An adhesive composition is provided that contains both a hydrophobic phase and a hydrophilic phase, wherin the hydrophobic phase is composed of a crosslinked hydrophobic polymer composition and the hydrophilic phase is a water-absorbent blend of a hydrophilic polymer and a complementary oligomer capable of crosslinking the hydrophilic polymer through hydrogen bonding, ionic bonding, and/or covalent bonding. The composition is useful as a bioadhesive, for affixing drug delivery systems, wound dressings, bandages, cushions, or the like to a body surface such as skin or mucosal tissue.

Two-phase, water-absorbent bioadhesive composition

A method for preparing hydrophilic pressure sensitive adhesive (PSA) compositions is provided, wherein the method enables preparation of adhesives having a particular, optimized degree of adhesion. That is, the hydrophilic PSA is comprised of a hydrophilic polymer and a complementary short-chain plasticizing agent, wherein the hydrophilic polymer and plasticizing agent are capable of hydrogen bonding or electrostatic bonding to each other and are present in a ratio that optimizes key characteristics of the adhesive composition, such as adhesive strength, cohesive strength and hydrophilicity. The adhesive is useful in a wide variety of contexts, e.g., as a biomedical adhesive for application to the skin or other body surface, and as such finds utility in the areas of drug delivery systems (e.g., topical, transdermal, transmucosal, iontophoretic), medical skin coverings and wound healing products and biomedical electrodes.

Preparation of hydrophilic pressure sensitive adhesives having optimized adhesive properties

Provided is a simple and efficient method for the large-scale production of a 4,4-difluoro-3,4-dihydroisoquinoline derivative. In the method for producing a 4,4-difluoro-3,4-dihydroisoquinoline derivative represented by general formula (1):
 
a compound represented by general formula (2):
 
is reacted with hydrogen fluoride.

Production method for 4, 4-difluoro-3,4-dihydroisoquinoline derivative

Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.

Novel jnk inhibitors

A composition is provided, wherein the composition comprises a water-swellable, water-insoluble polymer, a blend of a hydrophilic polymer and a complementary oligomer capable of hydrogen bonding to the hydrophilic polymer, and a whitening agent, preferably a peroxide. The composition finds utility as a tooth whitening composition and is applied to the teeth in need of whitening, and then removed when the degree of whitening has been achieved. In certain embodiments, the composition is translucent. Methods for preparing and using the compositions are also disclosed.

Hydrogel compositions for tooth whitening

A short route to the total synthesis of the core skeleton of the taxol ring system is described The same sequence of transformations can be carried out to make the 7-hydroxy series, and connect the additional carbon atoms required for the A-ring The number of steps to the taxane skeleton is 13, making it the shortest route from readily available inexpensive starting materials

Short synthetic route to taxol and taxol derivatives

The present invention provides a novel process for the conversion of α,β-unsaturated ketones. This invention is an improvement over existing processes in that it operates at neutral reaction conditions that prevent the formation of side reactions and that it is a single step, which proceeds with complete selectivity and gives a yield that is approximately 30% higher than the currently used processes. An example of this process is the conversion of 16-dehydroprogesterone into 17 α-hydroxyprogesterone.

Conversion of alpha,beta-unsaturated ketones and alpha,beta-unsaturated esters into alpha-hydroxy ketones and alpha-hydroxy esters using Mn(III) catalyst, phenylsilane and dioxygen

A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.

Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin

The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof, wherein the starting compound is biphenyl.

Synthesis of morphine and related derivatives

The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.

Philip D. Magnus

Papers

Short synthetic route to taxol and taxol derivatives

Conversion of alpha,beta-unsaturated ketones and alpha,beta-unsaturated esters into alpha-hydroxy ketones and alpha-hydroxy esters using Mn(III) catalyst, phenylsilane and dioxygen

Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin

Synthesis of morphine and related derivatives

Synthesis of navelbine analogs