CN101080417B - 吉西他滨的酰胺前体药物、其组合物以及应用 - Google Patents

吉西他滨的酰胺前体药物、其组合物以及应用 Download PDF

Info

Publication number
CN101080417B
CN101080417B CN2005800431815A CN200580043181A CN101080417B CN 101080417 B CN101080417 B CN 101080417B CN 2005800431815 A CN2005800431815 A CN 2005800431815A CN 200580043181 A CN200580043181 A CN 200580043181A CN 101080417 B CN101080417 B CN 101080417B
Authority
CN
China
Prior art keywords
compound
gemcitabine
formula
administered
cancer
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN2005800431815A
Other languages
English (en)
Chinese (zh)
Other versions
CN101080417A (zh
Inventor
D·M·本德尔
D·M·雷米克
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN101080417A publication Critical patent/CN101080417A/zh
Application granted granted Critical
Publication of CN101080417B publication Critical patent/CN101080417B/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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
    • C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)
CN2005800431815A 2004-12-17 2005-11-30 吉西他滨的酰胺前体药物、其组合物以及应用 Expired - Fee Related CN101080417B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US63742204P 2004-12-17 2004-12-17
US60/637,422 2004-12-17
PCT/US2005/043125 WO2006065525A1 (en) 2004-12-17 2005-11-30 Amide prodrug of gemcitabine, compositions and use thereof

Publications (2)

Publication Number Publication Date
CN101080417A CN101080417A (zh) 2007-11-28
CN101080417B true CN101080417B (zh) 2011-01-19

Family

ID=36168678

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2005800431815A Expired - Fee Related CN101080417B (zh) 2004-12-17 2005-11-30 吉西他滨的酰胺前体药物、其组合物以及应用

Country Status (31)

Country Link
US (1) US7691827B2 (enExample)
EP (1) EP1831237B1 (enExample)
JP (1) JP5022911B2 (enExample)
KR (1) KR100874052B1 (enExample)
CN (1) CN101080417B (enExample)
AR (1) AR055009A1 (enExample)
AT (1) ATE405573T1 (enExample)
AU (1) AU2005316922B2 (enExample)
BR (1) BRPI0519117A2 (enExample)
CA (1) CA2589850C (enExample)
CY (1) CY1108447T1 (enExample)
DE (1) DE602005009255D1 (enExample)
DK (1) DK1831237T3 (enExample)
EA (1) EA011868B1 (enExample)
ES (1) ES2310860T3 (enExample)
HR (1) HRP20080529T3 (enExample)
IL (1) IL183666A (enExample)
MA (1) MA29154B1 (enExample)
MX (1) MX2007007228A (enExample)
MY (1) MY143677A (enExample)
NO (1) NO20073368L (enExample)
NZ (1) NZ554732A (enExample)
PE (1) PE20060771A1 (enExample)
PL (1) PL1831237T3 (enExample)
PT (1) PT1831237E (enExample)
RS (1) RS50629B (enExample)
SI (1) SI1831237T1 (enExample)
TW (1) TWI326687B (enExample)
UA (1) UA86119C2 (enExample)
WO (1) WO2006065525A1 (enExample)
ZA (1) ZA200705019B (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2652633C (en) * 2006-06-21 2014-03-25 Eli Lilly And Company Crystalline forms of gemcitabine amide prodrug, compositions and use thereof
TWI436775B (zh) 2007-08-24 2014-05-11 Oncotherapy Science Inc 以抗原胜肽合併化療藥劑治療胰臟癌
CN101525361B (zh) * 2009-04-21 2010-11-17 济南圣鲁金药物技术开发有限公司 基于吉西他滨结构的前药及其合成方法及应用
GB0907551D0 (en) 2009-05-01 2009-06-10 Univ Dundee Treatment or prophylaxis of proliferative conditions
CN102432654A (zh) * 2011-09-26 2012-05-02 宋云龙 吉西他滨酰胺衍生物及其制备方法和用途
CA2890359A1 (en) 2012-11-07 2014-05-15 Zucai SUO Substituted gemcitabine aryl amide analogs and treatment methods using same
KR20150082606A (ko) 2012-11-13 2015-07-15 보옌 테라퓨틱스, 인크. 겜시타빈 전구약물 및 그의 용도
US10059733B2 (en) 2014-03-03 2018-08-28 Nucorion Pharmaceuticals, Inc. Gemcitabine analogs
WO2016078160A1 (zh) * 2014-11-17 2016-05-26 常州方圆制药有限公司 胞苷衍生物及其应用
US10435429B2 (en) 2017-10-03 2019-10-08 Nucorion Pharmaceuticals, Inc. 5-fluorouridine monophosphate cyclic triester compounds
AU2019207626B2 (en) 2018-01-10 2023-10-05 Nucorion Pharmaceuticals, Inc. Phosphor(n)amidatacetal and phosph(on)atalcetal compounds
US11427550B2 (en) 2018-01-19 2022-08-30 Nucorion Pharmaceuticals, Inc. 5-fluorouracil compounds
AU2019216531A1 (en) 2018-02-02 2020-09-24 Maverix Oncology, Inc. Small molecule drug conjugates of gemcitabine monophosphate
CN113166189A (zh) * 2018-04-26 2021-07-23 纳米医学控股有限公司 吉西他滨两亲性前体药物
CN108864250A (zh) * 2018-05-29 2018-11-23 北京大学 一种FAPα酶敏感的吉西他滨前体药物及其制备方法和应用
KR20210057025A (ko) * 2018-08-03 2021-05-20 셀릭스 바이오 프라이빗 리미티드 암의 치료를 위한 조성물 및 방법
MX2022000573A (es) 2019-07-17 2022-02-10 Nucorion Pharmaceuticals Inc Compuestos ciclicos de desoxirribonucleotido.
CN115605492B (zh) 2020-04-21 2025-09-16 配体制药股份有限公司 核苷酸前药化合物
PL442924A1 (pl) * 2022-11-23 2024-05-27 Politechnika Śląska Prolek - glikokoniugat pochodny gemcytabiny, jako związek o działaniu przeciwnowotworowym, sposób otrzymywania i zastosowanie

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4526988A (en) * 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
US4965374A (en) * 1987-08-28 1990-10-23 Eli Lilly And Company Process for and intermediates of 2',2'-difluoronucleosides
YU43193A (sh) * 1992-06-22 1997-01-08 Eli Lilly And Company 2'-deoksi-2',2'-difluoro(4-supstituisani)pirimidinski nukleozidi antivirusnog i antikancerogenog dejstva i međuproizvodi
RU2131880C1 (ru) * 1992-06-22 1999-06-20 Эли Лилли Энд Компани Способ получения обогащенных бета-аномером нуклеозидов
GB2321454A (en) * 1997-01-24 1998-07-29 Norsk Hydro As Gemcitabine esters and amides
ATE236188T1 (de) * 1997-01-24 2003-04-15 Conpharma As Gemcitabin-derivate
US6624142B2 (en) * 1997-12-30 2003-09-23 Enzon, Inc. Trimethyl lock based tetrapartate prodrugs
US5965119A (en) * 1997-12-30 1999-10-12 Enzon, Inc. Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents
US6376470B1 (en) * 1999-09-23 2002-04-23 Enzon, Inc. Polymer conjugates of ara-C and ara-C derivatives
WO2004041203A2 (en) * 2002-11-04 2004-05-21 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
US7846436B2 (en) * 2003-11-28 2010-12-07 Chemgenes Corporation Oligonucleotides and related compounds

Also Published As

Publication number Publication date
ES2310860T3 (es) 2009-01-16
HK1109903A1 (en) 2008-06-27
HRP20080529T3 (en) 2008-12-31
UA86119C2 (ru) 2009-03-25
DK1831237T3 (da) 2008-10-27
ZA200705019B (en) 2008-10-29
ATE405573T1 (de) 2008-09-15
IL183666A0 (en) 2007-09-20
CY1108447T1 (el) 2014-04-09
NZ554732A (en) 2010-09-30
PT1831237E (pt) 2008-09-22
CA2589850A1 (en) 2006-06-22
TW200634023A (en) 2006-10-01
DE602005009255D1 (de) 2008-10-02
TWI326687B (en) 2010-07-01
EA200701300A1 (ru) 2007-10-26
BRPI0519117A2 (pt) 2008-12-23
EA011868B1 (ru) 2009-06-30
PE20060771A1 (es) 2006-09-23
CN101080417A (zh) 2007-11-28
RS50629B (sr) 2010-06-30
KR100874052B1 (ko) 2008-12-12
KR20070086308A (ko) 2007-08-27
EP1831237A1 (en) 2007-09-12
MY143677A (en) 2011-06-30
AU2005316922B2 (en) 2011-08-25
MA29154B1 (fr) 2008-01-02
US20090156547A1 (en) 2009-06-18
IL183666A (en) 2011-09-27
EP1831237B1 (en) 2008-08-20
JP5022911B2 (ja) 2012-09-12
JP2008524218A (ja) 2008-07-10
WO2006065525A1 (en) 2006-06-22
CA2589850C (en) 2012-05-01
AR055009A1 (es) 2007-08-01
MX2007007228A (es) 2007-08-14
SI1831237T1 (sl) 2009-02-28
PL1831237T3 (pl) 2009-01-30
NO20073368L (no) 2007-07-16
AU2005316922A1 (en) 2006-06-22
US7691827B2 (en) 2010-04-06

Similar Documents

Publication Publication Date Title
CN101080417B (zh) 吉西他滨的酰胺前体药物、其组合物以及应用
US8114854B2 (en) Crystalline forms of gemcitabine amide prodrug, compositions and use thereof
CN108864250A (zh) 一种FAPα酶敏感的吉西他滨前体药物及其制备方法和应用
US7419965B2 (en) Nucleotide lipid ester derivatives
CA2707593A1 (en) Clofarabine phospholipid derivatives
EP3470403B1 (en) Taxoid compound and preparation method and use thereof
HK1116197A (en) Amide prodrug of gemcitabine, compositions and use thereof
HK1109903B (en) Amide prodrug of gemcitabine, compositions and use thereof
BRPI0713615A2 (pt) Formas cristalinas de pró-fármacos de amida de gemcitabina, composições de uso das mesmas

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1116197

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1116197

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20110119

Termination date: 20151130

EXPY Termination of patent right or utility model