RU2632206C2 - Новые алкилирующие средства - Google Patents

Новые алкилирующие средства Download PDF

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RU2632206C2
RU2632206C2 RU2014143994A RU2014143994A RU2632206C2 RU 2632206 C2 RU2632206 C2 RU 2632206C2 RU 2014143994 A RU2014143994 A RU 2014143994A RU 2014143994 A RU2014143994 A RU 2014143994A RU 2632206 C2 RU2632206 C2 RU 2632206C2
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Russia
Prior art keywords
methyl
indol
carbonyl
dihydro
thieno
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RU2014143994A
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English (en)
Russian (ru)
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RU2014143994A (ru
Inventor
Итало Берия
Микеле Карузо
Виттория ЛУПИ
Паоло Орсини
Маттео Сальса
Акилле Панцери
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НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic 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
    • A61K31/407—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K38/05—Dipeptides
    • 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
    • A61K38/06—Tripeptides
    • 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
    • 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
    • A61K47/54—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 an organic compound
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides 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)
RU2014143994A 2012-04-05 2013-03-28 Новые алкилирующие средства RU2632206C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP12163459.6 2012-04-05
EP12163459 2012-04-05
EP12176162.1 2012-07-12
EP12176162 2012-07-12
PCT/EP2013/056743 WO2013149948A1 (en) 2012-04-05 2013-03-28 New alkylating agents

Publications (2)

Publication Number Publication Date
RU2014143994A RU2014143994A (ru) 2016-05-27
RU2632206C2 true RU2632206C2 (ru) 2017-10-03

Family

ID=48092927

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2014143994A RU2632206C2 (ru) 2012-04-05 2013-03-28 Новые алкилирующие средства

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

Citations (2)

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GB2344818A (en) * 1998-12-16 2000-06-21 Pharmacia & Upjohn Spa Anti-tumour thieno-indole derivatives
RU2402548C2 (ru) * 2004-05-19 2010-10-27 Медарекс, Инк. Химические линкеры и их конъюгаты

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GB2344818A (en) * 1998-12-16 2000-06-21 Pharmacia & Upjohn Spa Anti-tumour thieno-indole derivatives
RU2402548C2 (ru) * 2004-05-19 2010-10-27 Медарекс, Инк. Химические линкеры и их конъюгаты

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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
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
DK2836494T3 (da) 2019-11-11
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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