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Reproductive system promoting medicine

An animal and compound technology, applied in the field of medicine of mammalian reproductive system, can solve the problems of no mention of modafinil, the difference of optical isomers, no mention of spermatogenesis effect, etc., so as to prevent low libido, The effect of improving sexual performance and promoting the increase of testicular volume and weight

Inactive Publication Date: 2008-09-17
北京康达成医药技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the patent includes the effects of modafinil and its optical variants in its claims, the description does not mention the specific spermatogenesis effect of the corresponding optical variants of modafinil at all, nor does it mention modafinil Differences in the Actions of Optical Isomers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: the preparation of (+)-2-[(benzhydryl)sulfinyl]acetamide

[0025] a) Preparation of (+)-2-[(diphenylmethyl)sulfinyl]acetic acid (+)-α-methylbenzylamine salt

[0026] Take 27.4g of vortexed benzhydrylsulfinyl acetic acid and add it to a 1000ml three-necked flask, add 500ml of water, add 13g of (+)-α-methylbenzylamine, heat to dissolve, filter while hot, and cool the filtrate naturally. Crystals were precipitated and filtered to obtain the product. This product was recrystallized twice in 300ml of water to give 17g of (+)-2-[(diphenylmethyl)sulfinyl]acetic acid (+)-α-methylbenzylamine salt, m.p.: 148-150°C , α D 20 =+93° (95% ethanol solution).

[0027] b) Preparation of (+)-2-[(benzhydryl)sulfinyl]acetic acid

[0028]Dissolve 17 g of the product obtained in the previous step in 800 ml of water at a temperature of 30-40° C., then add 7 ml of concentrated hydrochloric acid to stir and cool, and filter to obtain white crystals of (+)-2-[(benzhydryl)sulfin...

Embodiment 2

[0033] Embodiment 2: the preparation of (-)-2-[(benzhydryl) sulfinyl] acetamide

[0034] According to the method of European patent EP0233106, the operation is completely the same as in Example 1, except that (-)-α-methylbenzylamine is used instead of (+)-α-methylbenzylamine.

Embodiment 3

[0035] Embodiment 3: (+)-2-[(diphenylmethyl) sulfinyl] acetamide, (-)-2-[(diphenylmethyl) sulfinyl] acetamide and modafinil promote Male mammalian spermatogenesis 1

[0036] a) Animals: normal adult male SD rats, 80 in total, divided into drug group 1 (for (+)-2-[(diphenylmethyl)sulfinyl] acetamide), drug group 2 (for (- )-2-[(diphenylmethyl)sulfinyl]acetamide), 3 drug groups (modafinil) and 4 solvent control groups, 20 rats in each group.

[0037] b) Dosing method: gastric irrigation method, the solvent control group is fed with 3% starch paste solution 2ml / piece / day; The starch paste is prepared into a liquid medicine (2ml / piece / day). Adjust the dosage every two weeks.

[0038] c) Dosage: all drugs are 50 mg / kg / day.

[0039] d) Observation index: put to death after administration for 30 days, each animal gets the sperm, testis, epididymis tail and prostate tissue in the epididymis caudal cavity, observes the following indicators: sperm count and mobility, testis weight; ...

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Abstract

The invention relates to a drug reacting on the reproductive system of the mammalian, in particular to a drug which can be used for improving reproductive ability and sexuality of the male mammalian. The drug is characterized in that: more specifically, the drug is one of optical isomers in the 2-[(diphenylmethyl) sulfinyl] acetamide, namely (+)-2-[(diphenylmethyl) sulfinyl] acetamide and derivatives. The drug has the advantages that: the drug can be used for promoting increase of the quantity and improvement of the quality (such as survival rate, active degree and morphology of the sperm) of the sperm of the male mammalian, increasing the volume and the weight of the testis and improving sexuality; thus the drug can be used for improving reproductive ability and sexuality of the male mammalian and promoting reproductive health.

Description

(1) Technical field [0001] The invention relates to a medicine acting on the reproductive system of mammals, especially a medicine which can be used to improve the fertility and sexual ability of male mammals. More specifically, the present invention relates to (+)-2-[(diphenylmethyl)sulfinyl]acetamide and one of the optical isomers in 2-[(diphenylmethyl)sulfinyl]acetamide and Its derivatives, they can be used to promote the increase of sperm quantity and quality (such as sperm survival rate, mobility, shape, etc.) Ability to promote reproductive health, can be used to prevent and treat infertility, infertility or promote eugenics or prevent and treat low sexual ability. According to WHO regulations, sperm quality mainly includes sperm motility, deformity rate, survival rate, etc. Human is also one of mammals, so all mammals mentioned in this patent include human. (2) Background technology [0002] 2-[(Diphenylmethyl)sulfinyl]acetamide, the common name is Modafinil, the E...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61P15/08
Inventor 林善良李莉郜金军朱兴福陈小花
Owner 北京康达成医药技术有限公司
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