公开(公告)号：US20180044472A1

公开(公告)日：2018-02-15

申请号：US15727760

申请日：2017-10-09

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuhisa YAMANO ,  Toshiaki NAGATA ,  Hideki SAITOH

IPC: C08G69/48 ,  C08G69/10 ,  A61K39/39 ,  C08L77/04 ,  A61K47/34 ,  C08G69/08 ,  A61K39/00

CPC classification number: C08G69/48 ,  A61K39/39 ,  A61K47/34 ,  A61K47/42 ,  A61K2039/55555 ,  A61K2039/6093 ,  C08G69/08 ,  C08G69/10 ,  C08L77/04

Abstract: The present invention relates to a graft copolymer of a poly(amino acid) or a salt thereof and a hydrophobic primary amine compound or a salt thereof (e.g., a graft copolymer (γ-PGA-PAE) of poly(γ-glutamic acid) (γ-PGA) and phenylalanine ethyl ester (PAE)), an ionized graft copolymer of a poly(amino acid) or a salt thereof and a hydrophobic primary amine compound or a salt thereof, nanoparticles containing the ionized graft copolymer, and a production method thereof. The nanoparticles acquired in this way are useful as an adjuvant for producing a vaccine.

公开(公告)号：US20140303378A1

公开(公告)日：2014-10-09

申请号：US14303238

申请日：2014-06-12

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tomomi IKEMOTO ,  Hideya MIZUFUNE ,  Toshiaki NAGATA ,  Misayo SERA ,  Naohiro FUKUDA ,  Takeshi YAMASAKI

IPC: C07D207/337 ,  C07D207/36 ,  C07D207/30 ,  C07D207/48 ,  C07C225/14 ,  C07D207/333 ,  C07D401/12

CPC classification number: C07D207/337 ,  C07D207/30 ,  C07D207/333 ,  C07D207/34 ,  C07D207/36 ,  C07D207/48 ,  C07D401/12

Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Abstract translation: 本发明提供了可用作药物的磺酰基吡咯化合物的制备方法，用于该方法的中间体的制备方法和新的中间体。 本发明涉及一种制备磺酰基吡咯化合物（Ⅷ）的方法，其包括还原化合物（III）并水解还原产物得到化合物（Ⅳ），使化合物（Ⅳ）进行磺酰化反应得到化合物（Ⅵ）， 并使化合物（VI）进行胺化反应。

公开(公告)号：US20160177032A1

公开(公告)日：2016-06-23

申请号：US14392185

申请日：2014-06-25

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuhisa YAMANO ,  Toshiaki NAGATA ,  Hideki SAITOH

IPC: C08G69/48 ,  A61K39/39

CPC classification number: C08G69/48 ,  A61K39/39 ,  A61K47/34 ,  A61K2039/55555 ,  A61K2039/6093 ,  C08G69/08 ,  C08G69/10 ,  C08L77/04

Abstract: The present invention relates to a graft copolymer of a poly(amino acid) or a salt thereof and a hydrophobic primary amine compound or a salt thereof (e.g., a graft copolymer (γ-PGA-PAE) of poly(γ-glutamic acid) (γ-PGA) and phenylalanine ethyl ester (PAE)), an ionized graft copolymer of a poly(amino acid) or a salt thereof and a hydrophobic primary amine compound or a salt thereof, nanoparticles containing the ionized graft copolymer, and a production method thereof. The nanoparticles acquired in this way are useful as an adjuvant for producing a vaccine.

Abstract translation: 本发明涉及聚（氨基酸）或其盐与疏水性伯胺化合物或其盐的接枝共聚物（例如聚（γ-谷氨酸）的接枝共聚物（γ-PGA-PAE） （γ-PGA）和苯丙氨酸乙酯（PAE）），聚（氨基酸）或其盐和疏水性伯胺化合物或其盐的电离接枝共聚物，含有电离接枝共聚物的纳米粒子，以及生产 方法。 以这种方式获得的纳米颗粒可用作生产疫苗的佐剂。

公开(公告)号：US20190135852A1

公开(公告)日：2019-05-09

申请号：US16240677

申请日：2019-01-04

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuru NONOGAWA ,  Toshiaki NAGATA ,  Hideki SAITO ,  Tsuneo YASUMA

IPC: C07H19/207 ,  C07H19/073 ,  C07H19/167 ,  C07H1/00 ,  C07H19/06 ,  C07H21/04 ,  C07H19/067 ,  C07H19/16 ,  C07H21/00

Abstract: In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 and n are each as defined in Claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.