PE20030258A1 - Derivados de dolastatina con actividad antitumoral - Google Patents

Derivados de dolastatina con actividad antitumoral

Info

Publication number
PE20030258A1
PE20030258A1 PE2002000643A PE2002000643A PE20030258A1 PE 20030258 A1 PE20030258 A1 PE 20030258A1 PE 2002000643 A PE2002000643 A PE 2002000643A PE 2002000643 A PE2002000643 A PE 2002000643A PE 20030258 A1 PE20030258 A1 PE 20030258A1
Authority
PE
Peru
Prior art keywords
methyl
butyl
carbamoyl
metoxy
butyramide
Prior art date
Application number
PE2002000643A
Other languages
English (en)
Inventor
Mikio Taniguchi
Takehiro Okada
Toshihiko Fujii
Fumio Watanabe
Original Assignee
Hoffmann La Roche
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20030258A1 publication Critical patent/PE20030258A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A DERIVADOS DE DOLASTATINA 10 QUE TIENEN VARIOS GRUPOS TIO EN LA PARTE DE DOLAPROINA DE FORMULA I DONDE R1, R2, R3 SON H, ALQUILO C1-C4; R4 ES H, ALQUILO OPCIONALMENTE SUSTITUIDO CON HIDROXILO, ALCOXILO, AMINO, DIALQUILAMINO, CARBOXILO, ALCOXICARBONILO, CARBAMOILO, ALQUILCARBONILOXILO, HALOGENO, ALQUENILO, ALQUINILO, CICLOALQUILO C3-C7, ARILO, ENTRE OTROS; R5 ES ALQUILAMINO C1-C6, HIDROXILO, CICLOALQUILAMINO C3-C7, ARILAMINO, ARALQUILAMINO, BENZHIDRAZINO, ENTRE OTROS; n ES 0-2. SON COMPUESTOS PREFERIDOS N-[1-({1-SEC-BUTIL-4-[2-(1-METANOSULFINIL-2-FENETILCARBAMOIL-ETIL)-PIRROLIDIN-1-IL]-2-METOXI-4-OXO-BUTIL}-METIL-CARBAMOIL)-2-METIL-PROPIL]-2-DIMETILAMINO-3-METIL-BUTIRAMIDA; N-[1-({1-SEC-BUTIL-2-METOXI-4-OXO-4-[2-(2-FENETIL-CARBAMOIL-1-FENILSULFANIL-ETIL)-PIRROLIDIN-1-IL]-BUTIL}-METIL-CARBAMOIL)-2-METIL-PROPIL]-2-DIMETILAMINO-3-METIL-BUTIRAMIDA; N-[1-({1-SEC-BUTIL-2-METOXI-4-[2-(1-METILSULFANIL-2-FENETILCARBAMOIL-ETIL)-PIRROLIDIN-1-IL]-4-OXO-BUTIL}-METIL-CARBAMOIL)-2-METIL-PROPIL]-2-DIMETILAMINO-3-METIL-BUTIRAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON DERIVADOS DE DOLASTINA 10, PEPTIDO ANTIMITOTICO POTENTE MUESTRAN ACTIVIDAD ANTITUMORAL MEJORADA Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE CANCER
PE2002000643A 2001-07-19 2002-07-19 Derivados de dolastatina con actividad antitumoral PE20030258A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP01117410 2001-07-19

Publications (1)

Publication Number Publication Date
PE20030258A1 true PE20030258A1 (es) 2003-03-19

Family

ID=8178073

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000643A PE20030258A1 (es) 2001-07-19 2002-07-19 Derivados de dolastatina con actividad antitumoral

Country Status (30)

Country Link
US (1) US6737409B2 (es)
EP (1) EP1412328B1 (es)
JP (1) JP2004534859A (es)
KR (2) KR20060057652A (es)
CN (1) CN1553897A (es)
AR (1) AR036175A1 (es)
AT (1) ATE341537T1 (es)
BR (1) BR0211289A (es)
CA (1) CA2453987A1 (es)
CO (1) CO5550462A2 (es)
DE (1) DE60215179T2 (es)
DK (1) DK1412328T3 (es)
ES (1) ES2272763T3 (es)
GT (1) GT200200154A (es)
HR (1) HRP20040043A2 (es)
HU (1) HUP0401253A2 (es)
IL (1) IL159890A0 (es)
MX (1) MXPA04000577A (es)
MY (1) MY127718A (es)
NO (1) NO20040198L (es)
NZ (1) NZ530655A (es)
PA (1) PA8551001A1 (es)
PE (1) PE20030258A1 (es)
PL (1) PL367682A1 (es)
PT (1) PT1412328E (es)
RU (1) RU2296750C2 (es)
SI (1) SI1412328T1 (es)
UY (1) UY27388A1 (es)
WO (1) WO2003008378A1 (es)
ZA (1) ZA200400334B (es)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7256257B2 (en) 2001-04-30 2007-08-14 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
US7064211B2 (en) 2002-03-22 2006-06-20 Eisai Co., Ltd. Hemiasterlin derivatives and uses thereof
IL163868A0 (en) * 2002-03-22 2005-12-18 Eisai Co Ltd Hermiasterlin derivatives and uses thereof
ES2556641T3 (es) 2002-07-31 2016-01-19 Seattle Genetics, Inc. Conjugados de fármacos y su uso para tratar cáncer, una enfermedad autoinmune o una enfermedad infecciosa
KR101438983B1 (ko) 2003-11-06 2014-09-05 시애틀 지네틱스, 인크. 리간드에 접합될 수 있는 모노메틸발린 화합물
US7312343B2 (en) * 2004-06-02 2007-12-25 Hoffmann-La Roche Inc. Synthesis of α-amino-β-alkoxy-carboxylic acid esters
WO2006132670A2 (en) 2004-11-12 2006-12-14 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the n terminus
EP1828117A1 (en) * 2004-12-13 2007-09-05 F. Hoffmann-Roche AG Novel process for the manufacture of 3-pyrrolidin-2-yl-propionic acid derivatives
EP1827603A2 (en) * 2004-12-13 2007-09-05 F. Hoffmann-Roche AG Novel pharmaceutical composition containing at least one dolastatin 10 derivative
US20060161076A1 (en) * 2005-01-06 2006-07-20 Diamics, Inc. Systems and methods for collection of cell clusters
US20060189893A1 (en) * 2005-01-06 2006-08-24 Diamics, Inc. Systems and methods for detecting abnormal cells
MX2007008349A (es) * 2005-01-13 2007-07-25 Hoffmann La Roche Nueva sintesis de una etapa de aminas disustituidas utiles.
EP1883627B1 (en) 2005-05-18 2018-04-18 Pharmascience Inc. Bir domain binding compounds
EP3498289A1 (en) 2005-07-07 2019-06-19 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the c-terminus
WO2007008848A2 (en) * 2005-07-07 2007-01-18 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the c-terminus
US7750116B1 (en) 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
AU2007250443B2 (en) 2006-05-16 2013-06-13 Pharmascience Inc. IAP BIR domain binding compounds
US20080003652A1 (en) * 2006-06-28 2008-01-03 Hans Iding Novel enzymatic process for the manufacture of Boc-Dap-Oh priority to related application(s)
JP2010533495A (ja) 2007-07-16 2010-10-28 ジェネンテック, インコーポレイテッド ヒト化CD79b抗体およびイムノコンジュゲートならびにそれらの使用
PT2176296E (pt) 2007-07-16 2012-05-14 Genentech Inc Anticorpos e imunoconjugados anti-cd79b e métodos de utilização
MY157403A (en) 2008-01-31 2016-06-15 Genentech Inc Anti-cd79b antibodies and immunoconjugates and methods of use
PL2842575T3 (pl) 2008-03-18 2018-02-28 Seattle Genetics, Inc. Koniugaty aurystatyny lek łącznik
MX341687B (es) 2010-02-10 2016-08-30 Immunogen Inc "anticuerpos cd20 y su utilización".
ES2625637T3 (es) 2010-02-12 2017-07-20 Pharmascience Inc. Compuestos de unión al dominio BIR IAP
JP5791707B2 (ja) 2010-06-10 2015-10-07 シアトル ジェネティックス, インコーポレイテッド 新規アウリスタチン誘導体およびその使用
JP5933562B2 (ja) 2010-09-29 2016-06-15 シアトル ジェネティックス, インコーポレイテッド N−カルボキシアルキル−アウリスタチンおよびその使用
ES2543888T3 (es) * 2011-03-16 2015-08-25 Seattle Genetics, Inc. N-carboxialquil-auristatinas y su utilización
EP3170821B1 (en) * 2011-05-27 2021-09-15 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
JP6581774B2 (ja) * 2011-05-27 2019-09-25 アンブルックス, インコーポレイテッドAmbrx, Inc. 非天然アミノ酸結合ドラスタチン誘導体を含有する化合物またはその化合物の溶媒和物、およびドラスタチンアナログを誘導体化するための方法
ES2604766T3 (es) 2012-09-20 2017-03-09 Celltrion, Inc. Derivado de dolastatina-10, procedimiento de producción del mismo y composición de fármaco anticanceroso que contiene el mismo
ES2916722T3 (es) 2013-12-27 2022-07-05 Zymeworks Inc Sistemas de enlace que contienen sulfonamida para conjugados de fármacos
CA3069221C (en) 2014-09-23 2023-04-04 Genentech, Inc. Methods of using anti-cd79b immunoconjugates
CN105949277B (zh) * 2015-05-05 2019-03-01 成都永泰诺科技有限公司 一种抗肿瘤化合物及其用途
DK3438118T3 (da) * 2016-03-29 2023-05-30 Toray Industries Peptidderivat og anvendelse deraf
CN109021065B (zh) * 2017-06-08 2021-10-01 复旦大学 一种制备海兔毒素Dolastatin10的方法
AU2022338463A1 (en) 2021-09-03 2024-03-21 Toray Industries, Inc. Pharmaceutical composition for cancer treatment and/or prevention

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6323315B1 (en) 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides

Also Published As

Publication number Publication date
NO20040198L (no) 2004-02-19
BR0211289A (pt) 2004-08-03
MXPA04000577A (es) 2004-04-20
WO2003008378A1 (en) 2003-01-30
MY127718A (en) 2006-12-29
GT200200154A (es) 2003-05-16
EP1412328B1 (en) 2006-10-04
US6737409B2 (en) 2004-05-18
US20030055002A1 (en) 2003-03-20
ATE341537T1 (de) 2006-10-15
IL159890A0 (en) 2004-06-20
DK1412328T3 (da) 2007-02-12
CN1553897A (zh) 2004-12-08
JP2004534859A (ja) 2004-11-18
EP1412328A1 (en) 2004-04-28
AR036175A1 (es) 2004-08-18
KR20060057652A (ko) 2006-05-26
HRP20040043A2 (en) 2004-08-31
KR20040023661A (ko) 2004-03-18
ZA200400334B (en) 2005-06-29
KR100611540B1 (ko) 2006-08-10
PA8551001A1 (es) 2003-09-17
HUP0401253A2 (hu) 2004-12-28
DE60215179D1 (de) 2006-11-16
NZ530655A (en) 2006-08-31
PL367682A1 (en) 2005-03-07
SI1412328T1 (sl) 2007-02-28
CA2453987A1 (en) 2003-01-30
ES2272763T3 (es) 2007-05-01
DE60215179T2 (de) 2007-10-18
PT1412328E (pt) 2007-01-31
UY27388A1 (es) 2003-01-31
RU2296750C2 (ru) 2007-04-10
CO5550462A2 (es) 2005-08-31
RU2004105145A (ru) 2005-07-10

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