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Rilpivirine

  • Synonyms: TMC 278; R278474
  • ATC: J05AG05
  • Use: Lorem 
  • Chemical name: Lorem ipsum dolor sit amet, consetetur sadipscing elitr, sed diam
  • Formula: Lorem ipsum dolor sit amet,
  • MW:366.42 g/mol
  • CAS-RN:500287-72-9
  • InChI Key:YIBOMRUWOWDFLG-ONEGZZNKSA-N
  • InChI:InChI=1S/C22H18N6/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19/h3-9,11-13H,1-2H3,(H2,25,26,27,28)/b4-3+

Derivatives

    hydrochloride

  • Formula: C22H19ClN6
  • MW:402.88 g/mol
  • CAS-RN:700361-47-3

    fumarate

  • Formula: C26H22N6O4
  • MW:482.5 g/mol
  • CAS-RN:877817-88-4

Synthesis Path



















Substances Referenced in Synthesis Path

CAS-RN Formula Chemical Name CAS Index Name
141-90-2 C4H4N2OS 2-thiouracil
873-74-5 C7H6N2 4-aminobenzonitrile
244768-32-9 C11H11ClN4 4-[(4-chloro-pyrimidin-2-yl)amino]benzonitrile
500292-94-4 C11H12N2 (E)-3-(4-amino-3,5-dimethylphenyl)acrylonitrile
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem
Lorem Lorem Lorem Lorem

Trade Names

Country Trade Name Vendor Annotation
USA Lorem Lorem
Lorem Lorem
EU Lorem Lorem
Lorem Lorem
(wfm = withdrawn from market)

Formulations

  • Loremipsumdolorsitamet,consetetursadipscingelitr,seddiamnonumyeirmodtemporinviduntutlaboreetdoloremagnaaliquyam

References

    • Janssen, P. A. J. et al., J. Med. Chem., (2005) 48, 1901.
    • a-d Guillemont, J. et al., J. Med. Chem., (2005) 48, 2072.
    • Schils, D. et al., Org. Process. Res. Dev., (2008) 12(3), 530.
    • US 9999 9999999 (Janssen Pharms.; 7.10.2004; appl. 3.2.2004; EP-prior. 13.8.2001).
    • ea US 9999 9999999 (Johnson+Johnson; 27.7.2006; appl. 7.8.2003; EP-prior. 9.8.2002).
    • eb US 9999 9999999 (Johnson+Johnson; 9.11.2006; appl. 26.6.2006; EP-prior. 13.8.2001).
    • US 9999 9999999 (Johnson+Johnson; 10.7.2008; appl. 14.2.2008; EP-prior. 9.8.2002).
    • f WO 9999 999999 (Hetero Res. Foundation; 1.11.2012; appl. 16.2.2012; IN-prior. 25.4.2011).
  • hydrochloride salt:

    • US 9999 999999 (Janssen Pharms.; 25.5.2006; appl. 2.9.2005; EP-prior. 13.8.2001).
    • US 9999 999999 (Johnson+Johnson; 27.8.2009; appl. 28.7.2010; EP-prior. 13.8.2001).
  • fumarate salt:

    • US 9999 9999999 (Johnson+Johnson; 27.8.2009; appl. 2.7.2005; EP-prior. 3.9.2004).
  • use as antineoplastic agents:

    • US 9999 999999 (AstraZeneca; 25.9.2003; appl. 5.8.2002; GB-prior. 1.3.2000).
    • US 9999 999999 (AstraZeneca; 28.4.2005; appl. 24.11.2004; GB-prior. 1.3.2000).
  • solid state forms of Rilpivirine and salts:

    • WO 9999 999999 (Teva; 20.9.2012; appl. 19.3.2012; USA-prior. 12.5.2011).
  • aqueous suspensions of TMC278:

    • US 9999 9999999 (Tibotec Pharm.; 9.7.2009; appl. 22.6.2007; EP-prior. 23.6.2006).
  • combinations:

    • US 9999 999999 (Tibotec Pharm.; 21.8.2008; appl. 3.9.2004; EP-prior. 3.9.2003).