- PDIA4 INHIBITORS AND USE THEREOF FOR INHIBITING ?-CELL PATHOGENESIS AND TREATING DIABETES
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Disulfide-Isomerase A4 (PDIA4) inhibitors and use thereof for inhibiting pancreatic β-cell pathogenesis and treating diabetes are disclosed. Drug candidates that inhibit PDIA4 with IC50 values ranging from 4 μM to 300 nM are identified. The compounds are highly active in augmenting insulin secretion from pancreatic β-cells. The representative compound No. 8 (4,5-dimethoxy-2-propiolamidobenzoic acid), alone or in combination with metformin, is effective in preserving pancreatic β-cell function, treating and/or reversing, returning blood glucose concentration to a normal level in a diabetic.
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Page/Page column 14-15
(2021/06/11)
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- Quantitation and Taste Contribution of Sensory Active Molecules in Oat (Avena sativa L.)
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A total of 59 taste-active molecules were quantitated and then rated for their individual taste impact on the basis of dose-over-threshold factors in oat flour (Avena sativa L.). A sensitive high-performance liquid chromatography-tandem mass spectrometry
- Dawid, Corinna,Günther-Jordanland, Kirsten,Hofmann, Thomas
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p. 10097 - 10108
(2020/10/26)
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- QUINAZOLINONE COMPOUNDS
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New quinazolinone compounds are disclosed, as well as pharmaceutical compositions containing quinazolinones and methods for the treatment of diseases and conditions associated with mitochondrial dysfunction.
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Paragraph 0103; 0107
(2020/09/12)
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- Preparation method of targeted drug AZD3759 intermediate
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The invention discloses a preparation method of a targeted drug AZD3759 intermediate, which comprises the following steps of: firstly, 6-nitro veratric acid is hydrolyzed under alkaline conditions toobtain 2-nitro-4-methoxy-5-hydroxybenzoic acid, the 2-nitro-4-methoxy-5-hydroxybenzoic acid is then reduced by hydrazine hydrate under the action of catalyst ferric chloride hexahydrate activated carbon mixture to obtain 2-amino-4-methoxy-5-hydroxybenzoic acid, 2-amino-4-methoxy-5-hydroxybenzoic acid is reacted with formamidine acetate to obtain 4,6-dihydroxy-7-methoxyquinazoline, 4,6-dihydroxy-7-methoxyquinazoline is reacted with acetyl chloride under alkaline conditions to obtain 4-hydroxyl-6-acetoxy-7-methoxyquinazoline, finally 4-hydroxyl-6-acetoxy-7-methoxyquinazoline is reacted with 3-chlorine-2-fluoroaniline by Mitsunobu reaction under the action of triphenylphosphine and azo reagent to obtain 4-[(3-chloro-2-fluorophenyl)amino]-6-acetoxy-7-methoxyquinazoline. The invention reduces the synthesis steps, reduces the use of harmful compounds, reduces the production cost and optimizes the production operation.
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Paragraph 0048-0050
(2020/01/08)
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- A preparation method of gefitinib (by machine translation)
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The present invention relates to organic chemical and medical technology field, in particular relates to a preparation method of gefitinib. The present invention provides a preparation method of gefitinib, obtained by formula I compounds, the formula I compound preparation method comprises the following steps: nitration reaction, oxidation reaction, selective demethylation reaction, reduction reaction, a cyclization reaction, phenolic hydroxyl acetylation reaction. The present invention provides a preparation method can at the same time reducing the cost, it is easy for the refined purification, easy preparation and control of related impurities, the overall preparation process routes are greatly optimized, is suitable for industrial scale production. (by machine translation)
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Paragraph 0101-0103
(2019/05/16)
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- A 3, 4 - dihydro -7 - methoxy -4 - [...] -6 - ethoxylate ester preparation method (by machine translation)
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The present invention relates to organic chemical and medical technology field, in particular to a 3, 4 - dihydro - 7 - methoxy - 4 - [...] - 6 - ethoxylate ester preparation method. The present invention provides a gefitinib 3, 4 - dihydro - 7 - methoxy - 4 - [...] - 6 - ethoxylate ester preparation method comprises the following steps: nitration reaction, oxidation reaction, selective demethylation reaction, reduction reaction, a cyclization reaction, phenolic hydroxyl acetylation reaction. Preparation method provided by the invention can at the same time reducing the cost, it is easy for the refined purification, easy preparation and control of related impurities, the overall preparation process routes are greatly optimized, is suitable for industrial scale production. (by machine translation)
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Paragraph 0076-0078
(2019/05/16)
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- Novel quinazoline inhibitor
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The present invention relates to a novel quinazoline inhibitor, and disclose a compound represented by a formula (I) and a pharmaceutically acceptable salt thereof, a method for preparing the compoundrepresented by the formula (I) and the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a therapeutically effective amount of the compound represented by the formula(I) or the pharmaceutically acceptable salt thereof, and uses of the compound represented by the formula (I) and the pharmaceutically acceptable salt thereof. The formula (I) is defined in the specification.
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Paragraph 0183-0186
(2018/11/03)
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- EGFR PROTEOLYSIS TARGETING CHIMERIC MOLECULES AND ASSOCIATED METHODS OF USE
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The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 00558; 00559
(2018/07/29)
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- QUINAZOLINE INHIBITORS OF ACTIVATING MUTANT FORMS OF EPIDERMAL GROWTH FACTOR RECEPTOR
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The invention relates to compounds of formula(I), or a pharmaceutically acceptable salt thereof: Formula (I) which possess inhibitory activity against activating mutant forms of EGFR,and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti- cancer effect in a warm-blooded animal such as man.
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Page/Page column 35-36
(2014/09/29)
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- Quinazoline Inhibitors of activating mutant forms of Epidermal Growth Factor Receptor
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The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
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Paragraph 0214-0215
(2014/09/29)
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- CYCLOHEXYLOXY-SUBSTITUTED HETEROCYCLICS, MEDICINES CONTAINING THESE COMPOUNDS AND METHOD FOR THE PRODUCTION THEREOF
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The present invention relates to cyclohexyloxy-substituted heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organi
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- BICYCLIC HETEROCYCLES, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF, AND METHOD FOR PRODUCTION OF SAME
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The present invention relates to bicyclic heterocycles of general formula the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable p
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- BICYCLIC HETEROCYCLES, DRUGS CONTAINING SAID COMPOUNDS, USE THEREOF, AND METHOD FOR PRODUCTION THEREOF
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The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb and Rc are defined as in claim 1, their tautomers, their stereoisomers, their mixtures and their salts, in particular their physiolog
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Page/Page column 14
(2010/02/17)
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- Bicyclic heterocycles, medicaments containing these compounds, their use and process for preparing them
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The present invention relates to bicyclic heterocycles of the general formula (I), their tautomers, their stereoisomers, their mixtures and their salts, in particular physiologically tolerable salts with inorganic or organic acids, which have valuable pha
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Page/Page column 5
(2009/12/24)
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- Bicyclic heterocycles, drugs containing said compounds, the use thereof and method for preparing same
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The present invention relates to bicyclic heterocycles of general formula their tautomers, their stereoisomers, their mixtures and their salts, in particular their physiologically acceptable salts with inorganic or organic acids, which have valuable pharmacological properties, in particular an inhibitory action on the signal transduction mediated by tyrosine kinases, their use for the treatment of illnesses, in particular of tumoral diseases and of benign prostatic hyperplasia (BPH), of diseases of the lung and of the airways, and the preparation thereof.
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Page/Page column 6
(2010/11/27)
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- 2- (4-0X0-4H-QUINAZ0LIN-3-YL) ACETAMIDES AND THEIR USE AS VASOPRESSIN V3 ANTAGONISTS
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The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
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Page/Page column 35
(2010/11/23)
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- Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors
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Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.
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Page/Page column 11
(2008/06/13)
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- Solid-phase synthesis of 6-hydroxy-2,4-diaminoquinazolines
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A new method for the solid-phase synthesis of 6-hydroxy-2,4- diaminoquinazolines has been developed. The synthesis utilizes solid-phase bound 6-hydroxy-2,4-dichloroquinazoline as a key intermediate. Sequential substitution of the two chlorines furnishes t
- Wéber, Csaba,Bielik, Attila,Demeter, ádám,Borza, István,Szendrei, Gy?rgyi I.,Keseru, Gy?rgy M.,Greiner, István
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p. 9375 - 9380
(2007/10/03)
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- BICYCLIC HETEROCYCLES, DRUGS CONTAINING SAID COMPOUNDS, THE USE THEREOF AND METHOD FOR PREPARING THE SAME
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The invention relates to the bicyclic heterocycles of general formula (I), wherein R, R, R, R, X and n are defined as in claim 1, to their tautomers, stereoisomers, mixtures and salts thereof, especially the physiologically acceptable salts thereof with inorganic or organic acids. The inventive compounds have valuable pharmacological properties, especially they inhibit tyrosinkinase-mediated signal transduction. The invention also relates to the use of said compounds for treating diseases, especially tumor diseases and benign prostatic hyperplasia (BPH), diseases of the lung and respiratory tracts, and to the production of these compounds.
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Page/Page column 22-23
(2010/02/09)
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