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Title:
7-BROMO AND 7,7-DIBROMO-CEPHAM AND CEPHEM DERIVARIVES, THEIR PRODUCTION, AND MEDICINES AND VETERINARY MEDICINES CONTAINING THE COMPOUNDS
Document Type and Number:
Japanese Patent JPH11255771
Kind Code:
A
Abstract:

To obtain the subject new compounds useful for preventing, inhibiting or treating diseases caused by the uncontrolled release of a protease, especially emphysema or cystic fibrosis, as inhibitors against a protease, especially against human leucocytic esterase.

A compound of formula I {R1 and R2 are each H or Br; R3 is Br or OH; R4 is methyl; R5 is a group of the formula: OR6 [R6 is H, an alkyl (aryl)] or the like; (n) is 0-2} or a compound of formula II {R3 is methyl; R4 is H or a group of the formula: COOR5 [R5 is H or an alkyl (aryl)] or the like}. For example, 3-bromo-7,7-dibromo-3-methylcepham-4-carboxylic acid benzyl ester. The compound of formula I or formula II is obtained by thermally reacting a compound of formula III {R3 is a group of the formula: OR4 [R4 is H, an alkyl(aryl)] or the like; (n) is 1} in a solvent, if necessary, in the presence of tetrabutylammonium bromide, isolating the product and, if necessary, subsequently oxidizing the product.


Inventors:
LUKIC IRENA
Application Number:
JP36939698A
Publication Date:
September 21, 1999
Filing Date:
December 25, 1998
Export Citation:
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Assignee:
PLIVA PHARM & CHEM WORKS
International Classes:
A61K31/00; A61K31/545; A61K31/546; A61P11/00; A61P31/00; A61P31/04; A61P43/00; C07D501/00; C07D501/10; C07D501/62; (IPC1-7): C07D501/00; A61K31/00; A61K31/545; C07D501/10
Attorney, Agent or Firm:
Shigeru Yagita (2 outside)