55579-99-2Relevant articles and documents
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.
Substituted tetralins, chromans and related compounds in the treatment of asthma
-
, (2008/06/13)
PCT No. PCT/US87/02734 Sec. 371 Date Apr. 11, 1990 Sec. 102(e) Date Apr. 11, 1990 PCT Filed Oct. 19, 1987Substituted 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 comprising said compounds; a method of treatment with said compounds; and intermediates useful in the synthesis of said compounds.
2-(2-aminophenyl)-acetaldehyde dimethyl acetal: A novel reagent for the protection of carboxylic acids
Arai, Eri,Tokuyama, Hidetoshi,Linsell, Martin S.,Fukuyama, Tohru
, p. 71 - 74 (2007/10/03)
The synthesis and use of 2-(2-aminophenyl)-acetaldehyde dimethyl acetal 1 are described. The amides 2, derived from this amine and carboxylic acids, are stable under basic conditions and thus can be regarded as the protected carboxylic acids. The corresponding carboxylic acids are regenerated by conversion of 2 into indolylamides 3 by treatment with CSA and subsequent hydrolysis with LiOOH or NaOH. In addition, 3 can be easily converted to esters, amides, and aldehydes.
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
-
, (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