摘要:
A novel cyclic compound having a 4-pyridylalkylthio group having an (un)substituted amino group introduced therein or a salt of the compound. They are useful as a medicine. The cyclic compound is a compound represented by the following formula [I], which is useful for the treatment of diseases in which angiogenesis participates. In the following formula [I], ring A represents a benzene ring or a 5- or 6-membered aromatic heterocycle optionally fused with a cycloalkane ring; B represents alkylene; R1 and R2 each represents H, (substituted) aryl, (substituted) heterocyclic group, etc.; R3 and R4 each represents H, (substituted) alkyl, (substituted) cycloalkyl, -Z-R5, etc.; R5 represents (substituted) alkyl, (substituted) aryl, (substituted) heterocyclic group, etc.; X and Y each represents H, etc.; Z represents -CO-, -COO-, -CONR6-, -SO2-, etc.; R6 represents H, etc.; p is 0, 1, or 2; and q is 0 or 1.
摘要:
An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; R 1 represents a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, an amino group or the like; p represents an integer of 0 to 5; R 2 represents a halogen atom, an alkyl group, a hydroxy group or the like; q represents an integer of 0 to 2; R 3 represents a hydrogen atom, an alkyl group, an alkenyl group or the like; R 4 and R 5 represent a hydrogen atom or the like; R 6 represents a hydrogen atom or the like; A represents an alkylene group or the like; and R 7 represents OR 8 , NR 8 R 9 , SR 8 , S (O) R 8 or S (O) 2 R 8 , wherein R 8 represents an aryl group, a heterocyclic group or the like and R 9 represents a hydrogen atom or the like.
摘要翻译:本发明的目的是研究新型1,2-二氢喹啉衍生物的合成并找到该衍生物的药理作用。 由通式(1)表示的化合物或其盐在治疗糖皮质激素受体相关疾病方面是有效的。 在该式中,环X表示苯环或吡啶环; R 1表示卤素原子,烷基,羟基,烷氧基,氨基等; p表示0〜5的整数, R 2表示卤素原子,烷基,羟基等; q表示0〜2的整数, R 3表示氢原子,烷基,烯基等; R 4和R 5表示氢原子等; R 6表示氢原子等; A表示亚烷基等; 和R 7表示OR 8,NR 8 R 9,SR 8,S(O)R 8或S(O)2 R 8,其中R 8表示芳基,杂环基等,R 9表示氢 原子等。
摘要:
The present invention relates to a synthesis study of novel cyclic compounds having a quinolylalkylthio group represented by the formula (1), and pharmacological actions of the compounds.
In the formula, the ring X represents:
which may have halogen and/or alkyl; R 1 and R 2 independently represent hydrogen, alkyl, cycloalkyl, aryl or a (non) aromatic heterocycle; R 3 represents qinolyl; A represents sulfur, sulfinyl or sulfonyl; and B represents alkylene.
摘要翻译:本发明涉及具有由式(1)表示的喹啉基烷硫基的新型环状化合物的合成研究以及该化合物的药理作用。 在该式中,环X表示:其可具有卤素和/或烷基; R 1和R 2独立地表示氢,烷基,环烷基,芳基或(非)芳族杂环; R 3表示喹啉基; A代表硫,亚磺酰基或磺酰基; B表示亚烷基。
摘要:
Disclose is a novel pyrrole derivative having, as substituents, a ureido group, an aminocarbonyl group and a bicyclic group which may have a substituent, or a salt of the derivative. A compound represented by general formula (1) or a salt thereof has an inhibitory activity on the production of interleukin-6, and is therefore useful as a preventive and/or therapeutic agent for a disease associated with interleukin-6, ocular inflammatory diseases and the like. In the formula, R 1 represents a halogen atom, a hydrogen atom, a lower alkyl group which may have a substituent, a formyl group, or a lower alkylcarbonyl group which may have a substituent, R 2 represents a bicyclic hydrocarbon group which may have a substituent or a bicyclic heterocyclic group which may have a substituent, R 3 represents a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, or an acyl group.
摘要:
Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; R 1 represents a halogen atom, a hydrogen atom, a lower alkyl group or the like; R 2 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group, a lower alkynyl group which may have a substituent, a lower cycloalkyl group, an aryl group, a hydroxy group, a lower alkoxy group which may have a substituent or the like; and n represents 0, 1, 2, 3 or the like.
摘要翻译:本发明的目的是研究具有脲基和氨基羰基作为取代基的新型吡咯衍生物或其盐的合成,以发现其衍生物或其盐的药理作用,并找到药物 其通过口服给药对视网膜疾病等具有预防和/或治疗作用。 由通式(1)表示的化合物或其盐对白介素-6的产生具有抑制活性和/或对脉络膜新生血管形成的抑制作用,因此可用作疾病的预防和/或治疗剂 与白细胞介素-6相关,眼炎和/或视网膜疾病。 在该式中,环A表示苯环等; R 1表示卤原子,氢原子,低级烷基等; R 2表示卤素原子,可以具有取代基的低级烷基,低级烯基,可具有取代基的低级炔基,低级环烷基,芳基,羟基,低级烷氧基, 可以具有取代基等; n表示0,1,2,3等。