Abstract: Poly(diallylamine) blended with poly(N-methylolacrylamide) effectively detackifies over-sprayed paint in the circulating water of a wet paint spray booth operation. After detackification the dispersed paint is flocculated with hydrolyzed polyacrylamide, the paint waste is removed, and the clarified water is recirculated back into the paint spray booth operation.
Abstract: Disclosed are 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids. I, where the generic 2-aza group includes azido, acylamino, amino, alkylamino, dialkylamino, triazolyl, triazolinyl, aziridinyl, and their pharmaceutically acceptable salt, ester, anhydride and amide derivatives which are useful as antibiotics. Also disclosed are processes for the preparation of I from the known, appropriately substituted bicyclic keto ester II via the 2-azido central intermediate III: ##STR1## wherein R.sup.16 is H or CH.sub.3, preferably beta-methyl; R.sup.6, and R.sup.7 are independently hydrogen, linear, branched or cyclic C.sub.1 -C.sub.5 alkyl, which can be substituted with fluoro, hydroxy, protected hydroxy, sulfoxy, amino, protected amino, wherein R.sup.6 and R.sup.7 taken together can also be C.sub.2 -C.sub.4 alkylidene, similarly substituted; with the proviso that both R.sup.6 and R.sup.7 are not unsubstituted alkyl, R.sup.1 and R.sup.
Type:
Grant
Filed:
August 16, 1990
Date of Patent:
August 18, 1992
Assignee:
Merck
Inventors:
Burton G. Christensen, Ronald W. Ratcliffe, John C. Chabala
Abstract: A process for producing an antibiotic compound which is normally one of several minor components in the cultivation of Z. arboricola ATCC 20868 to be the primary product is described.
Type:
Grant
Filed:
June 18, 1990
Date of Patent:
August 11, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Jimmy M. Fountoulakis, Prakash S. Masurekar
Abstract: An orthophosphate salt and sodium silicate, when used in a 3:1 ratio by weight, and in a concentration of 0.1 to 100 mg/L, are found to have a synergistic effect in controlling the corrosion of carbon steel in an aqueous system, e.g., a municipal water supply system. The synergistic combination is also useful in reducing lead solubility and leaching, and in stabilizing soluble iron and manganese and their reaction products.
Abstract: N-tetrazolyl beta-lactams of the Formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.2 is hydrogen, alkyl having 1 to 6 carbon atoms or carboalkoxy having 2 to 7 carbon atoms; andZ is ##STR2## and W is ##STR3## thus forming a zwitterion, or Z is ##STR4## wherein R.sup.1 is benzyl, phenyloxymethyl or ##STR5## wherein Y is alkoxy or substituted alkoxy having 1 to 6 carbon atoms wherein the substituent on the alkoxy group is --COOH; andW is ##STR6## wherein R.sup.3 is H, M or --CH.sub.2 COOM, wherein M is a pharmaceutically acceptable cation are disclosed. The compounds are useful as antibiotics.
Type:
Grant
Filed:
November 16, 1983
Date of Patent:
August 11, 1992
Assignee:
Merck & Co., Inc.
Inventors:
W. Alexander Andrus, Burton G. Christensen, James V. Heck
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. 53527. The analog of Formula II is produced by chemical synthesis.
Type:
Grant
Filed:
January 23, 1991
Date of Patent:
August 11, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Yiu-kuen T. Lam, Raymond S. Chang, Otto D. Hensens, Cheryl D. Schwartz, Deborah L. Zink
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: New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
Type:
Grant
Filed:
January 29, 1990
Date of Patent:
July 21, 1992
Assignee:
Merck & Co., Inc.
Inventors:
James B. Doherty, Raymond A. Firestone, Paul E. Finke, William K. Hagmann, Shrenik K. Shah, Kevan R. Thompson
Abstract: Novel 1,3-Diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediated by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.
Type:
Grant
Filed:
June 12, 1991
Date of Patent:
July 21, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Donald W. Graham, John C. Chabala, Tesfaye Biftu, Michael N. Chang, Yuan-Ching P. Chiang, Shu S. Yang, Kathryn L. Thompson
Abstract: There is disclosed a series of macrolides isolated from the fermentation broth of a microorganism identified as MA-5000 which morphological analysis reveals to be a strain of Streptomyces hygroscopicus. The compounds structures are presented based upon analytical studies. The compounds have antifungal activity.
Type:
Grant
Filed:
February 25, 1991
Date of Patent:
July 14, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Richard W. Burg, Jerrold M. Liesch, Otto D. Hensens, Sebastian Hernandez
Abstract: A regeneratable polymer-supported Pd(O) catalytic deblocking process using a regeneratable polymer-supported Pd(O) catalyst in a biphasic system deblocks various allyl-protected ester, carbonates, carbamates and cinnamyl esters.
Type:
Grant
Filed:
November 7, 1990
Date of Patent:
June 23, 1992
Assignee:
Merck & Co., Inc.
Inventors:
David M. Tschaen, F. Edward Roberts, Thomas R. Verhoeven
Abstract: New immunosuppressive cyclosporin analogs are disclosed consisting of [dehydro-Ala].sup.8 cyclosporins and derived therefrom cyclosporins having a sulfur containing amino acid at position-8.
Type:
Grant
Filed:
February 27, 1990
Date of Patent:
June 16, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Arthur A. Patchett, David Taub, Robert T. Goegelman
Abstract: There are disclosed avermectin derivatives which incorporate a spacer between the disaccharide and the aglycone. The synthetic spacer-containing analogs are derived from the corresponding aglycones which in turn are prepared by chemical modification of naturally occurring avermectins. The compounds are active antiparasitic agents and compositions for that use are disclosed.
Abstract: Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.
Abstract: Compounds of the formula: ##STR1## which are potent inhibitors of human renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory compounds, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these conditions which employ these novel compounds.
Type:
Grant
Filed:
September 9, 1991
Date of Patent:
May 19, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Wallace T. Ashton, Christine L. Cantone, Richard L. Tolman
Abstract: A series of carboxyl-containing N-alkyldipeptides have been found to posess antiviral potency--specifically against herpes simplex virus--by selectively inhibiting the viral ribonucleotide reductase enzyme.
Type:
Grant
Filed:
July 28, 1989
Date of Patent:
May 5, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Richard L. Tolman, Wallace T. Ashton, Mu T. Wu