69232-47-9Relevant articles and documents
SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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Page/Page column 71, (2013/10/22)
The present invention belongs to the field of EPl receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EPl receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EPl receptor as well as to pharmaceutical compositions comprising them.
INDOLIZINE ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS
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Page/Page column 11, (2008/12/07)
The specific compounds of this list : {7-cyano-2-methyl-1-[4-(morpholine-4-sutfonyl)benzyl]indolizin-3-yl}acetic acid, {1 -(3-chloro-4-ethanesulfonylbenzyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro4-(morpholine-4-sulfonyl)benzyl]-7-cyano-2
Synthesis, antiviral activity, and pharmacokinetic evaluation of P3 pyridylmethyl analogs of oximinoarylsulfonyl HIV-1 protease inhibitors
Randolph, John T.,Huang, Peggy P.,Flosi, William J.,DeGoey, David,Klein, Larry L.,Yeung, Clinton M.,Flentge, Charles,Sun, Mingua,Zhao, Chen,Dekhtyar, Tatyana,Mo, Hongmei,Colletti, Lynn,Kati, Warren,Marsh, Kennan C.,Molla, Akhteruzzaman,Kempf, Dale J.
, p. 4035 - 4046 (2007/10/03)
As a continuation of the recently communicated discovery of oximinoarylsulfonamides as potent inhibitors of HIV-1 aspartyl protease, compounds bearing pyridylmethyl substituents at P3 were designed and synthesized. Potent analogs in this series provided low single-digit nanomolar EC50 values against both wild-type HIV and resistant mutant virus (A17), attenuated some 3- to 12-fold in the presence of 50% human serum. Pharmacokinetic results for compounds in this series showed good to excellent exposure when co-administered orally with an equal amount of ritonavir (5 mg/kg each) in the rat, with average AUC >8 μg h/mL. Similar dosing in dog resulted in significantly lower plasma levels (average AUC i = 2.4 nM).