154650-16-5Relevant academic research and scientific papers
Preparation method of 4-bromo-5-methyl-1H-indazole
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Paragraph 0007; 0022-0025; 0032-0035; 0040-0043, (2021/02/06)
The invention discloses a preparation method of 4-bromo-5-methyl-1H-indazole, wherein the preparation method comprises the specific steps: (1) reacting a compound (II) in the presence of lithium diisopropylamide to generate a lithium reagent, and reacting
Design, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors
Dong, Junmin,Pan, Xuan,Yang, Ying,Zhang, Guangyan,Xiao, Zhiyan,Liu, Zhanzhu
, (2021/06/22)
A series of exiguamine A analogues were designed and synthesized via 15 steps. Their inhibitory activities against IDO1 were tested and the structure-activity relationships were studied. Most compounds exhibited potent IDO1 inhibitory activities with IC50 values at the level of 10?7–10?8 M. Compound 21f was the most potent IDO1 inhibitor with an IC50 value of 65.3 nM, which was comparable with the positive control drug epacadostat (IC50 = 46 nM). Moreover, compound 21f showed higher selectivity for IDO1 over tryptophan 2,3-dioxygenase (TDO) and no cytotoxicity at its effective concentration, rending it justifiable for further optimization and evaluation.
INHIBITING HUMAN INTEGRIN α4β7
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Page/Page column 163; 198; 199, (2021/04/23)
Disclosed are small molecule antagonists of human α4β7 integrin, and methods of using them to treat a number of diseases and conditions.
QUINOXALINE DERIVATIVES
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Page/Page column 84, (2021/07/24)
The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
Dihydroisocoumarin derivative and preparation method and application thereof
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Paragraph 0039-0042; 0061-0065, (2022/01/10)
The present invention discloses a dihydroisocoumarin derivative and preparation method and application thereof, the dihydroisocoumarin derivative having a structure as shown in formula (I) or (II). The method of preparing dihydroisocoumarin derivatives of
2-(2-ACRYLOYL-2,6-DIAZASPIRO[3.4]OCTAN-6-YL)-6-(1H-INDAZOL-4-YL)-BENZONITRILE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF G12C MUTANT KRAS PROTEIN FOR INHIBITING TUMOR METASTASIS
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Page/Page column 135, (2020/05/28)
The present invention provides e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(lH-indazol-4-yl)-benzonitrile and e.g. 2-(2-acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-6-(1H-indazol-4-yl)- benzonitrile derivatives and related compounds of formula (I) as inhibitors of G12C mutant KRAS protein for treating tumor metastasis. The present description discloses exemplary compounds (e.g. pages 53 to 90; table 1; compounds I-1 to I-141), pharmacological data (e.g. page 125 to 128; table 2; example 1) and synthesis thereof (e.g. pages 129 to 143; examples 2 to 7). Exemplary compounds are e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(5-methyl-1H-indazol-4-yl)-4- morpholinobenzonitrile (example 2; compound I-1) and 6-(2- acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-3-methoxy-2-(5-methyl-1H- indazol-4-yl)-4-morpholinobenzonitrile (example 7; compound I-84).
COVALENT INHIBITORS OF KRAS
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Page/Page column 189, (2018/12/13)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1, R2a,
BORON-CONTAINING SMALL MOLECULES
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Paragraph 0309, (2017/09/19)
Compounds, pharmaceutical formulations, and methods of treating bacterial infections are disclosed.
(Aza)pyridopyrazolopyrimidinones and indazolopyrimidinones and their use
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Paragraph 0694 - 0697, (2015/05/13)
The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
(AZA)PYRIDOPYRAZOLOPYRIMIDINONES AND INDAZOLOPYRIMIDINONES AS INHIBITORS OF FIBRINOLYSIS
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Page/Page column 125, (2015/05/26)
The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
