- 6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
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Paragraph 0954; 0955
(2021/11/13)
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- N-(AZAARYL)CYCLOLACTAM-1-CARBOXAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
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An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.
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Paragraph 0143; 0294; 0295
(2020/03/23)
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- PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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Compounds of Formula I and methods of use as Interleukin-1 Receptor Associated Kinase 4 (IRAK4) inhibitors are described herein.
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Page/Page column 58
(2018/05/24)
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- Process for the Preparation of Triazole Antifungal Drug, Its Intermediates and Polymorphs Thereof
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A process for the preparation of 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1S,2S)-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one compound of formula-1, its intermediates and polymorphs thereof. (I)
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Paragraph 0327
(2014/12/09)
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- Catalytic enantioselective inverse electron demand hetero-diels-alder reaction with allylsilanes
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The first diastereo- and enantioselective inverse electron demand hetero-Diels-Alder reaction of β,γ-unsaturated α-ketoesters with allylsilanes is described. Chiral copper(II) catalysts successfully activate the β,γ-unsaturated α-ketoesters and promote the reaction with allylsilanes with excellent enantioselectivities. This process represents a new entry to chiral oxanes.
- Matsumura, Yuki,Suzuki, Takahiro,Sakakura, Akira,Ishihara, Kazuaki
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supporting information
p. 6131 - 6134
(2014/06/23)
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- Stereoselective synthesis of functionalised triol units by SnCl4 promoted allylation of α-benzyloxyaldehydes: Crucial role of the stoichiometry of the Lewis acid
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Enantiomerically pure syn-anti and syn-syn configured triol units are efficiently synthesized by the SnCl4 mediated allylation of chiral α-benzyloxyaldehydes with the uniquely functionalised allylstannane 9. Remarkably, the stereochemistry of t
- Dubost, Christophe,Leroy, Bernard,Markó, Istvan E.,Tinant, Bernard,Declercq, Jean-Paul,Bryans, Justin
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p. 7693 - 7704
(2007/10/03)
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- Microbial deracemization of α-substituted carboxylic acids: Substrate specificity and mechanistic investigation
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A new enzymatic method for the preparation of optically active α-substituted carboxylic acids is reported. This technique is called deracemization reaction, which provides us with a route to obtain the enantiomerically pure compounds, theoretically in 100% yield starting from the racemic mixture. This means that the synthesis of a racemate is almost equal to the synthesis of the optically active compound, and this concept is entirely different from the commonly accepted one in the asymmetric synthesis. Using the growing cell system of Nocardia diaphanozonaria JCM3208, racemates of 2-aryl- and 2-aryloxypropanoic acid are deracemized smoothly and (R)-form-enriched products are recovered in high chemical yield (>50%). In addition, using optically active starting compounds and deuterated derivatives as well as inhibitors, we have disclosed the fact that a new type of enzyme takes part in this biotransformation, and that the reaction proceeds probably via the same mechanism as that in rat liver.
- Kato, Dai-Ichiro,Mitsuda, Satoshi,Ohta, Hiromichi
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p. 7234 - 7242
(2007/10/03)
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- The "Aqueous" Prins Reaction
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(Equation presented) In this communication we demonstrate that Prins cyclization reactions occur under very mild conditions when cyclic α,β-unsaturated acetals are employed as oxocarbenium ion progenitors and allylsilanes are used as nucleophiles. Cycliza
- Aubele, Danielle L.,Lee, Christopher A.,Floreancig, Paul E.
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p. 4521 - 4523
(2007/10/03)
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- Asymmetric synthesis of (R)-(-)-chlozolinate through a chemoenzymatic procedure
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A new asymmetric synthesis of (R)-chlozolinate 1, an important antifungal agent, based on the enzymatic asymmetrization of diethyl 2-benzyloxy-2-methylmalonate, is reported.
- Guanti, Giuseppe,Banfi, Luca,Powles, Katharine,Rasparini, Marcello,Scolastico, Carlo,Fossati, Novella
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p. 271 - 277
(2007/10/03)
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- Almond oxynitrilase-catalyzed transformation of aldehydes is strongly influenced by naphthyl and alkoxy substituents
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Different α- and β-substituted aldehydes have been submitted to the catalytic action of almond oxynitrilase (PaHNL), in order to explore the influence of a stereocenter already present in the substrate on the selectivity of this enzyme. The results indicate that naphthyl and alkoxy substituents in the α- and also in the β-position to the aldehyde group significantly influence the stereochemical outcome of the PaHNL-catalyzed transformation.
- Roda, Gabriella,Riva, Sergio,Danieli, Bruno
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p. 3939 - 3949
(2007/10/03)
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- Aminodiol HIV protease inhibitors. Synthesis and structure - Activity relationships of P1/P1′ compounds: Correlation between lipophilicity and cytotoxicity
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A series of novel aminodiol inhibitors of HIV protease based on the lead compound 1 with structural modifications at P1′ were synthesized in order to reduce the cytotoxicity of 1. We have observed a high degree of correlation between the lipophilicity and the cytotoxicity of this series of inhibitors. It was found that appropriate substitution at the para position of the P1′ phenyl group of 1 resulted in the identification of equipotent (both against the enzyme and in cell culture) compounds (101, 10m, 10n, and 15c) which possess significantly decreased cytotoxicity.
- Chen, Ping,Cheng, Peter T. W.,Alam, Masud,Beyer, Barbara D.,Bisacchi, Gregory S.,Dejneka, Tamara,Evans, Adelaide J.,Greytok, Jill A.,Hermsmeier, Mark A.,Humphreys, W. Griffith,Jacobs, Glenn A.,Kocy, Octavian,Lin, Pin-Fang,Lis, Karen A.,Marella, Michael A.,Ryono, Denis E.,Sheaffer, Amy K.,Spergel, Steven H.,Sun, Chong-Qing,Tino, Joseph A.,Vite, Gregory,Colonno, Richard J.,Zahler, Robert,Barrish, Joel C.
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p. 1991 - 2007
(2007/10/03)
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- Labelled Representatives of a Possible Intermediate of Fosfomycin Biosythesis in Streptomyces fradiae: Preparation of (R,S)-(2-Hydroxypropyl)-, (R,S)-, (R)-, (S)-(2-Hydroxypropylpropyl- and (R,S)-(2-Hydroxypropyl)phosphonic acid
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Racemic methyl O-benzyllactate was reduced to the alcohol, transformed into the bromide and reacted with triethylphosphite to give the diethylphosphonate.Removal of protecting groups afforded a phosphonic acid which was purified as its cyclohexylammonium
- Hammerschmidt, Friedrich
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p. 389 - 398
(2007/10/02)
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