159184-14-2Relevant academic research and scientific papers
Discovery of TD-4306, a long-acting β2-agonist for the treatment of asthma and COPD
McKinnell, R. Murray,Klein, Uwe,Linsell, Martin S.,Moran, Edmund J.,Nodwell, Matthew B.,Pfeiffer, Juergen W.,Thomas, G. Roger,Yu, Cecile,Jacobsen, John R.
, p. 2871 - 2876 (2014/06/10)
A multivalent approach focused on amine-based secondary binding groups was applied to the discovery of long-acting inhaled β2-agonists. Addition of amine moieties to the neutral secondary binding group of an existing β2-agonist serie
CHITOSAN COVALENTLY LINKED WITH SMALL MOLECULE INTEGRIN ANTAGONIST FOR TARGETED DELIVERY
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Paragraph 0154; 0155; 0170; 0171, (2013/08/14)
The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X1, X4, R1, R2, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (α4β1) and alpha-V-beta-3 (αVβ3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins.
Synthesis and evaluation of novel phenylethanolamine derivatives containing acetanilides as potent and selective b 3-adrenergic receptor agonists
Maruyama, Tatsuya,Onda, Kenichi,Hayakawa, Masahiko,Suzuki, Takayuki,Kimizuka, Tetsuya,Matsui, Tetsuo,Takasu, Toshiyuki,Nagase, Itsuro,Hamada, Noritaka,Ohta, Mitsuaki
experimental part, p. 533 - 545 (2010/09/06)
In the search for potent and selective human β3-adrenergic receptor (AR) agonists as potential pharmacotherapies for the treatment of obesity and non-insulin dependent (type II) diabetes, we prepared a novel series of phenylethanolamine derivatives containing acetanilides and evaluated their biological activities at the human β3-, β2-, and β1-ARs. Among these compounds, the 6-amino-2-pyridylacetanilide (36b), 2-amino-5- methylthiazol- 4-ylacetanilide (36g), and 5-amino-1,2,4-thiadiazol-3- ylacetanilide (36h) derivatives showed potent agonistic activity at the β3-AR with functional selectivity over the β1- and β2-ARs. In addition, these compounds exhibited significant hypoglycemic activity in a rodent diabetic model.
Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-d-aspartate receptors
Mosley, Cara A.,Myers, Scott J.,Murray, Ernest E.,Santangelo, Rose,Tahirovic, Yesim A.,Kurtkaya, Natalie,Mullasseril, Praseeda,Yuan, Hongjie,Lyuboslavsky, Polina,Le, Phuong,Wilson, Lawrence J.,Yepes, Manuel,Dingledine, Ray,Traynelis, Stephen F.,Liotta, Dennis C.
experimental part, p. 6463 - 6480 (2011/03/17)
The synthesis and structure-activity relationship analysis of a novel class of amide-based biaryl NR2B-selective NMDA receptor antagonists are presented. Some of the studied compounds are potent, selective, non-competitive, and voltage-independent antagonists of NR2B-containing NMDA receptors. Like the founding member of this class of antagonists (ifenprodil), several interesting compounds of the series bind to the amino terminal domain of the NR2B subunit to inhibit function. Analogue potency is modulated by linker length, flexibility, and hydrogen bonding opportunities. However, unlike previously described classes of NR2B-selective NMDA antagonists that exhibit off-target activity at a variety of monoamine receptors, the compounds described herein show much diminished effects against the hERG channel and α1-adrenergic receptors. Selections of the compounds discussed have acceptable half-lives in vivo and are predicted to permeate the blood-brain barrier. These data together suggest that masking charged atoms on the linker region of NR2B-selective antagonists can decrease undesirable side effects while still maintaining on-target potency.
Trisubstituted pyrimidines
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, (2008/06/13)
The present invention relates to trisubstituted pyrimidines of formula wherein Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses in which β-amyloid modulators have a therapeutic benefit, the use th
Anilide derivatives and antiarrhythmic agents containing the same
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, (2008/06/13)
Preparation of antiarrhythmic agents containing novel anilide derivatives represented by the following formula as active ingredient provides a new type of antiarrhythmic agent of highly safe and effective, without effects on cardiac function.
Substituted phenyl sulfonamides as selective β 3 agonists for the treatment of diabetes and obesity
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, (2008/06/13)
Substituted phenylsulfonamides are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
