Pfizer Corporation

Peter J Whittle

Kenneth Richardson

John Adams Lowe, Iii

Andrew Simon Bell

Michael J Fray

Peter Thomas Stephenson

Alan Patrick Marchington

Kevin Cooper

The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.

6-phenylpyridyl-2-amine derivatives

6-phenyl-pyridin-2-ylamine derivatives

Triazole antifungal agents

Antifungal 1-[3-(substituted)-2-hydroxy-2-(perfluoroalkyl)-propyl]triazole derivatives wherein the 3-propyl substituent represents optionally substituted phenoxy, heteroaryloxy, alkylthio, alkylsulfinyl, alkylsulfonyl or optionally substituted carbamoyl.

Triazoles

Compounds of the general formula: ##STR1## wherein Ar is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and Het is a heterocyclic group which may optionally be substituted or fused to a phenyl, substituted phenyl or further heterocyclic ring; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.

Compounds of the general formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is 5-chloro-2-pyridyl, phenyl or phenyl substituted by from one to three substituents, each independently selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy; and n is zero or an integer from 1 to 5; method for their use in combatting fungal infections in plants, seeds and animals, including humans; and pharmaceutical and agricultural compositions containing them.

Antifungal 1-aryl-1-fluoroalkyl-2-(1H-1,2,4-triazol-1-yl)ethanols

Compounds of the formula ##STR1## a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is 5-chloro-2-pyridyl, phenyl or phenyl substituted by from 1 to 3 substituents, each independently selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy; and R.sup.1 is H, Cl, phenyl, phenyl substituted by from 1 to 3 substituents each independently selected from F, Cl, Br, I and CF.sub.3 or a heterocyclic group linked to the adjacent CF.sub.2 group by a ring carbon atom; method for their use in combatting fungal infections in plants, seeds and animals, including humans, and pharmaceutical and agricultural compositions containing them.

Antifungal 2-aryl-1,1-difluoro-3-(1H-1,2,4-triazol-1-yl)2-propanols

A fungicidal agent of the formula: ##STR1## or a pharmaceutically or agriculturally acceptable salt thereof, wherein R is 5-chloropyrid-2-yl or a phenyl group optionally substituted by 1 to 3 substituents each independently selected from F, Cl, Br, I, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; and ##STR2## where n is 0, 1, 2 or 3 and R.sup.2 is H or C.sub.1 -C.sub.4 alkyl.

Antifungal 2-aryl-2-hydroxy perfluoro-1-(1H-1,2,4-triazol-1-yl)

Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is (C.sub.1 -C.sub.5) perfluoroalkyl and R.sup.1 is H or CH.sub.3, method for their use in combatting fungal infections in plants, seeds and animals, including humans; and as antileishmanial agents, and pharmaceutical and agricultural compositions containing them.

1,3-Bis-(1H-1,2,4-triazol-1-yl)-2-perfluoro-alkylpropan-2-ol antifungal

1-Triazolyl-2-aryl-3-(5-trifluoromethylimidazol-1-yl)propan-2-ol derivatives useful in the treatment of fungal infections in humans, animals and plants, and their preparation.

Antifungal

Compounds of the formula ##STR1## wherein X is halo and R is an aryl group and their pharmaceutically acceptable salts are useful antifungal agents in animals, including man.

Bis-pyridyl containing triazoles

Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is 5-chloro-2-pyridyl, phenyl or phenyl substituted by from 1 to 3 substituents selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)-alkyl and (C.sub.1 -C.sub.4)alkoxy; X is a halogen atom, and n is zero or an integer from 1 to 5, method for their use in combatting fungal infections in plants, seeds and animals, including humans, and pharmaceutical and agricultural compositions containing them.

Antifungal 1-aryl-2-(1H-1,2,4-triazol-1yl)-1-perfluoroalkylethyl halides

Compounds of the formula: ##STR1## wherein Ar is phenyl substituted by from 1 to 3 substituents, each substituent being independently halo or CF.sub.3 ;

Antifungal S-arylmethyl- and S-heterocyclylmethyl ethers of

Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein m and n are independently 0, 1, 2, 3 or 4; method for their use in combatting fungal infections in plants, seeds and animals, including humans; and pharmaceutical and agricultural compositions containing said compounds or salts.

Growing community of inventors

Canterbury, United Kingdom

Peter J Whittle