摘要:
Novel isoquinoline derivatives of the general formula ##STR1## wherein R represents a lower alkyl group, a lower cycloalkyl group, or a group of the formula ##STR2## in which R.sup.2 represents a hydrogen atom, a halogen atom, a methyl group, a trifluoromethyl group, a methoxy group, a methylamino group or a dimethylami no group;R.sup.1 represents a hydrogen atom or a lower alkyl group; andY represents a carboxyl group, a cyano group, a carbamoyl group, a lower alkoxycarbonyl group or a lower alkylaminocarbonyl group;or a salt thereof; a process for the production thereof.The above compound is useful as an anti-inflammatory and analgesic agent.
摘要:
A compound represented by the formula ##STR1## wherein R.sup.1 represents a hydroxyl group, an alkanoyloxy group or a group of the formula ##STR2## in which R.sup.2 represents a hydrogen atom or a lower alkyl group, and R.sup.3 represents a hydrogen atom, a lower alkyl group, an alkanoyl group, a phenyl group, a carbamoyl group or a thiocarbamoyl group, or a salt thereof.The said compound can be prepared by reacting a compound represented by the formula ##STR3## with a compound of the formulaNH.sub.2 --R.sup.1 (III)wherein R.sup.1 is as defined hereinabove, or a salt thereof, and as required, alkanoylating the resulting compound of formula (I) in which R.sup.1 represents a hydroxyl group or an amino group, and as required, converting the resulting compound of formula (I) in which R.sup.1 is the group ##STR4## into its salt, and is useful for the treatment of inflammation, pain or rheumatism.
摘要:
A compound of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a methoxy group, and A is a C.sub.1 -C.sub.4 alkylene group, or a pharmaceutically acceptable salt thereof. This compound is useful as a medicine, particularly as a lipoxygenase inhibitor for polyunsaturated fatty acids.
摘要:
A compound represented by the formula ##STR1## wherein R.sub.1 represents a lower alkyl group; each of R.sub.2 and R.sub.3 represents an alkyl group having 1 to 3 carbon atoms; and each of R.sub.4, R.sub.5 and R.sub.6 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkanoyloxy group, an aralkyloxy group, a lower alkylthio group, a lower haloalkyl group, a hydroxyl group, a cyano group, a nitro group, an amino group, a mono- or di-(lower alkyl or aralkyl)amino group or a group of the formula ##STR2## in which R.sub.7 represents a lower alkylene group having at least 2 carbon atoms, one of R.sub.8 and R.sub.9 represents a hydrogen atom or a lower alkyl group and the other represents a lower alkyl group, and R.sub.10 represents a hydrogen atom or a lower alkyl group; or any two of R.sub.4, R.sub.5 and R.sub.6 which are adjacent to each other, together, represent a lower alkylenedioxy group, and a salt thereof; and a process for production thereof. This compound has 5-lipoxygenase inhibiting activity and is useful as a medicament.
摘要:
Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)-(A)n-Y, —CH2—CH(R4)-(A)n-Y, —CO-B1-A-Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor α-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases
摘要翻译:公开了由式(I)表示的取代的吡唑化合物或其盐,其中R 1是-CH(OH)-CH(R 4) - (A) -CH(R 4) - (A)n -Y, - CO(CH 2) -B 1 -I 1等(其中A是低级亚烷基; Y是可以被卤素取代的芳基等); R 4, SUP>是氢原子或低级烷基; B 1是-CH(R 4) - 或-N(R 4) - ;和n为0或1); R 2是氢原子,可以被羟基等取代的低级烷基或芳烷基; R 3是可以被卤素等取代的苯基或吡啶基; Q为吡啶基或喹啉基。 这些取代的吡唑化合物或其盐具有优异的p38MAP激酶抑制作用,因此可用于预防或治疗肿瘤坏死因子α相关疾病,白细胞介素1相关疾病,白细胞介素6相关疾病或环氧合酶II相关疾病
摘要:
Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)—(A)n—Y, —CH2—CH(R4)—(A)n—Y, —CO—B1—A—Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor &agr;-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases.
摘要翻译:公开了由式(I)表示的取代的吡唑化合物或其盐,其中R 1是-CH(OH)-CH(R 4) - (A)n Y,-CH 2 -CH(R 4) ) - (A)nY,-CO-B 1 -AY等(其中A是低级亚烷基; Y是可以被卤素取代的芳基等; R 4 >是氢原子或低级烷基; B 1是-CH(R 4) - 或-N(R 4) - ,n是0或1); R 2是氢原子,可以被羟基等取代的低级烷基或芳烷基; R 3是可被卤素等取代的苯基或吡啶基; Q为吡啶基或喹啉基。 这些取代的吡唑化合物或其盐具有优异的p38MAP激酶抑制作用,因此可用于预防或治疗肿瘤坏死因子α相关疾病,白细胞介素1相关疾病,白介素6相关疾病或环加氧酶II相关疾病。
摘要:
Aminopyrazole derivatives represented by formula (I), or salts thereof, wherein X1 and X2 are each a hydrogen atom or a halogen atom, or X1 and X2 may be united together to form a lower alkylenedioxy group, Q is a pyridyl group or a quinolyl group, R1 is a hydrogen atom, a substituted or unsubstituted lower alkyl or aryl group, R2 is a hydrogen atom, a lower alkyl group, or an aralkyl group, and R3 represents a hydrogen atom, an organic sulfonyl group, or —C(═Y)—R4 in which R4 is a hydrogen atom or an organic residue and Y is an oxygen or sulfur atom, provided that, when R3 is a hydrogen atom, R1 is a group other than a hydrogen atom and R2 is a hydrogen atom. These amimopyrazole derivatives or their salts have excellent p38MAP kinase inhibiting activities and are hence useful in the prevention or treatment of diseases associated with tumor necrosis sis factor &agr;, interleukin 1, interleukin 6 or cyclooxygenase II.
摘要:
In production of a reactive metal using a melting furnace for producing metal having a hearth, ingots can be efficiently produced by efficiently cooling the ingots extracted from the mold provided in the melting furnace. In addition, an apparatus structure in which multiple ingots can be produced with high efficiency and high quality from one hearth, is provided. A melting furnace for producing metal is provided, the furnace has a hearth for having molten metal formed by melting raw material, a mold in which the molten metal is poured, an extracting jig which is provided below the mold for extracting ingot cooled and solidified downwardly, a cooling member for cooling the ingot extracted downwardly of the mold, and an outer case for keeping the hearth, the mold, the extracting jig, and the cooling member separated from the air, wherein at least one mold and extracting jig are provided in the outer case, and the cooling member is provided between the outer case and the ingot, or between the multiple ingots.
摘要:
In production of a reactive metal using a melting furnace for producing metal having a hearth, ingots can be efficiently produced by efficiently cooling the ingots extracted from the mold provided in the melting furnace. In addition, an apparatus structure in which multiple ingots can be produced with high efficiency and high quality from one hearth, is provided. A melting furnace for producing metal is provided, the furnace has a hearth for having molten metal formed by melting raw material, a mold in which the molten metal is poured, an extracting jig which is provided below the mold for extracting ingot cooled and solidified downwardly, a cooling member for cooling the ingot extracted downwardly of the mold, and an outer case for keeping the hearth, the mold, the extracting jig, and the cooling member separated from the air, wherein at least one mold and extracting jig are provided in the outer case, and the cooling member is provided between the outer case and the ingot, or between the multiple ingots.
摘要:
The present invention provides a moisturizer comprising, as an active ingredient, a saccharide having 3-O-α-D-glucopyranosyl-D-glucose as a structural unit. The moisturizer of the present invention improves the water retention capacity of the stratum corneum, and is useful for prevention and improvement of rough skin.