Abstract: Liposomal bupivacaine compositions are prepared using an ammonium sulfate gradient loading procedure, at a pH which prevents precipitation of the drug from the loading solution. Also described are liposome suspensions comprising ‘GMV’ (giant multivesicular) liposomes and methods for their preparation. The liposomal compositions are characterized by high drug-to-lipid ratios and provide long term analgesia.

Abstract: A temperature-stable droplet is provided containing a temperature-stable hydrocolloid membrane. The hydrocolloid membrane encapsulates a liquid that contains at least one enzyme, a cell, a biological agent, a pharmaceutical agent, an immunological agent, or mixtures thereof, and at least one of a locust bean gum, a natural thickening agent, a guar, polyvinylpyrrolidone, Konjac mannan, methylcellulose, hydroxymethylcellulose, calcium gluconate, glucomannan, or mixtures thereof. Preferably, the hydrocolloid membrane comprises at least one of methoxy pectin, Konjac mannan, sodium alginate, or mixtures thereof, and at least one of a locust bean gum, methylcellulose, hydroxymethylcellulose, glucomannan, or mixtures thereof. The hydrocolloid membrane encapsulating the liquid is a thickness capable of holding the liquid without bursting through a temperature range of about −20° C. to about 90° C.

Abstract: The design and the synthesis of backbone cyclic peptide analogs which functionally mimic the nuclear localization signal (NLS) region of macromolecules is disclosed. The principles of the invention are exemplified for the NLS sequences of the human immunodeficiency virus type 1 proteins MA, Vpr, Tat and NLS-like sequences of HIV-1 protein Vif. We disclose the discovery of a novel, highly potent backbone cyclic peptide, designated BCvir, which inhibits nuclear import with an IC50 value of 35 nM. This inhibitory potency is to be compared to 12 &mgr;M exhibited by the linear parent HIV-1 MA NLS peptide. BCvir also reduced HIV-1 production by 75% in infected non-dividing cultured human T-cells and was relatively resistant to tryptic digestion. These properties render backbone cyclic peptide analogs of NLS or NLS-like sequences as candidates for novel drugs based on blocking nuclear import of viral genomes.

Abstract: Pharmaceutical compositions are described for preventing TNF toxicity, comprising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of &Dgr;6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to elevated levels of TNF, including septic shock, cachexia and trauma. They are also effective in the treatment of certain chronic degenerative diseases characterized by TNF production, including autoimmune diseases such as AIDS.

Abstract: A method of-treating a relatively aged animal to reverse age-related changes in the lipid composition of organ and tissue cells, such as heart muscle cells, and the ability of the animal to withstand respiratory stress. A suspension of small unilamellar vesicles composed predominantly of egg phosphatidyl choline is administered parenterally to the animal, preferably over a period of several days and at a dose level of between about 0.1 and 1 grams lipid per kg body weight per day. Changes in the heart muscle cells are reflected in decreased levels of serum creatine phosphokinase. Liposome administration is continued until the serum creatine phosphokinase level drops at least about 50%. Also disclosed are liposome treatment methods for increasing longevity and male fertility.

Abstract: Pharmaceutical compositions are described for preventing TNF toxicity, comprising as active ingredient the stereospecific (+) enantiomer having 3S, 4S configuration of delta 6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to elevated levels of TNF, including septic shock, cachexia and trauma. They are also effective in the treatment of certain chronic degenerative diseases characterized by TNF production, including autoimmune diseases.

Abstract: The present invention discloses genetically engineered plants which display altered structure or morphology. The transgenic plants express a cell wall modulation transgene or gene construct that results in the altered structure or morphology. The altered structure or morphology can be associated with, for example, altered biomass, growth, yield, greater or less resistance to biodegradation, more or less digestible to ruminants, altered cellulose content, larger leaves/normal hypocotyls or smaller leaves/longer hypocotyls, etc. compared to a non-transgenic plant of the same species. The cell wall modulation transgene can be any cellulose binding domain, a cellulose binding protein, or a cell wall modifying protein or enzyme such as endoxyloglucan transferase, xyloglucan endo-transglycosylase, an expansin, cellulose synthase, or a novel isolated endo-1,4-&bgr;-glucanase of Arabidopsis thaliana.

Abstract: The present invention relates to a novel class of compounds for treating hyperlipidemia, obesity and impaired glucose tolerance/noninsulin dependent diabetes mellitus without adversely affecting energy metabolism, and pharmaceutical compositions comprising the aforementioned compounds for the treatment of obesity, hyperlipidemia and maturity-onset diabetes.

Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N&agr;(&ohgr;-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N&agr;(&ohgr;-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is specifically exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Abstract: The invention is embodied in a process for synthesizing a new image representing a new viewpoint of a scene from at least two existing images of the scene taken from different respective viewspoints. The process begins by choosing a planar surface visible in the at least two of the existing images and transforming the at least two existing images relative to one another so as to bring the planar surface into perspective alignment in the at least two existing images, and then choosing a reference frame and computing parallax vectors between the two images of the projection of common scene points on the reference frame. Preferably, the reference frame comprises an image plane of a first one of the existing images. Preferably, the reference frame is co-planar with the planar surface.

Abstract: Liposomal bupivacaine compositions are prepared using an ammonium sulfate gradient loading procedure, at a pH which prevents precipitation of the drug from the loading solution. Also described are liposome suspensions comprising `GMV` (giant multivesicular) liposomes and methods for their preparation. The liposomal compositions are characterized by high drug-to-lipid ratios and provide long term analgesia.

Abstract: The invention provides a temperature-stable liquid droplet comprising a terature-stable hydrocolloid membrane. The hydrocolloid is chosen from low methoxy pectin, Konjac mannan, sodium alginate, or a mixture thereof. The membrane encapsulates a droplet of an edible product or a droplet containing a microorganism, an enzyme or a cell.

Abstract: Pharmaceutical compositions are described for preventing TNF toxicity, comprising as active ingredient the stereospecific (+) enantiomer, having 3S, 4S) configuration of .DELTA..sup.6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to elevated levels of TNF, including septic shock, cachexia and trauma. They are also effective in the treatment of certain chronic degenerative diseases characterized by TNF production, including autoimmune diseases.

Abstract: The invention relates to a sustained-release pharmaceutical delivery system for the administration of an antioxidant drug to a patient in need of such drug, wherein said delivery system comprises said drug in combination with a polymeric matrix, said matrix comprising a polymer which does not interact with said drug or a mixture of such polymers. The pharmaceutical delivery system of the invention is useful for the treatment of pathological conditions involving pathologically increased formation of active oxygen species.

Abstract: The invention relates to synthetic phosphorothioated or partially phosphorothioated oligodeoxynucleotides capable of selectively modulating hemopoietic bone marrow cells development. More particularly, the invention relates to synthetic antisense oligodeoxynucleotides directed against a region spanning the AUG initiation condon in human ACHE or 2HS genes, having phosphorothioate bonds linking between the nucleotide bases; synthetic antisense oligodeoxynucleotides directed against a region spanning the AUG initiation condon in human ACHE gene, 2HS gene or BCHE gene or against a 5'-region in the human CHED (cdc2 homolog) gene, having phosphorothioate bonds linking between the four 3'-terminus nucleotide bases. The invention also relates to pharmaceutical compositions comprising as active ingredient at least one synthetic phosphorothioated or partially phosphorothioated antisense oligodeoxynucleotides according to the invention in physiologically acceptable carrier in diluent.

Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Abstract: A human cataractous lens nuclei methanolic extract characterized in that it comprises substances having a molecular weight lower than 3000 daltons, inhibiting ATP hydrolysis by Na.sup.+,K.sup.+ -ATPase having affinity to the ouabain binding site on the enzyme and cross-reacting with an antibody directed against digoxin. Compounds of the general formula are disclosed: ##STR1## or of the general formula: ##STR2## in which R is hydrogen, an amino acid, a di- or tripeptide or a mono-, di- or trisaccharide. Pharmaceutical preparations and methods of using the compounds are also disclosed.

Abstract: A method for preparing mimics of a wide variety of drugs and other biologlly active molecules using molecular imprinting techniques, and the mimics produced thereby, is disclosed. Specifically, the mimic is designed by: (i) polymerization of functional monomers around a known drug or biologically active molecule (the template) that exhibits a desired activity; (ii) removal of the template molecule; and then (iii) polymerization of a second class of monomers in the void left by the template, to provide a new organic molecule which exhibits one or more desired properties which are similar to that of the template.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLX-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.

Abstract: A cellulose binding domain (CBD) having a high affinity for crystalline cellulose and chitin is disclosed, along with methods for the molecular cloning and recombinant production thereof. Fusion products comprising the CBD and a second protein are likewise described. A wide range of applications are contemplated for both the CBD and the fusion products, including drug delivery, affinity separations, and diagnostic techniques.