88712-56-5Relevant academic research and scientific papers
Compound and its as L-type calcium channel blocker or/and application of acetylcholine esterase inhibitors
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Paragraph 0298-0300; 0302; 0372; 0374; 0482; 0484; 0490, (2016/10/07)
Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament for the treatment of cardiovascular diseases, apoplexy or senile dementia are also disclosed in the present invention.
1,4-dihydropyridine-3,5-dicarboxylate Derivatives And Preparation And Use Thereof
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Paragraph 0121; 0122, (2014/03/21)
The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.
Synthesis and characterization of impurities of barnidipine hydrochloride, an antihypertensive drug substance
Cheng, Zhi-Gang,Dai, Xu-Yong,Li, Li-Wei,Wan, Qiong,Ma, Xiang,Xiang, Guang-Ya
, p. 1344 - 1352 (2014/02/14)
Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm × 4.6 mm, 5 m). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR). The identification of these impurities should be useful for quality control in the manufacture of barnidipine.
1,4-DIHYDROPYRIDINE -3,5-DICARBOXYLATE DERIVATIVES, PREPARATION METHODS AND USES THEREOF
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Paragraph 0106; 0107, (2014/03/25)
The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.
Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of nitrendipine analogues
Zhou, Kai,Wang, Xiao-Meng,Zhao, Yi-Zhi,Cao, Yong-Xiao,Fu, Qiang,Zhang, San-Qi
experimental part, p. 1325 - 1330 (2012/06/04)
The antihypertensive activity of nitrendipine analogues can be improved by properly lengthening its alkyl chain in 3- or 5-position. Nitrendipine and its seven analogues were synthesized, and their antihypertensive activities in spontaneously hypertensive rats (SHR) were evaluated by ig administration. It was found that 5-n-heptyl 3-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4- dihydropyridine- 3,5-dicarboxylate [(±)-5] exhibited the strongest antihypertensive effect amongst eight compounds. (?)-5-nheptyl 3-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine- 3,5-dicarboxylate [(+)-5] was also prepared. Antihypertensive activities of (±)-5 and (?)-5 in SHR were compared. The results showed that (±)-5 and (?)-5 had a higher potency than nitrendipine, and (+)-isomer was 1.79-fold the raceme at a dose of 2 mg/kg. Springer Science+Business Media, LLC 2010.
Synthesis and biological activity of the calcium modulator (R) and (S)-3-methyl 5-pentyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Zhang, Bang-le,He, Wei,Shi, Xin,Huan, Meng-lei,Huang, Qiu-ju,Zhou, Si-yuan
experimental part, p. 805 - 808 (2010/05/18)
An efficient total synthesis of (R) and (S)-3-methyl 5-pentyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate in high optical purities is reported. The useful step is the resolution of racemic 2, 6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid by using commercially available Cinchona alkaloids cinchonidine and quinidine as the resolving agents. Under the optimum conditions, the optical purities for R- and S-enantiomers are extremely high (ee >99.5%). The further dihydropyridine receptor binding activity assay shows that the S-enantiomer is more potent than R-enantiomer both in rat cardiac (approximately 19 times) and cerebral cortex membrane (12 times).
NOVEL PROCESS FOR THE PREPARATION OF LERCANIDIPINE
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Page/Page column 3, (2009/09/26)
The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of
A NOVEL PROCESS FOR THE PREPARATION OF LERCANIDIPINE
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Page/Page column 6-7, (2008/06/13)
The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of
Permanently charged chiral 1,4-dihydropyridines: Molecular probes of L- type calcium channels. Synthesis and pharmacological characterization of methyl (ω-trimethylalkylammonium) 1,4-dihydro-2,6-dimethyl-4-(3- nitrophenyl)-3,5-pyridinedicarboxylate iodide
Peri, Ravikumar,Padmanabhan, Seetharamaiyer,Rutledge, Aleta,Singh, Satpal,Triggle, David J.
, p. 2906 - 2914 (2007/10/03)
We report the synthesis of the single enantiomers of permanently charged dihydropyridine derivatives (DHPs with alkyl linker lengths of two and eight carbon atoms) and their activities on cardiac and neuronal L-type calcium channels. Permanently charged c
Asymmetric N-(3,3-diphenylpropyl)aminoalkyl esters of 4-aryl-2,6- dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acids with antihypertensive activity
Leonardi, Amedeo,Motta, Gianni,Pennini, Renzo,Testa, Rodolfo,Sironi, Giorgio,Catto, Alberto,Cerri, Alberto,Zappa, Marco,Bianchi, Giorgio,Nardi, Dante
, p. 399 - 420 (2007/10/03)
A series of asymmetric 4-aryl-1,4-dihydropyridine-3,5-dicarboxylates characterized by the presence of a 3,3-diphenylpropylamino moiety in one of the ester groups were synthesized. They exhibited remarkable antihypertensive activity in spontaneously hypertensive rats as well as affinity for the 1,4- dihydropyridines binding site labelled by 3H-nitrendipine in the calcium channel. Introduction of this bulky and lipophilic amine confers to the whole series an elevated level of antihypertensive activity and a long duration of action, a structure-dependent modulation of the activity being found only in the subset characterized by the presence of a branched propylene bridge between the ester and the amino groups. The presence of the amino group is essential for oral activity. Out of this series, compound 9u (Rec 15/2375- lercanidipine) was selected for clinical development and obtained marketing authorization as an antihypertensive in several countries.
