69879-22-7Relevant articles and documents
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.
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.
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.
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.
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.