Bristol-myers Squibb Compnay

Huan He

Yong-Jin Wu

Alexandre L'Heureux

Li-Qiang Sun

Jie Chen

Piyasena Hewawasam

Joanne J Bronson

Gene G Kinney

Pierre Dextraze

Jean-Paul Daris

Steven Dworetzky

Li-Quang Sun

The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Cycloalkylamine derivatives as NK-1/SSRI antagonists

The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Cyclopentylamine and cyclohexylamine derivatives as NK-1/SSRI antagonists

The present disclosure relates to chemical compounds and their use in treatment of human diseases. A particular embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salts or solvates thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Arylpyrrolidine derivatives as NK-1 /SSRI antagonists

The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R, R, R, R, R, R, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

3-Heterocyclic benzylamide derivatives as potassium channel openers

The present disclosure relates to chemical compounds and their use in human therapy. In a specific embodiment, compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Homopiperidine derivatives as NK-1 antagonists

The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I wherein R, R, R, R, R, R, Rand A are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said aryl hydroxyethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

1-aryl-2-hydroxyethyl amides as potassium channel openers

The present invention provides novel heterocyclic amides and related derivatives having the general Formula Iwherein R, R, R, R, R, R, A, B and Z are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said heterocyclic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

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Wallingford, CT, United States of America

Huan He