ES2061166T3 - Moleculas ligantes labiles por acido. - Google Patents

Moleculas ligantes labiles por acido.

Info

Publication number
ES2061166T3
ES2061166T3 ES91203439T ES91203439T ES2061166T3 ES 2061166 T3 ES2061166 T3 ES 2061166T3 ES 91203439 T ES91203439 T ES 91203439T ES 91203439 T ES91203439 T ES 91203439T ES 2061166 T3 ES2061166 T3 ES 2061166T3
Authority
ES
Spain
Prior art keywords
low
aralquilo
bajo
alkylene
aryl
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 - Lifetime
Application number
ES91203439T
Other languages
English (en)
Inventor
Petrus Johannes Boon
Franciscus Michael Kaspersen
Ebo Sybren Bos
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Akzo Nobel NV
Original Assignee
Akzo Nobel NV
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 Akzo Nobel NV filed Critical Akzo Nobel NV
Application granted granted Critical
Publication of ES2061166T3 publication Critical patent/ES2061166T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/60Two oxygen atoms, e.g. succinic anhydride
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/24Condensed ring systems having three or more rings
    • C07H15/252Naphthacene radicals, e.g. daunomycins, adriamycins

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Ultra Sonic Daignosis Equipment (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Mushroom Cultivation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

ESTA INVENCION SE REFIERE AL CAMPO DE LA INMUNOTERAPIA DEL CANCER, MAS ESPECIFICAMENTE A INMUNOCONJUGADOS DE MEDIO CITITOXICO CON UN MEDIO OBJETIVO, Y MAS ESPECIFICAMENTE A INMUNOCONJUGADOS DE ANTICUERPOS O FRAGMENTOS O DERIVADOS FUNCIONALES DE ANTICUERPOS ACOPLADOS A UNA SUSTANCIA CITOTOXICA TALES COMO DROGAS, TOXINAS O RADIOISOTOPOS. ESPECIALMENTE SE REFIERE A LA EMISION DE SUSTANCIAS LIGADAS A UN MEDIO OBJETIVO A TRAVES DE LA UTILIZACION DE MOLECULAS ENLACE CON ACIDO DERIVADOS DE COMPUESTOS DE LA FORMULA I: DONDE: R1 = H, ALQUILO BAJO, ALQUILO -N-BAJO; ALQUILO -O-BAJO; ALQUILO -S-BAJO; ARALQUILO -O-BAJO; ARALQUILO -S-BAJO; ARALQUILO -N-BAJO; ALQUILENO -O-BAJO; ALQUILENO -N-BAJO; ALQUILENO -S-BAJO; ARILO -N-BAJO: ARILO -O-BAJO; ARILO -S-BAJO; R2 = H, ALQUILO BAJO; ARALQUILO BAJO; ARILO BAJO; R3 ES: U OTRA ESTRUCTURA QUIMICA QUE SEA CAPAZ DE DECOLIZAR EL PAR DE ELECTRONES IONICOS DEL NITROGENO Y R4 ES UN GRUPO ACTIVO, CAPAZ DE LIGAR R3 A UNA MOLECULA PORTADORA, UNA SUSTANCIA PROTEINICA, UNANTICUERPO (FRAGMENTO), UN POLIMERO O UN ACIDO NUCLEICO.
ES91203439T 1990-12-31 1991-12-30 Moleculas ligantes labiles por acido. Expired - Lifetime ES2061166T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP90203526 1990-12-31

Publications (1)

Publication Number Publication Date
ES2061166T3 true ES2061166T3 (es) 1994-12-01

Family

ID=8205218

Family Applications (1)

Application Number Title Priority Date Filing Date
ES91203439T Expired - Lifetime ES2061166T3 (es) 1990-12-31 1991-12-30 Moleculas ligantes labiles por acido.

Country Status (17)

Country Link
US (1) US5306809A (es)
EP (1) EP0495265B1 (es)
JP (1) JPH04334377A (es)
KR (1) KR920012063A (es)
AT (1) ATE109476T1 (es)
AU (1) AU646121B2 (es)
CA (1) CA2058595A1 (es)
DE (1) DE69103255T2 (es)
DK (1) DK0495265T3 (es)
ES (1) ES2061166T3 (es)
FI (1) FI101678B1 (es)
HU (1) HUT60484A (es)
IE (1) IE65406B1 (es)
NO (1) NO180417C (es)
NZ (1) NZ241217A (es)
PT (1) PT99954B (es)
ZA (1) ZA9110203B (es)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5505931A (en) * 1993-03-04 1996-04-09 The Dow Chemical Company Acid cleavable compounds, their preparation and use as bifunctional acid-labile crosslinking agents
EP0638583A1 (en) * 1993-08-13 1995-02-15 Hoechst Aktiengesellschaft Aminosugar active substances, a process for their preparation and use as pharmaceuticals
DE4433890C2 (de) * 1994-09-22 1999-02-18 Deutsches Krebsforsch Konjugat aus einem Wirkstoff und einem nicht als körperfremd angesehenen, nativen Protein
EP0871490B1 (en) * 1995-12-22 2003-03-19 Bristol-Myers Squibb Company Branched hydrazone linkers
DE19636889A1 (de) 1996-09-11 1998-03-12 Felix Dr Kratz Antineoplastisch wirkende Transferrin- und Albuminkonjugate zytostatischer Verbindungen aus der Gruppe der Anthrazykline, Alkylantien, Antimetabolite und Cisplatin-Analoga und diese enthaltende Arzneimittel
US6030997A (en) * 1998-01-21 2000-02-29 Eilat; Eran Acid labile prodrugs
US6800616B2 (en) * 1998-02-26 2004-10-05 Supergen, Inc. Treatment of HIV infections
CA2248592A1 (en) * 1998-08-31 2000-02-29 Christopher D. Batich Microspheres for use in the treatment of cancer
US6140015A (en) * 1998-12-10 2000-10-31 International Business Machines Corporation Photoresist compositions with pendant polar-functionalized aromatic groups and acid-labile branching
TWI242000B (en) * 1998-12-10 2005-10-21 Univ Southern California Reversible aqueous pH sensitive lipidizing reagents, compositions and methods of use
CA2358420C (en) * 1999-03-11 2010-03-16 Ardenia Investments Ltd. New compounds for the treatment of cancer
US6706892B1 (en) 1999-09-07 2004-03-16 Conjuchem, Inc. Pulmonary delivery for bioconjugation
BRPI0003386B8 (pt) * 2000-08-08 2021-05-25 Cristalia Produtos Quim Farmaceuticos Ltda pró-droga homo ou heterodiméricas úteis no tratamento de doenças ou disfunções mediadas por fosfodiesterases; composições farmacêuticas contendo a pró-droga ou seus sais farmacêuticos aceitáveis; processo de obtenção destas pró-drogas
CZ20031262A3 (en) * 2000-10-16 2004-03-17 Neopharm, Inc. Liposomal formulation of mitoxantrone
US7589180B2 (en) 2001-05-11 2009-09-15 Abbott Laboratories Inc. Specific binding proteins and uses thereof
US20100056762A1 (en) 2001-05-11 2010-03-04 Old Lloyd J Specific binding proteins and uses thereof
GB0116143D0 (en) * 2001-07-02 2001-08-22 Amersham Pharm Biotech Uk Ltd Chemical capture reagent
KR100507968B1 (ko) * 2001-08-18 2005-08-17 한국과학기술연구원 자기집합체를 형성하는 항암제-키토산 복합체 및 그의제조방법
CA2822457C (en) 2001-12-14 2016-03-08 The University Of Wyoming Methods and compositions for controlled resease of drugs
US8361464B2 (en) 2002-03-01 2013-01-29 Immunomedics, Inc. Anthracycline-Antibody Conjugates for Cancer Therapy
US20050069551A1 (en) * 2002-03-08 2005-03-31 Emory University Cytotoxic compound-protein conjugates as suppressors of tumor growth and angiogenesis
EP1572078A4 (en) * 2002-03-08 2006-08-09 Univ Emory NEW CURCUMINOID FACTOR VIIa CONSTRUCTS AS MEANS OF SUPPRESSING TUMOR GROWTH AND ANGIOGENESIS
JP2005529931A (ja) * 2002-05-24 2005-10-06 マイラス コーポレイション 膜相互作用の可逆的改質
CN1733314A (zh) * 2004-08-11 2006-02-15 张阳德 半乳糖化白蛋白磁性阿霉素纳米粒的制备方法
CA2586913A1 (en) 2004-11-09 2006-05-18 University Of Southern California Targeted innate immunity
AU2006203889A1 (en) 2005-01-05 2006-07-13 Biogen Idec Ma Inc. CRIPTO binding molecules
JP2010508271A (ja) 2006-10-27 2010-03-18 ウェイ‐チャン シェン 脂質化インターフェロンおよびその使用
EP2126127B1 (en) * 2007-01-25 2016-09-28 Dana-Farber Cancer Institute, Inc. Use of anti-egfr antibodies in treatment of egfr mutant mediated disease
CA2680854C (en) * 2007-03-15 2017-02-14 Ludwig Institute For Cancer Research Treatment method using egfr antibodies and src inhibitors and related formulations
US9283276B2 (en) 2007-08-14 2016-03-15 Ludwig Institute For Cancer Research Ltd. Monoclonal antibody 175 targeting the EGF receptor and derivatives and uses thereof
US8618096B2 (en) * 2008-07-21 2013-12-31 The Regents Of The University Of California Prodrug compositions and methods for using the same in treating cancer and malaria
JP5472288B2 (ja) * 2009-03-17 2014-04-16 国立大学法人 東京大学 タンパク質の電荷調節剤、及びタンパク質内包高分子ミセル複合体
US8535948B2 (en) * 2009-03-26 2013-09-17 Institute For Systems Biology Method to determine protein interaction sites
EP2448966B1 (en) 2009-07-03 2018-11-14 Avipep Pty Ltd Immuno-conjugates and methods for producing them
US20110076232A1 (en) * 2009-09-29 2011-03-31 Ludwig Institute For Cancer Research Specific binding proteins and uses thereof
WO2011075786A1 (en) 2009-12-23 2011-06-30 Avipep Pty Ltd Immuno-conjugates and methods for producing them 2
RU2013103763A (ru) 2010-07-02 2014-08-10 Ангиохем Инк. Короткие и содержащие d-аминокислоты полипептиды для терапевтических конъюгатов и их применения
US9738707B2 (en) 2011-07-15 2017-08-22 Biogen Ma Inc. Heterodimeric Fc regions, binding molecules comprising same, and methods relating thereto
DK2744931T3 (en) 2011-08-18 2018-08-06 Affinity Biosciences Pty Ltd SOLUBLE POLYPEPTIDES
HUE039033T2 (hu) 2012-01-10 2018-12-28 Biogen Ma Inc Terápiás molekulák transzportjának fokozása a vér-agy gáton keresztül
GB201202268D0 (en) 2012-02-09 2012-03-28 Medical Res Council Intracellular immunity
WO2014057436A2 (en) 2012-10-10 2014-04-17 Adamed Sp. Z O.O. Anticancer conjugate
JP2016513098A (ja) 2013-02-07 2016-05-12 イミューノメディクス、インコーポレイテッドImmunomedics, Inc. 癌の標的治療用抗体と抱合した極めて強力なプロドラック形態の2−ピロリノドキソルビシン(p2pdox)
WO2014141094A1 (en) 2013-03-14 2014-09-18 Adamed Sp. Z O.O. Anticancer conjugate
WO2015123595A1 (en) 2014-02-14 2015-08-20 The Regents Of The University Of California Cyclic peroxides as prodrugs for selective delivery of agents
US10328159B2 (en) 2014-10-03 2019-06-25 Engenic Molecular Delivery Pty Ltd. Enhanced loading of intact, bacterially derived vesicles with small molecule compounds
BR102016018074A2 (pt) 2015-08-07 2021-11-16 ALX Oncology Inc. Construção variante de sirp-alfa, seu método de preparação e seus usos, molécula de ácido nucleico, vetor, célula hospedeira, e composição farmacêutica
WO2017027422A1 (en) 2015-08-07 2017-02-16 Alexo Therapeutics Inc. Constructs having a sirp-alpha domain or variant thereof
CN108473541B (zh) 2015-11-24 2023-05-12 特拉斯福特普拉斯公司 通过受体介导的化学疗法治疗癌症的肽化合物和肽缀合物
US10800817B2 (en) 2016-12-19 2020-10-13 Morehouse School Of Medicine Compositions and methods for treating diseases by inhibiting exosome release
WO2018118015A1 (en) 2016-12-19 2018-06-28 Morehouse School Of Medicine Compositions and methods for treating diseases by inhibiting exosome release
WO2020081174A1 (en) 2018-10-16 2020-04-23 Nant Holdings Ip, Llc Alpha emitter compositions and methods
KR20220044904A (ko) 2019-05-31 2022-04-12 알렉소 온콜로지 인크. 면역 관문 억제제와 병용하는 sirp 알파 fc 융합으로 암을 치료하는 방법
CN114845710A (zh) 2019-11-27 2022-08-02 Alx肿瘤生物技术公司 用于治疗癌症的组合疗法
BR112023022774A2 (pt) 2021-05-13 2024-01-02 Alx Oncology Inc Terapias de combinação para tratamento de câncer
US11180534B1 (en) 2021-06-04 2021-11-23 Morehouse School Of Medicine Compositions and methods for treating SARS-CoV-2 infections
CA3242639A1 (en) * 2022-01-14 2023-07-20 Regeneron Pharmaceuticals, Inc. Verrucarin A derivatives and their antibody-drug conjugates

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4631190A (en) * 1981-06-26 1986-12-23 Shen Wei C Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US4542225A (en) * 1984-08-29 1985-09-17 Dana-Farber Cancer Institute, Inc. Acid-cleavable compound
US4744981A (en) * 1985-10-17 1988-05-17 Neorx Corporation Trichothecene antibody conjugates
US4997913A (en) * 1986-06-30 1991-03-05 Oncogen pH-sensitive immunoconjugates and methods for their use in tumor therapy
US5140013A (en) * 1989-11-28 1992-08-18 Universite Laval Maleic anhydride derivatives used as conjugation agents of anti-tumor agents on desired carriers

Also Published As

Publication number Publication date
FI101678B (fi) 1998-08-14
HUT60484A (en) 1992-09-28
NO180417B (no) 1997-01-06
IE65406B1 (en) 1995-10-18
FI916131A0 (fi) 1991-12-27
KR920012063A (ko) 1992-07-25
NO180417C (no) 1997-04-16
IE914567A1 (en) 1992-07-01
PT99954A (pt) 1993-06-30
AU9009891A (en) 1993-01-28
DE69103255T2 (de) 1994-12-08
CA2058595A1 (en) 1992-07-01
AU646121B2 (en) 1994-02-10
FI101678B1 (fi) 1998-08-14
NO920040L (no) 1992-07-01
HU914133D0 (en) 1992-03-30
FI916131A7 (fi) 1992-07-01
EP0495265B1 (en) 1994-08-03
DE69103255D1 (de) 1994-09-08
US5306809A (en) 1994-04-26
NZ241217A (en) 1993-12-23
JPH04334377A (ja) 1992-11-20
EP0495265A1 (en) 1992-07-22
ZA9110203B (en) 1993-01-27
NO920040D0 (no) 1992-01-02
DK0495265T3 (da) 1995-01-02
PT99954B (pt) 1999-06-30
ATE109476T1 (de) 1994-08-15

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