Patents Represented by Attorney William H. Nicholson

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  • Microbial transformation process for antihypertensive products
    Patent number: 5132216
    Abstract: Fermentation of the microorganism Streptomyces sp. MA6744 (ATCC No. 55041) in the presence of the Angiotensin II (A II) receptor antagonist ##STR1## yields a 7-hydroxymethyl, a 5,7-dihydroxymethyl, a 7-carboxy and a 1'-hydroxy-5-hydroxymethyl analog, all of which are also A II antagonists useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
    Type: Grant
    Filed: June 7, 1991
    Date of Patent: July 21, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, George Doss
  • Angiotensin II antagonists incorporating a nitrogen containing six membered ring heterocycle
    Patent number: 5128327
    Abstract: There are disclosed compounds, containing a pyridine, pyrazine or pyrimidine functionality on the lower ring of Formula I, which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: March 25, 1991
    Date of Patent: July 7, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Malcolm MacCross, Nathan Mantlo, Thomas F. Walsh
  • Imidazole angiotensin II antagonists incorporating acidic functional groups
    Patent number: 5126342
    Abstract: There are disclosed substituted imidazole derivatives of Formula I which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: October 1, 1990
    Date of Patent: June 30, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Elizabeth M. Naylor, Arthur A. Patchett, Thomas F. Walsh
  • Substituted pyrollo-fused 6 membered heterocycles as angiotensin II antagonists
    Patent number: 5124335
    Abstract: Substituted pyrrolo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: June 23, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, Nathan B. Mantlo, William J. Greenlee
  • Substituted aromatic sulfonamides as antiglaucoma agents
    Patent number: 5120757
    Abstract: Carbonic anhydrase inhibitors of the thieno[2,3-b]thiopyran-2-sulfonamide type with a substituted-alkyl-amino group in the 4-position are topically effective in lowering intraocular pressure.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: June 9, 1992
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Process for iodinating or brominating the .alpha.-methylenic carbon of a secondary amide
    Patent number: 5120847
    Abstract: A novel, facile, and specific process for .alpha.-iodinating or .alpha.-brominating the .alpha.-methylenic carbon of a straight chain, branched chain, or cyclic secondary amide, such as a lactam or an azasteroid, comprises reacting the amide with trialkylsilyl-X (R.sub.3 Si--X), where X is Br, I, or Cl, and R is methyl, ethyl, or n-propyl, in the presence of I.sub.2 or Br.sub.2. The .alpha.-iodo- or .alpha.-bromo-amide is useful for making the .alpha.,.beta.-unsaturated amide through dehydrohalogenation.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: June 9, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Anthony O. King, Sandor Karady, Kevin Anderson, Newton L. Abramson, Richard F. Shuman
  • Process for preparing aldehydes from base sensitive amines
    Patent number: 5118810
    Abstract: There is disclosed a process for preparing aldehydes from base sensitive amines. The process can be employed to obtain carboxylic acid methyl esters. In particular, thiazolidine carboxylic methyl ester can be produced which is useful as an intermediate in the preparation of bicyclic lactam compounds. These bicyclic lactam compounds are potent angiotesin converting enzyme (ACE) inhibitors useful in the treatment of hypertension, congestive heart failure, and the like.
    Type: Grant
    Filed: July 6, 1990
    Date of Patent: June 2, 1992
    Assignee: Merck & Co., Inc.
    Inventor: Conrad Santini
  • Adjuncts in cancer chemotherapy
    Patent number: 5114919
    Abstract: Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.
    Type: Grant
    Filed: February 11, 1991
    Date of Patent: May 19, 1992
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David C. Remy
  • Benzofuran compounds as class III antiarrhythmic agents
    Patent number: 5112824
    Abstract: Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, X and Y are bridging groups and p is 0 or 1, and E is --S-- or --O--, are Class III antiarrhythmic agents.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: May 12, 1992
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Harold G. Selnick, Gerald S. Ponticello, David C. Remy, David A. Claremon, Jason M. Elliott
  • Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists
    Patent number: 5102880
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogren atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: September 5, 1991
    Date of Patent: April 7, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Substituted pyrimidinones as angiotensin II antagonists
    Patent number: 5100897
    Abstract: Novel substituted pyrimidinones of formula (I) which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: July 16, 1990
    Date of Patent: March 31, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Arthur A. Patchett, Thomas F. Walsh
  • Substituted thieno(2,3-B)(1,4)thiazine-6-sulfonamides as antiglaucoma agents
    Patent number: 5093332
    Abstract: Thieno[2,3-b][1,4]thiazine-6-sulfonamides having the structural formula: ##STR1## wherein Z, R.sup.1, R.sup.2, and n are as hereinafter defined, are carbonic anhydrase inhibitors useful in the topical treatment of elevated intraocular pressure and glaucoma.
    Type: Grant
    Filed: October 1, 1990
    Date of Patent: March 3, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Cecilia A. Hunt
  • Radiopharmaceutical bacteriostats
    Patent number: 5093105
    Abstract: Benzalkonium chloride and benzethonium chloride are each useful in radiopharmaceutical preparations as bacteriostatic agents which are compatible with anti-oxidants.
    Type: Grant
    Filed: April 9, 1991
    Date of Patent: March 3, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard J. Flanagan, Daniel Tartaglia
  • Indenyl hydroxamic acids and hydroxy ureas as inhibitors of 5-lipoxygenase
    Patent number: 5093356
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: March 3, 1992
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Pierre Hamel, Daniel Delorme
  • Trialkylsilyl trifluoromethanesulfonate mediated .alpha.-methylenic carbon functionalization of 4-AZA-5.alpha.-androstan-3-one steroids
    Patent number: 5091534
    Abstract: A novel single-pot trialkylsilyl trifluoromethanesulfonate (R.sub.3 Si--OTf) mediated process produces derivatives of 4-aza 3-keto steroids at the .alpha.-methylenic carbon through electrophilic substitution. These derivatives are useful in the preparation, through elimination of the substituent on the .alpha.-methylene carbon, of .DELTA.-1 olefin 4-aza 3-keto steroids which are potent inhibitors of 5-.alpha. reductase.
    Type: Grant
    Filed: August 27, 1990
    Date of Patent: February 25, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Anthony O. P. King, Sandor Karady, Kevin Anderson, Alan W. Douglas, Newton L. Abramson, Richard F. Shuman
  • Process for preparing an angiotensin II antagonist
    Patent number: 5089626
    Abstract: There is disclosed a process for preparing the active metabolite of an angiotensin II antagonist from its pro-drug compound.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: February 18, 1992
    Assignee: Merck & Co., Inc.
    Inventor: Anthony O. King
  • Novel fermentation product with antiparasitic activity
    Patent number: 5089530
    Abstract: The fermentation of a fungal organism identified as Chrysosporium meridarium produces a novel binaphthalene compound which is a highly potent antiparasitic, insecticidal, and anthelminthic agent.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: February 18, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Athanasios Tsipouras, Dan A. Ostlind, Otto D. Hensens, Deborah L. Zink
  • Microbial transformation process for producing an antihypertensive product
    Patent number: 5087702
    Abstract: Fermentation of the microorganism Streptomyces sp. (MA6750) ATCC No. 55042 in the presence of the Angiotensin II (A II) receptor antagonist of the following structure: ##STR1## yields an analog having a shikimate sugar-like moiety attached to the tetrazole, the said analog which is also an A II antagonist useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II angatonists.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: February 11, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, Byron H. Arison, Raymond F. White, Edward S. Inamine
  • Microbial transformation process for antihypertensive products
    Patent number: 5085992
    Abstract: Fermentation of the microorganism Streptomyces sp. MA6751 (ATCC No. 55043) in the presence of the Angiotensin II (A II) receptor antagonist ##STR1## yields an N2-tetrazole .beta.-glucuronide analog which is also an A II antagonist useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
    Type: Grant
    Filed: February 25, 1991
    Date of Patent: February 4, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, George Doss
  • Process for preparation of novel angiotensin II antagonists
    Patent number: 5066586
    Abstract: Novel biotransformation compounds I, II, III and IV are prepared by fermenting 3-[(2'-tetrazol-5-yl-biphenyl-4-yl) methyl]-7-methyl-2-propyl-3H-imidzao [4,5-b]pyridine in a culture of Streptomyces sp., Accession Number ATCC 55041. ##STR1## These novel compounds are Angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
    Type: Grant
    Filed: August 20, 1990
    Date of Patent: November 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, George Doss