EP 0575482 A1 19931229 - ANTIVIRAL ACTIVITY AND RESOLUTION OF 2-HYDROXYMETHYL-5-(5-FLUOROCYTOSIN-1-YL)-1,3-OXATHIOLANE.
Title (en)
ANTIVIRAL ACTIVITY AND RESOLUTION OF 2-HYDROXYMETHYL-5-(5-FLUOROCYTOSIN-1-YL)-1,3-OXATHIOLANE.
Title (de)
ANTIVIRALE AKTIVITÄT UND OPTISCHE TRENNUNG VON 2-HYDROXYMETHYL-5-(5-FLUORCYTOSIN-1-YL)-1,3-OXATHIOLAN.
Title (fr)
ACTIVITE ANTIVIRALE ET RESOLUTION DE 2-HYDROXYMETHYL-5-5-FLUOROCYTOSINE-1-YL-1,3-OXATHIOLANE.
Publication
Application
Priority
- US 65976091 A 19910222
- US 73608991 A 19910726
- US 83115392 A 19920212
Abstract (en)
[origin: WO9214743A2] A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N<4> alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
Abstract (fr)
L'invention décrit un procédé et une composition servant au traitement d'infections dues au VIH et au virus de l'hépatite B chez l'homme et comprenant l'administration d'une dose efficace de 2-hydroxyméthyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, d'un de ses dérivés acceptable pharmaceutiquement, y compris d'un dérivé alkylé ou acylé en 5' ou N4, ou d'un de ses sels acceptable pharmaceutiquement, contenus dans un vecteur acceptable pharmaceutiquement. L'invention décrit également un procédé de résolution d'un mélange racémique d'énantiomères de nucléosides, comprenant l'étape d'exposition dudit mélange racémique à une enzyme qui, de préférence, catalyse une réaction dans l'un des énantiomères.
IPC 1-7
IPC 8 full level
A61K 31/505 (2006.01); A61K 31/39 (2006.01); A61K 31/506 (2006.01); A61K 31/513 (2006.01); A61K 31/66 (2006.01); A61K 31/70 (2006.01); A61P 1/16 (2006.01); A61P 31/12 (2006.01); A61P 31/18 (2006.01); A61P 37/04 (2006.01); C07D 239/36 (2006.01); C07D 327/04 (2006.01); C07D 405/04 (2006.01); C07D 411/04 (2006.01); C07F 9/547 (2006.01); C07H 5/00 (2006.01); C07H 19/06 (2006.01); C07H 19/10 (2006.01); C12P 13/00 (2006.01); C12P 17/16 (2006.01); C12P 19/38 (2006.01); C12P 41/00 (2006.01)
IPC 8 main group level
CPC (source: EP)
A61P 1/16 (2017.12); A61P 31/12 (2017.12); A61P 31/18 (2017.12); A61P 35/00 (2017.12); A61P 37/04 (2017.12); C07D 405/04 (2013.01); C07D 411/04 (2013.01); C07H 19/06 (2013.01); C07H 19/10 (2013.01)
Citation (search report)
See references of WO 9214743A2
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IT LI LU MC NL SE
DOCDB simple family (publication)
WO 9214743 A2 19920903; WO 9214743 A3 19921029; AT E270291 T1 20040715; AT E469147 T1 20100615; AU 1561792 A 19920915; AU 3794395 A 19960314; AU 665187 B2 19951221; AU 679649 B2 19970703; AU 8077398 A 19981015; BG 62053 B1 19990129; BG 98062 A 19940429; BR 9205661 A 19940524; CA 2104399 A1 19920823; CA 2104399 C 20051018; CA 2513440 A1 19920903; CA 2513440 C 20101130; CN 100396785 C 20080625; CN 1037682 C 19980311; CN 1065065 A 19921007; CN 1084745 C 20020515; CN 1109108 C 20030521; CN 1127301 A 19960724; CN 1203232 A 19981230; CN 1418966 A 20030521; CZ 295074 B6 20050518; CZ 49792 A3 19930317; DE 69233379 D1 20040805; DE 69233379 T2 20050714; DE 69233786 D1 20100708; DK 0984013 T3 20041025; DK 1439177 T3 20100802; EP 0575482 A1 19931229; EP 0984013 A2 20000308; EP 0984013 A3 20000802; EP 0984013 B1 20040630; EP 1439177 A1 20040721; EP 1439177 B1 20100526; ES 2224547 T3 20050301; ES 2345102 T3 20100915; FI 114915 B 20050131; FI 20030932 A 20030624; FI 933684 A0 19930820; FI 933684 A 19930906; HK 1026419 A1 20001215; HU 211344 A9 19951128; HU 227823 B1 20120328; HU 9302377 D0 19931129; HU T65548 A 19940628; IE 920545 A1 19920826; IL 100965 A0 19921115; IL 100965 A 19991231; JP 2901160 B2 19990607; JP 3292830 B2 20020617; JP H06508605 A 19940929; JP H10147586 A 19980602; KR 0172590 B1 19990201; MX 9200747 A 19920901; MY 114350 A 20021031; NO 2005015 I1 20050711; NO 2005015 I2 20071001; NO 2008010 I1 20080707; NO 312399 B1 20020506; NO 932980 D0 19930820; NO 932980 L 19930820; NZ 241625 A 19960326; NZ 250842 A 19960326; PT 100151 A 19930531; PT 100151 B 19990930; RO 119365 B1 20040830; RO 122814 B1 20100226
DOCDB simple family (application)
US 9201339 W 19920220; AT 04076245 T 19920220; AT 99203367 T 19920220; AU 1561792 A 19920220; AU 3794395 A 19951120; AU 8077398 A 19980817; BG 9806293 A 19930820; BR 9205661 A 19920220; CA 2104399 A 19920220; CA 2513440 A 19920220; CN 02144033 A 20020930; CN 92101981 A 19920222; CN 95109814 A 19950818; CN 98108905 A 19980515; CS 49792 A 19920220; DE 69233379 T 19920220; DE 69233786 T 19920220; DK 04076245 T 19920220; DK 99203367 T 19920220; EP 04076245 A 19920220; EP 92908027 A 19920220; EP 99203367 A 19920220; ES 04076245 T 19920220; ES 99203367 T 19920220; FI 20030932 A 20030624; FI 933684 A 19930820; HK 00105566 A 19981228; HU 9302377 A 19920220; HU 9500510 P 19950628; IE 920545 A 19920221; IL 10096592 A 19920217; JP 34046997 A 19971106; JP 50754992 A 19920220; KR 930702516 A 19930821; MX 9200747 A 19920221; MY PI19920287 A 19920221; NO 2005015 C 20050701; NO 2008010 C 20080613; NO 932980 A 19930820; NZ 24162592 A 19920217; NZ 25084292 A 19920217; PT 10015192 A 19920221; RO 00400584 A 19920220; RO 9301137 A 19920220