摘要:
A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R101–R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10—R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.
摘要翻译:由下式表示的2-亚氨基吡咯烷衍生物:其中环B表示苯环,吡啶环等; R 101为-O-,卤素,C 1-6烷基等; R 5表示氢,C 1-6烷基,C 1-6烷氧基-C 1-6烷基 等等 R 6表示氢,C 1-6烷基,C 1-6烷氧基羰基等; Y 1表示单键,-CH 2 - 等; Y 2表示单键,-CO-等; 和Ar表示氢,由下式表示的基团:其中R 10 -R 14表示氢,C 1-6烷基,羟基 C 1-6烷氧基等; 并且R 11和R 12或R 12和R 13可以键合在一起形成5-8个 - 杂环]等,或其盐。
摘要:
A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R101-R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.
摘要翻译:由下式表示的2-亚氨基吡咯烷衍生物:其中环B表示苯环,吡啶环等; R 101为-O-,卤素,C 1-6烷基等; R 5表示氢,C 1-6烷基,C 1-6烷氧基-C 1-6烷基 等等 R 6表示氢,C 1-6烷基,C 1-6烷氧基羰基等; Y 1表示单键,-CH 2 - 等; Y 2表示单键,-CO-等; 和Ar表示氢,由下式表示的基团:其中R 10 -R 14表示氢,C 1-6烷基,羟基 C 1-6烷氧基等; 并且R 11和R 12或R 12和R 13可以键合在一起形成5-8个 - 杂环]等,或其盐。
摘要:
A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.
摘要:
A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10–R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.
摘要:
A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R101-R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10—R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.
摘要翻译:由下式表示的2-亚氨基吡咯烷衍生物:其中环B表示苯环,吡啶环等; R 101 -R 103代表氢,卤素,C 1-6烷基等; R 5表示氢,C 1-6烷基,C 1-6烷氧基-C 1-6烷基等; R 6表示氢,C 1-6烷基,C 1-6烷氧羰基等; Y 1表示单键,-CH 2 - 等; Y 2表示单键,-CO-等; 并且Ar表示氢,由下式表示的基团:其中R 10 -R 14表示氢,C 1-6烷基,羟基,C 1-6烷氧基等; 和R 11和R 12或R 12和R 13可以键合在一起形成5-至8-元杂环]等,或其盐。
摘要:
A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.
摘要翻译:由下式表示的2-亚氨基咪唑衍生物:其中R 1,R 2和R 3表示氢,任选取代的C 1-6烷基等; R 6表示氢,C 1-6烷基,C 1-6烷氧羰基等; Y 1表示单键,-CH 2 - 等; Y 2表示单键,-CO-等; 并且Ar表示氢,由下式表示的基团:其中R 10 -R 14表示氢,C 1-6烷基,羟基,C 1-6烷氧基等,R 11和R 12 >或R 12和R 13可以键合在一起形成5-至8-元杂环等}或其盐。
摘要:
A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.
摘要:
A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.
摘要:
One embodiment of the present invention is a pharmaceutical composition comprising at least one specific 2-iminopyrrolidine derivative and at least one other compound (B). Another embodiment of the present invention is a pharmaceutical composition comprising at least one specific 2-iminopyrrolidine derivative, which is to be used in combination with at least one other compound (B). According to the present invention, there are provided pharmaceutical compositions capable of treating or ameliorating diseases, such as heart diseases, effectively.
摘要:
The present invention provides methods for evaluating the regulation on prolyl 4-hydroxylase activity. The present invention also provides screening methods using the evaluation methods. Furthermore, the present invention provides methods of screening for compounds that are useful for treating or preventing fibrosis or rheumatoid arthritis. The present invention relates to methods for detecting regulatory activity on the synoviolin ubiquitination of prolyl 4-hydroxylase α subunit (P4HA1). It also relates to methods of screening for compounds with regulatory effect on the ubiquitination activity of synoviolin on P4HA1 based on these methods. Compounds discovered in the screening are useful for treating and/or preventing diseases caused by abnormalities in the prolyl 4-hydroxylase activity, such as fibrosis and rheumatoid arthritis.