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Benzoic acid compounds and use thereof as medicaments

  • US 5,864,039 A
  • Filed: 12/02/1997
  • Issued: 01/26/1999
  • Est. Priority Date: 03/30/1994
  • Status: Expired due to Fees
First Claim
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1. A benzoic acid compound of the formula ##STR72## wherein R1 is a halogen;

  • R2 is a lower alkoxy, a substituted lower alkoxy, a cycloalkyloxy or a cycloalkylalkoxy;

    m is 1 or 2; and

    A is ##STR73## wherein R3 is hydrogen, hydroxy, lower alkyl or lower alkoxy, p is an integer of 1-10, q is 2 or 3, and B is a group of the formula
    
    
    space="preserve" listing-type="equation">--N(R.sup.4)--X.sup.1 --R.sup.5,
    
    
    space="preserve" listing-type="equation">--N(R.sup.4)--X.sup.2 --N(R.sup.6)(R.sup.7),
    
    
    space="preserve" listing-type="equation">--X--N(R.sup.8)(R.sup.9),
    
    
    space="preserve" listing-type="equation">--Het,
    
    
    space="preserve" listing-type="equation">--N(R.sup.10)(R.sup.11),
    
    
    space="preserve" listing-type="equation">--X.sup.3 --R.sup.12 or
    
    
    space="preserve" listing-type="equation">--X.sup.4 --R.sup.13whereinX1 is CO, CS or SO2, X2 is CO or CS, R4 is hydrogen, lower alkyl, phenyl, substituted phenyl, aralkyl or substituted aralkyl, R5 is lower alkyl, cycloalkyl, crosslinked cycloalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl or ##STR74## wherein X5 is halogen, X6 is hydrogen or amino, and X7 is a direct bond, methylene, oxygen atom, NH or N--CH3,R6 and R7 are the same or different and each is hydrogen, lower alkyl, cycloalkyl, aryl, substituted aryl, aralkyl or substituted aralkyl, or R6 and R7 optionally form a ring together with the adjacent nitrogen atom, R8 and R9 are the same or different and each is hydrogen, lower alkyl, cycloalkyl, aryl, substituted aryl, aralkyl or substituted aralkyl or R8 and R9 optionally form a ring together with the adjacent nitrogen atom, Het is a 5- or 6-membered mono- or bicyclic heterocycle having amide or urea in the ring and having 1 to 5 hetero atom(s) selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, R10 and R11 are the same or different and each is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl or substituted heteroarylalkyl, X3 is oxygen atom or sulfur atom, R12 is lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl or substituted heteroarylalkyl, X4 is CO, CS, SO or SO2, and R13 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl or substituted heteroarylalkyl,an optical isomer thereof or a pharmaceutically acceptable salt thereof.

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