摘要:
The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
摘要:
A compound represented by the formula(I): wherein R 1 is a heterocyclic group, CHO or CH 2 OR 6 ; R 2 is an alkyl group; R 3 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro, cyano or a halogen-substituted alkyl group; R 4 is hydrogen atom, an alkyl group, a cycloalkyl group, an alkoxyalkyl group, an alkoxycarbonyl group, cyano, a halogen-substituted alkyl group, an aryl group or a heterocyclic group; R 5 is hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an alkanoyl group, an aroyl group, an alkoxycarbonyl group, an aryl group or a heterocyclic group; A is (1) - CH 2 ON=C(R 7 )-, (2) -CH 2 N(R 8 )-N=C(R 7 )-, (3) -CH=NOC(R 9 )(R 10 )- or (4)-CH=NN=C(R 7 )-; B is oxygen atom or NR 11 ; the wary line: ∼ indicates E isomer, Z isomer or a mixture of them, has a broad spectrum of fungicidal activity, and therefore, is excellent as fungicides.
摘要:
A process for preparing a compound represented by formula (Y1) or (Y2) [wherein R x is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R 1d is hydrogen, halogen, or the like; R 2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R 4d is a lower alkyl optionally substituted with substituent E, or the like; and R 6d is a lower alkyl group optionally substituted with substituent group E, or the like].
摘要:
The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins. A compound of the formula (I):
wherein R 1 , R 2a , R 2b , R 3 , R 4a , R 4b , ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
摘要:
A process for producing a carboxylic acid derivative represented by general formula [VIII], (wherein R , R , R and L are each as defined in the specification), which comprises reacting a benzyl halide with a cyano compound to give a phenylacetonitrile, reacting the nitrile with an alkyl nitrite in the presence of a base to give an alpha -hydroxyiminophenylacetonitrile, reacting the hydroxy nitrile with an alkylating agent to give an alpha -alkoxyiminophenylacetonitrile, hydrolyzing the alkoxy nitrile in the presence of a base, optionally after hydration and acid treatment, to give an alpha -alkoxyiminophenylacetic acid, and finally reacting the acid with a halogenating agent, or converting the acid into a corresponding metal salt and reacting the salt with an alkylating agent, or reacting the acid with a lower alcohol in the presence of an acidic catalyst. According to this process, the reactions can be advanced through the respective steps under mild conditions, and the target derivative [VIII] can be produced even without resort to high-pressure steam equipment, high-temperature heat medium equipment, refrigerator, and so forth. Further, this process is advantageous in that only a single solvent will suffice without the necessity for using various solvents according to the respective steps.
摘要:
A process for producing a carboxylic acid derivative represented by general formula [VIII], (wherein R¹, R², R³ and L are each as defined in the specification), which comprises reacting a benzyl halide with a cyano compound to give a phenylacetonitrile, reacting the nitrile with an alkyl nitrite in the presence of a base to give an α-hydroxyiminophenylacetonitrile, reacting the hydroxy nitrile with an alkylating agent to give an α-alkoxyiminophenylacetonitrile, hydrolyzing the alkoxy nitrile in the presence of a base, optionally after hydration and acid treatment, to give an α-alkoxyiminophenylacetic acid, and finally reacting the acid with a halogenating agent, or converting the acid into a corresponding metal salt and reacting the salt with an alkylating agent, or reacting the acid with a lower alcohol in the presence of an acidic catalyst. According to this process, the reactions can be advanced through the respective steps under mild conditions, and the target derivative [VIII] can be produced even without resort to high-pressure steam equipment, high-temperature heat medium equipment, refrigerator, and so forth. Further, this process is advantageous in that only a single solvent will suffice without the necessity for using various solvents according to the respective steps.