Non-peptide NK1 receptors antagonists

The neurokinins are a family of mammalian neuropeptides that are involved with numerous biological activities such as pain transmission, vasodilation, smooth muscle contraction, bronchoconstriction, activation of the immune system, and neurogenic inflammation. One such neuropeptide known as substanc...

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Bibliographische Detailangaben
Hauptverfasser: Creswell, Mark Wallace, Higginbottom, Michael, Horwell, David Christopher, Lewthwaite, Russel Andrew, Pritchard, Martyn Clive, Raphy, Jennifer
Format: Patent
Sprache:eng
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Zusammenfassung:The neurokinins are a family of mammalian neuropeptides that are involved with numerous biological activities such as pain transmission, vasodilation, smooth muscle contraction, bronchoconstriction, activation of the immune system, and neurogenic inflammation. One such neuropeptide known as substance P is widely distributed throughout the peripheral and central nervous system of mammals, and is known to mediate a variety of biological actions via interaction with three neurokinin (NK or tachykinin) receptor types known as NK , NK , and NK . Non-peptide acetamide derivatives of Formula I are specific NKantagonist, where R is aryl, Rand Rare H or alkyl, m, n and q are integers from 0 to 4, X is NRor NHCONH, Rand Rare H or alkyl, Ris naphthyl or indolyl, Rand Rare H or alkyl, and Ris aryl.The compounds are useful agents for treating inflammatory and allergic disorders, pain, anxiety, depression, schizophrenia and emesis.