HUE031405T2 - Kétszeresen acilezett GLP-l-származékok - Google Patents

Kétszeresen acilezett GLP-l-származékok Download PDF

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Publication number
HUE031405T2
HUE031405T2 HUE12713164A HUE12713164A HUE031405T2 HU E031405 T2 HUE031405 T2 HU E031405T2 HU E12713164 A HUE12713164 A HU E12713164A HU E12713164 A HUE12713164 A HU E12713164A HU E031405 T2 HUE031405 T2 HU E031405T2
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derivative
glp
ethoxy
chem
previous embodiments
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HUE12713164A
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English (en)
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Birgit Wieczorek
Jane Spetzler
Thomas Kruse
Lars Linderoth
Jacob Kofoed
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Novo Nordisk As
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol

Claims (7)

  1. KéT«2i-Resr.NA€ii,K/^.TT g t jm ^xArm αχ fkok SéulsadsM Igénypöiíök
    1, QLP~ I -sssslög sz&amp;rrnszé&amp;s* amely analóg tartalmas. egy elsü K. ankeosavat a CÖUM. (7-G7J (B1Q IÖ KÓ: I) '27-ss paafosóíáaak megfelelő púidéban; egy nsamdik k ampKPKval a Cd.lM GAl/i 36-os pozíciójának megteltéé póridéban. és legfeljebb IG amPSPsav eltérést a GLP- I i7-3?}Xs;l bsssehasoplidas abo! aeelső K atmaossv jelölése K7 j és a második X amjnoiery jelölése X''7 ahol a?, analóg Ktrtaimaesa ae 1 képles saerimí Gl.P-1-analógok Xi5sí;<^Xt83.s“C3iU”ía!yv 1 m-Xsa >?” í h r-· 3 e r ~A s p - X a a; >ykse:X:s ,s :,--.7¾¾ Xasi.r>Í3a?í''Xasí<i'-Afg-lys-Phs-lte-Gk{-XaaiH-ei5-Vaí'Kaaií-Gfy>‘Lys-X0a<jrXasj%*X3Í#, (ífépk# ékéi Xái- jélepíésé L-ldsaMdiim smidm:oprvptosík tx-ttldr*st-htsztldltu D-hisaddk>, de?amincv>ht.«ztl<h'n, 2-am«né* -niseúdisi, pdbátóxkMsandisy, htenohhabdpg ^T-aestlkhissaMfe d'SGombMdsmkhn, a-í%ermm}í:114dsmkllo, p--ntetü-hts2tíd«n; 3-pimHaí&amp;mn. .dpi rid; island vagy 'i-pkidikdaobe Xaa. jelentése Alá. Gly, Vsl, Lvu, lka l'ht, ke?, Lys, A;b, (;-andnoe;kk?pnpni)karbmnav, : k-am inteni: lolndl}·· ktnbottssv, (i-ctntsníKiklopentlSjkafbonsav, i l-smintabklohedkkadsonsaA (l-ambmcikkíhepbljkarbomav, vagy (Gami socik íookftl jkarfenns&amp;v; Xas;; jeleaíése Lys vagy- Hm; Xaai4 jelenSése Val vagy I .eu; Xaa-.s jelentése Ser. Arg, Ase, Gin vagy öle; Xaa;t) jelentése Tvt vagy Gitt; Xaa?o jelentése Len, Lys. vagy Mas; Xaa;.i jelentése Gly, Gitt, Lvs, vagy Aib; Xíiav>s jelentésé Gin, Gitt vagy Arg, Xaa >4 jelentése Alá vagy Lys; Xaajs jelestése Aki vagy Vak Xaa,, jelentése Trp vagy His. Xaa?4 jelentése Glu, Asm Gly, Gin vagy Arg; Xaa$? jelentése Gly, Alá, Gl«, Pro, l.ys. Arg, vagy rtjoós jelég; Xmj* jelentése See, Gly, Alá, GIp, -Gin, l»rn, Arg, vágy: pipes jaletg és Χμ;<> jelentése Gly vagy nines jelest; amely saátrnaxék tartalmas két kinyúló csoportot, amejyuk rendre a KaXbes és a fcaposogkbmk egy AsaxeXdtoikesesAdl, ídtóiá:k|ssyölé csoport a ktlvedsAik köstül választod·; Gh.em.-2 -and· Cltem, k Cbem, 2: ΙΑΧΚΑΟΧ^'-Ο'ΙΟ-Ι^ΑΙΟ^ Cbem. 1 H0(XM€ü:Ax4X'>-·*. adói y. értéke ó-lé, tartományba eső egéss: sedn, és y értéke 3-17,. tartományba: s»ö egésasKám; és aé össaéköié Glsétsa. 3-151 tssluboae:
    ahol k 2 Réka 05. OEogEbyOvasA GOss sxám, es δ Oíákg ÍAb 1:&amp;ríó|S#svbá @kd gggO |£ÍM; vágy győgyisxstiigg >3|fögödh#|ö séjíi, pbbfb vagy IsAara,
  2. 2, Αχ I. %0%ypwl 4¾ CH$&amp; S'IMM' .$ «Állá 140 íaiíotoáwyfes .«$§£*· <h« sxára
  3. 3, Ax Wrtí^lplfee xMrHiSisxáríKaxek, &amp;h<4 k Oibkg R. 4> Ax oioAHgánypöíMök #5ί<4·.'4#!#:« í> J, Ax albxb ig#í5>?p<íö5:£ík ^srmé^yík© ákgpptt aAkxóaxákv ahol a® öss2bkfk4 iggálám® O vábM agy Oki kotos gySköi &amp;?gály á k#NAlksx§k ksMII váfászkkOChOH. 8, JOvágy €k«ái, ?;. ?Á»rn.b;
    Akvagy Chem ?
  4. 8. Ax 5. Igénypont süerimi sasrrsagék, ahol x ΘΙ-wtetíés gybk ps» vas>jtl««* ahol ψ érMke 1: vagy 3.
    7, Az elöxö igénypontok bármelyike szerinti $z&amp;mwA< s&amp;öi ax össaálcöiő az OáS vagy a mááoílik E ••amioossv «|>s?iteo.-amioo*sopott|áhoak^3csolédik< §<. A® siöxi kboyposlök bámolyike sxeriRti xMrmxaOí, ahol x Oaáks 12» vagy ábal Gtean 3 a Mvpfe·· ?:·:> Cham. 2b ksgM szarlak:
    (Pí«m, 2 b) f, As 08x8 Ígébygosbok bárkpyxks ssamb xkáxmx®ék} sbgl x xAcfe 12» vagy V #Eks a 944 ssrkg ns&amp;oyba «# sgösxxxám,
  5. 18. Ax ál8a:8 IgbayiEakk: bángaly lka vsarkki szárasAí#, ahol a 6LF-4 kaklog g khyatkpbAbibosav·' vaköxásokxí tarialírazaa, a GLP-1 (7-17;-hex kpeví PkO 10 NO. !): íh> 221:» 26R. 270, 302 34R, 7aR, 30:. 320; (0)38¾ 37KS 381E34R, 38E, 3SH; (01) 23¥; 2¾ 37K, 38Ef 34R, 38E, 33;Q;)ysb) 250,28R, 2¾ 380, 340, 4>K, 381;; vagy tsxvb) 2Afb, 221;» 38R, 27K, 38B, 34R, 38E, 38B;, 380; vágy gyBgyOstóíag dógadhaíó sój% ;xímdj&amp; vagy é-mers.
  6. 11, Á í4< MmlMl smnmmk:. mséty » («X (yáj^ (s»i Cxidlds.iksvis) bfeslylft® sgydnidsllftl ál; <is»!:Kmv-vá:U>Há5ok egy ci.oporgáí U5f?alm$£2£.
  7. 12. Λ kftv«}k«a6k kö,íö] vsgyáte Kj*1·5 5-13 -! 2" [3 ->f ! f(4 S^' -4-k&amp;s^sí^ -^{1 Cl-1'4'· ksí silfgsí í>s 1>sl« kssí 3 *: Pí^í ylí5<Vp>i stímí ϊϊΙΙμϊϊΙ s>o |síös: l|íítöXí j scí? - t^lambaifötójetö^jace^ tm5stE3í3í1 j i^íis^sí jeíssxl i|'f ölti ': ?C11í.ras Cherc. S1:
    ^ilryvyj;v.[f2'i;iril(2Sv44:,arhx'\;---gÜ}Hl7-.arSH;\ÜbH>xí5<iskáai«kmv5Kgba1a;v)iltóHiü‘K>kíovdvKíívil' s*if:?{5o!biíí'íSRo!i]afrJ»o)ciftSfjs;J<.ívlJiKOí!!};srmíj<j){;:<!\i}s{('í<í]®£:£,tü’)-[AÍ'g''\Ííy.'i"X)iu"’.Arg. '\!.,yv,vj'G?.P-Mí-í3 7}>ps|s1:isíi ICvlö., Ohem. 55:
    :i><''' ”t" 1'C2 H2' I *"!5 -f114g'f'4 -kml?v>í< 5 -4- f ^ ^^ *kííí'bö:si 1¾¾5¢3st!>dekíi«ó U&amp;ϊϊχi ííí>]bytí&amp;físvs ií)jötöM Jötoxs |^ fϊ<?! í> títííáöil! &amp;mlsríö!« í:í»í:í] íífesí!!»*:«£ í 1 ΐοj ®íöx 0 eí^siJsís^íiy>-fV ^^^A® %lv^s2 Oííj A rg . s '^ | -01^-1 '•i'?- Gp-f^pt^Kílíp, Chem, (S1:
    Ntó ?-p~p~p "l'll-p-p·' ||C4SH'tÉ%4* i'4-[töpl "ksr^ös s ÍsmiSöTb^í^»sl|ömífí0^ío?ííJistssX3|ístó«- ii||^l8#Pm|l§ti##l|^8MIJ> ^^-Ρ'^^[3-|Ρ-ρ-Ρ4|ί4§}^^Ρ0χ^4-Ρ;0-<4'4ϊ^ίέίχΙΙϊ:5Ρχϊ)0«Ρ53ΡΙίίΜΡδ}- buiaööínsmisojeíoKJlstoxtjacsíjllaröjsolsfóxjjíHoxUaceinj-fVas'^jArg^ LyG\G k:pOiP\Ly:P]-GLP- ü G?G?}--pepkd.O-Gki, Chism. 82:
    ^^'-•p»|2ip--CP"p-[P|[P§)^-^p^sM“[!8''p~kSítíi:Gippó2pdé|iá8éibí);í!ai;spJMís.íKs!l!ássíá3ö|etó>:i]íÍ<>si!55!:e' 8 l]smihö]^oxlj«l«x:n8«#l]s Jsf^-p* Ρ4*ΝΡ· [2*p-||Pi)“4'-feíPos:!--4 *(! OpíGkssí fess fossx i >dek<mol I amfcio) - 4Μ 7)-p«puáil'G!ú*G!ys Chím 80:
    «^5lj<8ninoleíösfl»to^l|^í1!|t ^^-|[^ρ*Ρ'*||2·;Ρ4Ρ-|((4§)^*^^^ΕΗ*ρ.^4^^^Ι^#^)^^3%^#Ι]Λ· Cbefn. §1:
    vapf ;$y#|y:SsKati!sg éslíMS. 1.&amp; A* W£. 4W$WM-i$&amp;i0$M4M i^»§ a$k*ima?ás?a. f 4. Λ:>. ϊ - ;2. H:>.a:'-ypo;;?ok bármelyike s?eíuítí származék, íliábstfes.s vágy á&amp;M bssabft%g.if íSaíagségigfe,: t^láfkéMss&amp;f d&amp;sá&amp;föggd plabstéSMS k»bíil|M4iék éS^gjt P^étssxek-Axmd- sksm b#íbé!y ®spiö:KéSebsB tört#b áfkálísaMsfá, Mvsgj; fi^yíjpsfm&amp;rek javiSisára, p*^|í»:ÍMk'dö JavMsáís, Mvag^: áísbmsass betegség pm|fgssaié|áask lsbsiei:tetb^ sara vagy ntegíbbaésérite
HUE12713164A 2011-04-12 2012-04-12 Kétszeresen acilezett GLP-l-származékok HUE031405T2 (hu)

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US201161474913P 2011-04-13 2011-04-13

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US (5) US9266940B2 (hu)
EP (2) EP3225631B1 (hu)
JP (2) JP6022538B2 (hu)
KR (1) KR101972836B1 (hu)
CN (3) CN106117344B (hu)
AU (1) AU2012241894B2 (hu)
BR (1) BR112013026195A2 (hu)
CA (1) CA2832811A1 (hu)
DK (1) DK2696687T3 (hu)
ES (1) ES2612278T3 (hu)
HU (1) HUE031405T2 (hu)
IL (1) IL228386A (hu)
MX (1) MX355361B (hu)
MY (1) MY161450A (hu)
PL (1) PL2696687T3 (hu)
PT (1) PT2696687T (hu)
RU (1) RU2602601C2 (hu)
WO (1) WO2012140117A1 (hu)
ZA (1) ZA201307119B (hu)

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WO2011080102A2 (en) 2009-12-16 2011-07-07 Novo Nordisk A/S Glp-1 analogues and derivatives
RU2600440C3 (ru) 2010-12-16 2021-12-10 Ново Нордиск А/С Твердые композиции, содержащие агонист glp-1 и соль n-(8-(2-гидроксибензоил)амино)каприловой кислоты
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US10933120B2 (en) 2012-03-22 2021-03-02 Novo Nordisk A/S Compositions of GLP-1 peptides and preparation thereof
ES2715308T3 (es) 2012-03-22 2019-06-03 Novo Nordisk As Composiciones que comprenden un agente de suministro y su preparación
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EP2863895B1 (en) 2012-06-20 2021-04-14 Novo Nordisk A/S Tablet formulation comprising a peptide and a delivery agent
AR091866A1 (es) 2012-07-23 2015-03-04 Zealand Pharma As Analogos del glucagon
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
BR112015026325A2 (pt) 2013-05-02 2017-07-25 Novo Nordisk As dosagem oral de compostos glp-1
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US11034746B2 (en) 2021-06-15
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US10005827B2 (en) 2018-06-26
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