172023-97-1Relevant articles and documents
Insight into the complete substrate-binding pocket of ThiT by chemical and genetic mutations
Swier,Monjas,Ree?ing,Oudshoorn,Aisyah,Primke,Bakker,Van Olst,Ritschel,Faustino,Marrink,Hirsch,Slotboom
, p. 1121 - 1130 (2017)
Energy-coupling factor (ECF) transporters are involved in the uptake of micronutrients in bacteria. The transporters capture the substrate by high-affinity binding proteins, the so-called S-components. Here, we present the analysis of two regions of the s
FUSED BICYCLIC RAF INHIBITORS AND METHODS FOR USE THEREOF
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Paragraph 0345-0347, (2022/02/09)
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method o
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors
Degnan, Andrew P.,Tora, George O.,Han, Ying,Rajamani, Ramkumar,Bertekap, Robert,Krause, Rudolph,Davis, Carl D.,Hu, Joanna,Morgan, Daniel,Taylor, Sarah J.,Krause, Kelly,Li, Yu-Wen,Mattson, Gail,Cunningham, Melissa A.,Taber, Matthew T.,Lodge, Nicholas J.,Bronson, Joanne J.,Gillman, Kevin W.,Macor, John E.
, p. 3039 - 3043 (2015/06/22)
Depression is a serious illness that affects millions of patients. Current treatments are associated with a number of undesirable side effects. Neurokinin 1 receptor (NK1R) antagonists have recently been shown to potentiate the antidepressant e
Autotaxin inhibitors
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Page/Page column, (2014/06/25)
The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES
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Page/Page column 60, (2012/04/04)
The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
AMINO-PIPERIDINE DERIVATIVES AS CETP INHIBITORS
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Page/Page column 162, (2008/06/13)
The present invention provides a compound of formula (I), wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
NK-1 AND SEROTONIN TRANSPORTER INHIBITORS
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Page/Page column 62, (2010/11/28)
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
TRISUBSTITUTED AMINE COMPOUND
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Page/Page column 164-165, (2008/06/13)
The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES
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Page/Page column 54, (2008/06/13)
The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
Dibenzyl Amine Compounds and Derivatives
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Page/Page column 71, (2010/11/28)
Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.