JPWO2021211984A5 - - Google Patents
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- JPWO2021211984A5 JPWO2021211984A5 JP2022562664A JP2022562664A JPWO2021211984A5 JP WO2021211984 A5 JPWO2021211984 A5 JP WO2021211984A5 JP 2022562664 A JP2022562664 A JP 2022562664A JP 2022562664 A JP2022562664 A JP 2022562664A JP WO2021211984 A5 JPWO2021211984 A5 JP WO2021211984A5
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- JP
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- Prior art keywords
- formula
- compound
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- cancer
- composition
- 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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- 150000001875 compounds Chemical class 0.000 claims 36
- 239000000203 mixture Substances 0.000 claims 9
- 125000006850 spacer group Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 239000011230 binding agent Substances 0.000 claims 7
- 239000012634 fragment Substances 0.000 claims 7
- 239000000427 antigen Substances 0.000 claims 6
- 102000036639 antigens Human genes 0.000 claims 6
- 108091007433 antigens Proteins 0.000 claims 6
- YUOCYTRGANSSRY-UHFFFAOYSA-N pyrrolo[2,3-i][1,2]benzodiazepine Chemical compound C1=CN=NC2=C3C=CN=C3C=CC2=C1 YUOCYTRGANSSRY-UHFFFAOYSA-N 0.000 claims 6
- IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical group CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 claims 5
- 108010093470 monomethyl auristatin E Proteins 0.000 claims 5
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 4
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 4
- 229930189077 Rifamycin Natural products 0.000 claims 4
- 229930188854 dolastatin Natural products 0.000 claims 4
- 125000000404 glutamine group Chemical group N[C@@H](CCC(N)=O)C(=O)* 0.000 claims 4
- 239000012216 imaging agent Substances 0.000 claims 4
- 229960003292 rifamycin Drugs 0.000 claims 4
- HJYYPODYNSCCOU-ODRIEIDWSA-N rifamycin SV Chemical compound OC1=C(C(O)=C2C)C3=C(O)C=C1NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@H](C)[C@@H](OC)\C=C\O[C@@]1(C)OC2=C3C1=O HJYYPODYNSCCOU-ODRIEIDWSA-N 0.000 claims 4
- 230000001225 therapeutic effect Effects 0.000 claims 4
- DLKUYSQUHXBYPB-NSSHGSRYSA-N (2s,4r)-4-[[2-[(1r,3r)-1-acetyloxy-4-methyl-3-[3-methylbutanoyloxymethyl-[(2s,3s)-3-methyl-2-[[(2r)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]pentyl]-1,3-thiazole-4-carbonyl]amino]-2-methyl-5-(4-methylphenyl)pentanoic acid Chemical compound N([C@@H]([C@@H](C)CC)C(=O)N(COC(=O)CC(C)C)[C@H](C[C@@H](OC(C)=O)C=1SC=C(N=1)C(=O)N[C@H](C[C@H](C)C(O)=O)CC=1C=CC(C)=CC=1)C(C)C)C(=O)[C@H]1CCCCN1C DLKUYSQUHXBYPB-NSSHGSRYSA-N 0.000 claims 3
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 3
- 101001134216 Homo sapiens Macrophage scavenger receptor types I and II Proteins 0.000 claims 3
- 102100034184 Macrophage scavenger receptor types I and II Human genes 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 230000000843 anti-fungal effect Effects 0.000 claims 3
- 230000003110 anti-inflammatory effect Effects 0.000 claims 3
- 230000000840 anti-viral effect Effects 0.000 claims 3
- 229940121375 antifungal agent Drugs 0.000 claims 3
- 108010044540 auristatin Proteins 0.000 claims 3
- 230000003115 biocidal effect Effects 0.000 claims 3
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 3
- 229940127093 camptothecin Drugs 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 3
- AMRJKAQTDDKMCE-UHFFFAOYSA-N dolastatin Chemical compound CC(C)C(N(C)C)C(=O)NC(C(C)C)C(=O)N(C)C(C(C)C)C(OC)CC(=O)N1CCCC1C(OC)C(C)C(=O)NC(C=1SC=CN=1)CC1=CC=CC=C1 AMRJKAQTDDKMCE-UHFFFAOYSA-N 0.000 claims 3
- 239000002955 immunomodulating agent Substances 0.000 claims 3
- 230000002584 immunomodulator Effects 0.000 claims 3
- 229940121354 immunomodulator Drugs 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003431 steroids Chemical class 0.000 claims 3
- 229930184737 tubulysin Natural products 0.000 claims 3
- IGAZHQIYONOHQN-UHFFFAOYSA-N Alexa Fluor 555 Chemical compound C=12C=CC(=N)C(S(O)(=O)=O)=C2OC2=C(S(O)(=O)=O)C(N)=CC=C2C=1C1=CC=C(C(O)=O)C=C1C(O)=O IGAZHQIYONOHQN-UHFFFAOYSA-N 0.000 claims 2
- 239000012114 Alexa Fluor 647 Substances 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000002897 diene group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 239000012103 Alexa Fluor 488 Substances 0.000 claims 1
- 239000012109 Alexa Fluor 568 Substances 0.000 claims 1
- 239000012110 Alexa Fluor 594 Substances 0.000 claims 1
- 239000012099 Alexa Fluor family Substances 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 238000005698 Diels-Alder reaction Methods 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm 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
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 102000004243 Tubulin Human genes 0.000 claims 1
- 108090000704 Tubulin Proteins 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 230000001580 bacterial effect Effects 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000007850 fluorescent dye Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 206010061289 metastatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001302 tertiary amino group Chemical group 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063010903P | 2020-04-16 | 2020-04-16 | |
| US63/010,903 | 2020-04-16 | ||
| PCT/US2021/027707 WO2021211984A1 (fr) | 2020-04-16 | 2021-04-16 | Procédés de conjugaison de diels-alder |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023521885A JP2023521885A (ja) | 2023-05-25 |
| JPWO2021211984A5 true JPWO2021211984A5 (fr) | 2024-04-25 |
Family
ID=75870734
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022562664A Pending JP2023521885A (ja) | 2020-04-16 | 2021-04-16 | ディールス－アルダーコンジュゲーション方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US11701427B2 (fr) |
| EP (1) | EP4135775A1 (fr) |
| JP (1) | JP2023521885A (fr) |
| KR (1) | KR20230004651A (fr) |
| CN (1) | CN115968304A (fr) |
| AU (1) | AU2021255711A1 (fr) |
| CA (1) | CA3179154A1 (fr) |
| IL (1) | IL297027A (fr) |
| MX (1) | MX2022012821A (fr) |
| WO (1) | WO2021211984A1 (fr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202406934A (zh) * | 2022-05-03 | 2024-02-16 | 美商建南德克公司 | 抗Ｌｙ６Ｅ抗體、免疫結合物及其用途 |
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| JPS58180487A (ja) | 1982-04-16 | 1983-10-21 | Kyowa Hakko Kogyo Co Ltd | 抗生物質ｄｃ−８１およびその製造法 |
| IL85035A0 (en) | 1987-01-08 | 1988-06-30 | Int Genetic Eng | Polynucleotide molecule,a chimeric antibody with specificity for human b cell surface antigen,a process for the preparation and methods utilizing the same |
| US5208020A (en) | 1989-10-25 | 1993-05-04 | Immunogen Inc. | Cytotoxic agents comprising maytansinoids and their therapeutic use |
| LU91067I2 (fr) | 1991-06-14 | 2004-04-02 | Genentech Inc | Trastuzumab et ses variantes et dérivés immuno chimiques y compris les immotoxines |
| US5663149A (en) | 1994-12-13 | 1997-09-02 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides |
| US5714586A (en) | 1995-06-07 | 1998-02-03 | American Cyanamid Company | Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates |
| US6596541B2 (en) | 2000-10-31 | 2003-07-22 | Regeneron Pharmaceuticals, Inc. | Methods of modifying eukaryotic cells |
| US20070258987A1 (en) | 2000-11-28 | 2007-11-08 | Seattle Genetics, Inc. | Recombinant Anti-Cd30 Antibodies and Uses Thereof |
| JP5064037B2 (ja) | 2004-02-23 | 2012-10-31 | ジェネンテック， インコーポレイテッド | 複素環式自壊的リンカーおよび結合体 |
| AR048098A1 (es) | 2004-03-15 | 2006-03-29 | Wyeth Corp | Conjugados de caliqueamicina |
| EP2286844A3 (fr) | 2004-06-01 | 2012-08-22 | Genentech, Inc. | Conjugués anticorps-médicament et procédés |
| AU2005316844A1 (en) | 2004-11-29 | 2006-06-22 | Seattle Genetics, Inc. | Engineered antibodies and immunoconjugates |
| BRPI0617165B1 (pt) | 2005-10-07 | 2023-10-03 | Exelixis Inc | Compostos inibidores mek, composições farmacêuticas que os contem e métodos de uso dos mesmos |
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| JP2010528285A (ja) | 2007-05-23 | 2010-08-19 | ベンタナ・メデイカル・システムズ・インコーポレーテツド | 免疫組織化学およびｉｎｓｉｔｕハイブリダーゼーションのためのポリマー担体 |
| SG189817A1 (en) | 2008-04-30 | 2013-05-31 | Immunogen Inc | Potent conjugates and hydrophilic linkers |
| ES2536882T3 (es) | 2008-07-21 | 2015-05-29 | Polytherics Limited | Nuevos reactivos y procedimiento de conjugación de moléculas biológicas |
| KR101000067B1 (ko) | 2008-12-30 | 2010-12-10 | 엘지전자 주식회사 | 고효율 태양전지용 레이저 소성장치 및 고효율 태양전지 제조방법 |
| CA2770626A1 (fr) | 2009-08-10 | 2011-02-17 | Mark Smith | Fonctionnalisation de substrats solides |
| JP5972864B2 (ja) | 2010-04-15 | 2016-08-17 | メディミューン リミテッド | ピロロベンゾジアゼピン及びそれらのコンジュゲート |
| WO2012005982A2 (fr) | 2010-07-06 | 2012-01-12 | Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Rapporteur pour une terminaison par la arn polymérase ii |
| KR102434557B1 (ko) | 2010-08-02 | 2022-08-23 | 리제너론 파아마슈티컬스, 인크. | Ｖｌ 도메인을 포함하는 결합 단백질을 생성하는 마우스 |
| MX371526B (es) | 2011-05-27 | 2020-01-31 | Ambrx Inc | Composiciones que contienen, metodos que incluyen, y usos de derivados de dolastatina enlazados a aminoacidos no naturales. |
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| EP3388435B1 (fr) | 2011-10-14 | 2023-05-03 | Seagen Inc. | Pyrrolobenzodiazépines et conjugués ciblés |
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| JP6166728B2 (ja) | 2011-10-14 | 2017-07-19 | 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の製造に有用な合成方法及び中間体 |
| EA036202B1 (ru) | 2011-10-14 | 2020-10-14 | Сиэтл Дженетикс, Инк. | Пирролбензодиазепины и конъюгаты направленного действия |
| WO2013068874A1 (fr) | 2011-11-11 | 2013-05-16 | Pfizer Inc. | Conjugués anticorps-médicament |
| JP2015500287A (ja) | 2011-12-05 | 2015-01-05 | アイジェニカ・バイオセラピューティクス・インコーポレイテッドＩｇｅｎｉｃａ Ｂｉｏｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | 抗体−薬物のコンジュゲート、ならびに関連する化合物、組成物および方法 |
| EP2793949B1 (fr) | 2011-12-23 | 2018-08-22 | Innate Pharma | Conjugaison enzymatique d'anticorps |
| LT3912642T (lt) | 2012-10-23 | 2023-07-25 | Synaffix B.V. | Modifikuotas antikūnas, antikūno konjugatas ir jų gamybos būdas |
| EP2916872B1 (fr) | 2012-11-09 | 2019-02-27 | Innate Pharma | Etiquettes de reconnaissance pour la conjugaison à médiation par la tgase |
| KR102306490B1 (ko) | 2013-03-15 | 2021-09-28 | 리제너론 파아마슈티컬스, 인크. | 생물학적 활성 분자, 그의 접합체 및 치료 용도 |
| KR102252925B1 (ko) | 2013-08-26 | 2021-05-18 | 리제너론 파마슈티칼스 인코포레이티드 | 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 |
| CN106573074B (zh) | 2014-06-02 | 2022-04-12 | 里珍纳龙药品有限公司 | 生物活性分子偶联物、试剂和制备方法及其治疗用途 |
| CN107995912A (zh) | 2015-03-27 | 2018-05-04 | 里珍纳龙药品有限公司 | 美登素类衍生物、其偶联物和使用方法 |
| SG11201806322QA (en) | 2016-01-25 | 2018-08-30 | Regeneron Pharma | Maytansinoid derivatives, conjugates thereof, and methods of use |
| EP3419670A2 (fr) | 2016-02-26 | 2019-01-02 | Regeneron Pharmaceuticals, Inc. | Conjugaison optimisée d'anticorps spécifique d'un site de transglutaminase |
| IL270595B2 (en) | 2017-05-18 | 2023-09-01 | Regeneron Pharma | Bi-octahydrophenanthrene carboxamides and their protein conjugates |
| US12037411B2 (en) | 2018-04-30 | 2024-07-16 | Regeneron Pharmaceuticals, Inc. | Antibodies, and bispecific antigen-binding molecules that bind HER2 and/or APLP2, conjugates, and uses thereof |
-
2021
- 2021-04-16 EP EP21724433.4A patent/EP4135775A1/fr active Pending
- 2021-04-16 KR KR1020227040014A patent/KR20230004651A/ko active Search and Examination
- 2021-04-16 JP JP2022562664A patent/JP2023521885A/ja active Pending
- 2021-04-16 CN CN202180043012.0A patent/CN115968304A/zh active Pending
- 2021-04-16 IL IL297027A patent/IL297027A/en unknown
- 2021-04-16 CA CA3179154A patent/CA3179154A1/fr active Pending
- 2021-04-16 AU AU2021255711A patent/AU2021255711A1/en active Pending
- 2021-04-16 WO PCT/US2021/027707 patent/WO2021211984A1/fr unknown
- 2021-04-16 US US17/232,854 patent/US11701427B2/en active Active
- 2021-04-16 MX MX2022012821A patent/MX2022012821A/es unknown
-
2023
- 2023-05-12 US US18/196,863 patent/US20240207412A1/en active Pending
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