Abstract: The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.

Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: A composition for administration of a therapeutically effective dose of a topoisomerase inhibitor I or topoisomerase I/II inhibitor is described. The composition includes liposomes having an outer surface and an inner surface defining an aqueous liposome compartment, and being composed of a vesicle-forming lipid and of a vesicle-forming lipid derivatized with a hydrophilic polymer to form a coating of hydrophilic polymer chains on both the inner and outer surfaces of the liposomes. Entrapped in the liposomes is the topoisomerase inhibitor at a concentration of at least about 0.10 &mgr;mole drug per &mgr;mole lipid.

Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

Abstract: The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer.

Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

Abstract: Compound of formula (I): 1

Abstract: The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as Human Immunodeficiency Virus. In addition, these compounds are anti-neoplastic agents useful in the treatment of various forms of cancer. wherein R1 and R2 are independently —H, —OH, amino, alkylamino, dialkylamino, alkoxy, alkyl, haloalkyl or halogen; n is 2 to 6, X and X′ are independently —N or —NO2; Y and Y′ are independently —N or —CH, or —H; and the double-slash represents a double bond or no bond.

Abstract: A method for controlling cholesterol metabolism in a host, a screening assay for agents that can control cholesterol metabolism, and the agents that may be identified are practiced and determined in relation to the expression of PLTP in HepG2 cells and a clone from these cells, designated HepG2/PLTPpLuc. Particular agents that are covered comprise camptothecin, topotecan, derivatives thereof, metabolic byproducts thereof and small molecule mimics thereof.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.

Abstract: A process for the preparation of a compound of the formula 1

Abstract: An injectable pharmaceutical composition comprising: an aqueous suspension of microdroplets suitable for intravenous delivery, the microdroplets having a mean diameter between 200 Angstroms and one micron, the microdroplets comprising a substantially water-insoluble, pharmacologically acceptable liquid, a camptothecin dissolved in the water-insoluble, pharmacologically acceptable liquid, and an outer layer comprising a phospholipid. The pharmaceutical composition is particularly well suited for delivering camptothecins, particularly 9-nitro-camptothecin intravenously.

Abstract: A composition for administration of a therapeutically effective dose of a topoisomerase inhibitor I or topoisomerase I/II inhibitor is described. The composition includes liposomes having an outer surface and an inner surface defining an aqueous liposome compartment, and being composed of a vesicle-forming lipid and of a vesicle-forming lipid derivatized with a hydrophilic polymer to form a coating of hydrophilic polymer chains on both the inner and outer surfaces of the liposomes. Entrapped in the liposomes is the topoisomerase inhibitor at a concentration of at least about 0.10 &mgr;mole drug per &mgr;mole lipid.

Abstract: A method for administering a camptothecin to a patient comprising: injecting into a patient a pharmaceutical composition comprising an aqueous suspension of microdroplets suitable for intravenous delivery, the microdroplets having a mean diameter between 200 Angstroms and one micron, the microdroplets comprising a substantially water-insoluble, pharmacologically acceptable liquid, a camptothecin dissolved in the water-insoluble, pharmacologically acceptable liquid, and an outer layer comprising a phospholipid. The pharmaceutical composition is particularly well suited for delivering camptothecins, particularly 9-nitro-camptothecin intravenously.

Abstract: A pharmaceutical composition is provided which comprises an aqueous suspension of solid particles, the solid particles comprising a camptothecin, the solid particles having mean diameters between about 0.05 um and 10 um, the particles coated with a 0.3 nm to 3.0 um thick layer of a membrane-forming amphipathic lipid. The pharmaceutical composition is particularly well suited for delivering camptothecins, particularly 9-nitro-camptothecin intravenously.

Abstract: Compounds of the formula 1

Abstract: The invention provides pharmaceutical compositions containing PARP inhibitors and methods of using these compositions to prevent, treat or ameliorate glaucomatous retinopathy and/or optic neuropathy.

Abstract: Compounds of the formula 1

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.

Abstract: Compound of formula (I): 1

Abstract: The invention is in the field of cancer treatment. In particular, the present invention provides pharmaceutical compounds capable of interacting with mutant and non-mutant forms of cancer-related regulatory proteins such that the mutant protein regains the capacitv to properly interact with other macromolecules thereby restoring or stabilizing all or a portion of its wild type activity. Regulatory proteins include members of the p53 protein family such as. for example, p53, p63 and p73. The compounds of the invention are useful for cancer treatment. Methods for screening for such pharmacological compounds are also provided.

Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

Abstract: The invention provides a compound of formula I 1

Abstract: The invention relates to heterocyclic derivatives of the formula (I): A—B—X1—T1(R2)—L1—T2(R3)—X2—Q or pharmaceutically acceptable salts thereof, which possess antithrombotic and anticoagulant properties due to their inhibition of Factor Xa and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

Abstract: The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as Human Immunodeficiency Virus. In addition, these compounds are anti-neoplastic agents useful in the treatment of various forms of cancer.

Abstract: The invention provides compounds of formula I wherein R1 to R6 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.

Abstract: Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

Abstract: The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as Human Immunodeficiency Virus. In addition, these compounds are anti-neoplastic agents useful in the treatment of various forms of cancer. wherein R1 and R2 are independently —H, —OH, amino, alkylamino, dialkylamino, alkoxy, alkyl, haloalkyl or halogen; n is 2 to 6, X and X′ are independently —N or —NO2; Y and Y′ are independently —N or —CH, or —H; and the double-slash represents a double bond or no bond.