91392-33-5Relevant academic research and scientific papers
CHEMOSELECTIVE METHYLENE HYDROXYLATION IN AROMATIC MOLECULES
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Paragraph 0129; 0185, (2020/03/28)
A chemoselective and reactive Mn(CF3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic C—H hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.
Preparation method of apatinib intermediate
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Paragraph 0025-0034, (2020/10/21)
A preparation method of an apatinib intermediate belongs to the technical field of chemical synthesis of medicines. The preparation method comprises the following steps: nitration reaction: dropwise adding 1-phenyl-1-cyclohexonitrile as a compound II into a mixed acid of phosphoric acid, nitric acid and sulfuric acid, and stirring for reaction to obtain an apatinib intermediate primary product asa compound I; and refining: refining the obtained apatinib intermediate primary product by using a refining solvent to obtain an apatinib intermediate finished product serving as a compound I. The usage amount of nitric acid and concentrated sulfuric acid is remarkably reduced, and the pressure on the environment influence is reduced; the purity is high; the preparation cost is reduced; the stepsare simple and reasonable, the operation is convenient, and tedious post-treatment is avoided; and the preparation method is beneficial for obtaining raw material medicines with higher quality.
SOLID DRUG FORM OF N-(2,6-BIS(1-METHYLETHYL)PHENYL)-N'-((1-(4-(DIMETHYLAMINO)PHENYL)CYCLOPENTYL)METHYL)UREA HYDROCHLORIDE AND COMPOSITIONS, METHODS AND KITS RELATED THERETO
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Page/Page column 18, (2016/04/26)
A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.
Apatinib preparation method
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Paragraph 0045; 0048; 0049, (2017/04/28)
The present invention relates to an apatinib preparation method, wherein specifically an organic solvent is selected to perform refining crystallization to obtain the apatinib. The method of the present invention has advantages of simple operation and low cost, and is suitable for large-scale production.
NOVEL BENZAMIDE DERIVATIVES AS MODULATORS OF THE FOLLICLE STIMULATING HORMONE
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Page/Page column 99, (2008/12/04)
The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1 nare defined as in formula I; invention compounds are modulators of follicle-stimulating hormone - ("FSH") which are useful for male and female contraception as well as other disorders modulated by FSH receptor.
INHIBITORS OF C-FMS KINASE
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Page/Page column 33, (2008/06/13)
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, es
1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA INHIBITORS
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Page 233, 235, (2010/02/05)
The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
Inhibitors of Acyl-CoA: Cholesterol Acyltransferase (ACAT). 7. Development of a Series of Substituted N-Phenyl-N'-ureas with Enhanced Hypocholesterolemic Activity
Trivedi, Bharat K.,Purchase, Terri Stoeber,Holmes, Ann,Augelli-Szafran, Corinne E.,Essenburg, Arnold D.,et al.
, p. 1652 - 1659 (2007/10/02)
We recently described our initial structure-activity relationship (SAR) studies on a series of N-phenyl-N'-aralkyl- and N-phenyl-N'-(1-phenylcycloalkyl)ureas as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT).From this series of analogs, compou
Antihyperlipidemic and antiatherosclerotic urea and carbamate compounds
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, (2008/06/13)
Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood
