Patents Represented by Attorney Michael C. Sudol, Jr.
  • Patent number: 4968507
    Abstract: The instant invention is directed to an osmotic pump comprising:(A) at least one active agent surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 1, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
    Type: Grant
    Filed: July 15, 1987
    Date of Patent: November 6, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Gaylen M. Zentner, Gerald S. Rork, Kenneth J. Himmelstein
  • Patent number: 4946686
    Abstract: A drug delivery device for the controlled release of a therapeutically active ingredient into an environment of use is disclosed which comprises:(A) a core composition comprising(a) a plurality of controlled release solubility modulating units comprising solubility modulating agents each of which is a complexing agent or a surfactant and which is either (i) surround by a water insoluble cost containing at least one pore forming additive dispersed throughout said coat, or (ii) dispersed in an individual matrix substrate, and(b) A therapeutically active ingredient; and(B) a water insoluble microporous wall surrounding said core composition comprising:(i) a polymer material that is permeable to water but substantially impermeable to solute and(ii) 0.1 to 75% by weight, based on the total weight of (i) and (ii), of at least one water leachable pore forming additive dispersed throughout said wall.
    Type: Grant
    Filed: May 1, 1989
    Date of Patent: August 7, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Gregory A. McClelland, Gaylen M. Zentner
  • Patent number: 4946835
    Abstract: A novel dioxa-diazacyclohexadecenetetrone isolated from the fermentation of a cyanobacterium (Nostoc sp.) is described. The compound is a new antifungal agent with a specificity generally toward filamentous fungi but also effective against Cryptococcus sp.
    Type: Grant
    Filed: July 15, 1988
    Date of Patent: August 7, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Charles F. Hirsch, Jerrold M. Liesch, Michael J. Salvatore, Robert E. Schwartz, David F. Sesin
  • Patent number: 4886668
    Abstract: The instant invention is directed to a multiparticulate osmotic pump, for the controlled release of diltiazem L-malate to an environment of use, said pump comprising:(I) a carrier medium which does not maintain its integrity in the environment of use;(II) a multiple of tiny osmotic pump elements each comprising:(A) a core comprises diltiazem L-malate and an effective buffering amount of sodium bitartrate surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 0.5, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall,wherein the total amount of diltiazem L-malate in all of the osmotic pump elements is a therapeutically effective amount.
    Type: Grant
    Filed: September 24, 1987
    Date of Patent: December 12, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John L. Haslam, Gerald S. Rork
  • Patent number: 4880631
    Abstract: The instant invention is directed to an osmotic pump, for the controlled release of diltiazem L-malate to an environment of use, said pump comprising:(A) a core which comprises a therapeutically effective amount of diltiazem L-malate and an effective buffering amount of sodium bitartrate surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 0.5, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
    Type: Grant
    Filed: September 24, 1987
    Date of Patent: November 14, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John L. Haslam, Gerald S. Rork
  • Patent number: 4847289
    Abstract: 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.
    Type: Grant
    Filed: June 8, 1987
    Date of Patent: July 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Charles M. Habecker, Samuel L. Graham, Wasyl Halczenko, George D. Hartman, Harvey Schwam, Gerald S. Ponticello, Kenneth L. Shepard
  • Patent number: 4840963
    Abstract: 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.
    Type: Grant
    Filed: December 7, 1984
    Date of Patent: June 20, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Patent number: 4835276
    Abstract: 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 .alpha..sub.2 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,7,12-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl) -N-methyl-2-hydroxy-ethanesulfonamide hydrochloride.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: May 30, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ralph P. Volante, Richard Desmond, Ichiro Shinkai
  • Patent number: 4832957
    Abstract: 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. Treatment of parkinsonism with the controlled release formulation provides several advantages over treatment with the standard carbidopa/levodopa combinations presently employed.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: May 23, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Dempski, Edward C. Scholtz, Donald W. Nibbelink, Scott A. Reines
  • Patent number: 4824849
    Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: April 25, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
  • Patent number: 4820818
    Abstract: 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 temperatures.
    Type: Grant
    Filed: May 2, 1988
    Date of Patent: April 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ruth V. Wattley, Gerard R. Kieczykowski
  • Patent number: 4820848
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: April 4, 1988
    Date of Patent: April 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Ponticello, Charles N. Habecker
  • Patent number: 4816457
    Abstract: Heterocyclic aminoethanols of the formula:Het--CHOH--CH.sub.2 --NH-aralkylwhere Het is a 6-10 membered N-heterocycle are disclosed. The compounds are useful as pharmaceuticals.
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: March 28, 1989
    Inventors: John J. Baldwin, Joseph Atkinson, David E. McClure
  • Patent number: 4814452
    Abstract: 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 .alpha..sub.2 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,7,12-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl) -N-methyl-2-hydroxyethanesulfonamide hydrochloride, useful as an anti-depressant.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: March 21, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ralph P. Volante, Edward Corley, Ichiro Shinkai
  • Patent number: 4812463
    Abstract: Alkane sulfonamides with an electron withdrawing function .beta. to the sulfonamide group are topically effective carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: March 14, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Thomas H. Scholz
  • Patent number: 4808595
    Abstract: Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.
    Type: Grant
    Filed: May 5, 1988
    Date of Patent: February 28, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Jacob M. Hoffman, Jr.
  • Patent number: 4806562
    Abstract: Thieno[2,3-b]thiophene-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: February 21, 1989
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Patent number: 4803286
    Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.
    Type: Grant
    Filed: August 19, 1987
    Date of Patent: February 7, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, David C. Remy, David A. Claremon, Stella W. King
  • Patent number: 4798831
    Abstract: Thieno[2,3-b]furan-2-sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: January 17, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John D. Prugh, George D. Hartman, Wasyl Halczenko
  • Patent number: 4797413
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: January 10, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy