Schering Corporation

Other

Merck Sharp + Dohme Corp.

Shuyi Zhang

Xiaoyong Fu

Timothy L McAllister

Jianguo Yin

Agnes S Kim-Meade

Jason L Winters

Anantha R Sudhakar

Doris P Schumacher

Arthur G Taveras

Michael P Dwyer

Younong Yu

Kevin Joseph Klopfer

Michael R Reeder

Kelvin Yong

Kenneth Stanley Matthews

Mengwei Hu

Mathew Thomas Maust

Gerald Werne

Frank Bruno Guenter

Timothy D Cutarelli

Jin Wang

Yianguo Yin

Timothy L Macallister

Timothy Mcallister

This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.

Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds

The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure:  These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.

Crystalline polymorphs of a CXC-chemokine receptor ligand

This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.

Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives

Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C-C)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.

Synthesis of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide

Synthesis of 2-hydroxy-n,n-dimethyl-3-[[2-[[1(r)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide

A sustained release formulation as a unit dose contains 100 mg-1000 mg of Acetaminophen and 15 mg-150 mg of tramadol hydrochloride, which comprises of 1) an immediate release portion comprising of 25%-75% of the total effective amount of drug in the dosage form and 2) a sustained release portion comprising of a) 25%-75% of the total effective amount of drugs in the dosage form; b) 6%-50% of gelling polymers of the total formulation, and c) optionally an enteric coating at a level of 5%-40% of the total formulation. The set forth formulation dissolves 25%-60% of the total drug in the first hour, 50%-90% of the total drug in the first four hours and not less than 80% of the total drug in the first 12 hours using USP dissolution method II at 50 rpm.

Sustained release formulations containing acetaminophen and tramadol

Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C&#x2013;C)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.

Synthesis of 2-hydroxy-N,N-dimethyl-3-[ [2-[1 (R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]aminobenzamide

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Parsippany, NJ, United States of America

Shuyi Zhang