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Treatment and prophylaxis of diseases caused by parasites, or bacteria
   
Document Number
US Patent 5985935
Issued Date
November 16, 1999
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Abstract
Aromatic compounds, or prodrugs thereof, which contain an alkylating site and which are capable of alkylating the thiol group in N-acetyl-L-cysteine, in particular bis-aromatic .alpha.,.beta.-unsaturated ketones, are used for the preparation of pharmaceutical compositions or medicated feed, food or drinking water for the treatment or prophylaxis of diseases caused by microorganisms or parasites, in particular protozoa such as Leishmannia, Trypanosoma, Toxoplasma, Plasmodium, Pneumocystis, Babesia and Theileria, intestinal protozoa such as Trichormionas and Ciardia; Coccidia such as Eimeria, Isospora, Cryptosporidium; Cappilaria, Microsporidium, Sarcocystis. Trichlodina, Trichoditella, Dacihylogurus, Pseudodacthylogurus, Acantocephalus, Ichthylophtherius, Botrecephalus; and intracellular bacteria, in particular Mycobacterium, Legionella species, Listeria and Salmonella. Preferred compounds have the formula (II): X.sub.m --Ph--C(O)--CH.dbd.CH--Ph--Y.sub.n, wherein each phenyl group (Ph) may be mono- or polysubstituted; X and Y designate AR.sub.H or AZ, wherein A is O, S, NH or N(C.sub.1-6 alkyl), R.sub.H designates aliphatic hydrocarbyl, and Z is H or a masking group which is decomposed to liberate AH; m is 0, 1 or 2, and n is 0, 1, 2 or 3, whereby, when m is 2, then the two X are the same or different, and when n is 2 or 3, then the two or three Y are the same or different, with the proviso that n and m are not both 0. As examples of such compounds, chalcones, e.g. licochalcone A (obtainable i.a. from batches of Chinese licorice root of Glycyrrhiza species, e.g. G. uralensis or G. inflata) as well as hydroxy, alk(en)yl, and/or alk(en)yloxy analogues thereof are active in vitro and/or in vivo against i.a. L. major and P. falciparum.
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Number of Claims:
47
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Owner
Statens Seruminstitut (Copenhagen,DK)
Published
November 16, 1999
Application Number
08/302,726
Filed
November 1, 1994
US Classification
514/679  
Int'l Classification
A61K   31/34   (20060101)   C07C   323/00   (20060101)   C07C   323/59   (20060101)   C07C   271/44   (20060101)   C07C   49/84   (20060101)   C07C   47/575   (20060101)   C07D   207/333   (20060101)   C07D   207/00   (20060101)   C07C   271/00   (20060101)   C07C   49/835   (20060101)   C07C   49/00   (20060101)   C07C   47/52   (20060101)   C07K   5/02   (20060101)   C07K   5/00   (20060101)   A61K   31/135   (20060101)   A61K   31/12   (20060101)   A61K   31/27   (20060101)   A61K   31/21   (20060101)   A61K   31/165   (20060101)   A61K   31/22   (20060101)   C07D   303/00   (20060101)   C07D   303/32   (20060101)   C07C   45/78   (20060101)   C07C   45/62   (20060101)   C07C   45/67   (20060101)   C07C   45/00   (20060101)   C07C   45/74   (20060101)   C07D   307/00   (20060101)   C07C   45/71   (20060101)   C07D   307/46   (20060101)   C07D   311/00   (20060101)   C07D   311/64   (20060101)   C07C   69/00   (20060101)   C07C   69/24   (20060101)  
Examiner
Priority Data
Mar 06, 1992 [DK] 0312/92 Sep 30, 1992 [DK] 1208/92
USPTO Field of Search
514/679  
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