21567-18-0Relevant articles and documents
PROCESS FOR PREPARING 4- { (S) -2- (4-(4-CHLOROPHENOXY) PHENOXYMETHYL) PYRROLIDIN-1-YL) } BUTYRIC ACID AND SALTS THEREOF
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Page/Page column 16, (2011/02/24)
The present invention relates to a process for preparing 4-{(S)-2-[4-(4-chlorophenoxy)phenoxymethyl]pyrrolidin-1-yl}butyric acid and its salts.
Development of a scalable synthetic process for DG-051B, a first-in-class inhibitior of LTA4H
Enache, Livia A.,Kennedy, Isaac,Sullins, David W.,Chen, Wei,Ristic, Dragan,Stahl, Glenn L.,Dzekhtser, Sergey,Erickson, Robert A.,Yan, Changren,Muellner, Frank W.,Krohn, Michael D.,Winger, Jennifer,Sandanayaka, Vincent,Singh, Jasbir,Zembower, David E.,Kiselyov, Alex S.
experimental part, p. 1177 - 1184 (2010/04/22)
DG-051B is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention of heart attack. Process optimization led from a linear seven-step synthetic procedure to a convergent
BIARYL SUBSTITUTED HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION
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Page/Page column 25; 27; 29, (2008/06/13)
The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is
ANTIDIABETIC OXAZOLIDINEDIONES AND THIAZOLIDINEDIONES
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Page/Page column 33; 34, (2010/11/25)
Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia
PROCESS FOR THE PRODUCTION OF ANTIDIABETIC OXAZOLIDINEDIONES
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Page/Page column 8-10, (2008/06/13)
The present invention provides a convergent process for the preparation of a family of antidiabetic phenoxy-substituted phenoxybenzyl oxazolidinediones shown as structure I. The compounds are selective PPAR gamma partial agonists (SPPARM's), which are use
FUSED AROMATIC COMPOUNDS HAVING ANTI-DIABETIC ACTIVITY
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Page/Page column 38-39, (2010/11/23)
Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obes
Selective displacement of aryl fluorides with hydroquinone: Synthesis of 4-phenoxyphenols
Marcune, Benjamin F.,Hillier, Michael C.,Marcoux, Jean-Fran?ois,Humphrey, Guy R.
, p. 7823 - 7826 (2007/10/03)
The selective displacement of a variety of aryl fluorides with hydroquinone has been achieved to give substituted 4-phenoxyphenols 3. In some cases the addition of 18-crown-6 resulted in a significant rate enhancement, and the reactions could be carried out at lower temperature. One of these derivatives, 3a (X = Cl) was converted to 2-propyl-4-(4-chlorophenoxy)phenol 2a, a precursor to the PPARγ receptor agonist 1.
ANTIDIABETIC OXAZOLIDINEDIONES AND THIAZOLIDINEDIONES
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Page/Page column 30, (2010/02/13)
Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones of formula (I) are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well
5-Aryl thiazolidine-2,4-diones as selective PPARγ agonists
Koyama, Hiroo,Boueres, Julia K.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,Miller, Daniel J.,Tolman, Richard L.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 1801 - 1804 (2007/10/03)
A series of 5-aryl thiazolidine-2,4-diones containing 4-phenoxyphenyl side chains was designed, synthesized, and evaluated for PPAR agonist activities. One such compound 28 exhibited comparable levels of glucose correction to rosiglitazone in the db/db mouse type 2 diabetes animal model.
5-Aryl thiazolidine-2,4-diones: Discovery of PPAR dual α/γ agonists as antidiabetic agents
Desai, Ranjit C.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 2795 - 2798 (2007/10/03)
A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARα/γ agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.