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A compound, carbamoyl technology, applied in the field of diacylethylenediamine compounds, can solve problems such as no disclosure or implied compounds
Inactive Publication Date: 2012-04-04
ASTELLAS PHARMA INC
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[0016] However, none of the above-mentioned documents disclose or imply the c...
Method used
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preparation example Construction
[0124] This preparation method is a step of converting the carboxyl group of the compound (I-a) prepared by the first preparation method as the compound of the present invention into a formamide group or a bioisostere of the carboxyl group.
[0125] For example, in Z 1 for-CO-NH-SO 2 -C 1-6 Alkyl or -CO-NH-SO 2 -N(C 1-6 alkyl) 2 In the case of , it can be prepared by a fusion reaction with the corresponding sulfonamide; for example, in Z 1 for-CONH 2 In the case of , it can be prepared by a fusion reaction using ammonium chloride, ammonium hydroxide, ammonia solution, etc.; for example, in Z 1 In the case of a tetrazolyl group, after being induced into formamide, it is dehydrated to induce a nitro group by a conventional method, and then reacted with sodium azide to produce it. Alternatively, the carboxyl group can be converted to its bioisostere using methods known to those skilled in the art.
[0126] (Raw material synthesis 1)
[0127]
[0128] (where, A 1 Repr...
Embodiment
[0190] The preparation method of the compound represented by formula (I) or its salt will be described in more detail below based on the examples. Furthermore, the present invention is not limited to the compounds described in the following examples. In addition, the production methods of the raw material compounds are shown in the production examples. In addition, the preparation method of the compound represented by formula (I) is not limited to the preparation method of the specific examples shown below, and the compound represented by formula (I) can be prepared by a combination of these preparation methods or methods known to those skilled in the art. shows the compound.
[0191] In addition, in Examples, Preparation Examples, and the following tables, the following abbreviations are sometimes used.
[0192] Pr: Preparation number (preparation compound with " / Cl" behind the preparation number means that the preparation compound is isolated in the form of hydrochloride, ...
preparation example 1
[0194] Under ice-cooling, ethyl trans-4-hydroxycyclohexanecarboxylate (8g), benzyl 4-hydroxybenzoate (11.69g), 1,1'-(azobiscarbonyl)dipiperidine ( 15.24 g), THF (150 ml) was added dropwise to a mixture of tributylphosphine (14.9 ml), stirred at room temperature for 2 hours, and then stirred at 60° C. for 10 hours. After returning the reaction mixture to room temperature, it was filtered, washed with THF, and the filtrate was concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (hexane:ethyl acetate=85:15) to give benzyl 4-{[cis-4-(ethoxycarbonyl)cyclohexyl]oxy}benzoate 8.55 g of colorless oily substance of base ester.
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Abstract
Disclosed is a compound useful as an anti-obesity agent. Studies have been made on compounds which have a DGAT1 inhibitory activity and are therefore promising active ingredients for pharmaceutical compositions for treating obesity, type-II diabetes, fatty liver and diseases associated with the aforementioned diseases, and it is confirmed that a specific diacylethylenediamine compound has an excellent DGAT1 inhibitory activity. The diacylethylenediamine compound has a DGAT1 inhibitory activity and can be used as a prophylactic and/or therapeutic agent for obesity, type-II diabetes, fatty liver and diseases associated with the aforementioned diseases.
Description
technical field [0001] The present invention relates to diacylethylenediamine compounds useful as active ingredients of pharmaceutical compositions such as pharmaceutical compositions for treating obesity. Background technique [0002] Obesity is a state in which the balance of energy intake and energy consumption is disrupted in the body, and the remaining energy is excessively accumulated in adipose tissue in the form of neutral fat (mainly triglycerides); obesity and resistance Insulin-induced, diabetes, arteriosclerosis, non-alcoholic steatohepatitis, or the onset and development of hypertension and other diseases are closely related. In addition, it is known that accumulation of excess triglyceride in liver, muscle, etc. causes dysfunction in these tissues in addition to adipose tissue. In recent years, obese patients have increased due to changes in lifestyle, however, there are limited therapeutic methods for these obese patients, and the development of new obesity-t...
Claims
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