92398-47-5Relevant academic research and scientific papers
A two-aryl thio hydantoin derivatives and use thereof
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Paragraph 0356-0359, (2018/03/26)
The invention provides a novel diarylthiohydantoin derivative with the structure represented by formula I, and its application. In the formula, X is O or S; R1 and R2 can bee same to or different from each other, respectively represent hydrogen, a C1-6 alkyl group, a C1-6 alkoxy group, a C3-8 naphthenic base, and a C3-8 alkenyl group; R3 represents hydrogen, halogen atoms, a hydroxyl group, a cyano group and a nitro group; R4 and R5 can be same to or different from each other, and respectively represent hydrogen, halogen atoms, -C=(O)-N-(C1-4alkyl) and -(C1-4alkyl)-C(=O)-N-(C1-4 alkyl); and n is 1, 2, 3, or 4. The invention also relates to the application of the above compounds in excessive proliferative diseases.
NOVEL BETULINIC SUBSTITUTED AMIDE DERIVATIVES AS HIV INHIBITORS
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Page/Page column 80-81, (2017/02/24)
The present invention relates to novel betulinic substituted amide compounds of formula (I); and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y, Z1, Z2, Z3 and are Formula (II) as defined herein. The invention novel betulinic substituted amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Carboxamide derivatives, intermediate, preparation method, pharmaceutical composition and application
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Paragraph 0382; 0383; 0384, (2017/08/26)
The invention discloses a formamide derivative, an intermediate, a preparation method, a pharmaceutical composition and an application. The invention provides a formamide derivative shown in a formula 1 as well as pharmaceutically acceptable salt or solvates of the derivative. The formamide derivative disclosed by the invention is an inhibitor of 11 beta-hydroxysteroid dehydrogenase in a type I, can be used for preparing medicines for treating various diseases which are related to expression or activity of 11beta-HSD1, and has a good market development prospect.
Synthesis of the First Representatives of Spiro-1λ6-isothiazolidine-1,1,4-triones
Dobrydnev, Alexey V.,Popova, Maria V.,Saffon-Merceron, Nathalie,Listunov, Dymytrii,Volovenko, Yulian M.
, p. 2523 - 2528 (2015/09/01)
A strategy for the construction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones through the sulfonylation of 1-aminocyclopropane- and 1-aminocyclobutanecarboxylates with methanesulfonyl chloride followed by alkylation with methyl iodide and subsequent cyclization in the presence of potassium tert-butoxide in N,N-dimethylformamide is reported. An efficient synthesis of starting 1-aminocyclopropane- and 1-aminocyclobutanecarboxylic acids was developed. The reaction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones with N,N-dimethylformamide dimethyl acetal (DMF-DMA) gives 5′-[(Z)-(dimethylamino)methylene]spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones, the structure of which was confirmed by X-ray diffraction study.
A COMPOUND FOR INHIBITING 11B-HYDROXY STEROID DEHYDROGENASE 1, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 0371-0373; 0394-0396, (2014/08/06)
Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same for inhibiting human 11-β-hydroxy steroid dehydrogenase type 1 (11β-HSD1). The disclosed compound and the pharmaceutical composition including the same for inhibiting human 11-β-hydroxy steroid dehydrogenase type 1 (11β-HSD1) are excellent in activity and solubility, and is more efficient in formulation and transfer.
A COMPOUND FOR INHIBITING 11BETA-HYDROXY STEROID DEHYDROGENASE 1, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 674-677, (2013/03/26)
Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same for inhibiting human 11-beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1). The disclosed compound and the pharmaceutical composition including the same for inhibiting human 11-beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1) are excellent in activity and solubility, and is more efficient in formulation and transfer.
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious γ-secretase inhibitors (Part II)
Ye, Xiaocong M.,Konradi, Andrei W.,Smith, Jenifer,Aubele, Danielle L.,Garofalo, Albert W.,Marugg, Jennifer,Neitzel, Marty L.,Semko, Chris M.,Sham, Hing L.,Sun, Minghua,Truong, Anh P.,Wu, Jing,Zhang, Hongbin,Goldbach, Erich,Sauer, John-Michael,Brigham, Elizabeth F.,Bova, Michael,Basi, Guriqbal S.
scheme or table, p. 3502 - 3506 (2010/08/07)
Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement translated in an improved in vivo efficacy.
HEPATITIS C VIRUS INHIBITORS
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, (2009/12/02)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Hepatitis C Virus Inhibitors
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, (2009/12/24)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
Hepatitis C Virus Inhibitors
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Page/Page column 25, (2008/06/13)
Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
