Abstract: An antiarrhythmic agent of the formula ##STR1## or a pharmaceutically acceptable salt thereof; wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;X is O, ##STR2## or a direct link; and R.sup.2 and R.sup.3, which are the same or different, are each C.sub.1 -C.sub.4 alkyl, with the proviso that when X is ##STR3## R.sup.2 and R.sup.3 are the same.
Abstract: Novel aminopropanol derivatives of 1,4:3,6-dianhydro-hexitol nitrates of the general formula I ##STR1## in which X has the meaning given in the specification, processes for their preparation and their use in preventing and treating angina pectoris, systemic hypertension and pulmonary hypertension in mammals.
Type:
Grant
Filed:
November 23, 1988
Date of Patent:
January 2, 1990
Assignee:
Pfizer Inc.
Inventors:
Peter Stoss, Matyas Leitold, Rodney Yeates
Abstract: A steerable catheter having a Doppler crystal at the tip to measure the velocity of blood in vivo--and inferentially the blood flow. The catheter includes two passageways, one passageway being exposed to the blood stream with the other passsageway containing the electrical leads to the Doppler crystal. The one passageway is dimensioned for receiving a wire guide for accurately manipulating the catheter. Preferably, the catheter incorporates an inflatable angio-balloon operable to distend the blood vessel in the region of a stenosis. Thus, blood flow can be determined in the region of the stenosis before and/or after the vessel is distended. The passageways are preferably defined by a pair of generally concentric tubes with the doppler crystal doughnut-shaped and sealingly disposed at the tip of the catheter.
Abstract: A pressure regulator including high and low pressure chambers separated by a divider having an opening, a closing member biassed to a closing position for closing the opening with a biassing force according to a desired pressure differential between the chambers, and a damping device for damping the resulting force on the closing member. There is also disclosed a fluid drainage system having a suction chamber with a suction regulator, and various arrangements of diaphragms for measuring pressure differentials. An anti-spill device for the draining system is disclosed as well.
Type:
Grant
Filed:
August 6, 1987
Date of Patent:
December 26, 1989
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
Nicholas F. D'Antonio, Nicholas J. D'Antonio
Abstract: A two-step process for the synthesis of certain indol-2(3H)-ones from indoles, and the 3,3-dibromoindol-2-(3H)-ones which are intermediates in that process.
Abstract: An antifungal agent of the formula: ##STR1## wherein R is phenyl group which may be substituted by 1 to 3 substituents each independently selected from halo and CF.sub.3 ; R.sup.1 is either (a) a phenyl group substituted by a group of the formula --N.dbd.CH--N(C.sub.1 -C.sub.4 alkyl).sub.2, ##STR2## or (b) a 5- or 6-membered aromatic heterocyclic group which may be benzo-fused and substituted by 1 or 2 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl and halo-(C.sub.1 or C.sub.2 alkyl), said heterocyclic group being attached to the nitrogen atom of the piperazine ring by a carbon atom;andR.sup.2 is H or CH.sub.3 ; or an O-ester or O-ether thereof which is a C.sub.2 -C.sub.4 alkanoyl or benzoyl ester, or a C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or phenyl ether, said phenyl and benzoyl groups of said O-esters and O-ethers may be substituted by one or two substituents each selected from C.sub.1 -C.sub.4 alkyl, halo and halo-(C.sub.1 or C.sub.
Abstract: Arylpiperazinyl-ethyl (or butyl)-heterocyclic compounds and their pharmaceutically acceptable acid addition salts are neuroleptic agents. They are useful in the treatment of psychotic disorders.
Abstract: Novel 4-amino-6,7-dimethoxy-2-(6,7-disubstituted-1,2,3,4-tetrahydroisoquinol-2-y l)quinoline compounds have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. These compounds are useful in therapy as anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Preferred compounds include 4-amino-6,7-dimethoxy-2-(6-hydroxy-7-methoxy-1,2,3,4-tetrahydroisoquinol-2 -yl)quinoline and 4-amino-6,7-dimethoxy-2-(7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinol-2 -yl)quinoline. Methods for preparing these compounds from known starting materials are provided.
Abstract: 1-Phenylquinazoline-1H,3H-2,4-diones and 1-phenylpyrido-[2,3d]-pyrimidine-1H,3H-2,4-diones, their esters and acid addition salts, and pharmaceutical compositions containing such compounds have antidepressant, anti-inflammatory and analgesic activity.
Abstract: Process for transformation of Yarrowia lipolytica, vectors useful therefor comprising DNA of a microbial vector and chromosomal DNA of Y. lipolytica and transformants comprising said vectors in E. coli and Y. lipolytica, and integrative shuttle vectors for Escherichia-Yarrowia transgeneric cloning. Said vectors or subclones thereof enable creation of Y. lipolytica cloning vectors into which specific or random segments of DNA can be inserted and the resulting vectors used to transform a suitable host microbe, especially Y. lipolytica, to improve the fermentation characteristics thereof and hence their industrial utilization.The methodology described permits the cloning of genes from a gene library of Y. lipolytica by complementation with an integrating vector.
Abstract: Improved pharmaceutical salts of amlodipine, particularly the besylate salt, and pharmaceutical compositions thereof. These salts find utility as anti-ischaemic and anti-hypertensive agents.
Abstract: Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidiene-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.
Abstract: Devices and methods for transmitting neural signals from a proximal stump of a transected nerve to a prosthetic apparatus are disclosed employing microelectrodes, preferably conductive fiber networks, capable of sensing electrical signals from a nerve and transmitting such signals to a prosthetic apparatus; and a semipermeable guidance channel disposed about the microelectrodes. The channels include an opening adapted to receive the proximal stump of a transected nerve, such that the channel promotes the growth of the stump and the formation of an electrical connection between the transected nerve and the microelectrode.
Type:
Grant
Filed:
September 4, 1987
Date of Patent:
November 7, 1989
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
Patrick Aebischer, Robert F. Valentini, Pierre M. Galletti
Abstract: A series of novel, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, containing six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity in vitro against certain gram-positive microorganisms.
Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesic acetaminophen, antidepressant doxepin, bronchodilator pirbuterol, minor tranquilizer diazepam, or antihypertensive trimazosin.
Type:
Grant
Filed:
November 4, 1988
Date of Patent:
October 17, 1989
Assignee:
Pfizer Inc.
Inventors:
Thomas C. Crawford, Stanley L. Keely, David L. Larson, Joseph G. Lombardino, James J. Maciejko
Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.
Abstract: Intermediates and a stepwise process for the conversion of D-methionine or certain of its derivatives to optically active compounds of the formula ##STR1## wherein R is (C.sub.1 -C.sub.3) alkyl, phenyl or tolyl. The latter compounds are in turn useful as an intermediate in the preparation of penem antibiotic 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid and corresponding pharmaceutically acceptable salts and esters.
Abstract: A femoral hip implant for use in patients requiring a long distal section of the femoral component is provided. For example, it can be used in patients undergoing revision surgery or requiring an implant with a long stem because of a fracture in the femur or a bone defect (for example as a result of a tumor removal). The implant is specially curved in its distal section so that the implant avoids impingement on the wall of the medullary canal even in the region of the isthumus of the bone.
Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.
Type:
Grant
Filed:
December 1, 1988
Date of Patent:
September 26, 1989
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Process and intermediates for the conversion of 3R,4R-4-acetoxy-3-[1R-1-(silyloxy)ethyl]-2-acetidinones to antibacterial 5R,6S-6-(1R-1-hydroxyethyl)-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids, and the pharmaceutically-acceptable salts and pivaloyloxymethyl esters thereof.