- SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are piperidine dione compounds having the following structure (I) wherein RN, R1, R2, R3, R4, L,V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
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- SUBSTITUTED 3-((3-AMINOPHENYL)AMINO)PIPERIDINE-2,6-DIONE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are piperidine dione compounds having the following structure: wherein RN, R1, R2, R3, R4, X, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
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- Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists
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3-(tert-Butyl)-4-hydroxyphenyl 2,4-dichlorobenzoate (1) was discovered in our in-house high throughput screening as a moderate FXR antagonist. To improve the potency and the stability of the hit 1, forty derivatives were synthesized and SAR was systematically explored. The results turn out that replacing the 2,4-dichlorophenyl with 2,6-dichloro-4-amidophenyl shows great improvement in potency, replacing the benzoate with benzamide shows improvement in stability and slight declining of potency and 3-(tert-butyl)-4-hydroxyphenyl unit is essential in obtaining the FXR antagonistic activity.
- Song, Kebiao,Xu, Xing,Liu, Peng,Chen, Lili,Shen, Xu,Liu, Junhua,Hu, Lihong
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p. 6427 - 6436
(2015/10/05)
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- PYRROLONE OR PYRROLIDINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
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The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are melanin concentrating hormone receptor-1 (MCHR1) antagonists which may be used as medicaments.
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Paragraph 00143
(2014/03/26)
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- Synthesis and anticoccidial activities of eight novel ethyl 7-alkyl-6-(2-aryloxyethoxy)-4-hydroxyquinoline-3-carboxylates
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Eight novel ethyl 7-alkyl-6-(2-aryloxyethoxy)-4-hydroxyquinoline-3- carboxylates were synthesised and their structures were identifi ed by 1H NMR, MS, and IR spectra. The anticoccidial activities of these compounds were evaluated according to the ACI (the anticoccidial index) method. The results showed that two of these compounds exhibited anticoccidial activities against Eimeria tenella in the chicken' diet with a dose of 27 mg kg-1.
- Yan, Chun-Rong,Zeng, Xing-Yan,Yao, Yuan-Peng,Nie, Kui,Wang, Yu-Liang,Chen, Hua
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experimental part
p. 71 - 74
(2010/07/03)
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- NPY ANTAGONISTS, PREPARATION AND USES
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The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.
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Page/Page column 91
(2009/09/28)
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