Title:
【発明の名称】ベータ―チオプロピオニル―アミノ酸およびそのベータ―ラクタマーゼ阻害剤としての使用
Document Type and Number:
Japanese Patent JP2000506120
Kind Code:
A
Abstract:
PCT No. PCT/EP97/00516 Sec. 371 Date Jan. 13, 1999 Sec. 102(e) Date Jan. 13, 1999 PCT Filed Feb. 3, 1997 PCT Pub. No. WO97/30027 PCT Pub. Date Aug. 21, 1997A 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 of Formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R1 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms or by a mercapto, (C1-6)alkoxy, hydroxy, amino, nitro, carboxy, (C1-6)alkylcarbonyloxy, (C1-6)alkoxycarbonyl, formyl or (C1-6)alkylcarbonyl group, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl(C1-6)alkyl, heterocyclyl or heterocyclyl(C1-6)alkyl; R2 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl; 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-X-(CHR11)n, heterocyclyl or heterocyclyl-(CHR10)m-X-(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 X 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)p where p is 2 to 5. Some compounds are claimed per se.
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Inventors:
Bateson, John Hargreaves
Whitty, David Earl
Gurson, Brian Charles
Best, Desmond John
Payne, David John
Whitty, David Earl
Gurson, Brian Charles
Best, Desmond John
Payne, David John
Application Number:
JP52894697A
Publication Date:
May 23, 2000
Filing Date:
February 03, 1997
Export Citation:
Assignee:
SmithKline Beecham Public Limited Company
International Classes:
A61K31/00; A61K31/195; A61K31/198; A61K31/215; A61K31/216; A61K31/34; A61K31/341; A61K31/38; A61K31/381; A61K31/403; A61K31/404; A61K31/405; A61K31/425; A61K31/426; A61K31/43; A61K31/545; A61K45/06; A61P31/00; A61P31/04; A61P43/00; C07C323/41; C07C323/60; C07C327/30; C07D209/20; C07D209/26; C07D215/14; C07D231/12; C07D233/96; C07D277/20; C07D277/30; C07D307/54; C07D333/24; C07D333/26; C07D333/60; (IPC1-7): A61K31/198; A61P31/04; A61P43/00; A61K31/216; A61K31/405; A61K31/43; A61K31/545; C07C323/41; C07C327/30
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)