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.

Abstract: (Benzimidazol-1'-ymethyl)phenylacetaldehydes as Topical Anti-inflammatories.

Abstract: This invention is directed to a composition comprising a substantially purified protein which enhances endogenous stimulus-induced neurotransmitter release, said neurotransmitter being selected from the group consisting of acetylcholine, dopamine or serotonin, said protein having a binding affinity constant of at least 2.9.+-.0.8 nM for tritiated 3,3-bis(4-pyridinylmethyl)-1-phenylindolin-2-one as determined by a Scatchard analysis, and said protein being trypsin sensitive and phospholipase C insensitive.

Abstract: There are provided, novel no or low wax formulations for amantadine hydrochloride and methods for preparing such formulations.

Abstract: Polycyclic cognition enhancers having the general formula (1a), (1b) or (1c) are provided: ##STR1## wherein: R.sub.1 is a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;R.sub.2 and R.sub.3 are independently H, F, Cl, Br, NO.sub.2, CONH.sub.2, CON(R.sub.4)(R.sub.4 '), S(O).sub.m R.sub.4, CF.sub.3, or N(R.sub.4)(R.sub.4 ');R.sub.4 and R.sub.4 ' are independently H, alkyl having from 1 to 4 carbon atoms, CH.sub.2 Phe--W, or Phe--W;Phe is a phenyl group;R.sub.5 is --(CH.sub.2).sub.n --Y or --OCOR.sub.4 ;Y is H, OH, NH.sub.2, NHR.sub.4, N(R.sub.4)(R.sub.4 '), NHCOR.sub.4, NHCO.sub.2 R.sub.4, NHS(O).sub.2 R.sub.4, F, Cl, Br, OR.sub.4, S(O).sub.m R.sub.4, CO.sub.2 H, CO.sub.2 R.sub.4, CN, CON(R.sub.4)(R.sub.4 '), CONHR.sub.4, CONH.sub.2, COR.sub.4, Phe, Phe--W, --C.tbd.CCO.sub.2 R.sub.4, --CH.dbd.CHR.sub.4, --C.tbd.CR.sub.4, or a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;W is F, Cl, Br, R.sub.4, OR.sub.4, NO.sub.2, NH.

Abstract: (Indazol-1'-ymethyl)phenylacetaldehydes as Topical Anti-inflammatories.

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.

Abstract: A method of separating active and inactive/latent forms of PAI-1 is disclosed comprising loading a sample containing a mixture of active and inactive/latent forms of PAI-1 to either an anion or cation exchange resin of 10-50 micron particle size and eluting active and inactive/latent forms of PAI-1 from the resin into separate fractions. Also disclosed is a method of extracting soluble E. coli-expressed recombinant PAI-1 from the lysed E. coli host cells in a buffered solution, wherein the ionic strength of the buffered solution is 8-25 millisiemens.

Abstract: Pharmaceutical compositions for controlling, by topical administration, localized bleeding in a patient, the composition comprising active PAI-1 protein in an amount effective to control the localized bleeding when topically administered, and a vehicle suitable for the topical administration, as well as methods and kits employing the same, are disclosed.

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.

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: Intermediates for the preparation of 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.

Abstract: This invention relates to substituted naphthofurans as anti-inflammatory and anti-allergic agents, pharmaceutical compositions containing them, processes for their preparation, and their use as anti-inflammatory and anti-allergic agents. The naphthofurans are of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 is CN or COOR.sup.9 ;R.sup.2 and R.sup.8 independently are H, C.sub.1 -C.sub.4 alkyl, COR.sup.9 or COR.sup.10 ;R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are independently H, C.sub.1 -C.sub.4 alkyl, halogen, phenyl, CF.sub.3 or OR.sup.9 ;R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, or COR.sup.9 ; andR.sup.9 and R.sup.10 are independently C.sub.1 -C.sub.4 alkyl, halogen or aryl.

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.

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.

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.

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.

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: 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.