公开(公告)号：EP3101004B1

公开(公告)日：2018-12-05

申请号：EP15744067.8

申请日：2015-01-29

申请人： Japan Science and Technology Agency

发明人： KUNINOBU, Yoichiro ,  KANAI, Motomu ,  IDA, Haruka ,  NISHI, Mitsumi

IPC分类号： C07D213/53 ,  B01J31/22 ,  C07B61/00 ,  C07F5/04

CPC分类号： C07D213/53 ,  B01J31/1815 ,  B01J31/22 ,  B01J2231/40 ,  B01J2231/4277 ,  B01J2531/827 ,  C07F15/0033

摘要： There are provided a compound capable of being a novel ligand allowing regioselective borylation to be performed in the aromatic borylation reaction, and a catalyst using the same compound. There is provided a bipyridyl compound represented by a general formula (1): (wherein A represents a single bond, a vinylene group or an ethynylene group; X represents an oxygen atom or a sulfur atom; n pieces of R 1 may be the same or different, and R 1 represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted aryloxy group, an optionally substituted amino group, a cyano group, a nitro group, or an alkoxycarbonyl group, or two adjacent R 1 may form a saturated or unsaturated ring structure optionally containing a hetero atom together with the carbon atoms bonded to the two R 1 ; R 2 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, or an optionally substituted aryloxy group; and n represents a number of 1 to 4).

公开(公告)号：EP3101004A1

公开(公告)日：2016-12-07

申请号：EP15744067.8

申请日：2015-01-29

申请人： Japan Science and Technology Agency

发明人： KUNINOBU, Yoichiro ,  KANAI, Motomu ,  IDA, Haruka ,  NISHI, Mitsumi

IPC分类号： C07D213/53 ,  B01J31/22 ,  C07B61/00 ,  C07F5/04

CPC分类号： C07D213/53 ,  B01J31/1815 ,  B01J31/22 ,  B01J2231/40 ,  B01J2231/4277 ,  B01J2531/827 ,  C07F15/0033

摘要： There are provided a compound capable of being a novel ligand allowing regioselective borylation to be performed in the aromatic borylation reaction, and a catalyst using the same compound. There is provided a bipyridyl compound represented by a general formula (1):
(wherein A represents a single bond, a vinylene group or an ethynylene group;
X represents an oxygen atom or a sulfur atom;
n pieces of R 1 may be the same or different, and R 1 represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, an optionally substituted aryloxy group, an optionally substituted amino group, a cyano group, a nitro group, or an alkoxycarbonyl group, or two adjacent R 1 may form a saturated or unsaturated ring structure optionally containing a hetero atom together with the carbon atoms bonded to the two R 1 ;
R 2 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted alkoxy group, or an optionally substituted aryloxy group;
and
n represents a number of 1 to 4).

摘要翻译： 提供能够作为在芳族硼酸化反应中进行区域选择性硼酸化的新配体的化合物和使用相同化合物的催化剂。 提供由通式（1）表示的联吡啶基化合物：其中A表示单键，亚乙烯基或亚乙炔基; X表示氧原子或硫原子; n个R 1可以相同 或不同，R 1表示氢原子，卤素原子，任选取代的烃基，任选取代的烷氧基，任选取代的芳氧基，任选取代的氨基，氰基，硝基或烷氧基羰基 基团或两个相邻的R 1可以形成任选地含有杂原子和与两个R 1键合的碳原子的饱和或不饱和环结构; R 2表示氢原子，任选取代的烃基，任选取代的烷氧基 ，或任选取代的芳氧基; n表示1〜4的数）。

公开(公告)号：EP3266765B1

公开(公告)日：2019-10-02

申请号：EP16761669.7

申请日：2016-03-04

申请人： Japan Science and Technology Agency

发明人： KANAI, Motomu ,  SOMA, Yohei ,  SHIMIZU, Yusuke ,  TANIGUCHI, Atsuhiko ,  OISAKI, Kounosuke ,  KUNINOBU, Yoichiro

IPC分类号： C07D207/44 ,  A61K31/69 ,  A61P25/28 ,  C07D207/456 ,  C07D401/14 ,  C07D455/04 ,  C07F5/02 ,  A61K41/00

公开(公告)号：EP3590919A1

公开(公告)日：2020-01-08

申请号：EP18761809.5

申请日：2018-03-02

申请人： Japan Science and Technology Agency

发明人： NAGASHIMA, Hideo ,  TAHARA, Atsushi ,  KITAHARA, Ikumi ,  KUNINOBU, Yoichiro

IPC分类号： C07C225/10 ,  C07C209/28 ,  C07C211/56 ,  C07C221/00 ,  C07C253/30 ,  C07C255/58 ,  C07D265/38 ,  C07D285/14 ,  C07F5/02 ,  C09K3/00 ,  C09K11/06 ,  C07B61/00

摘要： Provided are a donor-acceptor type compound having a novel structure and its use.
An enamine compound represented by general formula (1)

(in the formula:
R 1 represents an electron-withdrawing group;
A represents a divalent aromatic hydrocarbon group which may contain a substituent, a divalent aromatic heterocyclic group which may contain a substituent or a divalent unsaturated aliphatic hydrocarbon group which may contain a substituent;
R 2 represents a hydrogen atom or a hydrocarbon group which may contain a substituent;
R 3 and R 4 are the same or different from each other and represent an aromatic hydrocarbon group which may contain a substituent or an aromatic heterocyclic group which may contain a substituent, or R 3 and R 4 together form an optionally substituted bicyclic aromatic heterocyclic group containing two or more nitrogen atoms or a nitrogen atom and an oxygen atom or a sulfur atom, or a tricyclic aromatic heterocyclic group which may contain a substituent; and
R 2 and A, or R 2 and R 3 may together form a cyclic structure).

公开(公告)号：EP3266765A1

公开(公告)日：2018-01-10

申请号：EP16761669.7

申请日：2016-03-04

申请人： Japan Science and Technology Agency

发明人： KANAI, Motomu ,  SOMA, Yohei ,  SHIMIZU, Yusuke ,  TANIGUCHI, Atsuhiko ,  OISAKI, Kounosuke ,  KUNINOBU, Yoichiro

IPC分类号： C07D207/44 ,  A61K31/69 ,  A61P25/28 ,  C07D207/456 ,  C07D401/14 ,  C07D455/04 ,  C07F5/02 ,  A61K41/00

CPC分类号： A61K31/69 ,  A61K31/4025 ,  A61K31/4725 ,  A61K41/00 ,  C07D207/44 ,  C07D207/456 ,  C07D207/46 ,  C07D215/06 ,  C07D401/14 ,  C07D455/04 ,  C07F5/02

摘要： Provided are a compound which is useful as an in vivo applicable, amyloid-oxygenating catalyst selective for amyloid and applicable not only to an Aβ peptide, but also to other amyloids and a drug containing the compound for preventing and/or treating amyloid-related diseases.
Disclosed is a boron-dipyrrin complex represented by the following formula (1)

wherein X 1 and X 2 are the same or different and each represent a halogenoalkyl group or a halogen atom;
R 1 represents a hydrogen atom, an alkyl group, or a group represented by formula (b):

R 2 and R 6 are the same or different and each represent a hydrogen atom or a halogen atom;
R 3 , R 4 , R 5 , and R 7 are the same or different and each represent a hydrogen atom, a halogen atom, or an alkyl group;
R 8 represents a hydrogen atom or -(CH 2 ) l -(Y) m -(CH 2 ) n -Z wherein Y represents -CO-, -CONH-, or a triazole ring, Z represents a carboxyl group, a sulfonic acid group, or a -CO-peptide residue, 1 and n each represent an integer of 1 to 6, and m represents 0 or 1;
R 9 and R 10 are the same or different and each represent a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, an amino group, a nitro group, or a cyano group; and
R 8 and R 10 together optionally form an alkylene group.

摘要翻译： 本发明提供可用作淀粉样蛋白选择性体内适用的淀粉样蛋白增氧催化剂的化合物，不仅适用于Aβ肽，而且适用于其他淀粉状蛋白和含有该淀粉样蛋白相关疾病的预防和/或治疗用化合物的药物 。 公开了由下式（1）表示的硼 - 双联吡啶配合物，其中X 1和X 2相同或不同并且各自表示卤代烷基或卤素原子; R 1表示氢原子，烷基或由式（b）表示的基团：R 2和R 6相同或不同并且各自表示氢原子或卤素原子; R3，R4，R5和R7相同或不同，各自表示氢原子，卤素原子或烷基; R8代表氢原子或 - （CH2）l-（Y）m-（CH2）nZ，其中Y代表-CO - ， - CONH-或三唑环，Z代表羧基，磺酸基或 -CO-肽残基，1和n各自表示1至6的整数，并且m表示0或1; R9和R10相同或不同，分别表示氢原子，烷基，烷氧基，卤素原子，氨基，硝基或氰基。 并且R 8和R 10一起任选地形成亚烷基。