Patents by Inventor Waclaw J. Rzeszotarski
Waclaw J. Rzeszotarski has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5395827Abstract: The present invention pertains to antagonists of excitatory amino acid neurotransmitter receptor antagonists, their method of preparation as well as compositions containing them which have the general formula: ##STR1## wherein n and m independently are 0, 1, 2, or 3; R.sub.1 is selected from the group consisting of hydrogen and R.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl, C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl, wherein if R.sub.2 is hydrogen, R.sub.1 is not hydrogen; R.sub.3 is selected from the group consisting of hydrogen and C.sub.1 to C.sub.6 lower alkyl; the stereoisomers thereof in their resolved or racemic form, and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 22, 1993Date of Patent: March 7, 1995Assignee: Guilford Pharmaceuticals Inc.Inventors: Waclaw J. Rzeszotarski, Suzanne R. Ellenberger, Maria E. Guzewska, John W. Ferkany, Gregory S. Hamilton, Raymond J. Patch, Edward W. Karbon, Jr
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Patent number: 5359098Abstract: Sigma binding site agents having the formula ##STR1## wherein A.sup.1, A.sup.2, A.sup.3, B, y and 2 are defined in the specification, W is halogen, which are novel intermediates useful in preparing the presently binding site agents.Type: GrantFiled: November 15, 1993Date of Patent: October 25, 1994Assignee: Guilford Pharmaceuticals Inc.Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
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Patent number: 5278174Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.Type: GrantFiled: May 17, 1991Date of Patent: January 11, 1994Assignee: Scios Nova, Inc.Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
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Patent number: 5175290Abstract: 1,3-Substituted-8-(oxo-substituted cycloalkyl)xanthines and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds include the cis and trans isomers of 1,3-dipropyl-8-(3-hydroxycyclopentyl)xanthine and the cis and trans isomers of 1,3-dipropyl-8-(4-hydroxycyclohexyl)xanthine. The compounds are potent and selective bronchodilators and/or cardiotonic agents.Type: GrantFiled: September 16, 1988Date of Patent: December 29, 1992Assignee: Marion Merrell Dow Inc.Inventors: Waclaw J. Rzeszotarski, Roger N. Hiner, Scott W. Feeney
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Patent number: 5135936Abstract: A group of four stereoisomers and their pharmaceutically acceptable salts are disclosed. The stereoisomers have formula I. ##STR1## In Formula I the asymmetric centers a and b may be the same or different and have either the absolute R or S configuration. Also disclosed are pharmaceutical compositions containing the stereoisomers and use of the stereoisomers as antihypertensive agents, as peripheral and cerebral vasodilators and as coronary therapeutic agents.The preferred compound is (R,R)-1-azabicyclo[2.2.2]oct-3-yl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.Type: GrantFiled: March 5, 1991Date of Patent: August 4, 1992Assignee: Marion Merrell Dow Inc.Inventors: Theodore C. Adams, Waclaw J. Rzeszotarski
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Patent number: 5049555Abstract: The invention pertains to a method and pharmaceutical compositions for treating, preventing or reducing neurodegeneration associated with chronic central nervous system or hypoxic, ischemic and hypoglycemic injury to the central nervous system and for the treatment of anxiety through the use of 2-amino-.omega.-phosphonoalkanoic acids having a cycloalkyl group bridging adjacent carbons on the alkyl chain, their pharmaceutically acceptable salts and derivatives as neuroprotectants and anxiolytics.Type: GrantFiled: December 19, 1988Date of Patent: September 17, 1991Assignee: Nova Pharmaceutical CorporationInventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, Suzanne R. Ellenberger, Lisa H. Conti, John W. Ferkany, Donald J. Kyle
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Patent number: 5036107Abstract: 1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one.The compounds are highly specific M.sub.1 -AChR antagonists with relatively prolonged duration of activity.Type: GrantFiled: November 16, 1989Date of Patent: July 30, 1991Assignee: Marion Merrell Dow Inc.Inventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, Daniel W. McPherson, Ciro J. Spagnuolo, Kenneth J. Natalie, Jr.
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Patent number: 5032593Abstract: 1,3-Alkyl substituted-8-phenylxanthines in which the straight chain alkyl substituents are different and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds have 1-n-propyl-3-methyl and 1-methyl-3-n-propyl substituents. The compounds are potent bronchodilators.Type: GrantFiled: July 1, 1988Date of Patent: July 16, 1991Assignee: Marion Merrell Dow Inc.Inventors: Waclaw J. Rzeszotarski, Ronald H. Erickson
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Patent number: 4975437Abstract: The four stereoisomers are disclosed having the formula: ##STR1## in which the asymmetric centers a and b are the same or different. The compounds are derived from the (+) and (-) alcohols and the (+) and (-) dihydropyridines and have either the absolute R or S configuration. Also disclosed are pharmaceutical compositions comprising an effective amount of the compounds in a pharmaceutically acceptable carrier and methods for producing cardiotonic activity using the compositions.Type: GrantFiled: December 14, 1989Date of Patent: December 4, 1990Assignee: Marion Laboratories, Inc.Inventors: John P. Carter, Waclaw J. Rzeszotarski
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Patent number: 4889860Abstract: A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a longacting analgesic or opiate abuse treatment agent or appetite suppressant having the general formula: ##STR1## wherein R is methyl, cyclopropylmethyl or allyl, and R.sub.1 is an unsubstituted or substituted aryl, aralkyl, heteroaryl, heteroaralkyl or a cycloalkyl group with or without a heteroatom like S,O,N; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: April 6, 1987Date of Patent: December 26, 1989Assignee: Nova Pharmaceutical CorporationInventors: Waclaw J. Rzeszotarski, Babu J. Mavunkel
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Patent number: 4877779Abstract: Novel compounds and their salts are disclosed having the Formulas: ##STR1## wherein: R.sub.1 is hydrogen, phenyl, 9H-fluoren-9-yl, 10,11-dihydro-5H-dibenzo [a,d]cyclohepten-5-yl, 5H-dibenzo[a,d]cyclohepten-5-yl, 1,2,3,4-tetrahydro-1-naphthyl, 9H-xanthen-9-yl, 9H-thioxanthen-9-yl, 2-chloro-9H-thioxanthen-9-yl, 4H-chromanyl, diphenylmethyl, phenylcycloalkylmethyl wherein the bridgehead methylene may optionally be substituted with a hydroxy group and any of the phenyl or benzo-fused rings may be substituted with one or more R.sub.5 groups wherein R.sub.5 is selected from halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy groups; andR.sub.2 and R.sub.3, which may be the same or different, are hydrogen, lower alkyl, phenylalkyl (C.sub.1 -C.sub.5), wherein the phenyl ring may be substituted with one or more R.sub.5 groups or NR.sub.2 R.sub.Type: GrantFiled: May 17, 1988Date of Patent: October 31, 1989Assignee: Marion Laboratories, Inc.Inventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, John P. Carter, Theodore C. Adams, Andrea C. Dupont, Carl Kaiser
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Patent number: 4843074Abstract: Novel 1-azabicyclo[2.2.2]octan-3-yl 2-aryl-3-azacyclo-2-hydroxypropionates and their quaternary salts and their use as antimuscarinic agents having antisecretory activity selective for the gastrointestinal tract are disclosed. The compounds have the formula: ##STR1## wherein: X=H, halogen, lower alkyl, lower alkoxy, hydroxy, andR=morpholinyl, thiomorpholinyl, piperidinyl, 1,4-dioxa-8-azaspiro[4.5]decanyl, 4-(2,6-dimethylmorpholinyl), 4-ketopiperidinyl, 4-hydroxypiperidinyl, 4-substituted piperazinyl (wherein the substituent is lower alkyl, hydroxyalkyl, acetoxyalkyl, or acyl).Also disclosed are pharmaceutical compositions for treatment of irritable bowel syndrome and methods for using such compounds.Type: GrantFiled: May 17, 1988Date of Patent: June 27, 1989Assignee: Marion Laboratories, Inc.Inventors: Waclaw J. Rzeszotarski, Vicki H. Audia, Moshe Weitzberg
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Patent number: 4783530Abstract: 1,3-alkylsubstituted-8-(3,4-,3- or 4-substituted phenyl)xanthines and pharmaceutically acceptable salts of such compounds are disclosed. The 3-substituents are hydrogen, dimethylaminomethyl, or 2,3-dihydroxypropyloxy. The 4-substituents are selected from hydroxy, cyano, --NHCON(R.sub.5).sub.2, --C(.dbd.NH)N(R.sub.5).sub.2, --NH--C(.dbd.NH)N(R.sub.5).sub.2, with each R.sub.5 independently being hydrogen or an alkyl group of one to three carbons and provided that when the 3-substituent is hydrogen the 4-substituent is not hydroxy or hydrogen.The compounds are potent adenosine receptor antagonists having relatively low lipophilicity. The compounds are intended for use as bronchodilators and cardiotonics.Type: GrantFiled: October 1, 1987Date of Patent: November 8, 1988Assignee: Marion Laboratories, Inc.Inventors: Waclaw J. Rzeszotarski, Rickey P. Hicks, Ronald H. Erickson
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Patent number: 4761405Abstract: The invention pertains to novel, potent anticonvulsants, analgesics, cognition enhancers and neuroprotectants achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-[2-(phosphonoalkylenyl)-cycloalkyl]-2-aminoalkanoic acids having general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C.sub.1 to C.sub.6), alkyl (C.sub.7 to C.sub.12), fatty acid chain (C.sub.13 to C.sub.24), aryl, aralkyl, hydroxyl; the stereoisomers being in their resolved or racemic form; n and m=0,1,2 or 3; z=0,1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts and derivatives thereof.Type: GrantFiled: March 4, 1987Date of Patent: August 2, 1988Assignee: Nova Pharmaceutical CorporationInventors: Waclaw J. Rzeszotarski, Donald J. Kyle
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Patent number: 4760069Abstract: A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a long-acting analgesic or opiate abuse treatment agent or appetite suppressant having the general formula: ##STR1## wherein R is methyl, cyclopropylmethyl or allyl, and R.sub.1 is an unsubstituted or substituted aryl, aralkyl, heteroaryl, heteroaralkyl or a cycloalkyl group with or without a heteroatom like S,O,N; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: September 23, 1985Date of Patent: July 26, 1988Assignee: Nova Pharmaceutical CorporationInventors: Waclaw J. Rzeszotarski, Babu J. Mavunkel
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Patent number: 4657899Abstract: The invention pertains to novel, potent anticonvulsants, analgesics and cognition enhancers achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-[2-phosphonoalkyleneyl)phenyl]-2-aminoalkanoic acids having general formula: ##STR1## Wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, --CH.dbd.CH--CH.dbd.CH.dbd., amino, nitro, trifluoromethyl or cyano; n and m=0, 1, 2, or 3; and the pharmaceutically acceptable salts and derivatives thereof.Type: GrantFiled: April 9, 1986Date of Patent: April 14, 1987Assignee: Nova Pharmaceutical CorporationInventors: Waclaw J. Rzeszotarski, Robert L. Hudkins, Maria E. Guzewska
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Patent number: 4644003Abstract: The present invention relates to antagonists of muscarinic acetylcholine receptors. More specifically, this invention contemplates highly selective antimuscarinic agents which are characterized as esters of 3-quinuclidinol and unsymmetrical alpha-disubstituted glycolic acids.These highly selective antimuscarinic agents permit efficacy at particular sites designated m.sub.1 -AChR without affecting the muscarinic acetylcholine receptors of other tissues characterized by sites designated m.sub.2 -AChR. Such efficacy requires lower quantities of the antagonist thereby lowering toxicity and other undesirable side effects.Type: GrantFiled: April 3, 1985Date of Patent: February 17, 1987Assignee: Research CorporationInventors: Waclaw J. Rzeszotarski, Raymond E. Gibson, William C. Eckelman, Richard C. Reba
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Patent number: 4541957Abstract: 17.alpha.-[(E)-2-Iodovinyl]-estra-1,3,5(10)-triene-3,17.beta.-diol wherein the iodine atom is radioactive can be produced from (E)-[3-acyloxy-17.beta.-hydroxyestra-1,3,5(10)-triene-17.alpha.-yl]vinyl dihydroxyborane in an excellent yield by iodinating the same and hydrolyzing the resulting 3-acyloxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol.Type: GrantFiled: September 7, 1983Date of Patent: September 17, 1985Assignee: The George Washington UniversityInventors: Iwao Nakatsuka, William Eckelman, Waclaw J. Rzeszotarski
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Patent number: 4431627Abstract: Compounds of the formula: ##STR1## wherein R is aryl, alkyl, cycloalkyl, phenyl, cyclopentyl, cyclohexyl, a ligand containing Tc-99m in chelated form or a ligand capable of chelating Tc-99m;R.sub.1 is H or lower alkyl;X is in the ortho-, meta or para- position, and is selected from the group consisting of .sup.125 I, .sup.123 I, .sup.127 I, I, .sup.18 F, .sup.75 Br, .sup.77 Br, NH.sub.2, and ##STR2## wherein R.sub.2 is in the 2,3, or 4 position and is selected from the group consisting of H and lower alkyl, provided that when R is a ligand capable of chelating Tc-99m or containing Tc-99m in chelated form, X is not a radioisotope and may also be H or lower alkyl;Z.sup..crclbar. is an anion; or the free amine thereof; anddenotes an asymmetric carbon atom.Type: GrantFiled: December 31, 1981Date of Patent: February 14, 1984Assignee: Research CorporationInventors: William C. Eckelman, Richard C. Reba, Waclaw J. Rzeszotarski, Raymond E. Gibson