Patents by Inventor Edward J. Cragoe, Jr.

Edward J. Cragoe, Jr. has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same
    Patent number: 4115573
    Abstract: The case involves novel N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same. The N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidines are excellent eukalemic agents possessing diuretic and natriuretic properties.
    Type: Grant
    Filed: March 4, 1977
    Date of Patent: September 19, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • Substituted 2-aminomethylphenyl sulfamates
    Patent number: 4113877
    Abstract: Substituted 2-aminomethylphenyl sulfamates and pharmaceutically acceptable acid addition salts wherein the sulfamate group is N-substituted with up to 2 groups and the phenyl nucleus is further substituted by from 2 to 4 nuclear substituents which are useful as diuretics and saluretics are disclosed. The products may be prepared by reacting a N-protected substituted 2-aminomethylphenol with a substituted sulfamoyl chloride to generate an intermediate which is N-deblocked to give the compounds of this invention.
    Type: Grant
    Filed: September 16, 1977
    Date of Patent: September 12, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Smith, Gerald E. Stokker, Edward J. Cragoe, Jr.
  • Interphenylene 8-aza-9-dioxothia-11,12-secoprostaglandins
    Patent number: 4112236
    Abstract: Interphenylene 8-aza-9-dioxothia-11,12-secoprostaglandins are prepared by the two-stage alkylation of the anion of a lower alkyl sulfonamide, R.sup.1 SO.sub.2 NH.sub.2, using first a compound of the formula: ##STR1## and second, a compound of the formula: ##STR2## The compounds produced have renal vasodilatory activity when administered orally and are therefore useful for treating patients with renal impairment.
    Type: Grant
    Filed: April 4, 1977
    Date of Patent: September 5, 1978
    Assignee: Merck & Co., Inc.
    Inventors: John B. Bicking, Edward J. Cragoe, Jr.
  • Inhibition of indoleamine-N-methyl transferase by 2-iminopyridines
    Patent number: 4105769
    Abstract: A method of inhibiting indoleamine-N-methyl transferase comprises the administration to a host of a therapeutically effective amount of 1-alkyl-2-iminopyrrolidines or 1-alkyl-2-iminopyridines or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 24, 1977
    Date of Patent: August 8, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Clarence S. Rooney, Joshua Rokach, Edward J. Cragoe, Jr.
  • 3-Thiazolidinyl heptanoic acids
    Patent number: 4102888
    Abstract: This invention relates to novel 8-aza-9-oxo-11-thia-, -11-oxothia-, and -11-dioxothia-prostanoic acid compounds, salts, and derivatives thereof and also to processes for the preparation of such compounds. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the treatment of certain autoimmune diseases, and in preventing thrombus formation.
    Type: Grant
    Filed: April 20, 1977
    Date of Patent: July 25, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Smith, Ta-Jyh Lee, Edward J. Cragoe, Jr.
  • 5-(Hydroxy (substituted) methyl)-2,3-dihydrobenzo furan-2-carboxylic acid and its derivatives
    Patent number: 4100294
    Abstract: 5-[Hydroxy(substituted)methyl]-2,3-dihydrobenzo-furan-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: July 11, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr., William Hoffman
  • 11,12-Secoprostaglandins
    Patent number: 4097504
    Abstract: This invention relates to 11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the treatment of hypertension, for the prevention of thrombus formation, in preventing gastric secretion, and as regulators of the immune response.
    Type: Grant
    Filed: December 17, 1976
    Date of Patent: June 27, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
  • (1-Oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio) alkanoic acids, and derivatives thereof
    Patent number: 4096267
    Abstract: [1-Oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]aklanoic acid, derivatives thereof, their salts, esters and amides are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. Also disclosed are processes for the preparation of such [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids, pharmaceutical compositions comprising therapeutically effective amounts of such compounds and methods of treatment comprising administering such compounds and compositions.
    Type: Grant
    Filed: June 10, 1975
    Date of Patent: June 20, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • 11,12-Secoprostaglandins
    Patent number: 4092356
    Abstract: This invention relates to 11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the treatment of hypertension, for the prevention of thrombus formation, in preventing gastric secretion, and as regulators of the immune response.
    Type: Grant
    Filed: December 17, 1976
    Date of Patent: May 30, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
  • 3,4-Dihydrospiro-2H-1,3-benzoxazines and their use in treating edema, abnormal electrolyte retention, and inflammation
    Patent number: 4092414
    Abstract: 3,4-Dihydrospiro-2H-1,3-benzoxazines are prepared by condensing aminomethylphenols with cyclic ketones. The products are diuretic and anti-inflammatory agents, and are useful in the treatment of autoimmune diseases, such as multiple sclerosis.
    Type: Grant
    Filed: February 19, 1976
    Date of Patent: May 30, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Everett M. Schultz, Gerald E. Stokker
  • 2-Imino-3-aminothiazolidines and indoleamine-N-methyltransferase inhibition
    Patent number: 4091105
    Abstract: 2-Imino-3-aminothiazolidines are inhibitors of indoleamine-N-methyl transferase in vivo.
    Type: Grant
    Filed: August 12, 1977
    Date of Patent: May 23, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Clarence S. Rooney, Grant W. Reader, Edward J. Cragoe, Jr.
  • 8-Aza-9-oxo(and dioxo)-thia-11,12-secoprostaglandins
    Patent number: 4091107
    Abstract: This invention relates to 8-aza-9-ozo(and dioxo)-thia-11,12-secoprostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the prevention of thrombus formation, to induce growth hormone release, and as regulators of the immune response.
    Type: Grant
    Filed: November 11, 1976
    Date of Patent: May 23, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., James H. Jones
  • 8-Aza-9-dioxothiaprostanoic acids
    Patent number: 4087435
    Abstract: Novel 8-aza-9-dioxothiaprostanoic acid compounds, their salts, and derivatives, are prepared from ethyl 7-(3-hydroxymethyl-2-isothiazolidinyl)-5-heptynoate S,S-dioxide by first hydrogenating the triple bond over a Lindlar catalyst, followed by mild oxidation, to produce the corresponding 3-formyl compound, which is condensed with the ylide prepared from dimethyl-(2-oxoheptyl)phosphonate to produce the .alpha.,.beta.-unsaturated ketone, followed by reduction to the corresponding carbinol, and ester hydrolysis. The compounds are useful especially for the treatment of patients with poorly functioning kidneys, as hypotensives, or as platelet aggregation inhibitors.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: May 2, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., James H. Jones, John B. Bicking
  • 2,3-Dihydro-6,7-disubstituted-5-acyl benzofuran-2-carboxylic acids
    Patent number: 4087542
    Abstract: 2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
    Type: Grant
    Filed: April 20, 1976
    Date of Patent: May 2, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • (3-Amino-5-substituted-6-fluoropyrazinoyl or pyrazamido)-guanidines and their derivatives bearing substituents on the guanidino nitrogens
    Patent number: 4087526
    Abstract: This invention is concerned with (3-amino-5-substituted-6-fluoropyrazinoyl or pyrazinamido)guanidine compounds and derivatives thereof bearing substituents on the guanidine nitrogens. These compounds possess useful natriuretic properties. Also included are processes for preparing these compounds and a novel intermediate used in the preparation of these compounds.
    Type: Grant
    Filed: July 23, 1976
    Date of Patent: May 2, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • 9-Thia-, 9-oxothia-, and 9-dioxothia-11,12-seco-prostaglandins and processes
    Patent number: 4085125
    Abstract: This invention relates to 9-thia-, 9-oxothia-, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.
    Type: Grant
    Filed: November 22, 1976
    Date of Patent: April 18, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
  • Pyrazinecarboxamides and processes for preparing same
    Patent number: 4085211
    Abstract: The case involves novel pyrazinecarboxamides and processes for preparing same. The pyrazinecarboxamides are excellent eukalemic agents possessing diuretic and natriuretic properties.
    Type: Grant
    Filed: September 13, 1976
    Date of Patent: April 18, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr., Charles N. Habecker
  • 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids
    Patent number: 4085219
    Abstract: 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids and their salt, ester, anhydride, amide and 5-tetrazolyl derivatives are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. The acid products are prepared by treating a 2,2-disubstituted-5-hydroxy(or mercapto)-1-indanone with an haloalkanoic acid or ester thereof and, if the ester is employed, hydrolyzing the ester.
    Type: Grant
    Filed: July 13, 1976
    Date of Patent: April 18, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • 6,7-Disubstituted-5-(acyl)benzofuran-2-carboxylic acids
    Patent number: 4085117
    Abstract: 6,7-Disubstituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
    Type: Grant
    Filed: October 18, 1976
    Date of Patent: April 18, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr., William F. Hoffman
  • 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkano acids
    Patent number: 4081554
    Abstract: 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids and their salt, ester, anhydride, amide and 5-tetrazolyl derivatives are disclosed. The products display a dual pharmaceutical utility in that they exhibit diuretic, saluretic and uricosuric activity. The acid products are prepared by treating a 2,2-disubstituted-5-hydroxy(or mercapto)-1-indanone with an haloalkanoic acid or ester thereof and, if the ester is employed, hydrolyzing the ester.
    Type: Grant
    Filed: July 13, 1976
    Date of Patent: March 28, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.