389068-22-8Relevant 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.
A PROCESS FOR PREPARING FESOTERODINE
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Page/Page column 11, (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 N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenyl-propaneamine
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Page/Page column 7, (2008/06/13)
A process is described for the preparation of N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenyl-propaneamine comprising substitution of the sulfonyloxy group of the compound of the formula in which the substituents R and R″ have the meanings stated in the description, in a solvent comprising an ionic liquid, to yield the tertiary amine of the formula and the subsequent deprotection thereof.
Process for preparing tolterodine
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Page/Page column 6, (2010/11/08)
A process for preparing tolterodine with high purity.
An improved, scalable, and impurity-free process for tolterodine tartrate
Srinivas, Keesari,Srinivasan, Neti,Reddy, Kikkuru Srirami,Ramakrishna, Muddasani,Reddy, Chinta Raveendra,Arunagiri, Muthulingam,Kumari, Routhu Lalitha,Venkataraman, Sundaram,Mathad, Vijayavitthal T.
, p. 314 - 318 (2012/12/24)
Tolterodine tartrate is an anticholinergic muscle relaxant used to treat urinary frequency, urinary urgency, and incontinence in people with unstable bladders. An improved, cost-effective, and impurity-free process for tolterodine tartrate suitable for la
PROCESS FOR PREPARATION OF 2-(3-DIISOPROPYLAMINO-1-PHENYLPROPYL)-4-HYDROXYMETHYL-PHENOL, A METABOLITE OF TOLTERODINE
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Page/Page column 7, (2008/06/13)
The present invention relates to processes for preparation of 2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethyl-phenol of Formula I, which is a metabolite of tolterodine.
TOLTERODINE, COMPOSITIONS AND USES THEREOF, AND PREPARATION OF THE SAME
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Page/Page column 15, (2008/06/13)
Racemic tolterodine free base in crystalline form, tolterodine with improved purity, compositions and uses thereof, and processes of preparing the same.