Abstract: Provided are substituted indoles, benzofurans, and benzothiophenes of the formula ##STR1## wherein X, R.sup.2 and R.sup.3 are described in the specification. These compounds are 5-lipoxygenase inhibitors and are useful as antiinflammatory agents.
Abstract: Topical polyethylene glycol based formulations for the delivery of 2-substituted-1-naphthols and indoles and particularly, 2-phenylmethyl-1-naphthol are provided. Said topical formulations exert excellent localized antiinflammatory activity while demonstrating low levels of skin penetration in vitro and in vivo thereby reducing unwanted side effects and reducing systemic toxicity associated with the active drug compounds.
Abstract: A process for the production of .sup.32 P-labeled nucleotides in accordance with an enzymatic pathway utilizing phosphotransacetylase and acetate kinase.
Abstract: A fluorene compound, 4,4'-[9H-fluoren-9-ylidenebis(methylene)]bispyrimidine, or a pharmaceutically acceptable salt thereof is useful in treating various neurological disorders in mammals. This compound has efficacy over a broad dosage range as measured by hypoxia induced cognition impairment and has a wide safety margin as measured by the ratio of cognition to the onset of overt symptoms.
Abstract: There are provided novel bis-napthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing intermediates to such compounds.
Type:
Grant
Filed:
June 7, 1990
Date of Patent:
February 4, 1992
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Robert J. Ardecky, Arthur D. Patten, Jung-Hui Sun
Abstract: Known and novel 4-aryl-4-piperidinecarbinols and heterocyclic analogs are useful as analgesics. Also provided are novel pyrrolidinecarbinols and hexahydroazepine carbinols which are useful as analgesics, antidepressants and, in some cases, as anorectic agents.
Abstract: Antifungal carbinols, particularly .alpha.-styryl carbinols, and the corresponding epoxy carbinols are provided. These carbinol compounds have the formula: ##STR1## or a pharmaceutically or agriculturally suitable salt thereof wherein E is a bond or an oxygen atom with the proviso that when E is oxygen; R, R.sup.1 are not halogen; andL, A, B, Q, R.sup.2, R.sup.3, R.sup.4 and n are as defined in the specification.
Type:
Grant
Filed:
October 23, 1990
Date of Patent:
January 28, 1992
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
John Cuomo, Richard S. Greenberg, Richard E. Olson
Abstract: 4-Quinolinecarboxylic acids and derivatives thereof, such as 2-(2'-fluoro-1,1'-biphenyl-4-yl)-6-fluoro-3-methyl-4-quinolinecarboxylic acid, are useful as immunodulatory and anti-inflammatory agents. Pharmaceutical formulations containing such compounds are useful for the treatment of autoimmune diseases, organ transplantation rejection, graft vs. host disease, multiple sclerosis, and chronic inflammatory diseases such as rheumatoid arthritis.
Type:
Grant
Filed:
June 28, 1990
Date of Patent:
January 28, 1992
Assignee:
The Du Pont Merck Pharmaceutical Company
Inventors:
Neil R. Ackerman, Bruce D. Jaffee, Scott E. Loveless, Russell H. Neubauer
Abstract: The invention relates to benzylketone phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylketone phospholipase A.sub.2 inhibitor. These compounds are also intermediates in the synthesis of other PLA.sub.2 inhibitors.
Abstract: There is disclosed a perfusable cell culture device capable of expansion and maintenance of biological cells, including mammalian, microbial, plant and insect cells in culture. The device comprises an upper and lower polymeric film layer and a gas and liquid permeable flow divider membrane. The flow divider membrane is affixed between the upper and lower polymeric layers and to the lower polymeric layer in a manner providing channels for fluid distribution of culture medium which is perfused at a controlled rate, uniformly across the flow divider membrane and to a bed of cells dispersed on the flow divider membrane.
Type:
Grant
Filed:
November 2, 1988
Date of Patent:
November 26, 1991
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Gary W. Howell, Joseph D. Irr, Ara T. Nahapetian
Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.
Type:
Grant
Filed:
August 23, 1990
Date of Patent:
November 12, 1991
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.
Type:
Grant
Filed:
April 7, 1988
Date of Patent:
October 22, 1991
Assignee:
The Du Pont Merck Pharmaceutical Company
Inventors:
David M. Stout, William L. Matier, Lawrence A. Black
Abstract: Pyridylphenyl nitrogen heterocycle-substituted carbinols and derivatives thereof and pharmaceutical compositions containing such compounds are useful for treating inflammatory diseases in mammals.
Abstract: Plasmid pUC8 and DNA coding for hIL-1.beta. are used to construct hybrid plasmids capable of high level expression in E. coli of soluble proteins, including mature hIL-1.beta. and derivatives of mature hIL-1.beta. having amino acid substitutions and insertions at one or all of positions 1 to 4 at the amino terminus. Derivatives of hIL-1.beta. with alterations at the N-terminus have been produced which have either enhanced or decreased bioactivity compared to native monocyte derived hIL-1.beta..
Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.
Type:
Grant
Filed:
July 24, 1990
Date of Patent:
August 27, 1991
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
Abstract: Benzo-fused cycloalkane and oxa- and thia- cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benzeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.
Type:
Grant
Filed:
December 21, 1989
Date of Patent:
August 27, 1991
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Penio Pennev, Parthasarathi Rajagopalan, Richard M. Scribner
Abstract: The invention relates to benzylamine phosphilipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylamine phospholipase A.sub.2 inhibitor.
Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-oxa or thio-lH-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetamide, possess useful antibacterial activity.
Abstract: Aminomethyl oxooxazolidinyl cycloalkylbenzene derivatives, such as l-N-[3-(2,3-dihydro-oxa or thia-1H-inden-5-yl)-2-oxooxazolidin-5-ylmethyl]acetamide, possess useful antibacterial activity.