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(12) Patent Application Publication (10) Pub. No.: US 2009/0203722 A1 Sherman Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2009/0203722 A1 Sherman Et Al US 20090203722A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/0203722 A1 Sherman et al. (43) Pub. Date: Aug. 13, 2009 (54) NOVEL COMPOSITIONS AND METHODS tion of application No. 10/047.367, filed on Jan. 14, FOR ENHANCING POTENCY OR REDUCING 2002, now abandoned, which is a continuation of ADVERSE SIDE EFFECTS OF OPOLD application No. 09/849,721, filed on May 4, 2001, now AGONSTS abandoned, which is a continuation of application No. 09/756,331, filed on Jan. 8, 2001, now abandoned, (75) Inventors: Barry M. Sherman, Hillsborough, which is a continuation of application No. 09/566,071, CA (US); Mary M. Remien, San filed on May 5, 2000, now abandoned, Continuation of Francisco, CA (US); Remi Barbier, application No. PCT/US00/12493, filed on May 5, San Francisco, CA (US); Kathleen 2OOO. Dumas, Cupertino, CA (US); Grant L. Schoenhard, San Carlos, Publication Classification CA (US) (51) Int. Cl. Correspondence Address: A63L/485 (2006.01) BELL, BOYD & LLOYD, LLP A63L/35 (2006.01) P.O. Box 1135 A6IP 25/00 (2006.01) CHICAGO, IL 60690 (US) (52) U.S. Cl. ......................................... 514/282; 514/646 (73) Assignee: PAIN THERAPEUTICS, INC., (57) ABSTRACT South San Francisco, CA (US) The invention generally relates to novel compositions and methods with an opioid agonist and an opioid antagonist to (21) Appl. No.: 11/456,079 differentially dose a human Subject so as to either enhance analgesic potency without attenuating an adverse side effect (22) Filed: Jul. 6, 2006 of the agonist, or alternatively maintain the analgesic potency of the agonist while attenuating an adverse side effect of the Related U.S. Application Data agonist. The invention additionally relates to novel opioid (63) Continuation of application No. 10/228,835, filed on compositions and methods for the gender-based dosing of Aug. 26, 2002, now abandoned, which is a continua men and women. Patent Application Publication Aug. 13, 2009 Sheet 1 of 73 US 2009/0203722 A1 g se s | Patent Application Publication Aug. 13, 2009 Sheet 2 of 73 US 2009/0203722 A1 s aS Patent Application Publication Aug. 13, 2009 Sheet 3 of 73 US 2009/0203722 A1 Patent Application Publication Aug. 13, 2009 Sheet 4 of 73 US 2009/0203722 A1 60| 9,0- TWAIA?OS Patent Application Publication US 2009/0203722 A1 EWILHEAOSEHOOS(Hd)HEITENNIWA SINEIlydTiv'NOIVT^?OdIVER1-01-INHINI Patent Application Publication Aug. 13, 2009 Sheet 7 of 73 US 2009/0203722 A1 BW||H?AOSE800S(Qld)BONEHEHHIGÅLISNEININIWASINHLydTiv'NQIYmdod?aeiforniini (SH6OH)3WILINAWSSESSY 8!99Þ8.?|0 Patent Application Publication US 2009/0203722 A1 8ET??10IJ SLO?IJ?QIGIOTISQISNIGLACIV Patent Application Publication US 2009/0203722 A1 'yºOldS HEGN30CNYd?080INGWIYEHIAGV6'9|- Patent Application Publication US 2009/0203722 A1 Patent Application Publication Aug. 13, 2009 Sheet 11 of 73 US 2009/0203722 A1 SET\/WU 0"|XINIM-XIN/MÅ50W09SW:?M|0'0!'0XIN 'y-OldSH3CN?0QNWdnogÐINAWIWAHIAG 0 Patent Application Publication Aug. 13, 2009 Sheet 12 of 73 US 2009/0203722 A1 (SºnOH)BWIL 98100YIN/OW09S}-b,-o-p-||·BWl'OXINER03SW-v~~ ~ ||89 -6'0 -S’O Patent Application Publication US 2009/0203722 A1 d C Patent Application Publication Aug. 13, 2009 Sheet 14 of 73 US 2009/0203722 A1 Patent Application Publication Aug. 13, 2009 Sheet 15 of 73 US 2009/0203722 A1 Patent Application Publication Patent Application Publication Aug. 13, 2009 Sheet 18 of 73 US 2009/0203722 A1 98iXINER09SW-º-º-º- BW||HBAOSE800S(Hd)BEITENNIYA SINH|1\d|BTWW33}NOLIWTndOd1\381-04-1NJANI $#{? 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Patent Application Publication Aug. 13, 2009 Sheet 27 of 73 US 2009/0203722 A1 Patent Application Publication Aug. 13, 2009 Sheet 28 of 73 US 2009/0203722 A1 NIWEHEITE8(Nd)SB800S83A0BW|| ???Jrori?iniSINH|1\dTiv''NOLIV?ndod NWBWNI?d 3BITBA(dd) 3800S Patent Application Publication Aug. 13, 2009 Sheet 30 of 73 US 2009/0203722 A1 ZZSTRIQ9ISI SJLO?I,IJIQIQIQUISQISNIQ?AQTY posrtvAN 33ua?ouuos (uoffpa?) Patent Application Publication Aug. 13, 2009 Sheet 31 of 73 US 2009/0203722 A1 |- INEWIWB8||y,NYEWdn080 Patent Application Publication Aug. 13, 2009 Sheet 32 of 73 US 2009/0203722 A1 SEITWW3)DZI |al |0'0XIN 'y-OldS|-HaGNESGNVd?089INGWIYEHIAG82Z'9|+ Patent Application Publication US 2009/0203722 A1 Patent Application Publication Aug. 13, 2009 Sheet 34 of 73 US 2009/0203722 A1 BWII(SunOH. 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N 8SSESEEEEEESSR, edO is 2 C c waxis is a KXXXXX& issus SS E Oa - & S h- & 0- - e t O O g S3 N 2 r t S. 2.O N: upg S2cit a iscs N: s - - 8 S. Hi SS & is g CESX 2 O O-a XX8&888 a - Y - -- ce ERS on a O 2 st ch S&3SE CD KCKCXXCXSSSSSSS ESSESSEES3 5 2. V) SXSX2S&SRS& 8ESSEE - C2 2 - mm.1 g He g S O a - ce a do es e es as a Lust 2SE s 22 a , O -a O . a2 5 p. is a 2 to 9 l5u d Patent Application Publication Aug. 13, 2009 Sheet 69 of 73 US 2009/0203722 A1 o E. 2 a r 29 d l 2 g HeCo- un Se s S t C2 - : d 3 2 - c 25r s 3 2 -3 l e Patent Application Publication Aug. 13, 2009 Sheet 70 of 73 US 2009/0203722 A1 o s 5 Patent Application Publication Aug. 13, 2009 Sheet 71 of 73 US 2009/0203722 A1 ?9'9||-|| LNHWSSESSWTWROT9XT|WQNWEW US 2009/0203722 A1 Aug. 13, 2009 NOVELCOMPOSITIONS AND METHODS than its N-allyl cogener, naloxone, and is active when given FOR ENHANCING POTENCY OR REDUCING orally. For example, 50 mg dosage forms of naltrexone, are ADVERSE SIDE EFFECTS OF OPOLD marketed as ReVia(R) in the United States or Trexan in other AGONSTS countries. Nalmefene (6-methylene-6-desoxy-N-cyclopro pyl-methyl-14-hydroxydihydroxydihydronor-morphine) CROSS-REFERENCE TO RELATED was also developed as a long acting, orally available, potent APPLICATIONS opioid antagonist, and has also been characterized as a pure 0001.
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