Patents Represented by Attorney Michael C. Sudol
  • Patent number: 5288486
    Abstract: The instant invention is directed to a process for enhancing the efficacy of alcohol-based skin antiseptics comprising adding at least one alcohol-soluble viscosifying agent to an alcohol-based disinfectant, thereby lowering its alcohol evaporation rate and markedly increasing the exposure time that disinfecting concentrations of alcohol are present on skin. The improved alcohol-based antiseptics thus obtained are also claimed.
    Type: Grant
    Filed: March 29, 1991
    Date of Patent: February 22, 1994
    Assignee: Calgon Corporation
    Inventor: John H. White
  • Patent number: 5023241
    Abstract: Novel avermectin derivatives are disclosed, wherein the 4"-hydroxy group is replaced by a substituted acylamino or benzoylamino group. These avermectin derivatives can be further derivatized at the 5- and 23-positions as ketoximes or O-substituted ketoximes. The 4"-substituted avermectin derivatives are prepared by the acylation of the known 4"-aminoavermectins with acylating reagents. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: June 11, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Bruce O. Linn, Helmut Mrozik
  • Patent number: 4968507
    Abstract: The instant invention is directed to an osmotic pump comprising:(A) at least one active agent surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 1, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
    Type: Grant
    Filed: July 15, 1987
    Date of Patent: November 6, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Gaylen M. Zentner, Gerald S. Rork, Kenneth J. Himmelstein
  • Patent number: 4946835
    Abstract: A novel dioxa-diazacyclohexadecenetetrone isolated from the fermentation of a cyanobacterium (Nostoc sp.) is described. The compound is a new antifungal agent with a specificity generally toward filamentous fungi but also effective against Cryptococcus sp.
    Type: Grant
    Filed: July 15, 1988
    Date of Patent: August 7, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Charles F. Hirsch, Jerrold M. Liesch, Michael J. Salvatore, Robert E. Schwartz, David F. Sesin
  • Patent number: 4946686
    Abstract: A drug delivery device for the controlled release of a therapeutically active ingredient into an environment of use is disclosed which comprises:(A) a core composition comprising(a) a plurality of controlled release solubility modulating units comprising solubility modulating agents each of which is a complexing agent or a surfactant and which is either (i) surround by a water insoluble cost containing at least one pore forming additive dispersed throughout said coat, or (ii) dispersed in an individual matrix substrate, and(b) A therapeutically active ingredient; and(B) a water insoluble microporous wall surrounding said core composition comprising:(i) a polymer material that is permeable to water but substantially impermeable to solute and(ii) 0.1 to 75% by weight, based on the total weight of (i) and (ii), of at least one water leachable pore forming additive dispersed throughout said wall.
    Type: Grant
    Filed: May 1, 1989
    Date of Patent: August 7, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Gregory A. McClelland, Gaylen M. Zentner
  • Patent number: 4942235
    Abstract: A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizi ne-2,4'-imidazolidin]-3'-yl)ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2 -yl)amino]ethyl]methanesulfonamide is described.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: July 17, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. DeCamp, Ralph P. Volante, Anthony O. King, Ichiro Shinkai
  • Patent number: 4935443
    Abstract: Disclosed are compounds having the formula: ##STR1## wherein: R.sub.1 is hydrogen, analkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group;R.sub.2 is an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group, an alkyl group having 1 to 6 carbon atoms which contains an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups having 1 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof.These compounds increase the sensitivity of hypoxic cancer cells to radiation. Methods of preparing such compounds, protocols for administering them to human patients and animals, and pharmaceutical compositions containing them are also disclosed.
    Type: Grant
    Filed: June 26, 1989
    Date of Patent: June 19, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Patent number: 4929549
    Abstract: Novel 5-carbamoylthieno[2,3-b]thiophene-2-sulfonamides and derivatives thereof are prepared in reactions of 5-methoxycarbonylthieno-[2,3-b]thiophene-2-sulfonamide with alkylamines, alkoxyalkylamines and hydroxyalkylamines. These compounds are useful for the treatment of elevated intraocular pressure in compositions including ophthalmic drops and inserts.
    Type: Grant
    Filed: February 8, 1989
    Date of Patent: May 29, 1990
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh
  • Patent number: 4898853
    Abstract: This invention relates to acetylenic esters that are useful in the treatment of fungal diseases and hypercholesterolemic conditions.
    Type: Grant
    Filed: August 1, 1989
    Date of Patent: February 6, 1990
    Assignee: Merck & Co. Inc.
    Inventors: James V. Heck, Michael D. Lewis
  • Patent number: 4897423
    Abstract: A compound of the formula: ##STR1## wherein: n is an integer 2,3,4, or 5; R.sub.1 is hydrogen or an alkyl group; andR.sub.2 and R.sub.3 are defined as follows:R.sub.2 is hydrogen or an alkyl group;R.sub.3 is hydrogen or an alkyl group; orR.sub.2 and R.sub.3 together form a heterocyclic ring, e.g. piperidine, pyrrolidine.The compounds have high radiosensitizing activity, and act as agents toxic to hypoxic cells in the absence of radiation.
    Type: Grant
    Filed: August 2, 1988
    Date of Patent: January 30, 1990
    Assignee: Merck & Co. Inc.
    Inventors: Walfred S. Saari, Edward L. Engelhardt
  • Patent number: 4897479
    Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof are disclosed. In these compounds, R.sup.1 is halogen, --SR.sup.4 wherein R.sup.4 is H or alkyl of 1 to 4 carbon atoms, --OCH.sub.3, --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, --NR.sup.4 R.sup.5 wherein R.sup.4 is as defined above and R.sup.5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy or R.sup.1 is --N(CH.sub.3).sub.3.sup.+ X.sup.-whereinX is halogen or --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms;R.sup.2 is H, alkanoyl of 1 to 8 carbon atoms or benzoyl;R.sup.3 is A or B whereinA is ##STR2## and B is ##STR3## wherein R.sup.6 and R.sup.7 are independently selected from H and ##STR4## wherein R.sup.8 and R.sup.9 are independently selected from pharmaceutically acceptable cations and H, or R.sup.6 and R.sup.
    Type: Grant
    Filed: February 29, 1988
    Date of Patent: January 30, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Richard L. Tolman, Wallace Ashton, Malcolm Maccoss
  • Patent number: 4894444
    Abstract: Immunologically intact protein or peptide immunogens are recovered from vaccines consisting of immunogen-aluminum hydroxide (alum) complexes. Recovery consists of dissolution of the complexes with an alkali metal salt of a carboxylic acid at a basic pH, reduction of the pH to physiological levels, removal of excess dissolvent and isolation of the protein or peptide immunogen.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Edgar M. Scattergood, Roy W. Grabner
  • Patent number: 4894370
    Abstract: Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No.
    Type: Grant
    Filed: March 25, 1988
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Yiu-kuen T. Lam, Raymond S. Chang, Otto D. Hensens, Cheryl D. Schwartz, Deborah L. Zink
  • Patent number: 4886668
    Abstract: The instant invention is directed to a multiparticulate osmotic pump, for the controlled release of diltiazem L-malate to an environment of use, said pump comprising:(I) a carrier medium which does not maintain its integrity in the environment of use;(II) a multiple of tiny osmotic pump elements each comprising:(A) a core comprises diltiazem L-malate and an effective buffering amount of sodium bitartrate surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 0.5, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall,wherein the total amount of diltiazem L-malate in all of the osmotic pump elements is a therapeutically effective amount.
    Type: Grant
    Filed: September 24, 1987
    Date of Patent: December 12, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John L. Haslam, Gerald S. Rork
  • Patent number: 4883814
    Abstract: 1-Aryloxy-3-(substituted alkylamino)-2-propanols having the general information: ##STR1## and their pharmaceutically acceptable salts exhibit cardioselective .beta.-adrenergic blocking activity, and are useful as antihypertensive, cardioprotective, antiarrhythmic and, antianginal agents.
    Type: Grant
    Filed: July 7, 1988
    Date of Patent: November 28, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 4883878
    Abstract: This invention relates to a novel process for preparing unsymmetrical dithioacetals and dithioketals from aryl aldehydes and ketones.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: November 28, 1989
    Assignee: Merck & Co. Inc.
    Inventors: Joseph S. Amato, James M. McNamara, Johnnie L. Leazer, Jr., Paul J. Reider, Robert A. Reamer
  • Patent number: 4880633
    Abstract: A multilaminate transdermal drug delivery system containing only dissolved drug in the drug reservoir is described. The delivery system comprises a backing layer, a reservoir layer and a membrane layer, wherein the drug in the reservoir is completely dissolved and the control of delivery is effected by the joint action of reservoir and membrane.
    Type: Grant
    Filed: July 7, 1988
    Date of Patent: November 14, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Alice E. Loper, Anup K. Majumdar
  • Patent number: 4880821
    Abstract: A compound of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are defined as follows:R.sub.1 is hydrogen, an alkyl group, or an alkyl group having one or more hydroxy groups;R.sub.2 is an alkyl group having one or more hydroxy groups, or an alkyl group containing an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups same or different, or two alkyl groups which together form a cyclic amine, e.g. piperidine;R.sub.3 is hydrogen or an alkyl group; andR.sub.4 is hydrogen or an alkyl group.The compounds have high radiosensitizing activity and selectivity for hypoxic cells.
    Type: Grant
    Filed: August 17, 1988
    Date of Patent: November 14, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Patent number: 4880820
    Abstract: (S)-9-(2,3-dihydroxy-1-propoxymethyl)guanine has potent antiherpetic activity which is superior to the corresponding racemic mixture or the (R)-enantiomer and also is much more potent than 9-(2-hydroxyethoxymethyl)guanine. Acyl derivatives (prodrugs) of the (S)-enantiomer, which are more effective than the corresponding (R)-enantiomer analogs or related racemic mixtures provide formulation advantages and even higher plasma half lives in animals or man than the (S)-isomer.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: November 14, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Laura F. Canning, Arthur K. Field, Richard L. Tolman
  • Patent number: 4880631
    Abstract: The instant invention is directed to an osmotic pump, for the controlled release of diltiazem L-malate to an environment of use, said pump comprising:(A) a core which comprises a therapeutically effective amount of diltiazem L-malate and an effective buffering amount of sodium bitartrate surrounded by(B) a rate controlling water insoluble wall, having a fluid permeability of 6.96.times.10.sup.-18 to 6.96.times.10.sup.-14 cm.sup.3 sec/g and a reflection coefficient of less than 0.5, prepared from:(i) a polymer permeable to water but impermeable to solute and(ii) 0.1 to 60% by weight, based on the total weight of (i) and (ii), of at least one pH insensitive pore forming additive dispersed throughout said wall.
    Type: Grant
    Filed: September 24, 1987
    Date of Patent: November 14, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John L. Haslam, Gerald S. Rork