摘要:
This invention relates to a flavone derivative represented by the formula (1) or a salt thereof, and also to a medicine containing the same. wherein A represents H, halogen, phenyl, naphthyl, a group of the formula (2) in which X is H or halogen, B is -CH=CH-, -CH=N-, -N(R 7 )- (R 7 : lower alkyl or alkoxyalkyl), -O- or -S-; W represents a single bond, -CH 2 O- or -CH=CH-; at least one of R 1 to R 4 represents -COOH, -CN, alkyloxycarbonyl, tetrazolyl or -CONHR 8 (R 8 : H, lower alkyl or phenylsulfonyl), the remainder thereof individually represent H, halogen, -OH, lower alkyl or lower alkoxyl; R 5 represents H, -OH, lower alkoxyl, -O(CH 2 ) m NR 9 R 10 (R 9 ,R 10 : H or lower alkyl, or coupled together with the adjacent N to form a phthalimido group; m: 1-5), or a group of the formula (3) (n: 1-5, ℓ: 2-3; and R 6 represents H, halogen, lower alkyl or lower alkoxyl. A situation where A is H or halogen, W is a single bond and R 5 is H is excluded. The compound (1) has excellent cys-LT 1 receptor antagonism.
摘要翻译:本发明涉及由式(1)表示的黄酮衍生物或其盐,以及含有该衍生物的药物。 其中A表示H,卤素,苯基,萘基,其中X是H或卤素的式(2)的基团,B是-CH = CH-,-CH = N-,-N(R 7) ) - (R 7:低级烷基或烷氧基烷基),-O-或-S-; W表示单键,-CH 2 O-或-CH = CH-; R 1至R 4中的至少一个表示-COOH,-CN,烷氧基羰基,四唑基或-CONHR 8(R 8:H,低级烷基或苯基磺酰基),其余部分分别表示H, 卤素,-OH,低级烷基或低级烷氧基; R 5表示H,-OH,低级烷氧基,-O(CH 2)m NR 9 R 10(R 9,R 10):H或低级烷基,或与相邻的N至 形成苯二甲酰亚氨基; m:1-5)或式(3)的基团(n:1-5,1:2-3; R 6表示H,卤素,低级烷基或低级烷氧基。 A为H或卤素,W为单键,R 5为H的情况除外。化合物(1)具有优异的cys-LT1受体拮抗作用。
摘要:
This invention relates to a flavone derivative represented by the formula (1) or a salt thereof, and also to a medicine containing the same. wherein A represents H, halogen, phenyl, naphthyl, a group of the formula (2) in which X is H or halogen, B is -CH=CH-, -CH=N-, -N(R 7 )- (R 7 : lower alkyl or alkoxyalkyl), -O- or -S-; W represents a single bond, -CH 2 O- or -CH=CH-; at least one of R 1 to R 4 represents -COOH, -CN, alkyloxycarbonyl, tetrazolyl or -CONHR 8 (R 8 : H, lower alkyl or phenylsulfonyl), the remainder thereof individually represent H, halogen, -OH, lower alkyl or lower alkoxyl; R 5 represents H, -OH, lower alkoxyl, -O(CH 2 ) m NR 9 R 10 (R 9 ,R 10 : H or lower alkyl, or coupled together with the adjacent N to form a phthalimido group; m: 1-5), or a group of the formula (3) (n: 1-5, ℓ: 2-3; and R 6 represents H, halogen, lower alkyl or lower alkoxyl. A situation where A is H or halogen, W is a single bond and R 5 is H is excluded. The compound (1) has excellent cys-LT 1 receptor antagonism.
摘要:
The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
摘要:
The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.
摘要:
The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.