Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5536750
    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: November 30, 1994
    Date of Patent: July 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel L. Graham
  • 3-aryl or heteroaryl-7-heteroaralkylamido cephalosporin compounds, compositions and methods of use
    Patent number: 5534507
    Abstract: A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-;Y represents CH or N;Y" represents (a) CR.sup.y 'R.sup.z ' with R.sup.y ' and R.sup.z ' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH.Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical editions and methods of use are also included.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 9, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Lovji D. Cama, James V. Heck
  • Prodrugs of inhibitors of farnesyl-protein transferase
    Patent number: 5534537
    Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
    Type: Grant
    Filed: March 29, 1995
    Date of Patent: July 9, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, Suzanne C. MacTough, Theresa M. Williams
  • Indole derivatives with affinity for the cannabinoid receptor
    Patent number: 5532237
    Abstract: Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating glaucoma because of the activity on the cannabinoid receptor.
    Type: Grant
    Filed: February 15, 1995
    Date of Patent: July 2, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Michel Gallant, Yves Gareau, Daniel Guay, Marc Labelle, Petpiboon Prasit
  • Carbapenem antibiotics, compositions containing such compounds and methods of use
    Patent number: 5532261
    Abstract: Compounds are disclosed represented by the formula: ##STR1## wherein Y is: ##STR2## or a pharmaceutically acceptable salt or ester thereof. ##STR3## represents an aromatic 6 membered ring; zero or one of T, U, V and W represents N.sup.+ R.sup.y and the remainder of T, U, V and W are independently selected from C and N, such that one of T, U, V and W represents N.sup.+ R.sup.y or N.Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: July 2, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Ravindra N. Guthikonda, Laura C. Meurer
  • Fluorescence assay of Ras farnesyl protein transferase
    Patent number: 5525479
    Abstract: This invention is directed to a continuous fluorescence assay of Ras farnesyl:protein transferase. This assay can be used to screen for inhibitors of farnesyl:protein transferase. The assay may also be modified to screen for inhibitors of other protein transferases.
    Type: Grant
    Filed: February 17, 1994
    Date of Patent: June 11, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, David L. Pompliano
  • Absorption enhancer/solubilizer combination for improved bioavailability of a zwitterionic compound
    Patent number: 5525596
    Abstract: Intestional absorption of zwitterionic compounds is enhanced when the compound is delivered with the absorption enhancer palmitoyl carnitine chloride and the solubilizing agent .beta.-cyclodextrin when compared to delivery with palmitoyl carnitine chloride or .beta.-cyclodextrin alone.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: June 11, 1996
    Assignee: Merck & Co., Inc.
    Inventor: Gerold L. Mosher
  • System and method for automatically feeding, inspecting and diverting tablets for continuous filling of tablet containers
    Patent number: 5522512
    Abstract: A system and method for automatically feeding, inspecting and diverting tablets for continuous filling of tablet containers includes a tablet conveyor system which divides the tablets in a plurality of tablet streams for inspection by color, size and shape. Following the tablet inspection, each tablet passes through a tablet diverter which diverts the tablets to a recycle stream, reject stream or one of two bottle filling positions based upon instruction from the inspection. A bottle conveyor system is provided which feeds empty bottles into a bottle escapement mechanism which positions the empty bottles for filling. Filled bottles are moved from the bottle escapement mechanism to an exit conveyor. The entire system is computer controlled by various control mechanisms to enable the system to be fully operational without operator assistance.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: June 4, 1996
    Assignee: Merck & Co., Inc.
    Inventors: John R. Archer, David E. Cumpstey, Richard H. Gray, Stephen Owen
  • Optic nerve health
    Patent number: 5523301
    Abstract: There is disclosed a method for maximizing the health of the optic nerve by application of topical .beta.-blockers to the eye. Maintaining or increasing retinal nerve fiber thickness has been found to have a link to the prevention of visual field loss and blindness.
    Type: Grant
    Filed: August 5, 1994
    Date of Patent: June 4, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Felix W. Amon, Bernard Schwartz
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5523456
    Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: June 4, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Gerald E. Stokker, Samuel L. Graham
  • Inhibitors of phosphoinositide-specific phospholipase C
    Patent number: 5519163
    Abstract: Novel .alpha.-hydroxyphosphonate compounds which inhibit mammalian phosphoinositide-specific phospholipase-C. The compounds are potent anti-inflammatory and analgesic agents and may be useful for the treatment of cancer.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: May 21, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Jackson B. Gibbs, Kenneth S. Koblan, Angus M. MacLeod, Kevin J. Merchant
  • Disposable reactor vessel
    Patent number: 5516491
    Abstract: A disposable transportable reactor vessel can be prepared by modifying an eye-dropper pipette. A HDPE plug is inserted in one end of the pipette to permit selective passage of fluid while preventing resin flow. The pipette is looped into the shape of a u-tube and inserted into a holder such that the pipette is axially aligned with the holder to facilitate use in a robotic system.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Gary S. Kath, Gregory W. King, Kevin Chapman
  • Aza cyclohexapeptide compounds
    Patent number: 5516756
    Abstract: The present invention is directed to novel aza cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski
  • Semi-synthetic lipopeptides, compositions containing said lipopeptides, and methods of use
    Patent number: 5516757
    Abstract: There are disclosed novel semi-synthetic lipopeptides of the formula (Seq. ID Nos. 1-6) ##STR1## wherein the substituents are defined herein, which show utility as antifungal and anti-Pneumocystis agents. Pharmaceutical compositions containing said compounds are also disclosed.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventor: James M. Balkovec
  • Pour-on formulations containing polymeric material
    Patent number: 5516761
    Abstract: There is disclosed a topical multiple-point-application formulation containing a solution of a polymeric material and an avermectin compound (active ingredient) which has been discovered to provide superior efficacy against ectoparasites, such as fleas and ticks and endoparasites such as nematodes and heartworms, when compared to conventional formulations. The formulation contains the avermectin active ingredient and up to 50% of the polymeric material.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: May 14, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Hoo-Kyun Choi, James B. Williams
  • Aza cyclohexapeptide compounds
    Patent number: 5514651
    Abstract: The present invention relates to aza cyclohexapeptide compounds of the formula (Seq ID Nos. 1-10) ##STR1## which may be useful as antibiotics, antifungal agents and for the treatment of Pneumocystis carinii infections.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: May 7, 1996
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Frances A. Bouffard, James F. Dropinski
  • Aza cyclohexapeptide compounds
    Patent number: 5514650
    Abstract: Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
    Type: Grant
    Filed: August 29, 1994
    Date of Patent: May 7, 1996
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Regina M. Black, Frances A. Bouffard
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5510371
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) 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 6, 1994
    Date of Patent: April 23, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Sheo B. Singh, George M. Garrity, Olga Genillourd, Russell B. Lingham, Isabel Martin, Mary N. Omstead, Keith C. Silverman, Deborah L. Zink
  • Asymmetric hydrogenation of beta- or gamma-ketoesters and beta- or gamma-ketoamides
    Patent number: 5508435
    Abstract: .beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50N/mm.sup.2 of hydrogen in the presence of a strong acid.
    Type: Grant
    Filed: January 5, 1994
    Date of Patent: April 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Joseph D. Armstrong, III, Lisa DiMichele, Alan W. Douglas, Jennifer L. Keller, Steven A. King, Andrew S. Thompson, Thomas R. Verhoeven
  • 2,6-diaryl pyridazinones with immunosuppressant activity
    Patent number: 5506228
    Abstract: A class of 2,6-diarylpyridazinones of general structural formula I have been identified that exhibit exhibit immunosuppressant activity with human T-lymphocytes, and are useful as an immunosuppressants. ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof, wherein:when M is S, R.sup.1 and R.sup.2 are selected from the following combinations:when R.sup.2 is 4-chloro, then R.sup.1 is 4-OCH.sub.3,2 -CH.sub.3, 4-Cl, 4-CH3,3-Cl, 3-CH3, 2-Cl, 4-H, 4-Br, 3-NO.sub.2 ; andwhen R.sup.2 is H, then R.sup.1 is 4-OCH.sub.3, andwhen M is --SO.sub.2 --, then R.sup.2 is H and R.sup.1 is 4-OCH.sub.3.As an immunosuppressant, these compounds are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: April 9, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Richard Norton, Mohammed K. A. Ibraham