Schering Corporation

Pharmacopeia Drug Discovery, Inc.

Pharmacopeia Inc.

Merck Sharp + Dohme Corp.

J Robert Merritt

John J Baldwin

Arthur G Taveras

Younong Yu

Jianhua Chao

Purakkattle J Biju

Ge Li

Cynthia J Aki

Michael P Dwyer

Jianping Chao

Gaifa Lai

Johan A Ferreira

Junying Zheng

Bernd Kaiser

Richard W Bond

Minglang Wu

Laura L Rokosz

Kingsley H Nelson, Jr

Evan A Hecker

Viyyoor Moopil Girijavallabhan

Daniel Lundell

Jay S Fine

James P Jakway

Kingsley H Nelson

Angelo Reggiani

James Jakway

There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

3,4-DI-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

3,4-di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and ischemia reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

Thiadiazoles as CXC- and CC- chemokine receptor ligands

Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.

Thiadiazoledioxides and thiadiazoleoxides as CXC- and CC-chemokine receptor ligands

Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

Isothiazole dioxides as CXC- and CC-chemokine receptor ligands

Thiadiazoles AS CXC- and CC- chemokine receptor ligands

3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

Disclosed are compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

3,4-di-substituted maleimide compounds as CXC chemokine receptor antagonists

3,4-di-substituted pyridazinediones as CXC chemokine receptor antagonists

Growing community of inventors

Ewing, NJ, United States of America

J Robert Merritt