Patents Represented by Attorney Paul D. Matukaitis
  • Patent number: 5310917
    Abstract: 4-Substituted-1,4-dihydropyridines are prepared by a cycloaddition reaction in which the cyclization is driven to completion, after thermal reaction, by addition of an acid. Felodipine, a vasodilator, is prepared by a cycloaddition reaction of ethyl 3-aminocrotonate with a suitably substituted dichlorobenzylidine under reaction conditions whereby the product crystallizes out of the reaction solution and may be directly isolated by filtration.
    Type: Grant
    Filed: July 28, 1992
    Date of Patent: May 10, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Joseph Auerbach
  • Patent number: 5306635
    Abstract: A gene of varicella-zoster virus (VZV) which encodes immunogenic outer surface viral proteins has been identified by DNA sequence analysis. Antibodies directed against peptides imputed from the DNA sequence can react with the glycoprotein, which itself is reactive with neutralizing antibodies. The amino-terminal sequence of the purified glycoprotein is identical to a portion of the amino acid sequence imputed from the DNA sequence. This glycoprotein is useful for the preparation of a vaccine against VZV.
    Type: Grant
    Filed: June 9, 1992
    Date of Patent: April 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Paul M. Keller, Mark W. Riemen, Ronald W. Ellis, Andrew J. Davison, Robert S. Lowe
  • Patent number: 5302604
    Abstract: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: April 12, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Kevin M. Byrne, Shieh-Shung T. Chen, Louis Kaplan, John G. MacConnell, Brian R. Petuch, Raymond F. White, Byron H. Arison
  • Patent number: 5294616
    Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
    Type: Grant
    Filed: March 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
  • Patent number: 5294627
    Abstract: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Bryon H. Arison, Shieh-Shung T. Chen, Raymond F. White, Brian R. Petuch
  • Patent number: 5292756
    Abstract: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
    Type: Grant
    Filed: March 25, 1992
    Date of Patent: March 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman
  • Patent number: 5292525
    Abstract: The use of aqueous compositions containing at least one chelating agent in the removal of alginates from cutaneous substrates to which they are bound is disclosed. Such compositions, which may also contain physiological salts and non-ionic surfactants, are particularly useful in the removal of alginate wound dressings from human or animal wounds, skin, or cellular tissue.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: March 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: R. A. Brenden, J. Burkey, F. T. Kirchner
  • Patent number: 5288725
    Abstract: A pyrroloquinoline compound of the following formula is disclosed: ##STR1## wherein H,C.sub.1-6 alkyl,R.sup.1 is: ##STR2## wherein R is H, C.sub.1-10 alkyl, or C.sub.1-6 alkyloxycarbonyl; R.sup.2 is:H,C.sub.1-6 alkyl, ##STR3## wherein R.sup.5 is C.sub.1-10 alkyl, aryl, or aryl C.sub.1-10 alkyl; R.sup.3 is:(CH.sub.2).sub.n NHR wherein R is H, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxycarbonyl; ##STR4## R.sup.4 is: H,C.sub.1-6 alkyl,C.sub.1-6 alkyloxycarbonyl,RCH.sub.2 --, wherein R is H, C.sub.1-6 alkyl or aryl, or ##STR5## X is O, or NR.sup.6 wherein R.sup.6 is equal to H or C.sub.1-6 alkyl and n is an integer from 1-3.The compounds of the invention exhibit bradykinin antagonist activity as well as activity with .alpha.-adrenergic, histaminergic, and muscarinic receptors.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: February 22, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Keith M. Witherup, Richard W. Ransom, Sandor L. Varga, Steven M. Pitzenberger, Victor J. Lotti, William J. Lumma
  • Patent number: 5286895
    Abstract: An acyclic tricarboxylic compound has been isolated from a culture of MF5453. The compound and its derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.
    Type: Grant
    Filed: December 7, 1992
    Date of Patent: February 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Guy H. Harris, Henry Joshua, Deborah L. Zink
  • Patent number: 5284758
    Abstract: This invention relates to a fungal microorganism Pseudodiplodia sp. (MF5767) isolated from bark discs of Hibiscus sp. and useful in a fermentation process to form compounds of formula (I): ##STR1## which are squalene synthetase inhibitors and thus useful as cholesterol lowering agents.
    Type: Grant
    Filed: August 14, 1992
    Date of Patent: February 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gerald F. Bills, Mary N. Omstead, Wendy H. Clapp, Fernando Pelaez
  • Patent number: 5283250
    Abstract: Non-peptidyl compounds characterized generally as quinolinyl/quinolinylalkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: August 2, 1991
    Date of Patent: February 1, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Dave Weissing, Mark Russell
  • Patent number: 5283256
    Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).
    Type: Grant
    Filed: July 22, 1992
    Date of Patent: February 1, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Claude Dufresne, Josep Guarro, Leeyuan Huang, Yu L. Kong, Russell B. Lingham, Maria S. Meinz, Keith C. Silverman, Sheo B. Singh
  • Patent number: 5281585
    Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: January 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
  • Patent number: 5278320
    Abstract: Compounds of Structural Formula (I) ##STR1## are produced by chemical modification of directed biosynthesis products. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: January 11, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Richard L. Monaghan
  • Patent number: 5270332
    Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents. The compounds also exhibit antifungal activity and are inhibitors of farnesyl-protein transferase.
    Type: Grant
    Filed: August 21, 1992
    Date of Patent: December 14, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Leeyuan Huang, John G. MacConnell, Jon D. Polishook, Raymond F. White
  • Patent number: 5244899
    Abstract: The compounds of this invention are azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: September 14, 1993
    Assignee: G. D. Searle and Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5242705
    Abstract: The present invention relates to a process for the preparation of a sweetener based on aspartame, which is in a dry form similar to that of a lump of sugar.According to the invention, this process comprises the preparation of a composition consisting in an aqueous dispersion of aspartame and at least one agent for modifying the texture, selected from polysaccharide with a high gelling power and monosaccharides or disaccharides with low calorific power, and the lyophilization of the resulting dispersion.Application: food industry; sugar substitute.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: September 7, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Christiane Cailler, Albert T. T. Luong, Isabelle Maroteaux
  • Patent number: 5240943
    Abstract: The present invention relates to compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof; wherein n is 0, 1 or 2;wherein R is H or lower alkyl of 1 to 6 carbon atoms;wherein X is selected from the group consisting of hydrogen, methane sulfonamide, nitro, cyano, imidazolyl, alkoxy of 1 to 6 carbon atoms and hydroxy; andwherein Ar is selected from the group consisting of pyridinyl, tetrahydronaphthalenyl, benzofuranyl, and Ph--CH.dbd.CH-- and phenyl all optionally substituted by methane sulfonamide, nitro, cyano, or imidazolyl with the proviso that when n is 1, Ar is other then phenyl;pharmaceutical compositions containing these compounds and a method for treating cardiac arrhythmias in mammals by administering the compositions.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: August 31, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Bipinchandra N. Desai, Konrad F. Koehler, Mark A. Russell
  • Patent number: 5239091
    Abstract: The present invention relates to 2-deoxy-N-acetyl-neuraminic acid derivatives and methods for their preparation.
    Type: Grant
    Filed: November 7, 1991
    Date of Patent: August 24, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Huey Wong, William J. Hennen
  • Patent number: 5234921
    Abstract: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: August 10, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Alan E. Moormann, Roger Nosal