174822-86-7Relevant academic research and scientific papers
2-AZASPIRO[3.4]OCTANE DERIVATIVES AS M4 AGONISTS
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Paragraph 0985-0988, (2021/04/17)
Provided herein are compounds according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.
Design, Synthesis, and Pharmacological Characterization of Heterobivalent Ligands for the Putative 5-HT2A/mGlu2Receptor Complex
Poulie, Christian B. M.,Liu, Na,Jensen, Anders A.,Bunch, Lennart
, p. 9928 - 9949 (2020/09/12)
We report the synthesis of the first series of heterobivalent ligands targeting the putative heteromeric 5-HT2A/mGlu2 receptor complex, based on the 5-HT2A antagonist MDL-100,907 and the mGlu2 ago-PAM JNJ-42491293. The functional properties of monovalent and heterobivalent ligands were characterized in 5-HT2A-, mGlu2/Gqo5-, 5-HT2A/mGlu2-, and 5-HT2A/mGlu2/Gqo5-expressing HEK293 cells using a Ca2+ imaging assay and a [3H]ketanserin binding assay. Pronounced functional crosstalk was observed between the two receptors in 5-HT2A/mGlu2 and 5-HT2A/mGlu2/Gqo5 cells. While the synthesized monovalent ligands retained the 5-HT2A antagonist and mGlu2 ago-PAM functionalities, the seven bivalent ligands inhibited 5-HT-induced responses in 5-HT2A/mGlu2 cells and both 5-HT- and Glu-induced responses in 5-HT2A/mGlu2/Gqo5 cells. However, no definitive correlation between the functional potency and spacer length of the ligands was observed, an observation substantiated by the binding affinities exhibited by the compounds in 5-HT2A, 5-HT2A/mGlu2, and 5-HT2A/mGlu2/Gqo5 cells. In conclusion, while functional crosstalk between 5-HT2A and mGlu2 was demonstrated, it remains unclear how these heterobivalent ligands interact with the putative receptor complex.
Enantiospecific sp2–sp3 Coupling of ortho- and para-Phenols with Secondary and Tertiary Boronic Esters
Wilson, Claire M.,Ganesh, Venkataraman,Noble, Adam,Aggarwal, Varinder K.
, p. 16318 - 16322 (2017/12/04)
The coupling of ortho- and para-phenols with secondary and tertiary boronic esters has been explored. In the case of para-substituted phenols, after reaction of a dilithio phenolate species with a boronic ester, treatment with Ph3BiF2 or Martin's sulfurane gave the coupled product with complete enantiospecificity. The methodology was applied to the synthesis of the broad spectrum antibacterial natural product (?)-4-(1,5-dimethylhex-4-enyl)-2-methyl phenol. For ortho-substituted phenols, initial incorporation of a benzotriazole on the phenol oxygen atom was required. Subsequent ortho-lithiation and borylation gave the coupled product, again with complete stereospecificity.
Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists
Gray, David L.,Xu, Wenjian,Campbell, Brian M.,Dounay, Amy B.,Barta, Nancy,Boroski, Susan,Denny, Lynne,Evans, Lori,Stratman, Nancy,Probert, Al
scheme or table, p. 6604 - 6607 (2010/06/12)
Compounds that are both norepinephrine reuptake inhibitors (NRI) and 5-HT1A partial agonists may have the potential to treat neuropsychiatric disorders including attention deficit hyperactivity disorder (ADHD) and depression. Targeted screening
Piperidinyl substituted cyclohexane-1,4-diamines
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Page/Page column 32, (2008/06/13)
The present invention relates to piperidine substituted cyclohexane-1,4-diamine compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as method of treatments.
2-(1H-INDOLYLSULFANYL) -ARYL AMINE DERIVATIVES FOR USE IN THE TREATMENT OF AFFECTIVE DISORDERS, PAIN, ADHD AND STRESS URINARY INCONTINENCE
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Page/Page column 38, (2008/06/13)
The present invention relates to aniline derivatives of the general formula I as the free base or salts thereof and their use.
Serotonin 5-HT1A and dopamin D2 receptor ligands
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, (2008/06/13)
The present invention relates to a novel series of 4-phenylpiperazines, 4-phenylpiperidines and 4-phenyl-1,2,3,6-tetrahydropyridines compounds of general formula (I) wherein A is alkylene, alkenylene, alkynylene, and C3-7cycloalkylene; R1is a C3-10alkyl, alkenyl, or alkynyl group, cycloalk(en)yl, cycloalk(en)yl-alk(en/yn)yl, trifluoromethylsulfonyl, or alkylsulfonyl, R2-R5are optional substituents; R9and R10are hydrogen, alkyl or together form an ethylene or propylene bridge; W is O or S; V is O, S, CR6R7, or NR8wherein R6, R7, and R8are hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, optionally substituted arylalkyl or aryl, or R6and R7constitute a 3-7 membered spiro ring; Z is —(CH2)m—, m being 2 or 3 or Z is —CH═CH—; X is N, C or CH; show effects on central serotonin 5-HT1Aand dopamine D2receptors. Thus the novel compounds are useful in the treatment of certain psychic and neurologic disorders, in particular psychosis.
