CO4940436A1 - Derivados de 5´-desoxicitidina y proceso de fabricacion de los mismos - Google Patents

Derivados de 5´-desoxicitidina y proceso de fabricacion de los mismos

Info

Publication number
CO4940436A1
CO4940436A1 CO98030313A CO98030313A CO4940436A1 CO 4940436 A1 CO4940436 A1 CO 4940436A1 CO 98030313 A CO98030313 A CO 98030313A CO 98030313 A CO98030313 A CO 98030313A CO 4940436 A1 CO4940436 A1 CO 4940436A1
Authority
CO
Colombia
Prior art keywords
group
benzyl
atom
substituted
hydrogen atom
Prior art date
Application number
CO98030313A
Other languages
English (en)
Inventor
Kazuo Hattori
Ishikawa Tohru
Ishitsuka Hideo
Kohchi Yasunori
Oikawa Nobuhiro
Shimma Nobuo
Suda Hitomi
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 CO4940436A1 publication Critical patent/CO4940436A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • 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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design 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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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

Un compuesto representado por la fórmula general (I): en la que R1 es un átomo de hidrógeno o un grupo fácilmente hidrolizable en condiciones fisiológicas; R2 es un átomo de hidrógeno o un grupo -CO-OR4 [en el que R4 es un grupo hidrocarbonado saturado o insaturado, lineal o ramificado, que consiste de uno a quince átomos de carbono, o un grupo de fórmula -(CH2 )n -Y (en el que Y es ciclohexilo o fenilo; n es un entero de 0 a 4)]; R3 es un átomo de hidrógeno, bromo, yodo o ciano, un grupo alquilo C1-4 [que puede estar substituido con átomo(s) de halógeno], un grupo vinilo o etinilo [que puede estar substituido con átomo(s) de halógeno, alquilo C1-4 , cicloalquilo, aralquilo, o un anillo aromático que puede tener uno o más átomo(s) de (N)], o un grupo aralquilo que puede estar substituido por 3-benciloxi-bencilo, 3-metoxi-bencilo; 3-bromo-bencilo, 3-metil-bencilo, o 3-hidroxi-bencilo; con la condición de que R2 y R3 no significan un átomo de hidrógeno simultáneamente.
CO98030313A 1997-06-02 1998-05-29 Derivados de 5´-desoxicitidina y proceso de fabricacion de los mismos CO4940436A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CO4940436A1 true CO4940436A1 (es) 2000-07-24

Family

ID=8226859

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98030313A CO4940436A1 (es) 1997-06-02 1998-05-29 Derivados de 5´-desoxicitidina y proceso de fabricacion de los mismos

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) TR199800988A3 (es)
TW (1) TW584636B (es)
ZA (1) ZA984478B (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030119724A1 (en) * 1995-11-22 2003-06-26 Ts`O Paul O.P. Ligands to enhance cellular uptake of biomolecules
DK1057831T3 (da) * 1999-05-26 2005-01-31 Hoffmann La Roche Fremgangsmåde til fremstilling af vinylpyrimidinderivater
EP1355672A2 (en) 2000-12-01 2003-10-29 Cell Works Inc. Conjugates of glycosylated/galactosylated peptide, bifunctional linker, and nucleotidic monomers/polymers, and related compositions and methods of use
KR20070098798A (ko) * 2004-12-03 2007-10-05 애드헤렉스 테크놀로지스 인크. Ｄｐｄ 억제제를 5-ｆｕ 및 5-ｆｕ 전구약물과 조합한투여방법
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
US8741858B2 (en) 2007-09-21 2014-06-03 Zhongxu Ren Oligomer-nucleoside phosphate conjugates
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
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
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
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
WO2009114814A2 (en) 2008-03-14 2009-09-17 Retrotope, Inc. Therapeutic substances that modulate genome methylation
US8603999B2 (en) * 2008-12-05 2013-12-10 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
WO2019152955A1 (en) 2018-02-02 2019-08-08 Steven Albert Everett Small molecule drug conjugates of gemcitabine monophosphate
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)

* Cited by examiner, † Cited by third party
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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
EP0160079B1 (en) * 1983-10-26 1990-01-31 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
AU6081294A (en) * 1993-05-14 1994-12-12 Pro-Neuron, Inc. Treatment of chemotherapeutic agent and antiviral agent toxicity with acylated pyrimidine nucleosides
AU690579B2 (en) * 1993-09-14 1998-04-30 Merrell Pharmaceuticals Inc. 5-(1-fluoro-vinyl)-1H-pyrimidine-2,4-dione derivatives useful as antineoplastic agents
US5476932A (en) * 1994-08-26 1995-12-19 Hoffmann-La Roche Inc. Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives
AU5998296A (en) * 1995-05-26 1996-12-11 F. Hoffmann-La Roche Ag Compositions of interleukin and pyrimidine nucleosides

Also Published As

Publication number Publication date
AR012878A1 (es) 2000-11-22
ITMI981196A1 (it) 1999-11-29
SA98190103B1 (ar) 2006-04-18
FR2763953A1 (fr) 1998-12-04
ATE440854T1 (de) 2009-09-15
GB2325931A (en) 1998-12-09
MA26503A1 (fr) 2004-12-20
KR100312899B1 (ko) 2002-03-08
GB9811762D0 (en) 1998-07-29
YU22598A (sh) 2001-12-26
CZ295706B6 (cs) 2005-10-12
TR199800988A2 (xx) 1998-12-21
AU6798598A (en) 1998-12-03
RU2238278C2 (ru) 2004-10-20
HUP9801256A2 (hu) 1999-05-28
ZA984478B (en) 1998-12-02
KR19990006547A (ko) 1999-01-25
HU9801256D0 (en) 1998-07-28
GB2325931B (en) 2001-07-25
PL326604A1 (en) 1998-12-07
NO982473L (no) 1998-12-03
AU746170B2 (en) 2002-04-18
CZ167598A3 (cs) 1998-12-16
TR199800988A3 (tr) 1998-12-21
RS50010B (sr) 2008-09-29
CN1201037A (zh) 1998-12-09
ES2142763B1 (es) 2001-04-01
HU227852B1 (en) 2012-05-02
TW584636B (en) 2004-04-21
PL192832B1 (pl) 2006-12-29
ES2142763A1 (es) 2000-04-16
ID19801A (id) 1998-08-06
BR9801744A (pt) 2000-03-21
NO982473D0 (no) 1998-05-29
HUP9801256A3 (en) 2004-03-01
JP3081185B2 (ja) 2000-08-28
HRP980290A2 (en) 1999-04-30
JPH10330395A (ja) 1998-12-15
SG66466A1 (en) 1999-07-20
NO316609B1 (no) 2004-03-08
DE19823484A1 (de) 1998-12-03
PE79599A1 (es) 1999-08-25
FR2763953B1 (fr) 2005-01-07
NZ330360A (en) 1999-03-29
CA2237368C (en) 2009-03-03
CA2237368A1 (en) 1998-12-02
US6211166B1 (en) 2001-04-03
US6114520A (en) 2000-09-05
DE69841086D1 (de) 2009-10-08
ES2329428T3 (es) 2009-11-25
MY128985A (en) 2007-03-30
IL124661A0 (en) 1998-12-06
CN1197871C (zh) 2005-04-20

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