Patents Represented by Attorney Michael C. Sudol

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  • Compounds useful in treating sickle cell anemia
    Patent number: 4699926
    Abstract: The present invention is directed to compounds of the general formula I and pharmaceutically acceptable salts thereof: ##STR1## wherein R=H or lower alkyl;R'=H, lower alkyl, benzyl, CH.sub.2 OH;A=(CH.sub.2).sub.1 to 5, >C(CH.sub.3).sub.2, >C (CH.sub.2).sub.3 ; andX=0 or 1.The present invention is also directed to a method of treating a person for sickle cell anemia comprising administering to the person a therapeutically effective dosage of the above compounds.In addition the invention includes the novel compound: ##STR2## which is inaccessible by synthetic procedures previously described for this general class of compounds.
    Type: Grant
    Filed: April 4, 1986
    Date of Patent: October 13, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Donald J. Abraham, Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr.
  • Morpholino pyridyl thiazole compound
    Patent number: 4697012
    Abstract: 2-Benzyl-4-(4-pyridyl)thiazoles and derivatives thereof have been made from converting a benzyl cyanide to the corresponding thioamide followed by condensation with a 4-bromoacetylpyridine. The thiazole derivatives are found to be effective immunoregulants.
    Type: Grant
    Filed: July 25, 1984
    Date of Patent: September 29, 1987
    Assignee: Merck & Co., Inc.
    Inventors: David A. Boulton, Ihor E. Kopka, Vernon L. Moore, Arsenio A. Pessolano
  • Chorine esters as absorption-enhancing agents for drug delivery through mucous membranes of the nasal, buccal, sublingual and vaginal cavities
    Patent number: 4692441
    Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: September 8, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Substituted hexahydro arylquinolizines as .alpha..sub.2 blockers
    Patent number: 4690928
    Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.6 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, antidiabetics, antiobesity and platelet aggregation inhibitors.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: September 1, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Joel R. Huff, Joseph P. Vacca, John J. Baldwin
  • Aralkylaminoethanol heterocyclic compounds
    Patent number: 4686222
    Abstract: Heterocyclic aminoethanols of the formulaHet--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: October 3, 1985
    Date of Patent: August 11, 1987
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Joseph G. Atkinson, John J. Baldwin, David E. McClure
  • Substituted benzo[b]furo- and benzo[b]thieno quinolizines
    Patent number: 4686226
    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, antiobesity and platelet aggregation inhibitors and modifiers of gastrointestinal motility.
    Type: Grant
    Filed: September 3, 1985
    Date of Patent: August 11, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Joel R. Huff, John J. Baldwin, Yojiro Sakurai, Joseph P. Vacca, James P. Guare, Jr.
  • Substituted cinnamyl-2,3-dihydrobenzofuran and analogs useful as anti-inflammatory agents
    Patent number: 4686235
    Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: August 11, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Norman P. Jensen, Milton L. Hammond, Robert A. Zambias, John McDonald, Kathleen M. Rupprecht
  • Substituted caprolactam derivatives as antihypertensives
    Patent number: 4680392
    Abstract: The invention in its broad aspects relates to caprolactam derivatives which are useful as angiotensin converting enxyme inhibitors and as antihypertensives.
    Type: Grant
    Filed: May 19, 1986
    Date of Patent: July 14, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Elbert E. Harris, Arthur A. Patchett, Eugene D. Thorsett
  • Analogs of substance P and eledoisin
    Patent number: 4680283
    Abstract: Analogs of substance P and eledoisin which are conformationally constrained by the presence of a lactam in the peptide chain demonstrate greater selectivity and increased protease stability and are useful as analgesic, anti-inflammatory, antihypertensive, central nervous system agents, and stimulants of lachrymal secretion. The compounds are prepared by standard peptide synthetic procedures.
    Type: Grant
    Filed: August 20, 1986
    Date of Patent: July 14, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Daniel F. Veber, Roger Freidinger
  • Substituted azetidinones as anti-inflammatory and antidegenerative agents
    Patent number: 4680391
    Abstract: New substituted azetidinones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
    Type: Grant
    Filed: April 10, 1985
    Date of Patent: July 14, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Raymond A. Firestone, Peter L. Barker
  • Prodrugs of antihypercholesterolemic compounds
    Patent number: 4678806
    Abstract: 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 the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.
    Type: Grant
    Filed: September 2, 1986
    Date of Patent: July 7, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Wasyl Halczenko, George Hartman, Steven M. Pitzenberger
  • 1,2(1,4)-dimethyl-4(2)-(2-hydroxyethyl)-5-nitro-imidazole antiprotozoal agents with reduced mutagenicity
    Patent number: 4678799
    Abstract: A group of 4-substituted-5-nitroimidazoles is described, having effective antiprotozoal activity with much less mutagenicity than is shown by known 5-nitroimidazoles.
    Type: Grant
    Filed: December 24, 1984
    Date of Patent: July 7, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Gerald T. Miwa, John S. Walsh
  • Substituted benzenesulfonamides
    Patent number: 4678855
    Abstract: Benzenesulfonamides with a substituted-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: October 9, 1985
    Date of Patent: July 7, 1987
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth L. Shepard
  • Novel synergistic compositions
    Patent number: 4678774
    Abstract: 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 semisynthetic derivatives thereof are compounds known to be highly effective broad-spectrum antiparasitic and pesticidal agents. However, when such compounds are formulated into the instant composition, the activity observed is increased to at least 10-times that which would be expected. The instant substrate is preferably a highly dispersed, amorphous form of hydrophyllic silicon dioxide.
    Type: Grant
    Filed: June 6, 1985
    Date of Patent: July 7, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Irving Putter, Daniel M. Stout
  • Cyclic ureas as dermal penetration enhancers
    Patent number: 4677131
    Abstract: 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.
    Type: Grant
    Filed: November 1, 1985
    Date of Patent: June 30, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Takeru Higuchi, Stefano A. Pogany
  • Antiglaucoma thieno-thiopyran and thieno-thiepin sulfonamide derivatives, compositions, and method of use thereof
    Patent number: 4677115
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: May 14, 1986
    Date of Patent: June 30, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Marcia E. Christy, Gerald S. Ponticello
  • Substituted diazapines and derivatives thereof useful in the treatment of cardiovascular disorders
    Patent number: 4677102
    Abstract: There are disclosed novel diazapines and derivatives thereof which are useful in the treatment of cardiovascular disorders.
    Type: Grant
    Filed: February 7, 1986
    Date of Patent: June 30, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David E. McClure, David A. Claremon
  • Substituted dihydroazepines useful as calcium channel blockers
    Patent number: 4677101
    Abstract: Substituted dihydroazepines, their preparation, and the use thereof as calcium channel blockers are disclosed.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: June 30, 1987
    Assignee: Merck & Co., Inc.
    Inventors: David A. Claremon, David E. McClure
  • Non-mutagenic 1,2-disubstituted 4-nitro-imidazoles useful as antiprotozoal agents
    Patent number: 4675337
    Abstract: 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 for antiprotozoal uses of said novel 1,2-disubstituted-4-nitroimidazole compounds are disclosed herein.
    Type: Grant
    Filed: February 28, 1986
    Date of Patent: June 23, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Gerald T. Miwa, Wen-Jen R. Wang, John S. Walsh
  • Substituted pyrimidines useful as calcium channel blockers
    Patent number: 4675321
    Abstract: Pharmaceutical compositions of specific substituted pyrimidines and methods of treatment of certain cardiovascular disorders are disclosed. Also disclosed are novel substituted acrylated pyrimidines which are useful as calcium channel blockers.
    Type: Grant
    Filed: February 7, 1986
    Date of Patent: June 23, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Steven M. Pitzenberger, David E. McClure