公开(公告)号：US09630940B2

公开(公告)日：2017-04-25

申请号：US15148716

申请日：2016-05-06

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Pandurang V. Chouthaiwale ,  Fujie Tanaka

IPC: C07D309/28 ,  C07D309/16 ,  C07C201/14 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07C205/55

CPC classification number: C07D309/28 ,  C07C201/14 ,  C07C205/55 ,  C07C2601/14 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04

Abstract: Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I: wherein R1 and R2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.

公开(公告)号：US20170217889A1

公开(公告)日：2017-08-03

申请号：US15509721

申请日：2015-09-09

Applicant: Okinawa Institute of Science and Technology School Corporation

Inventor： Pandurang Vilasrao Chouthaiwale ,  Fujie Tanaka

IPC: C07D213/79 ,  C07D405/04 ,  C07D213/803

CPC classification number: C07D213/79 ,  A61P35/00 ,  C07D213/803 ,  C07D405/04

Abstract: The present invention relates to novel 4-substituted pyridine-2,6-dicarboxylic acid derivatives, compounds of formula I, wherein R1 and R2 are defined herein. The compounds of formula I are useful for making pharmaceutical compositions to treat proliferative diseases. The present invention also relates to concise methods for preparing compounds of formula I that may be performed under mild reaction conditions.

公开(公告)号：US20150246927A1

公开(公告)日：2015-09-03

申请号：US14431935

申请日：2013-10-04

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Hai-Lei Cui ,  Fujie Tanaka

IPC: C07D491/107

CPC classification number: C07D491/107

Abstract: Disclosed is a compound of formula I: wherein R1?, R2?, R3?, R4?, R5?, n and m are defined herein. The compound of formula I is prepared by a concise, catalytic enantioselective formal hetero-Diels-Alder (hDA) reactions of enones with isatins and is useful for making pharmaceutical composition for the treatment of proliferative diseases.

Abstract translation: 公开了式I的化合物：其中R 1，R 2，R 3，R 4，R 5，n和m如本文所定义。 式I的化合物通过烯酮与异硬脂酸酯的简明的催化对映选择性形式的异二聚体 - 狄尔斯（hDA）反应制备，并且可用于制备用于治疗增殖性疾病的药物组合物。

公开(公告)号：US12116383B2

公开(公告)日：2024-10-15

申请号：US17841241

申请日：2022-06-15

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Fujie Tanaka ,  Sherida Johnson

IPC: C07H7/04 ,  C07H1/00

CPC classification number: C07H7/04 ,  C07H1/00

Abstract: The present invention provides a novel process for preparing an oligosaccharide C-glycoside derivative of formula I, comprising reacting a compound of formula II with compound of formula III in the presence of at least one primary or secondary amine and at least one additive [in the formulae, the substituents are as defined herein], and novel oligosaccharide C-glycoside derivatives that can be prepared using the process.

公开(公告)号：US09346780B2

公开(公告)日：2016-05-24

申请号：US14431945

申请日：2013-10-10

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Pandurang V. Chouthaiwale ,  Fujie Tanaka

IPC: A61K31/35 ,  C07D309/16 ,  C07D309/28 ,  C07D309/30 ,  C07D317/30 ,  C07C201/14 ,  C07D407/04 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07C205/55

CPC classification number: C07D309/28 ,  C07C201/14 ,  C07C205/55 ,  C07C2601/14 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04

Abstract: Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I: wherein R1 and R2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.

Abstract translation: 公开了制备式I的二氢-2H-吡喃衍生物的方法：其中R 1和R 2在本文中定义。 本发明的方法在简单的级联反应中和一锅中提供式I化合物。 通过本发明方法制备的式I化合物及其进一步转化的衍生物可用于制备用于治疗增殖性疾病的药物组合物。

公开(公告)号：US10988446B2

公开(公告)日：2021-04-27

申请号：US16321137

申请日：2016-09-28

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Fujie Tanaka ,  Feng Yin

IPC: C07D209/54 ,  C07D207/16 ,  C07C201/12 ,  C07C205/51

Abstract: The present invention relates to a process for preparing 3-pyrrolidine carboxylic acid derivatives, and particularly a simple process for preparing 5-substituted 3-pyrrolidine carboxylic acid derivatives. In addition, the present invention relates to a novel pyrrolidine carboxylic acid derivative, its manufacture, pharmaceutical compositions containing it and its use as a catalyst.

公开(公告)号：US10435383B2

公开(公告)日：2019-10-08

申请号：US15560858

申请日：2016-02-01

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Fujie Tanaka ,  Sherida Johnson

IPC: C07D307/22 ,  C07D309/14

Abstract: The present invention can provide novel C-glycoside derivatives which are biologically important under high stereoselective, mild, atom economical condition.

公开(公告)号：US10125074B2

公开(公告)日：2018-11-13

申请号：US15560868

申请日：2016-02-01

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Fujie Tanaka ,  Dongxin Zhang

IPC: C07C49/00 ,  C07C69/00 ,  C07C227/30 ,  C07C49/753 ,  C07C69/738 ,  C07D333/22 ,  C07D333/24 ,  C07C227/10 ,  C07C229/34 ,  C07C49/255 ,  C07C49/747 ,  C07C227/34 ,  C07C227/42 ,  A61K31/02 ,  A61K31/045

Abstract: The present invention relates to novel tertiary alcohol derivatives substituted with aryl and trifluoromethyl, and optical isomers thereof. In addition, the present invention also relates to methods for the preparation and use as enantiomer recognition agent thereof. The present invention provides pharmaceutical composition and use as therapeutically active substance thereof.

公开(公告)号：US09309261B2

公开(公告)日：2016-04-12

申请号：US14431935

申请日：2013-10-04

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Hai-Lei Cui ,  Fujie Tanaka

IPC: C07D491/107 ,  A61K31/407

CPC classification number: C07D491/107

Abstract: Disclosed is a compound of formula I: wherein R1?, R2?, R3?, R4?, R5?, n and m are defined herein. The compound of formula I is prepared by a concise, catalytic enantioselective formal hetero-Diels-Alder (hDA) reactions of enones with isatins and is useful for making pharmaceutical composition for the treatment of proliferative diseases.

Abstract translation: 公开了式I的化合物：其中R 1，R 2，R 3，R 4，R 5，n和m如本文所定义。 式I的化合物通过烯酮与异硬脂酸酯的简明的催化对映选择性形式的异二聚体 - 狄尔斯（hDA）反应制备，并且可用于制备用于治疗增殖性疾病的药物组合物。

公开(公告)号：US20150246896A1

公开(公告)日：2015-09-03

申请号：US14431945

申请日：2013-10-10

Applicant: OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

Inventor： Pandurang V. Chouthaiwale ,  Fujie Tanaka

IPC: C07D309/28 ,  C07D407/04 ,  C07D307/54 ,  C07D241/44 ,  C07D317/30 ,  C07C205/55 ,  C07D243/02

CPC classification number: C07D309/28 ,  C07C201/14 ,  C07C205/55 ,  C07C2601/14 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04

Abstract: Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I: wherein R1 and R2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.

Abstract translation: 公开了制备式I的二氢-2H-吡喃衍生物的方法：其中R 1和R 2在本文中定义。 本发明的方法在简单的级联反应中和一锅中提供式I化合物。 通过本发明方法制备的式I化合物及其进一步转化的衍生物可用于制备用于治疗增殖性疾病的药物组合物。