- A balufen green industrial production method (by machine translation)
-
The invention discloses a balufen green preparation method, which belongs to the technical field of drug synthesis. The method to the chlorobenzene as a starting material, by Knoevenagel condensation, alkali hydrolysis, sub-amide, alkali hydrolysis and Hofmann degradation 5 step reaction make the consistent with the clinical pharmaceutical balufen. Raw materials of this invention extremely easy, low cost, simple synthesis operation, are basically all aqueous reaction under the condition of, environmental pollution is very small, high yield, is a brand new industrial production balufen method. (by machine translation)
- -
-
Paragraph 0024; 0029
(2017/05/02)
-
- 2,6-dione-piperazine (piperidine) derivative and its application
-
The invention discloses a 2,6-diketone-piperazine (piperidine) type derivative and an application thereof. The derivative can be applied to preparation of medicines for preventing or treating central nervous system diseases. Animal experiment results show that the derivative has smaller ED50 and stronger action in MK-801-induced high activity and apomorphine-induced climbing animal models as well as has larger ED50 and larger therapeutic indexes in an animal catalepsy model. The derivative is a compound or salt thereof with a general formula (I).
- -
-
Paragraph 0061; 0069
(2016/10/07)
-
- Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands for α1-adrenoceptor subtypes
-
A number of new 4-phenylpiperidine-2,6-diones bearing at the 1-position an ω-[4-(substituted phenyl)piperazin-1-yl]alkyl moiety were designed and synthesized as ligands for the α1-adrenergic receptor (α1-AR) subtypes. Some synthesized compounds, tested in binding assays for the human cloned α1A-, α1B-, and α1D-AR subtypes, displayed affinities in the nanomolar range. Highest affinity values were found in derivatives having a butyl connecting chain between the 4-phenylpiperidine-2,6-dione and the phenylpiperazinyl moieties. 1-[4-[4-(2-Methoxyphenyl)piperazin-1-yl]butyl]-4-phenylpiperidine-2,6- dione (34) showed the best affinity for the α1A-AR (pKi= 8.74) and 10-fold selectivity compared to the other two α1-AR subtypes. Some representative compounds were also tested in order to evaluate their effects on the signal transduction pathway coupled to α1-AR subtypes. They all blocked norepinephrine-induced stimulation of inositol phospholipid hydrolysis, thus behaving as antagonists. Binding data were used to refine a previously developed pharmacophoric model for α1D-ARs. The revised model shows a highly predictive power and could be useful for the future design of high affinity α1D-AR ligands.
- Romeo, Giuseppe,Materia, Luisa,Modica, Maria N.,Pittalà, Valeria,Salerno, Loredana,Siracusa, Maria A.,Manetti, Fabrizio,Botta, Maurizio,Minneman, Kenneth P.
-
experimental part
p. 2676 - 2690
(2011/07/08)
-
