CO5550462A2 - Derivados de dolastatina 10 - Google Patents

Derivados de dolastatina 10

Info

Publication number
CO5550462A2
CO5550462A2 CO04003736A CO04003736A CO5550462A2 CO 5550462 A2 CO5550462 A2 CO 5550462A2 CO 04003736 A CO04003736 A CO 04003736A CO 04003736 A CO04003736 A CO 04003736A CO 5550462 A2 CO5550462 A2 CO 5550462A2
Authority
CO
Colombia
Prior art keywords
amino
dioxolyl
alkyl
alkoxy
optionally substituted
Prior art date
Application number
CO04003736A
Other languages
English (en)
Inventor
Toshihiko Fujii
Takehiro Okada
Mikio Taniguchi
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 CO5550462A2 publication Critical patent/CO5550462A2/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)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

1.- Un compuesto de la fórmula (I),en dondeR1, R2 y R3 son cada uno independientemente hidrógeno o(C1-C4)-alquilo;R4 es hidrógeno;alquilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en hidroxilo, alcoxilo, amino, mono- o di-alquilamino, carboxilo, alcoxicarbonilo, carbamoiloxilo, alquilcarboniloxilo, carbamoilo, o halógeno; alquenilo; alquinilo;(C3-C7)-cicloalquilo;arilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en halógeno, alcoxicarbonilo, carbamoilo, sulfamoilo, alquil-carboniloxilo,ciano, rnono- o di-alquilamino, alquilo, alcoxilo, fenilo, fenoxilo, trifluorometilo, trifluorometoxilo, tioalquilo, hidroxilo, alquilcarbonil-amino, heterociclilo, 1,3-dioxolilo, 1,4-dioxolilo, amino o bencilo; aralquilo con el grupo arilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en halógeno, alcoxicarbonilo, sulfamoílo, alquilcarboniloxilo, ciano, mono- o di-alquil-amino, alquilo, alcoxilo, fenilo, fenoxilo, trifluorometilo, trifluoro-metoxilo, tioalquilo, hidroxilo, alquilcarbonilamino, heterociclilo, 1,3-dioxolilo, 1,4-dioxolilo, amino o bencilo; oheterociclilalquilo;R5 es (C1-C6)-alquilamino; hidroxilo;(C3-C7)-cicloalquilamino sustituido opcionalmente por fenilo o bencilo;arilamino;aralquilamino con (C1-C4)-alquileno y el grupo arilo sustituido opcionalmente con uno a tres sustituyentes seleccionados del grupo consistente en halógeno, alcoxicarbonilo, sulfamoilo, alquilcarboniloxilo, carbamoiloxilo, ciano, mono- o di-alquilamino, alquilo, alcoxilo, fenilo, fenoxilo, trifluorometilo, trifluorometoxilo, tioalquilo, hidroxilo, alquilcarbonil-amino, heterociclilo, 1,3-dioxolilo, 1,4-dioxolilo, amino o bencilo;(C1-C4)-alcoxilo; benzhidrazino; ...
CO04003736A 2001-07-19 2004-01-20 Derivados de dolastatina 10 CO5550462A2 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CO5550462A2 true CO5550462A2 (es) 2005-08-31

Family

ID=8178073

Family Applications (1)

Application Number Title Priority Date Filing Date
CO04003736A CO5550462A2 (es) 2001-07-19 2004-01-20 Derivados de dolastatina 10

Country Status (30)

Country Link
US (1) US6737409B2 (es)
EP (1) EP1412328B1 (es)
JP (1) JP2004534859A (es)
KR (2) KR100611540B1 (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)

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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
WO2003082268A2 (en) 2002-03-22 2003-10-09 Eisai Co. Ltd Hemiasterlin derivatives and uses thereof in the treatment of cancer
EP2357006B1 (en) 2002-07-31 2015-09-16 Seattle Genetics, Inc. Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease
EP3120861B1 (en) 2003-11-06 2018-08-15 Seattle Genetics, Inc. Intermediate for conjugate preparation comprising auristatin derivatives and a linker
EP1756038A1 (en) * 2004-06-02 2007-02-28 F.Hoffmann-La Roche Ag Synthesis of amino-alkoxy-heptanoic alkyl ester
ES2715776T3 (es) 2004-11-12 2019-06-06 Seattle Genetics Inc Auristatinas que tienen una unidad de ácido aminobenzoico en el extremo N
KR20070086123A (ko) * 2004-12-13 2007-08-27 에프. 호프만-라 로슈 아게 하나 이상의 돌라스타틴 10 유도체를 포함하는 신규 약학조성물
MX2007006746A (es) * 2004-12-13 2007-07-09 Hoffmann La Roche Proceso novedoso para la manufactura de derivados del acido 3-pirrolidin-2-il-propionico.
US20060189893A1 (en) * 2005-01-06 2006-08-24 Diamics, Inc. Systems and methods for detecting abnormal cells
US20060161076A1 (en) * 2005-01-06 2006-07-20 Diamics, Inc. Systems and methods for collection of cell clusters
MX2007008349A (es) * 2005-01-13 2007-07-25 Hoffmann La Roche Nueva sintesis de una etapa de aminas disustituidas utiles.
WO2006122408A1 (en) 2005-05-18 2006-11-23 Aegera Therapeutics Inc. Bir domain binding compounds
WO2007008603A1 (en) * 2005-07-07 2007-01-18 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the c-terminus
US8871720B2 (en) * 2005-07-07 2014-10-28 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
JP5419685B2 (ja) 2006-05-16 2014-02-19 ファーマサイエンス・インコーポレイテッド Iapbirドメイン結合タンパク質
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)
SG183023A1 (en) 2007-07-16 2012-08-30 Genentech Inc Anti-cd79b antibodies and immunoconjugates and methods of use
RU2557319C2 (ru) 2007-07-16 2015-07-20 Дженентек, Инк. ГУМАНИЗИРОВАННЫЕ АНТИТЕЛА ПРОТИВ CD79b И ИММУНОКОНЪЮГАТЫ И СПОСОБЫ ПРИМЕНЕНИЯ
CN101981055B (zh) 2008-01-31 2016-03-09 健泰科生物技术公司 抗cd79b抗体和免疫偶联物及使用方法
ES2647927T3 (es) 2008-03-18 2017-12-27 Seattle Genetics, Inc. Conjugados enlazadores del fármaco auriestatina
WO2011100403A1 (en) 2010-02-10 2011-08-18 Immunogen, Inc Cd20 antibodies and uses thereof
EP2534170B1 (en) 2010-02-12 2017-04-19 Pharmascience Inc. Iap bir domain binding compounds
EP2579887B1 (de) 2010-06-10 2014-11-12 Seattle Genetics, Inc. Neue auristatin-derivate und ihre verwendung
ES2553874T3 (es) 2010-09-29 2015-12-14 Seattle Genetics, Inc. N-Carboxialquil-auristatinas y su uso
CN103764667B (zh) * 2011-03-16 2017-06-20 西雅图基因公司 N‑羧烷基耳他汀类及其应用
ES2690993T3 (es) 2011-05-27 2018-11-23 Ambrx, Inc. Composiciones que contienen y métodos que implican derivados de dolastatina enlazados con aminoácidos no naturales y usos de los mismos
EP2714685B1 (en) * 2011-05-27 2016-10-19 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
AU2013318779B2 (en) 2012-09-20 2016-07-28 Celltrion, Inc. Dolastatin-10 derivative, method of producing the same and anticancer drug composition containing the same
MX2016008444A (es) 2013-12-27 2017-01-11 Zymeworks Inc Sistemas de enlace que contienen sulfonamida para conjugados de farmacos.
WO2016049214A1 (en) 2014-09-23 2016-03-31 Genentech, Inc. METHOD 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
PT3438118T (pt) * 2016-03-29 2023-06-07 Toray Industries Derivado de peptídeo e utilização deste
CN109021065B (zh) * 2017-06-08 2021-10-01 复旦大学 一种制备海兔毒素Dolastatin10的方法
WO2023033129A1 (ja) 2021-09-03 2023-03-09 東レ株式会社 癌の治療及び/又は予防用医薬組成物

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
DE60215179D1 (de) 2006-11-16
US6737409B2 (en) 2004-05-18
RU2296750C2 (ru) 2007-04-10
ZA200400334B (en) 2005-06-29
CA2453987A1 (en) 2003-01-30
GT200200154A (es) 2003-05-16
PL367682A1 (en) 2005-03-07
ES2272763T3 (es) 2007-05-01
KR20060057652A (ko) 2006-05-26
NO20040198L (no) 2004-02-19
MXPA04000577A (es) 2004-04-20
SI1412328T1 (sl) 2007-02-28
ATE341537T1 (de) 2006-10-15
JP2004534859A (ja) 2004-11-18
DE60215179T2 (de) 2007-10-18
PA8551001A1 (es) 2003-09-17
DK1412328T3 (da) 2007-02-12
KR20040023661A (ko) 2004-03-18
EP1412328B1 (en) 2006-10-04
UY27388A1 (es) 2003-01-31
RU2004105145A (ru) 2005-07-10
US20030055002A1 (en) 2003-03-20
WO2003008378A1 (en) 2003-01-30
BR0211289A (pt) 2004-08-03
NZ530655A (en) 2006-08-31
MY127718A (en) 2006-12-29
HUP0401253A2 (hu) 2004-12-28
AR036175A1 (es) 2004-08-18
EP1412328A1 (en) 2004-04-28
IL159890A0 (en) 2004-06-20
CN1553897A (zh) 2004-12-08
PE20030258A1 (es) 2003-03-19
KR100611540B1 (ko) 2006-08-10
HRP20040043A2 (en) 2004-08-31
PT1412328E (pt) 2007-01-31

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