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Ubocom I' Iiiiiiiiiiiiiiiiiiiiiiii I'iii THETWO TORTOITUUS MALLITUANT20180243250A1 ANTONI MARINE ( 19) United States (12 ) Patent Application Publication (10 ) Pub. No. : US 2018/ 0243250 A1 Bolsöy (43 ) Pub . Date : Aug. 30 , 2018 (54 ) METHOD OF TREATING A DOPAMINE ( 30 ) Foreign Application Priority Data RELATED DISORDER IN A SUBJECT BY ADMINISTERING LEVODOPA , IN Sep . 4 , 2015 (SE ) .. .. .. PCT/ SE2015 / 050939 COMBINATION WITH A DOPAMINE DECARBOXYLASE INHIBITOR AND A CATECHOL - O -METHYLTRANSFERASE Publication Classification INHIBITOR (51 ) Int. Cl. A61K 31/ 198 (2006 .01 ) (71 ) Applicant : LobSor Pharmaceuticals Aktiebolag, A61P 25 / 16 ( 2006 .01 ) Knivsta (SE ) A61P 25 / 28 ( 2006 .01 ) U . S . CI. ( 72 ) Inventor : Roger Bolsöy, Knivsta (SE ) CPC . .. .. A61K 31 / 198 ( 2013 .01 ) ; A61P 25 / 16 ( 2018 .01 ) ; A61K 31/ 277 ( 2013 . 01 ) ; A61K (73 ) Assignees : LobSor Pharmaceuticals Aktiebolag , 2121/ 00 (2013 .01 ) ; AVIK 2300 /00 ( 2013 .01 ) ; Knivsta ( SE ) ; LobSor Pharmaceuticals Aktiebolag , Knivsta (SE ) A61P 25 / 28 ( 2018 .01 ) (21 ) Appl. No .: 15 /757 , 217 (57 ) ABSTRACT The invention relates to a method of treating a dopamine (22 ) PCT Filed : Sep . 5 , 2016 related disorder in a subject , the method comprises the steps of administering therapy to a subject, the therapy comprising ( 86 ) PCT No. : PCT/ SE16 / 50828 a plurality of doses of levodopa over a selected time period , $ 371 (c ) ( 1 ) , in combination with a dopamine decarboxylase inhibitor ( 2 ) Date : Mar. 2 , 2018 (DDI ) and a catechol- O -methyltransferase ( COMT) inhibi tor, wherein : ( i ) the dose of levodopa is lower; ( ii ) the dose Related U . S . Application Data of DDI is lower ; ( iii ) the dosing of levodopa is less frequent ; (60 ) Provisional application No . 62 /214 ,742 , filed on Sep . and /or (iv ) the dosing of DDI is less frequent As compared 4 , 2015 . with a reference regimen over the selected time period . Increased AUC09.ti - 24hwww. / dos .- . .- .- . *. * . .* .* . *. * . *. *. i' ubocom i' iiiiiiiiiiiiiiiiiiiiiiii i'iii .. LO *: rii'i Changeinscadesw mimit ', . ' ' '. '* ' * ' ' ' '* ', ', JU', ', ', 'i 20 * 60 100 1200 1. egida levando os was initiiniinisisisihin siswissenswisswinishiniwawa wasiwasi wisatawansininenh irsisinin sahibinin wwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwwww Patent Application Publication Aug . 30 , 2018 Sheet 1 of 4 US 2018 /0243250 A1 DHPA 120 , 00 { ??, ? 80, 00 60 ,00 %ofCarbidopa 40 ,00 20 ,00 . 0 ,00 4 , 5 5 5, 5 ply6 6 , 5 7 7, 5 FIG . 1 Degradation product from carbidopa ( % RRT Area 1 . 1 . 1 . 1 . 1 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 11 . 9 * . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . , 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . * ** UUUUUUU. .. » » » » » . .. .. .. FIG . 2 Patent Application Publication _ Aug . 30, 2018 Sheet 2 of 4 US 2018 / 0243250 A1 Degradation product from entacapone (AAT * ?????? *= ?????????????? ??????f ", "*- .9 K.?? A ' ' ' ' ' ' ?? ' ' ' ' ' ' . .. .. .. .. .. .. .. .? ' 212 . ?? . ? . ? . ? . .. .. .. .. .. 4 . .. .. -* 5 . .. .. ?? ?65 2 ]F ?? Fic , 3 fiam ir : yiSCSity ,init ; &b 2 clea y5 at 2 :3°C .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. .. : ); S& ? ???????? ".????;22????????':/( - : : -: : : .. ?* : : . *" ' * * ; F "; s • : :?? " .; : . .. : : : , ,'- * * * * , -: : : : .. Fic, 4 Patent Application Publication Aug . 30 , 2018 Sheet 3 of 4 US 2018 / 0243250 A1 ASSESS ? SSSSS ?????S ENSESS KSSR " . ." . " ." ." . " ." ." . " ." ." . " ." ." . " . " . " . " . " . " . " . " . " . " . " . " . " . " . " . " . " . " ?????? . - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. - .- . -. Airitiety ?????????????????????????? ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' . ' . ' , ' ' . ' . ' . ' . ' . ' . ' . ' . ' . ' . ' . ' ' ' ' . '. ' . rrrrrrrrrrrrrrrrrrrrrrrrrrrrrrrrrr. FE , SSRSS SSSSSSS SSSSSSSSSSSSSSSS " . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." , " . " ." . " . " " . " . " . " ." ." . " . " . " . " . " . " . ." , " , , , " ," . ". " ." . ", " , , ", " , *. * .* . *. *, . , Arti . " . " . " . " . " ." ." . " . " . " ." ." . " . " . " . " . " . " ." ." . " . " . " . " . " . " ." ." . " . " . " . " . " . " ." ." . " . " . " . " . " . " ." ." . " . " . " . " . " . " ." ." . 111114t . " . " . " . ". " ." ." . " . " . " ." ." . " . " . " . " . ". " , ?11: tt1111 " " " " " " " " " " " , " , , , , , " , , , " , ," , " . " ." . " . " ." . * . ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " ." . " . " . " . " . " . " . " . " . " . " . " ." . * . * . * . " . ". " ." . " . " . " . " ." ." . " . " . " . " . " ." ." . " . " . ???????:??????????? ????? 1444444444444i . ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' . f irst . ' x ' : ' . ' , ' . ' . ' . ' ' ' ' ' ' ' ' ' ' + ' . FIG . 6 Patent Application Publication Aug . 30 , 2018 Sheet 4 of 4 US 2018 /0243250 A1 Increased AUC0 - 24h / dos 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 . 1 .illi * ' ' ' ' ' ' ' L ' : ' : ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' : ' , ' ' .. '1 ', ' ' ' ' ' ' ' ', ' ', ' ', ' ', ' ', ' ', '1 ' , '1 ', ' ' ' ' '1 ', '1 ', '1 ', '1 ', '1 ', '1 ', ' ', ' . ChangeinAucidoswithcocon '. 14 .' '. '. 0 2 SC 22 342 og levende os FIG . 7 US 2018 /0243250 A1 Aug . 30 , 2018 METHOD OF TREATING A DOPAMINE other things , the present invention encompasses identifica RELATED DISORDER IN A SUBJECT BY tion of the source of a problem with certain known compo ADMINISTERING LEVODOPA , IN sitions and /or strategies for treating such diseases , disorders COMBINATION WITH A DOPAMINE or conditions and / or for administering relevant agents . DECARBOXYLASE INHIBITOR AND A [ 0008 ] In some embodiments , the present disclosure CATECHOL - O -METHYLTRANSFERASE encompasses the insight that administering a combination of INHIBITOR agents that includes each of ( i ) a dopamine replacement agents , ( ii ) a dopamine decarboxylase inhibitor (DDI ) , and CROSS REFERENCE TO RELATED ( iii ) a COMT inhibitor to a subject, particularly when one or APPLICATIONS more of the agents is delivered by intra - intestinal adminis [ 0001 ] This application claims priority to and the benefit tration of a pharmaceutical gel , provides certain unexpected of, and incorporates herein by reference , each of PCT No . advantages and / or solves one or more problems associated PCT/ SE2015 /050939 , filed Sep . 4 , 2015 and U . S . Provi with prior strategies for treating neurodegenerative disorders sional Application No . 62/ 214 , 742, filed Sep . 4 , 2015 . ( e . g ., PD ) . [0009 ] In some embodiments , the present disclosure pro vides methods in which a COMT inhibitor is administered in BACKGROUND combination with therapy that involves administering a [0002 ] Neurodegenerative disorders result when neurons dopamine replacement agents and / or a DDI by intra - intes normally do not reproduce or replace themselves , thus tinal administration of a pharmaceutical gel. damaged neurons cannot be replaced . Progressive degen [0010 ]. In some embodiments , the present invention eration and/ or death of neuronal cells often results in prob encompasses the insight that in various contexts may be lems with movement ( e . g ., ataxias ) , or mental functioning useful to deliver a COMT inhibitor by intra - intestinal ( e . g . , dementias ). Many neurodegenerative disorders are administration of a pharmaceutical gel, and provides par currently considered to be incurable . Examples of neurode ticular methods and reagents relating thereto . generative disorders include Parkinson ' s disease (“ PD " ) , [0011 ] Among other things, the present invention encom Alzheimer ' s disease (" AD ” ), and Huntington ' s disease passes identification of the source of a problem with certain (“ HD ” ) . known compositions and /or strategies for administering a [0003 ] Parkinson ' s disease is characterized by a progres dopamine replacement agent ( e . g ., levodopa ) . For example , sive degeneration of the dopaminergic pathway resulting in the present disclosure encompasses the recognition of a need reduced concentration of the neurotransmitter dopamine in for treatment strategies that minimize a subject ' s intake of the brain which manifests itself as symptoms of slowness of and /or exposure to the metabolic precursor, while maintain movement ( e . g . bradykinesia ) , rigidity , tremor and poor ing therapeutic benefit of such intake or exposure . The balance in the patient . present disclosure provides such treatment strategies ( e . g ., 100041 Biochemically , dopamine ( 3 , 4 - dihydroxypheneth compositions and /or methods that achieve reduced patient ylamine ) is formed by metabolism of dopamine precursors . exposure , while maintaining therapeutic benefit , as com For example , dopamine is formed by decarboxylation of the pared with a relevant reference strategy ( e . g . , a currently precursor levodopa ( L -dopa ; L - 3 , 4 - dihydroxyphenylala accepted standard therapy ) . nine ) through
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