- Heteroaromatic acetamide derivative, preparation and applications thereof
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The present invention provides a heteroaromatic acetamide derivative, a preparation and applications thereof, wherein the derivative comprises a pharmaceutically acceptable salt and/or a solvate thereof. According to the present invention, the experiment results prove that the heteroaromatic acetamide derivative can specifically bind to transient receptor potential ankyrin 1 (TRPA1) and inhibit orreduce the activity of TRPA1, and can be used for treating diseases mediated by TRPA1; and the inhibitor of the present invention further comprises a pharmaceutical composition of the compound, and amethods for preparing the compounds. The derivative has a general formula defined in the specification.
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Paragraph 0030; 0032; 0034-0035
(2019/11/04)
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- Preparing method of N-monosubstituted piperazine compound
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The invention discloses a preparing method of an N-monosubstituted piperazine compound shown in the formula (6). Piperazine monohydrochloride (1) and RX or RCl react in solvent to prepare monosubstituted piperazine dihydrochloride (4) or (5), alkali is added for neutralizing, and the product (6) is obtained through rectification steaming.
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Paragraph 0024; 0025
(2017/06/02)
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- DIARYL-CYCLYLALKYL DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted N-cyclylalkyl-diphenylpropanamide derivatives as shown in formula (1).
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- DIARYL UREA DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
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The invention relates to the use of diaryl urea derivatives for the manufacture of pharmaceutical compositions for the treatment of RET dependent disorders, especially RET dependent tumor diseases. The invention further relates to novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives and their use in the treatment of the animal or human body, especially in the treatment of a protein kinase dependent disease, to pharmaceutical compositions comprising such novel N-[4-pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives and to the use of such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N’-phenyl-urea derivatives for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as tumour diseases.
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Page/Page column 69
(2008/06/13)
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- Use of 2-Oxazolidinones As Latent Aziridine Equivalents. III. Preparation of N-Substituted Piperazines.
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A number of N-aryl and N-alkyl substituted piperazines 1 were prepared from variously substituted 2-oxazolidinone derivatives 3.The method involved treatment of 3 with HBr in glacial acetic acid followed by heating the resulting ring-opened salts 5 in alcoholic solvent.The piperazines 1a-1q were isolated by crystallization in yields ranging from 23-91percent.
- Poindexter, Graham S.,Bruce, Marc A.,LeBoulluec, Karen L.,Monkovic, Ivo
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p. 7331 - 7334
(2007/10/02)
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- Process for making 11-piperazino-diazepines, oxazepines, thiazepines and azepines
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This invention concerns a novel process for the preparation of 6-piperazinyl derivatives of morphantridine and corresponding ring-substituted and hereto analogues thereof, comprising reacting a compound of the formula: SPC1 Wherein A is benzene or thiophene, and X is --CH2 -- or a hetero atom or group, with a complex comprising titanium, zirconium, hafnium or vanadium and a corresponding piperazinyl derivative. The end products are in general known and useful as neuroleptics.
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