557056-07-2Relevant academic research and scientific papers
Five-membered heteroaromatic derivative, preparation method and application thereof
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Paragraph 0751-0755; 0915-0919, (2021/07/08)
The invention belongs to the technical field of medicines, and particularly relates to a five-membered heteroaromatic compound, a composition, a preparation method and application thereof. The compound or the composition can be used as an inhibitor of a retinoid-related orphan receptor [gamma]t (ROR [gamma]t). The invention also relates to a method for preparing the compound and the composition, and application of the compound and the composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
ROR [gamma]t inhibitor, preparation method and application thereof
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Paragraph 1293; 1295-1297, (2021/07/08)
The invention relates to the technical field of medicines, in particular to an ROR [gamma]t inhibitor, a preparation method and application thereof. The invention also relates to a pharmaceutical composition containing the compound, a method for preparing the pharmaceutical composition, and application of the compound or the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
Novel aminopyrimidine EGFR inhibitor
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Paragraph 2893-2898, (2021/03/24)
The present invention provides a novel aminopyrimidine compound that is a selective inhibitor of the fourth generation EGFR (T790M/C797S mutation), a pharmaceutical composition containing the compound, a useful intermediate for preparing the compound, and
MORPHOLINYL, PIPERAZINYL, OXAZEPANYL AND DIAZEPANYL O-GLYCOPROTEIN-2-ACETAMIDO-2-DEOXY-3-D-GLUCOPYRANOSIDASE INHIBITORS
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, (2020/07/04)
Described herein are compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, X, R1, R3, R4, Y1, Y2, m, n, and p are as defined herein.
Pan-Tropic Entry Inhibitors
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Page/Page column 38; 39, (2019/10/15)
This disclsore relates to compounds according to Formula (I), salts, prodrugs and pharmaceutical formulation comprising the compound are provided herein for the treatment of CXCR4 and CCR5 related conditions. The conditions may include viral infections, a
PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
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Paragraph 0809, (2018/05/24)
The present invention provides compounds, compositions thereof, and methods of using the same.
Discovery of novel N-aryl piperazine CXCR4 antagonists
Zhao, Huanyu,Prosser, Anthony R.,Liotta, Dennis C.,Wilson, Lawrence J.
, p. 4950 - 4955 (2015/10/28)
A novel series of CXCR4 antagonists with substituted piperazines as benzimidazole replacements is described. These compounds showed micromolar to nanomolar potency in CXCR4-mediated functional and HIV assays, namely inhibition of X4 HIV-1IIIB virus in MAGI-CCR5/CXCR4 cells and inhibition of SDF-1 induced calcium release in Chem-1 cells. Preliminary SAR investigations led to the identification of a series of N-aryl piperazines as the most potent compounds. Results show SAR that indicates type and position of the aromatic ring, as well as type of linker and stereochemistry are significant for activity. Profiling of several lead compounds showed that one (49b) reduced susceptibility towards CYP450 and hERG, and the best overall profile when considering both SDF-1 and HIV potencies (6-20 nM).
IMIDAZOPYRAZINE SYK INHIBITORS
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Paragraph 0439, (2014/01/08)
Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suf-fering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or dis-order are provided.
NOVEL AZETIDINE COMPOUNDS USEFUL IN THE TREATMENT OF FUNCTIONAL GASTROINTESTINAL DISORDERS, IBS AND FUNCTIONAL DYSPEPSIA
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Page/Page column 47, (2008/06/13)
The present invention relates to new azetidine compounds, to pharmaceutical compositions cotaining them and the use of said compounds in in the treatment of functional gastrointestinal disorders, IBS and functional dyspepsia. The compounds are neurokinin
Benzhydryl derivatives
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, (2008/06/13)
A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the
