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Title:
ホウ素化多官能ターゲティング薬物複合体、それらの使用及びそれらの調製方法
Document Type and Number:
Japanese Patent JP2020510666
Kind Code:
A
Abstract:
薬剤;水溶性部分(例えばポリエチレングリコール(PEG)鎖、シクロデキストリン);及びターゲティングユニットを組み入れる可逆的な共有結合;3成分多官能ホウ素錯体(B−錯体)が記載されている。B−錯体コアはワンステップで組み立てられ、例えばグルタチオン(GSH)の存在下では可逆的だが、ヒト血漿のようなさまざまな生体適合性条件で安定であることが証明された。このプラットフォームは、例えば葉酸受容体陽性のMDA−MB231癌細胞に対して高い選択性を示し、低いナノモル範囲のIC50を有する多官能複合体のモジュール構成を可能にした。【選択図】 なし

Inventors:
Gois, Pedro
Fabio, Santos
Application Number:
JP2019547506A
Publication Date:
April 09, 2020
Filing Date:
March 01, 2018
Export Citation:
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Assignee:
Hobione Scientia Limited
International Classes:
C07F5/02; A61K31/69; A61K45/00; A61K47/54; A61K47/60; A61K47/61; A61P25/00; A61P29/00; A61P35/00
Domestic Patent References:
JP2015505559A2015-02-23
Foreign References:
WO2013084199A12013-06-13
WO2014121291A22014-08-07
WO2015116774A12015-08-06
WO2016166319A12016-10-20
WO2014170628A12014-10-23
WO2013110005A12013-07-25
Other References:
CAL, PEDRO M. S. D.; SIEGLITZ, FLORIAN; SANTOS, FABIO M. F.; PARENTE CARVALHO, CATIA; GUERREIRO, ANA: "Site-selective installation of BASHY fluorescent dyes to Annexin V for targeted detection of apop", CHEMICAL COMMUNICATIONS (CAMBRIDGE, UNITED KINGDOM), vol. 53(2),, JPN7021005154, 2017, pages 368 - 371, ISSN: 0004986552
SANTOS: "A THREE-COMPONENT ASSEMBLY PROMOTED BY BORONIC ACIDS DELIVERS A MODULAR 以下備考", CHEMISTRY A EUROPEAN JOURNAL, vol. 22, JPN5020003116, 15 December 2015 (2015-12-15), pages 1631 - 1637, XP002781432, ISSN: 0004986553, DOI: 10.1002/chem.201503943
MONTALBANO, FRANCESCO; CAL, PEDRO M. S. D.; CARVALHO, MARTA A. B. R.; GONCALVES, LIDIA M.; LUCAS,: "Discovery of new heterocycles with activity against human neutrophile elastase based on a boron p", ORGANIC & BIOMOLECULAR CHEMISTRY, vol. 11(27),, JPN6021047179, 2013, pages 4465 - 4472, XP002781433, ISSN: 0004986554
RODRIGUEZ, MARIO; OCHOA, MA. EUGENIA; SANTILLAN, ROSA; FARFAN, NORBERTO; BARBA, VICTOR: "Imino Diels-Alder reaction of boronates: A new route to 3,4-dihydroquinolines", JOURNAL OF ORGANOMETALLIC CHEMISTRY, vol. 690(12),, JPN6021047177, 2005, pages 2975 - 2988, ISSN: 0004986555
HOPFL, HERBERT; SANCHEZ, MARIO; FARFAN, NORBERTO; BARBA, VICTOR: "Synthesis and comparative study of three monomeric boronates by spectroscopic methods and X-ray c", CANADIAN JOURNAL OF CHEMISTRY, vol. 76(10),, JPN7021005153, 1998, pages 1352 - 1360, ISSN: 0004650090
REYES, HORACIO; MUNOZ, BLANCA M.; FARFAN, NORBERTO; SANTILLAN, ROSA; ROJAS-LIMA, SUSANA; LACROIX, PA: "Synthesis, crystal structures, and quadratic nonlinear optical properties in a series of push-pull b", JOURNAL OF MATERIALS CHEMISTRY, vol. 12(10),, JPN7021005152, 2002, pages 2898 - 2903, ISSN: 0004650091
Attorney, Agent or Firm:
西浦 ▲嗣▼晴
High Miki Yoshiki
Tadashi Deyama