- HETEROCYCLIC COMPOUND
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Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
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Paragraph 1021; 1022
(2019/06/17)
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- Imidazolium Salt Catalyzed para -Selective Halogenation of Electron-Rich Arenes
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A highly para-selective halogenation of arenes bearing coordinating groups in the presence of a dimidazolium salt as a catalyst is reported. A series of electron-rich p-haloarenes were prepared in good yields and good to excellent selectivities. We also propose a plausible mechanism for the catalytic reaction.
- Chen, Jie,Xiong, Xiaoyu,Chen, Zenghua,Huang, Jianhui
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supporting information
p. 2831 - 2834
(2015/12/18)
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- CYCLOPENTYLBENZAMIDE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF PSYCHOTIC AND COGNITIVE DISORDERS
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The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, L, X, Ra, Rb, R1, R2 and R3 their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 65; 66
(2015/05/05)
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- NOVEL COMPOUND, AND KINESIN SPINDLE PROTEIN INHIBITOR AND APPLICATION THEREOF
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A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.
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Paragraph 0137-0138
(2013/10/22)
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- COMPOUND, KINESIN SPINDLE PROTEIN INHIBITOR, AND APPLICATION THEREOF
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A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.
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Paragraph 0152; 0153
(2013/12/04)
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- Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
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The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.
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Page/Page column 56
(2013/06/27)
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- DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound. The present invention discloses the unexpected utility of compounds that inhibit cKIT kinase across a broad range of c-KIT mutations, including complex occurrences of primary mutations (KIT exon 9 or 11) and secondary KIT mutations (exons 13, 14, 17 and 18) that may arise in individual, refractory GIST patients. Also unexpected is the utility of compounds of the present invention to inhibit the problematic exon 17 D816V c-KIT mutation, for which there is currently no effective therapy.
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Paragraph 0169
(2014/01/08)
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- Facile synthesis and herbicidal activities of new isoxazole derivatives via 1,3-dipolar cycloaddition reaction
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A series of cycloadducts via 1,3-dipolar cycloaddition reactions of generated nitrile oxides with N-(4-chloro-2-fluorophenyl) maleimides were described. The reaction of N-(4-chloro-2-fluorophenyl) maleimides with nitrile oxides gave 3,5-diaryl-3a,6a-dihydropyrroio[3,4-d]isoxazole-4,6-diones through syn-addition pattern. The title compounds were characterized by 1H NMR, IR, MS, and elemental analysis or HRMS. The single crystal structure of 6i was determined by X-ray diffraction. The herbicidal activities of the title compounds were evaluated. Some of them exhibited certain herbicidal activities against barnyardgrass and rape.
- Zhang, Chuan-Yu,Wang, Bao-Lei,Liu, Xing-Hai,Li, Yong-Hong,Wang, Su-Hua,Li, Zheng-Ming
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experimental part
p. 397 - 404
(2010/03/24)
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- PHENYLACETIC ACID DERIVATIVES
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Compounds of formula (I) pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.
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Page/Page column 25
(2008/06/13)
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- Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications
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Recent efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective 3-[(benzothiazol-2-yl)methyl]indole-N-alkanoic acid aldose reductase inhibitors. The lead candidate, 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat, 9) inhibits aldose reductase with an IC50 of 5 nM, while being 5400 times less active against aldehyde reductase, a related enzyme involved in the detoxification of reactive aldehydes. It lowers nerve and lens sorbitol levels with ED50's of 1.9 and 4.5 mg/kg/d po, respectively, in the 5-day STZ-induced diabetic rat model. In a 3-month diabetic intervention model (1 month of diabetes followed by 2 months of drug treatment at 5 mg/kg/d po), it normalizes polyols and reduces the motor nerve conduction velocity deficit by 59% relative to diabetic controls. It has a favorable pharmacokinetic profile (F, 82%; t1/2, 5.6 h; Vd, 0.694 L/kg) with good drug penetration in target tissues (Cmax in sciatic nerve and eye are 2.36 and 1.45 μg equiv/g, respectively, when dosed with [14C] lidorestat at 10 mg/kg po).
- Van Zandt, Michael C.,Jones, Michael L.,Gunn, David E.,Geraci, Leo S.,Jones, J. Howard,Sawicki, Diane R.,Sredy, Janet,Jacot, Jorge L.,DiCioccio, A. Thomas,Petrova, Tatiana,Mitschler, Andre,Podjarny, Alberto D.
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p. 3141 - 3152
(2007/10/03)
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- 1-(3-heterocyclyphenyl)-S-triazine-2,6,6-oxo or thiotrione herbicidal agents
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There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2, 4,6-oxo or thiotrione compound having the structural formula I STR1 Further provided are a composition and a method comprising that compound for the control of undesirable plant species.
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- 1-(3-heterocyclylphenyl)-s-triazine-2,4,6-oxo or thiotrione herbicidal agents
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There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I STR1 Further provided are a composition and a method comprising that compound for the control of undesirable plant species.
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- 1-(3-heterocyclylphenyl)-s-triazine-2,4,6-oxo or thiotrione herbicidal agents
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There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I STR1 Further provided are a composition and a method comprising that compound for the control of undesirable plant species.
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- Herbicidal aryl triazolinones
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Herbicidal compounds of the formula STR1 in which, for example, X is Br, Cl or F; Y is Cl or Br, R2 is CHF2, R3 is CH3, R is alkyl, dialkylamino, carboxymethyl, hydroxy, haloalkyl, or aryl, and R1 is H, Na, lower alkyl or --SO2 R.
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- Herbicidal aryl triazolinones
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Herbicidal compounds of the formula STR1 in which, for example, X is Br, Cl or F; Y is Cl or Br, R2 is CHF2, R3 is CH3 R is lower alkyl and R1 is H,Na, lower alkyl or --SO2 R.
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- Electrophilic fluorination of aromatic compounds
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A process for the electrophilic ring fluorination of aromatic compounds which comprises reacting a fluorinating agent from the group consisting of CF3 OF and CF2 (OF)2 with an aromatic compound of the formula STR1 where X is selected from the group consisting of STR2 and STR3 and Y is selected from the group consisting of --H, --CF3, --CN, --NO2, --Cl, and CH3.
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- Substituted isoindoles
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This invention relates to novel compounds of the formulae and their use as herbicides: STR1 wherein X is H, F, Cl, Br, CN, NO2 or OCH3 ; Y is H, F, or CH3 ; and Z is H, F, Cl, Br or OCH3 provided that (1) when Y
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- Cycloalkanapyrazole-3-carbonitrile herbicides
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Herbicidal cycloalkanapyrazoles of the formula: STR1 where N IS 3, 4 OR 5; R1 is hydrogen or methyl; X is fluorine, chlorine, bromine, iodine, cyano, or methoxy; Y is hydrogen, fluorine, or chlorine; Z is hydrogen or fluorine; and V is hydrogen, fluorine, chlorine or methoxy; provided that (a) when n is 3, R1 must be hydrogen; (b) when n is 5, R1 must be hydrogen, Y must be hydrogen or fluorine, Z and V must both be hydrogen, and X must be fluorine, chlorine or bromine; (c) when V is methoxy, X and Y must be chlorine, and Z must be hydrogen; and (d) when V is fluorine or chlorine, X must be fluorine, chlorine or bromine, and Z must be hydrogen.
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- Alkyl-substituted cycloalkanapyrazole herbicides
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Herbicidal alkyl-substituted cycloalkanapyrazoles of the formula: STR1 where N IS 3, 4 OR 5; R1 is hydrogen or methyl; Q is methyl; X is fluorine, chlorine, bromine, iodine, cyano or methoxy; Y is hydrogen, fluorine or chlorine; Z is hydrogen or fluorine; V is hydrogen, fluorine, chlorine or OR; and R is alkyl of 1 to 4 carbon atoms; with the proviso that A. when n is 3, R1 is hydrogen; B. when n is 5, R1 is hydrogen, Y is hydrogen or fluorine, Z and V are hydrogen and X is fluorine, chlorine or bromine; C. when V is OR, X and Y are chlorine and Z is hydrogen; D. when V is fluorine or chlorine, X is fluorine, chlorine or bromine and Z is hydrogen. Preferred for their higher activity or favorable cost or both are those compounds of formula I where, independently, 1. R1 is hydrogen and n is 4, 2. Y is hydrogen or fluorine, V is hydrogen and Z is hydrogen. Most preferred for their outstanding herbicidal activity are those compounds of formula I where n is 4, R1 is hydrogen, X is fluorine, chlorine or bromine, Y is hydrogen or fluorine, V is hydrogen and Z is hydrogen.
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- Herbicidal 2-fluoro-4-halo-phenyl-4,5,6,7-tetrahydro-2H-isoindole-1,3-diones
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This invention relates to herbicidal 2-fluoro-4-halo-phenyl-4,5,6,7-tetrahydro-2H-isoindole-1,3-diones. These compounds may be used for selective weed control in certain crops or for total vegetation control.
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- Herbicidal 2-substituted aryl-4,5,6,7-tetrahydro-2H-isoindole-1,3-diones
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This invention relates to herbicidal 2-substituted aryl-4,5,6,7-tetrahydro-2H-isoindole-1,3-diones. These compounds may be used for selective weed control in certain crops or for total vegetation control.
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- Cycloalkanapyrazole herbicides
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Herbicidal cycloalkanapyrazoles of the formula: STR1 where N IS 3, 4 OR 5; R1 is hydrogen or methyl; Q is fluorine, chlorine, bromine or iodine; X is fluorine, chlorine, bromine, iodine, cyano, methoxy or nitro; Y is hydrogen, fluorine, or chlorine; Z is hydrogen or fluorine; and V is hydrogen, fluorine, chlorine or methoxy with the proviso that A. when n is 5, R1 must be hydrogen, Q must be chlorine or bromine, Z and V must both be hydrogen and Y must be hydrogen or fluorine; B. when n is 3 or 4 and Q is fluorine or iodine, R1, Z and V must be hydrogen and Y must be hydrogen or fluorine; C. when n is 3 and R1 is methyl, Q must be chlorine or bromine, Y must be hydrogen or fluorine and Z and V must both be hydrogen; and, D. when V is other than hydrogen, X must be fluorine, chlorine or bromine and Z must be hydrogen.
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- 2-(Substituted-phenyl)-hexahydro- and tetrahydro-3-(2H)-cinnolinones as herbicides
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This invention relates to herbicidal 2-(substituted-phenyl)-hexahydro- and tetrahydro-3-(2H)-cinnolinones, to agricultural compositions containing such compounds, and to the method of use of these compounds as pre- and post-emergence herbicides.
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- 2-Aryl-3-chloro-2,4,6,7-tetrahydrothiopyrano[4,3-c]-pyrazoles
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Compounds of the formula STR1 where N IS 0, 1, OR 2; Q is chlorine or bromine; X is fluorine, chlorine, bromine, or cyano; Y is hydrogen, fluorine, or chlorine; and V is hydrogen, fluorine, chlorine or alkoxy of 1 to 3 carbon atoms.
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- Herbicidal 2-arylaminocarbonyl-1-cyclohexene-1-carboxylic acids and salts thereof
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This invention relates to herbicidal 2-arylaminocarbonyl-1-cyclohexene-1-carboxylic acids and salts thereof. These compounds may be used for selective weed control in certain crops or for total vegetation control.
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- 2-Aryl-5,6,7,8-tetrahydroimidazo[1,5a]-pyridine-1,3(2H,8aH)-diones as herbicides
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This invention relates to novel 2-Aryl-5,6,7,8-tetrahydroimidazo[1,5a]-pyridine-1,3(2H,8aH)-diones and their use as herbicides. These novel compounds may be used for selective weed control in certain crops or for total vegetation control.
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- Herbicidal isoindol-1-one derivatives
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This invention relates to herbicidal isoindol-1-one derivatives. These compounds have the general formulae: SPC1 Wherein R1 is hydrogen or methyl; R2 is hydrogen or alkyl of 1 to 4 carbons; X is fluorine, chlorine or bromine; Y is hydrogen or fluorine; Z is hydrogen or fluorine, provided that when Y and Z are both fluorine, X must also be fluorine; and A is --(CH2)4 -- or --CH=CH--CH=CH--, provided that when A is --CH=CH--CH=CH-- and Y is hydrogen, Z must be fluorine. Both geometric isomers, Formulae IIa and IIb, are encompassed by this invention. In particular, these compounds have demonstrated that they are active pre- and post-emergence herbicides and tend to do minimal damage to certain desirable crops, e.g., corn and wheat.
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- Herbicidal isobenzofuranones
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This invention relates to herbicidal isobenzofuranones. These compounds may be used for selective weed control in certain crops or for total vegetation control.
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- Herbicidal 2-(substituted aryl)-3a,4,5,6,7,7a-hexahydro-1H-isoindole-1,3(2H)-diones
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This invention relates to herbicidal 2-(substituted aryl)-3a,4,5,6,7,7a-hexahydro-1H-isoindole-1,3(2H)-diones. These compounds may be used for selective weed control for certain crops or for total vegetation control. In particular, the compounds may be utilized as rice herbicides and have the formula SPC1 Wherein X is Cl, Br or F, and Y is H or F, provided that when Y is F, X is F.
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