- PHARMACEUTICAL COMPOUNDS
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The invention provides a composition of matter which: ? (i) consists of at least 90 % by weight of an atropisomer (2A) and 0-10 % by weight of an atropisomer of formula (2B); or ? (ii) consists of at least 90 % by weight of an atropisomer (2B) and 0-10 %
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- PYRROLE DERIVATIVES AS PLK1 INHIBITORS
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The invention provides compounds of the formula (3): or a pharmaceutically acceptable salt or tautomer thereof. The compounds are useful in the treatment of cancers.
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- NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
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There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.)
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- High-efficacy 5-HT1A agonists for antidepressant treatment: A renewed opportunity
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We report the discovery of novel 5-HT1A receptor agonists and describe the process that led to the antidepressant candidate 9 (F 15599). 9 has nanomolar affinity for 5-HT1A binding sites and is over 1000-fold selective with respect to the other 5-HT1 receptor subtypes, 5-HT2-7 receptor families, and also numerous GPCRs, transporters, ion channels, and enzymes. In a cellular model of signal transduction, 9 activates h5-HT1A receptors with an efficacy superior to that of the prototypical 5-HT1A agonist (±)-8-OH-DPAT and comparators undergoing clinical trials. After acute oral administration in rats, 9 totally reverses immobility in the forced swimming test and produces behaviors characteristic of 5-HT1A receptor activation. However, these effects occurred at widely separated doses, suggesting that 9 discriminates between distinct populations of 5-HT1A receptors. While the clinical relevance of these observations is still unknown, this opens new perspectives for the treatment of depressive disorders.
- Maurel, Jean Louis,Autin, Jean-Marie,Funes, Philippe,Newman-Tancredi, Adrian,Colpaert, Francis,Vacher, Bernard
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p. 5024 - 5033
(2008/03/13)
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- Oxazoline antiproliferative agents
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Compounds having Formula I are useful for treating cancer. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of treating cancer in a mammal.
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