JP5933562B2 - Ｎ−カルボキシアルキル−アウリスタチンおよびその使用 - Google Patents
Ｎ−カルボキシアルキル−アウリスタチンおよびその使用 Download PDFInfo
- Publication number
- JP5933562B2 JP5933562B2 JP2013530690A JP2013530690A JP5933562B2 JP 5933562 B2 JP5933562 B2 JP 5933562B2 JP 2013530690 A JP2013530690 A JP 2013530690A JP 2013530690 A JP2013530690 A JP 2013530690A JP 5933562 B2 JP5933562 B2 JP 5933562B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- salt
- solvate
- methoxy
- compound
- 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.)
- Expired - Fee Related
Links
- 0 *C(*)(C1)[C@]1c1ccccc1 Chemical compound *C(*)(C1)[C@]1c1ccccc1 0.000 description 10
- XBPCUCUWBYBCDP-UHFFFAOYSA-N C(CC1)CCC1NC1CCCCC1 Chemical compound C(CC1)CCC1NC1CCCCC1 XBPCUCUWBYBCDP-UHFFFAOYSA-N 0.000 description 1
- IOCIZCDYZMWHIB-XPFSCBSXSA-N CC[C@H](C)C([C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@@H]([C@@H](C)O)C(NCc1ccccc1)=O)=O)OC)=O)OC)/C=C(\C)/C([C@H](C(C)C)NC([C@H](C(C)C)N(C)CCCC(O)=O)=O)=O Chemical compound CC[C@H](C)C([C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@@H]([C@@H](C)O)C(NCc1ccccc1)=O)=O)OC)=O)OC)/C=C(\C)/C([C@H](C(C)C)NC([C@H](C(C)C)N(C)CCCC(O)=O)=O)=O IOCIZCDYZMWHIB-XPFSCBSXSA-N 0.000 description 1
- NMXJXIUNOSSCCL-BSIAYEFVSA-N CC[C@H](C)[C@H](CC(C)CC([C@H](C(C)C)NC([C@H](C(C)C)N(C)CCCC(O)=O)=O)=O)[C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@@H](Cc1ccccc1)C(N)=O)=O)OC)=O)OC Chemical compound CC[C@H](C)[C@H](CC(C)CC([C@H](C(C)C)NC([C@H](C(C)C)N(C)CCCC(O)=O)=O)=O)[C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@@H](Cc1ccccc1)C(N)=O)=O)OC)=O)OC NMXJXIUNOSSCCL-BSIAYEFVSA-N 0.000 description 1
- FXWWKUWOOAUKGC-KNFINWGESA-N CC[C@H](C)[C@H](CCC(C)C([C@H](C(C)C)NC(C(C(C)C)N(C)CCCC(O)=O)=O)=O)[C@@H](CC(N(CCC1)[C@@H]1C([C@@H](C)C(N[C@@H](Cc1ccccc1)C(OCC1=CCC(C)C=C1)=O)=O)OC)=O)OC Chemical compound CC[C@H](C)[C@H](CCC(C)C([C@H](C(C)C)NC(C(C(C)C)N(C)CCCC(O)=O)=O)=O)[C@@H](CC(N(CCC1)[C@@H]1C([C@@H](C)C(N[C@@H](Cc1ccccc1)C(OCC1=CCC(C)C=C1)=O)=O)OC)=O)OC FXWWKUWOOAUKGC-KNFINWGESA-N 0.000 description 1
- LNEHHTWYEBGHBY-OUAUKWLOSA-N C[C@H]([C@H]([C@H](CCC1)N1C(OC(C)(C)C)=O)OC)C(O)=O Chemical compound C[C@H]([C@H]([C@H](CCC1)N1C(OC(C)(C)C)=O)OC)C(O)=O LNEHHTWYEBGHBY-OUAUKWLOSA-N 0.000 description 1
Classifications
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1021—Tetrapeptides with the first amino acid being acidic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
- C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
- C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Analytical Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10181966 | 2010-09-29 | ||
| EP10181966.2 | 2010-09-29 | ||
| EP11158466.0 | 2011-03-16 | ||
| EP11158466 | 2011-03-16 | ||
| PCT/EP2011/066658 WO2012041805A1 (de) | 2010-09-29 | 2011-09-26 | N-carboxyalkyl-auristatine und ihre verwendung |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013540114A JP2013540114A (ja) | 2013-10-31 |
| JP2013540114A5 JP2013540114A5 (https=) | 2014-09-18 |
| JP5933562B2 true JP5933562B2 (ja) | 2016-06-15 |
Family
ID=44674811
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013530690A Expired - Fee Related JP5933562B2 (ja) | 2010-09-29 | 2011-09-26 | Ｎ−カルボキシアルキル−アウリスタチンおよびその使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US8987209B2 (https=) |
| EP (1) | EP2621508B1 (https=) |
| JP (1) | JP5933562B2 (https=) |
| CN (1) | CN103379912B (https=) |
| CA (1) | CA2813056C (https=) |
| ES (1) | ES2553874T3 (https=) |
| WO (1) | WO2012041805A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8987209B2 (en) | 2010-09-29 | 2015-03-24 | Seattle Genetics, Inc. | N-carboxyalkyl-auristatin and the use thereof |
| US9029406B2 (en) | 2011-03-16 | 2015-05-12 | Seattle Genetics, Inc | N-carboxyalkylauristatins and use thereof |
| KR102023496B1 (ko) * | 2011-04-21 | 2019-09-20 | 시애틀 지네틱스, 인크. | 신규 결합제-약물 콘주게이트 (adc) 및 그의 용도 |
| US9981046B2 (en) | 2012-05-15 | 2018-05-29 | Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. | Drug-conjugates, conjugation methods, and uses thereof |
| FR3005051A1 (fr) * | 2013-04-25 | 2014-10-31 | Pf Medicament | Derives de la dolastatine 10 et d'auristatines |
| 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 |
| WO2015057876A1 (en) | 2013-10-15 | 2015-04-23 | Sorrento Therapeutics Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| BR112016012538A2 (pt) | 2013-12-17 | 2017-09-26 | Novartis Ag | peptídeos citotóxicos e conjugados dos mesmos |
| RU2692563C2 (ru) | 2014-04-25 | 2019-06-25 | Пьер Фабр Медикамент | Конъюгат антитела против igf-1r с лекарственным средством и его применение для лечения рака |
| BR112016024363A2 (pt) | 2014-04-25 | 2017-10-10 | Pf Medicament | conjugado de anticorpo-fármaco e seu uso para tratamento de câncer |
| CN106573956A (zh) | 2014-06-13 | 2017-04-19 | 诺华股份有限公司 | 澳瑞他汀衍生物及其缀合物 |
| EP3160513B1 (en) | 2014-06-30 | 2020-02-12 | Glykos Finland Oy | Saccharide derivative of a toxic payload and antibody conjugates thereof |
| EP3250238B1 (en) | 2015-01-28 | 2022-06-01 | Sorrento Therapeutics, Inc. | Antibody drug conjugates |
| CN106279352B (zh) | 2015-05-29 | 2020-05-22 | 上海新理念生物医药科技有限公司 | 海兔毒素10的衍生物及其应用 |
| EP3554544A4 (en) | 2016-12-16 | 2020-07-29 | Bluefin Biomedicine, Inc. | ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE |
| EP3725798B1 (en) * | 2017-12-15 | 2026-03-04 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Bioactive conjugate, preparation method therefor and use thereof |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO1999035164A1 (en) | 1998-01-09 | 1999-07-15 | Arizona Board Of Regents, A Body Corporate, Acting On Behalf Of Arizona State University | Anti-cryptococcal peptides |
| CA2370245A1 (en) | 1999-05-14 | 2000-11-23 | Boehringer Ingelheim Pharmaceuticals, Inc. | Enzyme-activated anti-tumor prodrug compounds |
| US6323315B1 (en) | 1999-09-10 | 2001-11-27 | Basf Aktiengesellschaft | Dolastatin peptides |
| US6884869B2 (en) | 2001-04-30 | 2005-04-26 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
| US6737409B2 (en) | 2001-07-19 | 2004-05-18 | Hoffmann-La Roche Inc. | Dolastatin 10 derivatives |
| WO2003026577A2 (en) | 2001-09-24 | 2003-04-03 | Seattle Genetics, Inc. | P-amidobenzylethers in drug delivery agents |
| US7091186B2 (en) | 2001-09-24 | 2006-08-15 | Seattle Genetics, Inc. | p-Amidobenzylethers in drug delivery agents |
| SI1545613T1 (sl) | 2002-07-31 | 2011-11-30 | Seattle Genetics Inc | Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni |
| US7498298B2 (en) | 2003-11-06 | 2009-03-03 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
| WO2006132670A2 (en) | 2004-11-12 | 2006-12-14 | Seattle Genetics, Inc. | Auristatins having an aminobenzoic acid unit at the n terminus |
| JP5171621B2 (ja) | 2005-07-07 | 2013-03-27 | シアトル ジェネティックス， インコーポレイテッド | フェニルアラニン側鎖修飾をｃ末端に有するモノメチルバリン化合物 |
| US8871720B2 (en) | 2005-07-07 | 2014-10-28 | Seattle Genetics, Inc. | Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus |
| CN101573384B (zh) * | 2006-10-27 | 2013-02-20 | 健泰科生物技术公司 | 抗体和免疫偶联物及其用途 |
| KR20140116546A (ko) * | 2006-10-27 | 2014-10-02 | 제넨테크, 인크. | 항체 및 면역접합체 및 이들의 용도 |
| JP5394246B2 (ja) * | 2007-03-30 | 2014-01-22 | ジェネンテック， インコーポレイテッド | 抗体及びイムノコンジュゲートとこれらの使用方法 |
| EP2265283B1 (en) | 2008-03-18 | 2014-09-03 | Seattle Genetics, Inc. | Auristatin drug linker conjugates |
| CN103200950B (zh) | 2010-06-10 | 2016-03-16 | 西雅图基因公司 | 新颖的耳他汀衍生物及其用途 |
| US8987209B2 (en) | 2010-09-29 | 2015-03-24 | Seattle Genetics, Inc. | N-carboxyalkyl-auristatin and the use thereof |
| US9029406B2 (en) | 2011-03-16 | 2015-05-12 | Seattle Genetics, Inc | N-carboxyalkylauristatins and use thereof |
| KR102023496B1 (ko) | 2011-04-21 | 2019-09-20 | 시애틀 지네틱스, 인크. | 신규 결합제-약물 콘주게이트 (adc) 및 그의 용도 |
| AU2012351685A1 (en) | 2011-12-14 | 2014-07-03 | Seattle Genetics, Inc. | FGFR antibody drug conjugates (ADCs) and the use thereof |
-
2011
- 2011-09-26 US US13/876,777 patent/US8987209B2/en active Active
- 2011-09-26 CA CA2813056A patent/CA2813056C/en not_active Expired - Fee Related
- 2011-09-26 JP JP2013530690A patent/JP5933562B2/ja not_active Expired - Fee Related
- 2011-09-26 EP EP11760500.6A patent/EP2621508B1/de not_active Not-in-force
- 2011-09-26 ES ES11760500.6T patent/ES2553874T3/es active Active
- 2011-09-26 CN CN201180057131.8A patent/CN103379912B/zh not_active Expired - Fee Related
- 2011-09-26 WO PCT/EP2011/066658 patent/WO2012041805A1/de not_active Ceased
-
2015
- 2015-02-05 US US14/615,005 patent/US20150148298A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| ES2553874T3 (es) | 2015-12-14 |
| EP2621508B1 (de) | 2015-08-26 |
| CN103379912B (zh) | 2016-03-16 |
| WO2012041805A1 (de) | 2012-04-05 |
| EP2621508A1 (de) | 2013-08-07 |
| HK1187527A1 (en) | 2014-04-11 |
| JP2013540114A (ja) | 2013-10-31 |
| US20130261064A1 (en) | 2013-10-03 |
| US8987209B2 (en) | 2015-03-24 |
| US20150148298A1 (en) | 2015-05-28 |
| CA2813056C (en) | 2018-09-18 |
| CA2813056A1 (en) | 2012-04-05 |
| CN103379912A (zh) | 2013-10-30 |
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