6453-07-2Relevant articles and documents
THIENOPYRIMIDINE DERIVATIVE AND USE THEREOF IN MEDICINE
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Paragraph 00229, (2018/08/12)
The present invention relates to a thienopyrimidine derivative and use thereof in medicine, and also to a pharmaceutical composition containing the compound. The compound or pharmaceutical composition is used for inhibiting acetyl-CoA carboxylase (ACC). The present invention also relates to a method of preparing such compound and pharmaceutical composition, as well as their use in the treatment or prevention of diseases regulated by acetyl-CoA carboxylase in mammals, especially in humans.
PROCESSES AND INTERMEDIATES FOR PREPARING A MACROCYCLIC PROTEASE INHIBITOR OF HCV
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Page/Page column 22; 32, (2017/01/09)
Disclosed is a process for the preparation of certain intermediates, e.g. those in the scheme below: which intermediates and processes are useful in the preparation of the macrocyclic HVC inhibitor Simeprevir.
The Synthesis of Novel Trans-Oxabicyclo[3,3,0]octane Systems as Potential Inhibitors of HIV Protease
Mahler, Mikael E.,Palmer, Michael J.
, p. 193 - 194 (2007/10/03)
The novel trans-3-oxabicyclo[3,3.0]octan-7-one system has been prepared by intramolecular ring closure of the corresponding cyclopentane diol. Peralkylation and benzylidene substitution of the octanone has allowed the preparation of tetra-alkylated potential inhibitors of HIV protease. Weak activity against HIV protease (IC50's 70-100μM) was observed.
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: New tools to discriminate between metabotropic glutamate receptor subtypes
Acher, Francine C.,Tellier, Frédérique J.,Azerad, Robert,Brabet, Isabelle N.,Fagni, Laurent,Pin, Jean R.
, p. 3119 - 3129 (2007/10/03)
The four stereoisomers of 1-aminocyclopentane-1,3,4-tricarboxylic acid {ACPT-I (18) and -II (19), (3R,4R)-III [(-)-20], and (3S,4S)-III [(+)-20]} have been synthesized and evaluated for their effects at glutamate receptors subtypes. ACPTs are ACPD analogues in which a third carboxylic group has been added at position 4 in the cyclopentane ring. None of the ACPT isomers showed a significant effect on ionotropic NMDA, KA, and AMPA receptors. On the other hand, ACPT-III (19) was found to be a general competitive antagonist for metabotropic receptors (mGluRs) and exhibited a similar affinity for mGluR1a (K(B) = 115 ± 2 μM), mGluR2 (K(B) = 88 ± 21 μM), and mGluR4a (K(B) = 77 ± 9 μM), the representative members of group I, II and III mGluRs, respectively. Two other isomers, ACPT-I (18) and (+)-(3S,4S)-ACPT-III [(+)- 20], were potent agonist at the group III receptors mGluR4a (EC50 = 7.2 ± 2.3 and 8.8 ± 3.2 μM) and competitive antagonists with low affinity for mGluR1a and mGluR2 (K(B) > 300 μM). Finally, (-)-(3R,4R)-ACPT-III [(-)-20] was a competitive antagonist with poor but significant affinity for mGluR4a (K(B) = 220 μM). These results demonstrate that the addition of a third carboxylic group to ACPD can change its activity (from agonist to antagonist) and either increase or decrease its selectivity and/or affinity for the various mGluR subtypes.
SYNTHESIS OF RING-ENLARGED CYCLOBUT-A AND CYCLOBUT-G ANALOGUES AS HIV INHIBITORS. PART 4
Boumchita, Hassane,Legraverend, Michel,Bisagni, Emile
, p. 1785 - 1792 (2007/10/02)
Two ring-expanded analogues (compounds 13 and 14) of the anti-HIV agents Cyclobut-A and Cyclobut-G are described.They were synthesized from trans-3,4-bis(hydroxymethyl)cyclobutylamine which was obtained from threo-3,4-bis(methoxycarbonyl)hexane dioic acid.Neither compound (13,14) was able to provide protection to CEM cells against HIV-1-infection.
Enzyme-Catalyzed Asymmetric Synthesis. 8. Enantioselectivity of Pig Liver Esterase Catalyzed Hydrolyses of 4-Substituted Meso Cyclopentane 1,2-Diesters
Gais, Hans-Joachim,Buelow, Gerd,Zatorski, Andrzej,Jentsch, Mathias,Maidonis, Peter,Hemmerle, Horst
, p. 5115 - 5122 (2007/10/02)
Hydrolyses of meso-1,2-cyclopentanedicarboxylic acid bis(methyl esters) bearing in the 4-position an oxo, methylene, cis-hydroxy, trans-hydroxy,cis-acetoxy, trans-acetoxy, cis-methoxy, cis-tert-butoxy, ethylenedioxy, propylenedioxy, dimethyl propylenediox
Diastereoselectivity of a Annulation. On the Question of a Dipole Effect on Diastereoselectivity of Olefin Addition
Trost, Barry M.,Lynch, Joseph,Renaut, Patrice
, p. 6313 - 6316 (2007/10/02)
The stereochemistry of addition to γ-alkoxy-α,β-unsaturated carbonyl systems is examined in the context of a palladium catalyzed cycloaddition.
A SYNTHESIS OF (+/-)-BREFELDIN A
Honda, Masanori,Hirata, Kazumasa,Sueoka, Hiroyuki,Katsuki, Tsutomu,Yamaguchi, Masaru
, p. 2679 - 2682 (2007/10/02)
A macrolide antibiotic, brefeldin A, was synthesized from trans-4-oxocyclopentane-1,2-dicarboxylic acid in a stereoselective manner, the intermediary hydroxyl acid being lactonized by the mixed 2,4,6-trichlorobenzoic acid anhydride - 4-dimethylaminopyridi