17403-03-1Relevant academic research and scientific papers
BENZYL-SUBSTITUTED TETRACYCLIC HETEROCYCLIC COMPOUNDS
-
Page/Page column 105-106, (2010/04/03)
The present invention pertains to Benzyl-substituted tetracyclic heterocyclic compounds of formula (I), as well as the resulting pharmaceutical compositions, and their use in the treatment or prophylaxis of diseases alleviated by inhibition of type 5 phosphodiesterases. Furthermore, the present invention pertains to the methods of manufacturing these Benzyl -substituted tetracyclic heterocyclic compounds.
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors
Deskus, Jeffrey A.,Epperson, James R.,Sloan, Charles P.,Cipollina, Joseph A.,Dextraze, Pierre,Qian-Cutrone, Jingfang,Gao, Qi,Ma, Baoqing,Beno, Brett R.,Mattson, Gail K.,Molski, Thaddeus F.,Krause, Rudolph G.,Taber, Matthew T.,Lodge, Nicholas J.,Mattson, Ronald J.
, p. 3099 - 3104 (2008/02/13)
A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were determined. In particular, a nitrile substituent at the C5 position of the indole ring gave poten
PIPERIDINE-INDOLE COMPOUNDS HAVING 5-HT6 AFFINITY
-
Page/Page column 13, (2010/11/28)
Described herein are indole compounds with affinity for the 5-HT6 receptor, which have general formula (I) wherein, R is selected from the group consisting of H and C1-4alkyl; R is selected from the group consisting of H, C1-4alkyl and benzyl; -----
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists
Cole, Derek C.,Ellingboe, John W.,Lennox, William J.,Mazandarani, Hossein,Smith, Deborah L.,Stock, Joseph R.,Zhang, Guoming,Zhou, Ping,Schechter, Lee E.
, p. 379 - 383 (2007/10/03)
The development of a series of N1-sulfonyl-3-(1,2,3,6- tetrahydropyridin-4-yl)indole 5-HT6 antagonists is described. Two analogs, 15g and 15y, had 0.4 and 3.0 nM affinity, and antagonized the production of adenylate cyclase at sub-nanomolar concentrations. A series of N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)indole derivatives was designed and synthesized. These compounds were shown to have high affinity for the 5-HT6 receptor. Two analogs, 4-[3-(1,2,3,6-tetrahydropyridin- 4-yl)-1H-indole-1-sulfonyl]-phenylamine 15g and 4-[3-(1,2,3,6-tetrahydropyridin- 4-yl)-5-methoxy-1H-indole-1-sulfonyl]-phenylamine 15y, had 0.4 and 3.0 nM affinity, respectively, and antagonized the production of adenylate cyclase at sub-nanomolar concentrations.
Piperidine-indole compounds having 5-HT6 affinity
-
, (2008/06/13)
Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: wherein: R1 is selected from the group consisting of H and C1-4alkyl; R2 is selected from the group consisting of H, C1-4alkyl and benzyl; - - - represents a single or double bond; R3 is selected from the group consisting of COR5 and SO2R5; R4a is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4b is selected from the group consisting of H, hydroxy, halo, C3-7cycloalkyloxy, C1-4alkoxy, C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R4c is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4d is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; and R5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C1-4alkoxy, C1-4alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C1-4alkylcarbonyl, C1-4alkoxycarbonyl and C1-4alkylS-. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
Treating psychic disorders with tetrahydropyridin-4-yl-1H-indoles
-
, (2008/06/13)
Novel antidepressant, antiemetic and neuroleptic compositions containing as the active ingredient at least one compound of the formula STR1 wherein R is selected from the group consisting of hydrogen and methoxy, R1 and R2 are individually selected from the group consisting of hydrogen and methyl and their non-toxic, pharmaceutically acceptable acid addition salts and a novel method of treating psychic disorders in warm-blooded animals.
