BR112012014475A8 - derivados de glp-1 duplo-acilados. - Google Patents

derivados de glp-1 duplo-acilados. Download PDF

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BR112012014475A8
BR112012014475A8 BR112012014475A BR112012014475A BR112012014475A8 BR 112012014475 A8 BR112012014475 A8 BR 112012014475A8 BR 112012014475 A BR112012014475 A BR 112012014475A BR 112012014475 A BR112012014475 A BR 112012014475A BR 112012014475 A8 BR112012014475 A8 BR 112012014475A8
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integer
range
glp
chemical
residue
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BR112012014475A
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BR112012014475A2 (pt
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Spetzler Jane
Lau Jesper
Tibor Kodra János
Linderoth Lars
William Garibay Patrick
Sauerberg Per
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Novo Nordisk As
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    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/65Insulin-like growth factors, i.e. somatomedins, e.g. IGF-1, IGF-2
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    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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    • G01MEASURING; TESTING
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Abstract

derivados de glp-1 duplo-acilados - a presente invenção refere-se a um derivado de um análogo de glp-1, cujo análogo compreende um primeiro resíduo k em uma posição correspondente à posição 37 de glp-1(7-37) (seq id no:1), um segundo resíduo k em uma posição correspondente à posição 26 de glp-1(7-37), e um máximo de vez modificações de aminoácidos em comparação com glp-1(7-37), em que o primeiro resíduo k é designado k ^37^, e segundo resíduo k é designado k ^26^, cujo derivado compreende duas porções de ligação de albumina anexadas a k ^26^ e k ^37^, respectivamente, em que a porção de ligação de albumina compreende uma porção de protração selecionada entre: produto químico 1: hooc-(ch ~2~)~-co-* produto químico 2: hooc-c~6~h ~4~-o-(ch ~2~)~-co-* produto químico 3: r ~1~c~h~-(ch ~2~)~-co-* produto químico 4: hooc- c ~4~sh~ 2~-(ch~ 2~)~ w~-co-* na qual x é um inteiro na faixa d 6 a 18, y é um inteiro na faixa de 3 a 17, z é um inteiro na faixa de 1 a 5, r ~1~ é um grupamento tendo uma massa molar não maior do que 150 da, e w é um inteiro na faixa de 6 a 18; com a condição de que quando a porção de protração é o produto químico 1, a porção de ligação de albumina compreende adicionalmente um encadeador de fórmula do produto químico 5: *-nh-(ch ~)~- (o- (ch~)~)~-o-o(ch~)~-co-*, em que k é um inteiro na faixa de 1 a 5, e n é um inteiro na faixa de 1 a 5; ou um sinal, amida, ou éster farmaceuticamente aceitável do mesmo. a invenção também se refere à aplicação farmacêutica do mesmo, por exemplo do tratamento e/ou na prevenção de todas as formas de diabetes e doenças relacionadas bem como a novos peptídeos correspondentes e intermediários de cadeia lateral. os derivados são adequados para administração oral.
BR112012014475A 2009-12-16 2010-12-16 derivados de glp-1 duplo-acilados. BR112012014475A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09179390 2009-12-16
US28860109P 2009-12-21 2009-12-21
PCT/EP2010/069932 WO2011080103A1 (en) 2009-12-16 2010-12-16 Double-acylated glp-1 derivatives

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BR112012014475A2 BR112012014475A2 (pt) 2018-04-24
BR112012014475A8 true BR112012014475A8 (pt) 2018-07-03

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US (4) US20120329711A1 (pt)
EP (4) EP3000482B1 (pt)
JP (5) JP6006118B2 (pt)
KR (1) KR101817607B1 (pt)
CN (6) CN104311657B (pt)
AU (1) AU2010338387B2 (pt)
BR (1) BR112012014475A8 (pt)
CA (1) CA2784757A1 (pt)
DK (1) DK2513140T3 (pt)
ES (2) ES2625735T3 (pt)
HU (1) HUE027229T2 (pt)
IL (1) IL219945A (pt)
MX (1) MX2012006634A (pt)
PL (1) PL2513140T3 (pt)
PT (1) PT2513140E (pt)
RU (1) RU2559540C2 (pt)
TW (1) TWI484974B (pt)
WO (3) WO2011080102A2 (pt)
ZA (1) ZA201204436B (pt)

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