- Preparation method of 5-bromo-7-methylindole
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The invention discloses a preparation method of 5-bromo-7-methylindole. The structure of an intermediate corresponds to a formula V. The preparation method comprises the following steps: using 4-bromo-2-methylaniline as an initial raw material, and carryi
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Paragraph 0061-0068; 0083-0090; 0105-0112; 0127-0134
(2021/07/01)
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- Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors
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In an in-house screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target.
- Yang, Bowen,Wu, Qian,Huan, Xiajuan,Wang, Yingqing,Sun, Yin,Yang, Yueyue,Liu, Tongchao,Wang, Xin,Chen, Lin,Xiong, Bing,Zhao, Dongmei,Miao, Zehong,Chen, Danqi
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supporting information
(2020/12/28)
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- Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay
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Inappropriate activation of endosomal TLR7 and TLR8 occurs in several autoimmune diseases, in particular systemic lupus erythematosus (SLE). Herein, the development of a TLR8 antagonist competition assay and its application for hit generation of dual TLR7
- Knoepfel, Thomas,Nimsgern, Pierre,Jacquier, Sébastien,Bourrel, Marjorie,Vangrevelinghe, Eric,Glatthar, Ralf,Behnke, Dirk,Alper, Phil B.,Michellys, Pierre-Yves,Deane, Jonathan,Junt, Tobias,Zipfel, Géraldine,Limonta, Sarah,Hawtin, Stuart,Andre, Cedric,Boulay, Thomas,Loetscher, Pius,Faller, Michael,Blank, Jutta,Feifel, Roland,Betschart, Claudia
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p. 8276 - 8295
(2020/08/24)
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- Isothiourea-Catalyzed Atroposelective N-Acylation of Sulfonamides
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We report herein an atroposelective N-acylation of sulfonamides using a commercially available isothiourea catalyst, (S)-HBTM, with a simple procedure. The N-sulfonyl anilide products can be obtained in good to high enantiopurity, which represents a new axially chiral scaffold. The application of the product as a chiral iodine catalyst is also demonstrated for the asymmetric α-oxytosylation of propiophenone.
- Ong, Jun-Yang,Ng, Xiao Qian,Lu, Shenci,Zhao, Yu
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supporting information
p. 6447 - 6451
(2020/09/02)
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- ARYL, HETEROARY, AND HETEROCYCLIC PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
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Page/Page column 638; 639
(2018/09/21)
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- PARAZOLE CONDENSED-RING DERIVATIVES AND PREPARATION METHOD THEREOF AND APPLICATION THEREOF IN TREATMENT OF CANCERS, INFLAMMATION AND IMMUNE DISEASES
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The present invention relates to pyrazole fused-ring derivatives, their preparation methods, and use thereof in medicine. In particular, the present invention relates to a novel derivative represented by formula (I), and a pharmaceutically acceptable salt
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Paragraph 0117; 0118
(2018/12/13)
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- Synthesis of shape-persistent macrocycles with three 1,8-diazaanthracene units and their packing in the single crystal
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The synthesis of four shape-persistent macrocycles with three 1,8-diazaanthracene units each is reported (2,3 a-3 c). For two of them single crystals could be obtained and the structures in the crystal be solved. The structures reveal that macrocycle 2 se
- Li, Ming,Klaerner, Frank-Gerrit,Sakamoto, Junji,Schlueter, A. Dieter
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supporting information
p. 13348 - 13354
(2013/10/08)
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- INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE
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Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-m
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Page/Page column 10
(2011/04/13)
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- 2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization
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We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter) demonstrated a unique inhibitor binding mode. Resulting inhibitors had IC50 values as low as 19 nM and moderate selectivity against a kinase panel. Compounds 15, 31a, and 31b inhibit TNFα production in peripheral human monocytes.
- Harris, Christopher M.,Ericsson, Anna M.,Argiriadi, Maria A.,Barberis, Claude,Borhani, David W.,Burchat, Andrew,Calderwood, David J.,Cunha, George A.,Dixon, Richard W.,Frank, Kristine E.,Johnson, Eric F.,Kamens, Joanne,Kwak, Silvia,Li, Biqin,Mullen, Kelly D.,Perron, Denise C.,Wang, Lu,Wishart, Neil,Wu, Xiaoyun,Zhang, Xiaolei,Zmetra, Tami R.,Talanian, Robert V.
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scheme or table
p. 334 - 337
(2010/04/02)
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- INHIBITORS OF IKK-β SERINE-THREONINE PROTEIN KINASE
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Cyclopentyl (2S,4E)-2-amino-5-{3-[4-carbamoyl-5 (carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl (2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-
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Page/Page column 20
(2009/12/05)
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- Asymmetric radical and anionic cyclizations of axially chiral carbamates
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Standard Boc, Alloc, and Cbz derivatives of N-2,4-dimethyl-6-iodophenyl-N- allyl anilines are axially chiral and can be readily resolved into atropisomers whose racemization barriers exceed 30 kcal/mol. The resolved axially chiral carbamates undergo radic
- Guthrie, David B.,Curran, Dennis P.
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supporting information; experimental part
p. 249 - 251
(2009/06/28)
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- Low-temperature Heck reactions of axially chiral o-iodoacrylanilides occur with chirality transfer: Implications for catalytic asymmetric Heck reactions
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Low-temperature Heck reactions of chiral o-iodoacrylanilides with achiral palladium catalysts occur with efficient transfer of chirality from the chiral axis of the precursor to the new stereocenter of the product. The results suggest that the primary ste
- Lapierre, Andre J. B.,Geib, Steven J.,Curran, Dennis P.
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p. 494 - 495
(2007/10/03)
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