22117-85-7Relevant academic research and scientific papers
Preparation method of 2-methoxy-5-sulfamoylbenzoic acid
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Paragraph 0016; 0018-0019; 0026-0027, (2020/05/14)
The invention provides a preparation method of 2-methoxy-5-sulfamoylbenzoic acid, comprising the following steps: carrying out bromination reaction on 4-methoxybenzenesulfonamide and bromine under theaction of a reducing agent to obtain 3-bromo-4-methoxybenzenesulfonamide; carrying out substitution reaction on 3-bromo-4-methoxybenzenesulfonamide and cuprous cyanide under the action of a catalystto generate 3-cyano-4-methoxybenzenesulfonamide; carrying out alcoholysis on the 3-cyano-4-methoxybenzenesulfonamide and methanol under the catalysis of an acid to obtain 2-methoxy-5-sulfonamide methyl benzoate; hydrolyzing 2-methoxy-5-sulfonamide methyl benzoate under an alkaline condition, and then acidifying to obtain the 2-methoxy-5-sulfamoylbenzoic acid. The preparation method of the 2-methoxy-5-sulfamoylbenzoic acid is mild in reaction condition, simple in process and equipment, convenient to operate and environmentally friendly.
NF-KB ACTIVATION INHIBITORS
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Page/Page column 83, (2008/06/13)
A medicament having inhibitory activity against NF-κB activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is 1○ a fused polycyclic heteroaryl group wherein the ring which binds directly to ―CONH― group in the formula (I) is a benzene ring, 2○ unsubstituted thiazol-2-yl group, or 3○ unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula -CONH-E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula ― CONH―E wherein E has the same meaning as that defined above.
THERAPEUTIC AGENT FOR CANCER
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Page/Page column 83, (2010/02/11)
A medicament for the prevention and/or treatment of cancers and the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is 1? a fused polycyclic heteroaryl group wherein the ring which binds directly to ―CONH― group in the formula (I) is a benzene ring, 2? unsubstituted thiazol-2-yl group, or 3? unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula ―CONH―E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula ― CONH―E wherein E has the same meaning as that defined above.
REMEDIES FOR NEURODEGENERATIVE DISEASES
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Page/Page column 82, (2010/02/12)
A medicament for preventive and/or therapeutic treatment of neurodegenerative diseases such as Alzheimer's disease or the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is 1○ a fused polycyclic heteroaryl group wherein the ring which binds directly to -CONH- group in the formula (I) is a benzene ring, 2○ unsubstituted thiazol-2-yl group, or 3○ unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -CONH-E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -CONH-E wherein E has the same meaning as that defined above.
IMMUNITY-RELATED PROTEIN KINASE INHIBITORS
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Page/Page column 134, (2010/02/10)
[From equivalent EP1510210A1] A medicament having an inhibitory activity against IKK-Aβ and/or MEKK-1 or other protein kinases structurally similar thereto, which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each of X and E has the same meaning as that defined above.
INHIBITORS AGAINST THE ACTIVATION OF AP-1 AND NFAT
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Page/Page column 132, (2008/06/13)
A medicament inhibiting the activation of AP-1 which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each of X and E has the same meaning as that defined above.
ANTIALLERGIC
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Page/Page column 138, (2010/02/11)
A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each ofX and E has the same meaning as that defined above.
INHIBITORS AGAINST THE PRODUCTION AND RELEASE OF INFLAMMATORY CYTOKINES
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, (2008/06/13)
A medicament having inhibitory activity against NF- κ B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
Synthesis and D2 Dopaminergic Activity of Pyrrolidinium, Tetrahydrothiophenium, and Tetrahydrothiophene Analogues of Sulpiride
Harrold, Marc W.,Wallace, Raye Ann,Farooqui, Tahira,Wallace, Lane J.,Uretsky, Norman,Miller, Duane D.
, p. 874 - 880 (2007/10/02)
All of the existing dopamine receptor models recognize the amine nitrogen of agonist and antagonist drugs as playing a crucial role in receptor interactions.However, there has been some controversy as to which molecular form of the amine, charged or uncharged, is most important in these interactions.We have synthesized and examined the biological activity of permanently charged and permanently uncharged analogues of the dopaminergic antagonist, sulpiride.Sulpiride and the permanently charged pyrrolidinium (6,7) and tetrahydrothiophenium (9) analogues were able to antagonize the inhibitory effect of apomorphine on the K+-induced release of acetylcholine from striatal slices.In contrast, the permanently uncharged tetrahydrothiophene analogue 8 was inactive at concentrations up to 100 μM.Additionally, both sulpiride and the tetrahydrothiophenium analogue were able to displace spiperone from D2 binding sites, while the tetrahydrothiophene analogue was unable to produce any significant displacement.These results are consistent with our previous observations on permanently charged chlorpromazine analogues and provide further evidence that dopaminergic antagonists bind in their charged molecular forms to anionic sites on the D2 receptor.
