Abstract: The present invention describes novel thiazolo[4,5-d]pyrimidines of formula: ##STR1## wherein R.sup.3 is a substituted aromatic or heteroaromatic group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.

Abstract: A high integrity liposome comprising at least one stabile lipid and at least one peptide-like therapeutic agent associated with said liposome, adapted for parenteral administration to an animal, including a human, and method according to manufacture and use. Immunizing dosage forms comprising a liposome and an immunogen, wherein said liposome and immunogen are present in an immunization dose. Additionally, a dosage form, including such form particularly adapted to producing an immune response, comprising a salt according to an organic acid derivative of a sterol and an immunogen wherein said organic acid derivative of a sterol and immunogen are present in an immunization dose, and method according to use is disclosed.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders are disclosed.

Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or II: ##STR1## and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.

Abstract: This invention relates to a method of prevention and/or treatment of thrombosis in a mammal without significantly altering bleeding time or coagulation. This invention further relates to methods of using selective inhibitors of the binding of vitronectin to the .alpha..sub.v .beta..sub.3 receptor, alone or in combination with other therapeutic agents, for the inhibition of thrombus formation and/or the treatment of thromboembolic disorders.

Abstract: Endotoxin incorporated into liposomes, lipid bilayers or lipid complexes can be detected by combining an aqueous suspension of the liposomes, lipid complexes or lipid bilayers with a suitable detergent. Preferable detergents, e.g., Lubrol-PX.TM. or a polyoxyethylene ether, solubilize the lipid bilayers, liposomes or lipid complexes at acceptable lipid concentrations, forming micelles therefrom which contain lipid bilayer, liposome or lipid complex lipid, detergent and endotoxin, should it be present. The micelles are then assayed for the presence of endotoxin.

Abstract: The present invention describes a method for the preparation of asymmetric N,N'-disubstituted cyclic ureas through the selective monodebenzylation of symmetric N,N'-disubstituted cyclic ureas using a dissolving metal reduction. The intermediates can be alkylated to give compounds which are useful as HIV protease inhibitors for the treatment of HIV infection.

Abstract: Tangential flow filtration is used in the size separation of particles, such as liposomes and lipid particles. These particles may be passed through a tangential flow filtration device of any pore size desired. Tangential flow filter systems of various pore sizes may be used sequentially to obtain particles such as lipid particles or liposomes having a defined size range.

Abstract: This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyl-S-, C.sub.1 -C.sub.6 alkyl-SO--, C.sub.1 -C.sub.6 alkyl-SO.sub.2 --, cyclopropyl, phenyl, --NH.sub.2, --NH(CH.sub.3), --NHC(.dbd.O)CH.sub.3, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2 or --CH.sub.2 C(.dbd.O)CF.sub.3 ; Ar.sup.1 and Ar.sup.2 are independently phenyl, halophenyl or thienyl; X is NH, O or S; and Y is hydrogen, --COOR.sup.3 or --CONR.sup.4 R.sup.5, wherein R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.6 alkyl.

Abstract: This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

Abstract: Pharmaceutical compositions are provided herein that contain, in addition to a pharmaceutically acceptable carrier, a lamellar lipid. The lipid is composed of an ether lipid and a lipid having a molecular shape that is complementary to the molecular shape of the glycerolipid. These compositions can be used therapeutically, for example, in the treatment of cancers and inflammatory conditions.

Abstract: Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration.

Abstract: Disclosed is a vaccine against an infective agent, the vaccine comprising a liposome having an exterior and an interior and having externally disposed affinity associated antigen material of at least one, preferably nonpartitioning, antigen representative of said infective agent. Also disclosed is a method of preparation and use of this vaccine.

Abstract: This invention provides an interdigitation-fusion liposome comprising an arachidonic acid metabolite, a lipid bilayer comprising a lipid and an aqueous compartment comprising a release-inhibiting buffer. Preferred arachidonic acid metabolites are the prostaglandins, particularly PGE.sub.1. The liposomal formulations can be used to treat animals, particularly humans, for diseases, disorders or conditions which can be ameliorated by prostaglandins, e.g., cell activation/adhesion disorders and inflammatory disorders.

Abstract: A composition comprises a free arachidonic acid metabolite and endocystosable particles such as phagocytosable or opsonizable particles, or particles binding to phagocytic receptors to serum proteins, and the like. The composition, in the form of a therapeutic formulation may be administered alone, or with other bioactive agents, for the treatment of a disorder characterized by cell activation/adhesion, inflammation or toxemia. A second method of treating such disorders comprises the administration of an endocytosable particle.

Abstract: Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration.

Abstract: This invention provides a composition containing a sized liposome comprising a lipid and an induce; the sized liposome has a diameter of at most about 1 micoron and the induces is present in an amount effective to induce interdigitation-fusion of the sized liposome. Also provided herein are interdigitation-fusion liposomes and gels, and methods of making the same.

Abstract: This invention provides a method of administering an arachidonic acid metabolite, such as prostaglandin E1, to an animal. The metabolite is given to the animal, typically a human, in association with a unilamellar liposome comprising a lipid and a release-inhibiting aqueous buffer. This method can be used to treat animals afflicted with disorders characterized by cell activation and adhesion, inflammation or toxemia.

Abstract: A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a tranamembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problem related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.