- 1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
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Paragraph 0217; 0219
(2020/08/30)
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- PYRAZOLOOXAZOLE COMPOUND
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A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism. wherein R1 and R2 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, a C1-6 alkyl group substituted with a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, etc; R3, R4 and R5 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C1-6 alkoxy-C1-6 alkyl group, a C3-6 cycloalkoxy-C1-6 alkyl group or a halogen atom; R6 is a hydrogen atom or a C1-6 alkyl group; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkylthio group.
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Page/Page column 16
(2011/04/25)
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- Organic compounds
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There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.
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Page/Page column 69
(2010/03/02)
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- Synthesis of 3-substituted and 3,4-disubstituted pyrazolin-5-ones
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The synthesis of 3-substituted and 3,4-disubstituted pyrazolin-5-ones from acylated ethyl acetoacetates and diethyl malonates is described. The reaction of acylated ethyl acetoacetates and diethyl acetylmalonate with hydrazine (98%) gave 3-substituted pyrazolin-5-ones and malonyldihydrazide, respectively, following a deacetylation-condensation sequence. The reaction of ethyl 2-acetyl-3-hydroxy-2-butenoate and diethyl 2-(1-hydroxyethylidene)malonate with hydrazine monohydrochloride yielded ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate and 4-ethoxycarbonyl-3-methylpyrazolin-5-one, respectively, following a dehydration-cyclocondensation sequence, in high yields.
- Jung, Jae-Chul,Watkins, E.Blake,Avery, Mitchell A
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p. 3639 - 3646
(2007/10/03)
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- Efficient synthesis of 4-ethoxycarbonyl pyrazolin-5-one derivatives
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Concise and efficient methods for the preparation of 3-substituted 4-ethoxycarbonylpyrazolin-5-ones are described. The synthetic strategies involve carbon-acylation in the presence of base, followed by ring cyclization with hydrazine or hydrazine monohydrochloride.
- Jung, Jae C.,Watkins, E Blake,Avery, Mitchell A.
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p. 3767 - 3777
(2007/10/03)
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- THE SELECTIVE METHYLATION OF 4-ETHOXYCARBONYL-3-METHYLPYRAZOLIN-5-ONE WITH DIMETHYL SULFATE
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The methylation of some pyrazolin-5-ones with dimethyl sulfate in different reaction conditions is described.It is found that it is possible achived selective introducing of methyl group in desired position of pyrazolin-5-one ring which is of great interest for preparation of many analgesics and antipyretics with pyrazolin-5-one unit.
- Jursic, Branco,Bregant, Nada
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p. 2087 - 2094
(2007/10/02)
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