Abstract: The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R1, R2, R3, R4 and R5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.

Abstract: The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R1, R2, R3, R4 and R5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.

Abstract: A method of generating a compound having at least one biological activity of a peptide. The method includes identifying a biologically active peptide, providing a first monomer which contains terminal reactive moieties and at least one functionalizable group, providing a second monomer which contains terminal reactive moieties and at least one functionalizable group, and reacting first and second monomer under stereo-and/or regiochemically controlled conditions to yield a compound in which the monomers are attached by way of terminal reactive moieties.

Abstract: Chemokine receptor antagonists, in particular, bicyclic diamine compounds of Formula (I) that act as antagonists of chemokine CCR2 and CCR3 receptors including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leucocyte accumulation are described herein.

Abstract: Chemokine receptor antagonists, in particular, bicyclic diamine compounds of Formula (I) that act as antagonists of chemokine CCR2 and CCR3 receptors including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leucocyte accumulation are described herein.

Abstract: The present invention provides a system for the production of chemical compounds and libraries of compounds that are complex, stereochemically and regioselectively pure, and may mimic the structural or functional properties of a peptide. The invention provides methods for producing collections of peptidomimetic compounds which, in one preferred embodiment, comprises (1) providing two diversifiable monomers containing terminal reactive moieties; (2) reacting the monomers under conditions that allow for the control of stereochemistry as well as chemoselectivity; and (3) generating diversifiable isolable compounds or libraries of compounds.