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Carboximide derivatives as useful uro-selective alpha-1A adrenoceptor blockers

A kind of solvate, selected technology, applied in the field of novel carboximide derivatives

Inactive Publication Date: 2005-06-15
RANBAXY LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention relates to novel α 1 - Development of adrenergic receptors that selectively relieve prostatic hypertrophy and essential hypertension without existing alpha 1A - Side effects of AR antagonists

Method used

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  • Carboximide derivatives as useful uro-selective alpha-1A adrenoceptor blockers
  • Carboximide derivatives as useful uro-selective alpha-1A adrenoceptor blockers
  • Carboximide derivatives as useful uro-selective alpha-1A adrenoceptor blockers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0070] Preparation of 1-carboxycyclohex-4-ene-2-[N-{3-(2-ethoxyphenyl)piperazin-1-yl}propyl]carboxamide (Compound 1).

[0071] 2-[3-{4-(2-ethoxyphenyl)piperazin-1-yl}propyl-3a,4,7,7a-tetrahydro-1H-isoindole-1,3(2H )-diketone hydrochloride (0.5g, 1.15mmol) was dissolved in aqueous sodium hydroxide solution (11.5ml, 0.2N) and heated to reflux for about 2 hours. After the reaction, the pH of the reactant was adjusted to about 7 with glacial acetic acid and extracted with chloroform (2×15 ml). The solvent was concentrated under reduced pressure and the crude product was crystallized from chloroform and diethyl ether to give 0.13 g of the title compound (25%), m.pt.128-131°C

[0072] MS m / z 430.5 (MH + )

[0073] IR(KBR cm -1 ): 1645.8 (C=O)

[0074] 1 H NMR (300MHZ, TFA) δ: 1.72-1.74 (3H, d), 2.59 (2H, br s), 2.80 (3H, br s), 2.93-2.99 (1H, d), 3.53 (1H, br s) , 3.69(1H, BRS), 3.86-3.98(m, 4H), 4.47-4.50(6H, m), 4.75-4.79(2H, m), 5.11-5.19(1H, m), 6.00-6.13(2H , BRD), 7.39...

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Abstract

Novel carboximide derivatives, which selectively inhibit binding to the alpha >-1A< adrenergic receptor, a receptor which has been shown to be important in the treatment of benign prostatic hyperplasia. The compounds of the present invention are potentially useful in the treatment of benign prostatic hyperplasia.

Description

field of invention [0001] The present invention relates to some novel carboximide (carboximide) derivatives, it can selectively inhibit and α 1A Binding of adrenergic receptors known to be important in the treatment of benign prostatic hyperplasia. The compounds of the present invention are promising for the treatment of benign prostatic hyperplasia. The present invention also relates to a method for synthesizing the novel compound, a pharmaceutical composition containing the compound, and a method for treating benign prostatic hyperplasia with the compound. Background of the invention [0002] Benign prostatic hyperplasia (BPH) is a non-malignant enlargement of the prostate gland, which is the most common benign tumor in men. About 50% of all men over the age of 65 have some degree of BPH and one-third of these men have clinical symptoms such as bladder outlet blockage (Hieble and Calne, Fed. Proc., 1986; 45: 2601) . Worldwide, benign and malignant disease of the prosta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/04A61K31/495A61P9/12A61P13/08A61P43/00C07C233/36C07C233/62C07D295/13
CPCA61P9/12A61P13/08A61P43/00C07D295/13
Inventor M·萨尔曼G·C·亚达弗S·沙马G·S·卡普科蒂A·楚格J·B·古普塔N·阿南德
Owner RANBAXY LAB LTD
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