79779-59-2Relevant articles and documents
N-Substituted 11-(4-piperidylene)-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2 -b]pyridines. Antihistamines with no sedating liability
Villani,Magatti,Vashi,Wong,Popper
, p. 1311 - 1314 (2007/10/02)
Conversion of the basic tertiary amino function of the potent antihistamine, azatadine (Optimine), to neutral carbamate function results in compounds which retain significant antihistamine activity with little or no CNS effects. In guinea pigs the N-ethoxycarbonyl derivative 4 had the same antihistamine potency as terfenadine, a clinically used non-sedating antihistamine. In mice, 4 was a potent antihistamine while lacking CNS effects. The 8-chloro-N-ethoxycarbonyl 5 (loratadine, Sch 29851) was the most potent antihistamine in the series, had no CNS side effects, and was selected for clinical evaluation.
Tricyclic-substituted piperidine antihistamines
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, (2008/06/13)
Antihistamines of the formula STR1 wherein STR2 is a 5 or 6 membered ring which is phenyl or heterocyclic; STR3 is a six membered ring which is 2,3 or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is STR4 is a nitrogen containing ring, STR5 must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is STR6 wherein p is 1 or 2 and n is 1 or 2, R1 is C1 to C6 alkyl, R2 is hydrogen or C1 to C6 alkyl, and the dotted line represents an optical double bond, R2 being absent if the double bond is present, and Y is substituted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.
ANTIHISTAMINIC 11-(4-PIPERIDYLIDENE)-5H-BENZO-[5,6]-CYCLOHEPTA-[1,2-B]-PYRIDINES
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, (2008/06/13)
11-(4-Piperidylidene)-5H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridines and their 5,6-dihydro derivatives are disclosed. The compounds are useful as antihistamines with little or no sedative effects.
