155302-27-5Relevant academic research and scientific papers
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties
Zajdel, Pawe?,Marciniec, Krzysztof,Sata?a, Grzegorz,Canale, Vittorio,Kos, Tomasz,Partyka, Anna,Jastrz?bska-Wi?sek, Magdalena,Weso?owska, Anna,Basińska-Ziobroń, Agnieszka,Wójcikowski, Jacek,Daniel, W?adys?awa A.,Bojarski, Andrzej J.,Popik, Piotr
, p. 618 - 622 (2016)
A series of N1-azinylsulfonyl-3-(1,2,3,6,tetrahyrdopyridin-4-yl)-1H-indole derivatives was designed to obtain highly potent 5-HT6 receptor ligands. The study allowed for the identification of 25 (4-{[5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-1-yl]sulfonyl}isoquinoline), a potent and selective 5-HT6 receptor antagonist. The selected compound, was evaluated in vivo in a novel object recognition (NOR) and forced swim (FST) tests in rats, demonstrating distinct pro-cognitive and antidepressant-like properties (MED = 1 mg/kg and 0.1 mg/kg, i.p., respectively). Compound SB-742457, used as comparator, reversed memory deficits in NOR task in similar doses, while in FST it was active in 10-30-fold higher dose (3 mg/kg). In contrast to SB-742457, which was active in Vogel test (MED = 3 mg/kg), compound 25 displayed no anxiolytic activity.
HETEROCYCLIC COMPOUND, APPLICATION THEREOF, AND COMPOSITION CONTAINING SAME
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, (2022/03/07)
A heterocyclic compound represented by formula XI, a pharmaceutically acceptable salt, a solvate, or a solvate of a pharmaceutically acceptable salt thereof, use thereof, and a composition containing the same. The compound is novel in structure and has good STAT5 inhibitory activity.
Substituted heterocyclic compounds and application of same to medicines
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Paragraph 0201; 0203; 0204; 0205; 0206, (2017/04/29)
The invention relates to substituted heterocyclic compounds and application of the same to medicines and specifically provides the novel substituted heterocyclic compounds or stereoisomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, and preparation methods thereof. The invention also relates to pharmaceutical compositions containing the compounds and application of the compounds or pharmaceutical compositions to treatment of diseases related to 5-HT6 receptors, especially Alzheimer's disease.
Substituted heterocyclic compounds and its application on the medicament (by machine translation)
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Paragraph 0192; 0193; 0194; 0195, (2017/06/02)
The invention relates to substituted heterocyclic compounds and its application on the medicament, in particular to a novel class of substituted heterocyclic compounds or its isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug, and their method of preparation. The invention also relates to the compounds of the invention pharmaceutical composition, and said compound or pharmaceutical compositions for the treatment5-HT6receptor-related diseases, in particular Alzheimer's disease in the use thereof. (by machine translation)
COMPOUNDS AND THERAPEUTIC USES THEREOF
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Page/Page column 70, (2013/02/28)
The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated w
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.
INDOLE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS
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Page 39, (2010/02/06)
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.
INDOLE DERIVATIVES
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, (2008/06/13)
Compounds of the formula STR1 wherein Z is STR2 R 1 is STR3 X is O, NH, or S; A, B, D, E, and F are each independently C, N, O, or S; wherein the remaining variables are defined in the specification, and the pharmaceutically acceptable salts thereof. Thes
