Sulfonamidnuyu connection

 

(57) Abstract:

The invention relates to sulfonamidnuyu to the compound of formula I, where R1- alkyl, alkenyl, quinil; a represents optionally substituted heterocyclic group, excluding benzimidazolyl, indolyl, 4,7-dehydrobenzperidol and 2,3-dihydrobenzofuranyl; X - alkylene, oxa, oxa(lower) alkylene; R2- optional substituted aryl, substituted biphenyl, its salts and pharmaceutical compositions comprising this compound. Sulfonamidnuyu compound effective in the treatment of diseases, the possibility of treatment which is based on the activity of the connection to reduce blood sugar levels, inhibitory activity against cGMP-PDE (especially PDE-V), the relaxation activity of smooth muscles, bronchodilatation activity, vasodilatation activity, activity for suppression of smooth muscle cells and anti-allergic activity. 7 C.p. f-crystals, 1 table.

Description text in facsimile form (see graphic part).

1. Sulfonamidnuyu compound of formula (I)

R1-SO2NH-A-X-R2(I)

where R1- alkyl, alkenyl, phenyl(lower)alkenyl, hinely, phenyl, optionally substituted replace what lagena;

Rather it represents a heterocyclic group selected from the group comprising 2,3-dehydrobenzperidol, imidazo[1,2-b]pyrazolyl, imidazo[1,2-a]pyridyl, 1H-imidazo[4,5-b]pyridyl, 3H-imidazo[4,5-b]pyridyl, pyrrolo[3,2-b] pyridyl, pyrazolo[1,2-a]pyridyl, benzothiazolyl, indolizinyl, 1H-indazole 2N-indazole, hinely, dihydroquinoxaline, tetrahydroquinoxaline, dihydroquinazolines, tetrahydroquinazoline, benzo[b]furanyl, benzo[b] thiophenyl and 1H-thieno[2,3-d] imidazolyl and named heterocyclic group optionally substituted by alkyl or oxo;

X - low alkylene, oxa(lower)alkylene or oxa;

R2is phenyl, optionally substituted by a Deputy selected from the group comprising alkyl, alkenyl, quinil, lower alkanoyl, lower alkoxy, phenyl, imidazolyl(lower)alkyl, piperidinyl(lower)alkyl, halogen, amino, lower alkanolamine, mono(lower)alkylamino, di(lower) alkylamino, N-(lower)alkyl-N-acylamino, lower alkylsulfonyl, phenyl(lower)alkylamino, phenylcarbonylamino, benzoylamine, lower alkylsulfonyl, lower alkylsulfonyl, lower alkylthio, cyano, carboxy, lower alkoxycarbonyl, cyclo(lower)alkylaminocarbonyl, mono(lower)allylcarbamate, nitro, halogen(nischalke, cyclo(lower)alkyl(lower)alkoxy, cyclo(lower)alkyl(lower)alkyl, phenoxy(lower)alkyl, lower alkylsulfonate(lower)alkyl, hydroxy(lower)alkyl, di(lower)alkylamino(lower)alkyl, phenyl(lower)alkoxy(lower)alkyl, phenylthio(lower)alkyl, thienyl(lower)alkoxy, pyridyloxy(lower)alkyl, phenyl(lower)alkylthio, phenylurea, lower alkoxy(lower)alkoxy, phenyl(lower)quinil, dioxothiazolidine(lower)alkyl and thienyl, optionally substituted with halogen; naphthyl, optionally substituted with halogen; 4-phenylphenyl, substituted with halogen; thienyl, optionally substituted with halogen; benzothiazyl, optionally substituted with halogen; chenail, optionally substituted with halogen; or benzooxazol, optionally substituted with halogen, or its salt.

2. Sulfonamidnuyu connection on p. 1, where R1- alkyl, alkenyl, phenyl(lower)alkenyl, phenyl, optionally substituted by a Deputy selected from the group comprising alkyl and alkenyl or thienyl, optionally substituted with halogen;

Rather it represents a heterocyclic group selected from the group which consists of 3H-imidazo[4,5-b]pyridyl, pyrazolo[1,5-a]pyridyl, indolizinyl, 1H-indazole, benzo[b]furanyl and benzo[b]thiophenyl, the kilen and R2is phenyl, optionally substituted by a Deputy selected from the group comprising alkyl, alkenyl, quinil, lower alkoxy, phenyl, halogen, di(lower)alkylamino, lower alkylthio, lower alkoxycarbonyl, nitro, halogen(lower)alkyl, phenyl(lower)alkyl, phenyl(lower)alkenyl, phenyl(lower)alkoxy, cyclo(lower)alkyl(lower)alkoxy, phenoxy(lower)alkyl, phenyl(lower)alkoxy(lower)alkyl, phenyl(lower)quinil and thienyl, optionally substituted with halogen; naphthyl, optionally substituted with halogen; or 4-phenylphenyl, substituted with halogen, or its salt.

3. Sulfonamidnuyu connection on p. 2, where a IS 3H-imidazo[4,5-b]pyridyl, 1H-indazole, or benzo[b]furanyl, and these heterocyclic groups are optionally substituted by alkyl; and R2is phenyl, substituted with halogen, and named phenyl optionally substituted by a Deputy selected from the group comprising alkyl, alkenyl, quinil, lower alkoxy, phenyl, halogen, di(lower)alkylamino, lower alkylthio, lower alkoxycarbonyl, nitro, halogen(lower)alkyl, phenyl(lower)alkyl, phenyl(lower)alkenyl, phenyl(lower)alkoxy, cyclo(lower)alkyl(lower)alkoxy, phenoxy(lower)alkyl, phenyl(lower)alkoxy(lower)alkyl, phenyl(lower>

4. Sulfonamidnuyu connection on p. 3, where a IS 3H-imidazo[4,5-b]pyridyl, substituted by 1 or 2 groups lower alkyl, or its salt.

5. Sulfonamidnuyu connection on p. 3, where a - lH-indazole substituted by one group of lower alkyl, or its salt.

6. Sulfonamidnuyu connection on p. 3, where a is benzo[b]furanyl, substituted 1 group of lower alkyl, or its salt.

7. Sulfonamidnuyu connection on p. 1 or its pharmaceutically acceptable salt, designed to obtain a pharmaceutical preparation for diseases whose treatment is based on activity of the compounds to reduce blood sugar levels, or diseases whose treatment is based on cGMP-PDE inhibitory activity, relaxation activity of smooth muscles, bronchodilatation activity, vasodilatation activity, activity for suppression of smooth muscle cells or anti-allergic activity.

Priority points and features:

27.06.1997 on PP.1-3 and 7, when R1- alkyl, lower alkenyl, phenyl(lower) alkenyl, hinely, phenyl, optionally substituted by a Deputy selected from the group comprising nitro, lower alkyl and lower alkenyl or thienyl, not zameshannye [1,2-b] pyrazolyl, imidazo [1,2-a] pyridyl, 1H-imidazo [4,5-b] pyridyl, 3H-imidazo [4,5-b] pyridyl, pyrrolo [3,2-b] pyridyl, pyrazolo [1,2-a] pyridyl, benzothiazolyl, indolizinyl, 1H-indazole 2N-indazole, hinely, dihydroquinoxaline, tetrahydroquinoxaline, dihydroquinazolines, tetrahydroquinazoline, benzo [b] furanyl, benzo [b] thiophenyl and 1H-thieno [2,3-d] imidazolyl and named heterocyclic group optionally substituted by lower alkyl or oxo; X - low alkylene, oxa(lower)alkylene or oxa; R2is phenyl, optionally substituted Deputy, selected from the group which includes lower alkyl, lower alkenyl, lower quinil, lower alkanoyl, lower alkoxy, phenyl, imidazolyl(lower)alkyl, piperidinyl(lower)alkyl, halogen, amino, lower alkanolamine, mono(lower)alkylamino, di(lower)alkylamino, N-(lower)alkyl-N-acylamino, lower alkylsulfonyl, phenyl(lower)alkylamino, phenylcarbonylamino, benzoylamine, lower alkylsulfonyl, lower alkylsulfonyl, lower alkylthio, cyano, carboxy, lowest alkoxycarbonyl, cyclo(lower)alkylaminocarbonyl, mono(lower)allylcarbamate, nitro, halogen(lower)alkyl, phenyl(lower)alkyl, phenyl(lower)alkenyl, phenyl(lower)alkoxy; naphthyl, optionally substituted, halogen is substituted with halogen; chenail, optionally substituted with halogen; or benzooxazol, optionally substituted with halogen; PP.4-6;

24.04.1998 on PP.1-3 and 7, when R1alkenyl other than the lowest alkenyl, phenyl, optionally substituted by alkyl, other than lower alkyl; And - the specified heterocyclic group, optionally substituted by alkyl, other than lower alkyl; R2is phenyl, optionally substituted by a Deputy selected from the group comprising alkyl, other than lower alkyl; alkenyl other than the lowest alkenyl; quinil other than the lowest quinil; (N-pyridyl-N-(lower)alkylamino)(lower)alkoxy, cyclo(lower)alkyl(lower)alkoxy, cyclo(lower)alkyl(lower)alkyl, phenoxy(lower)alkyl, lower alkylsulfonate(lower)alkyl, hydroxy(lower)alkyl, di(lower)alkylamino(lower)alkyl, phenyl(lower)alkoxy(lower)alkyl, phenylthio(lower)alkyl, thienyl(lower)alkoxy, pyridyloxy(lower)alkyl, phenyl(lower)alkylthio, phenylurea, lower alkoxy(lower)alkoxy, phenyl(lower)quinil, dioxothiazolidine(lower)alkyl and thienyl, optionally substituted with halogen.

 

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