Merck + Co., Inc.

Sandia Corporation

Daniel J Rush

C Jeffrey Brinker

Carol S Ashley

Kenneth J Shea

Michael J Kaufman

Darryl Y Sasaki

Cameron Cowden

Charles E Daitch

V Brett Cooper

Patricia Frech

There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo&lsqb;3,4-a&rsqb;phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.

Therapeutic polymorphs of a GABA-A alpha-5 inverse agonist and pamoate formulations of the same

Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline Anhydrous Form B, 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type A Monohydrate, and 3-Fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide polymorphic crystalline form Type B monohydrate, or a pharmaceutically acceptable salt thereof.

Pyrazinone thrombin inhibitors

A method is provided for molecularly imprinting the surface of a sol-gel material, by forming a solution comprised of a sol-gel material, a solvent, an imprinting molecule, and a functionalizing siloxane monomer of the form Si(OR).sub.3-n X.sub.n, wherein n is an integer between zero and three and X is a functional group capable of reacting with the imprinting molecule, evaporating the solvent, and removing the imprinting molecule to form the molecularly imprinted metal oxide sol-gel material. The use of metal oxide sol-gels allows the material porosity, pore size, density, surface area, hardness, electrostatic charge, polarity, optical density, and surface hydrophobicity to be tailored and be employed as sensors and in catalytic and separations operations.

Molecular receptors in metal oxide sol-gel materials prepared via

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Philadelphia, PA, United States of America

Daniel J Rush