Pfizer Corporation

Pfeizer Inc.

David A Cox

Ian T Barnish

Anthony G Evans

Braham Shroot

John C Danilewicz

Geoffrey E Gymer

John Edward Kemp

Allan L Ham

Michael Snarey

Novel substituted 1-phenyl-2-alkylamino-alkanols, 1-phenyl-2-alkylaminoalkanes and .alpha.-aminoalkyl phenyl ketones useful as heart stimulants are disclosed.

Phenyl-alkanolamine, alkylamine and .alpha.-aminoalkyl ketone

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

Antifungal thio-alkyl-imidazole derivatives

Novel substituted 1-phenyl-2-alkylamino-alkanols, 1-phenyl-2-alkylamino-alkanes and .alpha.-aminoalkyl phenyl ketones useful as heart stimulants are disclosed.

Phenyl-alkanolamine, alkylamine and alpha-aminoalkyl ketone derivatives

Novel antibacterial agents; namely, 7-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives having the formula: ##STR1## wherein R.sup.1 is thienyl, 2-furyl, phenyl, substituted thienyl or substituted phenyl; R is hydroxyl; R.sup.2 is hydrogen, hydroxy, acetoxy, carbamoyloxy, N-pyridyl, azido or heterocyclic thio group; R and R.sup.2 when taken together represent an oxygen atom; R.sup.3 is sulpho or COOR.sup.4' wherein R.sup.4' is hydrogen or R.sup.4 wherein R.sup.4 is lower alkyl, 5-indanyl, naphthyl, phenyl, or substituted phenyl, CONR.sup.5 R.sup.6, wherein each of R.sup.5 and R.sup.6 is hydrogen, lower alkyl or cycloalkyl; or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a saturated heterocyclic group; X is oxygen or sulphur, a direct link, carbonyl, methylene, hydroxymethylene, sulphinyl, sulphonyl or an imino group of the formula --NR.sup.7 --, wherein R.sup.7 is hydrogen, lower alkyl, lower alkenyl, or benzyl; and each of alk.sup.1 and alk.sup.2 is a divalent saturated aliphatic hydrocarbon group containing from 1 to 3 carbon atoms; the pharmaceutically acceptable salts thereof, and methods for their preparation.

7-D-(.alpha.-Acylamino-arylacetamido)-cephalosporanic acid derivatives

Novel antibacterial agents; namely, 7-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives having the formula: ##STR1## wherein R.sup.1 is thienyl, 2-furyl, phenyl, substituted thienyl or substituted phenyl; R is hydroxyl; R.sup.2 is hydrogen, hydroxy, acetoxy, carbamoyloxy, N-pyridyl, azido or heterocyclic thio group; R and R.sup.2 when taken together represent an oxygen atom; R.sup.3 is sulpho or COOR.sup.4.sup.' wherein R.sup.4.sup.' is hydrogen or R.sup.4 wherein R.sup.4 is lower alkyl, 5-indanyl, naphthyl, phenyl, or substituted phenyl, CONR.sup.5 R.sup.6, wherein each of R.sup.5 and R.sup.6 is hydrogen, lower alkyl or cycloalkyl; or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached form a saturated heterocyclic group; X is oxygen or sulphur, a direct link, carbonyl, methylene, hydroxymethylene, sulphinyl, sulphonyl or an imino group of the formula --NR.sup.7 --, wherein R.sup.7 is hydrogen, lower alkyl, lower alkenyl, or benzyl; and each of alk.sup.1 and alk.sup.2 is a divalent saturated aliphatic hydrocarbon group containing from 1 to 3 carbon atoms; the pharmaceutically acceptable salts thereof, and methods for their preparation.

7-D-(.alpha.-acylamino-arylacetamido)-cephalosporanic acid derivatives

Method of stimulating the heart employing substituted 1-phenyl-2-alkylamino-alkanols, 1-phenyl-2-alkylamino-alkanes and .alpha.-aminoalkyl phenyl ketones is disclosed.

Method of stimulating the heart employing ureido substituted

Certain novel 7-alkoxy-4-(N-[.omega.-(heteroaryl)alkyl]amino)quinazoline compounds, optionally bearing an alkyl or substituted alkyl group at the 2-position, an alkyl, benzyl, phenyl or alkoxyphenyl group on the 4-amino nitrogen atom, an alkyl or alkoxy group at the 5-position, and an alkyl alkoxy, hydroxy or amino group at the 6-position; and the acid-addition salts thereof. Compounds are cardiac stimulants.

4-Aminoquinazoline derivatives as cardiac stimulants

A series of novel substituted phenoxypropylamine derivatives have been prepared by reacting the appropriate 1-phenoxy-2,3-epoxypropane compound with a suitable organic amine reagent. The resulting 1-phenoxy-3-alkylaminopropan-2-ols are useful in the field of chemotherapy as anti-angina agents. Preferred members include compounds having an acetamido group substituted on the phenyl ring of the phenoxy moiety. Alternate methods of preparation are also provided.

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Canterbury, United Kingdom

David A Cox