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Attorney: Sudol, Jr.; Michael C.


Number of patents: 141
Last date: July 11, 1989

1        
NumberTitleIssue Date
4847289Thiophene sulfonamide antiglaucoma agents
Aryl (or aralkyl)-sulfonylthiophene-2-sulfonamides containing a basic functional group as a substituent are efficacious in the treatment of elevated intraocular pressure and glaucoma following topical ocular administration....
07/11/1989
48409632-Sulfamoyl-1H-indole derivatives for the treatment of elevated intraocular pressure
Novel 2-sulfamoyl-1H-indoles and derivatives thereof are shown to be useful for the treatment of elevated intraocular pressure in pharmaceutical compositions designed for systemic or topical ophthalmic administration....
06/20/1989
4835276Preparation of n-formamidoyl[(s)-1-t-butoxy-3-methyl-2-amino)]1,2,3,4 tetrahydrobenzo [b]furo [2,3-c]pyridine and derivatives
The present invention is directed to an enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one which is an intermediate in the production of the 댒 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,...
05/30/1989
4832957Controlled release combination of carbidopa/levodopa
A matrix or monolithic drug delivery system for the controlled release of carbidopa and levodopa consists of the two drugs uniformly dispersed in a polymer vehicle at a concentration that is greater than the solubility of either drug in the polymer. Treat...
05/23/1989
48248492 -adrenoceptor antagonistic arylquinolizines
Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective 댒 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, plat...
04/25/1989
4820818Process for the geometric stereoselective dehydration of 3-(9-chloro-5,6-dihydro-11H-11-hydroxy-pyrrolo-(2,1-B)(3)-benzazepin-11- yl)-N,N-dimethyl-1-propanamine
The muscle relaxant (E)-3-(9-chloro-5,6-dihydro-11H-pyrrolo[2,1-b][3]benzazepin-11-ylidene-N,N -dimethyl-1-propanamine is prepared by the geometric stereoselective dehydration of the intermediate carbinol with acidic agents and organic bases and low t...
04/11/1989
4820848Substituted aromatic sulfonamides as antiglaucoma agents
Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure....
04/11/1989
4816457Aralkylaminoethanol heterocyclic compounds
Heterocyclic aminoethanols of the formula: where Het is a 6-10 membered N-heterocycle are disclosed. The compounds are useful as pharmaceuticals....
03/28/1989
4814452Enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one
An enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one provides a key intermediate for the preparation of the 댒 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,7,12-hexahydro-2H-benzo[b]furo[2...
03/21/1989
4812463Alkanesulfonamides as antiglaucoma agents
Alkane sulfonamides with an electron withdrawing function ଲ to the sulfonamide group are topically effective carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma....
03/14/1989
4808595Furopyridine sulfonamides and their opthalmological compositions
Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma....
02/28/1989
4806562Substituted thieno[2,3-b]thiophene-2-sulfonamides as antiglaucoma agents
Thieno[2,3-b]thiophene-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma....
02/21/1989
4803286Amino-2-hydroxypropyloximinoheterocycle ଱-blockers
Certain amino-2-hydroxypropyloximinoheterocycles are ଲ-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia....
02/07/1989
4798831Substituted thieno[2,3-B]furan-2-sulfonamides as antiglaucoma agents
Thieno[2,3-b]furan-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma....
01/17/1989
4797413Thieno thiopyran sulfonamide derivatives, pharmaceutical compositions and use
Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure....
01/10/1989
4788203Cyclized N-substituted-tetrahydropyridine compounds, useful in the treatment of cardiovascular disorders
Novel cyclized N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular...
11/29/1988
4774243Dopamine agonists for treating elevated intraocular pressure
Topical ocular administration of a dopamine agonist is effective in lowering abnormally elevated intraocular pressure and is useful in the prevention and treatment of glaucoma and related ocular diseases....
09/27/1988
4738982HMG-CoA reductase inhibitors
Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## and pharmaceutically acceptable salt...
04/19/1988
4733787Tamper evident overcap
There is disclosed an overcap for a container with a primary cap for the removal of the contents thereof, whereby the overcap is easily assembled onto the container and completely surrounds the primary cap. When assembled, the overcap prevents access to t...
03/29/1988
4731360Acylcarnitines as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal compartments
Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs....
03/15/1988
4729989Enhancement of absorption of drugs from gastrointestinal tract using choline ester salts
Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs....
03/08/1988
4728664Uniquely non-mutagenic substituted nitroimidazole
There is disclosed a substituted nitroimidazole compound, 1-methyl-2-methylsulfonyl-4-nitroimidazole which is an antiprotozoal and bactericidal compound with the unique and surprising property of being totally non-mutagenic and thus of a much higher degre...
03/01/1988
4727151Labile quaternary ammonium salts as prodrugs
Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein N represents a tertiary aliphatic amine; wherein N represents an unsaturated amine; wherein R represents a member selected from the group con...
02/23/1988
4723958Pulsatile drug delivery system
There is provided a novel drug delivery system which provides for intermittent drug delivery with readily adjustable intervals between drug delivery pulses. This is accomplished by providing a multilayer device in which layers of active drug are readily e...
02/09/1988
47217915-amino or substituted amino 1,2,3-triazoles
Novel 5-amino or substituted amino 1,2,3-triazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with a...
01/26/1988
4719229Antihypercholesterolemic agents
Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents are represented by the following structural formulae (I) and (II): ##STR1## are disclosed....
01/12/1988
4710469Novel phosphotyrosyl protein phosphatase
A glycoprotein phosphotyrosyl protein phosphatase is isolated from human tissues, such as human placental membrane. Upon membrane solubilization and extraction of the enzyme it was subjected to chromatographic purification and isolation. The analytical an...
12/01/1987
4703034Novel cyclic tetrapeptide
There is disclosed a series of novel cyclic tetrapeptides related to somatostatin. The compounds have surprisingly been found to have the activity of increasing blood glucose when administered. The compounds are prepared using the solid phase or mixed anh...
10/27/1987
4692441Chorine esters as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal cavities
Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities....
09/08/1987
4686222Aralkylaminoethanol heterocyclic compounds
Heterocyclic aminoethanols of the formula where het is a 6-10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals....
08/11/1987
4678806Prodrugs of antihypercholesterolemic compounds
Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in th...
07/07/1987
46787991,2(1,4)-dimethyl-4(2)-(2-hydroxyethyl)-5-nitro-imidazole antiprotozoal agents with reduced mutagenicity
A group of 4-substituted-5-nitroimidazoles is described, having effective antiprotozoal activity with much less mutagenicity than is shown by known 5-nitroimidazoles....
07/07/1987
4678774Novel synergistic compositions
There are disclosed novel formulations of avermectin compounds and a substrate which demonstrate markedly enhanced insecticidal activity over that which would be observed with other formulations. Avermectin natural product compounds and certain semisynthe...
07/07/1987
4677131Cyclic ureas as dermal penetration enhancers
Certain novel cyclic ureas are disclosed herein as dermal penetration enhancers of drug absorption. Also disclosed herein are compositions, methods of treatment and processes for preparing said cyclic urea compounds....
06/30/1987
4675337Non-mutagenic 1,2-disubstituted 4-nitro-imidazoles useful as antiprotozoal agents
The invention relates to novel 1,2-disubstituted-4-nitroimidazole compounds that are useful as potent antiprotozoal agents and simultaneously possess non-mutagenicity as compared to known 4- or 5-nitroimidazole compounds. Also, compositions and methods fo...
06/23/1987
4670443Benzo(f)isoquinoline compounds useful as calcium entry blockers
Benzo(f)isoquinoline compounds, particularly, penta- and tetrahydrobenzo(f)isoquinoline dicarboxylic acid compounds, their preparation and their use as calcium entry blockers are disclosed....
06/02/1987
4668696Novel averonectin fermentation product of a microorganism with anthelmintic activity
There is disclosed a macrolide isolated from the fermentation broth, with 22,23-dihydro avermectin Bla aglycone as a substrate, of a known microorganism identified as MA-5853. The structure of the novel compound isolated from the microorganism is presente...
05/26/1987
4666937Avermectin bioconversion products
There are disclosed novel compounds which are derived from 22,23-dihydro avermectin Bla aglycone, 13-deoxy-22,23 dihydro overmectin Bla aglycone and 13-deoxy-22,23-dihydro overmectin Blb aglycone. The six compounds are hydroxy adducts of the substrate ave...
05/19/1987
4666901Substituted lactams useful as angiotensin converting enzyme inhibitors
Substituted lactams and related compounds and methods for their preparation are disclosed. These compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives....
05/19/1987
4663349Rectally absorbable form of L-dopa
The invention relates to compositions and methods of enhancing rectal absorption of L-dopa via the formation of an ester prodrug and optionally with a decarboxylase inhibitor....
05/05/1987
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