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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Crystallography & Structural Chemistry (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 |
|---|---|---|---|
| EP10181966.2 | 2010-09-29 | ||
| EP10181966 | 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 (enExample) | 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 (enExample) |
| EP (1) | EP2621508B1 (enExample) |
| JP (1) | JP5933562B2 (enExample) |
| CN (1) | CN103379912B (enExample) |
| CA (1) | CA2813056C (enExample) |
| ES (1) | ES2553874T3 (enExample) |
| WO (1) | WO2012041805A1 (enExample) |
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 |
| ES2543888T3 (es) | 2011-03-16 | 2015-08-25 | Seattle Genetics, Inc. | N-carboxialquil-auristatinas y su utilización |
| SG194567A1 (en) * | 2011-04-21 | 2013-12-30 | Seattle Genetics Inc | Novel binder-drug conjugates (adcs) and their use |
| CN104640572B (zh) | 2012-05-15 | 2018-04-27 | 索伦托医疗有限公司 | 药物偶联物，偶联方法，及其用途 |
| 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 |
| AU2014337317A1 (en) | 2013-10-15 | 2016-09-15 | Sorrento Therapeutics Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| WO2015095301A2 (en) | 2013-12-17 | 2015-06-25 | Irm Llc | Cytotoxic peptides and conjugates thereof |
| MA39909B1 (fr) | 2014-04-25 | 2019-05-31 | Pf Medicament | Conjugué anticorps de l'igf-1r-médicament et son utilisation pour le traitement du cancer |
| MX378281B (es) | 2014-04-25 | 2025-03-10 | Pf Medicament | Conjugado farmaco-anticuerpo y su uso para el tratamiento contra el cancer. |
| US9884817B2 (en) | 2014-06-13 | 2018-02-06 | Novartis Ag | Auristatin derivatives and conjugates thereof |
| US10973920B2 (en) | 2014-06-30 | 2021-04-13 | Glykos Finland Oy | Saccharide derivative of a toxic payload and antibody conjugates thereof |
| JP6871858B2 (ja) | 2015-01-28 | 2021-05-19 | ソレント・セラピューティクス・インコーポレイテッドＳｏｒｒｅｎｔｏ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | 抗体薬物コンジュゲート |
| 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 |
| CN119219654A (zh) * | 2017-12-15 | 2024-12-31 | 四川科伦博泰生物医药股份有限公司 | 生物活性物偶联物及其制备方法和用途 |
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 |
| ATE284412T1 (de) | 1998-01-09 | 2004-12-15 | Univ Arizona State | Anti-kryptokokkus peptide |
| MXPA01011502A (es) | 1999-05-14 | 2003-08-20 | Boehringer Ingelheim Pharma | Compuestos de tipo profarmaco anti-tumorigenos, activados por enzimas. |
| 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 |
| ES2369542T3 (es) | 2002-07-31 | 2011-12-01 | Seattle Genetics, Inc. | Conjugados de auristatina y su uso para tratar cáncer, una enfermedad autoinmune o una enfermedad infecciosa. |
| ES2605443T3 (es) | 2003-11-06 | 2017-03-14 | Seattle Genetics, Inc. | Conjugados de auristatina con anticuerpos anti-HER2 o anti-CD22 y su uso en terapia |
| JP2008519863A (ja) | 2004-11-12 | 2008-06-12 | シアトル ジェネティクス インコーポレイティッド | Ｎ末端にアミノ安息香酸単位を有するオーリスタチン |
| ES2708763T3 (es) | 2005-07-07 | 2019-04-11 | Seattle Genetics Inc | Compuestos de monometilvalina que tienen modificaciones de la cadena lateral de fenilalanina en el extremo C |
| WO2007008848A2 (en) | 2005-07-07 | 2007-01-18 | Seattle Genetics, Inc. | Monomethylvaline compounds having phenylalanine carboxy modifications at the c-terminus |
| PT2845866T (pt) | 2006-10-27 | 2017-08-09 | Genentech Inc | Anticorpos e imunoconjugados e utilizações dos mesmos |
| ZA200902161B (en) * | 2006-10-27 | 2010-06-30 | Genentech Inc | Antiobodies and immunoconjugates and uses therefor |
| 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 |
| WO2009117531A1 (en) | 2008-03-18 | 2009-09-24 | 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 |
| ES2543888T3 (es) | 2011-03-16 | 2015-08-25 | Seattle Genetics, Inc. | N-carboxialquil-auristatinas y su utilización |
| SG194567A1 (en) | 2011-04-21 | 2013-12-30 | Seattle Genetics Inc | Novel binder-drug conjugates (adcs) and their use |
| MX2014007121A (es) | 2011-12-14 | 2014-09-04 | Seattle Genetics Inc | Nuevos conjugados de principio activo-ligante (adc) y su uso. |
-
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 CN CN201180057131.8A patent/CN103379912B/zh not_active Expired - Fee Related
- 2011-09-26 ES ES11760500.6T patent/ES2553874T3/es active Active
- 2011-09-26 EP EP11760500.6A patent/EP2621508B1/de not_active Not-in-force
- 2011-09-26 WO PCT/EP2011/066658 patent/WO2012041805A1/de not_active Ceased
- 2011-09-26 JP JP2013530690A patent/JP5933562B2/ja not_active Expired - Fee Related
-
2015
- 2015-02-05 US US14/615,005 patent/US20150148298A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| HK1187527A1 (en) | 2014-04-11 |
| EP2621508B1 (de) | 2015-08-26 |
| WO2012041805A1 (de) | 2012-04-05 |
| CN103379912B (zh) | 2016-03-16 |
| ES2553874T3 (es) | 2015-12-14 |
| CA2813056C (en) | 2018-09-18 |
| CA2813056A1 (en) | 2012-04-05 |
| JP2013540114A (ja) | 2013-10-31 |
| US20150148298A1 (en) | 2015-05-28 |
| US20130261064A1 (en) | 2013-10-03 |
| US8987209B2 (en) | 2015-03-24 |
| CN103379912A (zh) | 2013-10-30 |
| EP2621508A1 (de) | 2013-08-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP5791707B2 (ja) | 新規アウリスタチン誘導体およびその使用 | |
| JP2013540114A (ja) | Ｎ−カルボキシアルキル−アウリスタチンおよびその使用 | |
| JP6023097B2 (ja) | Ｎカルボキシアルキルオーリスタチンおよびその使用 | |
| AU2025267536A1 (en) | Specific conjugation linkers, specific immunoconjugates thereof, methods of making and uses such conjugates thereof | |
| WO2012143496A2 (de) | Neue binder-wirkstoff konjugate (adcs) und ihre verwendung | |
| EP2790731A2 (de) | Fgfr-binder-wirkstoff konjugate und ihre verwendung | |
| TW202330539A (zh) | 用於治療、預防或管理過度增生性病症之化合物、醫藥組合物及方法 | |
| HK1184363B (en) | Novel auristatin derivatives and use thereof | |
| HK40049734B (en) | Cytostatic conjugates with integrin ligands | |
| HK1191034B (en) | N-carboxyalkyl-auristatins and use thereof | |
| HK1187527B (en) | N-carboxyalkyl auristatins and the use thereof | |
| NZ625745B2 (en) | FGFR antibody drug conjugates (ADCs) and the use thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140801 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20140801 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20150917 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20151215 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20160407 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20160502 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 5933562 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| S533 | Written request for registration of change of name |
Free format text: JAPANESE INTERMEDIATE CODE: R313533 |
|
| R350 | Written notification of registration of transfer |
Free format text: JAPANESE INTERMEDIATE CODE: R350 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |