88099-67-6Relevant academic research and scientific papers
NEW MACROCYCLIC LRRK2 KINASE INHIBITORS
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Page/Page column 421, (2021/11/13)
Compounds of formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description. Medicaments.
BICYCLIC HETEROCYCLE SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE MODULATORS
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Paragraph 00158, (2014/05/24)
Compounds having the following formula (I) or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a bicyclic heterocycle, and R1, R3, R4, R5 and R6 are as defined herein, that are useful as kinase modulators, including IRAK-4 modulation.
HETEROARYL SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE MODULATORS
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Paragraph 00229, (2019/03/15)
Compounds having the following formula (I) or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.
Synthesis of syn-γ-amino-β-hydroxyphosphonates by reduction of β-ketophosphonates derived from L-proline and L-serine
Ordonez, Mario,Lagunas-Rivera, Selene,Hernandez-Nunez, Emanuel,Labastida-Galvan, Victoria
scheme or table, p. 1291 - 1301 (2010/06/13)
The reduction of γ-N-benzylamino-β-ketophosphonates 6 and 10, readily available from L-proline and L-serine, respectively, can be carried out in high diastereoselectivity with catecholborane (CB) in THF at -78 °C to produce the syn-γ-N-benzylamino-β-hydro
Synthesis and pharmacological evaluation of novel γ-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors
Alstermark, Christer,Amin, Kosrat,Dinn, Sean R.,Elebring, Thomas,Fjellstr?m, Ola,Fitzpatrick, Kevin,Geiss, William B.,Gottfries, Johan,Guzzo, Peter R.,Harding, James P.,Holmén, Anders,Kothare, Mohit,Lehmann, Anders,Mattsson, Jan P.,Nilsson, Karolina,Sundén, Gunnel,Swanson, Marianne,Von Unge, Sverker,Woo, Alex M.,Wyle, Michael J.,Zheng, Xiaozhang
scheme or table, p. 4315 - 4320 (2009/05/30)
We have previously demonstrated that the prototypical GABAB receptor agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the most important mechanism for gastroesophageal reflux. Thus, GABAB agonists could be exploited for the treatment of gastroesophageal reflux disease. However, baclofen, which is used as an antispastic agent, and other previously known GABAB agonists can produce CNS side effects such as sedation, dizziness, nausea, and vomiting at higher doses. We now report the discovery of atypical GABAB agonists devoid of classical GABAB agonist related CNS side effects at therapeutic doses and the optimization of this type of compound for inhibition of TLESRs, which has resulted in a candidate drug (R)-7 (AZD3355) that is presently being evaluated in man.
PROCESS FOR THE SYNTHESIS OF ALKYL PHOSPHINIC ACIDS BY INITIATION OF AN AMINE AND AN AMINEOXIDE
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Page/Page column 11-12, (2009/01/20)
The present invention relates toa new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.
PROCESS FOR THE SYNTHESIS OF ALKYL PHOSPHINIC ACIDS BY INITIATION OF AN AMINE AND AN AMINEOXIDE
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Page/Page column 9-10, (2009/01/20)
The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.
NEW PROCESS FOR THE PREPARATION OF PHOSPHINIC ACID
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Page/Page column 8, (2008/06/13)
A new process for the synthesis of a compound of formula [Chemical formula should be inserted here. Please see paper copy] wherein A represents O or N; R?1? represents a C?1#191-C?6#191 alkyl; R?2? and R?3? each independently represents C?1#191-C?10#191 a
Stereochemistry of Catabolism of the DNA Base Thymine and of the Anticancer Drug 5-Fluorouracil
Gani, David,Hitchcock, Peter B.,Young, Douglas W.
, p. 1363 - 1372 (2007/10/02)
(2S)-3-Amino-2-methylpropanoic acid (6) and (2RS,3S)--3-amino-2-methylpropanoic acid (14) have been synthesized and used to provide an assay which shows that the catabolism of the DNA base thymine (1; R = Me) proceeds by overall anti addition of hydrogen to the pyrimidine at the si face at C-5 and the si face at C-6.X-Ray structure analysis of a derivative of the product of reaction of N,N-dibenzyl-L-serine methyl ester (15; R = Me) with (diethylamino)sulphur trifluoride followed by deprotection has shown it to be (2R)-3-amino-2-fluoropropanoic acid (19; R = H).This was identical with the product of catabolism of the anti-cancer drug 5-fluorouracil (1; R = F).Esters of (2R,3S)-- and (2R,3R)--3-amino-2-fluoropropanoic acids have been synthesized and used to provide an assay which shows that catabolism of the anti-cancer drug 5-fluorouracil (1; R = F) proceeds with the same absolute stereochemistry as is found in catabolism of thymine (1; R = Me).
