- Tetrahydroisoquinoline compounds
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The present invention provides a substituted aryl compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition and containing the same as PRMT5 inhibitor.
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Paragraph 0412-0417
(2021/10/13)
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- TETRAHYDROISOQUINOLINE COMPOUNDS
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The present invention relates to a novel class of tetrahydroisoquinoline compounds of formula I and to compositions comprising the same. The compounds and compositions of the present invention can be used as medicaments in the treatment of cancer.
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Page/Page column 27
(2019/08/20)
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- NEW ISOINDOLINE OR ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Compounds of formula (I): (I) wherein Het, R3, R4, R5, R7, R8, R9, T, p, p', q, and q' are as defined in the description are pro-apoptotic agents useful in the treatment of cancers and of a
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Page/Page column 31; 32
(2015/02/19)
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- Syntheses of the marine metabolites verongamine, hemibastadin-2, and aerothionin using the cyano ylide coupling methodology
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Syntheses of the marine metabolites verongamine, hemibastadin-2, and aerothionin have been accomplished by a methodology involving the conversion of a carboxylic acid to an acyl cyano phosphorane which may be oxidized to an α,β-diketo nitrile. This strong
- Wasserman, Harry H.,Wang, Jianji
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p. 5581 - 5586
(2007/10/03)
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- (+/-)-(N-alkylamino)benzazepine analogs: novel dopamine D1 receptor antagonists.
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(+/-)-(N-Alkylamino)benzazepine analogs were prepared as novel dopamine D1 receptor antagonists to further elucidate the role of these receptor subtypes in the pharmacology and toxicology of cocaine. In the first series of compounds, (+/-)-7-chloro-8-hydroxy-3- [6-(N,N-dimethylamino)-hexyl]-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepi ne (15) showed the highest affinity (Ki = 49.3 nM) and subtype-selectivity for dopamine D1 over dopamine D2, 5-HT2a, and 5-HT2c receptors. Compounds 7a [(+/-)-7-Chloro-8-hydroxy-3-[4-(N,N-dimethylamino)butyl]-1-phenyl- 2,3,4,5-tetrahydro-1H-3-benzazepine], 11 [(+/-)-7-chloro-8-hydroxy-3-[6-[(N,N-dimethylamino)hexyl]-1- phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-cyanoborane], and 15 were moderately potent dopamine D1 receptor antagonists as evidenced by their ability to block dopamine-stimulated adenylyl cyclase activity in rat caudate (predicted Ki values = 60, 34, and 21 nM, respectively). Compound 7a appears to be unique in that, despite its relatively potent inhibition of dopamine stimulated adenylyl cyclase, it demonstrated relatively weak binding affinity at the dopamine D1 receptors (Ki = 811 nM). Unlike previously reported N-alkylbenzazepines, where a significant loss in dopamine D1 receptor binding affinity was observed when successive increases in the alkyl side chain size at the benzazepine nitrogen were made, several of these novel N-alkylamino analogs demonstrated high-affinity binding with an optimal chain length of six carbons. This initial series of compounds appears to be identifying another binding domain on the dopamine D1 receptor protein that has not previously been characterized and that accepts an amino function. Further, these compounds may serve as templates for the design of peripherally active dopamine D1 receptor antagonists.
- Shah,Izenwasser,Geter-Douglass,Witkin,Newman
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p. 4284 - 4293
(2007/10/03)
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- Synthesis and Molecular Modeling of 1-Phenyl-1,2,3,4-tetrahydroisoquinolines and Related 5,6,8,9-Tetrahydro-13bH-dibenzoquinolizines as D1 Dopamine Antagonists
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New 1-phenyl-1,2,3,4-tetrahydroisoquinolines and related 5,6,8,9-tetrahydro-13bH-dibenzo-quinolizines were prepared as ring-contracted analogs of the prototypical 1-phenyl-2,3,4,5-tetrahydrobenzazepines (e.g., SCH23390) as a continuation of our studi
- Minor, Deborah L.,Wyrick, Steven D.,Charifson, Paul S.,Watts, Val J.,Nichols, David E.,Mailman, Richard B.
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p. 4317 - 4328
(2007/10/02)
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- Brominated tyrosine-derived metabolites from the sponge Ianthella basta
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Two novel metabolites, containing four bromotyrosine units, have been isolated from the sponge Ianthella basta.
- Kazlauskas,Lidgard,Murphy,Wells
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p. 2277 - 2280
(2007/10/02)
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