40245-26-9Relevant articles and documents
TRIAZOLE DERIVATIVES AND THEIR USE AS TANKYRASE INHIBITORS.
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Page/Page column 47; 66-68, (2022/02/06)
The present invention relates to compounds of general formula (I), tautomers, stereoisomers, N-oxides, pharmaceutically acceptable salts and pro-drug thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy: wherein: a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), -CN, -NO2, -N(R)2, and -SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); Y represents: an aryl or heteroaryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); a 5- or 6-membered, saturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or a C3-6 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); and Z represents: an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), -CN, -NO2, -OH, -N(R' )2 (where each R1 is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl), -SO2R2 (where R2 is H or C1-6 alkyl, e.g. H or C1-3 alkyl), -SO2N(R3)2 (where each R3 is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl), and -C(0)N(R4)2 (where each R4 is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl, or wherein both R4 groups, together with the intervening nitrogen atom, form a 3 to 6 membered saturated heterocyclic ring); or an unsaturated, 5- to 10-membered mono- or bicyclic heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), -CN, -NO2, -OH, -N(R')2 (where each R1 is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl), -SO2R2 (where R2 is H or C1-6 alkyl, e.g. H or C1-3 alkyl), -SO2N(R3)2 (where each R3 is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl), and -C(O)N(R4)2 (where each R4 is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl, or wherein both R4 groups, together with the intervening nitrogen atom, form a 3 to 6 membered saturated heterocyclic ring); with the proviso: that when the compound is other than an N-oxide of formula (I), Z must be substituted by at least one substituent selected from -OH, -N(R3)2, -SO2N(R3)2 and -C(O)N(R4)2, preferably by at least one substituent selected from -OH, -SO2N(R3)2 and -C(O)N(R4)2. These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.
Highly chemoselective deoxygenation of N-heterocyclic: N -oxides under transition metal-free conditions
Kim, Se Hyun,An, Ju Hyeon,Lee, Jun Hee
supporting information, p. 3735 - 3742 (2021/05/04)
Because their site-selective C-H functionalizations are now considered one of the most useful tools for synthesizing various N-heterocyclic compounds, the highly chemoselective deoxygenation of densely functionalized N-heterocyclic N-oxides has received much attention from the synthetic chemistry community. Here, we provide a protocol for the highly chemoselective deoxygenation of various functionalized N-oxides under visible light-mediated photoredox conditions with Na2-eosin Y as an organophotocatalyst. Mechanistic studies imply that the excited state of the organophotocatalyst is reductively quenched by Hantzsch esters. This operationally simple technique tolerates a wide range of functional groups and allows high-yield, multigram-scale deoxygenation. This journal is
Optical p Ka Control in a Bifunctional Iridium Complex
Demianets, Ivan,Hunt, Jonathan R.,Dawlaty, Jahan M.,Williams, Travis J.
supporting information, p. 200 - 204 (2019/01/21)
There are few ways to switch a catalyst's reactivity on or off, or change its selectivity, with external radiation; many of these involve photochemical activation of a catalyst. In the case of homogeneous late-transition-metal catalysts, the metal complex itself is frequently the chromophore involved in such reactivity switching. We show here a base-pendant ligand-metal bifunctional scaffold wherein a photobase, a compound that becomes more basic in the excited state (pKa a?), is used to switch the proton acceptor ability on an active site of the complex. The system differs from those with metal-centered chromophores, because the photobase operates independently of the metal. While excellent progress has been made in photoacid chemistry, neither a photoacid nor a photobase has been designed into the structure of a transition-metal catalyst where the metal is not part of the chromophore. We find that quinoline is an efficient photobase that preserves its unique properties in the close proximity of an iridium center: the efficacy of the photobase (9.3 a? a control in a transition-metal complex.
BRIDGED BICYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS
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Paragraph 1327-1328, (2019/05/15)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor
PLANT GROWTH REGULATOR
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Paragraph 0048, (2018/05/24)
PROBLEM TO BE SOLVED: To provide a plant growth regulator. SOLUTION: The plant growth regulator comprises a compound represented by general formula 1, or a salt or ester thereof. [In the formula, (A1-A2-A3-A4) is (N=CH-CH=CH) or (NH-CH2-CH2-CH2); R1 and R2 are each independently H, an alkyl group or a halogen atom; and R3 is a hydroxyl group or an alkoxy group.] SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
THERAPEUTIC AGENTS FOR OCULAR HYPERTENSION
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Paragraph 0116, (2015/07/02)
This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.
Catalytic formation of ketones from unactivated esters through rhodium chelation-assisted C-O bond activation
Wang, Jingjing,Zuo, Sujing,Chen, Weiqiang,Zhang, Xinrui,Tan, Kaixin,Tian, Yun,Wang, Jianhui
, p. 8217 - 8231 (2013/09/24)
A new method for building aryl aryl ketones containing heterocyclic rings through chelation-assisted C-O bond activation catalyzed by a rhodium complex has been developed. In this reaction, methyl quinoline-8-carboxylate, methyl quinoxaline-5-carboxylate, and their derivatives were reacted with an excess amount of a substituted phenyl boronic acid in the presence of a rhodium(I) complex to give substituted phenyl(quinolin-8-yl)methanone, phenylquinoxalin-5- ylmethanone, and their derivatives in medium to high yields. The current method offers a highly favorable synthetic pathway to efficiently build related drugs with an 8-benzoylquinoline core structure. This method may prove especially valuable for medicinal chemists for the late-stage introduction of versatile ketone moieties into complex scaffolds for diversity-oriented synthetic strategies.
THERAPEUTIC AGENTS FOR OCULAR HYPERTENSION
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Page/Page column 10; 28, (2012/01/15)
This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.
Therapeutic modulation of PPARgamma activity
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Page/Page column 80, (2010/02/14)
Modulators of PPARγ activity are used in methods of treating and/or preventing conditions such as osteoporosis, Alzheimer's disease, psoriasis and acne, and cancer.
