34598-50-0Relevant academic research and scientific papers
Thrombin inhibitors based on [5,5] trans-fused indane lactams
Pass, Martin,Abu-Rabie, Said,Baxter, Andrew,Conroy, Richard,Coote, Steven J.,Craven, Andrew P.,Finch, Harry,Hindley, Sean,Kelly, Henry A.,Lowdon, Andrew W.,McDonald, Edward,Mitchell, William L.,Pegg, Neil A.,Procopiou, Pan A.,Ramsden, Nigel G.,Thomas, Rhian,Walker, Dawn A.,Watson, Nigel S.,Jhoti, Harren,Mooney, Christopher J.,Tang, Chi-Man,Thomas, Pamela J.,Parry, Simon,Patel, Champa
, p. 1657 - 1662 (1999)
A series of trans-fused lactams containing the indane nucleus has been prepared. Compound 19 has much enhanced plasma stability compared with its lactone counterpart and shows appreciable in vitro anticoagulant activity.
Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1,3-diones: Dual inhibition against HIV reverse transcriptase-associated RNase H and polymerase with antiviral activities
Vernekar, Sanjeev Kumar V.,Liu, Zheng,Nagy, Eva,Miller, Lena,Kirby, Karen A.,Wilson, Daniel J.,Kankanala, Jayakanth,Sarafianos, Stefan G.,Parniak, Michael A.,Wang, Zhengqiang
, p. 651 - 664 (2015)
Reverse transcriptase (RT) associated ribonuclease H (RNase H) remains the only virally encoded enzymatic function not targeted by current chemotherapy against human immunodeficiency virus (HIV). Although numerous chemotypes have been reported to inhibit
Kinetic resolution of racemic benzofused alcohols catalysed by HMFO variants in presence of natural deep eutectic solvents
Fraaije, Marco,Lon?ar, Nikola,de Gonzalo, Gonzalo
, (2022/03/01)
5-Hydroxymethylfurfural oxidase (HMFO) has demonstrated to be a useful biocatalyst for the selective oxidation of alcohols employing oxygen as mild oxidant with no requirement of expensive organic cofactors. This wild-type HMFO biocatalyst and an engineered thermostable variant have been tested in the kinetic resolution of different benzofused alcohols. The use of natural deep eutectic solvents was also explored in HMFO-catalysed oxidation of alcohols. The oxidation of racemic 1-indanol showed a higher conversion and selectivity in presence of 60% v/v of different NADES, especially for those containing carbohydrates. By choosing properly the biocatalyst and the NADES, good enantioselectivity values can be obtained, demonstrating the advantages of employing these neoteric solvents in biocatalysed processes.
Development of Novel Phosphino-Oxazoline Ligands and Their Application in Asymmetric Alkynlylation of Benzylic Halides
Guo, Rui,Li, Junxia,Sang, Jiale,Xiao, Haijing,Zhang, Guozhu
supporting information, (2022/03/27)
A new set of stereochemically diverse phosphino-oxazoline ligands derived from simple L-amino acids and 2-(diphenylphosphaneyl)benzoic acid were developed. Those mono anionic tridentated N,N,P-ligands promote the Cu-catalyzed enantioselective radical coupling of terminal alkynes with a broad range of benzylic halides including benzo-fused cyclic α-halides and α-silyl benzyl halides in high yield and excellent enantioselectivity under mild reaction conditions. With multi distinct sites for structural modification, a diverse pool of chiral N,N,P-ligands is readily accessed, allowing for rapid optimization of the ligand structure for a specific substrate. Notably, the enantioselective alkynlylation of benzylic halides bonds in benzo-cyclic molecules has also been realized for the first time.
PERIPHERAL ALKYL AND ALKENYL CHAINS EXTENDED BENZENE DERIVATIVES AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME
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Paragraph 0063; 0164-0167, (2020/10/20)
The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX) / histone deacetylase (HD AC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.
Indene oxyacetic acid and preparation method and application thereof
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Paragraph 0055; 0057-0059, (2019/10/01)
The invention provides a compound shown in a formula I, or a conformational isomer thereof, or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a hydrate thereof, or a solvate thereof. Proved by experiment
JAK kinase inhibitor and application
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Paragraph 0096-0097; 0099-0101, (2018/09/08)
The present invention discloses a compound having the following general formula (I). The present invention also discloses a JAK kinase inhibitor comprising the compound and application of the compoundin preparation of a medicament for treating JAK-associated diseases. The JAK kinase inhibitor can inhibit the biological activities of JAK1, JAK2, JAK3 and TYK2 kinases involved in various kinds of signal transduction, can effectively treat various inflammatory diseases and various JAK-mediated signal transduction-driven diseases, and has a very broad application prospect.
Silylative Kinetic Resolution of Racemic 1-Indanol Derivatives Catalyzed by Chiral Guanidine
Yoshimatsu, Shuhei,Yamada, Akira,Nakata, Kenya
, p. 452 - 458 (2018/02/19)
Efficient kinetic resolution of racemic 1-indanol derivatives was achieved using triphenylchlorosilane by asymmetric silylation in the presence of chiral guanidine catalysts. The chiral guanidine catalyst (R,R)-N-(1-(β-naphthyl)ethyl)benzoguanidine was found to be highly efficient as only 0.5 mol % catalyst loading was sufficient to catalyze the reaction of various substrates with appropriate conversion and high s-values (up to 89). This catalyst system was successfully applied to the gram-scale silylative kinetic resolution of racemic 1-indanol with high selectivity.
Synthesis of Indole-Dihydroisoquinoline Sulfonyl Ureas via Three-Component Reactions
Pearson, Stuart E.,Fillery, Shaun M.,Goldberg, Kristin,Demeritt, Julie E.,Eden, Jonathan,Finlayson, Jonathan,Patel, Anil
, p. 4963 - 4981 (2018/12/13)
Isoquinolines activated with sulfamoyl chlorides were reacted with indoles in a 3-component reaction to generate a library of dihydroisoquinoline derivatives. Using a differential protecting group strategy, products could be further derivatised. Synthesis of isoquinoline starting materials using several different methods is also described.
Substituted ring compound and its method and use thereof
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Paragraph 0368; 0369, (2017/08/25)
The invention provides a substituted cyclic compound as well as a use method and application thereof. The compound is a compound as shown in a formula (I) or stereoisomers, stereomers, tautomers, nitric oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs of the compound as shown in the formula (I). The invention further provides a medicament composition containing the compound. The compound and the medicament composition are capable of regulating the activity of protein kinase in a biological sample body and are used for protecting, treating or relieving proliferative diseases of patients. The formula (I) is as shown in the specification.
