Astrazeneca Ab

Jeffrey Albert

James Woods

Thomas Richard Simpson

Yan Li

James Kang

Cristobal Alhambra

Ashokkumar Bhikkappa Shenvi

Peter Robert Bernstein

Cyrus Ohnmacht

Keith Russell

Gerard Koether

Gerald M Koether

Compounds of Formula I wherein R, A, R, R, R, R, R, n, m, q and r are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Alkylsulphonamide quinolines

Compounds of Formula I wherein R, A, R, R, R, R, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Alkyl sulfoxide quinolines as NK-3 receptor ligands

Compounds of Formula II wherein R, A, R, R, R, R, R, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

The present application relates to internally cyclized naphthamide compounds of the formula Ia (wherein R, R, R, R, R, R, R, R, R, R, X, X, Y, Z, and n are as defined herein), which are useful, for example, for antagonizing the pharmacological actions of the neurokinin 1 (NK) receptor. In particular, these compounds are useful in the treatment of diseases in which Substance P is involved such as, for example, major depressive disorder, severe anxiety disorders, stress disorders, major depressive disorder with anxiety, eating disorders, bipolar disorder, substance use disorder, schizophrenic disorders, psychotic disorders, movement disorders, cognitive disorders, depression and/or anxiety, mania or hypomania, aggressive behaviour, obesity, rheumatoid arthritis, Alzheimer's disease, cancer, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, Huntington's disease, chronic obstructive pulmonary disorder (COPD), hypertension, migraine, bladder hypermotility, and urticaria.

Neurokinin antagonists for use as medicaments

Compounds having the general formulawherein R, R, R, R, R, R, R, R, R, R, X, X, Y, Z and n are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.

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Wilmington, DE, United States of America

Jeffrey Albert