Patents Represented by Attorney Joseph F. DiPrima

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  • 2-(9-fluorenonyl)-carbapenem intermediates
    Patent number: 5356889
    Abstract: Disclosed are carbapenems of the formula ##STR1## which are 2-(9-fluorenonyl)-carbapenems useful as antibacterial agents. Intermediates for preparation of these compounds is also disclosed.
    Type: Grant
    Filed: October 26, 1992
    Date of Patent: October 18, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Lovji D. Cama, James V. Heck
  • Inhibitors of farnesyl protein transferase
    Patent number: 5352705
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
  • Microbial transformation product having immunosuppressive activity
    Patent number: 5352783
    Abstract: Microbial transformation of a macrolide immunosuppressant by the microorganism Streptomyces sp., (Merck Culture Collection MA 6960) ATCC No. 55387 yields a compound of the structural formula (I): ##STR1## This compound is an immunosuppressant 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: June 9, 1993
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ali Shafiee, Byron H. Arison, Shieh-Shung T. Chen, Randall R. Miller, Ralph A. Stearns
  • Process for the production of a novel endothelin antagonist
    Patent number: 5352800
    Abstract: Fermentation processes for the production of a compound of the Structural Formula I ##STR1## The compound of Structural Formula I has been shown to have endothelin antagonist activity and is therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure vasospasm, cerebral and cardia ischemia, myocardial infarction inflammatory diseases, Raynaud's disease, endotoxin shock and asthma.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: October 4, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gerard F. Bills, Michael A. Goetz, Robert A. Giacobbe, Lucia Herranz, E. Tracy Turner Jones, Fernando Pelaez, Yu L. Kong, Sheo B. Singh, Siobhan Stevens-Miles
  • 2-biphenyl-carbapenems
    Patent number: 5350846
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: January 25, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann
  • Triazolyl and tetrazolyl phenyl substituted carbapenems, compositions containing such compounds and methods of use
    Patent number: 5350746
    Abstract: Triazolyl and tetrazolyl phenyl substituted carbapenems of the formula I are disclosed. ##STR1## One or two of the variables X, Y and Z represent nitrogen atoms. The heteroaryl ting may be charged or uncharged.Pharmaceutical compositions and methods of treatment are also disclosed.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, James V. Heck
  • Spheronization process using charged resins
    Patent number: 5350584
    Abstract: The invention comprises a novel process for the spheronization of charged resins. Spherical multiparticlates are produced which range in size from 0.3 mm to 3 mm in diameter. The spherical particle product is microcrystalline-free. The process consists of the steps of mixing followed by wet granulation, spheronization and drying.
    Type: Grant
    Filed: June 26, 1992
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gregory A. McClelland, Gaylen M. Zentner
  • Unguinol and analogs are animal growth permittants
    Patent number: 5350763
    Abstract: Unguinol is a well-known metabolite of the fungi Aspergillus unguis and Aspergillus nidulans. Unguinol has been found to be an active growth permittant and promotant in animals, in particular, monogastric animals such as chickens. In addition, the fermentation broth also produced the additional known unguinol derivatives of folipastatin and 2-chloro unguinol as well as the novel 4-methyl derivative. All of these compounds are active animal growth permittants. Compositions containing such unguinol derivatives for use as growth permittants and promotants are also disclosed.
    Type: Grant
    Filed: June 11, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Scott D. Feighner, Gino M. Salituro, Jack L. Smith, Nancy N. Tsou
  • Inhibitors of farnesyl protein transferase
    Patent number: 5350867
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Sheo B. Singh
  • N,N-diacylpiperazines
    Patent number: 5348955
    Abstract: Diacylpiperazines of general structural formula: ##STR1## are: angiotensin II (A-II) antagonists with affinity for both AT.sub.1 and AT.sub.2 receptors useful in the treatment of hypertension, congestive heat failure, cerebrovascular, cognitive, and CNS disorders.
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Mu T. Wu
  • Substituted azetidinones as anti-inflammatory and antidegenerative agents
    Patent number: 5348953
    Abstract: New substituted azetidinones of the general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described.
    Type: Grant
    Filed: December 17, 1992
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James B. Doherty, Paul E. Finke, William K. Hagmann, Amy L. Kissinger, Malcolm MacCoss, Shrenik K. Shah
  • O-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides having immunosuppressive activity
    Patent number: 5349061
    Abstract: O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroaryl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. 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 12, 1993
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Peter J. Sinclair, Joung Goulet, Frederick Wong, Mark Goulet, William H. Parsons, Matthew J. Wyvratt
  • Vaccine delivery system
    Patent number: 5346481
    Abstract: A disposable vaccine delivery system containing a single dosage vaccine, having a compressible "hour-glass" shaped container portion filled with a needle, containing the vaccine, enclosed in a rigid clamp assembly having syringe-type activation means for compressing and expelling the vaccine contents into the human subject.
    Type: Grant
    Filed: October 14, 1993
    Date of Patent: September 13, 1994
    Assignee: Merck & Co., Inc.
    Inventor: Leonid Bunin
  • N,N-diacylpiperazine tachykinin antagonists
    Patent number: 5344830
    Abstract: Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: September 6, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
  • Imidazolidyl macrolides having immunosuppressive activity
    Patent number: 5344925
    Abstract: Imidazolidyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. 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: September 20, 1993
    Date of Patent: September 6, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Peter J. Sinclair, Frederick Wong, Matthew J. Wyvratt
  • Cationic-2-heteroarylphenyl-carbapenem antibacterial agents
    Patent number: 5342933
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: August 30, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank DiNinno, Susan M. Schmitt, Ravindra N. Guthikonda
  • Antagonists of immunosuppressive macrolides
    Patent number: 5342935
    Abstract: Hydroxymacrolides and derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation at C-20. These macrolides are useful as antagonists of FK-506-type immunosuppressants. The compounds of the present invention are useful for modifying dosages of FK-506-type immunosuppressants in the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, the compounds of the present invention have utility as antidotes for overdoses of FK-506-type immunosuppressants.
    Type: Grant
    Filed: December 2, 1992
    Date of Patent: August 30, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Thomas R. Beattie, Matthew J. Wyvratt, Francis J. Dumont
  • 2-phenanthridinyl carbaphenem antibacterial agent
    Patent number: 5336674
    Abstract: The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety typically having a substituent attached to the nitrogen of the phenanthridine and substituted at other positions by various neutral substituents. When there is substitution on the nitrogen of the phenathridine moiety that nitrogen is a charged quaternary nitrogen.
    Type: Grant
    Filed: January 27, 1993
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Mark L. Greenlee, Thomas A. Rano, Wendy Lee
  • Tricyclic thienothiopyran carbonic anhydrase inhibitors
    Patent number: 5334591
    Abstract: Conformationally constrained tricyclic thienothiopyran compounds are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
    Type: Grant
    Filed: March 4, 1993
    Date of Patent: August 2, 1994
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Kenneth L. Shepard, Gerald S. Ponticello, Theresa M. Williams
  • Six-membered ring fused imidazoles substituted with phenoxyphenylacetic acid derivatives
    Patent number: 5334598
    Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I have endothelin ##STR1## antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: August 2, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, Thomas F. Walsh, David L. Williams, Jr.