- Me2AlSEt-promoted domino dieckmann cyclization enables the total synthesis of polycyclic polyprenylated acylphloroglucinols
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A bioinspired, Me2AlSEt-promoted domino Dieckmann cyclization via an 8-membered ring intermediate to construct bicyclo[3.3.1]nonanes was developed, and the divergent syntheses of nine complex polycyclic polyprenylated acylphloroglucinols were a
- Wang, Liping,Sun, Lian,Wang, Xueying,Wu, Rong,Zhou, Hua,Zheng, Changwu,Xu, Hongxi
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supporting information
p. 8075 - 8079
(2019/10/14)
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- BICYCLIC HETEROARYL SUBSTITUTED COMPOUNDS
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Disclosed are compounds of Formula (I) to (IV): [INSERT CHEMICAL STRUCTURE HERE] or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmace
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Page/Page column 62
(2018/03/09)
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- ANTIVIRAL COMPOUNDS
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The present invention relates to novel compounds of general formula (I) wherein the groups X, and R1 to R4 have the meanings given in the description and claims, process for preparing these compounds and their use as for treating, preventing or ameliorating viral infections and their use for treating, preventing or ameliorating diseases which are associated with PLA2G16.
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Paragraph 0985
(2018/04/13)
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- A general method for making peptide therapeutics resistant to serine protease degradation: Application to dipeptidyl peptidase IV substrates
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Bioactive peptides have evolved to optimally fulfill specific biological functions, a fact which has long attracted attention for their use as therapeutic agents. While there have been some recent commercial successes fostered in part by advances in large-scale peptide synthesis, development of peptides as therapeutic agents has been significantly impeded by their inherent susceptibility to protease degradation in the bloodstream. Here we report that incorporation of specially designed amino acid analogues at the P1′ position, directly C-terminal of the enzyme cleavage site, renders peptides, including glucagon-like peptide-1 (7-36) amide (GLP-1) and six other examples, highly resistant to serine protease degradation without significant alteration of their biological activity. We demonstrate the applicability of the method to a variety of proteases, including dipeptidyl peptidase IV (DPP IV), dipeptidyl peptidase 8 (DPP8), fibroblast activation protein α (FAPα), α-lytic protease (αLP), trypsin, and chymotrypsin. In summary, the "P1′ modification" represents a simple, general, and highly adaptable method of generating enzymatically stable peptide-based therapeutics.
- Heard, Kathryn R.,Wu, Wengen,Li, Youhua,Zhao, Peng,Woznica, Iwona,Lai, Jack H.,Beinborn, Martin,Sanford, David G.,Dimare, Matthew T.,Chiluwal, Amrita K.,Peters, Diane E.,Whicher, Danielle,Sudmeier, James L.,Bachovchin, William W.
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supporting information
p. 8339 - 8351
(2013/12/04)
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- 184. Stereoselective Hydrolysis of Substituted Cyclopropanedicarboxylates with Pig Liver Esterase
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The hydrolysis of the meso-cyclopropane-1,2-dicarboxylates 1a-3a, 4, 5a, 6a, and 9, containing various substituents at C(3), and of the rac-3-phenylcyclopropane-1,2-dicarboxylates 7a, 8a, and 10 with pig liver esterase (PLE) is described.The stereoselectivity and absolute configurations of the products were determined.An interpretation of results was attempted on the basis of a recent active-site model for PLE.
- Walser, Paula,Renold, Peter,N'Goka, Victor,Hosseinzadeh, Fatemeh,Tamm, Christoph
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p. 1941 - 1952
(2007/10/02)
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- Process for the production of 3,3-dimethylglutaric acid or its esters
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Process for the production of 3,3-dimethylglutaric acid or its esters from dimedone. Dimedone is converted with ozone into an ozone-addition product. The latter is converted by hydrolysis into 3,3-dimethylglutaric acid or by alcoholysis into one of its esters.
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- INTRAMOLECULAR OXIDATIVE COUPLING OF THE BIS ENOLATE DERIVED FROM DIMETHYL β,β-DIMETHYLGLUTARATE: A FACILE STEREOSELECTIVE ROUTE TO A VERSATILE SYNTHON FOR PREPARATION OF INSECTICIDAL PYRETHROIDS
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Treatment of the bis enolate derived from dimethyl β,β-dimethylglutarate with silver chloride afforded dimethyl cis-3,3-dimethyl-1,2-cyclopropanedicarboxylate, a versatile synthon for the preparation of the acid component of cis-pyrethroids.A similar experiment utilizing iodine as the oxidant led to the isolation of the corresponding trans diester with good stereoselectivity.
- Babler, James H.,Haack, Richard A.
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p. 905 - 912
(2007/10/02)
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