Global patent index - EP 0968199 A1

EP 0968199 A1 2000-01-05 - ANTIBACTERIAL HETEROCYCLIC AMINO ACID DERIVATIVES

Title (en)

ANTIBACTERIAL HETEROCYCLIC AMINO ACID DERIVATIVES

Title (de)

ANTIBAKTERIELLE HETEROCYCLISCHE AMINOSÄUREDERIVATE

Title (fr)

DERIVES D'ACIDE AMINE HETEROCYCLIQUE ANTIBACTERIEN

Publication

EP 0968199 A1 (EN)

Application

EP 98913662 A

Priority

  • EP 9801278 W
  • GB 9704522 A

Abstract (en)

[origin: WO9839311A1] A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a beta -lactam antibiotic, a therapeutically effective amount of an amino acid derivative or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof: (i) or (ii), wherein X is S, S(O)p or CH2 where p is 1 or 2; R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R1 and R2 are selected from halogen, mercapto, (C1-6)alkyl optionally substituted by 1-3 halo, phenyl, (C1-6)alkoxy optionally substituted by 1-3 halo, hydroxy(C1-6)alkyl, mercapto(C1-6)alkyl, hydroxy, CO2R7, N(R7)2 or CON(R7)2 where each R7 is independently hydrogen or (C1-6)alkyl, OCONH2, nitro, (C1-6)alkylcarbonyloxy, (C1-6)alkoxycarbonyl(C1-6)alkyl, formyl, or (C1-6)alkylcarbonyl groups; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C3-7)cycloalkyl, fused aryl(C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl-(CHR10)m-X1-(CHR11)n, heterocyclyl or heterocyclyl-(CHR10)m-X1-(CHR11)n, where m is 0 to 3, n is 1 to 3, each R10 and R11 is independently hydrogen or (C1-4)alkyl and X1 is O, S(O)x where x is 0-2, or a bond; R4 is hydrogen, or an in vivo hydrolysable acyl group; and R5 and R6 are independently hydrogen and (C1-6)alkyl or together represent (CH2)q where q is 2 to 5.

IPC 1-7 (main, further and additional classification)

C07D 279/06; A61K 31/445; A61K 31/47; A61K 31/54; C07D 211/60; C07D 217/26

IPC 8 full level (invention and additional information)

A61K 31/445 (2006.01); A61K 31/47 (2006.01); A61K 31/472 (2006.01); A61K 31/54 (2006.01); A61P 31/04 (2006.01); A61P 43/00 (2006.01); C07D 211/60 (2006.01); C07D 217/26 (2006.01); C07D 279/06 (2006.01); C07D 279/08 (2006.01)

CPC (invention and additional information)

A61K 31/541 (2013.01); A61K 31/445 (2013.01); A61K 31/47 (2013.01); C07D 211/60 (2013.01); C07D 217/26 (2013.01); C07D 279/06 (2013.01)

Citation (search report)

See references of WO 9839311A1

Designated contracting state (EPC)

BE CH DE ES FR GB IT LI NL

EPO simple patent family

WO 9839311 A1 19980911; CA 2282691 A1 19980911; EP 0968199 A1 20000105; GB 9704522 D0 19970423; JP 2001515477 A 20010918

INPADOC legal status

2002-06-12 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20011211

2001-09-12 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20010730

2000-01-05 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 19990818

2000-01-05 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): BE CH DE ES FR GB IT LI NL