Abstract: Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.

Abstract: Certain naphthyridine compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.

Abstract: Certain tetrahydroisoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.

Abstract: This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50s of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metalloproteinases (ADAMs or reprolysins).

Abstract: A compound of the formula wherein R1, R2 R3, R4, R5, R6 and Q are as defined above, useful in the treatment of arthritis, cancer, and other diseases involving the dysregulated production/release of reprolysins such as TNF and other diseases characterized by matrix metalloproteinase activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID's), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.

Abstract: The present invention relates to novel triazolo-pyridines of the formula wherein X is >CH2, >NH, sulfur, >S?O, >SO2 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; s is an integer from 0-4; R3 is R4, R5—(NR6)—, R5—S—, R5—(S?O)—, R5—(SO2)—, R5—SO2—NR6—, R5—(NR6)—SO2—, R5—O—, R5—(C?O)—, R5—(NR6)—(C?O)—, R5—(C?O)—NR6—, R5—O—(C?O)—, R5—(C?O)—O—, R5—CR7?CR8— or R5—C?C_; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use.

Abstract: This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial agents that may be used to treat various bacterial infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.