- MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Provided are IDO inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases such as chronic viral infection, chronic bacterial infections, cancer, sepsis or a neurological disorder.
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Page/Page column 25-26
(2018/07/29)
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- RAF INHIBITOR COMPOUNDS
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This invention provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I); and use of a compound of Formula (I) for treating specified cancers.
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Page/Page column 35
(2013/09/26)
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- SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS
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The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
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Page/Page column 59
(2013/09/26)
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- NOVEL BENZIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THESE COMPOUNDS
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The present invention relates to novel benzimidazole derivatives of the formula (I) as defined in the description and in the claims, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.
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- First enantioselective total synthesis of (-)-tejedine
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(Matrix presented) The first enantioselective total synthesis of (-)-tejedine (1) is reported. Tejedine is a seco-bisbenzyltetrahydroisoquinoline isolated in 1998 as a minor component from Berberis vulgaris. The synthesis was achieved using a strategy employing four key steps, including a chiral auxiliary-assisted diastereoselective Bischler-Napieralski cyclization.
- Wang, You-Chu,Georghiou, Paris E.
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p. 2675 - 2678
(2007/10/03)
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- 1-phenyl-benzimidazole compounds and their use as GABA-a receptor modulators
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The present invention relates to novel benzimidazole compounds, represented by general formula (I) in which o is 0, 1, 2 or 3; R1represents an alkyl group, a phenyl group, or a monocyclic heterocyclic group, which groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkyl-alkyl, alkoxy, halogen, trifluoromethyl, cyano, amino and nitro; or R1represents a cyano group or a group of the formula -alkyl-CO2R2, alkenyl-CO2R2, —CO—R2, —CO2(CH2)mR2, or —C(R3)═N—OR2, R11represents a group of formula —CO2—R9, or R11represents a group of general formula (II) in which n is 0, 1, 2 or 3; or R11may represent a group of general formula (III), in which n is 0, 1, 2 or 3; the novel compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAAreceptor complex, such as for example anxiety, sleep disorders, anaestesia, memory disorders, and epilepsia or other convulsive disorders.
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- Synthetic studies towards western and eastern macropolypeptide subunits of Kistamycin
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The western subunit (fused bicyclic 16+15 membered ring) was synthesized by sequential intramolecular S(N)Ar reaction and the first 17-membered ring compound as model of the eastern subunit was obtained by an intramolecular Ni0 mediated coupling reaction.
- Beugelmans, Rene,Roussi, Georges,Zamora, Eduardo Gonzalez,Carbonnelle, Annie-Claude
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p. 5089 - 5112
(2007/10/03)
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