AR012878A1 - Un compuesto derivado de 5'-desoxicitidina, su uso, un proceso para fabricarlo, composiciones farmaceuticas que lo comprende, y un kit que comprende dicha composicion. - Google Patents

Un compuesto derivado de 5'-desoxicitidina, su uso, un proceso para fabricarlo, composiciones farmaceuticas que lo comprende, y un kit que comprende dicha composicion.

Info

Publication number
AR012878A1
AR012878A1 ARP980102474A ARP980102474A AR012878A1 AR 012878 A1 AR012878 A1 AR 012878A1 AR P980102474 A ARP980102474 A AR P980102474A AR P980102474 A ARP980102474 A AR P980102474A AR 012878 A1 AR012878 A1 AR 012878A1
Authority
AR
Argentina
Prior art keywords
group
substituted
manufacture
pharmaceutical compositions
atom
Prior art date
Application number
ARP980102474A
Other languages
English (en)
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 AR012878A1 publication Critical patent/AR012878A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos derivados de 5'-desoxicitidina representados por la formula general I, en la que R1 es un átomo de hidrogeno o un grupo fácilmentehidrolizable en condiciones fisiologicas; R2 es un átomo de hidrogeno o un grupo -CO-OR4, en el queR4 es un grupo hidrocarbonado saturado o insaturado,lineal o ramificado, que consiste en de uno a quince átomos de carbono, o un grupo de formula -(CH2)n-Y (en el que Y es ciclohexilo o fenilo; n es un enterode 0 a 4); R3 es un átomo de hidrogeno, bromo, yodo o ciano, un grupo alquilo C1-4, (que puede estar substituido con átomo(s) de halogeno), un grupo vinilo oetinilo ( que puede estar substituido con atomo(s) de halogeno, alquilo C1-4, cicloalquilo, aralquilo o un anillo aromático quepuede tener uno o másheteroátomo(s)), o un grupo aralquilo que puede estar substituido, para su uso en terapia médica, especialmente en terapia antitumoral. Un proceso parafabricarlos, composiciones farmacéuticas, que los comprenden, kits quecomprenden dichas composiciones, y el uso de los compuestos para la fabricacionde un medicamento para el tratamiento de tumores.
ARP980102474A 1997-06-02 1998-05-28 Un compuesto derivado de 5'-desoxicitidina, su uso, un proceso para fabricarlo, composiciones farmaceuticas que lo comprende, y un kit que comprende dicha composicion. AR012878A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP97108791 1997-06-02

Publications (1)

Publication Number Publication Date
AR012878A1 true AR012878A1 (es) 2000-11-22

Family

ID=8226859

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980102474A AR012878A1 (es) 1997-06-02 1998-05-28 Un compuesto derivado de 5'-desoxicitidina, su uso, un proceso para fabricarlo, composiciones farmaceuticas que lo comprende, y un kit que comprende dicha composicion.

Country Status (33)

Country Link
US (2) US6114520A (es)
JP (1) JP3081185B2 (es)
KR (1) KR100312899B1 (es)
CN (1) CN1197871C (es)
AR (1) AR012878A1 (es)
AT (1) ATE440854T1 (es)
AU (1) AU746170B2 (es)
BR (1) BR9801744A (es)
CA (1) CA2237368C (es)
CO (1) CO4940436A1 (es)
CZ (1) CZ295706B6 (es)
DE (2) DE69841086D1 (es)
ES (2) ES2329428T3 (es)
FR (1) FR2763953B1 (es)
GB (1) GB2325931B (es)
HR (1) HRP980290A2 (es)
HU (1) HU227852B1 (es)
ID (1) ID19801A (es)
IL (1) IL124661A0 (es)
IT (1) ITMI981196A1 (es)
MA (1) MA26503A1 (es)
MY (1) MY128985A (es)
NO (1) NO316609B1 (es)
NZ (1) NZ330360A (es)
PE (1) PE79599A1 (es)
PL (1) PL192832B1 (es)
RS (1) RS50010B (es)
RU (1) RU2238278C2 (es)
SA (1) SA98190103B1 (es)
SG (1) SG66466A1 (es)
TR (1) TR199800988A2 (es)
TW (1) TW584636B (es)
ZA (1) ZA984478B (es)

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US20030119724A1 (en) * 1995-11-22 2003-06-26 Ts`O Paul O.P. Ligands to enhance cellular uptake of biomolecules
ES2226647T3 (es) * 1999-05-26 2005-04-01 F. Hoffmann-La Roche Ag Proceso para la preparacion de derivados de vinil pirimidina.
JP2004536027A (ja) 2000-12-01 2004-12-02 ジョーンズ・ホプキンス・ユニーバーシティー グリコシル化/ガラクトシル化ペプチドの接合体、二官能性リンカー、およびヌクレオチドのモノマー/ポリマー、および関連する組成物および使用方法
MX2007006646A (es) * 2004-12-03 2007-11-16 Adherex Technologies Inc Metodos para administrar inhibidores de dihidropirimidina deshidrogenasa en combinacion con 5-fluorouracilo y profarmacos de 5-fluorouracilo.
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
US8741858B2 (en) 2007-09-21 2014-06-03 Zhongxu Ren Oligomer-nucleoside phosphate conjugates
CN101469008B (zh) * 2007-12-29 2013-08-07 上海特化医药科技有限公司 卡培他滨羟基衍生物、其制备方法和用于制备卡培他滨
WO2009082844A1 (fr) * 2007-12-28 2009-07-09 Topharman Shanghai Co., Ltd Dérivé hydroxyle de la capécitabine, ses procédés de préparation et ses utilisations pour préparer la capécitabine
WO2009094847A1 (fr) * 2007-12-28 2009-08-06 Topharman Shanghai Co., Ltd. Dérivé hydroxyle de capécitabine, procédés de préparation et d' utilisation de la capécitabine
WO2009082846A1 (fr) * 2007-12-28 2009-07-09 Topharman Shanghai Co., Ltd. Dérivé hydroxyle de la capécitabine, ses procédés de préparation et ses utilisations pour préparer la capécitabine
US8637486B2 (en) * 2008-03-14 2014-01-28 Retrotope, Inc. Therapeutic substances that modulate genome methylation
WO2010063080A1 (en) 2008-12-05 2010-06-10 Commonwealth Scientific And Industrial Research Organisation Amphiphile prodrugs
GB0907551D0 (en) 2009-05-01 2009-06-10 Univ Dundee Treatment or prophylaxis of proliferative conditions
EA201270551A1 (ru) * 2009-10-14 2012-12-28 Эдхиэрекс Текнолоджиз, Инк. Лечение нейротоксичности, ассоциированной с комбинациями 5-fu или его пролекарств с ингибиторами dpd
CN104926890B (zh) * 2015-06-04 2018-04-03 新乡学院 一种1,2‑o‑二乙酰基‑3,5‑o‑二苯甲酰基核糖的合成方法
KR20200118827A (ko) 2018-02-02 2020-10-16 마베릭스 온콜로지, 잉크. 젬시타빈 모노포스페이트의 소분자 약물 컨쥬게이트
CN113321694A (zh) * 2021-06-22 2021-08-31 药康众拓(江苏)医药科技有限公司 N4-羟基胞苷衍生物及其制备方法和用途

Family Cites Families (18)

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JPS5726278B2 (es) * 1973-03-13 1982-06-03
GB1561290A (en) * 1975-10-16 1980-02-20 Nyegaard & Co As Pyrimid - 2 - ones
US4071680A (en) * 1976-12-20 1978-01-31 Hoffmann-La Roche Inc. 5'-Deoxy-5-fluoropyrimidine nucleosides
CH633810A5 (en) * 1978-01-01 1982-12-31 Hoffmann La Roche Novel nucleosides and process for their preparation
US4328229A (en) * 1978-03-29 1982-05-04 Taiho Pharmaceutical Company Limited Anti-cancer composition for delivering 5-fluorouracil to cancer tissues
JPS5677226A (en) * 1979-11-27 1981-06-25 Taiho Yakuhin Kogyo Kk Antitumorigenic agent
WO1985001871A1 (en) * 1983-10-26 1985-05-09 Greer Sheldon B Method and materials for sensitizing neoplastic tissue to radiation
US5736531A (en) * 1987-10-28 1998-04-07 Pro-Neuron, Inc. Compositions of chemotherapeutic agent or antiviral agent with acylated pyrimidine nucleosides
CA1327358C (en) * 1987-11-17 1994-03-01 Morio Fujiu Fluoro cytidine derivatives
GB9020930D0 (en) * 1990-09-26 1990-11-07 Wellcome Found Pharmaceutical combinations
ATE173165T1 (de) * 1991-05-27 1998-11-15 Taiho Pharmaceutical Co Ltd Zusammensetzung, verfahren und instrument zur potenzierung der antitumoraktivität und zur behandlung von tumoren
DE4123520A1 (de) * 1991-07-16 1993-01-21 Inst Molekularbiologie Ak Mittel zur regeneration des blutbildes durch foerderung der leukozytenproliferation
TW254946B (es) * 1992-12-18 1995-08-21 Hoffmann La Roche
AU671491B2 (en) * 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
WO1994026761A1 (en) * 1993-05-14 1994-11-24 Pro-Neuron, Inc. Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides
NZ273161A (en) * 1993-09-14 1997-11-24 Merrell Pharma Inc 5-(1-flurovinyl)-1h-pyrimidine-2,4-dione derivatives; pharmaceutical compositions
US5476932A (en) * 1994-08-26 1995-12-19 Hoffmann-La Roche Inc. Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives
CA2220837A1 (en) * 1995-05-26 1996-11-28 Kazushige Mori Compositions of interleukin and pyrimidine nucleosides

Also Published As

Publication number Publication date
ES2142763A1 (es) 2000-04-16
ES2142763B1 (es) 2001-04-01
JP3081185B2 (ja) 2000-08-28
HUP9801256A3 (en) 2004-03-01
YU22598A (sh) 2001-12-26
NO982473L (no) 1998-12-03
ES2329428T3 (es) 2009-11-25
JPH10330395A (ja) 1998-12-15
ZA984478B (en) 1998-12-02
HU227852B1 (en) 2012-05-02
RU2238278C2 (ru) 2004-10-20
PL192832B1 (pl) 2006-12-29
ID19801A (id) 1998-08-06
SG66466A1 (en) 1999-07-20
PL326604A1 (en) 1998-12-07
MY128985A (en) 2007-03-30
CZ295706B6 (cs) 2005-10-12
MA26503A1 (fr) 2004-12-20
RS50010B (sr) 2008-09-29
HUP9801256A2 (hu) 1999-05-28
GB9811762D0 (en) 1998-07-29
TR199800988A3 (tr) 1998-12-21
IL124661A0 (en) 1998-12-06
NO982473D0 (no) 1998-05-29
HU9801256D0 (en) 1998-07-28
DE69841086D1 (de) 2009-10-08
NO316609B1 (no) 2004-03-08
KR19990006547A (ko) 1999-01-25
PE79599A1 (es) 1999-08-25
HRP980290A2 (en) 1999-04-30
FR2763953A1 (fr) 1998-12-04
SA98190103B1 (ar) 2006-04-18
ITMI981196A1 (it) 1999-11-29
TW584636B (en) 2004-04-21
AU6798598A (en) 1998-12-03
AU746170B2 (en) 2002-04-18
CA2237368C (en) 2009-03-03
FR2763953B1 (fr) 2005-01-07
KR100312899B1 (ko) 2002-03-08
ATE440854T1 (de) 2009-09-15
CA2237368A1 (en) 1998-12-02
US6114520A (en) 2000-09-05
CO4940436A1 (es) 2000-07-24
CN1201037A (zh) 1998-12-09
DE19823484A1 (de) 1998-12-03
NZ330360A (en) 1999-03-29
BR9801744A (pt) 2000-03-21
US6211166B1 (en) 2001-04-03
TR199800988A2 (xx) 1998-12-21
GB2325931B (en) 2001-07-25
GB2325931A (en) 1998-12-09
CN1197871C (zh) 2005-04-20
CZ167598A3 (cs) 1998-12-16

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