Abstract: This invention relates to (amidomethyl)nitrogen heterocyclic and pyrrolidine compounds, pharmaceutical compositions containing them, methods of using such compounds and processes for making such compounds.
Type:
Grant
Filed:
January 14, 1991
Date of Patent:
October 19, 1993
Assignee:
The Du Pont Merck Pharmaceutical Company
Inventors:
Robert S. Cheeseman, Hollis S. Kezar, III, Richard M. Scribner
Abstract: A novel M.sub.r 25,000 chymotrypsin-like protease, termed clipsin, which binds to a-1-AChy in a sodium dodecyl sulfate-resistant manner, preferentially degrades .beta.-APP, and shows high activity for a period of a few days in neonatal rat brain is disclosed. Preparation of clipsin in a form that allows clipsin proteolytic activity to be measured under conditions substantially free of the activity other cellular non-clipsin proteases is also disclosed. Further disclosed is a method of identifying potential therapeutic agents for the treatment of selected neuropathologies such as Down's syndrome and Alzheimer's disease by measuring or inhibition of clipsin.
Type:
Grant
Filed:
June 22, 1990
Date of Patent:
October 12, 1993
Assignee:
The Du Pont Merck Pharmaceutical Company
Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.
Type:
Grant
Filed:
September 28, 1990
Date of Patent:
October 12, 1993
Assignee:
The Du Pont Merck Pharmaceutical Company
Inventors:
Gary A. Cain, Thomas E. Christos, Sang W. Tam
Abstract: This invention relates to bags for the cryopreservation of mammalian cells and particularly for the long-term freezing of red blood cell. This invention also relates to methods of manufacturing such bags.
Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
Type:
Grant
Filed:
February 6, 1992
Date of Patent:
September 7, 1993
Assignee:
The Du Pont Merck Pharmaceutical Company
Inventors:
Gary A. Cain, Paul J. Gilligan, Sang W. Tam
Abstract: A method to assist in the diagnosis of Alzheimer's disease comprising detecting, in bodily fluids, two APP-related proteins, in soluble form, said proteins have an apparent molecular size of about 130 kDa and about 35 kDa, and each of said proteins shares at least one epitope with the C-terminus of APP corresponding substantially to amino acids 676-695 of APP as shown in FIG. 1.
Type:
Grant
Filed:
June 1, 1989
Date of Patent:
August 10, 1993
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
John P. Card, Leonard G. Davis, Robert G. Siman
Abstract: The invention relates to a method of treating psychosis in a mammal which comprises administering to the mammal an effective amount of a dopamine receptor antagonist antipsychotic and a sigma receptor antagonist having greater affinity for sigma receptors than for dopamine receptors, in an amount effective to selectively enhance the antipsychotic effects of the dopamine receptor antagonist relative to the adverse side effects of the dopamine receptor antagonist.
Abstract: High-affinity murine monoclonal antibodies to t-PA were prepared which prolong the in vivo functional half-life of t-PA without decreasing its plasminogen-activator activity.
Type:
Grant
Filed:
April 26, 1988
Date of Patent:
July 6, 1993
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Thomas M. Reilly, Andrew T. Chiu, Robert M. Knabb
Abstract: The present invention relates to novel 5H-[1,2]benzisothiazolo[2,3-a]quinoline-5-ones, processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods of using these compounds for the treatment of inflammatory disorders.
Abstract: The present invention relates to novel substituted 15-oxa-, 15-thia-, and 15-aza- dihydrolanosterols, to pharmaceutical compositions containing such compounds, and to methods of using these compounds to suppress the activity of 3-hydroxy-3- methylglutaryl coenzyme A reductase (HMGR), an enzyme which is important in cholesterol biosynthesis. The overall effect of these heterocyclic lanosterol analogs is to decrease cholesterol formation, thereby resulting in lower serum cholesterol levels in mammals, and impaired ergosterol synthesis in fungi.
Abstract: (Indol-1'-ylmethyl)-, (Indazol-1'-ylmethyl)-, (Benzimidazol-1'-ylmethyl)-, and (Benzotriazol-1'-ylmethyl)- phenylacetaldehydes as Topical Antiinflammatories.
Abstract: There are provided nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
Abstract: There are provided novel bis-naphthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing such compounds.
Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.
Abstract: 4-Quinoline-carboxylic acid derivatives, such as 2-(2'-fluoro-1,1'-biphenyl-4-yl)-6-fluoro-3-methyl-4-quinoline carboxylic acid, in combination with other immunosuppressive agents are useful for the treatment and/or prevention of transplantation rejection, graft vs. host disease, autoimmune diseases, and chronic inflammatory disease.
Abstract: Processes are provided for preparing crystalline moricizine hydrochloride from moricizine using hydrochloric acid, wherein the crystalline moricizine hydrochloride so obtained is substantially free of occluded water.
Abstract: Physically and chemically stable pharmaceutical compositions useful for administering etanidazole by injection are described. These compositions are essentially aqueous solutions having a pH less than or equal to 5.5, and containing etanidazole, a buffer system, and a tonicity-adjusting agent, and they are optionally stabilized by the addition of a stabilizing agent or by autoclaving.
Type:
Grant
Filed:
June 26, 1992
Date of Patent:
March 9, 1993
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Surendra M. Bahal, Kenneth S. Field, Michael B. Maurin
Abstract: Dihydrobenz[c]acridine carboxylic acid derivatives are provided which are useful for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, autoimmune diseases, psoriasis and chronic inflammatory diseases.
Abstract: Peptides comprising C-terminal boronic acid derivatives of lysine, ornithine, and arginine, homoarginine and corresponding isothiouronium analogs thereof, are reversible inhibitors of trypsin-like serine proteases such as thrombin, plasma kallikrein and plasmin.
Type:
Grant
Filed:
April 6, 1988
Date of Patent:
February 16, 1993
Assignee:
Du Pont Merck Pharmaceutical Company
Inventors:
Charles A. Kettner, Ashokkumar B. Shenvi
Abstract: Ketones having formulas (1)-(3) are provided by improved methods which involve the treatment of compounds having formulas (9)-(11) with aqueous base. ##STR1## wherein R.sub.x is NO.sub.2.