Patents by Inventor Gerard R. Kieczykowski

Gerard R. Kieczykowski 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).

  • Phenoxyphenylacetic acid derivatives
    Patent number: 5668176
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: September 16, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy Jo Kevin, Gerard R. Kieczykowski, Douglas J. Pettibone, James R. Tata, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Jay M. Matthews, Richard B. Toupence
  • Process for producing n-amino-1-hydroxy-alkyl-idene-1,1-bisphosphonic acids
    Patent number: 5648491
    Abstract: A process for continuously producing alkylpyrophosphonate, alkylpyrophosphate and multimers thereof and for producing 4-amino-1-hydroxyalkylidene-1,1-bisphosphonic acids or salts thereof.
    Type: Grant
    Filed: May 20, 1996
    Date of Patent: July 15, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Richard R. Dauer, Lisa DiMichele, Mauricio Futran, Gerard R. Kieczykowski
  • Aryl and heteroaryl macrolides having immunosuppressive activity
    Patent number: 5545734
    Abstract: Aryl and heteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by olefination at C-27. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases, and illnesses.
    Type: Grant
    Filed: October 25, 1994
    Date of Patent: August 13, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Gerard R. Kieczykowski, Hyun O. Ok, William H. Parsons, Kathleen M. Rupprecht
  • Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
    Patent number: 5510517
    Abstract: A process for continuously producing alkylpyrophosphonate, alkylpyrophosphate and multimers thereof and for producing 4-amino-1-hydroxyalkylidene-1,1-bisphosphonic acids or salts thereof.
    Type: Grant
    Filed: August 4, 1994
    Date of Patent: April 23, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Richard R. Dauer, Lisa DiMichele, Mauricio Futran, Gerard R. Kieczykowski
  • Process for preparing an antihypercalcemic agent
    Patent number: 5159108
    Abstract: Described is a new process for producing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP), a new antihypercalcemic agent. The process involves a 3-step sequence starting with 4-phthalimidobutanoyl chloride which can be practiced as a "one-pot" reaction sequence, without employing PCl.sub.3 or H.sub.3 PO.sub.3.
    Type: Grant
    Filed: August 1, 1991
    Date of Patent: October 27, 1992
    Assignee: Merck & Co., Inc.
    Inventor: Gerard R. Kieczykowski
  • Diphosphonate intermediate for preparing an antihypercalcemic agent
    Patent number: 5039819
    Abstract: Described is a new diphosphonate intermediate useful in a new process for producing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP), a new antihypercalcemic agent. The process involves a 3-step sequence starting with 4-phthalimidobutanoyl chloride which can be practiced as a "one-pot" reaction sequence, without employing PCl.sub.3 or H.sub.3 PO.sub.3. The new intermediate has the structure: ##STR1## where n=1-5.
    Type: Grant
    Filed: September 18, 1990
    Date of Patent: August 13, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Gerard R. Kieczykowski
  • Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP) or salts thereof
    Patent number: 5019651
    Abstract: An improved process is described for the preparation of 4-amino-1-hydroxybutylidene-1,1-bisophosphonic acid (ABP) or salts thereof which comprises:(a) reacting 4-aminobutyric acid with a mixture of phosphorous acid and PCl.sub.3 in the presence of methanesulfonic acid;(b) contacting the mixture from Step (a) with an aqueous hydrolysis mixture, wherein the pH is maintained in the range of 4 to 10 during the contacting; and(c) recovering said 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: May 28, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Gerard R. Kieczykowski
  • Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
    Patent number: 4922007
    Abstract: A process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-bisphosphonic acid or salts thereof which comprises:(a) reacting 4-aminobutyric acid with a mixture of phosphorous acid and PC1.sub.3 in the presence of methanesulfonic acid; and(b) recovering said 4-amino-1-hydroxybutylidene-1, 1-bisphosphonic acid or salts thereof.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: May 1, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Gerard R. Kieczykowski, David G. Melillo, Ronald B. Jobson
  • Process for the geometric stereoselective dehydration of 3-(9-chloro-5,6-dihydro-11H-11-hydroxy-pyrrolo-(2,1-B)(3)-benzazepin-11- yl)-N,N-dimethyl-1-propanamine
    Patent number: 4820818
    Abstract: The muscle relaxant (E)-3-(9-chloro-5,6-dihydro-11H-pyrrolo[2,1-b][3]benzazepin-11-ylidene-N,N -dimethyl-1-propanamine is prepared by the geometric stereoselective dehydration of the intermediate carbinol with acidic agents and organic bases and low temperatures.
    Type: Grant
    Filed: May 2, 1988
    Date of Patent: April 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ruth V. Wattley, Gerard R. Kieczykowski