865449-63-4Relevant academic research and scientific papers
Spiro derivative, preparation method thereof and application of spiro derivative in medicine
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Paragraph 1591-1593; 1598-1601, (2021/08/19)
The invention relates to a spiro derivative, a preparation method thereof and application of the spiro derivative in medicine. Specifically, the invention relates to the spiro derivative shown in a general formula (I), the preparation method thereof, a pharmaceutical composition containing the spiro derivative and application of the spiro derivative as a therapeutic agent, especially application of the spiro derivative as an RAF inhibitor and application of the spiro derivative in preparation of drugs for treating or preventing various diseases (including cancers) related to over-expression RAF activity.
PYRIDINE DERIVATIVES AS TMEM16A MODULATORS FOR USE IN THE TREATMENT OF RESPIRATORY CONDITIONS
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Page/Page column 148, (2021/01/29)
Compounds of general formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein are useful for treating respiratory di
NOVEL BIPHENYL COMPOUND OR SALT THEREOF
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Paragraph 0448, (2020/04/21)
The present invention provides a compound represented by Formula (I) or a salt thereof; an LSD1 inhibitor that contains the compound or a salt thereof as an active ingredient; a pharmaceutical composition that contains the compound or a salt thereof; and
METHOD FOR PREDICTING THERAPEUTIC EFFECT OF LSD1 INHIBITOR BASED ON EXPRESSION OF INSM1
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Paragraph 0502, (2020/04/21)
A method for predicting a therapeutic effect of a chemotherapy using an antitumor agent comprising an LSD1 inhibitor in a cancer patient based on an expression level of INSM1 in a sample containing tumor cells isolated from the cancer patient.
ANTI-TUMOR EFFECT POTENTIATOR USING NOVEL BIPHENYL COMPOUND
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Paragraph 0483-0484, (2020/04/21)
An antitumor formulation comprising a biphenyl compound having LSD1 inhibitory activity or a salt thereof and one or more other antitumor agents that are administered in combination, the compound being represented by Formula (I): wherein ring A, ring B, R
COMPOUNDS FOR TREATING RESPIRATORY DISEASE
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Page/Page column 144-145, (2020/12/30)
Compounds of general formula (I) and their tautomeric forms all enantiomers and isotopic variants and salts and solvates thereof: Formula (I), wherein (AA) represents a single or a double bond and R1, R2, X1, X2, X3, X4, X5, Y and Z are as defined herein; are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A.
MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
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Page/Page column 55; 54; 67-68, (2020/01/08)
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
NOVEL BIPHENYL COMPOUND OR SALT THEREOF
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Paragraph 0455, (2018/10/15)
A compound or a salt thereof represented by Formula (I). An LSD1 inhibitor containing the compound or a salt thereof as an active ingredient. A pharmaceutical composition containing the compound or salt thereof. An antitumor agent containing the compound
Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742
Yu, Wensheng,Zhou, Guowei,Coburn, Craig A.,Zeng, Qingbei,Tong, Ling,Dwyer, Michael P.,Hu, Bin,Zhong, Bin,Hao, Jinglai,Ji, Tao,Zan, Shuai,Chen, Lei,Mazzola, Robert,Kim, Jae-Hun,Sha, Deyou,Selyutin, Oleg,Rosenblum, Stuart B.,Lavey, Brian,Nair, Anilkumar G.,Heon Kim, Seong,Keertikar, Kerry M.,Rokosz, Laura,Agrawal, Sony,Liu, Rong,Xia, Ellen,Zhai, Ying,Curry, Stephanie,McMonagle, Patricia,Ingravallo, Paul,Asante-Appiah, Ernest,Chen, Shiying,Kozlowski, Joseph A.
, p. 4851 - 4856 (2016/09/13)
As part of an ongoing effort in NS5A inhibition at Merck we now describe our efforts for introducing substitution around the tetracyclic indole core of MK-8742. Fluoro substitution on the core combined with the fluoro substitutions on the proline ring improved the potency against GT1a Y93H significantly. However, no improvement on GT2b potency was achieved. Limiting the fluoro substitution to C-1 of the tetracyclic indole core had a positive impact on the potency against the resistance associated variants, such as GT1a Y93H and GT2b, and the PK profile as well. Compounds, such as 62, with reduced potency shifts between wild type GT1a to GT2b, GT1a Y93H, and GT1a L31V were identified.
SUBSTITUTED FUSED ARYL AND HETEROARYL DERIVATIVES AS PI3K INHIBITORS
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Page/Page column 107, (2011/07/07)
The present invention provides fused aryl and heteroaryl derivatives of Formula I that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases
