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:
This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.
摘要:
This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.
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:
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 method for manufacturing carbon material having good resistance to oxidation, comprising coating carbon material, which is a sintered body or a porous body, with an inorganic polysilazane; heating the carbon material coated with the inorganic polysilazane in an inert atmosphere to form amorphous silicon nitride on the surface of the carbon material; and reheating the heated carbon material in a non-nitriding and non-oxidizing atmosphere, the amorphous silicon nitride being decomposed and silicon carbide being formed on the surface of the carbon material; the reheating being conducted at a temperature of 1300.degree. C. to 1900.degree. C. and the non-nitriding and non-oxidizing atmosphere having a partial pressure of nitrogen determined with reference to a graph wherein the abscissa is a temperature in .degree.C. and the ordinate is partial pressure of nitrogen in atmospheres, the partial pressure being defined within an area under a line connecting a first point corresponding to 1300.degree. C. and 0.1 atmospheres and a second point corresponding to 1900.degree. C. and 20 atmospheres.
摘要:
A method for refining powders comprising the steps of: (a) adding polytetrafluoroethylene powders to non-oxide ceramic powders to form a mixture by mixing; and (b) heating the mixture in non-oxidizing atmosphere to convert oxides existing on the surface of the non-oxide ceramic powders into gaseous fluorides, and removing gaseous fluorides. The fluororesin is a polytetrafluoroethylene resin. The heating temperature in the non-oxidizing atmosphere is 500.degree. C. to 1300.degree. C.