Global Patent Index - EP 0434714 A1

EP 0434714 A1 19910703 - IN POSITION 3 SUBSTITUTED-5-BETA-AMIDOMETHYL-OXAZOLIDIN-2-ONES.

Title (en)

IN POSITION 3 SUBSTITUTED-5-BETA-AMIDOMETHYL-OXAZOLIDIN-2-ONES.

Title (de)

IN STELLUNG3-SUBSTITUIERTE 5-BETA-AMIDOMETHYLOXAZOLINDEN-2-ON-DERIVATE.

Title (fr)

5-BETA-AMIDOMETHYLE-OXAZOLIDINE-2-ONES A SUBSTITUTION EN POSITION 3.

Publication

EP 0434714 A1 19910703 (EN)

Application

EP 89909990 A 19890822

Priority

  • US 24498888 A 19880915
  • US 25385088 A 19881005
  • US 32494289 A 19890317

Abstract (en)

[origin: DK175940B1] of formulae (XI) and (XIII), 3-(fused ring substd.)phenyl-5 beta -(amidomethyl)oxazolidin-2-ones of formula (XXI), and 3-(N-substd.)phenyl-5 beta (aminodimethyl)oxazolidin-2-ones of formula (IV), and their salts are new: where in (XI); R1 = e.g. H, 1-12C alkyl (opt. substd. with 1-3 Cl), 3-12C cycloalkyl, 5-12C monosubstd. alkenyl, phenyl furanyl, tetrahydrofuranyl or 2-thiophene etc. 2 of R2, R3, R4 = H and the other = e.g. H, F, Cl, Br, I or 1-6C alkyl etc. R5 = e.g. H, 1-12C alkyl, benzyl, phenethyl, 3-7C cycloalkyl, 2-12C alkenyl contg. 1-3 double bonds, 2-12C alkynyl contg. 1 triple bond, -CHO etc. in (XIII), X1 = Ac, -COOtBn, -COOCH2Ph or -COO(CH2)2SiMe3; R2, R3, R4 = as above; and R6 = I, N3 or NH2; in (XXI), R1 = as above; R2 or R4 = H and the other together with R3 is -(CH2)n3-(CR10-1R10-2)n7 -CO-(CR10-3R10-4)n8-(CH2)n4-, -(CH2)n5-CH=CH-(CH2)n6- or -(CH2)n3-(CR10-1 R10-2)n7-C(:NOR7)-(CR10-3R10-4)n8-(CH2)n4-; n3, n4 = 0-3; n7, n8 = 0 or 1; R10-1, R10-2 = H or 1-3C alkyl or together complete spirocyclopropyl; R10-3, R10-4 = H or 1-3C alkyl or together complete spirocyclopropyl; with the provisos that (1) n7 + n8 = 1 or (b) n7 = 1 and one of R10-1 or R10-2 is not H; n5, n6 = 0-2; n5 + n6 = 1 or 2; R7 = H, 1-4C alkyl, -CH2COOH or -CH2COOR7-1; R7-1 = 1-4C alkyl; R5 or R6 = H and the other is as for R5 in (XI) above; in (IV), R1, R2, R3, R4 = as in (XI); W1 and W2 together = -NR5-N=CR'6-, -NR5-CR''6=N-or -NR5-N=N-; and R5 = as in (XI); R'6 = H or 1-3C alkyl; and R''6 = H, 1-6C alkyl, SH, SMe, Set, SPh, SOMe, SOPh, SO2Me or SO2Ph.

Abstract (fr)

Des 5'-indolinyloxazolidine-2-ones de la formule (XI), 3-phényle (à substitution par combinaison cyclique condensée)-5beta-amidométhyloxazolidine-2-ones (XXI), et 3-phényle(à substitution azote)-5beta-amidométhyloxazolidine-2-ones (LV) sont des agents antibactériens utiles; et les intermédiaires (VI), (VII) et (VIII) sont utiles à leur production.

IPC 1-7

A61K 31/42; C07D 263/20; C07D 413/04; C07D 413/14

IPC 8 full level

C07D 263/24 (2006.01); A61K 31/42 (2006.01); A61K 31/421 (2006.01); A61P 31/04 (2006.01); A61P 31/12 (2006.01); A61P 37/04 (2006.01); C07D 263/20 (2006.01); C07D 413/04 (2006.01)

CPC (source: EP KR)

A61P 31/04 (2018.01 - EP); A61P 31/12 (2018.01 - EP); A61P 37/04 (2018.01 - EP); C07D 263/20 (2013.01 - EP); C07D 413/04 (2013.01 - EP KR)

Designated contracting state (EPC)

AT BE CH DE FR GB IT LI LU NL SE

DOCDB simple family (publication)

EP 0359418 A1 19900321; EP 0359418 B1 19941012; AT E112773 T1 19941015; AT E201870 T1 20010615; AU 4195789 A 19900402; AU 617871 B2 19911205; CA 1335103 C 19950404; DE 68918792 D1 19941117; DE 68918792 T2 19950330; DE 68929303 D1 20010712; DE 68929303 T2 20020502; DK 175696 B1 20050124; DK 175940 B1 20050801; DK 200401246 A 20040818; DK 45591 A 19910313; DK 45591 D0 19910313; EP 0434714 A1 19910703; EP 0609905 A1 19940810; EP 0609905 B1 20010606; ES 2157934 T3 20010901; GR 3036491 T3 20011130; HK 1002234 A1 19980807; JP 2865211 B2 19990308; JP 3188418 B2 20010716; JP H04500665 A 19920206; JP H1180139 A 19990326; KR 0138262 B1 19980515; KR 900701780 A 19901204; LV 12888 B 20021220; TW 219936 B 19940201; WO 9002744 A1 19900322

DOCDB simple family (application)

EP 89308506 A 19890822; AT 89308506 T 19890822; AT 94102762 T 19890822; AU 4195789 A 19890822; CA 609594 A 19890828; DE 68918792 T 19890822; DE 68929303 T 19890822; DK 45591 A 19910313; DK PA200401246 A 20040818; EP 89909990 A 19890822; EP 94102762 A 19890822; ES 94102762 T 19890822; GR 20010401350 T 20010831; HK 98101252 A 19980218; JP 19194998 A 19980707; JP 50925589 A 19890822; KR 900701012 A 19900515; LV 020104 A 20020606; TW 78106662 A 19890829; US 8903548 W 19890822