- Method for synthesizing 1-(3-aminopropyl)imidazole from imidazole
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The invention discloses a method for synthesizing 1-(3-aminopropyl)imidazole from imidazole. The method comprises the following steps: a, adding 28-32 parts by weight of the imidazole, 55-65 parts byweight of acrylonitrile, and 0.9-1.1 parts by weight of ethyl acetate into a reaction kettle, rapidly raising the temperature to 42-44 DEG C under sealed conditions, and performing stirring continuously for 22-28min; and introducing a nitrogen gas for cooling until the temperature is -5 DEG C, adding dilute sulfuric acid to adjust the pH value to 2.2-2.4, and performing stirring for 10-20min for precipitating a crystal; b, washing the crystal with saturated salt water, performing vacuum drying, and performing cooling to normal temperature to obtain N-(2-cyanoethyl)imidazole and other steps. The preparation method provided by the invention is scientific and simple, strictly controls the formula ratio, and controls the reaction conditions, the raw materials are easy to obtain, the usage amount of the raw materials is small, the cost is low, and the prepared 1-(3-aminopropyl)imidazole has high purity, a high yield and stable performance, and is suitable for industrialized production.
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Paragraph 0035-0037; 0042-0044; 0049-0051
(2018/04/26)
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- Pyrrole and pyrazole compound of preparation and use as medicaments (by machine translation)
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The invention relates to the field of medical technology, this invention has offered a kind of sulfonamide and nitrogen mixed uncle butane pyrrole and pyrazole compound, including optical isomers, racemic modification, and any combination of the trans isomer or a pharmaceutically acceptable salt thereof, having a structure of formula (I); the invention also provides the preparation method of the compound and its application, in particular in the preparation of anti-tumor drug application. (by machine translation)
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Paragraph 0079; 0080; 0081; 0082
(2018/03/26)
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- Gyrrolone and pyrromonazole compound and its use as medicine
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The present invention belongs to the technical field of medicine. Provided in the present invention is pyrrolidone compounds, including optical isomers, racemates, cis and trans isomers and any combination thereof or pharmaceutically acceptable salts thereof, having a structure as shown in formula (I). The compounds of the present invention can be used as a small molecule inhibitor for p53-MDM2/X protein interactions. The compounds of the present invention can be used to prepare antineoplastic or anti-inflammatory drugs.
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Paragraph 0076-0079
(2016/11/14)
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- CINNAMIC ACID AMIDE DERIVATIVE
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The present invention provides a cinnamic acid amide derivative having an excellent analgesic action. The cinnamic acid amide derivative of the present invention is a compound showing excellent analgesic actions to not only a nociceptive pain model animal but also a neuropathic pain model animal, which is very useful as an agent for treating various pain diseases showing acute or chronic pains or neuropathic pains.
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Paragraph 0060; 0082
(2015/11/24)
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- Encapsulation of a catalytic imidazolium salt into avidin: Towards the development of a biohybrid catalyst active in ionic liquids
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Herein, we report the development of biohybrid catalysts that are capable of catalyzing the aldol reaction. The use of biotinylated imidazolium salts in combination with racemic or enantiomerically pure catalytic anions allowed us to study the adaptive and cooperative positioning of the anionic catalyst inside the protein. Supramolecular encapsulation of the biotinylated catalyst into avidin resulted in good selectivity for the aldol reaction performed in ionic liquid/water mixtures. Biohybrid catalysts capable of catalyzing the aldol reaction are prepared from avidin and biotinylated imidazolium salts with either racemic or enantiomerically pure catalytic anions. Supramolecular encapsulation (see figure) of the biotinylated catalyst in avidin resulted in good selectivities for the aldol reaction when performed in ionic liquid/water mixtures and the adaptive and cooperative positioning of the anionic catalyst inside the avidin protein is discussed. Copyright
- Gauchot, Vincent,Branca, Mathieu,Schmitzer, Andreea
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supporting information
p. 1530 - 1538
(2014/03/21)
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- METHODS OF MODULATING CFTR ACTIVITY
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The invention encompasses methods of modulating CFTR activity in a subject in need thereof comprising administering an effective amount of a compound of Formula (I). The invention also encompasses methods of treating a condition associated with CFTR activity or condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a compound of Formula (I).
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Page/Page column 97; 98
(2015/01/16)
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- Carbamate-appended N-alkylsulfonamides as inhibitors of γ-secretase
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The synthesis and γ-secretase inhibition data for a series of carbamate-appended N-alkylsulfonamides are described. Carbamate 54 was found to significantly reduce brain Aβ in transgenic mice. 54 was also found to possess markedly improved brain levels in transgenic mice compared to previously disclosed 1 and 2.
- Bergstrom, Carl P.,Sloan, Charles P.,Lau, Wai-Yu,Smith, David W.,Zheng, Ming,Hansel, Steven B.,Polson, Craig T.,Corsa, Jason A.,Barten, Donna M.,Felsenstein, Kevin M.,Roberts, Susan B.
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p. 464 - 468
(2008/12/21)
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- A new class of histamine H3-receptor antagonists: Synthesis and structure - Activity relationships of 7,8,9,10-Tetrahydro-6H-cyclohepta[b]quinolines
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The synthesis and biological evaluation of novel cycloheptaquinoline antagonists of the human H3 receptor are described. Two series of compounds, bearing either an amino substituent or an alkyne linker at the 11-position, were investigated. Modifications of the amino substituents, optimization of chain length and the effect of conformational restraints are described. Several compounds with high affinity and selectivity for the H3 receptor were discovered.
- Turner, Sean C.,Esbenshade, Timothy A.,Bennani, Youssef L.,Hancock, Arthur A.
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p. 2131 - 2135
(2007/10/03)
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- 2-aminobenzoxazole derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminobenzoxazole derivative compounds of the following formula: wherein R1 to R4 and Z have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminobenzoxazole derivative compounds.
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- 4-unsubstituted dihydroisoquinolinone derivatives and combinatorial libraries thereof
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The present invention relates to novel dihydroisoquinolinone (DHQ) derivative compounds of the following formula: wherein R1to R7, X, Y, Z, b, c and d have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing DHQ derivative compounds.
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- 2-aminopyridine derivatives and combinatorial libraries thereof
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The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1to R5have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
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- Method for inhibiting advanced glycosylation of proteins using aminosubstituted imidazoles
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The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging), Accordingly, a composition is disclosed which comprises 2-aminoimidazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation, The method comprises contacting the target protein with the composition, Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
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- N-(Substituted phenyl)-N'-[(1H-imidazol-1-yl) and (1H-1,2,4-triazol-1-yl)alkyl]ureas
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N-(Substituted phenyl)-N'-[(1H-imidazol-1-yl) and (1H-1,2,4-triazol-1-yl)alkyl]ureas which are inhibitors of thromboxane synthetase enzyme.
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- N-[(1H-imidazol-1-yl) and (1H-1,2,4-triazol-1-yl)-alkyl]benzenesulfonamides and thromboxane synthetase/antihypertensive compositions
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This invention concerns novel N-[(1H-imidazol-1-yl), (1H-1,2,4-triazol-1-yl) and (3-pyridyl)alkyl]benzenesulfonamides which are useful as inhibitors of thromboxane synthetase enzyme and/or as antihypertensive agents.
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- Thromboxane synthetase enzyme inhibiting N-[(1H-imidazol-1-yl) and (1H-1,2,4-triazol-1-yl)alkyl]pyridinecarboxamides
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This invention concerns novel N-[(1H-imidazol-1-yl) and (1H-1,2,4-triazol-1-yl)alkyl]pyridinecarboxamides which are useful as inhibitors of thromboxane synthetase and/or as hypotensive agents in the treatment of hypertension and myocardial ischemia.
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- Substituted N-[ω-(1H-imidazol-1-yl)alkyl]-amides
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This disclosure describes novel N-[ω-(1H-imidazol-1-yl)alkyl]amides which possess the property of inhibiting the enzyme thromboxane synthetase.
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- meso (Methine) Functionalization of Octa-alkylporphyrins
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meso-Acetoxymethylocta-alkylporphyrins react with a variety of nucleophiles such as alcohols (to give the corresponding alkoxymethylporphyrins), amines (yielding aminomethylporphyrins), and Grignard reagents (to give meso-alkylporphyrins).Treatment of the meso-acetoxymethylporphyrins with thiol reagents accomplishes reduction to give the meso-methylporphyrin rather than the sulphide.Making use of these meso-functionalization reactions, potential cytochrome P450 models and a model for the tense form of hemoglobin are synthesized.
- Smith, Kevin M.,Bisset, Graham M. F.
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p. 2625 - 2630
(2007/10/02)
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- N-(Heterocycl ic-alkyl)-9-xanthenylamines
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The compounds are N-(imidazolylalkyl, imidazolinylalkyl and tetrahydropyrimidylalkyl)-9-xanthenylamines which have gastric acid secretion inhibitory activity.
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