214601-54-4Relevant articles and documents
Ligand-Phospholipid Conjugation: A Versatile Strategy for Developing Long-Acting Ligands That Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand
Kawamura, Shuhei,Ito, Yoshihiko,Hirokawa, Takatsugu,Hikiyama, Eriko,Yamada, Shizuo,Shuto, Satoshi
, p. 4020 - 4029 (2018/05/07)
We hypothesized that if drug localization can be restricted to a particular subcellular domain where their target proteins reside, the drugs could bind to their target proteins without being metabolized and/or excreted, which would significantly extend the half-life of the corresponding drug-target complex. Thus, we designed ligand-phospholipid conjugates in which the ligand is conjugated with a phospholipid through a polyethylene glycol linker to restrict the subcellular localization of the ligand in the vicinity of the lipid bilayer. Here, we present the design, synthesis, pharmacological activity, and binding mode analysis of ligand-phospholipid conjugates with muscarinic acetylcholine receptors as the target proteins. These results demonstrate that ligand-phospholipid conjugation can be a versatile strategy for developing long-acting ligands that bind to membrane proteins in drug discovery.
PHOSPHOLIPID CONJUGATE
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, (2017/02/28)
PROBLEM TO BE SOLVED: To provide a compound that suitably interacts with a receptor existing on a cell surface to regulate its activity, to provide a pharmaceutical composition containing the compound, and to provide a method for treating a disease using the compound, and the like. SOLUTION: The above mentioned object is achieved by providing a compound represented by general formula: P-S-L (where, P is a phospholipid moiety; S is a spacer moiety which includes a structure represented by -(PEG)n- wherein n is an integer equal or greater than 5; L is a ligand moiety of a cytoplasmic membrane receptor). SELECTED DRAWING: Figure 3 COPYRIGHT: (C)2016,JPOandINPIT
DESFESOTERODINE SALTS
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, (2014/01/08)
The invention relates to substantially pure Desfesoterodine salts, Desfesoterodine salts, solid state forms thereof and pharmaceutical compositions comprising one or more of the Desfesoterodine salts and/or solid state forms thereof.
A PROCESS FOR PREPARING FESOTERODINE
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, (2012/10/18)
The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of fesoterodine and pharmaceutically acceptable salts thereof which involves use and preparation of R(+) benzyl tolterodine and fumarate salt of R(+)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol.
PROCESS FOR THE PREPARATION OF MUSCARINIC RECEPTOR ANTAGONIST
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, (2012/08/07)
The present invention relates to novel and improved processes for the preparation of (r)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenylisobutyrate represented by the following structural formula-1 and its pharmaceutically acceptable salts thereof.
Therapeutically active diarylpropylamines; their pharmaceutically acceptable salts; a method for their preparation and method for their use
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, (2008/06/13)
The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary tract incontinence, and methods for preparing the compounds of Formula (I).