Abstract: A series of novel 6-substituted-5-oxo-6H-pyrido[2,3-d]pyridazine-8-ylacetic acid and 7-substituted-8-oxo-7H-pyrido[2,3-d]pyridazine-5-ylacetic acid compounds have been prepared, including their C.sub.1 -C.sub.6 alkyl ester derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. Typical member compounds include those acids wherein the ring substitutent is always attached to the available ring-nitrogen atom and is either a lower aralkyl group or a lower heteroaralkyl group. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Methods for preparing these compounds from known starting materials are provided.
Type:
Grant
Filed:
May 11, 1989
Date of Patent:
February 26, 1991
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski
Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of a non-steroidal antiinflammatory agent such as piroxicam, or a pharmaceutically acceptable salt thereof, with 5'-guanylic acid or N-acetyl-L-methionine, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 19, 1987
Date of Patent:
February 19, 1991
Assignee:
Pfizer Inc.
Inventors:
Thomas C. Crawford, David L. Larson, Joseph G. Lombardino
Abstract: Device for oral administration of a medicament to a ruminant animal comprises a rilaminate sheet (1) containing the medicament rolled into a tube retained in the rolled configuration by a film (3) of material which disintegrates in the rumen to allow unrolling of the sheet. The tube ends are closed by plugs (2) which keep the tube closed during passage of the device through the oesophagus.
Type:
Grant
Filed:
June 26, 1989
Date of Patent:
February 19, 1991
Assignee:
Pfizer Inc.
Inventors:
William T. R. Grimshaw, Andrew J. Weatherley
Abstract: Novel, semi-crystalline depsipeptide polymers and copolymers particularly suitable for use in fabricating bioabsorbable medical implant devices such as sutures or clips and obtained through ring-opening polymerization of certain 3-substituted-2,5-morpholinediones prepared by reacting a naturally occurring alpha-amino acid with an alpha-halo acid chloride in inert solvent in the presence of an acid acceptor.
Abstract: A method for preventing adhesion utilizes a viscoelastic gel formed from xanthan gum. The gel is more viscous than blood and is soluble in aqueous solutions. The gel is placed between the tissues by a syringe. The method includes mixing the xanthan gum with either a saline solution or Tyrode's solution to form the gel.
Abstract: Anti-anxiety agents; namely, 1-(heterocyclylcarbonyl)-3-[4-(2-pyrimidinyl)-1-piperazinyl]propanes and 1-(heterocyclylsulfonyl)-3-[4-(2-pyrimidinyl)-1-(piperazinyl)]propanes; and methods for their preparation and use.
Abstract: A reservoir outlet control device for controlling fluid flow from a reservoir. The device is particularly suitable for controlling fluid outflow from a blood collecting and blood delivery reservoir.
Type:
Grant
Filed:
March 29, 1989
Date of Patent:
February 19, 1991
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
Douglas M. Spranger, Karl D. Kirk, III, Robert Cohen, Preston J. Keeler, III, Jeffrey A. Stein
Abstract: A new acidic polycyclic antibiotic UK-61,689 has the formula: ##STR1## or a pharmaceutically acceptable cationic salt thereof. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis and swine dysentery as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants.
Type:
Grant
Filed:
February 20, 1990
Date of Patent:
February 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Alexander C. Goudie, Nigel D. A. Walshe
Abstract: A series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these compounds are certain other 5-amino-2,5-disubstituted-4-hydroxypentanoic acid derivatives.
Type:
Grant
Filed:
March 22, 1990
Date of Patent:
February 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Edward F. Kleinman, Robert L. Rosati, Jasjit S. Bindra
Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.
Type:
Grant
Filed:
May 8, 1989
Date of Patent:
February 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
Abstract: Broad spectrum antiparasitic agents of formula (I) having utility as anthelmintics, ectoparasiticides, insecticides, acaricides and animal growth promotants ##STR1## wherein Y is a single bond or a double bond; R.sup.1 is OH; provided that when Y is a single bond R.sup.1 is present and when Y is a double bond R.sup.1 is absent; R.sup.2 is .dbd.CH.sub.2 or a group of the formula --(X)--C(R.sup.5).dbd.CHR.sup.6 ; R.sup.3 is H or CH.sub.3 ; R.sup.5 and R.sup.6 are both H; R.sup.5 is H and R.sup.6 is C.sub.1 -C.sub.3 alkyl; or one of R.sup.5 and R.sup.6 is H and the other is C.sub.2 -C.sub.6 alkoxycarbonyl, phenyl, substituted phenyl, heteroaryl or substituted heteroaryl; and X is a direct bond or an alkylene group having from 2 to 6 carbon atoms which may be straight or branched-chain; with the proviso that R.sup.5 and R.sup.6 are not both hydrogen when X is --CH(CH.sub.3)CH.sub.2 --; processes and intermediates therefor, and compositions thereof.
Abstract: A new glycopeptide antibiotic UK-68,597 can be prepared by submerged aerobic propagation in aqueous nutrient media of Actinoplanes sp. ATCC 53533. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis, swine dysentery and theileriosis as well as being effective in promotion of growth and/or improving efficiency of feed utilization in poultry, swine and ruminants.
Type:
Grant
Filed:
June 15, 1989
Date of Patent:
February 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Hiroshi Maeda, Junsuke Tone, John C. Ruddock, Kelvin S. Holdom
Abstract: A guide wire for an intravascular catheter is disclosed. In one embodiment, the guide wire has Doppler means positioned on the distal end, with preferred Doppler means being piezoelectric ceramics or piezoelectric polymeric materials, both having electrical leads connected thereto. In another embodiment, the guide wire has a Laser Doppler means.
Type:
Grant
Filed:
November 13, 1989
Date of Patent:
February 12, 1991
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
D. Russell Pflueger, Cliff N. Cottonaro, Scott M. Evans
Abstract: An efficient, multistep process for the synthesis of certain 6-(1-hydroxyethyl) 2-substituted penem antibiotics from 2-[4R-(triphenylmethylthio)-3S-(1R-(dimethyl-t-butylsilyloxy)ethyl)-2-azet idon-1 yl]acetic acid ester.
Abstract: Triazole antifungal agents of the formula ##STR1## where R is 5-chloropyrid-2-yl or 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; and R.sup.1 is H or CH.sub.3 ; and their O-esters, O-ethers and pharmaceutically and agriculturally acceptable salts. The compounds are useful as human and agricultural antifungal agents.
Abstract: A new acidic polycyclic ether antibiotic UK-58,852 has the formula: ##STR1## wherein R and R.sup.1 are both hydrogen, and can be prepared by the submerged aerobic propagation in aqueous nutrient media of Actinomadura sp. ATCC 39697. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis, swine dysentery and theileriosis as well as being effective in promotion of growth and/or improving efficiency of feed utilization is swine and ruminants. Two minor components, where R is H and R.sup.1 is CH.sub.3 and wherein R and R.sup.1 are both CH.sub.3, have also been isolated from the fermentation.
Type:
Grant
Filed:
February 8, 1988
Date of Patent:
February 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, Hiroshi Maeda, John C. Ruddock, Junsuke Tone
Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl) alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrythmias. Said sulfonamide base compounds are of the formula: ##STR1## wherein R and R.sup.1 are each C.sub.1 -C.sub.4 alkyl; X is --CH.sub.2 --, --CO--or --CO(OH)--; n is two, three or four; and "Het--" is a nitrogen-containing heterocyclic group wherein said heterocyclic group is phenyl or benzyl-substituted 2H-pyridazin-3-on-2-yl, or it is 2H-phthalazin-1-on-2-yl, 4-halo-2H-phthalizin-1-on-2-yl or 4-(C.sub.1 -C.sub.4 alkyl)-2H-phthalazin-1-on-2-yl, 2H-isoindolin-1-on-2-yl, 3H-quinazolin-4-on-3-yl, 2H-3,4-dihydroisoquinol-1-on-2-yl, 2H-isoquinol-on-2-yl, 1H-3,4-dihydroquinol-2-on-1-yl, benzoxazol-2-on-3-yl, quinol-2-on-1-yl, quinol-2-yl or indol-2-yl, each optionally mono substituted with halogen or C.sub.1 -C.sub.
Type:
Grant
Filed:
June 2, 1989
Date of Patent:
February 5, 1991
Assignee:
Pfizer Inc.
Inventors:
John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
Abstract: 4-Phenyl-1,2,3,4-tetrahydro-1-naphthalenamine derivatives have been found useful for the treatment of psychosis, inflammation and as immunosuppressants.