Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.

Abstract: The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

Abstract: Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: 1

Abstract: The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

Abstract: The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: The present invention is directed to compounds of formula (I), 1

Abstract: The invention concerns novel azole or triazole derivatives of formula (Ia) or (Ib), wherein: X, Ar1, Ar2, Ar3, A, B and R1 are such as defined in the description, the method for preparing same and their use as fungicides.

Abstract: Therapeutic compounds and methods for modulating amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is modulated by the administration to a subject of an effective amount of a therapeutic compound comprising a phosphonate group and a carboxylate group, a congener thereof, or a pharmaceutically acceptable salt or ester thereof. In preferred embodiments, an interaction between an amyloidogenic protein and a basement membrane constituent is modulated.

Abstract: This invention features compounds having formula (I): 1

Abstract: A topical composition and the method using the composition, which contains an antifungal agent and a low potency anti-inflammatory steroid which is safe and effective such as desonide or its derivative. The low potency steroid agent does not cause side effects such as skin atrophy, striae and hypopigmentation.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: Methods and compositions employing as active ingredient hepoxilins and hepoxilin analog useful for inhibiting thromboxane formation and antagonising thrombbxane activity. Methods and compositions employing these compounds provide treatment for a number of disease conditions.

Abstract: The present application describes novel spiro-cyclic &bgr;-amino acid derivatives of formula I: 1

Abstract: The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.

Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.

Abstract: The present invention relates to therapeutically active novel spiro[2,4]heptane amino carboxy compounds and derivatives thereof. Also provided is a method of preparing compounds of Formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: The present application describes novel &bgr;-amino acid derivatives of formula I: 1

Abstract: The present invention relates to novel naphthalene derivatives of formula (I), wherein R1, R2, R3 and X are as defined in the description, and preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.

Abstract: This invention concerns the use of compounds of formula 1

Abstract: This invention relates to compounds of the Formula (I): 1

Abstract: A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): 1

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1

Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: This invention relates to compounds of the general formula: 1

Abstract: This invention relates to purine compounds of formula (I): 1

Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.

Abstract: The invention relates to novel 3, 5, and/or 6 swainsoninc analogues, processes for their preparation and their use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.

Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: The invention relates to new &agr;-arylethylpiperazine derivatives, which are useful as neurokinin receptor antagonists (NK1antagonists). It also relates to processes for the preparation of said &agr;-arylethylpiperazine derivatives, to their use for the prevention and/or treatment of a condition associated with pathogical levels of substance P in a patient and to pharmaceutical compositions containing them.

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: The present invention relates to compounds of formula (I) wherein R1 and R2 are independently selected from C1-6alkyl; one of R4 and R5 is a group of formula (IA): R3, R6, R7, R8, R9, R10 and R11 and the other of R4 and R5 are as defined within, pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and there use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.

Abstract: Novel alkenylphosphonic acid esters of the following general formula (I):

Abstract: The present invention refers to synthetic protease inhibitors having an axis of symmetry C2 or pseudo-C2 characterised by possessing, in the central portion: (1) preferably, a dihydroxyethylene function, which is isosteric with a peptidic bond; (2) a peptidemimetic bridge between the two nitrogens of the main chain and (3) radicals capable of mimetising amino acids. These new protease inhibitors are a base for the preparation of anti-viral formulations capable of inhibiting HIV virus proliferation.

Abstract: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: wherein Y is a radical of Formulae II or III: in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

Abstract: Novel phospholipid derivatives of the General Formula I: 1

Abstract: Novel cyclo azaphospha hydrocarbons according to formula I are provided. The compounds are useful as metalloprotease inhibitors.

Abstract: A method or composition is disclosed for the treatment of disorders associated with apoptosis using N-heterocyclic glyoxylamide compounds.

Abstract: The invention relates to the use of organophosphorus compounds of the general formula (I) 1

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.