Abstract: Oil and water emulsions containing alkylphosphoryl choline or alkylglycerophosphoryl choline surfactants are disclosed. The surfactants have the following general structures: ##STR1## In the above general structures, R.sub.1, R.sub.2 or R.sub.3 is alkyl, alkenyl, fluoroalkyl and alkenyl; and PC is the phosphoryl choline. The emulsions are useful as oxygen transport agents, artificial bloods or red blood cell substitutes.
Abstract: The present invention relates to a method of treating or preventing emesis in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives and related compounds.
Type:
Grant
Filed:
June 4, 1993
Date of Patent:
February 28, 1995
Assignee:
Pfizer Inc.
Inventors:
Manoj C. Desai, John A. Lowe, III, John W. Watson
Abstract: 1-Hetero substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
Type:
Grant
Filed:
September 14, 1993
Date of Patent:
January 10, 1995
Assignee:
Sterling Winthrop Inc.
Inventors:
Diane L. DeHaven-Hudkins, William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller
Abstract: A pharmaceutical dosage form comprising an HMG-CoA reductase inhibitor compound, e.g., fluvastatin sodium, is disclosed which is stabilized against pH-related degradation by an alkaline stabilizing medium capable of imparting a pH of at least 8 to an aqueous solution or dispersion of the composition.
Type:
Grant
Filed:
December 22, 1992
Date of Patent:
October 18, 1994
Assignee:
Sandoz Ltd.
Inventors:
Mohan B. Kabadi, Richard V. Vivilecchia
Abstract: The present invention is directed to the use of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines in the manufacture of a medicament for producing an orexigenic effect.
Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate, enantiomers, racemates, diastereomers or mixtures thereof or geometric isomer or mixtures thereof, and pharmaceutically acceptable salts thereof. The compounds of formula I inhibit enzyme carnitine acyltransferase 1 (CAT-1) and are therefore useful in the prevention of injury to ischemic tissue, and can limit infarct size, improve cardiac function and prevent arrhythmias during and following a myocardial infarction.
Type:
Grant
Filed:
March 13, 1992
Date of Patent:
September 6, 1994
Assignee:
Hoffman-La Roche Inc.
Inventors:
Robert W. Guthrie, John G. Mullin, Jr., David F. Kachensky, Richard W. Kierstead, Jefferson W. Tilley, Guy P. Heathers, Alan J. Higgins, Ronald A. LeMahieu
Abstract: A composition for treating a Sjoegren syndrome disease is disclosed. The composition comprising derivative of spirooxathiolane-quinuclidine of the following formula (I), ##STR1## wherein Z is .dbd.CR.sup.1 R.sup.2, wherein R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen, alkyl, cyclopentyl, cyclohexyl, aryl, diarylmethylol, or alkyl which may be substituted by one or more aryl groups, or an acid addition salt thereof, or an acid addition salt thereof, as an effective component. Especially effective is an administration of a hydrochloric acid addition salt of 2-methylspiro(1,3-oxathiolane-5,3')quinuclidine.
Abstract: The invention relates to the use of a compound which is an antagonist of 5-HT at 5-HT.sub.3 receptors and promotes gastric emptying in conjunction with an H.sup.+ K.sup.+ ATPase inhibitor in the treatment of gastrointestinal disorders.
Abstract: The invention provides compounds of formula I ##STR1## wherein W, D, R.sup.1, R.sup.2, R.sup.3, X, m, n and p are as defined in the description. The compound have valuable pesticidal activity especially against fungi, insects, nematodes, acarids and weeds.
Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
Type:
Grant
Filed:
February 6, 1992
Date of Patent:
March 22, 1994
Assignee:
The Du Pont Merck Pharmaceutical Company
Inventors:
Gary A. Cain, Paul J. Gilligan, Sang W. Tam
Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
Type:
Grant
Filed:
June 18, 1992
Date of Patent:
November 30, 1993
Assignee:
The Du Pont Merck Pharmaceutical Company
Inventors:
Gary A. Cain, Paul J. Gilligan, Sang W. Tam
Abstract: This invention relates to N-aryl-3-aryl-4-substituted-2,3,4,5-tetrahydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.
Abstract: Certain novel compounds having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.
Abstract: A quinazoline of the formula:- ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.
Abstract: The invention relates to a method of treating cocaine abuse or addiction in a mammal which comprises administering to the mammal an effective amount of a sigma receptor antagonist lacking or having relatively weak dopamine receptor-blocking activity, to reduce the pharmacological effects of the cocaine.
Abstract: The invention relates to a method of treating drug abuse or addiction involving amphetamine or amphetamine-related drugs with pharmacological effects similar to amphetamine in a mammal which comprises administering to the mammal an effective amount, to reduce the pharmacological effects of the amphetamine or amphetamine-related drug, of certain piperidine sigma receptor antagonists.
Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
Type:
Grant
Filed:
August 20, 1990
Date of Patent:
April 28, 1992
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Gary A. Cain, Paul J. Gilligan, Sang W. Tam
Abstract: The present invention describes a group of polyhydroxylated indolizidines and quinolizidines and their esters. These compounds are prepared starting from 2,6-dideoxy-2,6-dideoxy-2,6-imino-1,3,4,5-tetrakis-O- (phenylmethyl)-D-glycero-L-gulo-heptitol or a corresponding N-substituted compound. The compounds are useful in the treatment of diabetes and as .alpha.-glucosidase I inhibitors.
Type:
Grant
Filed:
March 30, 1990
Date of Patent:
July 2, 1991
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Paul S. Liu, Mohinder S. Kang, Roland S. Rogers, Barry L. Rhinehart
Abstract: Novel 1-alkyl substituted benzimidazole derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.
Type:
Grant
Filed:
February 6, 1989
Date of Patent:
July 24, 1990
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans E. Janssens, Gaston S. M. Diels, Joseph L. G. Torremans, Francois M. Sommen
Abstract: This invention provides novel 4H-quinolizin-4-one compounds which exhibit a selective inhibitory activity against IgE-antibody formation, and have utility for treatment of diseases associated with IgE formation in mammals, such as allergic bronchial asthma, allergic rhinitis, atopic dermatitis, hypersensitiveness, and the like.
Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and --B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.
Abstract: This invention provides novel 4H-quinolizin-4-one compounds which exhibit a selective inhibitory activity against IgE-antibody formation, and have utility for treatment of diseases associated with IgE formation in mammals, such as allergic bronchial asthma, allergic rhinitis, atopic dermatitis, hypersensitiveness, and the like.
Abstract: This invention provides novel 4H-quinolizin-4-one compounds which exhibit a selective inhibitory activity against IgE-antibody formation, and have utility for treatment of diseases associated with IgE formation in mammals, such as allergic bronchial asthma, allergic rhinitis, atopic dermatitis, hypersensitiveness, and the like.
Abstract: A formulation comprised of soft gelatin and glycine in a proportion of about 3:1 to 2:1 by weight, to which can be added mineral oligoelements and vitamins, which, when administered orally, exerts in a relatively short time a moisturizing activity on skin suffering from dryness.
Abstract: The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein A is an optionally substituted phenyl or heteroaromatic radical, R.sub.6 and R.sub.7 are hydrogen or lower alkyl, X is an alkylene chain containing up to 6 carbon atoms, Y is a valency bond or a >C.dbd.O group and B is an optionally substituted phenyl or heteroaromatic radical, as well as of their pharmacologically acceptable salts for the treatment of blood flow disturbances. The present invention also provides pharmaceutical compositions which contain these compounds.
Type:
Grant
Filed:
January 20, 1987
Date of Patent:
October 25, 1988
Assignee:
Boehringer Mannheim GmbH
Inventors:
Erwin Bohm, Jens-Peter Holck, Wolfgang Kampe, Herbert Leinert, Bernd Muller-Beckmann, Klaus Strein
Abstract: This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.
Abstract: Novel N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.
Abstract: Octahydroquinolizine and corresponding octahydroquinolizinium compounds of formulae (I) and (Va): ##STR1## where A is a 3 to 7 membered carbocyclic ring, R.sup.1 is a substituent, n is 0-2, x is 0-3, and Y is an anion. Also, pharmaceutical compositions for treating pain containing (I) and methods for synthesis and use as well as novel intermediates in the synthesis.
Abstract: The invention relates to novel quinolizinone compounds, of inhibitory activity on allergies and ulcers, of the formula: ##STR1## wherein R.sup.1 is carboxy, carbamoyl Y.sup.1, phenylcarbamoyl which may have hydroxy, cyano or thiocarbamoyl,R.sup.7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl;R.sup.2 is hydrogen, hydroxy, lower alkyl or lower alkoxy; andR.sup.
Abstract: The invention relates to novel quinolizinone compounds having inhibitory activity on allergies and ulcers, of the formula: ##STR1## wherein R.sup.1 is tetrazolylcarbamoyl;R.sup.7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl;R.sup.2 is hydrogen, hydroxy, lower alkyl or lower alkoxy;R.sup.
Abstract: A perfluorobicyclo compound of the general formula: ##STR1## wherein either or both of Ring A and Ring B may optionally be substituted with lower perfluoroalkyl group(s) and m and n each represent 3 or 4.
Abstract: 1,4-Dihydropyridines of the formula ##STR1## in which n is 0,1 or 2, andR.sup.1 to R.sup.7 can have a wide variety of meanings, which possess inotropic action, and many of which are new, are useful in increasing the influx of Ca.sup.++ into cells, particularly in combatting coronary and vascular diseases, hypertension swelling in the mucous membranes and diseases involving increased blood sugar or an incorrect salt and fluid balance.
Abstract: Oxazolidinone compounds useful as fungicides of Formula I ##STR1## wherein: W is O or S;Z is --(CH.sub.2).sub.n OR.sup.6 or --OCH(R.sup.11)(CH.sub.2).sub.m R.sup.6 ;n is 0-4;m is 0--3;R.sup.6 is phenyl substituted with C.sub.3 -C.sub.8 trialkylsilyl; or quinolinyl, isoquinolinyl, quinolinyl, quinolinyl, quinoxalinyl, benzo[b]thienyl, benzo[b]furanyl, indoly, N-methylindolyl, isoindolyl, indolizinyl, indazolyl, benzimidazolyl, benzthiazolyl, benzoxazolyl, benzisothiazolyl, or benzisooxazolyl each optionally substituted; andR.sup.1, R.sup.2, R.sup.3 , R.sub.4, R.sub.5, and R.sup.11 are defined in the disclosure, are disclosed.
Type:
Grant
Filed:
November 15, 1993
Date of Patent:
January 3, 1995
Assignee:
E. I. Du Pont de Nemours and Company, Inc.