Abstract: Methods are disclosed for preparing partial and complete esters of poly-&ggr;-glutamic acid, and of the cross-linking of such esters by light of predetermined wavelength. The final products of the present invention are useful in local drug delivery in depot form, for guided tissue regeneration, and for inhibition of post-surgical adhesion.
Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.
Abstract: The entire hepatitis B virus pre-S antigen gene linked in one contiguous reading frame to the hepatitus B virus surface antigen gene has been expressed in Saccharomyces cerevisiae. The expressed protein aggregates into a particulate form which displays the major antigenic sites encoded by both domains, thereby highlighting the utility of yeast as a host for the expression of pre-S domains. This protein is useful in in vitro diagnostic systems and as a vaccine for the treatment and prevention of hepatitis B virus-induced diseases and/or infections.
Type:
Grant
Filed:
June 29, 1987
Date of Patent:
July 28, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Ronald W. Ellis, Peter J. Kniskern, Hagopian Arpi
Abstract: A microporous, cellulosic coating useful in combination with osmotically controlled drug delivery devices is disclosed. In one embodiment, this coating results from application to core tablets of a coating dispersion comprised of a synthetic latex formed by emulsification of cellulosic polymers stabilized by surfactants, containing a water-soluble pore forming agent and a plasticizer.
Abstract: A controlled release drug delivery device, comprised of swellable polymers, whose degree of swelling in an environment of use is controlled by swelling modulators blended within the polymers, is disclosed. The swelling modulators can include buffers, osmagents, surfactants or combinations thereof surrounded by a microporous coating or interspersed within individual matrices. The combination of controlled release swelling modulators with swellable polymers may be applied to regulate patterns of beneficial agent (typically a drug) release.
Type:
Grant
Filed:
November 7, 1989
Date of Patent:
June 9, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Gregory A. McClelland, Gaylen M. Zentner
Abstract: Carbonic anhydrase inhibitors of the thieno[2,3-b]thiopyran-2-sulfonamide type with a substituted-alkyl-amino group in the 4-position are topically effective in lowering intraocular pressure.
Abstract: Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, X and Y are bridging groups and p is 0 or 1, and E is --S-- or --O--, are Class III antiarrhythmic agents.
Type:
Grant
Filed:
July 15, 1991
Date of Patent:
May 12, 1992
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Harold G. Selnick, Gerald S. Ponticello, David C. Remy, David A. Claremon, Jason M. Elliott
Abstract: Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with .alpha.-aminoheptanoic acid result in analogs of ANF having increased potencies and metabolic stability.
Type:
Grant
Filed:
June 4, 1990
Date of Patent:
February 25, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Ruth F. Nutt, Terrence M. Ciccarone, Stephen F. Brady, Daniel F. Veber
Abstract: 4-Alkylamino-6-(C.sub.3-5 -hydrocarbyl)thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxides wherein the 4-alkylamino group is an ethylamino or propylamino are powerful carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
Type:
Grant
Filed:
May 17, 1990
Date of Patent:
February 25, 1992
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Gerald S. Ponticello, Kenneth L. Shepard, Theresa M. Williams
Abstract: The GAL4 protein is rate-limiting in quantity as a positive regulator for galactose-inducible promoters in strains of yeast. Novel strains are described in which the GAL4 protein can be overproduced in a regulatable fashion. These strains are useful for the regulatable expression in yeast of heterologous genes whose expression is driven by a galactose-inducible promoter.
Type:
Grant
Filed:
July 10, 1986
Date of Patent:
November 26, 1991
Assignee:
Merck & Co., Inc.
Inventors:
James E. Hopper, Loren D. Schultz, Kathryn J. Hofmann, Ronald W. Ellis
Abstract: Novel peptides having potent natriuretic activity are disclosed with the following amino acid sequence: ##STR1## wherein X is L-Ile, D-Ile, D-allo-Ile, L-Met or D-Met, Y is Gly, L-Ala or D-Ala, A is optionally absent or is Ser, Ser-Ser, Arg-Ser-Ser, Arg-Arg-Ser-Ser, Leu-Arg-Arg-Ser-Ser or Ser-Leu-Arg-Arg-Ser-Ser and B is optionally absent or is Asn, Asn-Ser, Asn-Ser-Phe, Asn-Ser-Phe-Arg, or Asn-Ser-Phe-Arg-Tyr, provided that at least one of Y.sup.10, Y.sup.16, Y.sup.20 or Y.sup.22 is Ala or D-Ala, and the amides, lower alkyl esters and the physiologically acceptable metal salts and acid addition salts thereof.
Type:
Grant
Filed:
August 23, 1990
Date of Patent:
October 15, 1991
Assignee:
Merck & Co., Inc.
Inventors:
Ruth F. Nutt, Theresa M. Williams, Daniel F. Veber, Terry A. Lyle
Abstract: Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of heptapeptides that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting acitivity of GRP.
Type:
Grant
Filed:
August 3, 1989
Date of Patent:
September 10, 1991
Assignee:
Merck and Co., Inc.
Inventors:
Allen I. Oliff, David C. Heimbrook, Mark W. Riemen, Victor M. Garsky
Abstract: The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl-methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of borane-dimethyl sulfide reductions of ketones to secondary alcohols.
Type:
Grant
Filed:
April 18, 1990
Date of Patent:
August 13, 1991
Assignee:
Merck & Co., Inc.
Inventors:
Thomas J. Blacklock, Todd K. Jones, David J. Mathre, Lyndon C. Xavier
Abstract: Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, and E is --S-- or --O--, are Class III antiarrhythmic agents.
Type:
Grant
Filed:
December 8, 1989
Date of Patent:
July 16, 1991
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
Abstract: Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members and Q is a nitrogen containing heterocycle, are antiarrhythmic agents.
Type:
Grant
Filed:
December 8, 1989
Date of Patent:
July 16, 1991
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
Abstract: Hepatitis B PreS2+S antigen is isolated from plasma by adsorption on an affinity chromatography column, elution with a chaotropic agent and treatment with concentrated urea at an elevated temperature. The process retains all or substantially all of the preS2+S antigen.
Type:
Grant
Filed:
September 1, 1988
Date of Patent:
July 9, 1991
Assignee:
Merck & Co., Inc.
Inventors:
Alexander U. Bertland, II, William J. Miller
Abstract: Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of peptide derivatives that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting activity of GRP.
Abstract: Hepatitis A virus is attenuated by propagation in cell culture in vitro by direct inoculation of the cell cultures with a human clinical specimen containing the virus.
Type:
Grant
Filed:
May 14, 1984
Date of Patent:
June 4, 1991
Assignee:
Merck & Co., Inc.
Inventors:
Paula A. Giesa, Maurice R. Hilleman, Philip J. Provost