55580-00-2Relevant academic research and scientific papers
Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza- benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists
Rueeger, Heinrich,Gerspacher, Marc,Buehlmayer, Peter,Rigollier, Pascal,Yamaguchi, Yasuchika,Schmidlin, Tibur,Whitebread, Steven,Nuesslein-Hildesheim, Barbara,Nick, Hanspeter,Cricione, Leoluca
, p. 2451 - 2457 (2007/10/03)
Combination of structural elements from a potent Y5 antagonist (2) with thiazole fragments that exhibit weak Y5 affinities followed by lead optimisation led to the discovery of (5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen-2-yl)- piperidin-4-ylmethyl-amino and (4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen-2- yl)-piperidin-4-ylmethyl-amino derivatives. Both classes of compounds are capable of delivering potent and selective orally and centrally bioavailable NPY Y5 receptor antagonists.
Conformationally Restricted Tetrahydro-1-benzoxepin Analogs of Hallucinogenic Phenethylamines
Monte, Aaron P.,Marona-Lewicka, Danuta,Cozzi, Nicholas V.,Nelson, David L.,Nichols, David E.
, p. 651 - 663 (2007/10/03)
Tetrahydro-1-benzoxepin analogs of prototypical 4-substituted-2,5-dimethoxyphenylisopropylamines were prepared as agents having restricted conformational mobility in the 2-alkoxy group and alkylamine sidechain. The derivatives were evaluated for their abi
Substituted tetralins, chromans and related compounds in the treatment of asthma, arthritis and related diseases
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, (2008/06/13)
Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
A New Class of Antiarrhythmic Agents: Mannich Bases of 3,4-Dihydro-1-benzoxepin-5(2H)-ones and Related Compounds
Khanna, J. M.,Tandon, V. K.,Kar, K.,Sur, R. N.
, p. 71 - 77 (2007/10/02)
Mannich bases derived from 3,4-dihydro-1-benzoxepin-5(2H)-ones, chromanones and 6,7,8,9-tetrahydrobenzocyclohepten-5(H)-one have been synthesised and shown to possess marked antiarrhythmic activity; 3,4-dihydro-7-methyl-4-(1-piperidinomethyl)- and 3,4-dih
Ethers of 3,4-dihydro-1-benzoxepin-5-one oxime to treat intestinal disorders
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, (2008/06/13)
Therapeutic compositions, particularly for treating intestinal disorders, and a method of treating colopathics by administering an effective amount of the compositions are described. The compositions contain a therapeutically effective amount of at least one isomer of the oximino group of the compound having the formula: STR1 in which: R is selected from the group consisting of halogen atoms and lower alkoxy groups; n is an integer 2 or 3, and Z1 and Z2 are the same or different lower alkyl groups, or NZ1 Z2 represents a saturated heterocyclic group which may have a second heteroatom selected from the group consisting of N and O, and the addition salts of the amino group with pharmaceutically acceptable acids, with a physiological acceptable excipient.
