- Pd(II)-Catalyzed Direct ?-C(sp3)-H Arylation between Free β2-Amino Esters and β3-Amino Esters and Aryl Iodides Using a Catalytic Transient Directing Group
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Pd(II)-catalyzed direct ?-C(sp3)-H arylation coupling with free β2-amino esters and β3-amino esters using a commercially available catalytic transient directing group has been developed. This approach features high efficiency, broad substrate tolerance, easily accessible starting materials, and mild reaction conditions.
- Wang, Zhaohui,Fu, Yangjie,Zhang, Qiyu,Liu, Hong,Wang, Jiang
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p. 7683 - 7693
(2020/07/15)
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- SUBSTITUTED DIHYDRO-1H-PYRROLO[3,2-c]PYRIDIN-4(5H)-ONES AS RIPK3 INHIBITORS
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Compounds having Formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK3 modulation. All the variables defined herein.
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Page/Page column 110; 111
(2016/07/05)
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- USE OF CONDENSED BENZO[B]THIAZINE DERIVATIVES AS CYTOPROTECTANTS
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The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters,pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds.
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Page/Page column 64
(2014/12/12)
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- 4 -HYDROXY- ISOQUINOLINE COMPOUNDS AS HIF HYDROXYLASE INHIBITORS
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The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias.
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Paragraph 0258
(2013/09/26)
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- BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS
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Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SlP receptors.
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Page/Page column 61
(2011/02/24)
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- TASK CHANNEL ANTAGONISTS
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This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders
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Page/Page column 53
(2011/09/21)
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- TASK CHANNEL ANTAGONISTS
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This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders
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Page/Page column 52
(2011/09/30)
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- Synthesis of sterically hindered 3,5,5-trimethyl 2,6-dioxo tetrahydro pyrimidine as HCV protease inhibitors
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An efficient route for the synthesis of sterically hindered substituted and unsubstituted 2,6-dioxo tetrahydropyrimidines from amine 1 is described. These analogs are active against HCV NS3 serine protease. The biological data for some of the representati
- Nair, Latha G.,Bogen, Stephane,Doll, Ronald J.,Shih,Njoroge, F. George
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scheme or table
p. 1276 - 1279
(2010/04/29)
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- POLO-LIKE KINASE INHIBITORS
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Compounds of the following formula are provided for use with kinases, wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful
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Page/Page column 207; 208
(2009/06/27)
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- Structural modification of the P2′ position of 2,7-dialkyl- substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: The discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets
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Due to its function in the rate limiting initial step of the renin-angiotensin system, renin is a particularly promising target for drugs designed to control hypertension, a growing risk to health worldwide. Despite vast efforts over more than two decades
- Maibaum, Jürgen,Stutz, Stefan,G?schke, Richard,Rigollier, Pascal,Yamaguchi, Yasuchika,Cumin, Frédéric,Rahuel, Joseph,Baum, Hans-Peter,Cohen, Nissim-Claude,Schnell, Christian R.,Fuhrer, Walter,Gruetter, Markus G.,Schilling, Walter,Wood, Jeanette M.
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p. 4832 - 4844
(2008/03/12)
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- AMIDE SUBSTITUTED IMIDAZOPYRIDINES, IMIDAZOQUINOLINES, AND IMIDAZONAPHTHYRIDINES
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Imidazopyridine, imidazoquinoline, and imidazonaphthyridine compounds having an amide substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
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Page/Page column 51
(2010/11/28)
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- The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic
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The Asp-Pro sequence of the cyclic peptide Ac-HN-Tyr-Cys*-Asp-Pro-Cys*-OH (1) could be replaced with the achiral dipeptide mimetic 1-(2-aminoethyl)cyclpentylcarboxylic acid with retention of potent inhibition of the VCAM-VLA-4 interaction. (C) Elsevier Science Ltd. All rights reserved.
- Fotouhi, Nader,Joshi, Pramod,Fry, David,Cook, Charles,Tilley, Jefferson W.,Kaplan, Gerry,Hanglow, Angela,Rowan, Karen,Schwinge, Virginia,Wolitzky, Barry
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p. 1171 - 1173
(2007/10/03)
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