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一种酰胺衍生物、药物的技术，应用在酰胺衍生物领域，能够解决没有报道受体拮抗活性IBS有效性等问题
Inactive Publication Date: 2009-03-11
ASTELLAS PHARMA INC
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However, the 5-HT of these compounds has not been reported 2B and 5-HT 7 Receptor antagonist activity and effectiveness against IBS
Method used
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preparation example Construction
[0250] (the fifth preparation method other preparation methods)
[0251] Compounds of the present invention with various functional groups such as amino, carboxyl, amido, hydroxyl, alkylamino, alkoxy, etc., can be obtained by using compounds of the present invention with corresponding nitro, ester, carboxyl, amino, hydroxyl, etc. The starting materials are easily synthesized using methods known to those skilled in the art or their modifications. For example, it can be produced by the following reaction.
[0252] 5-a: Restore (1)
[0253] A compound having an amino group can be prepared by reducing a compound having a nitro group. For example, the reaction can be performed using a hydrogenation reaction using palladium-carbon, Raney nickel, or the like as a catalyst.
[0254] 5-b: Restore (2)
[0255] A compound having a hydroxyalkyl group can be prepared by reducing a compound having an ester group. For example, the reaction can be performed using lithium aluminum hydride...
Embodiment
[0341] Hereinafter, production examples of the compounds of the present invention will be given, and the production methods of the compounds of the present invention will be described in detail, but the present invention is not limited to these examples. In addition, novel compounds are also included in the raw material compounds of the compounds of the present invention, and the production methods of these compounds will be described as production examples.
[0342] In addition, the code|symbol in manufacture example, an Example, and the table|surface mentioned later shows the following meaning (the same applies hereinafter).
[0343] Rex: Manufacturing example number, Ex: Example number, Str: Structural formula, Dat: Physical data, FAB: FAB-MS (POS) (M unless otherwise specified + +1), ESI: ESI-MS (POS) (M unless otherwise specified + +1); NMR: 1 δ (ppm) of characteristic peaks in H-NMR), Sal: Salt (empty column or no description indicates free matter, and the number befor...
manufacture example 1
[0345] Suspend 5.00 g of 4-hydrazinobenzoic acid in 50 ml of ethanol, add 5.6 ml of 3-pentanone and 2.7 ml of sulfuric acid, and stir at 85° C. for 24 hours. After ethanol was distilled off under reduced pressure, water was added to the residue under ice cooling, followed by stirring at that temperature for 30 minutes. The resulting solid was filtered and washed with water to obtain 6.34 g of ethyl 2-ethyl-3-methyl-1H-indole-5-carboxylate as a brown solid.
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Abstract
To provide a compound which can be used for the prevention and / or treatment of a disease associated with a 5-HT2B receptor or a 5-HT7 receptor, particularly for the treatment of irritable bowel syndrome (IBS). It is found that an amide derivative having a nitrogenated bicyclic hetero ring such as an indole or a pharmaceutically acceptable salt thereof has a potent antagonistic effect on both of a 5-HT2B receptor and a 5-HT7 receptor. The compound having an antagonistic effect on both of these receptors shows a better pharmacological activity compared to an antagonist alone which is selective to either of these receptors. Therefore, the compound is useful for the prevention and / or treatment of a disease associated with a 5-HT2B receptor or a 5-HT7 receptor, particularly for the treatment of irritable bowel syndrome (IBS).
Description
technical field [0001] The present invention relates to amide derivatives useful as pharmaceuticals, especially therapeutic drugs for irritable bowel syndrome. Background technique [0002] Serotonin (5-HT) is a monoamine neurotransmitter that exhibits various physiological effects through 5-HT receptors. 5-HT receptors can be divided into 5-HT 1 to 5-HT 7 of 7 families. Especially known 5-HT 2 The receptor has 5-HT 2A , 5-HT 2B and 5-HT 2C 3 subtypes (Non-Patent Document 1). [0003] Irritable bowel syndrome (IBS) is a condition of long-lasting abdominal pain or discomfort. IBS can be divided into diarrhea type, constipation type and mixed type of diarrhea and constipation according to its symptoms. In either type, the literature points to a causal relationship between the pathological state and the amount of 5-HT in the blood. For example, a document (Non-Patent Document 2) pointed out that the postprandial blood 5-HT concentration of patients with diarrhea-type ...
Claims
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