Lumos Pharma, Inc.

Ilex Products, Inc.

Southwest Research Institute

Genzyme Corporation

Fgh Biotech, Inc.

Baylor College of Medicine

Tvardi Therapeutics, Inc.

William R Cantrell, Jr

William E Bauta

Dennis P Lovett

Jose Puente

Brian E Schulmeier

Michael Wade Tidwell

David John Tweardy

Brian D Burke

Michael Joseph Rubal

Robert D Gutierrez

Sofia De Achaval Wied

Methods for removing residual solvent from Nalmefene Hydrochloride (HCl) and producing crystalline Nalmefene HCl monohydrate, monosolvate or crystalline Nalmefene HCl dihydrate are described. In embodiments, the methods include recrystallizing Nalmefene HCl from a solvate that includes Nalmefene HCl, water, and a first solvent, wherein the first solvent has a molar volume of at least 98 cm. Crystalline Nalmefene HCl with a desirably low amount of residual solvent is also described.

Technologies for removing residual solvent from nalmefene hydrochloride and producing crystalline nalmefene hydrochloride monohydrate, monosolvate, or crystalline nalmefene hydrochloride dihydrate

Provided herein is a process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, using cynamide in the reaction. 

Synthesis of cyclocreatine and analogs thereof

Provided herein is a process and intermediates for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, using cyanamide in the reaction. 

The present invention relates to methods and strategies for large-scale synthesis of compounds having the chemical structure: The R substituents are H, methyl, isopropyl, benzyl, cyclohexyl, cyclopropylmethyl, methoxy, tert-butyloxycarbonyl, methanesulfonyl, p-toluenesulfonyl, quinolinesulfonyl, or thiophenesulfonyl groups. The method comprises condensing prothionamide with a halo nitroacetophenone to form a nitrophenyl substituted thiazole, reducing the nitro group to form an amine and derivatizing the amine to produce the compound.

Synthesis of fatostatin based polycyclic compounds

The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system (CNS) bioavailability and their associated methods of preparation including their use for treatment of exposure to AChE inhibitors such as an organophosphate (OP) insecticides and nerve agents.

Reactivators of organophosphorous inhibited acetylcholinesterase

The present invention for the stereoselective preparation of 2-deoxy-&#x3b2;-D-adenine nucleosides wherein a blocked 2-deoxy-&#x3b1;-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.

Process for preparing purine nucleosides

The present invention provides a process for the preparation of homophthlate esters useful in the preparation of homophthalic anhydride reactants.

Process for preparing homophthalate derivatives

The present invention provides for the preparation &bgr;-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy-&bgr;-D-adenine nucleosides wherein a blocked 2-deoxy-&agr;-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of &bgr; to &agr;-anomer is at least 99:1.

The present invention provides a process from preparing isocoumarin-3-yl derivatives comprising reacting a homophthalic anhydride derivative with a carbonyl compound, wherein the carbonyl group is substituted with an acyl activating group, in the presence of a reaction medium comprising a solvent and a base. The invention also encompasses a process for the preparation of homophthalate esters useful in the preparation of homophthalic anhydride reactants as well as an integrated process wherein the twp reactions are carried out sequentially to afford the desired isocoumarin derivative.

Growing community of inventors

San Antonio, TX, United States of America

William R Cantrell, Jr