公开(公告)号：US20240182445A1

公开(公告)日：2024-06-06

申请号：US17769293

申请日：2020-10-23

Applicant: ONO PHARMACEUTICAL CO., LTD. ,  VANDERBILT UNIVERSITY

Inventor： Craig W LINDSLEY ,  Darren W ENGERS ,  Elizabeth S CHILDRESS ,  Sean R BOLLINGER ,  Joza SCHMITT ,  Aaron T GARRISON ,  Charles K PERRY ,  Jerod S DENTON ,  Motoyuki TANAKA

IPC: C07D401/14 ,  A61P25/28 ,  C07D401/12 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D401/14 ,  A61P25/28 ,  C07D401/12 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D471/04

Abstract: Disclosed is a compound of formula (I): in which all symbols are defined in the description. Also disclosed are pharmaceutical compositions including the compounds, methods of making the compounds, kits comprising the compounds and methods of using the compounds to prevent and/or treat disorders associated with dysregulation of TREK-1, TREK-2 or both TREK-1 and TREK-2 in a mammal.

公开(公告)号：US20240190824A1

公开(公告)日：2024-06-13

申请号：US17769300

申请日：2020-10-23

Applicant: ONO PHARMACEUTICAL CO., LTD. ,  VANDERBILT UNIVERSITY

Inventor： Craig W LINDSLEY ,  Darren W ENGERS ,  Elizabeth S CHILDRESS ,  Sean R BOLLINGER ,  Joza SCHMITT ,  Trevor C CHOPKO ,  Jerod S DENTON ,  Motoyuki TANAKA ,  Haruto KURATA

IPC: C07D213/75 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/12

CPC classification number: C07D213/75 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/12

Abstract: Disclosed is a compound of formula (I): in which all symbols are defined in the description. Also disclosed are pharmaceutical compositions including the compounds, methods of making the compounds, kits comprising the compounds and methods of using the compounds to treat disorders associated with dysregulation of TREK-1, TREK-2 or both TREK-1 and TREK-2 in a mammal.

公开(公告)号：US20180334458A1

公开(公告)日：2018-11-22

申请号：US16050266

申请日：2018-07-31

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Motoyuki TANAKA ,  Takashi KONDO ,  Yasuo HIROOKA ,  Taihei NISHIYAMA ,  Atsushi HIRAMATSU ,  Tomoyuki KODA ,  Sho KOUYAMA

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61P43/00 ,  A61K9/20 ,  A61K31/444

CPC classification number: C07D471/04 ,  A61K9/20 ,  A61K31/444 ,  A61K31/519 ,  A61P43/00 ,  C07D487/04

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

公开(公告)号：US20200140435A1

公开(公告)日：2020-05-07

申请号：US16720486

申请日：2019-12-19

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Motoyuki TANAKA ,  Takashi KONDO ,  Yasuo HIROOKA ,  Taihei NISHIYAMA ,  Atsushi HIRAMATSU ,  Tomoyuki KODA ,  Sho KOUYAMA

IPC: C07D471/04 ,  A61K31/444 ,  A61K9/20 ,  A61K31/519 ,  C07D487/04 ,  A61P43/00 ,  C07D401/14

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

公开(公告)号：US20190352304A1

公开(公告)日：2019-11-21

申请号：US16527489

申请日：2019-07-31

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Motoyuki TANAKA ,  Takashi KONDO ,  Yasuo HIROOKA ,  Taihei NISHIYAMA ,  Atsushi HIRAMATSU ,  Tomoyuki KODA ,  Sho KOUYAMA

IPC: C07D471/04 ,  A61P43/00 ,  C07D487/04 ,  A61K31/444 ,  A61K9/20 ,  A61K31/519

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

公开(公告)号：US20140072576A1

公开(公告)日：2014-03-13

申请号：US14075538

申请日：2013-11-08

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Masaya KOKUBO ,  Motoyuki TANAKA ,  Hiroshi OCHIAI ,  Yoshikazu TAKAOKA ,  Shiro SHIBAYAMA

IPC: A61K31/695 ,  C07D233/64 ,  A61K45/06 ,  C07D471/10 ,  A61K31/435 ,  A61K31/5377 ,  C07F7/18 ,  A61K31/4178

CPC classification number: A61K31/695 ,  A61K31/4178 ,  A61K31/435 ,  A61K31/5377 ,  A61K45/06 ,  C07D233/64 ,  C07D471/10 ,  C07F7/1804

Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.

Abstract translation: 本发明涉及由式（I）表示的化合物：其中所有符号如本文所定义，其盐，其溶剂化物或其前药。 本发明的化合物对CXCR4具有拮抗作用，因此可用作CXCR4介导的疾病的预防和/或治疗剂，例如炎性和免疫疾病（例如类风湿性关节炎，关节炎，视网膜病变，肺纤维化 ，移植器官的排斥等），过敏性疾病，感染（例如，人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心血管疾病，代谢疾病和癌性疾病（例如， 癌症，癌症转移等）或再生治疗剂。

公开(公告)号：US20230138003A1

公开(公告)日：2023-05-04

申请号：US18088045

申请日：2022-12-23

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Motoyuki TANAKA ,  Takashi KONDO ,  Yasuo HIROOKA ,  Taihei NISHIYAMA ,  Atsushi HIRAMATSU ,  Tomoyuki KODA ,  Sho KOUYAMA

IPC: C07D471/04 ,  A61K31/444 ,  A61P43/00 ,  C07D401/14 ,  A61K9/20 ,  A61K31/519 ,  C07D487/04

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

公开(公告)号：US20210009586A1

公开(公告)日：2021-01-14

申请号：US17027922

申请日：2020-09-22

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Motoyuki TANAKA ,  Takashi KONDO ,  Yasuo HIROOKA ,  Taihei NISHIYAMA ,  Atsushi HIRAMATSU ,  Tomoyuki KODA ,  Sho KOUYAMA

IPC: C07D471/04 ,  A61K31/444 ,  A61P43/00 ,  C07D401/14 ,  A61K9/20 ,  A61K31/519 ,  C07D487/04

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.

公开(公告)号：US20170349580A1

公开(公告)日：2017-12-07

申请号：US15534247

申请日：2015-12-09

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Motoyuki TANAKA ,  Takashi KONDO ,  Yasuo HIROOKA ,  Taihei NISHIYAMA ,  Atsushi HIRAMATSU ,  Tomoyuki KODA ,  Sho KOUYAMA

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/444 ,  C07D487/04 ,  A61K9/20

CPC classification number: C07D471/04 ,  A61K9/20 ,  A61K31/444 ,  A61K31/519 ,  A61P43/00 ,  C07D487/04

Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.