BENZYL ARALKYL ETHER COMPOUNDS, METHOD FOR PREPARING SAME, INTERMEDIATE COMPOUNDS, USE OF SAID COMPOUNDS, METHOD FOR TREATMENT AND/OR PREVENTION, PHARMACEUTICAL COMPOSITION AND MEDICAMENT CONTAINING SAME
申请人:Keppler Artur Franz
公开号:US20120196908A1
公开(公告)日:2012-08-02
This invention describes new antifungal compounds that are aralkyl benzyl ethers of the formula (I):
wherein: Ar represents aryl, imidazolil, 1,2,4-triazolyl, benzimidazolil;
R
1
, R
2
, R
4
and R
5
are independently hydrogen, halogen, C
1-6
alkyl;
R
3
represents halogen, C
1-6
alkyl or O—R′ where R′ represents hydrogen or lower alkyl;
R
6
represents aryl, substituted aryl, trifluoromethyl, trichloromethyl or O—R′ where R′ represents hydrogen or lower alkyl; being the substituents of the aryl a halogen or a radical tetrazolyl;
n and m represent independently an integer between 0 and 5;
With the proviso that when Ar is imidazolil, R
3
is chlorine, R
6
is p-phenyl and R
1
, R
2
, R
4
and R
5
are hydrogen, n must be different from 2.
When n and m are not 0 and 1, R
3
or R
6
can be represented by substituents not necessarily equal.
This invention also refers to their salts, solvates, prodrugs, esters, enantiomers and/or pharmaceutically acceptable diastereoisomers, or mixtures thereof, processes for the preparation of these compounds, intermediate compounds, pharmaceutical compositions comprising such compounds and/or derivatives, including those compounds and/or derivatives, as well as the uses and methods of these compounds and/or derivatives for the treatment and/or prevention of conditions and/or diseases caused by microorganisms such as fungi, bacteria and/or protozoa, for the inhibition of proliferation and/or survival of said microorganisms, for the treatment and/or prevention of colonization of microorganisms in an individual, and for the manufacture of a medicine.
该发明描述了一种新的抗真菌化合物,它们是公式(I)的芳基烷基苯醚,其中:Ar代表芳基,咪唑基,1,2,4-三唑基,苯并咪唑基;R1、R2、R4和R5独立地代表氢、卤素、C1-6烷基;R3代表卤素、C1-6烷基或O—R′,其中R′代表氢或较低的烷基;R6代表芳基、取代芳基、三氟甲基、三氯甲基或O—R′,其中R′代表氢或较低的烷基;芳基的取代基是卤素或四唑基基团;n和m分别表示介于0和5之间的整数;但是当Ar为咪唑基,R3为氯,R6为对苯基且R1、R2、R4和R5为氢时,n必须不等于2。当n和m不为0和1时,R3或R6可以用不必相等的取代基表示。该发明还涉及它们的盐、溶剂合物、前药、酯、对映体和/或药学上可接受的对映异构体或它们的混合物,制备这些化合物的过程,中间体化合物,包括这些化合物和/或衍生物的制药组合物,以及这些化合物和/或衍生物的用途和方法,用于治疗和/或预防由微生物引起的疾病和/或疾病,如真菌、细菌和/或原虫,用于抑制这些微生物的增殖和/或生存,用于治疗和/或预防微生物在个体中的定殖,并用于制药。