179899-22-0Relevant articles and documents
1,2,3,4-tetrahydroquinoline compound and synthetic method and application thereof
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, (2017/07/01)
The invention relates to 1,2,3,4-tetrahydroquinoline compound and a synthetic method and application thereof. In a structure formula of the compound, the R1 is nitro or trifluoromethyl or 3-nitrophenylnitrobenzene sulfonyl or cyano, the R2 is hydrogen or methyl, the R3 is methyl formate or butyl formate, and the R4 is methyl. An aromatic ring of the 1,2,3,4-tetrahydroquinoline compound contains a series of electron withdrawing groups. The synthetic method is simple, economical, environment-friendly, easy to operate, easy to control, higher in product purity and yield and good in development prospect in industrial production; in addition, the synthetic method is also a novel synthetic method in atom economy; furthermore, the 1,2,3,4-tetrahydroquinoline compound can serve as intermediate to be used for preparing antagonist medicine.
Androgen receptor modulator compounds and methods
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, (2008/06/13)
Non-steroidal compounds that are high affinity, high selectivity modulators for androgen receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring androgen receptor agonist, partial agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the androgen receptor modulator compounds.
Switching Androgen Receptor Antagonists to Agonists by Modifying C-Ring Substituents on Piperidinoquinolinone
Zhi, Lin,Tegley, Christopher M.,Marschke, Keith B.,Jones, Todd K.
, p. 1008 - 1012 (2007/10/03)
New nonsteroidal human androgen receptor (hAR) agonists were developed from an hAR antagonist pharmacophore, 2(1H-piperidinoquinolinone. (+/-)-trans-7,8-diethyl-4-trifluoromethyl-2(1H)-piperidinoquinolinone was synthesized and demonstrated p
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2- dihydropyridono[5,6-g]quinolines
Hamann, Lawrence G.,Higuchi, Robert I.,Zhi, Lin,Edwards, James P.,Wang, Xiao-Ning,Marschke, Keith B.,Kong, James W.,Farmer, Luc J.,Jones, Todd K.
, p. 623 - 639 (2007/10/03)
A new nonsteroidal antiandrogenic pharmacophore has been discovered using cell-based cotransfection assays with human androgen receptor (hAR). This series of AR antagonists is structurally characterized by a linear tricyclic 1,2-dihydropyridono[5,6-g]quinoline core. Analogues inhibit AR- mediated reporter gene expression and bind to AR as potently as or better than any known AR antagonists. Several analogues also showed excellent in vivo activity in classic rodent models of AR antagonism, inhibiting growth of rat ventral prostate and seminal vesicles, without accompanying increases in serum gonadotropin and testosterone levels, as is seen with other AR antagonists. Investigations of structure - activity relationships surrounding this pharmacophore resulted in molecules with complete specificity for AR, antagonist activity on an AR mutant commonly observed in prostate cancer patients, and improved in vivo efficacy. Molecules based on this series of compounds have the potential to provide unique and effective clinical opportunities for treatment of prostate cancer and other androgen-dependent diseases.
Tricyclic steroid receptor modulator compounds and methods
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, (2008/06/13)
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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, (2008/06/13)
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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, (2008/06/13)
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
Steroid receptor modulator compounds and methods
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, (2008/06/13)
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
-
, (2008/06/13)
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
-
, (2008/06/13)
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.