135065-69-9Relevant academic research and scientific papers
HPK1 ANTAGONISTS AND USES THEREOF
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Paragraph 0836; 0837, (2021/03/19)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
DIHYDROPYRIMIDINE COMPOUND AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0189; 0190, (2019/07/18)
The present invention relates to a dihydropyrimidine compound having an antiviral activity, a pharmaceutical composition comprising same, a preparation method therefor and the uses thereof in the prevention or treatment of viral diseases including, but no
Development of the First Generation of Disulfide-Based Subtype-Selective and Potent Covalent Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors
Liu, Yifu,Xie, Zuoquan,Zhao, Dan,Zhu, Jin,Mao, Fei,Tang, Shuai,Xu, Hui,Luo, Cheng,Geng, Meiyu,Huang, Min,Li, Jian
, p. 2227 - 2244 (2017/04/03)
Pyruvate dehydrogenase kinases (PDKs) are overexpressed in most cancer cells and are responsible for aberrant glucose metabolism. We previously described bis(4-morpholinyl thiocarbonyl)-disulfide (JX06, 16) as the first covalent inhibitor of PDK1. Here, on the basis of the scaffold of 16, we identify two novel types of disulfide-based PDK1 inhibitors. The most potent analogue, 3a, effectively inhibits PDK1 both at the molecular (kinact/Ki = 4.17 × 103 M-1 s-1) and the cellular level (down to 0.1 μM). In contrast to 16, 3a is a potent and subtype-selective inhibitor of PDK1 with >40-fold selectivity for PDK2-4. 3a also significantly alters glucose metabolic pathways in A549 cells by decreasing ECAR and increasing ROS. Moreover, in the xenograft models, 3a shows significant antitumor activity with no negative effect to the mice weight. Collectively, these data demonstrate that 3a may be an excellent lead compound for the treatment of cancer as a first-generation subtype-selective and covalent PDK1 inhibitor.
Synthesis of reboxetine intermediate and carnitine acetyltransferase inhibitor via NBS-induced electrophilic multicomponent reaction
Zhou, Jing,Yeung, Ying-Yeung
, p. 4644 - 4649 (2014/06/09)
N-Bromosuccinimide-induced electrophilic multicomponent reaction has been applied to the synthesis of Reboxetine intermediate, a highly potent selective norepinephrine reuptake inhibitor. By simply changing the olefinic partner, the synthesis of a carniti
4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors
Lim, Chae Jo,Oh, Kwang-Seok,Ha, Jae Du,Lee, Jeong Hyun,Seo, Ho Won,Chae, Chong Hack,Kim, Dae-Ghon,Lee, Mi-Jin,Lee, Byung Ho
, p. 4080 - 4083 (2014/09/29)
Erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2 (EphA2) is an attractive therapeutic target for suppressing tumor progression. In our efforts to discover novel small molecules to inhibit EphA2, a class of compound based on 4-substituted quinazoline containing 7-(morpholin-2-ylmethoxy) group was identified as a novel hit by high throughput screening campaign. Structural modification of parent quinazoline scaffolds by introducing substituents on aniline displayed potent inhibitory activities toward EphA2.
TETRAAZA-CYCLOPENTA[A]INDENYL AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 64, (2013/07/05)
The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
8-Substituted isoquinoline derivative and the use thereof
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Page/Page column 145, (2010/11/03)
The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKKβ inhibiting activity and the like and is useful for the prevention and/or treatment of IKKβ-associated diseases or symptoms and the like.
Pleuromutilin derivatives having a purine ring. Part 2: Influence of the central spacer on the antibacterial activity against Gram-positive pathogens
Hirokawa, Yoshimi,Kinoshita, Hironori,Tanaka, Tomoyuki,Nakamura, Takanori,Fujimoto, Koichi,Kashimoto, Shigeki,Kojima, Tsuyoshi,Kato, Shiro
scheme or table, p. 170 - 174 (2009/05/07)
Structural modification of the 4-piperidinethio moiety, as a spacer of the first pleuromutilin analogues 2A and 2B having a purine ring, led to discovery of the novel pleuromutilin derivatives 14B and 17B. These compounds with good solubility in water showed promising in vitro antibacterial activity against various Gram-positive bacteria including MRSA, PRSP, and VRE and have potent in vivo efficacy.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 43, (2008/06/13)
Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
NOVEL CYCLIC AMINOBENZOIC ACID DERIVATIVE
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Page/Page column 55-56, (2010/11/27)
The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or - (CH2)n- (n represents 0,1 or 2) ; X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and -COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.
