- 8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity
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Several new, potent dopamine subtype 2 (DA D2) active compounds with serotonin subtype 2A (5-HT2A) pharmacology are presented. 8-Substituted 3,4-dihydroquinolinones, tetrahydroquinolines, and N-acyl tetrahydroquinolines were evaluated in primary assays. Subtle changes on this novel scaffold translated to large changes in potency and selectivity in vitro. These compounds show promise as novel atypical antipsychotics for the treatment of schizophrenia.
- Singer, Jamie M.,Barr, Bridget M.,Coughenour, Linda L.,Gregory, Tracy F.,Walters, Michael A.
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p. 4560 - 4563
(2007/10/03)
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- PHENYLALKYL AND PYRIDYLALKYL PIPERAZINE DERIVATIVES
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This invention relates to compounds of the formula (1) wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.
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- Heterocyclic substituted piperazines for the treatment of schizophrenia
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This invention relates to compounds of the formula 1 wherein Ar, A, R2, R3, Y and ring Q are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disord
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Page/Page column 19
(2010/02/06)
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- A Convergent Synthesis of 14-Membered F-O-G Ring Analogs of the Teicoplanin Binding Pocket via Intramolecular SNAr Reaction
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An intramolecular SNAr reaction for efficient macrocyclization via biaryl ether formation was developed for syntheses of the 14-membered macrocycles 2 and 3 related to F-O-G ring of teicoplanin 1.Chloride as well as fluoride could be used as the leaving group in this reaction.However, the latter was prefered since it required milder conditions.Both ortho and para nitro, fluoro disubstituted aromatic rings were suitable for the macrocyclization reaction with tethered aryl oxides.The nonproteinogenic α-amino acid 23, required for the synthesis of 3, was prepared via an asymmetric Strecker synthesis using (R)-phenylglycinol as a chiral auxiliary.The overall synthetic strategy was convergent, and the cyclization could be performed in the presence of the highly sensitive arylglycine unit without racemization.
- Zhu, Jieping,Beugelmans, Rene,Bourdet, Sebastien,Chastanet, Jacqueline,Roussi, George
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p. 6389 - 6396
(2007/10/03)
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- Oxindoles as sleep-inducers
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Sleep inducers of the formula: STR1 wherein R is hydrogen or halo of atomic weight of from 18 to 36, R' is hydrogen, halo or CF3 and R° is hydrogen or lower alkyl. Preparation by cyclizing a 2-nitro-phenylacetic acid is also disclosed.
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