- MACROCYCLIC INHIBITORS OF PEPTIDYLARGININE DEIMINASES
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The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
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Page/Page column 377; 410-411
(2021/11/06)
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- SYNTHESIS OF ANTIVIRAL COMPOUND
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The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
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Paragraph 0225
(2014/01/07)
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- Enantioselective epoxidation of α,β-enones promoted by (1R,3S,4S)-2-azanorbornyl-3-methanol as an organocatalyst
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(1R,3S,4S)-2-Azanorbornyl-3-methanol was synthesized form (R)-1-phenylethylamine and used as a catalyst for the enantioselective epoxidation of α,β-enones to afford the corresponding epoxides in good yields and high enantioselectivities at room temperature.
- Lu, Jun,Xu, Yun-He,Liu, Feng,Loh, Teck-Peng
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supporting information; scheme or table
p. 6007 - 6008
(2009/04/04)
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- 2-CYANOPYRROLIDINECARBOXAMIDE COMPOUND
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A compound of the formula (I) or a pharmaceutically acceptable salt thereof: [wherein X1 and X2 each is independently lower alkylene; X3 is =CH2, =CHF or =CF2; R1 is substituent, R2 and R3 each is independently H or lower alkyl; n is 0, 1, 2, 3 or 4.] having the activity inhibiting DPP-IV activity. They are therefore useful in the treatment of conditions mediated by DPP-IV, such as NIDDM.
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Page/Page column 115-116
(2008/06/13)
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- Aza-Diels - Alder reaction of methyl 2-[(R)-1-phenylethyl]iminoethanoate with cyclopentadiene using practical and environmentally friendly biphasic solvent system
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Aza-Diels - Alder reaction between 2-[(R)-1-phenylethyl]imino-ethanoate (1) and cyclopentadiene using the biphasic solvent system (TMSCl-CH 3OH/toluene) gave (1S,3S,4R)-2-[(R)-1-phenylethyl]-2-aza-bicyclo[2.2. 1]hept-5-ene-3-carboxylates (3a) i
- Hashimoto, Norio,Yasuda, Hironobu,Hayashi, Masaru,Tanabe, Yoo
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p. 105 - 109
(2012/12/24)
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- A rigid dirhodium(II) carboxylate as an efficient catalyst for the asymmetric cyclopropanation of olefins
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The dirhodium(II) complex 7 of (1S,3R,4R)-2-(p-tert-butylphenylsulphonyl)-2-aza-bicyclo[2.2.1]heptane-3- carboxylic acid (3) (or its enantiomer) was synthesised in four steps from cyclopentadiene, (R)- or (S)-phenylethylamine and methyl glyoxylate. Comple
- Bertilsson, Sophie K.,Andersson, Pher G.
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- REACTION D'AZA-DIELS-ALDER DIASTEREOSELECTIVE: UTILISATION DE LA 1-PHENYLETHYL IMINE DE GLYOXYLATE D'ALKYLE POUR LA SYNTHESES DE DERIVES D'α-AMINO ACIDES CYCLIQUES
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The use of trifluoroacetic acid-boron trifluoride combination is highly effective in dichloromethane for the activation of 1-phenylethylimine of methyl or ethyl glyoxylates as heterodienophiles in Diels-Alder cycloaddition reactions with a series of conju
- Abraham, Herve,Stella, Lucien
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p. 9707 - 9718
(2007/10/02)
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- Asymmetric aza-diels-alder reaction using the chiral 1-phenyl ethyl imine of methyl glyoxylate
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The Diels-Alder reaction between cyclopentadiene and the chiral 1-phenyl-ethyl imine of methyl glyoxylate takes place very easily by activation with trifluoroacetic acid and boron trifluoride etherate to provide diastereoselectively (total face selectivit
- Stella,Abraham,Feneau-Dupont,Tinant,Declercq
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p. 2603 - 2606
(2007/10/02)
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