Patent classifications
A61P31/08
Intermediates useful in the synthesis of compounds as modulators of protein kinases
The present invention provides compounds of formula (10), formula (12), formula (14) and formula (15) ##STR00001## wherein R, R.sup.1, R.sup.2, Cy.sup.1 and X are as described herein.
PSGL-1 MODULATORS AND USES THEREOF
The present invention relates to the seminal discovery that P-selectin glycoprotein ligand-1 (PSGL-1) modulates the immune system and immune responses. Specifically, the present invention provides PSGL-1 agonists and antagonists which increase the survival of multifunctional T cells and viral clearance. The present invention further provides methods of treating infectious diseases, cancer and immune and inflammatory diseases and disorders using a PSGL-1 modulator.
Oral pharmaceutical dispersion compositions
The invention provides an oral pharmaceutical composition, optionally in dose unit form, comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic.
HETEROCYCLIC AMIDES USEFUL AS PROTEIN MODULATORS
Disclosed are compounds having the formula:
##STR00001## wherein q, r, s, A, B, C, R.sup.A1, R.sup.A2, R.sup.B1, R.sup.B2, R.sup.C1, R.sup.C2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.14, R.sup.15, R.sup.16, and R.sup.17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
Heterocyclic amides useful as protein modulators
Disclosed are compounds having the formula: ##STR00001## wherein q, r, s, A, B, C, R.sup.A1, R.sup.A2, R.sup.B1, R.sup.B2, R.sup.C1, R.sup.C2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.14, R.sup.15, R.sup.16, and R.sup.17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
Boron-Containing Small Molecules
This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
Compositions of, and methods for, alpha-1 anti trypsin Fc fusion molecules
A novel method of treating and preventing bacterial diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of Gram negative, Gram positive and acid fast bacilli in general and tuberculosis (TB), Mycobacterium avium complex (MAC), and anthrax in particular. Thus, the invention relates to modulation of cellular activities, including macrophage activity, and the like. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made inhibitors of serine protease.
VACCINE COMPOSITION CONTAINING SYNTHETIC ADJUVANT
Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.
METHODS OF USING A VACCINE COMPOSITION CONTAINING SYNTHETIC ADJUVANT
Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glycopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.
Lipopeptide- and lipoprotein-conjugates and its use
The present invention relates to new lipopeptide- and lipoprotein molecules and lipopeptide- and lipoprotein-conjugates. In particular, the present invention relates to new lipopeptide- and lipoprotein molecules and lipopeptide- and lipoprotein-conjugates comprising a lipid-containing moiety representing an adjuvant moiety, a peptide or protein moiety whereby said peptide or protein moiety represents at least one antigenic structure, the antigen-moiety, and, optionally, a conjugate moiety, preferably a monodisperse polyethyleneglycol unit. Said compounds are particularly useful for therapeutic or prophylactic vaccination by mucosal or systemic administration, preferably mucosal and systemic vaccination. That is, the present invention relates in another aspect to pharmaceutical compositions comprising the compounds according to the present invention, in particular, said pharmaceutical compositions are vaccines. In addition, said pharmaceutical compositions are useful for the prophylaxis or treatment of infectious diseases, inflammatory and autoimmune diseases, cancer, allergies or for the control of fertility in human or animal populations.