IP Library › Granted Patent US 7,211,592
Granted Patent B2
US 7,211,592 · App. 10/939,936 · Granted May 1, 2007

Substituted an unsubstituted benzooxathiazoles and compounds derived therefrom

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Quick Facts
Patent No.
US 7,211,592
App. No.
10/939,936
Granted
May 1, 2007
Kind
B2
Abstract

The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.

Claims (80)

1. A compound of the formula I

in which

X is CH 2 , O or NH;

Y is CH 2 , O or NH;

R1, R2, R3 are each independently of one another

OH, COOH;

CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-,3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl; or in each case two of the radicals R1 and R2 or R2 and R3 or R1 and R3 together form a fused aryl radical, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

or its physiologically acceptable salts or prodrugs.

2. A compound of the formula I as claimed in claim 1 , wherein

X is O or NH;

Y is O or NH;

R1 is OH, COOH;

CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

R2 is OH, COOH;

CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

R3 is OH, COOH;

CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

or its physiologically acceptable salts or prodrugs.

3. A compound of the formula I as claimed in claim 1 , wherein

X is O or NH;

Y is NH;

R1 is OH, COOH;

CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

R2 is OH, COOH;

CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

R3 is COO(C 1 –C 6 )alkyl, CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

O—(C 1 –C 6 )alkyl;

(C 1 –C 6 )alkyl, (C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

or its physiologically acceptable salts or prodrugs.

4. A compound of the formula I as claimed in claim 1 , wherein

X is O;

Y is NH;

R1 is OH, COOH;

CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

R2 is OH, COOH;

COO(C 1 –C 6 )alkyl, CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-, 3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

R3 is COO(C 1 –C 6 )alkyl; CONH 2 , CONH(C 1 –C 16 )alkyl, CONH(C 1 –C 16 )alkenyl, CONH(C 1 –C 6 )alkyl-phenyl, where phenyl may be mono- to trisubstituted by O—(C 1 –C 10 )alkyl or O—(C 1 –C 10 )alkyl-phenyl, CONH(C 1 –C 6 )alkyl-benzimidazole, where the benzimidazole ring may be mono- to trisubstituted by S-phenyl, wherein the S-phenyl may be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

O—(C 1 –C 6 )alkyl;

(C 2 –C 6 )alkenyl, (C 2 –C 6 )alkynyl, (C 1 –C 6 )alkyl-COOH, (C 1 –C 6 )alkyl-aryl, where aryl may be phenyl, naphthyl, biphenyl, thienyl or pyridyl and the aryl moiety may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

Phenyl, biphenyl, 1- or 2-naphthyl, 2-,3- or 4-pyridyl, 2- or 3-furanyl or 2- or 3-thienyl, where the phenyl, biphenyl, naphthyl, pyridyl, furanyl or thienyl rings may in each case be mono- to trisubstituted by F, Cl, Br, I, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 –C 10 )alkyl, NH 2 , NH(C 1 –C 6 )alkyl, COOH, COO(C 1 –C 6 )alkyl, CONH 2 ;

(C 3 –C 18 )cycloalkyl, where in the alkyl radicals one or more hydrogens may be replaced by fluorine or one hydrogen may be replaced by OH, (C 1 –C 6 )alkyl-phenyl or O—(C 1 –C 6 )alkyl-phenyl,

NCO, NSO 3 —(C 1 –C 10 )alkyl;

or its physiologically acceptable salts or prodrugs.

5. A pharmaceutical composition comprising an effective amount of at least one compound as claimed in claim 1 and a pharmaceutically acceptable excipient.

6. A method of preparing a pharmaceutical composition comprising the steps of mixing one or more compounds of claim 1 with one or more pharmaceutically acceptable excipients and bringing this mixture into a form suitable for administration.