10-12 | 2017-12-06 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
| WO2014057114A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sàrl | Pyrrolobenzodiazepine-anti-psma antibody conjugates |
| HUE041274T2 (hu) | 2012-10-12 | 2019-05-28 | Adc Therapeutics Sa | Pirrolobenzodiazepin-anti-PSMA-antitest konjugátumok |
| JP6367204B2 (ja) | 2012-10-12 | 2018-08-01 | メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ | 結合用のピロロベンゾジアゼピン誘導体の合成および中間体 |
| WO2014089177A2 (en) | 2012-12-04 | 2014-06-12 | Massachusetts Institute Of Technology | Compounds, conjugates and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines |
| CA2894959C (en) | 2012-12-21 | 2022-01-11 | Spirogen Sarl | Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases |
| 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 |
| ES2731779T3 (es) | 2013-03-13 | 2019-11-19 | Medimmune Ltd | Pirrolobenzodiazepinas y conjugados de las mismas |
| AU2014248640B2 (en) | 2013-03-13 | 2018-03-01 | Seagen Inc. | Cyclodextrin and antibody-drug conjugate formulations |
| ES2843786T3 (es) | 2013-03-13 | 2021-07-20 | Seagen Inc | Filtración con carbono activado para la purificación de ADC de benzodiazepina |
| MX363787B (es) | 2013-03-13 | 2019-04-03 | Medimmune Ltd | Pirrolobenzodiazepinas y conjugados de los mismos. |
| US10570151B2 (en) | 2013-03-15 | 2020-02-25 | Regeneron Pharmaceuticals, Inc. | Biologically active molecules, conjugates thereof, and therapeutic uses |
| US10208125B2 (en) | 2013-07-15 | 2019-02-19 | University of Pittsburgh—of the Commonwealth System of Higher Education | Anti-mucin 1 binding agents and uses thereof |
| EA038192B1 (ru) | 2013-08-26 | 2021-07-21 | Регенерон Фармасьютикалз, Инк. | Фармацевтические композиции, содержащие диастереомеры макролида, способы их синтезирования и терапевтическое применение |
| GB201317981D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| GB201317982D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
| EP3054985B1 (en) | 2013-10-11 | 2018-12-26 | Medimmune Limited | 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 |
| CA3187392A1 (en) | 2013-10-15 | 2015-04-23 | Seagen Inc. | Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics |
| MX385651B (es) | 2013-12-19 | 2025-03-18 | Seagen Inc | Enlazadores de carbamato de metileno para su uso en conjugados de farmacos dirigidos. |
| EA035809B1 (ru) | 2014-03-11 | 2020-08-14 | Регенерон Фармасьютикалс, Инк. | АНТИТЕЛА ПРОТИВ EGFRvIII И ИХ ПРИМЕНЕНИЯ |
| GB201409653D0 (en) * | 2014-05-30 | 2014-07-16 | Stell Dr Anneliese | Pyrrolobenzodiazepine therapeutic agents |
| JP6531166B2 (ja) | 2014-09-10 | 2019-06-12 | メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ | ピロロベンゾジアゼピン及びそのコンジュゲート |
| PT3191135T (pt) | 2014-09-12 | 2020-11-12 | Genentech Inc | Anticorpos anti-her2 e imunoconjugados |
| GB201416112D0 (en) | 2014-09-12 | 2014-10-29 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates 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 |
| PE20171185A1 (es) | 2015-01-14 | 2017-08-22 | Bristol Myers Squibb Co | Dimeros de benzodiazepina unidos con puentes de heteroarileno, conjugados de estos, y sus metodos de preparacion y uso |
| AU2016206798A1 (en) | 2015-01-14 | 2017-08-31 | Bristol-Myers Squibb Company | Benzodiazepine dimers, conjugates thereof, and methods of making and using |
| CN107428844A (zh) * | 2015-03-05 | 2017-12-01 | 发展生物工程与基因技术的彼得和特劳德尔·恩格尔霍恩基金会 | 用于将肽呈递在细胞表面上的系统 |
| BR112017020149A8 (pt) | 2015-03-27 | 2023-05-02 | Regeneron Pharma | Derivados de maitansinoide, conjugados dos mesmos e métodos de uso |
| 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 |
| CN108391434A (zh) | 2015-06-23 | 2018-08-10 | 百时美施贵宝公司 | 大环苯并二氮杂*二聚体、其缀合物、制备和用途 |
| US11191844B2 (en) | 2015-07-06 | 2021-12-07 | Regeneran Pharmaceuticals, Inc. | Multispecific antigen-binding molecules and uses thereof |
| MA43345A (fr) | 2015-10-02 | 2018-08-08 | Hoffmann La Roche | Conjugués anticorps-médicaments de pyrrolobenzodiazépine et méthodes d'utilisation |
| SG10202010590UA (en) | 2015-12-04 | 2020-12-30 | Seattle Genetics Inc | Conjugates of quaternized tubulysin compounds |
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| MA43094B1 (fr) | 2016-01-25 | 2020-10-28 | Regeneron Pharma | Dérivés de maytansinoïde, leurs conjugués, et procédés d'utilisation |
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| US10918627B2 (en) | 2016-05-11 | 2021-02-16 | Massachusetts Institute Of Technology | Convergent and enantioselective total synthesis of Communesin analogs |
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| GB201617466D0 (en) | 2016-10-14 | 2016-11-30 | Medimmune Ltd | Pyrrolobenzodiazepine conjugates |
| KR102835535B1 (ko) | 2016-11-08 | 2025-07-18 | 리제너론 파마슈티칼스 인코포레이티드 | 스테로이드 및 이의 단백질-접합체 |
| 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 |
| GB201619490D0 (en) * | 2016-11-17 | 2017-01-04 | Medimmune Ltd | Pyrrolobenzodiazepine conjugates |
| JP7350313B2 (ja) | 2016-12-16 | 2023-09-26 | ブルーフィン バイオメディシン， インコーポレイテッド | 抗ｃｕｂドメイン含有タンパク質１（ｃｄｃｐ１）抗体、抗体薬物コンジュゲート、およびその使用方法 |
| KR102725761B1 (ko) | 2017-01-20 | 2024-11-04 | 하이델베르크 파마 리서치 게엠베하 | Cd137+ 세포의 고갈을 위한 조성물 및 방법 |
| EP3544636B1 (en) | 2017-02-08 | 2021-03-31 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
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