BR112016017993A2 - Gama-aminoácidos beta-substituídos e análogos como agentes quimioterapêuticos - Google Patents

Gama-aminoácidos beta-substituídos e análogos como agentes quimioterapêuticos

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Publication number
BR112016017993A2
BR112016017993A2 BR112016017993A BR112016017993A BR112016017993A2 BR 112016017993 A2 BR112016017993 A2 BR 112016017993A2 BR 112016017993 A BR112016017993 A BR 112016017993A BR 112016017993 A BR112016017993 A BR 112016017993A BR 112016017993 A2 BR112016017993 A2 BR 112016017993A2
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Prior art keywords
beta
amino acids
gamma
substituted amino
analogues
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BR112016017993A
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English (en)
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Jandeleit Bernd
Fischer Wolf-Nicolas
J Koller Kerry
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Quadriga Biosciences Inc
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Application filed by Quadriga Biosciences Inc filed Critical Quadriga Biosciences Inc
Publication of BR112016017993A2 publication Critical patent/BR112016017993A2/pt

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    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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Abstract

GAMA-AMINOÁCIDOS BETA-SUBSTITUÍDOS E ANÁLOGOS COMO AGENTES QUIMIOTERAPÊUTICOS. Aminoácidos (Beta)-substituídos, derivados de (gama)-aminoácidos (Beta)-substituídos e análogos de (gama)-aminoácidos (Beta)-substituídos e (bio) isosteres e seu uso como agentes quimioterapêuticos são divulgados. Derivados de (gama)-aminoácidos (Beta)-substituídos e análogos de (gama)-aminoácidos (Beta)-substituídos e (bio) isosteres são substratos LAT1/4F2hc, capazes de passar através da barreira de sangue cerebral e exibe captação rápida e retenção em tumores expressando o transportador LAT1/4F2hc. Método de sintetização de derivados de (gama)-aminoácidos (Beta)-substituídos e análogos de (gama)-aminoácidos (Beta)-substituídos e (bio) isosteres e métodos de usar os compostos para tratar tumores também são divulgados. Derivados de (gama)-aminoácidos (Beta)-substituídos e análogos de (gama)-aminoácidos (Beta)-substituídos e (bio) isosteres exibem captação seletiva em células de tumor expressando transportador LAT1/4F2hc e acumulam em células cancerosas quando administrados a um paciente in vivo. Os derivados de (gama)-aminoácidos (Beta)-substituídos e análogos de (gama)-aminoácidos (Beta)-substituídos e (bio) isosteres exibem uma eficácia aumentada em uma variedade de tipos de tumor.
BR112016017993A 2014-02-03 2015-02-03 Gama-aminoácidos beta-substituídos e análogos como agentes quimioterapêuticos BR112016017993A2 (pt)

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US201461935235P 2014-02-03 2014-02-03
PCT/US2015/014299 WO2015117146A1 (en) 2014-02-03 2015-02-03 Beta-substituted gamma-amino acids and analogs as chemotherapeutic agents

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US (3) US9394236B2 (pt)
EP (1) EP3102194A1 (pt)
JP (2) JP6271766B2 (pt)
CN (1) CN106132406B (pt)
BR (1) BR112016017993A2 (pt)
IL (1) IL247098A0 (pt)
TW (1) TWI585066B (pt)
WO (1) WO2015117146A1 (pt)

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CN108947947A (zh) * 2017-05-17 2018-12-07 北京新领先医药科技发展有限公司 一种沃拉帕沙中间体的制备方法
CN113024637B (zh) * 2021-03-10 2023-05-16 江西师范大学 一种以水溶性炔酰胺作为缩合剂制备卡非佐米的方法
CN117247339B (zh) * 2023-11-16 2024-03-12 潍坊富邦药业有限公司 一种烷基胺衍生物的制备方法

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CN106132406A (zh) 2016-11-16
CN106132406B (zh) 2020-03-27
EP3102194A1 (en) 2016-12-14
TW201629005A (zh) 2016-08-16
US9937139B2 (en) 2018-04-10
JP2018016644A (ja) 2018-02-01
JP2017508786A (ja) 2017-03-30
US20150218085A1 (en) 2015-08-06
US9682921B2 (en) 2017-06-20
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TWI585066B (zh) 2017-06-01
US20170246135A1 (en) 2017-08-31

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