Patents Assigned to Merck
  • Patent number: 4727062
    Abstract: Described are 3-halovinylglycines and their amino acid dipeptide and oligopeptide conjugates, a new class of efficient antibacterial agents, pharmaceutical compositions containing them as active ingredients, and methods of synthesis. The compounds are thought to interfere in bacterial cell wall synthesis.
    Type: Grant
    Filed: March 17, 1986
    Date of Patent: February 23, 1988
    Assignee: Merck & Co., Inc.
    Inventors: David Taub, Robert H. Abeles, Arthur A. Patchett
  • Patent number: 4727147
    Abstract: Racemic 1-(4-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline can be resolved by seeding the supersaturated solution of racemic 1-(4-methoxybenzyl)-octahydroisoquinolinium acetate with its enantiomeric forms and crystallizing the optically active acetate corresponding to the configuration of the seed crystals. The continuous form of the process permits obtaining the two enantiomers together.
    Type: Grant
    Filed: October 3, 1985
    Date of Patent: February 23, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Willi Wintermeyer, Fritz Reiff, Hans R. Muller, Josef Conti
  • Patent number: 4726911
    Abstract: Compounds of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --R.sup.2 IwhereinR.sup.1 and R.sup.2 are each an alkyl group having 1-10 C atoms, in which one or two non-adjacent CH.sub.2 groups can also be replaced by O atoms and/or CO groups and/or --OCO-- groups and/or --COO-- groups and/or --CH.dbd.CH-- groups, or are F, Cl, Br, CN or R.sup.3 --A.sup.3 --Z.sup.2 --,A.sup.1 is --A--, --A.sup.4 --A-- or --A--A.sup.4 --,A is a 1,3-dioxane-2,5-diyl or 1,3-dithiane-2,5-diyl group which is monosubstituted or polysubstituted in the 2-position and/or 4-position by alkyl each having 1-10 C atoms and/or in the 5-position by alkyl, alkoxy, fluorinated alkyl or fluorinated alkoxy each having 1-5 C atoms, or by F, Cl, Br or CN,A.sup.2, A.sup.3 and A.sup.4 each are 1,3-dithiane-2,5-diyl, piperidine-1,4-diyl, 1,4-bicyclo[2,2,2]octylene, decahydronaphthalene-2,6-diyl, 1,2,3,4-tetrahydronaphthalene-2,6-diyl, 1,4-phenylene, 1,4-phenylene which is substituted by one or two F and/or Cl atoms and/or CH.sub.
    Type: Grant
    Filed: October 17, 1985
    Date of Patent: February 23, 1988
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Joachim Krause, Peter Fuss, Reinhard Hittich, Bernhard Scheuble
  • Patent number: 4725594
    Abstract: Carbapenems having the formula: ##STR1## wherein: R.sup.1 is H;R.sup.4 and R.sup.5 are independently H, CH.sub.3 --, CH.sub.3 CH.sub.2 --, (CH.sub.3).sub.2 CH--, HOCH.sub.2 --, CH.sub.3 CH(OH)--, (CH.sub.3).sub.2 C(OH)--, FCH.sub.2, F.sub.2 CH--, F.sub.3 C--, CH.sub.3 CH(F)--, CH.sub.3 CF.sub.2 --, (CH.sub.3).sub.2 C(F)--; X is --S--, --SO--, --SO.sub.2 --, --O-- or --NH; L is a bridging group comprising substituted or unsubstituted C.sub.1 --C.sub.4 straight, C.sub.2 -C.sub.6 branched or C.sub.3 -C.sub.7 cycloalkyl groups wherein the substituents are selected from C.sub.1 -C.sub.6 alkyl, O--C.sub.1 -C.sub.6 alkyl, S--C.sub.1 -C.sub.6 alkyl, CF.sub.3, N(C.sub.1 -C.sub.6 alkyl).sub.2 ; Y is a carboxy-containing substituent; Het is internally alkylated heteroarylium, ##STR2## or externally alkylated heteroarylium, ##STR3## their preparation and antibiotic use are disclosed.
    Type: Grant
    Filed: December 13, 1984
    Date of Patent: February 16, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Burton G. Christensen, James V. Heck, Ronald W. Ratcliffe, Thomas N. Salzmann
  • Patent number: 4725606
    Abstract: 2-Benzyl-4-(4-pyridyl)thiazoles and derivatives thereof have been made from converting a benzyl cyanide to the corresponding thioamide followed by condensation with a 4-bromoacetylpyridine. The thiazole derivatives are found to be effective immunoregulants.
    Type: Grant
    Filed: August 21, 1986
    Date of Patent: February 16, 1988
    Assignee: Merck & Co., Inc.
    Inventors: David A. Boulton, Vernon L. Moore, Ihor E. Kopka, Arsenio A. Pessolano
  • Patent number: 4723958
    Abstract: There is provided a novel drug delivery system which provides for intermittent drug delivery with readily adjustable intervals between drug delivery pulses. This is accomplished by providing a multilayer device in which layers of active drug are readily expandable or erodable when contacted with the environment in which the drug is to be administered. The drug layer is alternated with an inert layer and a multiplicity of such layers are contained within a tube impervious to such environment but provided with an opening into such environment. The multiplicity of such layers is driven along the length of such tube towards the opening. The interval between pulses is determined by the rate the layers are driven along the tube and the sizes of the layers. The duration of the pulse is determined by the rate of expansion or dispersion of the active layer into the environment, wherein the rate of expansion or dispersion is greater than the rate the layers are driven along the tube.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: February 9, 1988
    Assignee: Merck & Co., Inc.
    Inventors: David G. Pope, Alan E. Royce
  • Patent number: 4724237
    Abstract: Novel 2-substituted-aminomethyl-1,4-benzodiazepines which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.
    Type: Grant
    Filed: June 26, 1984
    Date of Patent: February 9, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Roger M. Freidinger
  • Patent number: 4724097
    Abstract: New bicyclohexylethanes of formula IR1--Cy--Cy--CH2CH2--A--(Cy)n--R2 (I)wherein R1 is alkyl; R2 is alkyl, in which one or two non-adjacent CH.sub.2 groups can be replaced by 0 atoms, or is F, Cl, Br, CN, --COOalkyl or --O--CO--alkyl; or one of the radicals R.sup.1 and R.sup.2 can also be H; A is Cy, or 1,4-phenylene which is unsubstituted or substituted by one or two F and/or Cl atoms and/or CH.sub.3 groups or by a CN group; Cy is 1,4-cyclohexylene and n is 0 or 1; the alkyl groups in each case containing 1-10 C atoms, with the proviso that n is 1 if A is Cy and R2 is CN, can be used as constituents of dielectrics for electrooptical display elements.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: February 9, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Michael Romer, Rudolf Fidenschink, Joachim Krause, Bernhard Scheuble, Georg Weber
  • Patent number: 4724145
    Abstract: High levels of immunity are achieved in chickens inoculated intramuscularly or orally with E. acervulina extract immunogens. These extracts contain at least 20 polypeptides which induce a protective immune response not only against E. acervulina but also against E. tenella and E. maxima. The resulting immunity prevents intestinal lesions and reduces the number of viable oocysts in vaccinated and challenged birds. One or more of these polypeptides can be used as an immunogen to protect against coccidiosis.
    Type: Grant
    Filed: November 18, 1985
    Date of Patent: February 9, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Peter K. Murray, Balbir S. Bhogal, Ethel B. Jacobson, Mark S. Crane, Dennis M. Schmatz, Stefan Galuska
  • Patent number: 4722804
    Abstract: A liquid crystal composition having a positive dielectric anisotropy in the nematic phase, comprising of each 3 wt % or more of 2-(4-alkoxyphenyl)-5-alkylpyrimidine compound and of a cyanobiphenyl compound.
    Type: Grant
    Filed: February 28, 1986
    Date of Patent: February 2, 1988
    Assignees: Sharp Kabushiki Kaisha, Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Yutaka Ishii, Fumiaki Funada, Masataka Matsuura
  • Patent number: 4723005
    Abstract: New anisotropic compounds of the formula (1) are useful in liquid crystal mixtures for electrooptical displays; at least one of the end groups of the compounds (1) is an alkyl group which carries cyano or halogen in a terminal or non-terminal position. This offers advantages for longitudinal polarization and/or cross-polarization of the anisotropic compounds with the aid of the comparatively highly polarizing cyano or halogen substituents, in particular high clear points, low .DELTA..epsilon./.epsilon..perp. values and/or negative .DELTA..epsilon. values.
    Type: Grant
    Filed: September 10, 1984
    Date of Patent: February 2, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Tuong Huynh-Ba, Maged A. Osman
  • Patent number: 4721734
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, chlorine, phenyl, dialkylamino of 2-4 carbon atoms or alkyl or alkoxy each of up to 18 carbon atoms; R.sub.2 is hydrogen, chlorine, bromine or alkyl or alkoxy each of up to 4 carbon atoms; R.sub.3 and R.sub.4, which can be the same or different, each is hydrogen or alkyl of up to 6 carbon atoms; R.sub.5 is hydrogen or alkyl or alkanoyl each of up to 4 carbon atoms; and R.sub.6 is hydrogen or methyl, with the proviso that not all of R.sub.1 to R.sub.6 simultaneously are hydrogen, are effective photosensitizers, especially for photopolymerization of unsaturated compounds and for hardening of printing dyes.
    Type: Grant
    Filed: August 31, 1984
    Date of Patent: January 26, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Juergen Gehlhaus, Manfred Kieser
  • Patent number: 4721776
    Abstract: New amino acid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CHR.sup.4 --(CHR.sup.5).sub.n CO--B--D Iin which X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, B, D and n have the meanings defined herein, and their salts inhibit the activity of human plasma renin.
    Type: Grant
    Filed: November 14, 1986
    Date of Patent: January 26, 1988
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Peter Raddatz, Gunter Holzemann, Claus J. Schmitges, Klaus O. Minck
  • Patent number: 4721794
    Abstract: Thiophene-2-sulfonamides with a 5-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: January 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Patent number: 4721708
    Abstract: Novel N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.
    Type: Grant
    Filed: November 26, 1985
    Date of Patent: January 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Brian T. Phillips
  • Patent number: 4721791
    Abstract: Novel 5-amino or substituted amino 1,2,3-triazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance.
    Type: Grant
    Filed: May 19, 1986
    Date of Patent: January 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Elbert Harris, Richard L. Tolman
  • Patent number: 4720389
    Abstract: A fermented malt beverage having improved foam stability and desirable lace, cling, and clarity is described. The beverage is stabilized by adding 5-400 ppm by weight of combined xanthan gum and a galactomannan, e.g., guar gum or locust bean gum, or the glucomannan konjak gum.
    Type: Grant
    Filed: April 22, 1986
    Date of Patent: January 19, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth Clare, Margaret A. Lawson
  • Patent number: 4720505
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: January 19, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, John W. Gillard, Joshua Rokach
  • Patent number: 4720438
    Abstract: A process for producing a molded clay article having pearly luster, comprised coating a molded clay article with a mixture of (1) a glaze adjusted to have the sum of the R.sub.2 O groups in the Seger formula in the range of 0 to 0.55 mole and (2) a pearlescent pigment comprising mica powder particles having a coating of transparent metal oxide; and firing the coated clay article at a temperature not exceeding 900.degree. C.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: January 19, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Takaji Watanabe, Katsuhisa Nitta
  • Patent number: 4720503
    Abstract: N-substituted fused-heterocyclic carboxamide derivatives, for example, N-(2,2-diphenylethenyl)-3-hydroxythieno[3,2-b]thiophene-2-carboxamide can be prepared by ring closure between an appropriately substituted halo-thiophene ester, e.g., methyl 3-bromo-thiophene-2-carboxylate, and mercaptoacetamide followed by condensation with diphenylacetaldehyde. Alternatively, the ring closure can be carried out between an appropriately substituted mercaptothiophene ester, e.g., methyl 3-mercaptothiophene-2-carboxylate and a haloacetamide to afford the fused-heterocyclic intermediate, 3-hydroxythieno[3,2-b]thiophene-2-carboxamide. N-alkenylation of the intermediate will then lead to the final products.
    Type: Grant
    Filed: August 2, 1985
    Date of Patent: January 19, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Allan N. Tischler, Debra L. Allison