Pfizer Corporation

Chris John Helal

Mark Allen Sanner

Frank S Menniti

Patricia A Seymour

Michael K Ahlijanian

Christoper B Cooper

Lit-Fui Lau

Chakrapani Subramanyam

Jotham Wadsworth Coe

Scot Richard Mente

Jennifer Elizabeth Davoren

Ivan Viktorovich Efremov

Steven Victor O'Neil

Amy Beth Dounay

David Lawrence Firman Gray

Jaclyn Louise Henderson

Christopher Blair Cooper

Anabella Villalobos

Annabella Villalobos

John Arthur Allen

Edward Raymond Guilmette

Anthony Richard Harris

Deane Milford Nason

Wenjian Xu

The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced &#x3b2;-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

Heteroaromatic compounds and their use as dopamine D1 ligands

The invention provides compounds of formula 1 wherein R, R, R, and Rare as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission. Also described are pharmaceutical compositions and methods comprising compounds of formula 1 for treating male fertility and sperm motility; diabetes mellitus; impaired glucose tolerance; metabolic syndrome or syndrome X; polycystic ovary syndrome; adipogenesis and obesity; myogenesis and frailty, for example age-related decline in physical performance; acute sarcopenia, for example muscle atrophy and/or cachexia associated with burns, bed rest, limb immobilization, or major thoracic, abdominal, and/or orthopedic surgery; sepsis; hair loss, hair thinning, and balding; and immunodeficiency.

Imidazole derivatives

Thiazole derivatives

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Mystic, CT, United States of America

Chris John Helal