HUE034235T2 - Kannabidiol prodrugok alkalmazása helyi és bõrön keresztüli bevezetésben mikrotûkkel - Google Patents

Kannabidiol prodrugok alkalmazása helyi és bõrön keresztüli bevezetésben mikrotûkkel Download PDF

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Publication number
HUE034235T2
HUE034235T2 HUE10755265A HUE10755265A HUE034235T2 HU E034235 T2 HUE034235 T2 HU E034235T2 HU E10755265 A HUE10755265 A HU E10755265A HU E10755265 A HUE10755265 A HU E10755265A HU E034235 T2 HUE034235 T2 HU E034235T2
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cannabidiol
microneedle
pharmaceutical composition
acid
prodrug
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HUE10755265A
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English (en)
Inventor
Audra Lynn Stinchcomb
Stan Lee Banks
Miroslaw Jerzy Golinski
Jeffrey Lynn Howard
Dana Carmel Hammell
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Zynerba Pharmaceuticals Inc
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Publication of HUE034235T2 publication Critical patent/HUE034235T2/hu

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    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/12—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
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Claims (3)

  1. BP247347S kânnâsiâ f^ödruscm áikmmm&u hilyi is bőrön x&mmQü: ssverr èfsin míkrőtókkil SZABADALMI IGÍNVPONTÖK i; Mlkrotûs gyögpaar sgoigálíate mntor karsnabídioi (saanabídlo!] predrug {eiSgyoaysbsfl bőmé: ksmMtüll ítraeeéermall vagy helyi (topical) bevaaetesère egy emlőebe, amely rendszer a hőveíkeadkei tartalmamé a) agy gyógyászati kompcslekx amely agy kannabidloi prodrygoUarialmatL ahol m a kPvetkeaő képletlel bír:
    ahos Xgsinntáseregy .Anion (osaoteppny: ssmsí^ pyögyásaáís^; Pákákból Ätel« Is b) agy iníktop (mfettoedte) #en#zé$ (Pdayf; anói :& gyógyászati ίο^Ι|οϋΦ is - ^j^|i;/|: Äö$I eif^à##pi :S§pît a Äo& ókobíioxlo §M^Ä-Ät vs§^ # alllitö átrendezés beválté** után. vagy â m&mtö «!r»ott*2is oeva;;at#eeve) egykiepHit} 2 As 1. sgèoypont oxeànti gyógyszer szolgáltató tondssir, aboi δ kennabiskol paxirug s gyógyászait kompozíciónak mintegy Os1 :Mî A ííi I; :¾ kp&p|i prpii^ pÉs®ls^«lK; mintegy 5 és nxnfegy 30%-a közötti tartományában ttómeg/tófneg) vagy mintegy 10% As mintegy 20%-a kősód tartományában : A. |pi
    ||:
    ||i
    ::A 3, a? 1, igénypont eset inti gyógyszer szolgáltató renbszan ebei a gytgyàazati kompoddá hiorooà: tormâiàbsa van, eienyoaas shot s Ndrc-gü be vsa építve agy M^sc- vagy tartály (?eeervgir;> ipaû tapaszba (peieb), 4, A? 1 ^eny-pent ezbdnti gyógyász szolgáltató rendszer, spot a gyógyászati köPtpoztciő tartalmas továbbá spy COX >sn:nkork amsiy a Következők kosai váteszmato ki: aszpirin, óikiofenak, diansak iseioprofett, kumiproién, ibepaiéry sneometedn, keioproièn ketoroiaX ernten amsas (mefenamk: ació>, meioxMm, nabameton. naptexón, oisdxin. oxaprozim peo-ekácx szálasaiéi, ssuiíaszatáXin. exmindak, toimstin, molexdak, $0-533, FR 122047. etoooiák, sdakoxib, roiekodb. vakískosib, parekoxib. tuoxfakoxid és etbekextb.
  2. 5, As 1. igénypont szerinti gyógyszer szolgáltató rendszer aboi a gyógyászati kompezició tmtslmsx ioyabeá egy Pahatoíásíokosét (penetration enhancer). amely a kővetkezők közül választható ki: izosslaariesav. ok tán sa v, oídnsav, omllslkonok laarllsikohok etikaeát, ixödxspikmlilsztáÍ. etóii-szteerel metlNaurát, dkso&amp;ngpil-aómál ρίΐοοηηηχοηοΐδοίηΐ takahidrofurlunipikohoi palieiépgiám tust, poiisÍ|ngfkd; proptilnglml. 2-C2-éímd'atoxi}-etanöl, ólssiiongiíkol monometiláter. poiietiSsnedci aikani liera;. paiieálénoxid rrxxnomatiiáterek, poiteiiténaxló ciimebléterek. bioreilósznifoxid, glicerin, eeetoenalsav észter. N-alkk-pifrokdork törpének, mekianoi. meinyrmoioat DAnic-nén, m<möote=n; cined, oieit-cleát, eland. propánok Orbánok 2-büinnol, pentánéi, ki-poniand. hexend. oktános, nonsnoi, dékánok boazkdkohoi, Pöiyxsmer 231 Posyxamsr 132, Pciyxemor 1§4, Pdyserbde 20: Pölysoróáie S3, 8r| 30, Búj 33,8>'ii Θ3, 8nj ®. Spa« 20, Span 40, Spsa 30, Span SO. ïwo*n 20. îwson 40. Im 00, ivvoors 00, Myti 45: Myrj 51, blyg 52 es Rigiyöl 340, oidnyôsen a baóotoiéklokoxó a gybgyâssali όηηχχχόοχχιοΚ oxoisgy 0..1 os roiatogy 40%-a kèxdtli tarfôyRnyylban (ioaropPomfep}. s-niniegy 0:1 és mintegy 33%-s kosôiti tartofnènyàbas (tömog/iónysg), mintegy 0,1 lo minisgv 20%-o közötti tartonsányában (tbínegdönieg? vagy mintogy 1 és mintegy 10%-P kösblii tartornányápan (tömog/foinag} von ioieo €, Az i. ájériypom sxannti gylgyw 6Zöig«ö ronPoxok aboi δ gyógyászati kompozíció iortaiaux? toxlbfeá ogyx kissob mosokníaiomogn (tower) aiknboik ameiy a kovetkosók koabi vóiasalnatö ki: otand és izopropwol.
  3. 7. As 1 iponypnat skä^üs gyógyír sxoigáitatö roncks^r, onoi a gyógyássaii kompoxicíó sxotgàkans a kannsbid«; prodrag gyógyásxabiag natókcny mennyiségit egy adott kiOtanarnon at< s-nsly i ^övstkaxok kóxta yáiasxtnatd ki: mintegy 1 mt mintegy ! ' o , ^ , - 'X y·- 0 > a ' ' ggx -, i ' »--cy 'N Oia m» logt x4 ufa a'tagy 43^ά ' 'epypA ¢51,pniefy δ nap, mintegy δ nap és mlniegy 7 nap íl M i i; igénypontok párpiaiyiKei Siapnt; :p|g^r szöigáliáió raapslPí bPtsgsègi áilepöíofc λ**»«^!.** ·?&amp;ν> âüapo? a Követek koa» választató Ki· akut ha?oyaim.% gyuüacias {paws-Ä **#**= iMPi*W m^mm hasnyéimaigy (pancmatio) rák, imalygis (nausea). hányás (emesis), sorvadás·:* (wasting, »amèvm*, nsv-^vaaas, teefterâpiâsaa tnduÄ émeiyfáé éé iilnyá Cyenyting), sikoheifPlyasstésia^sdaifeanassp^í §«tép^ gyulladásos béifandoüanasségek. izületi gyulladás iÂÉj, hőrgyulsdás (darmsaltis): rhsuiMsOié ^íé?#'h H*>léná$· sbtfarkas (systemic lupus erylhemslosush dint :iÜ^iNâ.;:Â?ôpafta. Svsomo«· (smogies), égések (bura), s&amp;au^dgs {«^>«0 featosiSi;: &amp;&amp;*# smm rnm^m {uicerp ^márnimm^ (p*^ &amp;*m m*m ^gyulladás (direct den*»*}. ekcéma nelyagos, h^esa-ioÂ)ù i^»Äpi«ÄÄ hssado bőrqyuHadás (exfbüaiive őermitfis), §omoafert<M&amp; (bposis fengotdm% bornalyagosodês smyos iSdkíorrnéjú börvürösség (erythema multiforme) {péiéàsi Sîë^^sofl^ftôrêffta)·; •dlrmatitts}. izüietmsrevnèges osigolyabánislorn {ankylosing: spondylitis), gikkeiysőmöíes Étíféu'.jiíytK«**a> »fsoi*«»»· Raiisfdeie sgindrw?>s, %sayény (ρ% pgmniészeeadéa léhénérosáieiodsiS;?. írnésödlágos i^nfes tâfssasom: ia]aasmaa: menstruáciéná! t$m·. Éumtápi». il» és káa : (nluseoskSiaíaí) f^dsíong muté? utáni: nearopelikue kömpfcáaik, polymyositis, akut. nem d^iaps tsnosynoÄ% syéktomlégyuiiádss (bursitis), bufyoKgydii&amp;saa (epiamrdyiitis). daleset yfötú dásnlizüiet; gyulladás töstsöéftníitis), esöntlzbiéli gyuliádss, rhsumatéid: aîmsd^ i&amp;iewlffya'’' gyulladás {ayncnáti^ és 3 bainövekeöésptiása. S. A:? 1. igénypont serins gyógyszer sshgáltslé rendszer, ahdi sgyégyásMi kompozleíG táftsimszdh aiaiaboiskat: (!) ksnnahidiol prodrug a mintegy CM % és m;n!sgy 40% kőzett! tartományban; |íi): agy vagy (ebb iätsmldöszer (ao-solven?) a mintegy ö,1 % mintegy tö% kópttí kanornáhyPn; (ki) egy kis molekutetsmsgSkiovyer) aikoho! a mintegy 1 $% és; mintegy M% ÄSiti tapmanypap; as; (ív) víz olyan mannyiaégPnf pmgtyafegandő a;knmpod!c!Qhsg, hagy aine a áOO'iVot (fomegrtonieg). 1ö. A S. igénypont; szerinti gyógyszer szolgáltaié rendszer. ahol á Kannábídipl poxirug a gyógyászati komböginjéban my-^n mennylségban van jelen, amely a mintegy S% és mintegy 3Ö% közötti tartományban (tömeg/tömeg) van, vagy á: mintegy 10'S is : mintegy 2C% közötti tartományban (íoineg/tömeg) van. 11 A o igénypont saarlng gpgyszer szeigástato Ä Ä * ifsÄszef a tkővétkezék ködül iVáisakthai kk atari!, Pristaíkofwl as ezek kevatikaí, 12, A §. igénypont szerint! gyégpzar agoígáltató rasmszar. atm! a gyógyászati xompoîicio hidragèi lOitnaiaban vmn, giorsyoaan ahol a hidfögll ba van építve agy mátrix- vagy tartály yaservoin típusú tapaszba (patch) m A a igénypont szerinti gyégysgér szöigiitäirshpzah §-##s^ kémpoglclö &amp;Mm® továosáipy φ§\ΰΜ ameíy aikövatkedök kézüi: váíasdthatS:ki: nem-fa-iagos COX innsoitor, ΟΟΧΊ inhip-mn %s bOXi inhibitor, 14, ügyOfet: smeiy a következők közi vâisazthsfèki;
    észből X jeisîriiése *Ρη·οη. arnsiy ayögpsMiisg sllopöhafössvakPî pâmîpik,
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