Patents Assigned to Merck and Co., Inc.
  • 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
  • Cyclohexapeptidyl hydroxypropionitrile compounds
    Patent number: 5348940
    Abstract: Certain propionitrile compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described. A novel process for their preparation is also described.
    Type: Grant
    Filed: September 3, 1992
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Robert A. Zambias
  • Stabilizers for fibroblast growth factors
    Patent number: 5348941
    Abstract: Medicinal compositions containing fibroblast growth factor are stabilized against loss of biological activity by including in said composition a stabilizing amount of phytic add, phosvitin, phosphate buffer, (NH.sub.4).sub.6 P.sub.4 O.sub.13, Na.sub.5 P.sub.3 O.sub.10, Na.sub.4 P.sub.2 O.sub.7 and Na.sub.3 P.sub.3 O.sub.9, adenosine tetra, tri, di and mono phosphate and related diadenosine compounds plus other single and multi-phosphorylated mono and di-nucleotides, poly-aspartic acid, poly-adenylic-guanylic add and related compounds, double stranded deoxyribonucleic add, single stranded deoxyfibonucleic acid and poly-glutamic acid. Medicinal compositions for topical use are combined with a viscous excipient such as a water soluble polysaccharide with said combination with a second stabilizier.
    Type: Grant
    Filed: April 1, 1992
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: C. Russell Middaugh, Pei-Kuo Tsai, David B. Volkin
  • Antifungal compound and compositions containing the compound
    Patent number: 5348970
    Abstract: A compound of the formula 1: ##STR1## is produced via fermentation of a fungal isolate ATCC no. 74235. The organism is included herein, as well as a process for production of the compound, a pharmaceutical composition and a method of treatment.
    Type: Grant
    Filed: September 22, 1993
    Date of Patent: September 20, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, Janet C. Onishi, Gerald F. Bills, Robert A. Giacobbe, Fernando Pelaez, Maria T. Diez, Francisca Vicente, Julian Gorrochategui, Gregory L. Helms, Barnali Pramanik
  • 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
  • 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
  • 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
  • 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
  • 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
  • Composition and process for gelatin-free soft capsules
    Patent number: 5342626
    Abstract: The present invention relates to a polymer composition comprised of gellan, carrageenan and mannan gums and a process for producing flexible films for encapsulation comprising the gellan, carrageenan and mannan gum composition. The mannan gums include the galactomannans and the glucomannans. Advantageously, soft capsules of the above composition are produced using the novel process. The composition comprises a blend of a gellan gum: (carrageenan/mannan gum) wherein the gellan gum concentration ranges from about 0.1 to 50 weight percent and the ratio of carrageenan/locust bean gum ranges from 3:1 to 1:3. Additional reagents are added to this gum blend to form a film-forming polymer composition useful in the production of gelatin-free capsules or microcapsules.
    Type: Grant
    Filed: April 27, 1993
    Date of Patent: August 30, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Philip E. Winston, Jr., Frank J. Miskiel, Raymond C. Valli
  • 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
  • Process for the preparation of 2-diazo-3-trisubstituted silyloxy 3-butenoates
    Patent number: 5340927
    Abstract: A novel process for preparing 2-diazo-3-trisubstituted silyloxy-3-butenoates, synthons useful in the conversion of 3-substituted-4-acetoxy azetidinones and penicillin to thienamycin, imipenem and other carbapenem antibiotic compounds is provided, comprising the reaction of the appropriate diazo acetoacetate with the substituted silane, base and salt.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: August 23, 1994
    Assignee: Merck & Co., Inc.
    Inventor: David L. Hughes
  • Fibrinogen receptor antagonists
    Patent number: 5340798
    Abstract: The present invention comprises fibrinogen receptor antagonist compounds, compositions containing them and methods for using them to inhibit fibrinogen binding to blood platelets. Compounds of the invention have the following formula ##STR1## wherein Z is ##STR2## X is COOH, CH.sub.2 SH or SH; R.sup.1 is Y--R.sup.3, wherein R.sup.3 is alkyl and Y is amino, pyridinyl, pyrimidinyl or piperidinyl;R.sup.2 is H, alkyl, aryl, or arylalkyl; andR.sup.4 is alkyl, heteroalkyl, aryl or heteroaryl, wherein the aryl or heteroaryl group can be mono- or bi-cyclic.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: August 23, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ruth F. Nutt, Daniel F. Veber
  • Protein for inhibiting collagen-stimulated platelet aggregation
    Patent number: 5340726
    Abstract: A protein which inhibits collagen-stimulated platelet aggregation. The protein has a molecular weight of approximately 17,000. A method of isolating the protein from Ornithodoros moubata and using the protein to prevent or delay blood coagulation by blocking the stimulation of platelet aggregation by collagen is also described. The protein is useful in the prevention, prophylaxis, therapy and treatment of thrombotic diseases.
    Type: Grant
    Filed: August 16, 1993
    Date of Patent: August 23, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Thomas M. Connolly, Paul M. Keller, Lloyd H. Waxman
  • Inhibitors of farnesyl protein transferase
    Patent number: 5340828
    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: September 30, 1991
    Date of Patent: August 23, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, S. Jane deSolms
  • Fibrinogen receptor antagonists
    Patent number: 5338723
    Abstract: A fibrinogen receptor antagonist of the formula ##STR1## wherein XX represents a synthetic alpha-amino acid containing a linear side chain and ZZ represents a sequence of 1, 2, 3 or 4 amino acids.
    Type: Grant
    Filed: September 21, 1992
    Date of Patent: August 16, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ruth F. Nutt, Stephen F. Brady, Daniel F. Veber, Mark E. Duggan
  • DNA encoding glioma-derived growth factor having vascular endothelial cell growth promoting activity
    Patent number: 5338840
    Abstract: Glioma-derived growth factor is purified from the culture media used to maintain mammalian glioma cells. The protein stimulates mitogenesis of mammalian vascular endothelial cells and is useful for the promotion of vascular development and repair. This unique growth factor is also useful in the promotion of tissue repair.
    Type: Grant
    Filed: May 27, 1992
    Date of Patent: August 16, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Marvin L. Bayne, Kenneth A. Thomas, Jr., Gregory L. Conn
  • Boron containing intermediates useful in the preparation of carbapenems
    Patent number: 5338875
    Abstract: The present invention is directed to intermediates of the following formula which are useful in the preparation of Carbapenem-antibiotics ##STR1##
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: August 16, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ann DeCamp, Ulf H. Dolling, Yulan Li, Dale L. Rieger, Nobuyoshi Yasuda, Lyndon C. Xavier
  • Substituted triazoles as angiotensin II antagonists
    Patent number: 5336778
    Abstract: Novel substituted triazoles of the formula (I), which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Christine L. Cantone, Linda L. Chang, Malcolm Maccoss, Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
  • Process for crystalline cyclic lipopeptides
    Patent number: 5336756
    Abstract: A process for obtaining a compound of the formula ##STR1## in crystalline form by solubilizing the compound in warm aqueous n-propanol and then allowing the solution to stand at ambient temperature until crystal formation is substantially complete is described. The crystalline compound obtained thereby is also described.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: August 9, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Robert E. Schwartz, August J. Kempf, David J. Mathre