Antiarrhythmic Patents (Class 514/821)
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Patent number: 5198211Abstract: In accordance with the present invention, a method is provided for treating myocardial damage. More particularly, the present invention relates to a method for treating myocardial damage comprising injecting a non-emulsion, homogeneous solution of certain ethylene oxide-propylene oxide condensation surface-active copolymers.The surface-active copolymer can be an ethylene oxide-propylene oxide condensation product with the following general formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (C.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O) has a molecular weight of approximately 950 to 4000 daltons, preferably approximately 1200 to 3500 daltons, and b is an integer such that the hydrophile portion represented by (C.sub.2 H.sub.4 O) constitutes approximately 50% to 90% by weight of the compound.Type: GrantFiled: December 4, 1991Date of Patent: March 30, 1993Assignee: Emory UniversityInventors: Robert L. Hunter, Alexander Duncan
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Patent number: 5187162Abstract: Methods of preventing neural tissue damage caused by excitotoxicity due to increased release of excitatory amino acids by increasing extracellular concentrations of adenosine in and around the neural tissue are provided. These methods are especially useful in treating neurodegenerative diseases such as Parkinson's Disease, Alzheimer's Disease, Amyotrophic Lateral Sclerosis or Huntington's Disease.Type: GrantFiled: September 12, 1990Date of Patent: February 16, 1993Assignee: Gensia PharmaceuticalsInventors: Paul Marangos, Harry E. Gruber
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Patent number: 5158978Abstract: A method for the treatment of patients with acute cardiovascular compromise by administering a therapeutically effective amount of thyroid hormones. Methods of administration are included.Type: GrantFiled: June 18, 1991Date of Patent: October 27, 1992Assignee: British Technology Group (U.S.A.)Inventor: Leo Rubin
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Patent number: 5153178Abstract: Compositions and methods for increasing the contractility of the mammalian heart as shown by a positive inotropic effect are disclosed, employing protoberberine alkaloids such as berberine, discretine, xylopinine, berrberubine, tetrahydropalmatine, and stepharotine in combination with cardiac glycosides such as ouabain, digoxin, digitoxin, deslanoside and digitalis.Type: GrantFiled: August 1, 1988Date of Patent: October 6, 1992Inventor: Peter R. Maroko
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Patent number: 5112807Abstract: A new compound, which we have named "Leualacin" has the formula (I): ##STR1## and may be prepared by cultivation of a microorganism of the genus Hapsidospora, especially Hapsidospora irregularis. The compound may be used for the treatment and prophylaxis of cardiovascular diseases and disorders, especially hypertension.Type: GrantFiled: September 5, 1989Date of Patent: May 12, 1992Assignee: Sankyo Company, LimitedInventors: Kiyoshi Hamano, Kouhei Furuya, Kazuhiko Tanzawa, Takeshi Kagasaki, Masaaki Miyamoto, Takeshi Kinoshita
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Patent number: 5093131Abstract: Sleep apnea is treated by administering a therapeutically effective amount of 2-isopropyl-2,8-bis(3,4-dimethoxyphenyl)-6-methyl-6-azaoctane nitrile to a subject.Type: GrantFiled: March 14, 1990Date of Patent: March 3, 1992Assignee: Rohm Pharma GmbHInventors: Karl-Dieter Volger, Werner Mohrke
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Patent number: 5089526Abstract: A process is provided for preventing or ameliorating arrhythmia by administering to mammals, including man, an effective dose of d-sotalol to lengthen the action potential duration of cardiac cell without blockade of beta-adrenergic receptor sites.Type: GrantFiled: December 23, 1986Date of Patent: February 18, 1992Assignee: Bristol-Myers CompanyInventors: Arthur Simon, Jeff A. Thomis
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Patent number: 5032598Abstract: Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members and Q is a nitrogen containing heterocycle, are antiarrhythmic agents.Type: GrantFiled: December 8, 1989Date of Patent: July 16, 1991Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
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Patent number: 5032604Abstract: Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, and E is --S-- or --O--, are Class III antiarrhythmic agents.Type: GrantFiled: December 8, 1989Date of Patent: July 16, 1991Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
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Patent number: 5028599Abstract: In accordance with the present invention, a method is provided for treating myocardial damage. More particularly, the present invention relates to a method for treating myocardial damage comprising injecting certain ethylene oxide-propylene oxide condensation surface-active copolymers.The surface-active copolymer can be an ethylene oxide-propylene oxide condensation product with the following general formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (C.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O) has a molecular weight of approximately 950 to 4000, preferably approximately 1200 to 3500, and b is an integer such that the hydrophile portion represented by (C.sub.2 H.sub.4 O) constitutes approximately 50% to 90% by weight of the compound.Type: GrantFiled: May 11, 1990Date of Patent: July 2, 1991Assignee: Emory UniversityInventor: Robert L. Hunter
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Patent number: 5017609Abstract: A pharmaceutical composition is disclosed, which contains a short-acting .beta.-blocking compound of the formula ##STR1## wherein R.sub.1 may be an alkyl, cycloalkyl, alkenyl, alkynyl, alkyl carboxymethyl, aryl carboxymethyl, aryl or aralkyl, A may be an alkylene or alkenylene, X may be independently amino, hydrogen, halogen, hydroxy, alkoxy, aryloxy, aralkyl, cyano, amido or trifluoromethyl, n is an integer from 1 to about 4, R may be an alkyl, propargyl, dimethylpropargyl or hydroxyalkyl; or a pharmaceutically acceptable salt thereof in a hydroalcoholic solution further containing a physiologically acceptable buffering agent, ethanol and a physiologically acceptable liquid polyhydric compound. A method for treatment or prophylaxis of cardiac disorders using the composition of the present invention is also disclosed.Type: GrantFiled: November 16, 1989Date of Patent: May 21, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Agustin Escobar, Dietmar Wagenknecht, Ahmad W. Malick
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Patent number: 5008288Abstract: Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active compounds to desired sites in the body, e.g. skeletal muscle or the heart. The pharmaceutically active compound can be a protease inhibitor, a cardioactive drug for combating arrythmia, etc. The linkage is chemical through one or more alcohol, carboxyl or amine groups using reagents such as glutaraldehyde, dicarboxylic acid anhydrides and acid halides and carbodiimides. Carnitine derivatives are also incorporated into liposomes which are then used as carriers of active pharmaceutical agents.Type: GrantFiled: May 4, 1989Date of Patent: April 16, 1991Inventors: Alfred Stracher, Leo Kesner
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Pyrimidinedione compounds, method of producing the same and antiarrythmic agents containing the same
Patent number: 5008267Abstract: A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain containing at least two nitrogen atoms. The pyrimidinedione derivative is useful for a medical treatment of cardiac arrhythmias.Type: GrantFiled: October 24, 1989Date of Patent: April 16, 1991Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Tsutomu Katakami, Tatsuro Yokoyama, Michihiko Miyamoto, Haruki Mori, Nobuya Kawauchi, Tadahito Nobori, Kunio Sannohe, Joji Kamiya, Masaaki Ishii, Kanji Yoshihara -
Patent number: 4999363Abstract: Novel tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 6, 1989Date of Patent: March 12, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 4980379Abstract: A method to enhance the efficacy of cardioversion, defibrillation, cardiac pacing, and cardiopulmonary resuscitation and to treat post-resuscitation asystole, bradyarrhythmias, electromechanical dissociation, and hemodynamic collapse by administering to a human or animal an effective amount of an adenosine antagonist that competitively inhibits adenosine or that reduces the level of adenosine present in myocardial and vascular tissues and associated fluids.Type: GrantFiled: June 30, 1988Date of Patent: December 25, 1990Assignee: The University of VirginiaInventors: Luiz Belardinelli, Robert C. Wesley, Jr.
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Patent number: 4977165Abstract: A piperidine compound has the generic formula and is useful to treat arrhythmia. ##STR1## in which R.sup.1 is a lower alkyl and W is: ##STR2## X is --S--, --SO-- or --SO.sub.2 --, R.sup.2 is hydrogen or --(CH.sub.2).sub.n --Y, n is an integer of 1 to 5, Y is an aryl, pyridyl or a substituted pyridyl, X' is --CO-- or --CH(OH)--,p is an integer of 1 to 4, R.sup.12 is hydrogen or a lower alkyl, Y' is --(CH.sub.2).sub.m --A, m is 1 or 2, A is an aryl, a substituted aryl, pyridyl or a substituted pyridyl, R.sup.12 and Y may form a 5- or 6-membered ring or a 5- or 6-membered ring having one or more substituents andR.sup.22 is hydrogen, a halogen, a lower alkyl, a lower alkoxy or hydroxy.Type: GrantFiled: August 19, 1988Date of Patent: December 11, 1990Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji
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Patent number: 4963549Abstract: The present invention relates to the use of 6-[4-(N.sup.3 -methyl-N.sup.2 -cyanoguanidino)phenyl]-5-methyl-4,5-dihydro-3-(2H)-pyridazinone in a method of treating or preventing cardiac arrhythmias.Type: GrantFiled: September 27, 1988Date of Patent: October 16, 1990Inventors: Alan L. Rothaul, Lars M. Wood, Robert W. Gristwood
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Patent number: 4956389Abstract: Compound of general formula I ##STR1## and its addition salts with a pharmaceutically acceptable acid is described. The compound is prepared by reacting bis-(2-(3,4-dimethoxy-phenyl)ethyl)amine with formaldehyde in a reducing medium. The compound is effective in the treatment of cardiovascular diseases and disturbances in cerebral circulation.Type: GrantFiled: January 14, 1985Date of Patent: September 11, 1990Assignees: Yason S.R.L., SIR International S.A.Inventors: Giuseppe Quadro, Jean Cahn
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Patent number: 4952586Abstract: A composition is provided which includes a balanced combination of an edrophonium component and an atropine component. A preferred embodiment has 0.5 mg of edrophonium chloride and 8 micrograms of atropine sulfate, with respect to patient weight. The inventive composition is useful to antagonize nondepolarizing blockade during medical treatment when muscle relaxation is no longer necessary, provides extremely rapid onset of action and results in minimal heart rate changes.Type: GrantFiled: October 18, 1988Date of Patent: August 28, 1990Assignee: The Regents of the University of CaliforniaInventors: Robert B. Morris, Roy Cronnelly, Ronald Dean Miller
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Patent number: 4945114Abstract: Therapeutic agents containing enantiomers of propafenone, the preparation of the said agents and their use for certain groups of patients.Type: GrantFiled: July 29, 1988Date of Patent: July 31, 1990Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, deceased, Rainer Schlecker, Josef Gries, Gerda Von Philipsborn, Liliane Unger
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Patent number: 4922021Abstract: The invention is directed to 1-(2,6-Dimethyl-Phenyl-amino)-2-Dimethyl-amino-Propane and the pharmaceutical composition thereof useful for the treatment of cardiac rhythm disorders.Type: GrantFiled: September 14, 1988Date of Patent: May 1, 1990Assignee: BASF AktiensellschaftInventors: Zoltan Zubovics, Lajos Toldy, Gyorgy Rabloczky, Andras Varro, Ferene Andrasi, Sandor Elek, Istvan Elekes
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Patent number: 4912092Abstract: Methods for increasing extracellular concentrations of adenosine for the prophylactic or affirmative treatment of diseases of the immune, nervous, cardiac, and vascular systems involving admimistering to a patient purine nucleoside and purine nucleoside-related analogs which increase extracellular adenosine concentration, and methods for stabilizing mast cells by the suppression of mast cell activation using such compounds.Type: GrantFiled: July 29, 1987Date of Patent: March 27, 1990Assignee: The Regents of the University of CaliforniaInventor: Harry E. Gruber
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Patent number: 4885313Abstract: Novel 3,4-dihydroxyphenylethylamine derivatives possess dopaminergic activity in animals and are therefore useful in the treatment of iner alia congestive heart failure, renal failure and reversible obstructive airways disease.The compounds are generally administered in the form of a pharmaceutical composition comprising the active ingredient in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.Type: GrantFiled: December 2, 1987Date of Patent: December 5, 1989Assignee: Fisons plcInventors: John Dixon, Francis Ince
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Patent number: 4883804Abstract: There are described compounds of formula I, ##STR1## in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O).sub.n, wherein n is 0, 1 or 2;Y represents O or NH,l and m each independently represent 2, 3 or 4,R.sub.10 represents phenyl substituted by one or more substituents R.sub.23, which may be the same or different; or R.sub.10 represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,R.sub.15 represents hydrogen or together with R.sub.23 forms a (CH.sub.2).sub.p chain, wherein p represents 0, 1 or 2;R.sub.20, R.sub.21, R.sub.22 and R.sub.23, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR.sub.25, SH, NO.sub.2, halogen, CF.sub.3, SO.sub.2 R.sub.30, CH.sub.2 OH or OH, wherein R.sub.25 represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO.sub.2 alkyl C 1 to 6, and R.sub.30 represents alkyl C 1 to 6 or NH.sub.Type: GrantFiled: November 19, 1986Date of Patent: November 28, 1989Assignee: Fisons plcInventors: Francis Ince, Brian Springthorpe, John Dixon
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Patent number: 4866040Abstract: Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active compounds to desired sites in the body, e.g. skeletal muscle or the heart. The pharmaceutically active compound can be a protease inhibitor, a cardioactive drug for combating arrythmia, etc. The linkage is chemical through one or more alcohol, carboxyl or amine groups using reagents such as glutaraldehyde, dicarboxylic acid anhydrides and acid halides and carbodiimides. Carnitine derivatives are also incorporated into liposomes which are then used as carriers of active pharmaceutical agents.Type: GrantFiled: January 15, 1987Date of Patent: September 12, 1989Inventors: Alfred Stracher, Leo Kesner
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Patent number: 4859707Abstract: This invention relates to sulfur-substituted phenylacetamides of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are H or CH.sub.3 ; R.sub.4 is SR.sub.5, ##STR2## R.sub.5 and R.sub.6 may be the same or different and are lower alkyl containing 1-4 carbon atoms and R.sub.5 and R.sub.6 may be taken together with S to form a 5-7 member ring; and X.sup.- is a pharmaceutically acceptable anion, which exhibit arrhythmia activity.Type: GrantFiled: August 23, 1983Date of Patent: August 22, 1989Assignee: Key Pharmaceuticals, Inc.Inventors: Thorsteinn Loftsson, Nicholas Bodor
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Patent number: 4791137Abstract: Pharmaceutical and veterinary compositions having as essential active ingredient at least one benzofuran derivative of the general formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof in which R represents an amino, monoethylamino or diethylamino radical and X.sub.1 and X.sub.2 represent hydrogen or iodine with the proviso that when R represents diethylamino X.sub.1 and X.sub.2 are different.These compositions are useful for the treatment of ischemic cardiac disorders.Type: GrantFiled: December 2, 1986Date of Patent: December 13, 1988Assignee: SanofiInventors: Marcel Descamps, Yves Berger
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Patent number: 4780314Abstract: This invention relates to a novel recovery process for obtaining the small molecular weight, digitalis-like factor, and further relates to purification of the digitalis-like factor. This invention also relates to the identification and characterization of the factor and to therapeutic uses for the purified factor.Type: GrantFiled: October 30, 1985Date of Patent: October 25, 1988Assignee: Brigham and Women's HospitalInventor: Steven W. Graves
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Patent number: 4775743Abstract: New peptide derivatives represented by the following general formulaR.sub.1 -Pro-Hyp-R.sub.2wherein R.sub.1 is a hydrophobic radical, R.sub.2 is a hydrophilic radical, Pro is prolyl and Hyp is hydroxyprolyl show more powerful inhibitory action against platelet agglutination than conventional drugs and have potential use as anti-agglutination agent. The peptide derivative can be prepared by condensing a peptide containing a hydrophobic radical with a carboxylic acid containing a hydrophilic radical. The peptide derivative can be used in the form of parenteral injections, tablets, capsules or powder, the typical daily dose being in the range from 1 mg to 500 mg for adults.Type: GrantFiled: September 10, 1986Date of Patent: October 4, 1988Assignee: Green Cross CorporationInventors: Tsutomu Mimura, Yasuhiro Kohama, Chikara Fukaya, Masahiro Watanabe, Kazumasa Yokoyama
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Patent number: 4724235Abstract: N-(Arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue. The compounds are useful in the treatment of cardiac arrhythmia.Type: GrantFiled: March 31, 1986Date of Patent: February 9, 1988Assignee: A. H. Robins Company, IncorporatedInventors: James R. Shanklin, Jr., Christopher P. Johnson, III
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Patent number: 4720487Abstract: This invention relates to bornane derivatives of the formula: ##STR1## wherein Z stands for: ##STR2## and Y stands for an arabinose, xylose or ribose rest, the acetylated form of the same, with either a pyrane or furane configuration and bound to the R rest to lead either to the .alpha. or to the .beta. anomer, to a process for the preparation of these compounds and to therapeutic compositions comprising one of them as an essential ingredient.Type: GrantFiled: April 1, 1985Date of Patent: January 19, 1988Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventor: Andre Esanu
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Patent number: 4719237Abstract: A method useful for alleviating cardiac arrhythmias such as tachycardias in animals by administering to arrhythmic animals an antiarrhythmic amount of 4,4'-(isopropylidenedithio)bis (2,6-di-t-butylphenol), probucol.Type: GrantFiled: January 28, 1986Date of Patent: January 12, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Donald McCaughan
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Patent number: 4707499Abstract: This invention relates to 3-alkyl-5-[(substituted amino) methyl]dihydro-3-phenyl-2(3H)-furanones and imino analogs thereof, and to the pharmaceutical compositions containing such compounds, that are useful as inhibitors of cardiac arrhythmias and are therefore useful in the treatment of irregular heartbeat. This invention also relates to the use of such compounds and pharmaceutical compositions in the treatment of irregular heartbeat.Type: GrantFiled: December 1, 1986Date of Patent: November 17, 1987Assignee: G. D. Searle & Co.Inventors: John S. Baran, Harman S. Lowrie
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Patent number: 4678786Abstract: This invention relates to (isopropyl and tertiary butyl-amino-2-hydroxypropoxy)phenyl-3[2H]-pyridazinones which have .beta.-adrenoceptor antagonist activity.Type: GrantFiled: August 13, 1986Date of Patent: July 7, 1987Assignee: Smith Kline & French Laboratories LimitedInventors: Anthony M. Roe, William J. Coates, Robert A. Slater, Stephen P. Breukelman, George D. Meakins
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Patent number: 4661514Abstract: Pharmaceutical and veterinary compositions having as essential active ingredient at least one benzofuran derivative of the general formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof in which R represents an amino, monoethylamino or diethylamino radical and X.sub.1 and X.sub.2 represent hydrogen or iodine with the proviso that when R represents diethylamino X.sub.1 and X.sub.2 are different.These compositions are useful for the treatment of ischemic cardiac disorders.Type: GrantFiled: December 11, 1985Date of Patent: April 28, 1987Assignee: SanofiInventors: Marcel Descamps, Yves Berger
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Patent number: 4657929Abstract: There are provided pharmaceutical compounds useful in treating hypertension, heart diseases and renal failure. These compounds are 4-hydroxy phenethylamines wherein the 3 position on the phenyl nucleus is occupied by either an amino, amide, carbamyl, urea sulfonamide, substituted alkyl or fluorine atom, and the amine group is further linked to another phenyl radical through an alkylene radical which may contain nitrogen, oxygen, sulfur or cyclic hydrocarbon radicals as intervening groups.Type: GrantFiled: October 18, 1984Date of Patent: April 14, 1987Assignee: Fisons plcInventors: Francis Ince, Alan C. Tinker
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Patent number: 4656178Abstract: A novel pharmaceutical composition possessing an antiarrhythmic effect comprises an active principle - a hydrobromide salt of an alkaloid, viz. lappaconitine having the following formula ##STR1## The composition of the present invention is used in the treatment of various diseases accompanied by the heart rhythm disturbances such as is chemic heart disease, diverse kinds of cardiomyopathy and the like.Type: GrantFiled: April 24, 1985Date of Patent: April 7, 1987Inventors: Sabir J. Junusov, Marat S. Junusov, Vladimir A. Telnov, Farkhad N. Dzhagangirov, Fakhritdin Satritdinov, Karimzhan Taizhanov
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Patent number: 4638008Abstract: This invention provides a group of antiarrythmic agents of the formula: ##STR1## in which R.sub.1 is --CO.sub.2 H, --CO.sub.2 (CH.sub.2).sub.n --NR.sub.4 R.sub.5, --CONR.sub.6 R.sub.7, --NHCO.sub.2 R.sub.8 or --NHCO.sub.2 (CH.sub.2).sub.o --NR.sub.9 R.sub.10 where R.sub.4 and R.sub.5 are H or alkyl of 1 to 6 carbon atoms and n is 1 to 6; R.sub.6 and R.sub.7 are H or alkyl of 1 to 6 carbon atoms; R.sub.8 is alkyl of 1 to 6 carbon atoms; and R.sub.9 and R.sub.10 are alkyl of 2 to 6 carbon atoms and o is 1 to 6;R.sub.2 and R.sub.3 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; andm is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, and a method for their use.Type: GrantFiled: June 3, 1985Date of Patent: January 20, 1987Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Meier E. Freed, Thomas J. Colatsky
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Patent number: 4621085Abstract: The present invention relates to pharmaceutical preparations with cardiac, particularly anti-arrhythmic activity. These preparations comprise, as an active principle, at least one compound of formula I: ##STR1## where R represents a lipophilic radical. The pharmaceutical compositions may comprise this compound in the presence of other pharmaceutical excipients and adjuvants.Type: GrantFiled: April 3, 1985Date of Patent: November 4, 1986Assignee: Rohm GmbH Chemische FabrikInventors: Ulrich Borchard, Ernst Mutschler, Werner Moehrke, Karl-Dieter Voelger, Erwin Wolf
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Patent number: 4618680Abstract: 4-Hydroxy-3-methoxy-N-[2-[2-(1-methyl-2-piperidinyl)ethyl]-phenyl]benzamide is an antiarrhythmic agent having relatively low toxicity and increased duration of action.Type: GrantFiled: November 27, 1981Date of Patent: October 21, 1986Assignee: Mead Johnson & CompanyInventors: Robert F. Mayol, Richard E. Gammans
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Patent number: 4613619Abstract: The invention concerns novel anti-arrhythmic amino-alcohol derivatives, characterized by the general formula (1) ##STR1## or pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2 and R.sub.3 each independently represent hydrogen, alkyl having 1-6 carbon atoms, alkoxy having 1-6 carbon atoms, acyloxy having 1-6 carbon atoms, hydroxy, halogen or optionally alkyl-substituted amino;R.sub.4 represents hydrogen, hydroxy or alkyl having 1-6 carbon atoms,R.sub.5 represents hydrogen or alkyl having 1-6 carbon atoms,R.sub.6 represents hydrogen, acyl having 1-18 carbon atoms or alkyl having 1-6 carbon atoms,R.sub.7 and R.sub.8 each independently represent hydrogen or alkyl having 1-6 carbon atoms,X represents a direct bond or an oxygen atom, andn and m each independently are integers having a value of 1 or 2, whereby the sum of n and m is 2 or 3.Type: GrantFiled: February 22, 1985Date of Patent: September 23, 1986Assignee: AKZO N.V.Inventors: Thomas Sleigh, David S. Savage, John K. Clark
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Patent number: 4613607Abstract: Antiarhythmic medicaments containing, as active substance, a compound of the formula: ##STR1## in which n is 1 or 2, X and Y are fixed in positions 5, 6, 7 or 8 on the quinoline cycle and each represents a hydrogen atom or an alkoxy group having 1 to 3 carbons, R is a hydrogen atom or an alkyl group having 1 to 4 carbons, cycloalkyl having 3 to 8 carbons, phenyl or phenyl substituted by alkoxy having 1 to 4 carbons, R.sub.1 is a hydrogen atom or an alkyl group having 1 to 4 carbons or a phenylalkyl group of which the alkyl part has 1 to 3 carbons, R.sub.2 is a hydrogen atom, an alkyl group having 1 to 2 carbons or an alkenyl group having 2 to 4 carbons.Type: GrantFiled: September 30, 1983Date of Patent: September 23, 1986Assignee: Pharmuka LaboratoiresInventors: Claude G. A. Gueremy, Michel A. P. Mestre, Christian L. A. Renault
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Patent number: 4612320Abstract: Compounds of the general formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n have the meanings given in the description, are useful for treating cardiac disorders.Type: GrantFiled: March 12, 1984Date of Patent: September 16, 1986Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, Josef Gries, Claus D. Mueller, Dieter Lenke
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Patent number: 4604394Abstract: Pharmaceutical compositions and methods useful in the treatment of cardiac arrhythmias are described.Type: GrantFiled: October 1, 1984Date of Patent: August 5, 1986Assignee: Merck & Co., Inc.Inventors: Gregory J. Kaczorowski, Peter K. S. Siegl
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Patent number: 4603138Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein,Ar is optionally substituted phenyl or naphthyl, or pyridyl;E is O, S or a bond;R.sub.5 is hydrogen, andJ is C.sub.3-5 polymethylene, optionally substituted by one or two groups selected from methyl or optionally derivatized hydroxy; orAr and R.sub.5 together form a group ##STR2## where Ar.sup.1 is optionally substituted 1,2-phenylene;Z is O or CH.sub.2, andm is 0 or 1, when E is O or S, or 1 when E is bond;R.sub.1 is hydrogen, C.sub.1-4 alkyl optionally substituted phenyl; C.sub.3-8 alkanoyl, or phenyl C.sub.2-8 alkanoyl, any phenyl moiety being optionally substituted; a group COR.sub.2 where R.sub.2 is C.sub.2-3 alkoxy, phenyl C.sub.1-4 alkoxy, the phenyl moiety being optionally substituted, or C.sub.1-4 alkoxy C.sub.3-4 alkoxy; or a group CXNHR.sub.3 where X is O or S and R.sub.3 is C.sub.2-4 alkyl, C.sub.2-4 alkenyl, phenyl or phenyl C.sub.Type: GrantFiled: June 9, 1983Date of Patent: July 29, 1986Assignee: Beecham Wuelfing GmbH & Co. KGInventor: Harald Maschler
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Patent number: 4596827Abstract: The present invention relates to a new class of alkylsulfonamidophenylalkylamines which are potent antiarrhythmic agents having good oral bioavailability properties.Type: GrantFiled: November 7, 1985Date of Patent: June 24, 1986Assignee: Eli Lilly and CompanyInventors: Bryan B. Molloy, Mitchell I. Steinberg
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Patent number: 4594343Abstract: Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.Type: GrantFiled: October 19, 1984Date of Patent: June 10, 1986Inventors: James R. Shanklin, Jr., James M. Wilkinson, II
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Patent number: 4575513Abstract: Pharmaceutical and veterinary compositions having as essential active ingredient at least one benzofuran derivative of the general formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof in which R represents an amino, monoethylamino or diethylamino radical and X.sub.1 and X.sub.2 represent hydrogen or iodine with the proviso that when R represents diethylamino X.sub.1 and X.sub.2 are different.These compositions are useful for the treatment of ischemic cardiac disorders.Type: GrantFiled: July 5, 1984Date of Patent: March 11, 1986Assignee: SanofiInventors: Marcel Descamps, Yves Berger
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Patent number: 4558052Abstract: 10-bromosandwicine and 10-bromoisosandwicine and acid addition salts thereof are disclosed. There novel compounds possess valuable pharmacological properties e.g. heart rhythm regulatory properties. Furthermore they are valuable intermediates for the preparation of 10-brominated N.sub.b -quaternary sandwicine derivatives which exhibit heart rhythm regulatory and adrenolytic properties. 10-bromosandwicine is prepared by brominating sandwicine and can subsequently be isomerized into 10-bromoisosandwicine.Type: GrantFiled: June 8, 1984Date of Patent: December 10, 1985Assignee: Kali-Chemie Pharma GmbHInventors: Wolfgang Kehrbach, Joachim Wegener
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Patent number: 4556664Abstract: A method and pharmaceutical composition are disclosed for treating cardiac arrhythmias employing as an active ingredient at least one compound selected from piperidine-2-carboxylic acid-2,6-dimethyl anilide; piperidine-2-carboxylic acid-2,4-dimethyl anilide; piperidine-2-carboxylic acid-2,4,6-trimethyl anilide; and piperidine-2-carboxylic acid-2-methyl-5-chloro anilide.Type: GrantFiled: March 13, 1984Date of Patent: December 3, 1985Assignee: Gunnar A. K. AbergInventors: Gunnar A. K. Aberg, Peter R. Maroko, Bo T. af Ekenstam