E.r. Squibb & Sons, Inc.

Hans Hoehn

Theodor Denzel

Jack Bernstein

Berthold Richard Vogt

B Richard Vogt

Ernst Schulze

Theodore Denzel

Hans Joachim Schneider

Compounds are provided having the structure ##STR1## wherein R.sup.1 is lower alkyl; phenyl-lower alkyl; phenyl; substituted phenyl wherein the phenyl group bears one or two halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, cyano or nitro groups; 5- or 6-membered monocyclic aromatic heterocyclics containing one hetero atom, namely, O, S or N, such as furanyl, pyridinyl or thiophenyl; and substituted heterocyclics wherein any of the above heterocyclics bears one halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, cyano or nitro group;

Antimicrobial derivatives of 3-(1H-imidazol-1-yl)-2-propen-1-ones

New imidazolylethoxymethyl derivatives of thiazole are provided having the general formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenoxy-lower alkyl, phenyl-lower alkyl or substituted or unsubstituted phenyl;

Imidazolylethoxymethyl derivatives of thiazole

Imidazolylethoxy derivatives of quinoline-2- or 4-methanols having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.

Imidazolylethoxy derivatives of quinoline-2- or 4-methanols,

Compounds are provided having the structure ##STR1## wherein R.sup.1 is lower alkyl; phenyl-lower alkyl; phenyl; substituted phenyl wherein the phenyl group bears one or two halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylothio, cyano or nitro groups; 5- or 6-membered monocyclic aromatic heterocyclics containing one hetero atom, namely, O, S or N, such as furanyl, pyridinyl or thiophenyl; and substituted heterocyclics wherein any of the above heterocyclics bears one halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, cyano or nitro group;

Antibacterial and antifungal derivatives of

New 4H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidin-5(8H)on e and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.

4H-Pyrazolo[4',3':5,6]pyri

Compounds are provided having the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl; substituted or unsubstituted phenyl-lower alkyl; substituted or unsubstituted phenyl; substituted or unsubstituted 5- or 6-membered monocyclic aromatic heterocyclic containing one O, S or N atom; in the above substituted groups, the phenyl groups bear one or two substituents and the heterocyclic bears one substituent which may be a halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, cyano or nitro group;

4-(2-(1H-Imidazol-1-ylmethyl)-1,3-dioxol

Imidazolylethoxymethyl derivatives of dioxoloquinolines having the general formula ##STR1## and their acid addition salts are useful as antifungal and antibacterial agents.

Antimicrobial imidazolylethoxymethyl derivatives of 1,3-dioxolo

New imidazole derivatives of 1,5,6,11-tetrahydrobenzo[5,6]cyclohepta[1,2-b]pyrazolo[4,3-e]-pyridines have the general formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each may be hydrogen, lower alkyl, phenyl-lower alkyl, phenyl or substituted phenyl, and R.sup.3 and R.sup.4 may be the same or different and each may be hydrogen, halogen, lower alkyl, or lower alkoxy. They and the salts thereof are useful as antimicrobial agents, and in particular as antifungal agents.

Imidazole derivatives of

Compounds are provided having the structure ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each may be hydrogen, lower alkyl, phenyl-lower alkyl, phenyl, substituted phenyl wherein the phenyl group bears one halogen, hydroxy, lower alkyl, lower alkylthio, cyano or nitro group; R.sup.3 is halogen; and R.sup.4 and R.sup.5 may be the same or different and each may be hydrogen, hydroxy, lower alkoxy, lower alkylthio or halogen. These compounds as well as acid addition salts thereof are useful as antimicrobial agents.

Imidazolylethoxymethyl derivatives of pyrazole

Imidazolylethoxymethyl derivatives of 1,3-dioxolo quinolines

New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.

8H-Pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine

New 2,3-dihydro-3-(1H-imidazol-1-ylmethylene)-4H-1-benzothiopyran-4-ones are provided having the general formula ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, lower alkyl, halogen, lower alkoxy, lower alkylthio, phenyl-lower alkyl, phenyl or substituted phenyl;

2,3-Dihydro-3-(1H-imidazol-1-ylmethylene)-4H-1-benzothiopyran-4-ones

The new amino derivatives of pyrido[2,3-d]pyridazine carboxylic esters and acids have the general formula ##STR1## They are useful as analgesic, anti-inflammatory agents and central nervous system depressants. In addition, this type of compound increases the intracellular concentration of adenosine-3',5'-cyclic monophosphate.

Amino derivatives of pyrido(2,3-d)pyridazine carboxylic acids and esters

New 2,3-dihydro-2-[(1H-imidazol-1-yl)-methylene]-1H-inden-1-ones are provided having the general formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each is hydrogen, lower alkyl, halogen, lower alkoxy, lower alkylthio, phenyl-lower alkyl, phenyl or substituted phenyl. The above compounds and their salts are useful as antifungal and antibacterial agents.

2,3-Dihydro-2-[(1H-imidazol-1-yl)-methylene]-1H-inden-1-ones

New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]-pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.

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Hans Hoehn