A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/155 (2006.01) A61K 31/18 (2006.01) A61K 31/33 (2006.01) A61K 31/34 (2006.01) A61K 31/38 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/47 (2006.01) A61K 45/00 (2006.01) A61K 31/00 (2006.01)
Patent
CA 2246407
Use of inhibitors of the sodium-hydrogen exchanger for the production of a pharmaceutical for the treatment of disorders which are caused by protozoa Inhibitors of the sodium-hydrogen exchanger are suitable on their own or in combination with other classes of active compound for the production of a medicament for the treatment of diseases which are caused by protozoa; thus of diseases which are caused by animal- and human-pathogenic protozoa, such as by intracellularly active parasites of the classes Apicomplexa and Zoomastigophorea, in particular trypanosomes, plasmodia (malaria pathogens), leishmanias, babesias and theilerias, cryptosporidiidae, sarcocystidae, amoebae, coccidia and trichomonads. NHE inhibitors are particularly preferably suitable for the production of a medicament for the treatment of tropical malaria, of tertian malaria, of quartan malaria, as well as toxoplasmosis, of coccidiosis, of intestinal sarcosporidosis, of cryptosporidosis, of Chargas' disease and of the cutaneous and visceral as well as other forms of leishmaniases; and also for the production of a medicament for the treatment of animals which have been infected by animal-pathogenic protozoa, such as by Theileria parva, the pathogen of East Coast fever of cattle, Babesia begemina, the pathogen of Texas fever in cattle and buffalo, Babesia bovis, the pathogen of European bovine babesiosis, and babesioses in dogs, cats and sheep, sarcocystidae, the pathogens of sarcocystoses in sheep, cattle and pigs, cryptosporidiidae, the pathogens of cryptosporidosis in cattle and birds, coccidia, the pathogens of coccidioses of rabbits, cattle, sheep, goats and pigs, but in particular of chickens and turkeys. 378 where the phenyl is not substituted or is substituted by 1 - 3 substituents selected from the group consisting of F, Cl, CF3, methyl, methoxy and NR(11)R(12); R(11) and R(12) independently of one another are H, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; R(6) and R(7) independently of one another are hydrogen, F, Cl, Br, I, CN, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, perfluoroalkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, or phenyl, which is not substituted or is substituted by 1 - 3 substituents selected from the group consisting of F, Cl, CF3, methyl, methoxy and NR(14)R(15); R(14) and R(15) independently of one another are H, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; and their pharmaceutically tolerable salts.
Utilisation d'inhibiteurs de l'échangeur sodium-hydrogène (NHE) pour la production d'un composé pharmaceutique permettant de traiter les troubles causés par les protozoaires. Les inhibiteurs de l'échangeur sodium-hydrogène sont utiles seuls ou en combinaison avec d'autres classes de composés actifs pour la production d'un médicament destiné au traitement de maladies provoquées par les protozoaires, notamment les maladies causées par les protozoaires pathogènes pour les animaux et l'homme, comme les parasites actifs au niveau intracellulaire, appartenant aux classes Apicomplexa et Zoomastigophorea, en particulier les trypanosomes, plasmodia (agents pathogènes de la malaria), leishmania, babesia et theileria, cryptosporidiida, sarcocystida, amoeba, coccidia et trichomonadales. Les inhibiteurs NHE sont préférables particulièrement pour la production d'un médicament permettant de traiter la malaria tropicale, la tierce bénigne, la fièvre quarte, ainsi que la toxoplasmose, la coccidiose, la sarcosporidose intestinale, la cryptosporidose, la maladie de Chargas, les leishmaniases cutanées et viscérales et d'autres formes de leishmaniases; et pour la production d'un médicament permettant de traiter des animaux qui ont été infectés par des protozoaires pathogènes pour les animaux, comme Theileria parva, pathogène de la fièvre de la côte orientale chez le bétail, Babesia begemina, pathogène de la fièvre du Texas chez le bétail et le bison, Babesia bovis, pathogène de la babésiose européenne chez les bovins et de la babésiose chez le chien, le chat et le mouton, sarcocystida, pathogène de la sarcocystose chez le mouton, le bétail et le porc, cryptosporidiida, pathogène de la cryptosporidose chez le bétail et les oiseaux, coccidia, pathogène de la coccidiose chez le lapin, le bétail, le mouton, la chèvre et le porc, et surtout chez le poulet et la dinde. Le phényle est sans ou avec substitution par 1-3 substituants choisis parmi F, Cl, et les groupes CF3, méthyle, méthoxy et NR(11)R(12); R(11) et R(12) sont, indépendamment l'un de l'autre, H, un groupe alkyle de 1, 2, 3 ou 4 atomes de carbone, ou perfluoroalkyle de 1, 2, 3 ou 4 atomes de carbone; R(6) et R(7) sont, indépendamment l'un de l'autre, de l'hydrogène, F, Cl, Br, I, CN, un groupe alkyle de 1, 2, 3, 4, 5, 6, 7 ou 8 atomes de carbone, perfluoroalkyle de 1, 2, 3, 4, 5, 6, 7 ou 8 atomes de carbone, cycloalkyle de 3, 4, 5, 6, 7 ou 8 atomes de carbone, ou un phényle sans ou avec substitution par 1-3 substituants choisis parmi F, Cl, CF3, un groupe méthyle, méthoxy et NR(14)R(15); R(14) et R(15) sont, indépendamment l'un de l'autre, H, un alkyle de 1, 2, 3 ou 4 atomes de carbone ou un perfluoroalkyle de 1, 2, 3 ou 4 atomes de carbone. L'invention concerne également leurs sels pharmacocompatibles.
Lang Hans Jochen
Lanzer Michael
Sanchez Cecilia
Wiesner Jochen
Wuensch Stefan
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst Marion Roussel Deutschland Gmbh
Sanofi-Aventis Deutschland Gmbh
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