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A technology of pyridone and derivatives, applied in the field of pyridone derivatives, can solve the problem of no MCH receptor antagonism and the like
Inactive Publication Date: 2007-03-14
บันยิว ฟาร์มาซูติคัล โค แอลทีดี
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[0011] In addition, PCT International Publication No. WO03/68232 pamphlet discloses several pyrido
Method used
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[0511] (1) Preparation of 4-benzyloxypyridine 1-oxide
[0512] Under ice cooling, 20.3 mL of benzyl alcohol was added to a 200 mL DMF suspension of 7.50 g (0.188 mmol) of sodium hydride (60% oily), and the mixture was stirred at room temperature for 1 hour. Under stirring, 25.5 g (182 mmol) of 4-nitropyridine 1-oxide was added in small portions, and the mixture was stirred at room temperature for 1 hour. The solvent was concentrated under reduced pressure, 1 L of chloroform was added to the obtained residue, and the insoluble matter was filtered through 100 g of Celite. The filtrate was concentrated, and then acetone was added to obtain 24.8 g of the title compound (69%).
[0513] (2) Preparation of 4-benzyloxy-1H-pyridin-2-one
[0514] 24.8 g (123 mmol) of 4-benzyloxypyridine 1-oxide was refluxed in 150 mL of acetic anhydride for 1.5 hours. After cooling to room temperature, it was concentrated under redu...
Embodiment 2-10
[0524] In Example 1(5), 2-(dimethylamino)ethanol was replaced with the corresponding compound, and the same operation as in Example 1 was performed to obtain the compound of Example 2-10.
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Abstract
The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R 1 and R 2 may be same or different and stands for H, etc., or R 1 and R 2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X 1 -X 3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X 4 -X 7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y 1 and Y 3 may be same or different and stand for single bond, -0-, -NR-, -S-, etc ; Y 2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z 1 and Z 2 may be same or different and stand for single bond or lower alkylene; or R 1 , L and Z 2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R 1 binds; and Ar stands for aromatic carbocyclic group, etc.
Description
Technical field [0001] The present invention relates to a novel pyridone derivative. The derivative acts as a melanin-concentrating hormone receptor antagonist, and can be used for the prevention, treatment or treatment of various circulatory system diseases, nervous system diseases, metabolic system diseases, reproductive system diseases, respiratory diseases, digestive tract diseases, etc. medicine. Background technique [0002] Melanin-concentrating hormone (hereinafter referred to as "MCH") is a cyclic peptide hormone / neuropeptide that was first isolated from the pituitary gland of salmon by Kawauchi et al. in 1983 [Nature, Vol. 305, p. 321 (1983)]. It is known to functionally antagonize melanocyte stimulating hormone in fish, cause melanin granules in melanocytes to agglutinate, and participate in changes in body color [International Review of Cytology, vol. 126, page 1 (1991); Trends in Endocrinology and Metabolism, Volume 5, Page 120 (1994)]. In addition, in mammals, neuro...
Claims
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