Use of C2-substituted indan-1-ol systems for preparing medicaments for the prophylaxis or treatment of obesity

Abstract

Embodiments of the invention relate to methods of reducing weight in mammals and for the prophylaxis or treatment of obesity comprising administration of of C2-substituted indan-1-ol systems and their physiologically acceptable salts and physiologically functional derivatives. Compounds for use in the methods of the embodiments of the invention include compounds of the formula (I) in which the radicals are as defined, and their physiologically acceptable salts.

We claim:  
     
         1 . A method of controling weight in a mammal comprising administering to the mammal at least one compound chosen from at least one compound of the formula (I)  
       
         
           
           
               
               
           
         
       
       in which 
 R1,R2,R3,R4 independently of one another are H, F, Cl, Br, I, CN; N 3 , NO 2 , OH, O(C 1 -C 8 )-alkyl, O(C 3 -C 4  and C 6 -C 8 )-cycloalkyl, O—CH 2 -phenyl, O-phenyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 0 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N-[(C 1 -C 8 )-alkyl] 2 , N-[(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 1 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H, SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —NH—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , NH—SO 2 —(C 1 -C 8 )-alkyl, NH—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, (C 2 -C 8 )-alkenyl, (C 2 -C 8 )-alkynyl, wherein the alkyl, cycloalkyl, alkenyl and alkynyl groups in each case have zero to seven hydrogen atoms replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH 3 , O—CH 2 -Ph, NH 2 , NH—CO—CH 3  or N(COOCH 2 Ph) 2 ; or 
 phenyl, 1- or 2-naphthyl,  
 5-tetrazolyl, 1-[(C 1 -C 6 )-alkyl]-5-tetrazolyl,  
 2-[(C 1 -C 6 )-alkyl]-5-tetrazolyl;  
 1-imidazolyl,  
 1- or 4-[1,2,4]-triazolyl,  
 2- or 3-thienyl,  
 2- or 3-furyl,  
 2-, 3- or 4-pyridyl,  
 2-, 4- or 5-oxazolyl,  
 3-, 4- or 5-isoxazolyl,  
 2-, 4- or 5-thiazolyl,  
 3-, 4- or 5-isothiazolyl  
 where the aryl radical or heterocycle is unsubstituted or substituted one to two times by F, Cl, Br, CN, OH, (C 1 -C 4 )-alkyl, CF 3 , O—(C 1 -C 4 )-alkyl, S(O) 0-2 (C 1 -C 6 )-alkyl, NH 2 , NH—SO 2 —(C 1 -C 4 )-alkyl,  
 COOH, CO—O—(C 1 -C 4 )-alkyl, CO—NH 2 , wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
 
 or R2 and R3 together form the group —O—CH 2 —O—;  
 X is S, SO, or SO 2 ;  
 Y is (CH 2 ) p , where p is 0, 1, 2 or 3;  
 R5 is CF 3 , (C 1 -C 18 )-alkyl, or (C 3 -C 8 )-cycloalkyl, wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine; 
 (CH 2 ) r —COR6, where r is 1-6 and R6 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ;  
 CH 2 —CH(NHR7)—COR8, where R7 is H, C(O)—(C 1 -C 4 )-alkyl or C(O)O—(C 1 -C 4 )-alkyl and R8 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ; or  
 phenyl, 1- or 2-naphthyl, biphenyl or a heterocyclic radical, where the rings or ring systems are unsubstituted or substituted one or two times by F, Cl, Br, I, CN, OH, O(C 1 -C 8 )-alkyl, O(C 3 -C 8 )-cycloalkyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N-[(C 1 -C 8 )-alkyl] 2 , N-[(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 2 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H; SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —N H—(C 3 -C 8 )-cycloalkyl, N H—SO 2 —N H 2 , N H—SO 2 —(C 1 -C 8 )-alkyl, NH—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, where in the alkyl and cycloalkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
 
 or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.  
 
     
     
         2 . The method of  claim 1 , wherein 
 R1, R4 independently of one another are 
 H, F, Cl, Br, I, CN, N 3 , NO 2 , OH, O(C 1 -C 8 )-alkyl, O(C 3 -C 4  and C 6 -C 8 )-cycloalkyl, O—CH 2 -phenyl, O-phenyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N[(C 1 -C 8 )-alkyl] 2 , N[(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 1 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H, SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —NH—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , NH—SO 2 —(C 1 -C 8 )-alkyl, NH—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO-O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )—, alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, (C 2 -C 8 )-alkenyl, (C 2 -C 8 )-alkynyl, where in the alkyl, cycloalkyl, alkenyl and alkynyl groups in each case have zero to seven hydrogen atoms replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH 3 , O—CH 2 —Ph, NH 2 , NH—CO—CH 3  or N(COOCH 2 Ph) 2 ; or  
 phenyl, 1- or 2-naphthyl,  
 5-tetrazolyl, 1-[(C 1 -C 6 )-alkyl]-5-tetrazolyl, 2-[(C 1 -C 6 )-alkyl]-5-tetrazolyl,  
 1-imidazolyl,  
 1- or 4-[1,2,4]-triazolyl,  
 2- or 3-thienyl,  
 2- or 3-furyl,  
 2-, 3- or 4-pyridyl,  
 2-, 4- or 5-oxazolyl,  
 3-, 4- or 5-isoxazolyl,  
 2-, 4- or 5-thiazolyl, or  
 3-, 4- or 5-isothiazolyl  
 where the aryl radical or heterocycle are unsubstituted or substituted one or two times by  
 F, Cl, Br, CN,  
 OH, (C 1 -C 4 )-alkyl, CF 3 , O—(C 1 -C 4 )-alkyl,  
 S(O)0-2(C 1 -C 6 )-alkyl, NH 2 , NH—SO 2 —(C 1 -C 4 )-alkyl,  
 COOH, CO—O—(C 1 -C 4 )-alkyl, or CO—NH 2  wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
   R2, R3 independently of one another are 
 H, F, Cl, Br, I, CN, N 3 , NO 2 , O(C 1 -C 8 )-alkyl, O(C 3 -C 8 )-cycloalkyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N [(C 1 -C 8 )-alkyl] 2 , N-[(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 1 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H, SO 2 —NH 2 , SO 2 —NH—(C 5 -C 8 )-alkyl, SO 2 —NH—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , NH—SO 2 —(C 1 -C 8 )-alkyl, NH—SO 2 —(C 5 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, (C 2 -C 8 )-alkenyl, or (C 2 -C 8 )-alkynyl, where in the alkyl, cycloalkyl, alkenyl and alkynyl groups in each case have zero to seven hydrogen atoms replaced by fluorine,  
 or one hydrogen may be replaced by OH, OC(O)CH 3 , O—CH 2 —Ph, NH 2 , NH—CO—CH 3  or N(COOCH 2 Ph) 2 ; or  
 phenyl, 1- or 2-naphthyl,  
 5-tetrazolyl,  
 1-[(C 1 -C 6 )-alkyl]-5-tetrazolyl,  
 2-[(C 1 -C 6 )-alkyl]-5-tetrazolyl,  
 1-imidazolyl,  
 1- or 4-[1,2,4]-triazolyl,  
 2- or 3-thienyl,  
 2- or 3-furyl,  
 2-, 3- or 4-pyridyl,  
 2-, 4- or 5-oxazolyl,  
 3-, 4- or 5-isoxazolyl,  
 2-, 4- or 5-thiazolyl, or  
 3-, 4- or 5-isothiazolyl  
 where the heterocycle is unsubstituted or substituted one or two times by F, Cl, Br, CN, OH, (C 1 -C 4 )-alkyl, CF 3 , O—(C 1 -C 4 )-alkyl,  
 S(O) 0-2 (C 1 -C 6 )-alkyl, NH 2 , NH—SO 2 —(C 1 -C 4 )-alkyl,  
 COOH, CO—O—(C 1 -C 4 )-alkyl, or CO—NH 2  wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
   or R2 and R3 together form the group —O—CH 2 —O—;    where in each case at least one of the radicals R1, R2, R3 and R4 is different from hydrogen;    X is S, SO, or SO 2 ;    Y is (CH 2 ) p , where p is 0, 1, 2 or 3;    R5 is (C 1 -C 18 )-alkyl, or (C 3 -C 4 — and C 6 -C 8 )-cycloalkyl, wherein the alkyl or cycloalkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine; 
 (CH 2 ) r —COR6, where r is 1-6 and R6 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ;  
 CH 2 —CH(NHR7)—COR8, where R7 is H, C(O)—(C 1 -C 6 )-alkyl or C(O)O— 
 (C 1 -C 6 )-alkyl and R8 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ;  
 phenyl, 1- or 2-naphthyl, biphenyl or a heterocyclic radical, where the rings or ring systems are unsubstituted or substituted up to two times by O(C 1 -C 8 )-alkyl, O(C 3 -C 8 )-cycloalkyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N-[(C 1 -C 8 )-alkyl]2, N-[(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 2 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H, SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —NH—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , NH—SO 2 —(C 1 -C 18 )-alkyl, NH—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, or (C 3 -C 8 )-cycloalkyl, where in the alkyl and cycloalkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
   or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         3 . The method of  claim 1 , wherein 
 R1, R4 independently of one another are H, F, Cl, or Br;    R2, R3 independently of one another are 
 H, F, Cl, Br, CN,CONH 2 , NH—SO 2 —(C 1 -C 8 )-alkyl, O—(C 1 -C 8 )-alkyl, COOH, (C 1 -C 8 )-alkyl, (C 1 -C 8 )-alkenyl, or (C 1 -C 8 )-alkynyl, where in the alkyl, alkenyl and alkynyl groups in each case have zero to seven hydrogen atoms replaced by fluorine; or  
 phenyl or 1-imidazolyl; where the rings are unsubstituted or substituted one or two times by  
 F, Cl, Br, CN, OH, (C 1 -C 4 )-alkyl, CF 3 , O—(C 1 -C 4 )-alkyl,  
 wherein the alkyl groups in each case have zero to seven hydrogen atoms may be replaced by fluorine;  
   where in each case at least one of the radicals R1, R2, R3 and R4 is different from hydrogen;    X is S, SO, or SO 2 ;    Y is (CH 2 ) p , where p is 0 or 1;    R5 is (C 1 -C 18 )-alkyl, or (C 3 -C 4 — and C 6 -C 8 )-cycloalkyl, wherein the alkyl or cycloalkyl groups have zero to seven hydrogen atoms replaced by fluorine; 
 (CH 2 ) r —CO—O—(C 1 -C 6 )-alkyl, where r is 1-6;  
 CH 2 —CH(NHR7)—COR8, where R7 is H, C(O)—(C 1 -C 4 )-alkyl or C(O)O—(C 1 -C 4 )-alkyl and R8 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ;  
 phenyl, or a heterocyclic radical;  
   or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         4 . The method of  claim 1 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 3 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         5 . The method of  claim 1 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 3 ,    X is S, and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         6 . The method of  claim 1 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 2 CH 3 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         7 . The method of  claim 1 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH(CH 3 ) 2 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         8 . The method according to  claim 1 , wherein said at least one compound is administered in combination with at least one weight controlling active compound.  
     
     
         9 . The method of  claim 8 , wherein said at least one weight controlling active compound is chosen from cathine, phenylpropanolamine, amfepramone, mefenorex, ephedrine, leptin, dexamphetamine, amphetamine, fenfluramine, dexfenfluramine, sibutramine, orlistat, mazindol or phentermine or salts thereof.  
     
     
         10 . A method for the treatment of obesity in a mammal comprising administering to a mammal in need thereof at least one compound chosen from at least one compound of the formula (I)  
       
         
           
           
               
               
           
         
       
       in which 
 R1,R2,R3,R4 independently of one another are H, F, Cl, Br, I, CN; N 3 , NO 2 , OH, O(C 1 -C 8 )-alkyl, O(C 3 -C 4  and C 6 -C 8 )-cycloalkyl, O—CH 2 -phenyl, O-phenyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N[(C 1 -C 8 )-alkyl] 2 , N [(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 1 -C 8 )—alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H, SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —NH—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , NH—SO 2 —(C 1 -C 8 )-alkyl, NH—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, (C 2 -C 8 )-alkenyl, (C 2 -C 8 )-alkynyl, wherein the alkyl, cycloalkyl, alkenyl and alkynyl groups in each case have zero to seven hydrogen atoms replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH 3 , O—CH 2 -Ph, NH 2 , NH—CO—CH 3  or N(COOCH 2 Ph) 2 ; or 
 phenyl, 1- or 2-naphthyl,  
 5-tetrazolyl, 1-[(C 1 -C 6 )-alkyl]-5-tetrazolyl,  
 2-[(C 1 -C 6 )-alkyl]-5-tetrazolyl;  
 1-imidazolyl,  
 1- or 4-[1,2,4]-triazolyl,  
 2- or 3-thienyl,  
 2- or 3-furyl,  
 2-, 3- or 4-pyridyl,  
 2-, 4- or 5-oxazolyl,  
 3-, 4- or 5-isoxazolyl,  
 2-, 4- or 5-thiazolyl,  
 3-, 4- or 5-isothiazolyl  
 where the aryl radical or heterocycle is unsubstituted or substituted one to two times by F, Cl, Br, CN, OH, (C 1 -C 4 )-alkyl, CF 3 , O—(C 1 -C 4 )-alkyl, S(O) 0-2 (C 1 -C 6 )-alkyl, NH 2 , NH—SO 2 —(C 1 -C 4 )-alkyl,  
 COOH, CO—O—(C 1 -C 4 )-alkyl, CO—NH 2 , wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
 
 or R2 and R3 together form the group —O—CH 2 —O—;  
 X is S, SO, or SO 2 ;  
 Y is (CH 2 ) p , where p is 0, 1, 2 or 3;  
 R5 is CF 3 , (C 1 -C 18 )-alkyl, or (C 3 -C 8 )-cycloalkyl, wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine; 
 (CH 2 ) r —COR6, where r is 1-6 and R6 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ;  
 CH 2 —CH(NHR7)—COR8, where R7 is H, C(O)—(C 1 -C 4 )-alkyl or C(O)O—(C 1 -C 4 )-alkyl and R8 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ; or  
 phenyl, 1- or 2-naphthyl, biphenyl or a heterocyclic radical, where the rings or ring systems are unsubstituted or substituted one or two times by F, Cl, Br, I, CN, OH, O(C 1 -C 8 )-alkyl, O(C 3 -C 8 )-cycloalkyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N-[(C 1 -C 8 )-alkyl] 2 , N-[(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 2 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H; SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —N H—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , N H—SO 2 —(C 1 -C 8 )-alkyl, NH—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, where in the alkyl and cycloalkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
 
 or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.  
 
     
     
         11 . The method of  claim 10 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 3 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         12 . The method of  claim 10 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 3     X is S, and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         13 . The method of  claim 10 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 2 CH 3 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0 or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         14 . The method of  claim 10 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH(CH 3 ) 2 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         15 . The method according to  claim 10 , wherein said at least one compound is administered in combination with at least one weight controlling active compound.  
     
     
         16 . The method of  claim 15 , wherein said at least one weight controlling active compound is chosen from cathine, phenylpropanolamine, amfepramone, mefenorex, ephedrine, leptin, dexamphetamine, amphetamine, fenfluramine, dexfenfluramine, sibutramine, orlistat, mazindol or phentermine or salts thereof.  
     
     
         17 . A method for the treatment of at least one disorder chosen from type II diabetes, arteriosclerosis, hyperlipidemia, and high blood pressure in a mammal comprising administering to a mammal in need thereof at least one compound chosen from at least one compound of the formula (I)  
       
         
           
           
               
               
           
         
       
       in which 
 R1,R2,R3,R4 independently of one another are H, F, Cl, Br, I, CN; N 3 , NO 2 , OH, O(C 1 -C 8 )-alkyl, O(C 3 -C 4  and C 6 -C 8 )-cycloalkyl, O—CH 2 -phenyl, O-phenyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N-[(C 1 -C 8 )-alkyl] 2 , N-[(C 3 -C 8 )-cycloalkyl] 2 , NH—CO—(C 1 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H, SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —NH—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , NH—SO 2 —(C 1 -C 8 )-alkyl, NH—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, (C 2 -C 8 )-alkenyl, (C 2 -C 8 )-alkynyl, wherein the alkyl, cycloalkyl, alkenyl and alkynyl groups in each case have zero to seven hydrogen atoms replaced by fluorine, or one hydrogen may be replaced by OH, OC(O)CH 3 , O—CH 2 -Ph, NH 2 , NH—CO—CH 3  or N(COOCH 2 Ph) 2 ; or 
 phenyl, 1- or 2-naphthyl,  
 5-tetrazolyl, 1-[(C 1 -C 6 )-alkyl]-5-tetrazolyl,  
 2-[(C 1 -C 6 )-alkyl]-5-tetrazolyl;  
 1-imidazolyl,  
 1- or 4-[1,2,4]-triazolyl,  
 2- or 3-thienyl,  
 2- or 3-furyl,  
 2-, 3- or 4-pyridyl,  
 2-, 4- or 5-oxazolyl,  
 3-, 4- or 5-isoxazolyl,  
 2-, 4- or 5-thiazolyl,  
 3-, 4- or 5-isothiazolyl  
 where the aryl radical or heterocycle is unsubstituted or substituted one to two times by F, Cl, Br, CN, OH, (C 1 -C 4 )-alkyl, CF 3 , O—(C 1 -C 4 )-alkyl, S(O) 0-2 (C 1 -C 6 )-alkyl, NH 2 , NH—SO 2 —(C 1 -C 4 )-alkyl,  
 COOH, CO—O—(C 1 -C 4 )-alkyl, CO—NH 2 , wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
 
 or R2 and R3 together form the group —O—CH 2 —O—;  
 X is S, SO, or SO 2 ;  
 Y is (CH 2 ) p , where p is 0, 1, 2 or 3;  
 R5 is CF 3 , (C 1 -C 18 )-alkyl, or (C 3 -C 8 )-cycloalkyl, wherein the alkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine; 
 (CH 2 ) r —COR6, where r is 1-6 and R6 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ;  
 CH 2 —CH(NHR7)—COR8, where R7 is H, C(O)—(C 1 -C 4 )-alkyl or C(O)O—(C 1 -C 4 )-alkyl and R8 is OH, O—(C 1 -C 6 )-alkyl or NH 2 ; or  
 phenyl, 1- or 2-naphthyl, biphenyl or a heterocyclic radical, where the rings or ring systems are unsubstituted or substituted one or two times by F, Cl, Br, I, CN, OH, O(C 1 -C 8 )-alkyl, O(C 3 -C 8 )-cycloalkyl, O—CO—(C 1 -C 8 )-alkyl, O—CO—(C 3 -C 8 )-cycloalkyl, S(O) 0-2 (C 1 -C 8 )-alkyl, S(O) 0-2 (C 3 -C 8 )-cycloalkyl, NH 2 , NH—(C 1 -C 8 )-alkyl, NH—(C 3 -C 8 )-cycloalkyl, N-[(C 1 -C 8 )-alkyl] 2 , N [(C 3 -C 8 )-cycloalkyl] 2 , N H—CO—(C 2 -C 8 )-alkyl, NH—CO—(C 3 -C 8 )-cycloalkyl, SO 3 H; SO 2 —NH 2 , SO 2 —NH—(C 1 -C 8 )-alkyl, SO 2 —NH—(C 3 -C 8 )-cycloalkyl, NH—SO 2 —NH 2 , NH—SO 2 —(C 1 -C 8 )-alkyl, N H—SO 2 —(C 3 -C 8 )-cycloalkyl, O—CH 2 —COOH, O—CH 2 —CO—O(C 1 -C 8 )-alkyl, COOH, CO—O(C 1 -C 8 )-alkyl, CO—O—(C 3 -C 8 )-cycloalkyl, CO—NH 2 , CO—NH(C 1 -C 8 )-alkyl, CO—N-[(C 1 -C 8 )-alkyl] 2 , (C 1 -C 8 )-alkyl, (C 3 -C 8 )-cycloalkyl, where in the alkyl and cycloalkyl groups in each case have zero to seven hydrogen atoms replaced by fluorine;  
 
 or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.  
 
     
     
         18 . The method of  claim 17 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 3 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         19 . The method of  claim 17 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 3 ,    X is S, and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         20 . The method of  claim 17 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH 2 CH 3 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         21 . The method of  claim 17 , wherein 
 R1 is H,    R2 is Cl,    R3 is H,    R4 is H,    R5 is CH(CH 3 ) 2 ,    X is SO 2 , and    Y is (CH 2 ) p  where p is 0    or a physiologically tolerable salt thereof, in any stereoisomeric form, or a mixture of any such compounds in any ratio.    
     
     
         22 . The method according to  claim 1 , wherein said at least one compound is administered in combination with at least one antidiabetic compound.  
     
     
         23 . The method of  claim 22 , wherein said at least one antidiabetic compound is chosen from insulins, amylin GL-1 and GLP-2 derivatives, and oral hypoglycemic active compounds.  
     
     
         24 . The method of  claim 23 , wherein said oral hypoglycemic active compounds are chosen form sulfonyl ureas, biguamides, meglitinides, oxadiazolidinediones, thiazolidinediones, glucosidase inhibitors, glucagon receptor antagonists, GLP-1 agonists, potassium channel openers, insulin sensitizers, activators of insulin receptor kinase, glycogen phosphorylase inhibitors, and modulators of glucose uptake and glucose elimination,  
     
     
         25 . The method of  claim 24 , wherein said sulfonylureas are chosen from tolbutamide, glibenclamide, glimepiride, glipizide, gliquidone, glisoxepide, glibornuride and gliclazide.  
     
     
         26 . The method according to  claim 1 , wherein said at least one compound is administered in combination with at least one additional compound chosen from antihyperlipidemic active compounds and antilipidemic active compounds.  
     
     
         27 . The method according to  claim 26 , wherein said at least one additional compound is chosen from cholestyramine, colestipol, clofibrate, gemfibrozil, lovastatin, pravastatin, simvastatin, atorvastatin, cerivastatin, fluvastatin, probucol, ezetimibe and dextrothyroxine.  
     
     
         28 . The method according to  claim 1 , wherein said at least one compound is administered in combination with at least one antihypertensive active compound.  
     
     
         29 . The method according to  claim 28 , wherein said at least one antihypertensive active compound is chosen from betablockers, ACE (angiotensin-converting enzyme) inhibitors, calcium channel blockers and alphablockers.