- Diaryl-substituted 1, 1-ethylene compounds and preparation method and application thereof
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The invention discloses diaryl-substituted 1, 1-ethylene compounds shown as general formulas I, II, III and IV, and a preparation method and application thereof, and the compounds can be used for preparing medicines related to tumor treatment, tubulin activity inhibition and HDAC activity inhibition.
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Paragraph 0088-0090
(2021/02/24)
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- Compounds for the treatment of metabolic disorders
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Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
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Page/Page column 104; 105
(2016/03/12)
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- Synthesis and bioactivity of substituted benzoylguanidine derivatives as potent Na+/H+ exchanger inhibitors
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A novel series of substituted benzoylguanidine derivatives were designed and synthesized in order to evaluate their NHE1 inhibitory activity. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and eight compounds showed more potent NHE1 inhibitory activity than Cariporide. Compound 6f with an IC50 value of 1.08 × 10-10 molmiddot;L-1, was 39 times more potent than lead compound CPU-X-050420 in vitro tests. A novel series of 5-(2-(4-(2,3,4-trimethoxybenzyl)piperazin-1-yl)acetyl)benzoylguanidine derivatives 6a-6i have been synthesized and screened for their NHE1 inhibitory activity. Copyright
- Jin, Ning,Yang, Yun,Xu, Wenting,Yang, Xiaozhi,Gong, Guoqing,Xu, Yungen
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experimental part
p. 333 - 340
(2012/05/19)
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- COMPOSITION AND PROCESS - 356
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There is provided a process for the preparation of a compound of Formula 1, the use of said process in the preparation of a compound of Formula 5 or a phosphate, sulphate, hydrogensulphate, malate, citrate, tartrate or fumarate salt thereof, and the use of the fumarate salt in a composition for use in therapy.
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Page/Page column 32
(2009/12/28)
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- NF-KB ACTIVATION INHIBITORS
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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.
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Page/Page column 80
(2008/06/13)
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- THERAPEUTIC AGENT FOR CANCER
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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.
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Page/Page column 80
(2010/02/11)
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- REMEDIES FOR NEURODEGENERATIVE DISEASES
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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.
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Page/Page column 79
(2010/02/12)
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- IMMUNITY-RELATED PROTEIN KINASE INHIBITORS
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[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.
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Page/Page column 131
(2010/02/10)
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- INHIBITORS AGAINST THE ACTIVATION OF AP-1 AND NFAT
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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.
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Page/Page column 129
(2008/06/13)
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- ANTIALLERGIC
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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.
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Page/Page column 135
(2010/02/11)
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- Bicyclyl or heterobicyclylmethanesulfonylamino-substituted n-hydroxyformamides
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Compounds of formula (I): R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl, are useful in the treatment and prophylaxis of conditions mediated by s-CD23.
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- INHIBITORS AGAINST THE PRODUCTION AND RELEASE OF INFLAMMATORY CYTOKINES
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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.
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- Compounds for the treatment of metabolic disorders
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Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
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- Mass tags for quantitative analysis
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The present invention relates generally to novel protein modification reagents for fractionation and quantitative (differential) profiling of proteins in a complex mixture. The reagents react with amino acids or other protein components or structures and function as mass tags. The present invention provides methods of making the protein modification reagents and methods of using the protein modification reagents for quantitative analysis of proteins.
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- Pharmaceutically active bicyclic-heterocyclic amines
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The pharmaceutically active bicyclic heterocyclic amines (XXX) STR1 where W1 is --N= or --CH=; W3 is --N= or --CH=; W5 is --N= or --CR5 -- with the proviso that W5 is --CR5 -- when both W1 and W3 are --N= which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.
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- Alkyliron and Alkylcobalt Reagents, VIII. - Alkyl-Iron(II) Compounds as Reagents and Catalysts for the Transformation of Acyl Chlorides into Ketones
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Me2Fe, Bu2Fe, Me3FeLi, or Bu3FeLi - prepared in situ by reduction of FeCl3 to FeCl2 and subsequent alkylation with MeLi, MeMgBr, BuLi, or BuMgBr - are useful reagents for the conversion of acyl chlorides into ketones.The system (RMgX + catalytic amount of FeCl3) react like the FeII reagents with acyl chlorides to give ketones even at -65 deg C.Competition experiments with benzoyl chloride/2-methoxybenzoyl chloride show that the selectivity increases (competition constants Kk = 9.9, 10.7, 10.9, 15.0, ca. 110) in the sequence MeFeCl, Me2Fe, Me3Fe(MgBr), Me4Fe(MgBr)2, and catalytic system (MeMgBr + 2.5 mol percent FeCl3) (= 2, 3, 4, 5, and 40MeMgBr per 1 FeCl3, respectively).A new hypothesis on the nature of the active catalyst is discussed. Key Words: Organoiron compounds / Iron catalysts / Ketone synthesis
- Kauffmann, Thomas,Voss, Karl-Uwe,Neiteler, Gabriele
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p. 1453 - 1460
(2007/10/02)
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- NOVEL ANTIHYPERTENSIVE AGENT
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This invention is to the compound 5-2-3-(1,3-benzodioxol-5-yl)-1-methylpropyl!amino!-1-hydroxyethyl!-2-methoxyben zamide having the formula, STR1 pharmaceutically acceptable salts and individual optical isomers thereof, pharmaceutical compositions comprising as the active ingredient the compound of Formula 1 or salts or isomers thereof and the use of said compound, or salt or isomer thereof or pharmaceutical composition comprising same in the treatment of hypertension.
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