Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders. Processes for preparing these inhibitors are also disclosed.

Abstract: A transdermal electrotransport drug delivery device having an anode, a cathode and a source of electrical power electrically connected to the anode and the cathode. At least one of the anode and the cathode includes an electrode and a reservoir comprised of a housing composed of a polymeric material and an aqueous medium in contact with the housing. The aqueous medium includes (i) a drug or an electrolyte salt or a mixture thereof, (ii) propylene glycol, and (iii) an antimicrobial agent in an amount sufficient to inhibit microbial growth in the aqueous medium. The propylene glycol prevents the antimicrobial agent from being adsorbed by other materials used in the construction of the delivery device. A process for preparing a transdermal electrotransport drug delivery device is also provided.

Abstract: Skin patches (20) having a microprojection array (10), a reservoir (18) containing an antigenic agent and an immune response augmenting adjuvant, and methods of using same to vaccinate animals (e.g., humans) is disclosed. In a preferred embodiment, the microprojection arrays (10) are composed of a photoetched and micro-punched titanium foil (14). The microprojections (12) are coated with a liquid formulation containing a vaccine antigen and an adjuvant such as glucosaminyl muramyl dipeptide, dried, and applied to skin of the animal to be vaccinated using an impact applicator. The microprojections (12) create superficial pathways through the stratum corneum to facilitate permeation of antigenic agent and adjuvant. Antigen dose and depth of penetration can be controlled. This technology has broad applicability for a wide variety of therapeutic vaccines to improve efficacy, and convenience of use.

Abstract: The device including a plurality of stratum corneum-piercing microprojections, and a solid coating disposed upon the microprojections, wherein the solid coating includes at least one beneficial agent and a biocompatible carrier is provided. The device is applied to the skin of a living animal (e.g., a human), causing the microprojections to pierce the stratum corneum and deliver an effective dose of the agent to the animal.

Abstract: A device (12) and method are provided for percutaneous transdermal delivery of a potent pharmacologically active agent. The agent is dissolved in water to form an aqueous coating solution having an appropriate viscosity for coating extremely tiny skin piercing elements (10). The coating solution is applied to the skin piercing elements (10) using known coating techniques and then dried. The device (12) is applied to the skin of a living animal (e.g., a human), causing the microprotrusions (10) to pierce the stratum corneum and deliver a therapeutically effect dose of the agent to the animal.

Abstract: An electrotransport device for delivering or sampling an agent through a body surface by electrotransport, the device having a housing including an upper, exterior housing portion and a lower housing portion, the housing enclosing electronic components, and at least one hydratable or hydrated reservoir containing water or an at least partially aqueous solution of the agent. At least a portion of the housing is composed of an ethylene-octene copolymer.

Abstract: The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.