title: Rho kinase inhibitors: a patent review (2012 - 2013).
abstract: BACKGROUND
  The Rho kinase/ROCK is critical in vital signal transduction pathways central to many essential cellular activities. Since ROCK possess multiple substrates, modulation of ROCK activity is useful for treatment of many diseases.
  
  
  METHODS
  Significant progress has been made in the development of ROCK inhibitors over the past two years (Jan 2012 to Aug 2013). Patent search in this review was based on FPO IP Research and Communities and Espacenet Patent Search. In this review, patent applications will be classified into four groups for discussions. The grouping is mainly based on structures or scaffolds (groups 1 and 2) and biological functions of ROCK inhibitors (groups 3 and 4). These four groups are i) ROCK inhibitors based on classical structural elements for ROCK inhibition; ii) ROCK inhibitors based on new scaffolds; iii) bis-functional ROCK inhibitors; and iv) novel applications of ROCK inhibitors.
  
  
  CONCLUSIONS
  Although currently only one ROCK inhibitor (fasudil) is used as a drug, more drugs based on ROCK inhibition are expected to be advanced into market in the near future. Several directions should be considered for future development of ROCK inhibitors, such as soft ROCK inhibitors, bis-functional ROCK inhibitors, ROCK2 isoform-selective inhibitors, and ROCK inhibitors as antiproliferation agents.
authors.affiliation: Translational Research Institute, The Scripps Research Institute , Scripps Florida, #2A1, 130 Scripps Way, Jupiter, FL 33458 , USA +1 561 228 2201 ; yfeng@scripps.edu.
authors.forename: Yangbo
authors.initials: Y
authors.lastname: Feng
authors.forename: Philip V
authors.initials: PV
authors.lastname: LoGrasso
mesh_terms: D000818:Animals; D015195:Drug Design; D006801:Humans; D007880:Legislation, Drug; D015394:Molecular Structure; D058990:Molecular Targeted Therapy; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D047428:Protein Kinase Inhibitors; D054460:rho-Associated Kinases