公开(公告)号：US20210206716A1

公开(公告)日：2021-07-08

申请号：US17210215

申请日：2021-03-23

Applicant: Daiichi Sankyo Company, Limited

Inventor： Tsuyoshi Soneda ,  Yuji Nakamura ,  Koji Matsumoto ,  Naomi Tanaka ,  Taichi Fukunaga

IPC: C07C275/42 ,  C07C323/44 ,  C07D207/10 ,  C07D211/06 ,  C07D333/36

Abstract: An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: wherein R1 and R2 are the same or different, and represent a C1-C6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.

公开(公告)号：US20220144765A1

公开(公告)日：2022-05-12

申请号：US17585381

申请日：2022-01-26

Applicant: Daiichi Sankyo Company, Limited

Inventor： Tsuyoshi Soneda ,  Yuji Nakamura ,  Koji Matsumoto ,  Naomi Tanaka ,  Taichi Fukunaga

IPC: C07C275/42 ,  C07C323/44 ,  C07D207/10 ,  C07D211/06 ,  C07D333/36

Abstract: An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: wherein R1 and R2 are the same or different, and represent a C1-C6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.

公开(公告)号：US20180327399A1

公开(公告)日：2018-11-15

申请号：US15764264

申请日：2016-09-28

Applicant: Daiichi Sankyo Company, Limited

Inventor： Manoj Kumar Khera ,  Tarun Mathur ,  Jitendra A. Sattigeri ,  Nobuhisa Masuda ,  Tsuyoshi Soneda ,  Yoshiko Kagoshima ,  Toshiyuki Konosu ,  Tetsuya Suzuki ,  Makoto Yamaoka ,  Ryo Itooka

IPC: C07D417/14 ,  A61P31/04

CPC classification number: C07D417/14 ,  A61P31/04

Abstract: Problem to be Solved There is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use.Solution to the Problem As a result of intensive research, the present inventors have found that a compound represented by general formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof inhibits DNA gyrase GyrB subunit and/or topoisomerase IV ParE subunit possesses excellent solubility and a safety profile for use in humans for the treatment of bacterial infectious diseases.

公开(公告)号：US10399968B2

公开(公告)日：2019-09-03

申请号：US15764264

申请日：2016-09-28

Applicant: Daiichi Sankyo Company, Limited

Inventor： Manoj Kumar Khera ,  Tarun Mathur ,  Jitendra A. Sattigeri ,  Nobuhisa Masuda ,  Tsuyoshi Soneda ,  Yoshiko Kagoshima ,  Toshiyuki Konosu ,  Tetsuya Suzuki ,  Makoto Yamaoka ,  Ryo Itooka

IPC: C07D417/14 ,  A61P31/04

Abstract: Problem to be SolvedThere is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use.Solution to the ProblemAs a result of intensive research, the present inventors have found that a compound represented by general formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof inhibits DNA gyrase GyrB subunit and/or topoisomerase IV ParE subunit possesses excellent solubility and a safety profile for use in humans for the treatment of bacterial infectious diseases.

公开(公告)号：US08927588B2

公开(公告)日：2015-01-06

申请号：US14027077

申请日：2013-09-13

Applicant: Daiichi Sankyo Company, Limited

Inventor： Tsuyoshi Soneda ,  Hiroshi Takeshita ,  Yoshiko Kagoshima ,  Yuko Yamamoto ,  Takafumi Hosokawa ,  Toshiyuki Konosu ,  Nobuhisa Masuda ,  Takuya Uchida ,  Issei Achiwa ,  Junichi Kuroyanagi ,  Tetsunori Fujisawa ,  Aki Yokomizo ,  Tetsuji Noguchi

IPC: C07D233/90 ,  C07D413/14 ,  C07D495/16 ,  C07D487/04 ,  C07D233/66 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/06 ,  C07D487/12 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D233/66 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/06 ,  C07D487/12 ,  C07D495/04 ,  C07D495/16 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.

Abstract translation: 为了开发具有新的作用机制的抗生素，本发明人已经搜索到具有弱的细胞毒性，在水中的高溶解度的物理性质，抑制DNA促旋酶GyrB和拓扑异构酶IV ParE亚基的效果以及足够的抗细菌 活动。 结果，本发明人通过发现由通式（1）表示的本发明的化合物，其药理学可接受的盐及其前药具有期望的性质而完成了本发明。 本发明提供包含式（1）表示的化合物，其药理学可接受的盐或其前药作为活性成分的药物组合物（特别是感染性疾病的预防或治疗组合物）。

公开(公告)号：US11981686B2

公开(公告)日：2024-05-14

申请号：US17425520

申请日：2020-01-23

Applicant: DAIICHI SANKYO COMPANY, LIMITED

Inventor： Junya Kawai ,  Osamu Iwamoto ,  Yuma Umezaki ,  Katsuyoshi Nakajima ,  Hiroyuki Tsuruoka ,  Keiji Saito ,  Nobuya Kurikawa ,  Natsumi Nishihama ,  Shinji Tanaka ,  Momoko Ogitani ,  Tomohiro Honda ,  Wataru Saitoh ,  Tsuyoshi Soneda ,  Nobuyuki Ohkawa

IPC: C07D513/18 ,  C07D513/04

CPC classification number: C07D513/18 ,  C07D513/04

Abstract: An object of the present invention is to provide a compound that has a specific chemical structure having an activation effect on SIRT6 and is useful as an active component for preventing and treating inflammatory diseases, and the present invention relates to a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof,






where each symbol in Formula (1) has the same definition as that described in the specification.

公开(公告)号：US08975263B2

公开(公告)日：2015-03-10

申请号：US14291860

申请日：2014-05-30

Applicant: Daiichi Sankyo Company, Limited

Inventor： Shigeo Yamanoi ,  Katsuji Kagechika ,  Tsuyoshi Soneda ,  Yuichi Ochiai ,  Hidenori Namiki ,  Fuminao Doi ,  Madoka Hoshino ,  Shoko Yoshida

IPC: C07D405/10 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D405/10 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent glucose lowering effect.A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C1-C3 alkyl group, each substituent R2 may be the same or different and may each represent a C1-C3 alkyl group, R3 represents an optionally substituted pyridyl group or the like, R4 and R5, which are the same or different, each represent a C1-C3 alkyl group, R6 and R7, which are the same or different, each represent a C1-C3 alkyl group, and n represents 0 to 3.

Abstract translation: 本发明涉及具有优异葡萄糖降低作用的化合物或其药理学上可接受的盐。 由以下通式（I）表示的化合物或其药学上可接受的盐：其中R1表示C1-C3烷基，各取代基R2可以相同或不同，可各自表示C1-C3烷基，R3表示 任选取代的吡啶基等，R 4和R 5相同或不同，各自表示C1-C3烷基，R6和R7相同或不同，分别表示C1-C3烷基，和 n表示0〜3。

公开(公告)号：US20140073622A1

公开(公告)日：2014-03-13

申请号：US14027077

申请日：2013-09-13

Applicant: Daiichi Sankyo Company, Limited

Inventor： Tsuyoshi Soneda ,  Hiroshi Takeshita ,  Yoshiko Kagoshima ,  Yuko Yamamoto ,  Takafumi Hosokawa ,  Toshiyuki Konosu ,  Nobuhisa Masuda ,  Takuya Uchida ,  Issei Achiwa ,  Junichi Kuroyanagi ,  Tetsunori Fujisawa ,  Aki Yokomizo ,  Tetsuji Noguchi

IPC: C07D513/04 ,  C07D401/12 ,  C07D417/12 ,  C07D403/12 ,  C07D495/16 ,  C07D233/90 ,  C07D413/14 ,  C07D401/14 ,  C07D487/04 ,  C07D417/14 ,  C07D413/12

CPC classification number: C07D487/04 ,  C07D233/66 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/06 ,  C07D487/12 ,  C07D495/04 ,  C07D495/16 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.

Abstract translation: 为了开发具有新的作用机制的抗生素，本发明人已经搜索到具有弱的细胞毒性，在水中的高溶解度的物理性质，抑制DNA促旋酶GyrB和拓扑异构酶IV ParE亚基的效果以及足够的抗细菌 活动。 结果，本发明人通过发现由通式（1）表示的本发明的化合物，其药理学可接受的盐及其前药具有期望的性质而完成了本发明。 本发明提供包含式（1）表示的化合物，其药理学可接受的盐或其前药作为活性成分的药物组合物（特别是感染性疾病的预防或治疗组合物）。

公开(公告)号：US10968169B2

公开(公告)日：2021-04-06

申请号：US16339305

申请日：2017-10-05

Applicant: Daiichi Sankyo Company, Limited

Inventor： Tsuyoshi Soneda ,  Yuji Nakamura ,  Koji Matsumoto ,  Naomi Tanaka ,  Taichi Fukunaga

IPC: C07C275/42 ,  C07C323/44 ,  C07D207/10 ,  C07D211/06 ,  C07D333/36

Abstract: An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect, and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: wherein R1 and R2 are the same or different, and represent a C1-C6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.

公开(公告)号：US10925848B2

公开(公告)日：2021-02-23

申请号：US16487401

申请日：2018-02-20

Applicant: Daiichi Sankyo Company, Limited

Inventor： Tsuyoshi Soneda ,  Hiroki Sakai ,  Koji Matsumoto ,  Naomi Tanaka ,  Taichi Fukunaga

IPC: A61P43/00 ,  A61P13/12 ,  A61K31/198 ,  A61K31/277 ,  C07C237/36 ,  C07C237/44

Abstract: An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect, and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. Provided is a pharmaceutical composition containing, as an active ingredient, a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula (I), R1 and R2 are the same or different, and represent a C1-C6 alkyl group, a halogeno C1-C6 alkyl group or a C3-C6 cycloalkyl group; n represents 0, 1 or 2; each X represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a halogen atom or the like; and Y represents a hydrogen atom, a C1-C6 alkoxy group, a C3-C6 cycloalkoxy group or a halogeno C1-C6 alkoxy group.