141699-58-3Relevant academic research and scientific papers
BROAD-SPECTRUM CARBAPENEMS
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, (2021/05/29)
The present disclosure provides broad-spectrum carbapenem derivatives and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such derivatives and/or compositions.
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND METHODS OF USE THEREOF
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Page/Page column 170-171, (2021/06/26)
Provided herein are compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer 5 or a metabolic disease.
RET inhibitor and pharmaceutical composition and application thereof
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Paragraph 0356; 0364-0365, (2021/10/27)
The invention belongs to the field of medicines, and relates to an RET inhibitor and a pharmaceutical composition and application thereof. Specifically, the invention relates to a compound as shown in a formula (I), or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound as shown in the formula (I). The invention also relates to pharmaceutical compositions comprising the compounds, and uses of the compounds and pharmaceutical compositions thereof in the preparation of a medicine which is especially used for the treatment and prevention of RET-related diseases and disorders, including cancers, irritable bowel syndrome and/or pain associated with irritable bowel syndrome.
RET Inhibitor. Pharmaceutical composition and use thereof
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Paragraph 0301-0303, (2021/10/27)
The invention belongs to the field of medicines, and relates to RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I, and a pharmaceutical composition thereof in the manufacture of a medicament, in particular for the treatment and prophylaxis of diseases and disorders associated and RET.
RET Inhibitor. Pharmaceutical composition and use thereof
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Paragraph 0324-0327; 0408; 0412-0413, (2021/10/27)
The invention belongs to the field of medicines, and relates to RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I, and a pharmaceutical composition thereof in the manufacture of a medicament, in particular for the treatment and prophylaxis of diseases and disorders associated and RET.
RET Inhibitor. Pharmaceutical composition and use thereof
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Paragraph 0316-0317, (2021/11/26)
The invention belongs to the field of medicines, and relates to a novel RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a geometric isomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I, and a pharmaceutical composition thereof in the manufacture of a medicament, in particular for the treatment and prevention and RET of diseases and disorders associated with irritable bowel syndrome.
AZETIDINE DERIVATIVE, AND PRODRUG THEREOF
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Paragraph 0143; 0145, (2021/04/16)
An object of the present invention is to provide a compound useful as a therapeutic or prophylactic drug for a disease involving the immune system, by suppressing a function of immune cells by suppressing proliferation of activated T cells or suppressing production of interferon alpha (IFN-α) by activated plasmacytoid dendritic cells (pDC), particularly an autoimmune disease such as systemic lupus erythematosus (SLE) and lupus nephritis in SLE patients. The present invention provides a compound represented by general formula (I) : [wherein X, R1, R2, R3, R4, R5 and R6 are as described in the description], or a pharmaceutically acceptable salt thereof.
ATF6 MODULATORS AND USES THEREOF
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Paragraph 253, (2021/04/17)
Compounds (1-2) as modulators of Activating Transcription Factor 6 (ATF6) are provided. The compounds may find use as therapeutic agents for the treatment of diseases or disorders mediated by ATF6 and may find particular use in the treatment of viral infections, neurodegenerative diseases, vascular diseases, or cancer. (Formula (1-2))
AZAINDOLE DERIVATIVE AND USE THEREOF AS FGFR AND C-MET INHIBITOR
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Paragraph 0134, (2021/05/29)
A series of pyrazolopymidine derivatives, and use thereof in the preparation of a medicament for treating disease associated with FGFR and c-Met. The pyrazolopymidine derivative is a compound represented by formula (I), a tautomer, or a pharmaceutically acceptable salt thereof.
HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor
Holm, Patrik,éles, János,Balázs, Ottilia,Fodor, László,Greiner, István,Horváth, Anita,Kóti, János,Kiss, László,Kolok, Sándor,Kostyalik, Diána,Krámos, Balázs,Lévay, Gy?rgy,Ledneczki, István,Lendvai, Balázs,Mahó, Sándor,Molnár, Katalin Dudás,Némethy, Zsolt,Szigetvári, áron,Tapolcsányi, Pál,Thán, Márta,Vágó, István,Vastag, Mónika,Visegrády, András
, (2021/06/22)
HTS campaign of the corporate compound collection resulted in a novel, oxalic acid diamide scaffold of α7 nACh receptor positive allosteric modulators. During the hit expansion, several derivatives, such as 4, 11, 17 demonstrated not only high in vitro potency, but also in vivo efficacy in the mouse place recognition test. The advanced hit molecule 11 was further optimized by the elimination of the putatively mutagenic aromatic-amine building block that resulted in a novel, aminomethylindole compound family. The most balanced physico-chemical and pharmacological profile was found in case of compound 55. Docking study revealed an intersubunit binding site to be the most probable for our compounds. 55 demonstrated favorable cognitive enhancing profile not only in scopolamine-induced amnesia (place recognition test in mice) but also in natural forgetting (novel object recognition test in rats). Compound 55 was, furthermore, active in a cognitive paradigm of high translational value, namely in the rat touch screen visual discrimination test. Therefore, 55 was selected as a lead compound for further optimization. Based on the obtained favorable results, the invented aminomethylindole cluster may provide a viable approach for cognitive enhancement through positive allosteric modulation of α7 nAChRs.
