1711-88-2Relevant academic research and scientific papers
C5A RECEPTOR MODULATORS
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Page/Page column 90; 91, (2019/08/08)
The present invention relates to derivatives of formula (I) wherein ring A, X, Y, Z, R1, R2, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as C5a receptor modulators.
2,4,6,7-TETRAHYDRO-PYRAZOLO[4,3-D]PYRIMIDIN-5-ONE DERIVATIVES AND RELATED COMPOUNDS AS C5A RECEPTOR MODULATORS FOR TREATING VASCULITIS AND INFLAMMATORY DISEASES
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Page/Page column 104, (2019/08/20)
The present invention relates to derivatives of formula (I) wherein Ring A, X, Y, Z, RA, R1, R2, R3 and R4 are The present invention discloses derivatives of formula (I), wherein Ring A, X, Y, Z, RA, R1, R2, R3 and R4 are as described in the description, and in particular e.g. 2,4,6,7-tetrahydro-pyrazolo[4,3- d]pyrimidin-5-one derivatives and related compounds, their preparation, pharmaceutically acceptable salts thereof, their use as pharmaceuticals, pharmaceutical compositions containing one or more compounds of formula (I), and especially their use as C5a receptor modulators for treating e.g. vasculitis and inflammatory diseases.
Amicarbazone synthesis method
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Paragraph 0016; 0017; 0018, (2017/10/07)
The invention discloses an amicarbazone synthesis method, which comprises: synthesizing tert-butyl isocyanate; synthesizing 5-methyl-1,3,4-oxadiazol-2(3H)-one; synthesizing 4-amino-3-isopropyl-5-oxo-1-H-1,2,4-triazole (triazolinone); adding hydrazine hydrate and a second NaOH solution to a third reactor, uniformly stirring, heating to a temperature of 90-100 DEG C, adding the prepared 5-methyl-1,3,4-oxadiazol-2(3H)-one in a dropwise manner, carrying out a reaction after completing the adding, cooling to a room temperature, adding a second solvent, adjusting the pH value to a neutral pH value, freezing for 2-2.5 h, filtering, washing the filter cake, re-crystallizing, and drying to obtain triazolinone; and synthesizing the amicarbazone, wherein triazolinone, potassium hydroxide, a second catalyst and a third solvent are added to a fourth reactor, the prepared tert-butyl isocyanate is added in a dropwise manner, and a heating reaction is performed to obtain the amicarbazone. According to the present invention, the synthesis method has advantages of mild reaction conditions, no requirement of special equipment, good economy, high total yield and good industrial prospect.
Process for preparing substituted oxadiazolones
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, (2008/06/13)
Substituted oxadiazolones of the formula (I) STR1 in which R represents optionally substituted alkyl, are obtained in good yields and high purity on reacting in a first step carboxylic acids of the general formula (II) with hydrazine hydrate in the presen
