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| Number | Title | Issue Date |
| 4847289 | Thiophene 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 |
| 4840963 | 2-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 |
| 4835276 | Preparation 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 |
| 4832957 | Controlled 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 |
| 4824849 | 2 -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 |
| 4820818 | Process 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 |
| 4820848 | Substituted 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 |
| 4816457 | Aralkylaminoethanol 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 |
| 4814452 | Enantioselective 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 |
| 4812463 | Alkanesulfonamides 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 |
| 4808595 | Furopyridine 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 |
| 4806562 | Substituted 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 |
| 4803286 | Amino-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 |
| 4798831 | Substituted 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 |
| 4797413 | Thieno 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 |
| 4788203 | Cyclized 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 |
| 4774243 | Dopamine 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 |
| 4738982 | HMG-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 |
| 4733787 | Tamper 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 |
| 4731360 | Acylcarnitines 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 |
| 4729989 | Enhancement 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 |
| 4728664 | Uniquely 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 |
| 4727151 | Labile 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 |
| 4723958 | Pulsatile 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 |
| 4721791 | 5-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 |
| 4719229 | Antihypercholesterolemic 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 |
| 4710469 | Novel 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 |
| 4703034 | Novel 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 |
| 4692441 | Chorine 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 |
| 4686222 | Aralkylaminoethanol 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 |
| 4678806 | Prodrugs 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 |
| 4678799 | 1,2(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 |
| 4678774 | Novel 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 |
| 4677131 | Cyclic 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 |
| 4675337 | Non-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 |
| 4670443 | Benzo(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 |
| 4668696 | Novel 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 |
| 4666937 | Avermectin 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 |
| 4666901 | Substituted 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 |
| 4663349 | Rectally 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 |