69879-22-7Relevant academic research and scientific papers
Preparation method of small molecule tyrosine kinase inhibitor
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Paragraph 0098-0101, (2021/09/29)
The invention provides a preparation method of a small molecule tyrosine kinase inhibitor. , The compound II is subjected to a condensation reaction with the compound I, and then the ester is reduced to an aldehyde using a reducing agent, and the compound V product and the condensation reaction are reacted to obtain a compound. The preparation method disclosed by the invention is easy to obtain. The method has the advantages of mild reaction, environment friendliness, suitability for industrial production and certain safety.
CRYSTAL OF PYRIDO[3,4-D]PYRIMIDINE DERIVATIVE OR SOLVATE THEREOF
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Paragraph 0213-0216, (2021/09/10)
Provided is a crystal of a novel pyrido[3, 4-d]pyrimidine derivative having excellent CDK 4/6 inhibitory activity. A crystal of a compound represented by formula (I). In the formula, R1 represents a hydrogen atom or a C1-3 alkyl group; R2 represents a hydrogen atom or an oxo group; L represents a single bond or a C1-3 alkylene group; and X represents CH or N.
CRYSTAL FORM, SALT TYPE OF SUBSTITUTED 2-HYDRO-PYRAZOLE DERIVATIVE AND PREPARATION METHOD THEREFOR
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, (2019/07/10)
A crystal form and a salt type of a substituted 2-hydro-pyrazole derivative, preparation method therefor, and use of the crystal form and the salt type in preparation of a medicament for treating cancers such as breast cancer, lung cancer and the like.
PYRIDO[3, 4-D]PYRIMIDINE DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Paragraph 0180; 0181, (2019/10/16)
The purpose of the present invention is to provide a compound that has excellent CDK4/6 inhibitory activity. The present invention is a compound represented by formula (I) or a pharmaceutically acceptable salt of the compound.
AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF
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Paragraph 0458; 0489, (2018/12/02)
The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.
PYRIDO[3,4-d]PYRIMIDINE DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Paragraph 0177; 0178, (2018/04/19)
The purpose of the present invention is to provide a compound having an excellent CDK4/6 inhibiting activity. The present invention is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
(E)-3-Heteroarylidenechroman-4-ones as potent and selective monoamine oxidase-B inhibitors
Desideri, Nicoletta,Proietti Monaco, Luca,Fioravanti, Rossella,Biava, Mariangela,Yá?ez, Matilde,Alcaro, Stefano,Ortuso, Francesco
, p. 292 - 300 (2016/05/10)
A series of (E)-3-heteroarylidenechroman-4-ones (1a-r) was designed, synthesized and investigated in vitro for their ability to inhibit the enzymatic activity of both human monoamine oxidase (hMAO) isoforms, hMAO-A and hMAO-B. All the compounds were found to be selective hMAO-B inhibitors showing IC50 values in the nanomolar or micromolar range. (E)-5,7-Dichloro-3-{[(2-(dimethylamino)pyrimidin-5-yl]methylene}chroman-4-one (1c) was the most interesting compound identified in this study, endowed with higher hMAO-B potency (IC50 Combining double low line 10.58 nM) and selectivity (SI > 9452) with respect to the reference selective inhibitor selegiline (IC50 Combining double low line 19.60 nM, IC50 > 3431). Molecular modelling studies were performed for rationalizing at molecular level the target selective inhibition of our compounds, revealing a remarkable contribution of hydrogen bond network and water solvent.
2-BENZOYLIMIDAZOPYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
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Page/Page column 7, (2009/06/27)
The present invention is related to a compound of formula (I) wherein R1, R2, R3, R4 and X are as defined herein, or an acid-addition salt thereof, its preparation and therapeutic use in the treatment or prevention of diseases involving the Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.
BASIC AMINE COMPOUND AND USE THEREOF
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Page/Page column 55, (2010/11/24)
Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A 1 and A 2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH 2 , C(=O), NR 11 , or CHR 35 and D represents a group represented by the following formula (6): where Q represents a single bond, NR 12 , or a group represented by the formula (13): and Y represents a group represented by the following formula (7) : where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents -NR 25 R 26 ; and R 1 to R 26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.
Heteroarylethanol-pyridylalkylamines for controlling animal growth
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, (2008/06/13)
A compound for promoting livestock production and for controlling obesity in humans and animals, of the formula STR1 in which A represents =CH-- or =N--, R0 represents hydrogen or methyl, R1 and R3 each independently represents hydrogen, hydroxyl, halogen, cyano, alkyl, halogenoalkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio, NHSO2 -alkyl, R2 represents hydrogen, hydroxyl, alkoxy or the radical --NR5 R6, R4 represents hydrogen, C1 -C10 -alkyl which is optionally substituted by hydroxyl, halogen, alkoxy, acyloxy or the radical --NH7 R8, or represents the radical COR9 or the radical --O--Z--R10, Z represents C1 -C10 -alkylene, -alkenylene or alkynylene, R5 represents hydrogen or alkyl, R6 represents hydrogen, alkyl, halogenoalkyl or acyl, or R5 and R6 together with the adjoining N atom form a saturated or unsaturated heterocyclic 4-, 5- or 6-membered ring, R7 and R8 each independently represents hydrogen, optionally substituted alkyl, optionally substituted aryl, R9 represents hydroxyl, alkoxy or the radical --NR7 R8, R10 represents hydroxyl, alkoxy, acyloxy, optionally substituted aryloxy or aralkyloxy, with the substituent R4 and the alkylamino group in the pyridyl ring of the formula I being in the p position with respect to one another, or a physiologically tolerated salt thereof, or, if A represents nitrogen, optionally the N-oxide thereof.
