CN103764667B - N‑羧烷基耳他汀类及其应用 - Google Patents
N‑羧烷基耳他汀类及其应用 Download PDFInfo
- Publication number
- CN103764667B CN103764667B CN201280019732.4A CN201280019732A CN103764667B CN 103764667 B CN103764667 B CN 103764667B CN 201280019732 A CN201280019732 A CN 201280019732A CN 103764667 B CN103764667 B CN 103764667B
- Authority
- CN
- China
- Prior art keywords
- formula
- methyl
- compound
- phenyl
- group
- 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[C@](C1NCCC*1)C(*)=C(*)OC Chemical compound C[C@](C1NCCC*1)C(*)=C(*)OC 0.000 description 2
Classifications
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
- A61K47/6415—Toxins or lectins, e.g. clostridial toxins or Pseudomonas exotoxins
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11158481.9 | 2011-03-16 | ||
| EP11158481 | 2011-03-16 | ||
| PCT/EP2012/054294 WO2012123423A1 (de) | 2011-03-16 | 2012-03-12 | N-carboxyalkyl-auristatine und ihre verwendung |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103764667A CN103764667A (zh) | 2014-04-30 |
| CN103764667B true CN103764667B (zh) | 2017-06-20 |
Family
ID=45812791
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280019732.4A Expired - Fee Related CN103764667B (zh) | 2011-03-16 | 2012-03-12 | N‑羧烷基耳他汀类及其应用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9029406B2 (https=) |
| EP (1) | EP2686336B1 (https=) |
| JP (2) | JP6023097B2 (https=) |
| CN (1) | CN103764667B (https=) |
| CA (1) | CA2829736C (https=) |
| ES (1) | ES2543888T3 (https=) |
| WO (1) | WO2012123423A1 (https=) |
Families Citing this family (14)
| 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 |
| KR102023496B1 (ko) * | 2011-04-21 | 2019-09-20 | 시애틀 지네틱스, 인크. | 신규 결합제-약물 콘주게이트 (adc) 및 그의 용도 |
| MY168297A (en) | 2011-11-17 | 2018-10-23 | Pfizer | Cytotoxic Peptides and Antibody Drug Conjugates Thereof |
| US10226535B2 (en) | 2012-12-10 | 2019-03-12 | Mersana Therapeutics, Inc. | Auristatin compounds and conjugates 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 |
| BR112016012538A2 (pt) | 2013-12-17 | 2017-09-26 | Novartis Ag | peptídeos citotóxicos e conjugados dos mesmos |
| RU2729194C2 (ru) | 2013-12-27 | 2020-08-05 | Займворкс Инк. | Сульфонамидсодержащие связывающие системы для лекарственных конъюгатов |
| 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 |
| 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 |
| CN111393346B (zh) * | 2020-06-02 | 2020-08-25 | 凯莱英生命科学技术(天津)有限公司 | N-Boc-Dolaproine及Boc-Dap DCHA的合成方法 |
| MX2024002571A (es) | 2021-09-03 | 2024-03-20 | Toray Industries | Composicion farmaceutica para tratamiento y/o prevencion de cancer. |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002088172A2 (en) * | 2001-04-30 | 2002-11-07 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
| WO2003008378A1 (en) * | 2001-07-19 | 2003-01-30 | F.Hoffmann-La Roche Ag | Dolastatin 10 derivatives |
| WO2005081711A2 (en) * | 2003-11-06 | 2005-09-09 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
Family Cites Families (14)
| 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 |
| WO2003026577A2 (en) | 2001-09-24 | 2003-04-03 | 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 |
| 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 |
| KR20140116546A (ko) | 2006-10-27 | 2014-10-02 | 제넨테크, 인크. | 항체 및 면역접합체 및 이들의 용도 |
| 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 |
| KR102023496B1 (ko) | 2011-04-21 | 2019-09-20 | 시애틀 지네틱스, 인크. | 신규 결합제-약물 콘주게이트 (adc) 및 그의 용도 |
-
2012
- 2012-03-12 US US14/004,699 patent/US9029406B2/en active Active
- 2012-03-12 CN CN201280019732.4A patent/CN103764667B/zh not_active Expired - Fee Related
- 2012-03-12 WO PCT/EP2012/054294 patent/WO2012123423A1/de not_active Ceased
- 2012-03-12 ES ES12708034.9T patent/ES2543888T3/es active Active
- 2012-03-12 EP EP12708034.9A patent/EP2686336B1/de active Active
- 2012-03-12 JP JP2013558400A patent/JP6023097B2/ja active Active
- 2012-03-12 CA CA2829736A patent/CA2829736C/en active Active
-
2016
- 2016-07-25 JP JP2016145282A patent/JP2016185987A/ja not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002088172A2 (en) * | 2001-04-30 | 2002-11-07 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
| WO2003008378A1 (en) * | 2001-07-19 | 2003-01-30 | F.Hoffmann-La Roche Ag | Dolastatin 10 derivatives |
| WO2005081711A2 (en) * | 2003-11-06 | 2005-09-09 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2829736A1 (en) | 2012-09-20 |
| EP2686336B1 (de) | 2015-05-06 |
| US9029406B2 (en) | 2015-05-12 |
| WO2012123423A1 (de) | 2012-09-20 |
| JP6023097B2 (ja) | 2016-11-09 |
| CN103764667A (zh) | 2014-04-30 |
| HK1191034A1 (en) | 2014-07-18 |
| US20140080763A1 (en) | 2014-03-20 |
| CA2829736C (en) | 2020-07-21 |
| JP2016185987A (ja) | 2016-10-27 |
| ES2543888T3 (es) | 2015-08-25 |
| EP2686336A1 (de) | 2014-01-22 |
| JP2014515735A (ja) | 2014-07-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20170620 |