- Insight into the complete substrate-binding pocket of ThiT by chemical and genetic mutations
-
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
- Swier,Monjas,Ree?ing,Oudshoorn,Aisyah,Primke,Bakker,Van Olst,Ritschel,Faustino,Marrink,Hirsch,Slotboom
-
-
Read Online
- FUSED BICYCLIC RAF INHIBITORS AND METHODS FOR USE THEREOF
-
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
- -
-
Paragraph 0345-0347
(2022/02/09)
-
- Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors
-
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
- 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)
-
- Autotaxin inhibitors
-
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.
- -
-
Page/Page column
(2014/06/25)
-
- DERIVATIVES OF N-ACYL-N'-PHENYLPIPERAZINE USEFUL (INTER ALIA) FOR THE PROPHYLAXIS OR TREATMENT OF DIABETES
-
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.
- -
-
Page/Page column 60
(2012/04/04)
-
- AMINO-PIPERIDINE DERIVATIVES AS CETP INHIBITORS
-
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.
- -
-
Page/Page column 162
(2008/06/13)
-
- Dibenzyl Amine Compounds and Derivatives
-
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.
- -
-
Page/Page column 71
(2010/11/28)
-
- NK-1 AND SEROTONIN TRANSPORTER INHIBITORS
-
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.
- -
-
Page/Page column 62
(2010/11/28)
-
- TRISUBSTITUTED AMINE COMPOUND
-
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.
- -
-
Page/Page column 164-165
(2008/06/13)
-
- A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES
-
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.
- -
-
Page/Page column 54
(2008/06/13)
-
- CETP INHIBITORS
-
Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formu
- -
-
Page/Page column 65
(2010/02/14)
-