- THERAPEUTIC COMPOUNDS
-
The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.
- -
-
Page/Page column 25; 26
(2013/03/28)
-
- Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR) selective agonists: Novel analogues of 4-[1-(3,5,5,8,8- Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and (E)-3-(3-(1,2,3,4-tetrahydro-1,1,
-
Three unreported analogues of 4-[1-(3,5,5,8,8-pentamethyl-5-6-7-8- tetrahydro-2-naphthyl)ethynyl]benzoic acid (1), otherwise known as bexarotene, as well as four novel analogues of (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6- pentamethylnaphthalen-7-yl)-4-hydr
- Jurutka, Peter W.,Kaneko, Ichiro,Yang, Joanna,Bhogal, Jaskaran S.,Swierski, Johnathon C.,Tabacaru, Christa R.,Montano, Luis A.,Huynh, Chanh C.,Jama, Rabia A.,Mahelona, Ryan D.,Sarnowski, Joseph T.,Marcus, Lisa M.,Quezada, Alexis,Lemming, Brittney,Tedesco, Maria A.,Fischer, Audra J.,Mohamed, Said A.,Ziller, Joseph W.,Ma, Ning,Gray, Geoffrey M.,Van Der Vaart, Arjan,Marshall, Pamela A.,Wagner, Carl E.
-
p. 8432 - 8454
(2013/12/04)
-
- Syntheses of isotopically labeled 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro- 2-naphthyl)ethenyl]benzoic acid (LGD1069), a potent retinoid X receptor-selective ligand
-
LGD1069, 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethenyl] benzoic acid, is the first retinoid X receptor (RXR) selective retinoid to enter clinical trials for treatment of dermatological diseases and cancer. In order to examine biological properties such as receptor binding, metabolism and bioavailability, [13C]-, [14C]-, and [3H]-labeled LGD1069 is required. Herein, we describe synthetic methods for preparing isotopically labeled homologs of LGD 1069 as well as comparative competition binding data for [6,7-3H]-LGD1069 and [3H]-9-cis retinoic acid with RXR active retinoids. The final radiolabeled products, [6,7-3H]-LGD1069 and 3-[14C]-LGD1069 have specific activities of 56 Ci/mmol and 49 mCi/mmol, respectively. Radiochemical purities are 99.5% for [6,7-3H]-LGD1069 and 99.0% for 3-[14C]-LGD1069. The chemical purity is 99.0% for 3-[13CD3]-LGD1069. Competition binding studies with known retinoids show similar K(d) values when either [6,7-3H]-LGD1069 or [3H]-9-cis retinoic acid is used as the radioligand.
- Zhang,Badea,Enyeart,Berger,Mais,Boehm
-
p. 701 - 712
(2007/10/02)
-