- SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE
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The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
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Page/Page column 169
(2020/12/11)
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- Cyclic gyrase and topoisomerase IV inhibitor
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The invention belongs to the technical field of medicament, and particularly relates to a compound shown in formula (I) (please see the formula (I) in the description), and acceptable salt, ester or stereoisomer of the compound in pharmacy. R1, R2, a ring
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Paragraph 0158; 0159; 0160
(2017/01/02)
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- Enantiopure synthesis of 7-(1-pyrindanyl)propargyl ethers as rasagiline analogues via chemical or enzymatic resolution of 1-pyrindan-7-ol
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In this work, the enantiopure synthesis of 7-(1-pyrindanyl)propargyl ethers - rasagiline analogues - via chemical and/or enzymatic resolution of the racemic precursor 1-pyrindan-7-ol is described. (R)-Methoxyphenylacetic acid - (R)-MPAA - and (S)-methoxyphenylacetic acid - (S)-MPAA were used as chemical resolution agents, whereas Candida antarctica lipase B (CALB) was employed as kinetic resolution catalyst. The enzymatic resolution was successfully achieved by two different approaches: (1) transesterification of racemic 1-pyrindan-7-ol, which was found to selectively acylate the (R)-enantiomer with high efficiency; (2) hydrolysis of the racemic 7-(1-pyrindanyl)acetate, which was also highly selective to the (R)-enantiomer. The enzymatic hydrolysis was performed in a non-aqueous solvent using a lipase with significant absorbed water content. The configuration of the two enantiomers of 1-pyrindan-7-ol (and consequently of the 7-(1-pyrindanyl)propargyl ethers) were unequivocally determined by X-ray crystallography and/or specific optical rotation.
- Sousa, Carlos A. D.,Sampaio-Dias, Ivo E.,Rizzo-Aguiar, Fabio,Garcia-Mera, Xerardo,Rodríguez-Borges, José E.
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p. 104509 - 104515
(2015/12/24)
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- Organocatalysts with carbon-centered activity for CO2 reduction with boranes
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We report two organocatalysts for CO2 hydroboration to methylborylethers, which upon hydrolysis can produce methanol. These organocatalysts feature carbon-centered reversible CO2 binding, broad borane scopes, and high catalytic activities.
- Yang, Yanxin,Xu, Maotong,Song, Datong
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supporting information
p. 11293 - 11296
(2015/07/07)
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- Synthesis of New Propargylated 1-Pyrindane Derivatives as Rasagiline Analogues
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Rasagiline is a compound with important neuroprotective activity applicable to the treatment of neurodegenerative diseases. This work describes an easy and straightforward methodology to the synthesis of new propargylated rasagiline analogues derived from commercially available 6,7-dihydro-5H-cyclopenta[b] pyridine. Georg Thieme Verlag Stuttgart - New York.
- Pereira, Cidáliasilva,Salgado, Sofia,Rizzo-Aguiar, Fabio,Garcia-Mera, Xerardo,Rodríguez-Borges, Josée.
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supporting information
p. 837 - 838
(2013/05/21)
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- DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS
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The instant invention relates to derivatives of formula (I) and their application in therapeutics.
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Page/Page column 45
(2011/10/03)
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- Derivatives of aminoindanes, their preparation and their application in therapeutics
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The instant invention relates to derivatives of formula (I) and their application in therapeutics.
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Page/Page column 25
(2011/10/12)
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- Palladium-catalyzed acetoxylation of sp3 C-H bonds using molecular oxygen
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Molecular oxygen as oxidant to promote palladium-catalyzed acetoxylation of sp3 C-H bonds to afford α-oxygenated products is reported.
- Jiang, Huanfeng,Chen, Huoji,Wang, Azhong,Liu, Xiaohang
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supporting information; experimental part
p. 7259 - 7261
(2011/01/07)
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- FUSED AND SPIROCYCLE COMPOUNDS AND THE USE THEREOF
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The invention relates to fused and spirocycle compounds of Formula (I), or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
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Page/Page column 73
(2008/06/13)
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- A New Approach to the Preparation of 1,6- and 1,7-Naphthyridines
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Substituted 1,6- and 1,7-naphthyridines can be prepared by a simple route from readily available pyrindane; this method is more flexible and produces higher yields than previous routes.
- Giam, C. S.,Ambrozich, Deborah
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p. 265 - 266
(2007/10/02)
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