公开(公告)号：AU706448B2

公开(公告)日：1999-06-17

申请号：AU6395496

申请日：1996-06-25

Applicant: PATHOGENESIS CORP

Inventor： BAKER WILLIAM R ,  SHAOPEI CAI ,  KEELER ERIC L

IPC: A61K31/535 ,  A61K31/55 ,  A61P31/00 ,  C07D487/04 ,  C07D498/04 ,  C07D498/00 ,  C07D403/00 ,  C07D235/02 ,  C07D223/16

Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial and clostridium infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): (II) wherein R1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NK2, where R2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR3 or SO2R4CONR4R5, where R4 and R5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected CH2, CO, CR4R5 or NR4, where R4 and R5 are as defined above; provided that when n is 2 or 3, the compounds of formula II can be additionally substituted as follows: (IIa) (IIb) wherein R6, R7, R8 and R9 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis and Clostridium difficile.

公开(公告)号：CA2225822C

公开(公告)日：2010-02-16

申请号：CA2225822

申请日：1996-06-25

Applicant: PATHOGENESIS CORP

Inventor： BAKER WILLIAM R ,  SHAOPEI CAI ,  KEELER ERIC L

IPC: C07D498/04 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  A61P31/00 ,  C07D487/04 ,  C07D513/04

Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic microbes in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial, Clostridium, Cryptosporidium and Helicobacter infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): (see formula II) The methods, compounds and compositions are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, Clostridium difficile, Cryptosporidium parvum, and Helicobacter pylori, and may be used alone, or in combination with other antimicrobial agents.

公开(公告)号：CA2225822A1

公开(公告)日：1997-01-16

申请号：CA2225822

申请日：1996-06-25

Applicant: PATHOGENESIS CORP

Inventor： SHAOPEI CAI ,  BAKER WILLIAM R ,  KEELER ERIC L

IPC: A61K31/535 ,  A61K31/55 ,  A61P31/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/505 ,  A61K31/54

Abstract: Method, compounds and compositions are provided for inhibiting the growth of pathogenic microbes in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial, Clostridium, Cryptosporidium and Helicobacter infections, in vivo using bicyclic nitroimidazole compounds. The methods, compounds and compositions are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, Clostridium difficile, Cryptosporidium parvum, and Helicobacter pylori, and may be used alone, or in combination with other antimicrobial agents.

公开(公告)号：AU6395496A

公开(公告)日：1997-01-30

申请号：AU6395496

申请日：1996-06-25

Applicant: PATHOGENESIS CORP

Inventor： BAKER WILLIAM R ,  SHAOPEI CAI ,  KEELER ERIC L

IPC: A61K31/535 ,  A61K31/55 ,  A61P31/00 ,  C07D487/04 ,  C07D498/04 ,  C07D498/00 ,  C07D403/00 ,  C07D235/02 ,  C07D223/16

Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial and clostridium infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): (II) wherein R1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NK2, where R2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR3 or SO2R4CONR4R5, where R4 and R5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected CH2, CO, CR4R5 or NR4, where R4 and R5 are as defined above; provided that when n is 2 or 3, the compounds of formula II can be additionally substituted as follows: (IIa) (IIb) wherein R6, R7, R8 and R9 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis and Clostridium difficile.