Abstract: The present invention relates to a novel dibenzoxazepine derivative, its synthesis, and its use as an ?v integrin receptor antagonist. More particularly, the compound of the present invention is an antagonist of the integrin receptors ?v?3 and ?v?5 and therefor useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, artheroscietosis, inflammatory arthritis, cancer and metastatic tumor growth.

Abstract: The present invention relates to cyclic urea derivatives, their synthesis, and their use as ?v integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ?v?3 and/or ?v?5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.

Abstract: A process is provided for the preparation of 2,5-di-(3?-aminopropyl)pyridine which is useful in the synthesis of ?v?3 integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

Abstract: The present invention relates to a novel enantioselective bioreduction using a yeast microorganism for the preparation of the chiral allylic alcohols of structural formula I (R is hydrogen or methyl) which are useful in the asymmetric synthesis of integrin &agr;v&bgr;3 receptor antagonists.

Abstract: The tris(hydroxymethyl)aminomethane (“TRIS”) salt of 3-(pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid is a potent antagonist of the integrin &agr;v&bgr;3 receptor and is useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salt as well as pharmaceutical compositions containing the salt and methods of using the salt.

Abstract: A novel process is provided for the preparation of optionally protected 2,5-di-(3′-aminopropyl)-pyridines which are useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.

Abstract: The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonists

Abstract: Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents.

Abstract: The present invention relates to novel crystalline forms of the integrin &agr;v&bgr;3 antagonist 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid.

Abstract: The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.