Pfizer Corporation

Pfeizer Inc.

Geoffrey E Gymer

Kenneth Richardson

Alan Stobie

David Hepworth

Donald Stuart Middleton

Chikara Uchida

Mark David Andrews

Mavis Diane Adam

Harry Ralph Howard

Seiji Nukui

Kiyoshi Kawamura

Harry R Howard, Jr

Mikio Morita

Hirohide Noguchi

David A Cox

Sachiko Mihara

Braham Shroot

Mark Leonard Elliott

Subramaniyan Narayanaswami

David Fenwick

The invention relates to compounds of formula I 

Phenyl heterocyclyl ethers

This invention provides compounds of the formula (I) and (II):or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein Ris hydrogen or halo; Rand Rare independently hydrogen or Calkyl; Rand Rare independently hydrogen or Calkyl; Ris hydrogen, Calkyl, Calkoxy (C)alkyl or Calkyl substituted by up to 3 substituents selected from the groups consisting of Ccycloalkyl, aryl, heteroaryl and heterocyclic; Rand Rare hydrogen or taken together may form alkylene chain having one or two carbon atoms; Ris Calkyl or Ccycloalkyl; Ris Calkyl or NRR; L is (CRR)or NR; M is NRor (CRR); Rand Rare independently hydrogen or Calkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and Calkyl; with the proviso that when Ris Calkyl, L is not NR. These compounds have 5-HTreceptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators

Imidazopyridine compounds as 5-HT4 receptor modulators

A compound of general formula (I) wherein R and R are H, C -C alkyl or (CH ) (C -C cycloalkyl) wherein d&equals;0, 1, 2 or 3; or R and R together with the nitrogen to which they are attached form an azetidine ring; Z or Y is &mdash;SR and the other Z or Y is halogen or &mdash;R ; wherein R is C -C alkyl optionally substituted with fluorine; except that R is not CF ; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R and R , which may be the same or different, are: A&mdash;X, wherein A&equals;&mdash;CH&boxH;CH&mdash; or &mdash;(CH ) &mdash; where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR R , SO NR R , SO NHC(&boxH;O)R , OH, C alkoxy, NR SO R , NO , NR R , CN, CO R , CHO, SR , S(O)R or SO R ; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R ; wherein R is hydroxy, C -C alkoxy, F, C -C alkyl, haloalkyl, haloalkoxy, &mdash;NH , &mdash;NH(C -C alkyl) or &mdash;N(C -C alkyl) .

Phenoxybenzylamine derivatives as SSRIs

Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof, wherein R is 5-chloro-2-pyridyl, or phenyl optionally substituted by 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; R.sup.1 is CN, CSNH.sub.2 or CONR.sup.2 R.sup.3 where either

3-aryl-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butyramide and derivatives as

The invention provides triazole antifungal compounds of the formula: ##STR1## wherein R is either (a) a phenyl group optionally substituted with 1 to 3 substituents, each selected independently from halo and CF.sub.3 ; or

Triazole antifungal agents

Triazoles of the formula ##STR1## where R is phenyl 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, or R is 5-chloro-pyrid-2-yl; and R.sup.1 is H, CH.sub.3 or F; and their pharmaceutically and agriculturally acceptable salts. The compounds are useful as human and agricultural fungicides.

Compounds of the general formula: ##STR1## wherein R is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and R.sup.1 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkanoyl, or C.sub.1-2 alkyl substituted by C.sub.2-4 alkenyl with the provisos that when R.sup.1 is H or C.sub.2-4 alkanoyl, n is 0; and when n is 2, R.sup.1 is C.sub.1-3 alkyl; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.

Antifungal S-ethers of 2-aryl-3-mercapto-1-(1H-1,2,4-triazol-1-yl)

Triazole antifungal agents of the formula: ##STR1## and their O-esters and O-ethers, where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;

Triazole antifungal agents of the formula: ##STR1## and their O-esters and O-ethers, where R is a phenyl group optionally substituted by 1 to 3 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; R.sup.1 is selected from (a) ##STR2## (C.sub.1 -C.sub.4 alkyl), (b) --SO.sub.2 (C.sub.1 -C.sub.4 alkyl), (C) --SO.sub.2 NR.sup.2 R.sup.3 where either R.sup.2 and R.sup.3 are both C.sub.1 -C.sub.4 alkyl, or R.sup.2 and R.sup.3 together with the N atom to which they are attached represent piperidino, (d) --NHSO.sub.2 (C.sub.1 -C.sub.4 alkyl) and (e) --CONR.sup.4 R.sup.5 where either R.sup.4 is H or C.sub.1 -C.sub.4 alkyl and R.sup.5 is C.sub.1 -C.sub.4 alkyl, or R.sup.4 and R.sup.5 together with the N atom to which they are attached represent piperidino;

Compounds of the general formula: ##STR1## wherein Ar is dichlorophenyl and Het is 1-methyltetrazol-5-yl, 1,2,4-triazol-3-yl, 1-methyl-1,2,4-triazol-3-yl, 2-methyl-1,2,4-triazol-3-yl, 4-methyl-1,2,4-triazol-3-yl, imidazol-2-yl or 1-methylimidazol-2-yl and their pharmaceutically acceptable acid addition salts are antifungal agents in humans and other animals.

A series of novel 2-aryl-1-(imidazol-1-yl)-8-(4-piperazin-1-ylphenoxy)octan-2-ol derivatives has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as antifungal agents for the treatment of various topical, mucosal and systemic fungal infections in animals, including humans. Preferred member compounds include 2-(2,4-dichlorophenyl)-1-(imidazol-1-yl)-8-[4-ethylpiperazin-1-yl)phenoxy] octan-2-ol, 2-(2,4-dichlorophenyl)-1-(imidazol-1-yl)-8-[4-(4-n-propylpiperazin-1-yl)ph enoxy]octan-2-ol and 2-(2,4-dichlorophenyl)-1-(imidazol-1-yl)-8-[4-(4-isopropylpiperazin-1-yl)p henoxy]octan-2-ol, respectively. Methods for preparing these compounds from known starting materials are provided.

2-Aryl-1-(imidazol-1-yl)-8-(4-piperazin-1-ylphenoxy) octan-2-ol

Novel 1-aryl-2-(1-imidazolyl)-alkyl sulphides having anti-fungal properties are disclosed.

Antifungal thio-alkyl-imidazole derivatives

Novel 1-aryl-2-(1-imidazolyl)alkyl ethers and thioethers having anti-fungal properties are disclosed.

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Sandwich, United Kingdom

Geoffrey E Gymer