- COMPOUND AS ACC INHIBITOR AND USE THEREOF
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Disclosed are a class of compounds which are inhibitors of acetyl-CoA carboxylase (ACC) and the use thereof. In particular, provided are compounds as shown in formula I or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, and methods for preparing the same, and pharmaceutical compositions comprising the compounds and the use of the compounds or compositions for treating and/or preventing diseases associated with ACC expression, such as fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases. The compound has a good inhibitory activity against ACC and shows good promise to be a therapeutic drug for fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases.
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Paragraph 0331; 0332
(2020/06/15)
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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Paragraph 00743; 00744
(2018/05/15)
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- Intramolecularly Hydrogen-Bonded Aromatic Pentamers as Modularly Tunable Macrocyclic Receptors for Selective Recognition of Metal Ions
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Despite the tremendous progress that has been made in macrocyclic chemistry since the discovery of corands, cryptands, and spherands more than four decades ago, macrocyclic systems possessing a high level of controllability in structural configuration con
- Liu, Ying,Shen, Jie,Sun, Chang,Ren, Changliang,Zeng, Huaqiang
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supporting information
p. 12055 - 12063
(2015/10/05)
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- Patterned recognition of amines and ammonium ions by a stimuli-responsive foldamer-based hexameric oligophenol host
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A stimuli-responsive hexameric oligophenol host undergoes amine-induced co-operative folding from a more fluorescent, more linear structure into less fluorescent, more curved or helically folded states, enabling easy identification and classification of the bound amine guests. The Royal Society of Chemistry 2013.
- Sun, Chang,Ren, Changliang,Wei, Yuchen,Qin, Bo,Zeng, Huaqiang
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supporting information
p. 5307 - 5309
(2013/06/27)
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- Electrochemical C-H amination: Synthesis of aromatic primary amines via N -arylpyridinium ions
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We have developed a new method for C-H amination of aromatic compounds based on electrochemical oxidation of aromatic compounds in the presence of pyridine followed by the reaction of the resulting N-arylpyridinium ions with an alkylamine. This new transformation serves as a powerful method for synthesizing aromatic primary amines from aromatic compounds without using metal catalysts and harsh chemical reagents. High chemoselectivity of the present method is demonstrated by C-H amination of aromatic compounds bearing a nitro group to give a key intermediate for the synthesis of VLA-4 antagonist.
- Morofuji, Tatsuya,Shimizu, Akihiro,Yoshida, Jun-Ichi
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supporting information
p. 5000 - 5003
(2013/05/22)
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- Synthesis, structural investigations, hydrogen-deuterium exchange studies, and molecular modeling of conformationally stablilized aromatic oligoamides
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Biasing the conformational preferences of aromatic oligoamides by internally placing intramolecular hydrogen bonds has led to a series of stably folded molecular strands. This article presents the results from extensive solid-state, solution, and computational studies on these folding oligomers. Depending on its backbone length, an oligoamide adopts a crescent or helical conformation. Surprisingly, despite the highly repetitive nature of the backbone, the internally placed, otherwise very similar intramolecular hydrogen bonds showed significantly different stabilities as demonstrated by hydrogen-deuterium exchange data. It was also observed that the hydrogen-bonding strength can be tuned by adjusting the substituents attached to the exterior of the aromatic backbones. Examining the amide hydrogen-deuterium exchange rates of trimers revealed that a six-membered hydrogen bond nearing the ester end is the weakest among all the four intramolecular hydrogen bonds of a molecule. This observation was verified by ab initio quantum mechanical calculations at the level of B3LYP/6-31G. Such a "weak point" creates the "battle of the bulge" where backbone twisting is centered, which is consistently observed in the solid-state structures of the four trimer molecules studied. In the solid state, the oligomers assemble into interesting one-dimensional structures. A pronounced columnar packing of short oligomers (i.e., dimers, trimers, and tetramer) and channel-like, potentially ion-conducting stacks of longer oligomers (i.e., tetramer, pentamer, and hexamer) were observed.
- Yan, Yan,Qin, Bo,Ren, Changliang,Yip, Yeow Kwan,Ye, Ruijuan,Zeng, Huaqiang,Chen, Xiuying,Su, Haibin,Zhang, Dawei
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supporting information; experimental part
p. 5869 - 5879
(2010/07/13)
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- Benzene Sulfonamide Thiazole and Oxazole Compounds
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The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 85
(2009/12/23)
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- Helical organization in foldable aromatic oligoamides by a continuous hydrogen-bonding network
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Introduction of a continuous internal hydrogen-bonding network suppressed the conformational flexibility of a series of oligoaromatic foldamers with a lengthened backbone. The helical ordering over up to six aromatic repeating units was established in solution by a 2D NOESY study and in the solid state by an X-ray diffraction method. Computational molecular modeling further corroborates the experimentally observed helical propagation in this class of foldable molecular strands.
- Yan, Yan,Qin, Bo,Shu, Yingying,Chen, Xiuying,Yip, Yeow Kwan,Zhang, Dawei,Su, Haibin,Zeng, Huaqiang
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supporting information; experimental part
p. 1201 - 1204
(2009/08/07)
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- Crystallographic evidence of an unusual, pentagon-shaped folding pattern in a circular aromatic pentamer
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(Figure Presented) Introduction of a continuous hydrogen-bonding network suppressed the conformational flexibility of an oligomeric backbone. Cyclization of a rigidified, suitably sized oligomer led to a circular aromatic pentamer. Its crystal structure d
- Qin, Bo,Chen, Xiuying,Fang, Xiao,Shu, Yingying,Yip, Yeow Kwan,Yan, Yan,Pan, Siyan,Ong, Wei Qiang,Ren, Changliang,Su, Haibin,Zeng, Huaqiang
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supporting information; experimental part
p. 5127 - 5130
(2009/05/30)
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- HETEROCYCLIC COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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A heterocyclic compound of the formula (I): wherein B1 is -C(R2)= or -N=; R1' is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R5 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is -C(-Y)=C(-RA)-C(-R3)=C(-R4)-, etc. wherein Y is OH, etc.; RA is -COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.
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Page/Page column 48
(2008/06/13)
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- NITROGEN-CONTAINING HETEROARYL COMPOUNDS HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.
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