Abstract: The present invention is an efficient synthetic route to 2?,3?-dideoxy-2?,3?-didehydro-nucleosides from available precursors with the option of introducing functionality as needed, such as, the 2?,3?-dideoxy and 2?- or 3?-deoxyribo-nucleoside analogs as well as additional derivatives obtained by subsequent functional group manipulations. Briefly, the present invention discloses a method for the preparation of ?-D and ?-L-2?,3?-dideoxy-2?,3?-didehydro-nucleosides starting from appropriately substituted ribonucleosides in two, optionally three steps: Step (1) a haloacylation, such as haloacetylation, and in particular, bromoacetylation; Step (2) a reductive elimination; and optionally, Step (3) a deprotection. The haloacylation of step (1) can form the 2?-acyl-3?-halonucleoside, the 3?-acyl-2?-halonucleoside, or a mixture thereof.

Abstract: An efficient synthetic route to antiviral 2?,3?-dideoxy-2?,3?-didehydro-nucleosides, such as 2?,3?-dideoxy and 2?- or 3?-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of ?-D and ?-L-2?,3?-dideoxy-2?,3?-didehydro-nucleosides is described that includes: activating a compound of structure (1) wherein B is a pyrimidine or purine base and Y is O, S or CH2 with an acyl halide of the formula X—C(?O)R1, X—C(?O)C(R1)2OC(?O)R1 or X—C(?O)OR1 (wherein X is a halogen, and each R1 is independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2?,3?-dideoxy-2?,3?-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2?-acyl-3?-halonucleoside, the 3?-acyl-2?-halonucleoside, or a mixture thereof.

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: 1

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: from its corresponding 3-cyano-4-fluorophenyl-pyrazole and intermediates useful therein.

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: from its corresponding 3-cyano-4-fluorophenyl-pyrazole and intermediates useful therein.

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: 1

Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

Abstract: The present invention is an efficient synthetic route to 2′,3′-dideoxy-2′,3 ′-didehydro-nucleosides from available precursors with the option of introducing functionality as needed, such as, the 2′,3′-dideoxy and 2′- or 3′-deoxyribo-nucleoside analogs as well as additional derivatives obtained by subsequent functional group manipulations. Briefly, the present invention discloses a method for the preparation of &bgr;-D and &bgr;-L-2′,3′-dideoxy-2′,3′-didehydro-nucleosides starting from appropriately substituted ribonucleosides in two, optionally three steps: Step (1) a haloacylation, such as haloacetylation, and in particular, bromoacetylation; Step (2) a reductive elimination; and optionally, Step (3) a deprotection. The haloacylation of step (1) can form the 2′-acyl-3′-halonucleoside, the 3′-acyl-2′-halonucleoside, or a mixture thereof.

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: 1

Abstract: The present invention relates to processes for the preparation of macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

Abstract: The present invention relates generally to cyclic carbamates and isoxazolidines or Formula (I) or their pharmaceutically acceptable salts thereof, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: This invention relates to 1,3,4-thiadiazoles and 1,3,4-Oxadiazoles of Formula (I) which are useful as antagonists of .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion and the tretment of angioginic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions.