DK2836494T3 - Nye alkyleringsmidler - Google Patents

Nye alkyleringsmidler Download PDF

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Publication number
DK2836494T3
DK2836494T3 DK13715931T DK13715931T DK2836494T3 DK 2836494 T3 DK2836494 T3 DK 2836494T3 DK 13715931 T DK13715931 T DK 13715931T DK 13715931 T DK13715931 T DK 13715931T DK 2836494 T3 DK2836494 T3 DK 2836494T3
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DK
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Prior art keywords
alkyling
agents
new
new alkyling
alkyling agents
Prior art date
Application number
DK13715931T
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Danish (da)
English (en)
Inventor
Italo Beria
Michele Caruso
Paolo Orsini
Achille Panzeri
Vittoria Lupi
Matteo Salsa
Original Assignee
Nerviano Medical Sciences Srl
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Publication of DK2836494T3 publication Critical patent/DK2836494T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/54Medicinal 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 an organic compound
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
DK13715931T 2012-04-05 2013-03-28 Nye alkyleringsmidler DK2836494T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12163459 2012-04-05
EP12176162 2012-07-12
PCT/EP2013/056743 WO2013149948A1 (en) 2012-04-05 2013-03-28 New alkylating agents

Publications (1)

Publication Number Publication Date
DK2836494T3 true DK2836494T3 (da) 2019-11-11

Family

ID=48092927

Family Applications (1)

Application Number Title Priority Date Filing Date
DK13715931T DK2836494T3 (da) 2012-04-05 2013-03-28 Nye alkyleringsmidler

Country Status (10)

Country Link
US (2) US9527863B2 (enExample)
EP (2) EP3587426B1 (enExample)
JP (2) JP6314128B2 (enExample)
CN (2) CN107011358B (enExample)
DK (1) DK2836494T3 (enExample)
ES (2) ES2755719T3 (enExample)
HR (1) HRP20221356T1 (enExample)
HU (1) HUE060655T2 (enExample)
RU (1) RU2632206C2 (enExample)
WO (1) WO2013149948A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2836493B1 (en) * 2012-04-05 2018-06-20 Nerviano Medical Sciences S.r.l. Functionalized thieno-indole derivatives for the treatment of cancer
ES2755719T3 (es) 2012-04-05 2020-04-23 Nerviano Medical Sciences Srl Nuevos agentes alquilantes
ES2738657T3 (es) * 2013-09-25 2020-01-24 Nerviano Medical Sciences Srl Derivados de tieno[2,3-e]indol como nuevos antitumorales
BR112017018706B1 (pt) 2015-03-20 2023-01-24 Pfizer Inc Agentes citotóxicos bifuncionais contendo o farmacoforo cti, composição farmacêutica e uso dos mesmos
DK3325489T3 (da) * 2015-07-21 2020-02-17 Nerviano Medical Sciences Srl Asymmetrisk fremgangsmåde til fremstilling af thien-indolderivater
EP3165532B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Auristatin derivatives, linker-drugs and ligand-drug conjugates
ES2902179T3 (es) * 2016-08-19 2022-03-25 Bristol Myers Squibb Co Compuestos de seco-ciclopropapirroloindol, conjugados de anticuerpo-fármaco de los mismos y métodos de elaboración y uso
WO2022053570A1 (en) * 2020-09-09 2022-03-17 Clinuvel Pharmaceuticals Ltd (Uk) Pyrrolidine compounds to treat xeroderma pigmentosum

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE10940T1 (de) * 1981-05-12 1985-01-15 Imperial Chemical Industries Plc Pyrrolderivate.
CA1238907A (en) * 1984-02-21 1988-07-05 Robert C. Kelly 1,2,8,8a-tetrahydrocyclopropa¬c|pyrrolo(3,2-e)- indol-4(5h)-ones and related compounds
US5659022A (en) * 1996-01-05 1997-08-19 Epoch Pharmaceuticals, Inc. Oligonucleotide-cyclopropapyrroloindole conjugates as sequence specific hybridization and crosslinking agents for nucleic acids
JP3045706B1 (ja) * 1998-09-14 2000-05-29 科学技術振興事業団 Dnaの特定塩基配列をアルキル化する化合物及びその合成法
GB2344818A (en) * 1998-12-16 2000-06-21 Pharmacia & Upjohn Spa Anti-tumour thieno-indole derivatives
GB0015447D0 (en) * 2000-06-23 2000-08-16 Pharmacia & Upjohn Spa Combined therapy against tumors comprising substituted acryloyl derivates and alkylating agents
EP1243276A1 (en) 2001-03-23 2002-09-25 Franciscus Marinus Hendrikus De Groot Elongated and multiple spacers containing activatible prodrugs
US7129261B2 (en) * 2001-05-31 2006-10-31 Medarex, Inc. Cytotoxic agents
JP2005502703A (ja) * 2001-09-07 2005-01-27 ザ スクリプス リサーチ インスティテュート Cc−1065およびデュオカルマイシンのcbi類似体
WO2003026577A2 (en) * 2001-09-24 2003-04-03 Seattle Genetics, Inc. P-amidobenzylethers in drug delivery agents
US6756397B2 (en) * 2002-04-05 2004-06-29 Immunogen, Inc. Prodrugs of CC-1065 analogs
WO2004043493A1 (en) 2002-11-14 2004-05-27 Syntarga B.V. Prodrugs built as multiple self-elimination-release spacers
WO2004069201A2 (en) * 2003-02-03 2004-08-19 Medlogics Device Corporation Compounds useful in coating stents to prevent and treat stenosis and restenosis
TW200526204A (en) * 2004-02-03 2005-08-16 Pharmacia Italia Spa 1h-thieno[2,3-c]pyrazole derivatives useful as kinase inhibitors
US7282590B2 (en) 2004-02-12 2007-10-16 The Research Foundation Of State University Of New York Drug conjugates
MXPA06012144A (es) 2004-04-21 2007-01-31 Alza Corp Conjugado polimerico liberable bajo condiciones tioliticas suaves.
WO2005112919A2 (en) * 2004-05-19 2005-12-01 Medarex, Inc. Self-immolative linkers and drug conjugates
RU2402548C2 (ru) * 2004-05-19 2010-10-27 Медарекс, Инк. Химические линкеры и их конъюгаты
US8288557B2 (en) 2004-07-23 2012-10-16 Endocyte, Inc. Bivalent linkers and conjugates thereof
CN101415679A (zh) * 2006-02-02 2009-04-22 辛塔佳有限公司 水溶性cc-1065类似物及其缀合物
ES2509820T3 (es) * 2006-12-20 2014-10-20 Nerviano Medical Sciences S.R.L. Derivados de indazol como inhibidores de la cinasa para el tratamiento del cáncer
JP6067222B2 (ja) 2008-07-15 2017-01-25 ジェネンテック, インコーポレイテッド アントラサイクリン誘導体コンジュゲート、その調製方法及び抗腫瘍化合物としてのその用途
ES2755719T3 (es) 2012-04-05 2020-04-23 Nerviano Medical Sciences Srl Nuevos agentes alquilantes
EP2836493B1 (en) * 2012-04-05 2018-06-20 Nerviano Medical Sciences S.r.l. Functionalized thieno-indole derivatives for the treatment of cancer

Also Published As

Publication number Publication date
JP6314128B2 (ja) 2018-04-18
HK1203957A1 (en) 2015-11-06
US20150051154A1 (en) 2015-02-19
HUE060655T2 (hu) 2023-04-28
EP2836494B1 (en) 2019-08-21
RU2632206C2 (ru) 2017-10-03
EP3587426A1 (en) 2020-01-01
US9527863B2 (en) 2016-12-27
ES2755719T3 (es) 2020-04-23
HRP20221356T1 (hr) 2022-12-23
CN104220442B (zh) 2016-11-23
CN107011358A (zh) 2017-08-04
RU2014143994A (ru) 2016-05-27
EP3587426B1 (en) 2022-08-10
ES2929759T3 (es) 2022-12-01
JP2018070599A (ja) 2018-05-10
CN107011358B (zh) 2020-05-05
EP2836494A1 (en) 2015-02-18
CN104220442A (zh) 2014-12-17
US20170071907A1 (en) 2017-03-16
US10071074B2 (en) 2018-09-11
JP2015514101A (ja) 2015-05-18
WO2013149948A1 (en) 2013-10-10

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