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USOO9050343B2 (12) United States Patent (10) Patent No.: US 9,050,343 B2 Peters et al. (45) Date of Patent: Jun. 9, 2015 (54) COMBINATION OF PIMAVANSERIN AND 4,332,804 A 6, 1982 Clark RSPERIDONE FOR THE TREATMENT OF 13. A 9. at: al PSYCHOSIS 4,367,232 A 1/1983 Boix-Igleasias et al. (71) Applicants: Perry Peters, San Diego, CA (US); 3. A SME,R al David Furlano, San Diego, CA (US); 5,214,055 A 5/1993 Peglion et al. Daun Bahr, San Diego, CA (US); 5,216,165 A 6/1993 Mobilio et al. Daniel Van Kammen, San Diego, CA 5,461,066 A 10, 1995 Gericke et al. (US) 5,595,872 A 1/1997 Wetterau, II et al. 5,621,010 A 4/1997 Sueda et al. (72) Inventors: Perry Peters, San Diego, CA (US); 5,707,798 A 1/1998 Brann David Furlano, San Diego, CA (US); 3. A E. Shet al. Daun Bahr, San Diego, CA (US); 5,869,488 A 2, 1999 Shue et al. Daniel Van Kammen, San Diego, CA 5,877,173 A 3/1999 Olney et al. (US); Mark Brann, Rye, NH (US) 5,912,132 A 6/1999 Brann 5,955,281 A 9, 1999 Brann (73) Assignee: ACADIA Pharmaceuticals Inc., San 6,107,324 A 8, 2000 Behan et al. Diego, CA (US) 6,140,509 A 10/2000 Behan et al. 6,150,393 A 11/2000 Behan et al. (*) Notice: Subject to any disclaimer, the term of this E. R f29: y s al patent is extended or adjusted under 35 6,486,153- B1 1 1/2002 Castrooyes Pineiroet al. et al. U.S.C. 154(b) by 89 days. 6,670,137 B2 12/2003 VanMechelen et al. 6,756,393 B2 6/2004 Andersson et al. (21) Appl. No.: 13/754,769 6,815,458 B2 11/2004 Andersson et al. 6,911,452 B2 6/2005 Schlienger (22) Filed: Jan. 30, 2013 7,022,698 B2 4/2006 Hamied et al. 7,041,667 B1 5/2006 Armour et al. (65) Prior Publication Data 7,115,634 B2 10/2006 Thurieau et al. 7,253,186 B2 8/2007 Andersson et al. US 2013/0143901 A1 Jun. 6, 2013 7,601,740 B2 10/2009 Weiner et al. (Continued) Related U.S. Application Data (62) Division of application No. 12/051,807, filed on Mar. FOREIGN PATENT DOCUMENTS 19, 2008, now abandoned. CA 984843 3, 1976 (60) Provisional application No. 60/895,735, filed on Mar. EP 0 005 3.18 11, 1979 19, 2007, provisional application No. 60/908,921, (Continued) filed on Mar. 29, 2007, provisional application No. 61/012,771, filed on Dec. 10, 2007, provisional OTHER PUBLICATIONS application No. 61/026,092, filed on Feb. 4, 2008. Poewe (Movement Disorders vol. 18, Suppl. 6, 2003, pp.S80-S87).* (51) Int. Cl. (Continued) A 6LX3/59 (2006.01) A6 IK3I/4468 (2006.01) 3. f 3:08: Primary Examiner — David J Blanchard A6 IK3 L/455 (2006.01) Assistant Examiner — Garen Gotfredson A 6LX3/553 (2006.01) (74) Attorney, Agent, or Firm — Jones Day A6 IK3I/554 (2006.01) (52) U.S. Cl. CPC ............... A6 IK3I/519 (2013.01); A61 K3I/00 (57) ABSTRACT (2013.01); A61K3I/4468 (2013.01); A61 K 3 1/4515 (2013.01); A61 K3I/5513 (2013.01); Combinations of 5-HT2A inverse agonists or antagonists A61 K3I/554 (2013.01) Such as pimavanserin with antipsychotics Such as risperidone (58) Field of Classification Search are shown to induce a rapid onset of antipsychotic action and None increase the number of responders when compared to therapy See application file for complete search history. with the antipsychotic alone. These effects can be achieved at a low dose of the antipsychotic, thereby reducing the inci (56) References Cited dence of side effects. The combinations are also effective at decreases the incidence of weight gain and increased glucose U.S. PATENT DOCUMENTS or prolactin levels caused by the antipsychotic. 3,983,234 A 9/1976 Sayers 4,138.492. 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