- 4-oxa-4,5,6,7-tetrahydro benzo[B] furan-3-carboxylic compound and application thereof
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The invention discloses a 4-oxa-4,5,6,7-tetrahydro benzo[B] furan-3-carboxylic compound which is of a structure as shown in the formula I. A preparation method of the 4-oxa-4,5,6,7-tetrahydro benzo[B] furan-3-carboxylic compound is quick, convenient and l
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Paragraph 0024; 0025; 0026; 0027
(2017/07/20)
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- NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS
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Novel tricyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
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Page/Page column 46
(2015/07/07)
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- NOVEL TRICYCLIC CALCIUM SENSING RECEPTOR ANTAGONISTS FOR THE TREATMENT OF OSTEOPOROSIS
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Novel tricyclic compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing osteoporosis and similar conditions. The compounds are effective as calcium sensing receptor antagonists. Pharmaceutical compositions and methods of treatment are also included.
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Page/Page column 46
(2015/07/07)
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- Microwave-assisted synthesis of tetrahydroindoles
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An efficient synthesis of tetrahydroindoles with different substituents in position 1 is described. Microwave-assisted aminolysis of 4-oxo-4,5,6,7-tetrahydrobenzofuran with different primary amines gives the corresponding tetrahydroindoles in few minutes.
- Piras, Leonarda,Ghiron, Chiara,Minetto, Giacomo,Taddei, Maurizio
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p. 459 - 462
(2008/09/17)
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- Fused pyrrolecarboxamides: GABA brain receptor ligands
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Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
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Page/Page column 22
(2008/06/13)
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- CERTAIN FUSED PYRROLECARBOXAMIDES A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
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Disclosed are compounds of formula I: STR1 wherein R 8 and R. sub.9 independently represent hydrogen or organic substituents; W represents optionally substituted thiazolyl or quinoxalinyl; X is hydrogen, hydroxy or lower alkyl; andT is hydrogen, halogen, hydroxy, nitro, amino or alkyl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptor. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
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- CERTAIN PYRROLO PYRIDINE-3-CARBOXAMIDES; A NEW CLASS OF GABA BRAIN RECEPTOR LIGANDS
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The present invention encompasses structures of the formula: STR1 or the pharmaceutically acceptable non-toxic salts thereof wherein: STR2 wherein: W represents substituted or unsubstituted phenyl;X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R. sub.3 is hydrogen or an organic group;R 4 is hydrogen or substituted or unsubstituted organic substituent;R 5 and R 6 represent organic, and inorganic substituents; andn is 1, 2, 3, or 4, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
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- Chemo-enzymatic synthesis and characterization of L-tryptophans selectively 13C-enriched or hydroxylated in the six-membered ring using transformed Escherichia coli cells
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L-(3a-13C)- and L-(6-13C)tryptophan have been synthesized from simple labelled compounds via a single reaction scheme based on the conversion of 1,3-cyclohexanedione into indole.The labelled indoles have been converted in one step into the corresponding L-tryptophans using transformed Escherichia coli cells with large amounts of the enzyme, tryptophan synthease.The same reaction scheme has been used for the synthesis of 4- and 7-indolol.These hydroxyindoles together with 5-indolol have been converted into 4-, 7- and 5-hydroxy-L-tryptophan, respectively, using theEscherichia coli cells.The latter compound is the immediate precursor of the neurotransmitter, serotonin.It appears that 7-indolol is the only indole derivative which is converted faster than unsubstituted indole by the enzyme, tryptophan synthease.With the preparation of L-(3a-13C)- and L-(6-13C)tryptophan, we have completed the series of indoles and L-tryptophans with a stable isotope (13C, 15N or 2H) in the aromatic ring.In this paper, we also discuss the NMR parameters of these mono-isotopically labelled systems.
- Berg, E. M. M. van den,Jansen, F. J. H. M.,Goede, A. T. J. W. de,Baldew, A. U.,Lugtenburg, J.
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p. 287 - 297
(2007/10/02)
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- A CONVENIENT SYNTHESIS OF 4-HYDROXYBENZO-(B)-FURAN, (KARANJOL)
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The synthesis of karanjol from tetrahydro-(b)-furan intermediates is described.
- Kneen, Geoffrey,Maddocks, Peter J.
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p. 1635 - 1640
(2007/10/02)
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