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cu») United States US 20104 cz) Patent Application Publication — co) Pub. No.: US 2010/0173927 Al Le Bourdonnec et al. (54) BELOXEPIN AND ANALOGS FOR THE TREATMENT OF PAIN, Bertrand Le Bourdonnee, East Fallowfield, PA (US); Roland Dole, King of Prussia, PA (US} (75) Inventors Comespondence Address DECHERT LLP P.O, BOX 390460 MOUNTAIN VIEW, CA 94039-0460 (US) (73) Assignee: Adolor Corporation, Exton, PA wus) (21) Appl.No: — 127180,858 (22) Filed Mar. 30,2010, 3) (0) oy 6 on This (43) Pub, Date Jul. 8, 2010 Related Application Data Continuation of application No. 12/388,982, filed on Feb, 19, 2000, Provisional application No. 61/029,916, filed on Feb, 19, 2008, provisional application No. 61/0S0.921, filed on May 6, 2008. Publication Classification Int. cl. AGIK 314353 2006.01) A61P 25700 (2006.01), US. Cl stanss ABSTRACT present disclosure provides methods oft ‘with beloxepin and/or beloxepin analogs. US 2010/0173927 AI Jul. 8,2010 Sheet 1 of 16 Patent Application Publication swes6 9°} = ploysany ersi4en, dnoip jg =U ies pajeas-ajo14en 0} paredwioo go'0 > d= , ALNAWLVSYUL-LSOd NIN OF NIN OZ NIW 09 NIN Of o * oraiyen jose a ¥ eroquen jomsis 3 (SWVud NI) G@IOHS3YHL NVAW WOW 08 ‘S10IH3A moro reee AraBing og SAE FT SPY INS $1 UH (AI B4/Bw 0¢) udoxojag Jo raya o1UApo| b ‘Sls US 2010/0173927 AI Jul. 8, 2010 Sheet 2 of 16 Patent Application Publication Brup-jsod seynulw o¢ ye pese} e1em s|EWIUY swelB 2°} = afo1yap, sjewlue payesedo-weys y = u ‘(sdnoi9 NS) 2-7 =U S}e1 INS G7 payean-ajoiyan 0} paredwiod gQ‘0 > d , (dl S/W) urdexojeq o¢ OL e OIHSA = WHS. ee] ° ez a B 2 = Q 60 Zz Zh @ 2 g P1P1YSA 40 %ZSB- BL AsaBing so seq 91 SIA INS $7 U! (4 34/8u1 O¢ pur | ‘¢) udoxojag Jo iayq o1uAPOTenUY Zold