20364-30-1Relevant articles and documents
SUBSTITUTED, SATURATED AND UNSATURATED N-HETEROCYCLIC CARBOXAMIDES AND RELATED COMPOUNDS FOR THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00406, (2021/04/01)
The invention provides substituted, saturated and unsaturated N-heterocyclic carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
Iron-Catalyzed Intramolecular Aminations of C(sp3)?H Bonds in Alkylaryl Azides
Alt, Isabel T.,Guttroff, Claudia,Plietker, Bernd
, p. 10582 - 10586 (2017/08/22)
The nucleophilic iron complex Bu4N[Fe(CO)3(NO)] (TBA[Fe]) catalyzes the direct intramolecular amination of unactivated C(sp3)?H bonds in alkylaryl azides, which results in the formation of substituted indoline and tetrahydroquinoline derivatives.
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.
Heterocyclic Syntheses Through Electrophilic Ring Closure Reactions of ortho-Allylaniline Systems
Raner, Kevin D.,Ward, A. David
, p. 1749 - 1760 (2007/10/02)
Amide derivatives of 2-allylanilines have been prepared by metallation of the amide derivatives of the corresponding 2-bromoanilines and subsequent reaction with an allylic halide.The electrophile-promoted cyclization of these compounds has been investiga
207. Photo-Emde Degradation of 1,2,3,4-Tetrahydroquinolinium Salts
Partali, Vassilia,Jolidon, Synese,Hansen, Hans-Juergen
, p. 1952 - 1960 (2007/10/02)
It is shown that 1,1-dimethyl-1,2,3,4-tetrahydroquinolinium ions undergo, under direct irradiation through quartz in CH3OH and independent of the nature of the counterion (I-, BF4-), a reductive cleavage of the N(1)-C(8a) bond (photo-Emde degradation).The corresponding N,N-dimethyl-3-phenylpropylamines are formed in high yields and without contamination by Hofmann degradation products of the tetrahydroquinolinium salts.Me groups at C(2) as well as substituents at C(6) (CH3, Cl, CH3O) favour the photo-Emde degradation.The aromatic Cl-substituent is reductively split off in the course of the photoreaction.