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Extract from the Register of European Patents

EP About this file: EP2298783

EP2298783 - Anti-viral nucleoside analogs and methods for treating viral infections, especially hiv infections [Right-click to bookmark this link]
StatusNo opposition filed within time limit
Status updated on  12.10.2018
Database last updated on 31.08.2024
FormerThe patent has been granted
Status updated on  03.11.2017
FormerGrant of patent is intended
Status updated on  04.07.2017
FormerExamination is in progress
Status updated on  25.11.2016
Most recent event   Tooltip26.06.2020Lapse of the patent in a contracting state
New state(s): CY		published on 29.07.2020  [2020/31]
Applicant(s)For all designated states
Yale University
Two Whitney Avenue
New Haven, CT 06510 / US
For all designated states
Cheng, Yung-Chi
961 Baldwin Rd.
Woodbridge, CT 06525 / US
For all designated states
Tanaka, Hiromichi
3-7-1006 Ohdana-Nishi, Tsuzuki-ku
Yokohama 224-0028 / JP
[2017/49]
Former [2011/12]For all designated states
Yale University
Two Whitney Avenue
New Haven, CT 06511 / US
For all designated states
Cheng, Yung-Chi
961 Baldwin Rd.
Woodbridge, CT 06525 / US
For all designated states
Tanaka, Hiromichi
3-7-1006 Ohdana-Nishi, Tsuzuki-ku
Yokohama 224-0028 / JP
Inventor(s)01 / Cheng, Yung-Chi
961 BALDWIN RD.
WOODBRIDGE, CT 06525 / US
02 / Tanaka, Hiromichi
3-7-1006 OHDANA-NISHI, TSUZUKI-KU
YOKOHAMA 224-0028 / JP
03 / Baba, Masanori
3-54-19 KOUTOKUJIDAI
KAGOSHIMA Fukuoka 891-0103 / JP
 [2017/49]
Former [2011/12]01 / Cheng, Yung-Chi
961 BALDWIN RD.
WOODBRIDGE, CT 06525 / US
02 / Tanaka, Hiromichi
3-7-1006 OHDANA-NISHI, TSUZUKI-KU
YOKOHAMA 224-0028 / JP
03 / Baba, Masanori
3-54-19 KOUTOKUJIDAI
KAGOSHIMA Fukuoka 891-0103 / JP
Representative(s)Dall'Olio, Giancarlo, et al
Invention S.r.l.
Via delle Armi 1
40137 Bologna / IT
[2017/49]
Former [2011/12]Dall'Olio, Giancarlo, et al
Invention S.r.l. Via delle Armi 1
40137 Bologna / IT
Application number, filing date10155533.218.02.2004
[2011/12]
Priority number, dateUS2003044855419.03.2003         Original published format: US 448554
[2011/12]
Filing languageEN
Procedural languageEN
PublicationType: A1 Application with search report 
No.:EP2298783
Date:23.03.2011
Language:EN
[2011/12]
Type: B1 Patent specification 
No.:EP2298783
Date:06.12.2017
Language:EN
[2017/49]
Search report(s)(Supplementary) European search report - dispatched on:EP11.01.2011
ClassificationIPC:C07H19/10, A61K31/7068, A61P31/18
[2011/12]
CPC:
C07D405/04 (EP,US); C07H19/10 (EP,KR,US); A61K31/522 (EP,US);
A61K31/675 (EP,US); A61K31/7072 (EP,US); A61K31/7076 (EP,KR,US);
A61P31/12 (EP); A61P31/14 (EP); A61P31/18 (EP);
A61P31/22 (EP); A61P37/04 (EP); A61P43/00 (EP);
C07H19/06 (EP,US); C07H19/14 (KR); C07H19/16 (EP,KR,US);
C07H19/20 (EP,US); Y02A50/30 (EP,US) (-)
C-Set:
A61K31/522, A61K2300/00 (EP,US);
A61K31/675, A61K2300/00 (US,EP);
A61K31/7072, A61K2300/00 (US,EP);
A61K31/7076, A61K2300/00 (US,EP)
Designated contracting statesAT,   BE,   BG,   CH,   CY,   CZ,   DE,   DK,   EE,   ES,   FI,   FR,   GB,   GR,   HU,   IE,   IT,   LI,   LU,   MC,   NL,   PT,   RO,   SE,   SI,   SK,   TR [2017/49]
Former [2011/12]AT,  BE,  BG,  CH,  CY,  CZ,  DE,  DK,  EE,  ES,  FI,  FR,  GB,  GR,  HU,  IE,  IT,  LI,  LU,  MC,  NL,  PT,  RO,  SE,  SI,  SK,  TR 
TitleGerman:Antivirale Nukleosid-Analoga und Verfahren zur Behandlung von Virusinfektionen, insbesondere HIV-Infektionen[2011/12]
English:Anti-viral nucleoside analogs and methods for treating viral infections, especially hiv infections[2011/12]
French:Analogues de nucléoside anti-viraux et procédé pour le traitement d'infections virales, en particulier des infections par VIH[2011/12]
Examination procedure22.09.2011Amendment by applicant (claims and/or description)
23.09.2011Examination requested  [2011/44]
18.09.2013Despatch of a communication from the examining division (Time limit: M06)
17.03.2014Reply to a communication from the examining division
19.05.2015Despatch of a communication from the examining division (Time limit: M06)
20.11.2015Reply to a communication from the examining division
29.03.2016Despatch of a communication from the examining division (Time limit: M06)
29.09.2016Reply to a communication from the examining division
13.10.2016Despatch of a communication from the examining division (Time limit: M06)
12.04.2017Reply to a communication from the examining division
04.07.2017Communication of intention to grant the patent
26.10.2017Fee for grant paid
26.10.2017Fee for publishing/printing paid
26.10.2017Receipt of the translation of the claim(s)
Parent application(s)   TooltipEP04775776.0  / EP1653976
Divisional application(s)The date of the Examining Division's first communication in respect of the earliest application for which a communication has been issued (EP20040775776) is  27.08.2009
Opposition(s)07.09.2018No opposition filed within time limit [2018/46]
Fees paidRenewal fee
04.03.2010Renewal fee patent year 03
04.03.2010Renewal fee patent year 04
04.03.2010Renewal fee patent year 05
04.03.2010Renewal fee patent year 06
04.03.2010Renewal fee patent year 07
23.02.2011Renewal fee patent year 08
24.02.2012Renewal fee patent year 09
27.02.2013Renewal fee patent year 10
27.02.2014Renewal fee patent year 11
26.02.2015Renewal fee patent year 12
26.02.2016Renewal fee patent year 13
27.02.2017Renewal fee patent year 14
Opt-out from the exclusive  Tooltip
competence of the Unified
Patent Court		 See the Register of the Unified Patent Court for opt-out data
Responsibility for the accuracy, completeness or quality of the data displayed under the link provided lies entirely with the Unified Patent Court.
Lapses during opposition  TooltipHU18.02.2004
AT06.12.2017
CY06.12.2017
CZ06.12.2017
DK06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
PT06.12.2017
RO06.12.2017
SE06.12.2017
SI06.12.2017
SK06.12.2017
TR06.12.2017
IE18.02.2018
LU18.02.2018
BE28.02.2018
CH28.02.2018
LI28.02.2018
BG06.03.2018
GR07.03.2018
[2020/31]
Former [2020/27]HU18.02.2004
AT06.12.2017
CZ06.12.2017
DK06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
PT06.12.2017
RO06.12.2017
SE06.12.2017
SI06.12.2017
SK06.12.2017
TR06.12.2017
IE18.02.2018
LU18.02.2018
BE28.02.2018
CH28.02.2018
LI28.02.2018
BG06.03.2018
GR07.03.2018
Former [2020/16]AT06.12.2017
CZ06.12.2017
DK06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
RO06.12.2017
SE06.12.2017
SI06.12.2017
SK06.12.2017
TR06.12.2017
IE18.02.2018
LU18.02.2018
BE28.02.2018
CH28.02.2018
LI28.02.2018
BG06.03.2018
GR07.03.2018
Former [2019/12]AT06.12.2017
CZ06.12.2017
DK06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
RO06.12.2017
SE06.12.2017
SI06.12.2017
SK06.12.2017
IE18.02.2018
LU18.02.2018
BE28.02.2018
CH28.02.2018
LI28.02.2018
BG06.03.2018
GR07.03.2018
Former [2019/09]AT06.12.2017
CZ06.12.2017
DK06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
RO06.12.2017
SE06.12.2017
SI06.12.2017
SK06.12.2017
IE18.02.2018
LU18.02.2018
CH28.02.2018
LI28.02.2018
BG06.03.2018
GR07.03.2018
Former [2018/52]AT06.12.2017
CZ06.12.2017
DK06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
RO06.12.2017
SE06.12.2017
SI06.12.2017
SK06.12.2017
LU18.02.2018
CH28.02.2018
LI28.02.2018
BG06.03.2018
GR07.03.2018
Former [2018/51]AT06.12.2017
CZ06.12.2017
DK06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
RO06.12.2017
SE06.12.2017
SK06.12.2017
CH28.02.2018
LI28.02.2018
BG06.03.2018
GR07.03.2018
Former [2018/44]AT06.12.2017
CZ06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
MC06.12.2017
NL06.12.2017
RO06.12.2017
SE06.12.2017
SK06.12.2017
BG06.03.2018
GR07.03.2018
Former [2018/40]AT06.12.2017
CZ06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
IT06.12.2017
NL06.12.2017
RO06.12.2017
SE06.12.2017
SK06.12.2017
BG06.03.2018
GR07.03.2018
Former [2018/38]AT06.12.2017
CZ06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
NL06.12.2017
SE06.12.2017
SK06.12.2017
BG06.03.2018
GR07.03.2018
Former [2018/37]CZ06.12.2017
EE06.12.2017
ES06.12.2017
FI06.12.2017
NL06.12.2017
SE06.12.2017
SK06.12.2017
BG06.03.2018
GR07.03.2018
Former [2018/34]ES06.12.2017
FI06.12.2017
NL06.12.2017
SE06.12.2017
BG06.03.2018
GR07.03.2018
Former [2018/24]ES06.12.2017
FI06.12.2017
SE06.12.2017
BG06.03.2018
GR07.03.2018
Former [2018/23]ES06.12.2017
FI06.12.2017
SE06.12.2017
GR07.03.2018
Former [2018/22]ES06.12.2017
FI06.12.2017
Documents cited:Search[XP]US2004006007  (GOSSELIN GILLES [FR], et al) [XP] 1,3,12 * paragraph [0305] * * paragraph [0308] * * claims 3, 20, 30 *;
 [X]  - WAGA T ET AL, "SYNTHESIS AND BIOLOGICAL EVALUATON OF 4'-C-METHYL NUCLEOSIDES", NUCLEOSIDES & NUCLEOTIDES, MARCEL DEKKER, INC, US, (19960101), vol. 15, no. 1 - 03, ISSN 0732-8311, pages 287 - 304, XP000973778 [X] 1,3,12,16,21,22 * compounds 29, 31, 32, 40, 41, 42 * * table; page 294 *

DOI:   http://dx.doi.org/10.1080/07328319608002385
 [X]  - HARAGUCHI KAZUHIRO ET AL, "Allylic Substitution of 3',4'-Unsaturated Nucleosides: Organosilicon-Base Stereoselective Access to 4'-C-Branched 2',3'-Didehydro-2',3'- dideoxyribonucleosides", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, EASTON.; US, (19960101), vol. 61, doi:10.1021/JO9516190, ISSN 0022-3263, pages 851 - 858, XP002247984 [X] 1 * page 854; compounds 26, 34, 36 *

DOI:   http://dx.doi.org/10.1021/jo9516190
 [X]  - KATO K ET AL, "Enantio- and diastereoselective synthesis of 4'-alpha-substituted carbocyclic nucleosides", TETRAHEDRON ASYMMETRY, PERGAMON PRESS LTD, OXFORD, GB, vol. 9, no. 6, ISSN 0957-4166, (19980327), pages 911 - 914, (19980327), XP027117867 [X] 1 * page 912; compound 5a *
 [XP]  - KAZUHIRO HARAGUCHI ET AL, "Synthesis of a Highly Active New Anti-HIV Agent 2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, (2003), vol. 13, pages 3775 - 3777, XP002614995 [XP] 3,9,11,12,16,21,22 * page 3776; compounds 13, 14, 15 *

DOI:   http://dx.doi.org/10.1016/J.BMCL.2003.07.009
by applicantUS4880784
 US5179084
 US5491135
 US5532215
 US5821242
 US5891874
 US6114327
 US6180604
 US6232120
 US6240690
 US6316505
 US6316492
    - NOMURA ET AL., J MED. CHEM., (1999), vol. 42, pages 2901 - 2908
    - OHRUI ET AL., J MED. CHEM., (2000), vol. 43, pages 4516 - 4525
    - J. P. H. VERHEYDEN; J. G. MOFFATT, J ORG. CHEM., (1974), vol. 39, pages 3573 - 3579
    - B. V. JOSHI; C. B. REESE, TETRAHEDRON LETT., (1992), vol. 32, pages 2371 - 2374
    - KATO ET AL., CHEM. PHARM. BULL., (1999), vol. 47, pages 1256 - 1264
    - P. CALLANT; L. D'HAENES; M. VANDEWALLE, SYNTH. COMMUN., (1984), vol. 14, pages 155 - 161
    - I. GILLAIZEAU; I. M. LAGOJA; S. P. NOLAN; V. AUCAGNE; J. ROZENSKI; P. HERDEWIJN; L. A. AGROFOGLIO, EUR. J ORG. CHEM., (2003), pages 666 - 671
    - AUGUST, E. M.; M. E. MARONGIU; T. S. LIN; W. H. PRUSOF£, "Initial studies on the cellular pharmacology of 3'-deoxythymidin-2'-ene (d4T): a potent and selective inhibitor of human immunodeficiency virus", BIOCHEM PHARMACOL, (1988), vol. 37, doi:doi:10.1016/0006-2952(88)90655-7, pages 4419 - 22, XP025515242

DOI:   http://dx.doi.org/10.1016/0006-2952(88)90655-7
    - BRIDGES, E. G.; G. E. DUTSCHMAN; E. A. GULLEN; Y. C. CHENG, "Favorable interaction of beta-L(-) nucleoside analogues with clinically approved anti-HIV nucleoside analogues for the treatment of human immunodeficiency virus", BIOCHEM PHARMACOL, (1996), vol. 51, pages 731 - 6
    - BRINKMAN, K.; H. J. TER HOFSTEDE; D. M. BURGER; J. A. SMEITINK; P. P. KOOPMANS, "Adverse effects of reverse transcriptase inhibitors: mitochondrial toxicity as common pathway", AIDS, (1998), vol. 12, pages 1735 - 44, XP008008118
    - BROWNE, M. J.; K. H. MAYER; S. B. CHAFEE; M. N. DUDLEY; M. R. POSNER; S. M. STEINBERG; K. K. GRAHAM; S. M. GELETKO; S. H. ZINNER;, "2',3'-didehydro-3'-deoxythymidine (d4T) in patients with AIDS or AIDS-related complex: a phase I trial", JINFECT DIS, (1993), vol. 167, pages 21 - 9
    - CHEN, C. H.; Y. C. CHENG, "Delayed cytotoxicity and selective loss of mitochondrial DNA in cells treated with the anti-human immunodeficiency virus compound 2',3'-dideoxycytidine", JBIOL CHEM, (1989), vol. 264, pages 11934 - 7
    - CHEN, C. H.; M. VAZQUEZ-PADUA; Y. C. CHENG, "Effect of anti-human immunodeficiency virus nucleoside analogs on mitochondrial DNA and its implication for delayed toxicity", MOL PHARMACOL, (1991), vol. 39, pages 625 - 8, XP008008115
    - "Thymidine Kinase from Blast Cells of Myelocytic Leukemia", CHENG, Y. C, Methods in Enzymology, ACADEMIC PRESS, (1978), vol. LI, pages 365 - 371
    - COATES, J. A.; N. CAMMACK; H. J. JENKINSON; A. J. JOWETT; M. I. JOWETT; B. A. PEARSON; C. R. PENN; P. L. ROUSE; K. C. VINER; J. M., "(-)-2'-deoxy-3'-thiacytidine is a potent, highly selective inhibitor of human immunodeficiency virus type 1 and type 2 replication in vitro", ANTIMICROB AGENTS CHEMOTHER, (1992), vol. 36, pages 733 - 9
    - COATES, J. A.; N. CAMMACK; H. J. JENKINSON; I. M. MUTTON; B. A. PEARSON; R. STORER; J. M. CAMERON; C. R. PENN, "The separated enantiomers of 2'-deoxy-3'- thiacytidine (BCH 189) both inhibit human immunodeficiency virus replication in vitro", ANTIMICROB AGENTS CHEMOTHER, (1992), vol. 36, pages 202 - 5, XP000578441
    - DE CLERCQ, E., "HIV resistance to reverse transcriptase inhibitors", BIOCHEM PHARMACOL, (1994), vol. 47, doi:doi:10.1016/0006-2952(94)90001-9, pages 155 - 69, XP025553345

DOI:   http://dx.doi.org/10.1016/0006-2952(94)90001-9
    - DOONG, S. L.; C. H. TSAI; R. F. SCHINAZI; D. C. LIOTTA; Y. C. CHENG, "Inhibition of the replication of hepatitis B virus in vitro by 2',3'-dideoxy-3'-thiacytidine and related analogues", PROC NATL ACAD SCI U S A, (1991), vol. 88, doi:doi:10.1073/pnas.88.19.8495, pages 8495 - 9, XP002067580

DOI:   http://dx.doi.org/10.1073/pnas.88.19.8495
    - DUTSCHMAN, G. E.; E. G. BRIDGES; S. H. LIU; E. GULLEN; X. GUO; M. KUKHANOVA; Y. C. CHENG, "Metabolism of 2',3'-dideoxy-2',3'-didehydro-beta-L(-)-5-fluorocytidine and its activity in combination with clinically approved anti-human immunodeficiency virus beta-D(+) nucleoside analogs in vitro", ANTIMICROB AGENTS CHEMOTHER, (1998), vol. 42, pages 1799 - 804
    - FENG, J. Y.; A. A. JOHNSON; K. A. JOHNSON; K. S. ANDERSON, "Insights into the molecular mechanism of mitochondrial toxicity by AIDS drugs", JBIOL CHEM, (2001), vol. 276, pages 23 832 - 7
    - GELMON, K.; J. S. MONTANER; M. FANNING; J. R. SMITH; J. FALUTZ; C. TSOUKAS; J. GILL; G. WELLS; M. O'SHAUGHNESSY; M. WAINBERG ET AL, "Nature, time course and dose dependence of zidovudine-related side effects: results from the Multicenter Canadian Azidothymidine Trial", AIDS, (1989), vol. 3, pages 555 - 61
    - GOSSELIN, G.; R. F. SCHINAZI; J. P. SOMMADOSSI; C. MATHE; M. C. BERGOGNE; A. M. AUBERTIN; A. KIRN; J. L. IMBACH, "Anti-human immunodeficiency virus activities of the beta-L enantiomer of 2',3'-dideoxycytidine and its 5-fluoro derivative in vitro", ANTIMICROB AGENTS CHEMOTHER, (1994), vol. 3, no. 8, pages 1292 - 7
    - HAMAMOTO, Y.; H. NAKASHIMA; T. MATSUI; A. MATSUDA; T. UEDA; N. YAMAMOTO, "Inhibitory effect of 2',3'-didehydro-2',3'-dideoxynucleosides on infectivity, cytopathic effects, and replication of human immunodeficiency virus", ANTIMICROB AGENTS CHEMOTHER, (1987), vol. 31, pages 907 - 10
    - HARAGUCHI, K.; S. TAKEDA; H. TANAKA; T. NITANDA; M. BABA; G. E. DUTSCHMAN; Y. C. CHENG, "Synthesis of a Highly Active New Anti-HIV Agent 2', 3'-Didehydro-3'deoxy-4'-ethynylthymidine", BIOORG MED CHEM SETTER, (2003), vol. 13, doi:doi:10.1016/J.BMCL.2003.07.009, pages 3775 - 3777, XP002660976

DOI:   http://dx.doi.org/10.1016/J.BMCL.2003.07.009
    - JOHNSON, A. A.; A. S. RAY; J. HANES; Z. SUO; J. M. COLACINO; K. S. ANDERSON; K. A. JOHNSON, "Toxicity of antiviral nucleoside analogs and the human mitochondrial DNA polymerase", JBIOL CHEM, (2001), vol. 276, pages 40847 - 57
    - LARDER, B. A., "Viral resistance and the selection of antiretroviral combinations", J ACQUIR IMMUNE DEFIC SYNDR HUM RETROVIROL, (1995), vol. 10, no. 1, pages 28 - 33
    - LARDER, B. A.; B. CHESEBRO; D. D. RICHMAN, "Susceptibilities of zidovudine-susceptible and -resistant human immunodeficiency virus isolates to antiviral agents determined by using a quantitative plaque reduction assay", ANTIMICROB AGENTS CHEMOTHER, (1990), vol. 34, pages 436 - 41, XP009005039
    - LEE, L. S.; Y. C. CHENG, "Human deoxythymidine kinase. I.Purification and general properties of the cytoplasmic and mitochondrial isozymes derived from blast cells of acute myelocytic leukemia", JBIOL CHEM, (1976), vol. 251, pages 2600 - 2604
    - LEWIS, W.; M. C. DALAKAS, "Mitochondrial toxicity of antiviral drugs", NAT MED, (1995), vol. 1, doi:doi:10.1038/nm0595-417, pages 417 - 22, XP000882362

DOI:   http://dx.doi.org/10.1038/nm0595-417
    - LIN, T. S.; M. Z. LUO; M. C. LIU; S. B. PAI; G. E. DUTSCHMAN; Y. C. CHENG, "Antiviral activity of 2',3'-dideoxy-beta-L-5-fluorocytidine (beta-L-FddC) and 2',3'-dideoxy-beta-L-cytidine (beta-L-ddC) against hepatitis B virus and human immunodeficiency virus type 1 in vitro", BIOCHEM PHARMACOL, (1994), vol. 47, pages 171 - 4
    - LIN, T. S.; M. Z. LUO; M. C. LIU; S. B. PAI; G. E. DUTSCHMAN; Y. C. CHENG, "Synthesis and biological evaluation of 2',3'-dideoxy-L-pyrimidine nucleosides as potential antiviral agents against human immunodeficiency virus (HIV) and hepatitis B virus (HBV)", JMED CHEM, (1994), vol. 37, doi:doi:10.1021/jm00032a013, pages 798 - 803, XP002002033

DOI:   http://dx.doi.org/10.1021/jm00032a013
    - LIN, T. S.; M. Z. LUO; M. C. LIU; Y. L. ZHU; E. GULLEN; G. E. DUTSCHMAN; Y. C. CHENG, "Design and synthesis of 2',3'-dideoxy-2',3'-didehydro-beta-L-cytidine (beta-L-d4C) and 2',3'-dideoxy 2',3'-didehydro-beta-L-5-fluorocytidine (beta-L-Fd4C), two exceptionally potent inhibitors of human hepatitis B virus (HBV) and potent inhibitors of human immunodeficiency virus (HIV) in vitro", JMED CHEM, (1996), vol. 39, doi:doi:10.1021/jm950836q, pages 1757 - 9, XP001052613

DOI:   http://dx.doi.org/10.1021/jm950836q
    - LIN, T. S.; R. F. SCHINAZI; M. S. CHEN; E. KINNEY-THOMAS; W. H. PRUSOFF, "Antiviral activity of 2',3'-dideoxycytidin-2'-ene (2',3'-dideoxy-2',3'-didehydrocytidine) against human immunodeficiency virus in vitro", BIOCHEM PHARMACOL, (1987), vol. 36, doi:doi:10.1016/0006-2952(87)90287-5, pages 311 - 6, XP023737369

DOI:   http://dx.doi.org/10.1016/0006-2952(87)90287-5
    - LIN, T. S.; R. F. SCHINAZI; W. H. PRUSOF£, "Potent and selective in vitro activity of 3'-deoxythymidin-2'-ene (3'-deoxy-2',3'-didehydrothymidine) against human immunodeficiency virus", BIOCHEM PHARMACOL, (1987), vol. 36, doi:doi:10.1016/0006-2952(87)90253-X, pages 2713 - 8, XP023730619

DOI:   http://dx.doi.org/10.1016/0006-2952(87)90253-X
    - LU, Z. H.; R. ZHANG; R. B. DIASIO, "Comparison of dihydropyrimidine dehydrogenase from human, rat, pig and cow liver. Biochemical and immunological properties", BIOCHEM PHARMACOL, (1993), vol. 46, doi:doi:10.1016/0006-2952(93)90505-Q, pages 945 - 52, XP023757565

DOI:   http://dx.doi.org/10.1016/0006-2952(93)90505-Q
    - MAAG, H.; R. M. RYDZEWSKI; M. J. MCROBERTS; D. CRAWFORD-RUTH; J. P. VERHEYDEN; E. J. PRISBE, "Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides", JMED CHEM, (1992), vol. 35, doi:doi:10.1021/jm00086a013, pages 1440 - 51, XP002277180

DOI:   http://dx.doi.org/10.1021/jm00086a013
    - MEDINA, D. J.; C. H. TSAI; G. D. HSIUNG; Y. C. CHENG, "Comparison of Mitochondrial Morphology, Mitochondrial DNA Content, and Cell Viability in Cultured Cells Treated with Three Anti-Human Immunodeficiency Virus Dideoxynucleosides", ANTIMICROB AGENTS CHEMOTHER, (1994), vol. 38, pages 1824 - 1828, XP002213604
    - MELLORS, J. W.; G. E. DUTSCHMAN; G. J. IM; E. TRAMONTANO; S. R. WINKLER; Y. C. CHENG, "In vitro selection and molecular characterization of human immunodeficiency virus-1 resistant to non-nucleoside inhibitors of reverse transcriptase", MOL PHARMACOL, (1992), vol. 41, pages 446 - 51
    - O-YANG, C.; H. Y. WU; B. FRASER-SMITH; K. A. M. WALKER, "Synthesis of 4'-Cyanothymidine and Analogs as Potent Inhibitors of HIV", TETRAHEDRON LETTERS, (1992), vol. 33, doi:doi:10.1016/S0040-4039(00)77667-2, pages 37 - 40, XP002969549

DOI:   http://dx.doi.org/10.1016/S0040-4039(00)77667-2
    - "Disruption of Energy Metabolism and Mitochondrial Function", PARKER, W. B.; Y. C. CHENG, Neurotoxicology: Approaches and Methods, ACADEMIC PRESS INC., (1995), pages 483 - 490
    - PARKER, W. B.; Y. C. CHENG, "Mitochondrial Toxicity of Antiviral Nucleoside Analogs", THE JOURNAL OF HIH REASEARCH, (1994), vol. 6, pages 57 - 61
    - RICHMAN, D. D., "Resistance of clinical isolates of human immunodeficiency virus to antiretroviral agents", ANTIMICROB AGENTS CHEMOTHER, (1993), vol. 37, pages 1207 - 13
    - RICHMAN, D. D.; M. A. FISCHL; M. H. GRIECO; M. S. GOTTLIEB; P. A. VOLBERDING; O. L. LASKIN; J. M. LEEDOM; J. E. GROOPMAN; D. MILDV, "The toxicity of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A double-blind, placebo-controlled trial", NENGL JMED, (1987), vol. 317, pages 192 - 7
    - SCHINAZI, R. F.; C. K. CHU; A. PECK; A. MCMILLAN; R. MATHIS; D. CANNON; L. S. JEONG; J. W. BEACH; W. B. CHOI; S. YEOLA ET AL., "Activities of the four optical isomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) against human immunodeficiency virus type 1 in human lymphocytes", ANTIMICROB AGENTS CHEMOTHER, (1992), vol. 36, pages 672 - 6, XP000578440
    - SOMMADOSSI, J. P.; Z. ZHOU; M. J. HITCHCOCK; H. M. MCCLURE; M. EL KOUNI; E. CRETTON, "Catabolism of 2',3'-Didehydro-2',3-DideoxyThymidine (D4T) in Isolated Hepatocytes and in Rhesus Monkeys", PROC.ANNU. MEETINGAMERICAN CANCER RESEARCH, (1992), vol. 33, page A3253
    - YARCHOAN, R.; J. M. PLUDA; R. V. THOMAS; H. MITSUYA; P. BROUWERS; K. M. WYVILL; N. HARTMAN; D. G. JOHNS; S. BRODER, "Long-term toxicity/activity profile of 2',3'-dideoxyinosine in AIDS or AIDS-related complex", LANCET, (1990), vol. 336, pages 526 - 9
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