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(12) Patent Application Publication (10) Pub. No.: US 2009/0053329 A1 Peters Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2009/0053329 A1 Peters Et Al US 2009.0053329A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/0053329 A1 Peters et al. (43) Pub. Date: Feb. 26, 2009 (54) COMBINATIONS OF 5-HT2A INVERSE 61/012,771, filed on Dec. 10, 2007, provisional appli AGONSTS AND ANTAGONSTS WITH cation No. 61/026,092, filed on Feb. 4, 2008. ANTIPSYCHOTICS Publication Classification (75) Inventors: Perry Peters, San Diego, CA (US); (51) Int. Cl. David Furlano, San Diego, CA A633/00 (2006.01) (US); Daun Bahr, San Diego, CA A6II 3/445 (2006.01) (US); Daniel Van Kammen, San A 6LX 3/59 (2006.01) Diego, CA (US); Mark Brann, A6II 3/438 (2006.01) Rye, NH (US) A6IP 25/18 (2006.01) Correspondence Address: A 6LX 3L/2197 (2006.01) KNOBBE MARTENS OLSON & BEAR LLP A6II 3/54 (2006.01) 2040 MAINSTREET, FOURTEENTH FLOOR A6II 3/55 (2006.01) IRVINE, CA 92.614 (US) (52) U.S. Cl. .................... 424/722:514/329; 514/259.41: 514/278; 514/254.06; 514/222.2: 514/212.01 (73) Assignee: Acadia Pharmaceuticals, Inc., San Diego, CA (US) (57) ABSTRACT Combinations of 5-HT2A inverse agonists or antagonists (21) Appl. No.: 12/051,807 Such as pimavanserin with antipsychotics Such as risperidone are shown to induce a rapid onset of antipsychotic action and (22) Filed: Mar. 19, 2008 increase the number of responders when compared to therapy with the antipsychotic alone. These effects can be achieved at Related U.S. Application Data a low dose of the antipsychotic, thereby reducing the inci (60) Provisional application No. 60/895,735, filed on Mar. dence of side effects. The combinations are also effective at 19, 2007, provisional application No. 60/908,921, decreases the incidence of weight gain and increased glucose filed on Mar. 29, 2007, provisional application No. or prolactin levels caused by the antipsychotic. Patent Application Publication Feb. 26, 2009 Sheet 1 of 42 US 2009/0053329 A1 ??OOOT|OI!OD|_| || spusogWWWW N_^N_/N_/N_/ ;---;:N Patent Application Publication Feb. 26, 2009 Sheet 2 of 42 US 2009/0053329 A1 Patent Application Publication Feb. 26, 2009 Sheet 3 of 42 US 2009/0053329 A1 Z sºusogW\\W No.Ø \;~~)N Patent Application Publication Feb. 26, 2009 Sheet 5 of 42 US 2009/0053329 A1 FIG. 3A p=0.001 ÇO O ×××××××××××××××ae ?aw asXXXXXXXXXXXXXXX] No. ZOZOXXXXXXXXXXX FIG. 3B Patent Application Publication Feb. 26, 2009 Sheet 6 of 42 US 2009/0053329 A1 . i s eleoS 8AISO SSNW eueSeguOly e5ueUO Patent Application Publication Feb. 26, 2009 Sheet 7 of 42 US 2009/0053329 A1 99ÁÐG SIH/NId 9ÁBO CITSIH– CIHSIH— eleoS eNe5eNSSNW euleSeguOly effueUO Patent Application Publication Feb. 26, 2009 Sheet 8 of 42 US 2009/0053329 A1 i s s g : s CN s CO CO CO CN t y S. eleOS A6OOuledoUOKSeleue) SSNW euleSe UO) effueuC) Patent Application Publication Feb. 26, 2009 Sheet 9 of 42 US 2009/0053329 A1 s GT CO CO O LO O LO O LO O LO d O CP t t CN CN c? c? s eleOSQnSUOIUSOO SSNV eueSeguOlgefueuo Patent Application Publication Feb. 26, 2009 Sheet 10 of 42 US 2009/0053329 A1 9;ÁBO 99ÁBO 9°{DIH 9ÁBO S90 euleSeguOly, ebueuo Patent Application Publication Feb. 26, 2009 Sheet 11 of 42 US 2009/0053329 A1 FIG. 7A p=0.05 FIG. 7B Patent Application Publication Feb. 26, 2009 Sheet 12 of 42 US 2009/0053329 A1 99Áed V8ºOIH 9ÁBO OJHSIH– 09 G| 0|- SeeWuoe|Old eueSeguO effueu) Patent Application Publication Feb. 26, 2009 Sheet 13 of 42 US 2009/0053329 A1 {{8"OIH 06 08 09 09 07 09 02 Seeue-juoe|Old eUIeSe uOuefueuo Patent Application Publication Feb. 26, 2009 Sheet 14 of 42 US 2009/0053329 A1 N 2 Lo N Co c\, y c. CO C C O (?e|Oulu) eSOOn) Patent Application Publication Feb. 26, 2009 Sheet 15 of 42 US 2009/0053329 A1 CO O) 8. CO - C -- Ch O C & s : 3. & & & SJepuOdSe % Patent Application Publication Feb. 26, 2009 Sheet 16 of 42 US 2009/0053329 A1 SIH6uu9—w—S?H+CHOV–––6uZ—?— ["OIH SQ O r SiepuOGSe% Patent Application Publication Feb. 26, 2009 Sheet 17 of 42 US 2009/0053329 A1 3OOO 2500 S 2000 O Veh--Weh--Weh &d 1500 A Veh-HVeh-i-Amp 3 O ACP-103+Veh-i-Amp it 1000 2 O -- Veh-i-haloperidol-HAmp 500 -- ACP-103+haloperidol-i-Amp O Veh O.OOO3 O.OO1 O.OO3 OO1 O.O3 DOSe of haloperidol (mg/kg) 1OO 80 60 ?h s SQ 40 2O -O- Veh--haloperidol--Amp -- ACP-103+haloperidol--Amp O O.OOO3 OOO, O.OO3 O.O. O.O3 DOse of haloperidol (mg/kg) FIG. 12B Patent Application Publication Feb. 26, 2009 Sheet 18 of 42 US 2009/0053329 A1 125 100 75 - H haloperidol 50 - - ACP-103 -O- ACP-103+haloperidol 25 O. O15 0.3 DOSe of Compound (mg/kg) FIG. 13A O.08 O.04 -- haloperidol - H ACP-103 -O- ACP-103+haloperidol O.O2 O.O4. O.O6 0.08 O. ACP-103 IDs (mg/kg) FIG. 13B Patent Application Publication Feb. 26, 2009 Sheet 19 of 42 US 2009/0053329 A1 125 100 S 75 -- risperidone 50 - ACP-103 -O- ACP-103+risperidone 25 O O.OO1 O.003 0.01 003 0.1 O.3 DOSe of Compound (mg/kg) OOO4 9. 2 OOO3 -- risperidone - - ACP-103 8 0.002 -O- ACP-103+risperidone ad O 0.001 O O.O2 O.O4 OO6 O.O8 O.1 ACP-103 ID (mg/kg) FIG. 14B Patent Application Publication Feb. 26, 2009 Sheet 20 of 42 US 2009/0053329 A1 5000 4000 O Veh--Weh-|-Veh 3: 3000 A Veh--Weh+Amp C s O ACP103 (0.03)+Veh-i-Amp 2000 --Weh-Haripiprazole+Amp 2 -- ACP103 (0.03)+aripiprazole--Amp 1000 O O Veh O.O. O.O3 O. 0.3 1 DOSe Ofaripiprazole (mg/kg, SC) FIG. 15A 120 - 100 S. o E 80 CD S2 g 8 60 -H Veh-Haripiprazole+Amp s8. 40 -- ACP103 (0.03)+aripiprazole+Amp SS 20 O O.O1 O.O3 O. 0.3 1 DOSe Ofaripiprazole (mg/kg, SC) FIG. 15B Patent Application Publication Feb. 26, 2009 Sheet 21 of 42 US 2009/0053329 A1 5OOO 4000 5. O Veh--Weh--Weh ; 3000 A Veh+Veh--Amp > O ACP103 (0.03)+Veh-i-Amp 2OOO --Weh-quetiapine-HAmp 3. -- ACP103 (0.03)+quetiapine--Amp 1000 o O Veh O. 1 O.3 1 3 10 DOSe Of Guetiapine (mg/kg, SC) O 120 S 100 C CD 8O C2 2 f 60 - HVeh-quetiapine +Amp 40 in -- ACP103 (0.03)+quetiapine + Amp s SQ O. O3 1 3 O DOSe Ofaripiprazole (mg/kg, SC) FIG. 16B Patent Application Publication Feb. 26, 2009 Sheet 22 of 42 US 2009/0053329 A1 CD y O CO O O g 9.is, N cs S v - ? S - os O CD T CN, < C C CD O O CO CO s CN O O O O (6)/6u)0'Oeudepenb Patent Application Publication Feb. 26, 2009 Sheet 23 of 42 US 2009/0053329 A1 is Patent Application Publication Feb. 26, 2009 Sheet 24 of 42 US 2009/0053329 A1 S ON wn F (t cro it 2 -Lg 22 is is f ?h LL LI O O D > < CC - LO C. Lo O LO C. Lo C CO CO CN CN Y - O O. SJOJ AJOUJeW 6u!)IONN Patent Application Publication Feb. 26, 2009 Sheet 25 of 42 US 2009/0053329 A1 "... FIG. 20A 120 - H ACP-103 + ?pean (0.01) g 100 : 60 7 PMT. W. DOse of ACP-103 (mg/kg FIG. 20B Patent Application Publication Feb. 26, 2009 Sheet 26 of 42 US 2009/0053329 A1 OO 80 60 -O- Vehicle + 40 -O- ACP-103 (1) + - ACP-103 (3) + 20 -H ACP-103 (10) + 0.03 O. O3 1 DOSe of haloperidol (mg/kg) FIG 21 A 100 80 60 -O- Vehicle + -O- ACP-103 (1) + 40 -- ACP-103 (3) + -H ACP-103 (10) + DOSe of risperidone (mg/kg) FIG 21B Patent Application Publication Feb. 26, 2009 Sheet 27 of 42 US 2009/0053329 A1 s s ss s (/n|Uu) SeNeuhoe Old Patent Application Publication Feb. 26, 2009 Sheet 28 of 42 US 2009/0053329 A1 O) E C) O O S CD Ol C/2 --1 -1 -F1 : l2 I-PF1 2 I-P1 21 OF1 Il-2 LH1 3.333 21-H1 3 4-H1 -P-P4. CD O O O D O O Crd CY) CN CN -- - (u/6u) uOpenueouOO euSe|d peoped Patent Application Publication Feb. 26, 2009 Sheet 29 of 42 US 2009/0053329 A1 0'06 0'08 0'09 0'09 KOuednooOJOCeOe 94. Patent Application Publication Feb. 26, 2009 Sheet 30 of 42 US 2009/0053329 A1 SZ"OIH )NN\ 00|| 06 08 0/ 09 09 07 09 0Z 0|| (%) AOuednooOJOOleOe Patent Application Publication Feb. 26, 2009 Sheet 31 of 42 US 2009/0053329 A1 Co LO co s O) O CO CO N CO CO (%) AOuednooOJOCeO9 Patent Application Publication Feb. 26, 2009 Sheet 32 of 42 US 2009/0053329 A1 (NNNNNJNI (%) KOuednooOJOdeOe Patent Application Publication Feb. 26, 2009 Sheet 33 of 42 US 2009/0053329 A1 JO?d009)ZO— JO|d800)VÕIH9- VLZ'OIH (%) NOuednooOJOdeOe Patent Application Publication Feb. 26, 2009 Sheet 34 of 42 US 2009/0053329 A1 {{LZ'OIH (%) WOuednooOJOldeOe Patent Application Publication Feb. 26, 2009 Sheet 35 of 42 US 2009/0053329 A1 JO?d?00.ZG— 101d300)VZLHG- V87'OIH 06 G8 09 9/ 99 09 99 09 (%) KOuednooOJOICe09 Patent Application Publication Feb.
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