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
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 238000004519 manufacturing process Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 229910052740 iodine Inorganic materials 0.000 abstract 2
- HLPAJQITBMEOML-XVFCMESISA-N 4-amino-1-[(2r,3r,4s,5r)-3,4-dihydroxy-5-methyloxolan-2-yl]pyrimidin-2-one Chemical compound O[C@@H]1[C@H](O)[C@@H](C)O[C@H]1N1C(=O)N=C(N)C=C1 HLPAJQITBMEOML-XVFCMESISA-N 0.000 abstract 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000011630 iodine Chemical group 0.000 abstract 1
- 238000013160 medical therapy Methods 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000004962 physiological condition Effects 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 abstract 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 1
- 229920002554 vinyl polymer Polymers 0.000 abstract 1
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)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (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
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.
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) |
Families Citing this family (20)
| 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 |
| US6906182B2 (en) | 2000-12-01 | 2005-06-14 | Cell Works Therapeutics, Inc. | Conjugates of glycosylated/galactosylated peptide, bifunctional linker, and nucleotidic monomers/polymers, and related compositions and method of use |
| CN101068549A (zh) * | 2004-12-03 | 2007-11-07 | 阿迪赫里克斯技术公司 | 与5－fu和5－fu前药组合施用dpd抑制剂的方法 |
| 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 |
| NZ574362A (en) * | 2006-07-24 | 2010-10-29 | Taiho Pharmaceutical Co Ltd | 3'-ethynylcytidine derivative |
| WO2009042064A2 (en) | 2007-09-21 | 2009-04-02 | Nektar Therapeutics Al, Corporation | Oligomer-nucleoside phosphate conjugates |
| KR101013312B1 (ko) * | 2007-11-19 | 2011-02-09 | 한미홀딩스 주식회사 | 카페시타빈의 제조방법 및 이에 사용되는 β-아노머가강화된 트리알킬카보네이트 화합물의 제조방법 |
| 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 |
| 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 |
| 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 |
| BR112012008951A2 (pt) * | 2009-10-14 | 2019-09-24 | Adherex Tech Inc | tratamento de neurotoxidez associada com combinações de 5-fu ou seus profármacos e inibidores de 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 |
| EP3746134A1 (en) | 2018-02-02 | 2020-12-09 | Maverix Oncology, Inc. | 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| JP2614164B2 (ja) * | 1991-05-27 | 1997-05-28 | 大鵬薬品工業株式会社 | 抗腫瘍効果増強のための及び腫瘍治療のための組成物 |
| 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 |
| CA2170608C (en) * | 1993-09-14 | 1999-03-30 | James R. Mccarthy | 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 |
| WO1996037214A2 (en) * | 1995-05-26 | 1996-11-28 | F. Hoffmann-La Roche Ag | Compositions of interleukin and pyrimidine nucleosides |
-
1998
- 1998-05-04 NZ NZ330360A patent/NZ330360A/xx unknown
- 1998-05-12 CA CA002237368A patent/CA2237368C/en not_active Expired - Lifetime
- 1998-05-15 SG SG1998001066A patent/SG66466A1/en unknown
- 1998-05-20 AU AU67985/98A patent/AU746170B2/en not_active Expired
- 1998-05-22 ES ES98109318T patent/ES2329428T3/es not_active Expired - Lifetime
- 1998-05-22 DE DE69841086T patent/DE69841086D1/de not_active Expired - Lifetime
- 1998-05-22 AT AT98109318T patent/ATE440854T1/de not_active IP Right Cessation
- 1998-05-25 RS YUP-225/98A patent/RS50010B/sr unknown
- 1998-05-26 DE DE19823484A patent/DE19823484A1/de not_active Ceased
- 1998-05-26 SA SA98190103A patent/SA98190103B1/ar unknown
- 1998-05-26 ZA ZA984478A patent/ZA984478B/xx unknown
- 1998-05-27 IL IL12466198A patent/IL124661A0/xx not_active IP Right Cessation
- 1998-05-28 AR ARP980102474A patent/AR012878A1/es not_active Application Discontinuation
- 1998-05-28 ID IDP980787A patent/ID19801A/id unknown
- 1998-05-29 ES ES009801125A patent/ES2142763B1/es not_active Expired - Fee Related
- 1998-05-29 NO NO982473A patent/NO316609B1/no not_active IP Right Cessation
- 1998-05-29 FR FR9806804A patent/FR2763953B1/fr not_active Expired - Lifetime
- 1998-05-29 CO CO98030313A patent/CO4940436A1/es unknown
- 1998-05-29 CZ CZ19981675A patent/CZ295706B6/cs not_active IP Right Cessation
- 1998-05-29 HU HU9801256A patent/HU227852B1/hu unknown
- 1998-05-29 MY MYPI98002409A patent/MY128985A/en unknown
- 1998-05-29 IT IT98MI001196A patent/ITMI981196A1/it unknown
- 1998-06-01 PE PE1998000438A patent/PE79599A1/es not_active Application Discontinuation
- 1998-06-01 PL PL326604A patent/PL192832B1/pl not_active IP Right Cessation
- 1998-06-01 CN CNB981087256A patent/CN1197871C/zh not_active Expired - Lifetime
- 1998-06-01 MA MA25095A patent/MA26503A1/fr unknown
- 1998-06-01 RU RU98110369A patent/RU2238278C2/ru not_active IP Right Cessation
- 1998-06-01 GB GB9811762A patent/GB2325931B/en not_active Expired - Lifetime
- 1998-06-01 BR BR9801744A patent/BR9801744A/pt not_active Application Discontinuation
- 1998-06-01 HR HR97108791.1A patent/HRP980290A2/hr not_active Application Discontinuation
- 1998-06-01 KR KR1019980020195A patent/KR100312899B1/ko not_active Expired - Lifetime
- 1998-06-02 TR TR1998/00988A patent/TR199800988A2/xx unknown
- 1998-06-02 TW TW087108626A patent/TW584636B/zh not_active IP Right Cessation
- 1998-06-02 JP JP10152574A patent/JP3081185B2/ja not_active Expired - Lifetime
-
2000
- 2000-01-14 US US09/484,174 patent/US6114520A/en not_active Expired - Lifetime
- 2000-03-24 US US09/534,156 patent/US6211166B1/en not_active Expired - Lifetime
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Legal Events
| Date | Code | Title | Description |
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| FC | Refusal |