Patents Represented by Attorney Harry E. Westlake, Jr.

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  • Process for selective reduction of nitroarginyl peptides with titanium (III)
    Patent number: 4152322
    Abstract: Nitroarginyl peptides are selectively reduced to the corresponding arginyl peptides by titanium (III). The nitro protecting group which is labile toward nucleophilic reagents is retained through part of a synthesis and selectively removed prior to treatment with nucleophiles such as hydrazine and ammonia. The selectivity of titanium (III) for removal of the nitro functionality increases the flexibility of this protecting group in the synthesis of arginyl peptides. The present novel process is useful in the synthesis of medicinal peptides such as molluscan cardiac stimulant H-Phe-Met-Arg-Phe-NH.sub.2.
    Type: Grant
    Filed: April 28, 1978
    Date of Patent: May 1, 1979
    Assignee: Merck & Co., Inc.
    Inventor: Roger M. Freidinger
  • MgO Impregnated activated carbon and its use in an improved vegetable oil refining process
    Patent number: 4150045
    Abstract: A novel impregnated activated carbon, containing from about 1.0 percent to about 15.0 percent by weight of MgO, has been found to be useful in a method of decolorizing a crude vegetable oil or a degummed vegetable oil, and removing organic acids therefrom, as well as in a process for making a refined edible vegetable oil wherein a crude vegetable oil is degummed, passed through the impregnated activated carbon, and subjected to steam distillation at reduced pressure. A novel method of preparing the MgO impregnated activated carbon has also been discovered.
    Type: Grant
    Filed: April 24, 1978
    Date of Patent: April 17, 1979
    Assignee: Calgon Corporation
    Inventor: Rabindra K. Sinha
  • Interphenylene 11,12-secoprostaglandins
    Patent number: 4150235
    Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.
    Type: Grant
    Filed: December 17, 1976
    Date of Patent: April 17, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking
  • Polypeptide possessing thymic activity
    Patent number: 4148886
    Abstract: The novel thymic factor polypeptide hormone, elaborated by the thymus and und in the blood serum, is isolated. The hormone is useful for the treatment of autoimmune diseases and for selectively stimulating T-cell activity in aging subjects.
    Type: Grant
    Filed: April 25, 1978
    Date of Patent: April 10, 1979
    Assignee: Institute National de la Sante & de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Bach, Jean Hamburger
  • Antipsychotic, antiserotonin and antihistaminic pyrrolo[2,1-b][3]benzazepines
    Patent number: 4148903
    Abstract: Pyrrolo[2,1-b][3]benzazepines with a piperidinylidene group in the 11-position have utility as antipsychotic agents. They also demonstrate antiserotonin and antihistaminic activity. They are prepared by reaction of a pyrrolo[2,1-b][3]benzazepin-11-one with a piperidinyl magnesium halide followed by dehydration.
    Type: Grant
    Filed: July 28, 1977
    Date of Patent: April 10, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Joseph G. Atkinson, Clarence S. Rooney, Patrice C. Belanger, David C. Remy
  • Somatostatin analogs
    Patent number: 4146612
    Abstract: Somatostatin analogs having the structural formula: ##STR1## wherein A is Phe, Tyr, O-Me-Tyr,B is Phe, Tyr,C is Thr, Val,R is H or COOH,wherein the ring formed by the peptide backbone contains 26 atoms and pharmaceutically acceptable non-toxic acid addition salts and carboxylic acid salts thereof are prepared by the solid phase method. These peptides have the property of inhibiting release of insulin, inhibiting growth hormone release and inhibiting glucagon release in humans and animals without materially affecting gastric secretion.
    Type: Grant
    Filed: June 29, 1978
    Date of Patent: March 27, 1979
    Assignee: Merck & Co., Inc.
    Inventor: Daniel F. Veber
  • Pyrazine-2-carbonyloxyguanidines
    Patent number: 4145551
    Abstract: The case involves novel pyrazine-2-carbonyloxyguanidines and processes for preparing same. The pyrazine-2-carbonyloxyguanidines are eukalemic or antikaliuretic agents possessing diuretic and natriuretic properties.
    Type: Grant
    Filed: January 9, 1978
    Date of Patent: March 20, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr., Mark G. Bock
  • Dihydroxybenzisoxazolin-3-yl-substituted-5-nitroimidazoles as antibacterials and antiprotozoals
    Patent number: 4144345
    Abstract: Dihydroxybenzisoxazolin-3-yl-substituted-1-methyl-5-nitroimidazoles having the hydroxy- groups on adjacent 4,5-; 5,6- or 6,7-positions of the isoxazolin group. These compounds have antibacterial and antiprotozoal activity in humans and animals. They are particularly active against trypanosomiasis and trichomoniasis.
    Type: Grant
    Filed: January 6, 1978
    Date of Patent: March 13, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Helmut H. Mrozik, Peter Kulsa
  • Heterocycle substituted (3-loweralkylamino-2-R.sub.1 O-propoxy)pyridines
    Patent number: 4144343
    Abstract: Heterocycle substituted (3-loweralkylamino-2-R.sub.1 O-propoxy)pyridines, their pharmaceutically acceptable salts and their preparation are disclosed. These pyridines have pharmaceutical properties such as anti-hypertensive activity of rapid onset.
    Type: Grant
    Filed: January 4, 1978
    Date of Patent: March 13, 1979
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Esters of .alpha.-methyl-3,4-OR-phenylalanines
    Patent number: 4143146
    Abstract: Derivatives of .alpha.-methyl-3,4-dihydroxyphenylalanine which are useful in compositions as anti-hypertensive agents.
    Type: Grant
    Filed: November 14, 1977
    Date of Patent: March 6, 1979
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Somatostatin analogs
    Patent number: 4140767
    Abstract: Bicyclic somatostatin analogs and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid phase method. These analogs have the property of inhibiting the release of growth hormone without affecting the level of gastric secretions or without affecting the level of gastric secretions, insulin and glucagon in humans and animals. The compounds are particularly useful in the treatment of acromegaly and diabetic retinopathy. Due to the bicyclic structure, these analogs are resistant to enzymatic metabolism and have a longer duration of activity than somatostatin.
    Type: Grant
    Filed: December 1, 1977
    Date of Patent: February 20, 1979
    Assignee: Merck & Co., Inc.
    Inventor: Daniel F. Veber
  • Interphenylene 11,12-secoprostaglandins
    Patent number: 4140861
    Abstract: Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.
    Type: Grant
    Filed: May 18, 1978
    Date of Patent: February 20, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking
  • N-pyrazinecarbonyl-N'-acylguanidines
    Patent number: 4140776
    Abstract: The case involves novel N-pyrazinecarbonyl-N'-acylguanidines and processes for preparing same. The N-pyrazinecarbonyl-N'-acylguanidines are eukalemic agents possessing diuretic and natriuretic properties.
    Type: Grant
    Filed: September 16, 1977
    Date of Patent: February 20, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
  • Somatostatin analogs
    Patent number: 4139526
    Abstract: Bicyclic somatostatin analogs and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid phase method. These analogs have the property of inhibiting the release of insulin, glucagon and growth hormone in humans and animals. The compounds are particularly useful in the treatment of diabetes. Due to the bicyclic structure, these analogs are resistant to enzymatic metabolism and have a longer duration of activity.
    Type: Grant
    Filed: December 1, 1977
    Date of Patent: February 13, 1979
    Assignee: Merck & Co., Inc.
    Inventor: Daniel F. Veber
  • Polypeptide possessing thymic activity
    Patent number: 4133804
    Abstract: The novel thymic factor polypeptide hormone, elaborated by the thymus and und in the blood serum, is isolated. The hormone is useful for the treatment of autoimmune diseases and for selectively stimulating T-cell activity in aging subjects.
    Type: Grant
    Filed: September 22, 1976
    Date of Patent: January 9, 1979
    Assignee: Institut National de la Sante et de la Recherche Medicale (Inserm)
    Inventors: Jean-Francois Bach, Jean Hamburger
  • N-(Benzoxazolinyl-2-one)-tricyclic dicarboximides
    Patent number: 4132799
    Abstract: Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives; and methods of treatment comprising administering such compounds and compositions.
    Type: Grant
    Filed: September 8, 1977
    Date of Patent: January 2, 1979
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, William J. Paleveda, Jr.
  • Process for preparing somatostatin analog
    Patent number: 4130554
    Abstract: Somatostatin analog, hereinafter designated des(Ala.sup.1 -Gly.sup.2)desaminocys.sup.3 -somatostatin, having the structure: ##STR1## is prepared by controlled stepwise procedures starting with individual amino acid components. This peptide has the property of lowering blood glucose, inhibiting gastric secretion and inhibiting growth hormone release in humans and animals.
    Type: Grant
    Filed: April 8, 1975
    Date of Patent: December 19, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Frederick W. Holly, William J. Paleveda, Robert G. Strachan, Daniel F. Veber
  • Substituted benzoylacrylanilides
    Patent number: 4130661
    Abstract: Novel substituted benzoylacrylanilides are prepared by reacting a substituted benzoylacrylic acid with a substituted aniline in the presence of a coupling agent. These acrylanilides have significant anticoccidial activity.
    Type: Grant
    Filed: June 30, 1977
    Date of Patent: December 19, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Peter Kulsa, Dale R. Hoff, Helmut H. Mrozik
  • 9-Thia- and oxothia- and 9-dioxothia-11,12-seco-prostaglandins
    Patent number: 4128564
    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: October 25, 1977
    Date of Patent: December 5, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., John B. Bicking, Robert L. Smith
  • Derivatives of thiadiazolo[3,4-d]pyrimidine
    Patent number: 4127721
    Abstract: 9-(Dihalobenzyl)adenines are prepared uncontaminated with other positional isomers in a series of mild transformations starting from 4,5,6-triaminopyrimidine and proceeding via 7-(N-formyl-N-dihalobenzyl)-amino[1,2,5]thiadiazolo[3,4-d]pyrimidine. The resulting compounds have anticoccidial activity and are useful in controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.
    Type: Grant
    Filed: November 21, 1977
    Date of Patent: November 28, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Roger J. Tull, George D. Hartman, Leonard M. Weinstock