Sch-351125 and Sch-350634. Schering-Plough.
Schering-Plough is developing Sch-351125 (Sch-C), the lead in a series of CCR5 inhibitors, for the potential treatment of HIV infection. By March 2001, it had entered phase I studies in the US, however, by April 2001, these had been suspended based in part on observed QTc prolongation at the highest dose. By December 2001, a new phase I trial had been initiated in France. The company has continued to investigate a number of second-generation CCR5 receptor antagonists, including Sch-350634, for the potential treatment of HIV infection. Although it was reported at two separate meetings in early 2001 that Sch-350634 was in phase I/II trials, in April 2001, Schering-Plough confirmed that the compound was not in clinical development at that time and that a preclinical toxicology program was scheduled for late 2001. In December 2001, Morgan Stanley predicted a 2004 launch for a compound arising from the CCR5 inhibitor program, with sales of US$100 million in 2004, US$200 million in 2005, rising to US$300 million in 2006.
Esté
José A
JA
Retrovirology Laboratory IrsiCaixa, Hospital Universitari Germans Trias i Pujol, Universitat Autónoma de Barcelona, Badalona, Spain. jaeste@ns.hugtip.scs.es
D019380:Anti-HIV Agents / Q000009:adverse effects / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D065100:CCR5 Receptor Antagonists; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D003497:Cyclic N-Oxides / Q000009:adverse effects / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D010091:Oximes; D010879:Piperazines / Q000009:adverse effects / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D010880:Piperidines; D011725:Pyridines / Q000009:adverse effects / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship
C438584:1-((2,4-dimethyl-3-pyridinyl)carbonyl)-4-methyl-4-(3-methyl-4-(1-(4-(trifluoromethyl)phenyl)ethyl)-1-piperazinyl)piperidine N1-oxide; D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D003497:Cyclic N-Oxides; D010091:Oximes; D010879:Piperazines; D010880:Piperidines; D011725:Pyridines; C438583:Ancriviroc