CN1980898B - 核苷衍生物及其治疗用途 - Google Patents

核苷衍生物及其治疗用途 Download PDF

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Publication number
CN1980898B
CN1980898B CN2005800178253A CN200580017825A CN1980898B CN 1980898 B CN1980898 B CN 1980898B CN 2005800178253 A CN2005800178253 A CN 2005800178253A CN 200580017825 A CN200580017825 A CN 200580017825A CN 1980898 B CN1980898 B CN 1980898B
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CN
China
Prior art keywords
tumor
compound
purposes
tumors
nmr
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
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CN2005800178253A
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English (en)
Chinese (zh)
Other versions
CN1980898A (zh
Inventor
安昌浩
崔元准
李永福
郑乐臣
李相国
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Baishi Pharmaceutical Suzhou Co ltd
Original Assignee
Rexahn Corp
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Publication date
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Publication of CN1980898A publication Critical patent/CN1980898A/zh
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Publication of CN1980898B publication Critical patent/CN1980898B/zh
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Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
CN2005800178253A 2004-04-01 2005-04-01 核苷衍生物及其治疗用途 Expired - Fee Related CN1980898B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55814104P 2004-04-01 2004-04-01
US60/558,141 2004-04-01
PCT/US2005/011313 WO2005097757A2 (en) 2004-04-01 2005-04-01 Nucleoside derivatives and therapeutic use thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2010105546004A Division CN102091072A (zh) 2004-04-01 2005-04-01 核苷衍生物及其治疗用途

Publications (2)

Publication Number Publication Date
CN1980898A CN1980898A (zh) 2007-06-13
CN1980898B true CN1980898B (zh) 2011-01-12

Family

ID=34979006

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2005800178253A Expired - Fee Related CN1980898B (zh) 2004-04-01 2005-04-01 核苷衍生物及其治疗用途
CN2010105546004A Pending CN102091072A (zh) 2004-04-01 2005-04-01 核苷衍生物及其治疗用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2010105546004A Pending CN102091072A (zh) 2004-04-01 2005-04-01 核苷衍生物及其治疗用途

Country Status (15)

Country Link
US (1) US7405214B2 (enExample)
EP (1) EP1732902B1 (enExample)
JP (2) JP5001832B2 (enExample)
KR (1) KR100926596B1 (enExample)
CN (2) CN1980898B (enExample)
AT (1) ATE453628T1 (enExample)
AU (1) AU2005230676B2 (enExample)
BR (1) BRPI0509553B8 (enExample)
CA (1) CA2562965C (enExample)
DE (1) DE602005018620D1 (enExample)
ES (1) ES2334803T3 (enExample)
IN (1) IN2014DN04587A (enExample)
MX (1) MXPA06011141A (enExample)
PL (1) PL1732902T3 (enExample)
WO (1) WO2005097757A2 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9315534B2 (en) * 2007-08-10 2016-04-19 Board Of Regents Of The University Of Nebraska Radiologic agents for monitoring alzheimer's disease progression and Evaluating a Response to Therapy and processes for the preparation of such agents
EP2515650A4 (en) * 2009-12-23 2013-05-29 Univ Nebraska TARGETED RADIOACTIVELY MARKED COMPOUNDS AND THEIR USE FOR THE TREATMENT AND DIAGNOSIS OF CANCER
CA3160553A1 (en) * 2013-03-15 2014-09-18 Rexahn Pharmaceuticals, Inc. Process for the preparation of 4-amino-1-((1s,4r,5s)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1h-pyrimidin-2-one
AU2016276783B2 (en) 2015-06-09 2020-07-02 Rexahn Pharmaceuticals, Inc. Fluorocyclopentenylcytosine uses and processes of preparation

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4975434A (en) * 1986-05-27 1990-12-04 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Antiviral and anticancer cyclopentenyl cytosine
WO2002032920A2 (en) * 2000-10-18 2002-04-25 Pharmasset Limited Modified nucleosides for treatment of viral infections and abnormal cellular proliferation

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6187674A (ja) * 1984-10-06 1986-05-06 Yoshitomi Pharmaceut Ind Ltd シクロペンテン環を有する新規ヌクレオシド
TWI299664B (en) * 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4975434A (en) * 1986-05-27 1990-12-04 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Antiviral and anticancer cyclopentenyl cytosine
WO2002032920A2 (en) * 2000-10-18 2002-04-25 Pharmasset Limited Modified nucleosides for treatment of viral infections and abnormal cellular proliferation

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
C.K.Chu, et al.Antiviral activity of Cyclopentenyl nucleosides againstorthopoxViruses (Smallpox, monkeypox and cowpox).Bioorganic & Medicinal Chmisitry Letters13 1.2003,13(1),9-12. *
Hronowski, et al.Synthesis of cyclopentane analogsof5-fluorouracilnucleosides.Canadian Journal of Chemistry70 4.1992,70(4),1162-1169. *
Jeong Lak Shin, et al.Design, synthesis and biologicalevaluationoffluoroneplanocinA as the novelmechanism-basedinhibitorofS-adenosylhomocysteunehydrolase.Journal of Medicinal Chmistry46 2.2003,46(2),201-203. *
Victor E. Marquez, et al.Cyclopentenylcytosine. ACarbocyclicNucleosidewithAntitumorand Antiviral Properties.Journal of Medicinal Chmistry31 9.1988,31(9),1687-1694. *

Also Published As

Publication number Publication date
EP1732902A2 (en) 2006-12-20
KR100926596B1 (ko) 2009-11-11
DE602005018620D1 (de) 2010-02-11
JP2012107072A (ja) 2012-06-07
CN102091072A (zh) 2011-06-15
MXPA06011141A (es) 2007-08-14
KR20070012685A (ko) 2007-01-26
CA2562965A1 (en) 2005-10-20
BRPI0509553B1 (pt) 2019-06-18
AU2005230676B2 (en) 2010-10-07
ES2334803T3 (es) 2010-03-16
WO2005097757A3 (en) 2005-12-08
CN1980898A (zh) 2007-06-13
BRPI0509553B8 (pt) 2021-05-25
ATE453628T1 (de) 2010-01-15
BRPI0509553A (pt) 2007-09-18
EP1732902B1 (en) 2009-12-30
US7405214B2 (en) 2008-07-29
JP5001832B2 (ja) 2012-08-15
JP2007531736A (ja) 2007-11-08
CA2562965C (en) 2013-10-29
US20050222185A1 (en) 2005-10-06
PL1732902T3 (pl) 2010-06-30
WO2005097757A2 (en) 2005-10-20
IN2014DN04587A (enExample) 2015-07-10
AU2005230676A1 (en) 2005-10-20

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C06 Publication
PB01 Publication
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SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
TR01 Transfer of patent right

Effective date of registration: 20200811

Address after: Unit e284, A1 building, 218 Xinghu street, Suzhou Industrial Park, Jiangsu Province

Patentee after: Baishi Pharmaceutical (Suzhou) Co.,Ltd.

Address before: American Maryland

Patentee before: REXAHN Corp.

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PP01 Preservation of patent right

Effective date of registration: 20230824

Granted publication date: 20110112

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Date of cancellation: 20240328

Granted publication date: 20110112

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

Granted publication date: 20110112