摘要:
A naphthalene derivative having the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or a non-toxic salt moiety; R.sup.2 and R.sup.3 independently represent a hydrogen atom or --OR.sup.4 where R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group;A represents a group: ##STR2## [where X.sup.1 and X.sup.2 represents an oxygen atom or N--OR.sup.5 (where R.sup.5 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], a group: ##STR3## [where Y.sup.1 and Y.sup.2 independently an oxygen atom or a group N--OR.sup.6 (where R.sup.6 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], or a group: ##STR4## (where n is 0 or 1); and B represents --(CH.sub.2).sub.m -- wherein m is an integer of 1, to 8,--(CH.sub.2).sub.m.sbsb.1 --O--(CH.sub.2).sub.m.sbsb.2 -- wherein m.sub.1 and m.sub.2 are independently 1 or 2, or ##STR5## wherein m.sub.3 is 0 or 1.
摘要:
A production method of an acetamidopyrrolidine derivative or a salt thereof comprising the reaction steps represented by the following formula: wherein R1 represents a hydrogen atom or a C1-C6 alkyl group; R13, R14, R15 and R16 each represent independently a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxyl group, a C1-C6 haloalkyl group or a C1-C6 haloalkoxy group; and R21 represents an ester-type protecting group.
摘要翻译:一种乙酰胺基吡咯烷衍生物或其盐的制备方法,包括由下式表示的反应步骤:其中R 1表示氢原子或C 1 -C 3 > 6个烷基; R 13,R 14,R 15和R 16各自独立地表示氢原子,卤素原子, C 1 -C 6烷基,C 1 -C 6烷氧基,羟基,C 1 -C 6烷基,C 1 -C 6烷基, C 1 -C 6卤代烷基或C 1 -C 6 -C 6卤代烷氧基; C 1 -C 6卤代烷基或C 1 -C 6 - R 21表示酯型保护基。
摘要:
There is provided an industrial production method of an aminopyrrolidine derivative having chemokine receptor antagonist activity represented by the following formula, a synthetic intermediate thereof and a production method thereof: wherein R11 is H, C1-C6 alkyl or C2-C7 alkanoyl; R12, R14, R15, R16 and R17 are H, halogen, optionally halogenated C1-C6 alkyl, optionally halogenated C1-C6 alkoxy, hydroxyl or C2-C7 alkoxycarbonyl; R23, R24, R25 and R26 are H, halogen, optionally halogenated C1-C6 alkyl, optionally halogenated C1-C6 alkoxy or hydroxyl; and R3 is H or C1-C6 alkyl.
摘要翻译:提供了具有下式表示的趋化因子受体拮抗剂活性的氨基吡咯烷衍生物及其合成中间体及其制备方法的工业生产方法:其中R 11是H,C 1 C 6 -C 6烷基或C 2 -C 7烷酰基; R 12,R 14,R 15,R 16和R 17均为 H,卤素,任选卤代C 1 -C 6烷基,任意卤代C 1 -C 6烷氧基, 羟基或C 2 -C 7烷氧基羰基; R 23,R 24,R 25和R 26是H,卤素,任选卤代的C 1 -C 12烷基, C 1 -C 6烷基,任选卤代C 1 -C 6烷氧基或羟基; R 3是H或C 1 -C 6烷基。
摘要:
The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
摘要:
According to this invention, there is provided an indole derivative having the general formula (I) wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R1 and R2 each stand for a hydrogen atom or an alkyl group, independently, or (ii) R1 and R2 as taken together form a cycloalkyl group or an aromatic ring, or (iii) R1 and R2 as taken together form a heterocyclic ring, and R3 is a hydrogen atom, a (C1-C10)alkyl group or others, R4 is a substituted alkyl group and R5 is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group and so on, as novel compounds by a novel chemical synthetic process. The indole derivative of formula (I) exhibits a useful chymase inhibitory activity.
摘要:
The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
摘要:
Novel benzene derivatives of the formula (I) shown below, pharmacological salts thereof, pharmacological solvates of the above-mentioned benzene derivatives and salts, pharmaceutical compositions including, as active ingredients, the above-mentioned compounds, and especially, prophylactic or therapeutic medicines for allergic diseases. ##STR1## wherein R.sup.1 =H, C.sub.1 -C.sub.12 cyclic or straight or branched chain alkyl group (which may be substituted by one or more C.sub.6 -C.sub.10 aryloxy groups), C.sub.7 -C.sub.12 aralkyl group (of which the aryl group may be substituted one or more of halogen, methyl and methoxy, or C.sub.3 -C.sub.10 alkenyl which may be substituted by one or more phenyl groups; A=O, S or CH.sub.2 group, B=CO or CZ.sub.2 CO group (Z=H or F), R.sup.2 =H or C.sub.1 -C.sub.4 alkyl group, X=halogen or methyl group, and Y=H, NO.sub.2 or CN group.
摘要:
Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R.sub.1, R.sub.2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.
摘要:
Disclosed is a process for producing A-form crystals of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid, comprising: a step of dissolving by heating 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid in one or a plurality of solvents as a good solvent, selected from the group consisting of 1-propanol, 2-propanol, ethanol, and acetone; a step of cooling the solution; and a step of adding to the solution a hydrocarbon solvent as a poor solvent.
摘要:
Two crystal forms of (R)-3-[2-(2-amino-5-trifluoromethoxybenzamido)acetamido]-1-(6-methylindol-3-ylmethyl)pyrrolidine which exhibit specific X-ray powder diffraction patterns or infrared absorption spectra, amorphous form thereof, a pharmaceutical composition containing the crystal or amorphous form as an active ingredient, as well as methods for preparing them are provided.