- INDOLE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS
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Disclosed are novel compounds of the formula I wherein M1 is CH or N and M2 is C(R3) or N; R1 is optionally substituted indolyl or an aza derivative thereof; R2 is optionally substituted aryl or heteroaryl; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I in combination with a H1 receptor antagonist.
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- Phenylindole derivatives as 5-HT2A receptor antagonists
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3-(Piperidin-4-yl)-1H-indole derivatives bearing an optionally substituted phenyl moiety at the 2-position of the indole ring system and an alkyl or aryl-alkyl substituent on the nitrogen atom of the piperndine ring are selective antagonists of the human 5-HT2Areceptor. They are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including psychotic disorders such as schizophrenia.
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- 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT(2A) antagonists
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A series of 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT(2A) receptor. 3-(8-Phenethyl-8-aza-bicyclo[3.2.1]oct-3-yI)-2-phenyl-1H-indole is a high-affinity (1.2nM), selective (>800 fold over h5-HT(2C) and hD2 receptors) antagonist at the h5-HT(2A) receptor with oral bioavailability in rats. (C) 2000 Elsevier Science Ltd.
- Crawforth, James,Goodacre, Simon,Maxey, Robert,Bourrain, Sylvie,Patel, Smita,Marwood, Rosemarie,O'Connor, Desmond,Herbert, Richard,Hutson, Peter,Rowley, Michael
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p. 2701 - 2703
(2007/10/03)
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