156755-37-2Relevant 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
PROCESS FOR THE PREPARATION OF FESOTERODINE
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Paragraph 0032; 0048, (2015/01/07)
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 from O-benzyl tolterodine.
PROCESS FOR THE PREPARATION OF FESOTERODINE OR ITS SALTS
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, (2013/04/13)
The present invention relates to a process for the preparation of fesoterodine or its salts.
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.
PROCESSES FOR THE PREPARATION OF FESOTERODINE
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, (2012/03/26)
The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.
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.
IMPROVED PROCESS FOR DIPHENYLPROPYLAMINE DERIVATIVES
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, (2011/12/04)
The present invention relates to an improved process for the preparation of biologically active diphenylpropylamine derivatives. The present invention specifically relates to an improved fesoterodine of formula (I) and its pharmaceutically acceptable salts.
SOLID STATE FORMS OF FESOTERODINE INTERMEDIATES
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Page/Page column 8, (2011/06/19)
Provided herein are novel solid state forms of fesoterodine intermediates, (R)-4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-benzoic acid and (R)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol, and processes for their preparation thereof. The solid state intermediates are useful for preparing fesoterodine or a pharmaceutically acceptable salt thereof in high purity.
FESOTERODINE SUBSTANTIALLY FREE OF DEHYDROXY IMPURITY
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Page/Page column 8; 24, (2010/04/03)
Provided herein is an impurity of fesoterodine, fesoterodine dehydroxy impurity, 2-[(lR)-3- [bis(l-methylethyl)amino]-l-phenylpropyl]-4-methylphenyl isobutyrate, and a process for preparing and isolating thereof. Provided further herein is a highly pure fesoterodine or a pharmaceutically acceptable salt thereof substantially free of fesoterodine dehydroxy impurity, process for the preparation thereof, and pharmaceutical compositions comprising highly pure fesoterodine or a pharmaceutically acceptable salt thereof substantially free of dehydroxy impurity. Provided also herein is a pharmaceutical composition comprising solid particles of pure fesoterodine fumarate substantially free of dehydroxy impurity, wherein 90 volume-percent of the particles (D90) have a size of less than about 200 microns.