公开(公告)号：US20220055986A1

公开(公告)日：2022-02-24

申请号：US17521004

申请日：2021-11-08

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Toshihide WATANABE ,  Kensuke KUSUMI ,  Satomi IMAIDE ,  Toshimitsu ENDO ,  Takaki KOMIYA ,  Naomi TSUBURAYA

IPC: C07D205/04 ,  C07C49/252 ,  C07C49/577

Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

公开(公告)号：US20190030010A1

公开(公告)日：2019-01-31

申请号：US16148647

申请日：2018-10-01

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Atsushi NAGANAWA ,  Kensuke KUSUMI ,  Kazuhiro OTSUKI ,  Tetsuya SEKIGUCHI ,  Akito KAKUUCHI ,  Koji SHINOZAKI ,  Hiroshi YAMAMOTO ,  Shigeyuki NONAKA

IPC: A61K31/445 ,  A61K31/397 ,  A61K31/4545 ,  A61K31/40 ,  A61K31/4523 ,  A61K31/453 ,  C07D211/52 ,  C07D207/16 ,  C07D207/12 ,  C07D205/04 ,  C07D401/12 ,  C07D211/48 ,  C07D405/12 ,  A61K31/454

Abstract: The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

公开(公告)号：US20180042908A1

公开(公告)日：2018-02-15

申请号：US15784376

申请日：2017-10-16

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Atsushi NAGANAWA ,  Kensuke KUSUMI ,  Kazuhiro OTSUKI ,  Tetsuya SEKIGUCHI ,  Akito KAKUUCHI ,  Koji SHINOZAKI ,  Hiroshi YAMAMOTO ,  Shigeyuki NONAKA

IPC: A61K31/445 ,  A61K31/454 ,  A61K31/453 ,  A61K31/4523 ,  A61K31/40 ,  A61K31/397 ,  C07D401/12 ,  C07D207/12 ,  C07D211/52 ,  C07D207/16 ,  C07D211/48 ,  C07D205/04 ,  A61K31/4545 ,  C07D405/12

CPC classification number: A61K31/445 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4523 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D211/48 ,  C07D211/52 ,  C07D401/12 ,  C07D405/12

Abstract: The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

公开(公告)号：US20190031605A1

公开(公告)日：2019-01-31

申请号：US16073620

申请日：2017-01-27

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Toshihide WATANABE ,  Kensuke KUSUMI ,  Yuichi INAGAKI

IPC: C07D205/04 ,  C07D223/16 ,  C07D405/12 ,  C07D207/16 ,  C07C229/42 ,  C07C69/612 ,  C07C33/30 ,  C07C43/23 ,  C07C33/34 ,  C07C49/84 ,  C07C409/38 ,  C07D217/26 ,  C07D417/12 ,  C07D403/12

Abstract: A compound represented by general formula (I-1): wherein the symbols are defined in the specification, has a selective S1P5 receptor binding activity and modulates the function of an S1P5 receptor, and can therefore be a therapeutic agent for a S1P5-mediated disease, for example, neurodegenerative diseases such as schizophrenia, Binswanger's disease and the like.

公开(公告)号：US20160213660A1

公开(公告)日：2016-07-28

申请号：US15089690

申请日：2016-04-04

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Atsushi NAGANAWA ,  Kensuke KUSUMI ,  Kazuhiro OTSUKI ,  Tetsuya SEKIGUCHI ,  Akito KAKUUCHI ,  Koji SHINOZAKI ,  Hiroshi YAMAMOTO ,  Shigeyuki NONAKA

IPC: A61K31/445 ,  A61K31/453 ,  A61K31/40 ,  A61K31/454 ,  A61K31/397 ,  A61K31/4545 ,  A61K31/4523

CPC classification number: A61K31/445 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4523 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  C07D205/04 ,  C07D207/12 ,  C07D207/16 ,  C07D211/48 ,  C07D211/52 ,  C07D401/12 ,  C07D405/12

Abstract: The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Abstract translation: 式（I-1）的化合物：其中所有符号具有与说明书中所述相同的含义，具有两个环状基团，特别是特定取代位置的苯氧基，因此具有高的人S1P2拮抗活性。 因此，该化合物可用作S1P2介导的疾病如血管收缩，纤维化和呼吸系统疾病引起的疾病的治疗剂。

公开(公告)号：US20240327342A1

公开(公告)日：2024-10-03

申请号：US18744303

申请日：2024-06-14

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Toshihide WATANABE ,  Kensuke KUSUMI ,  Satomi IMAIDE ,  Toshimitsu ENDO ,  Takaki KOMIYA ,  Naomi TSUBURAYA

IPC: C07D205/04 ,  C07C49/252 ,  C07C49/577

CPC classification number: C07D205/04 ,  C07C49/252 ,  C07C49/577

Abstract: A compound represented by the general formula (V)




wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

公开(公告)号：US20210087141A1

公开(公告)日：2021-03-25

申请号：US16970865

申请日：2019-02-21

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Toshihide WATANABE ,  Kensuke KUSUMI ,  Satomi IMAIDE ,  Toshimitsu ENDO ,  Takaki KOMIYA ,  Naomi TSUBURAYA

IPC: C07D205/04 ,  C07C49/577 ,  C07C49/252

Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

公开(公告)号：US20230014137A1

公开(公告)日：2023-01-19

申请号：US17779260

申请日：2020-11-27

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Yuzo IWAKI ,  Toshimitsu ENDO ,  Kensuke KUSUMI

IPC: C07D207/22 ,  C07D207/34 ,  C07D471/04 ,  C07D495/04 ,  C07D209/70 ,  C07D409/12 ,  C07D417/04 ,  C07D405/04 ,  C07D513/04 ,  C07D487/04 ,  C07F9/572 ,  C07D403/04 ,  C07D413/04

Abstract: A pharmaceutical containing a compound having an agonist activity for LPA3 as an active ingredient, wherein the compound is of formula (IY): wherein all symbols represent the same meaning as described in the specification, and which is useful as a preventive and/or therapeutic agent for, e.g., essential thrombocythemia or reactive thrombocytosis.

公开(公告)号：US20170327439A1

公开(公告)日：2017-11-16

申请号：US15532389

申请日：2014-12-03

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Kensuke KUSUMI ,  Haruto KURATA ,  Atsushi NAGANAWA ,  Yasuyo KODERA ,  Yuichi INAGAKI ,  Hiroya TAKIZAWA ,  Mark Allan WOLF ,  Joseph RAKER

IPC: C07C13/48 ,  C07D205/04 ,  A61K31/397 ,  A61K31/19 ,  A61K31/015 ,  C07D401/10 ,  C07C13/20 ,  C07C2602/10

CPC classification number: C07C13/48 ,  A61K31/015 ,  A61K31/19 ,  A61K31/397 ,  C07C13/20 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/16 ,  C07D401/10 ,  C07D403/10

Abstract: A compound represented by general formula (I) (wherein, all the symbols are as defined in the specification) has a selective S1P5 receptor agonist activity due to having a linker from a phenyl group to a cyclic substituent in a dihydronaphthalene skeleton; .i.e., due to having a short linker of one atom or less as L in general formula (I), and can therefore serve as an agent for treating S1P5-mediated disease, e.g., neurodegenerative disease such as schizophrenia.

公开(公告)号：US20160039757A1

公开(公告)日：2016-02-11

申请号：US14780152

申请日：2014-03-25

Applicant: ONO PHARMACEUTICAL CO., LTD.

Inventor： Kensuke KUSUMI ,  Atsushi NAGANAWA ,  Kazuhiro OTSUKI ,  Tetsuya SEKIGUCHI ,  Koji SHINOZAKI ,  Hiroshi YAMAMOTO ,  Yasuko YAMAMOTO

IPC: C07D211/52 ,  C07D207/12

CPC classification number: C07D211/52 ,  C07D207/12 ,  C07D211/44 ,  C07D211/48

Abstract: An object of the present invention is to provide a compound having strong human S1P2 antagonistic activity in order to develop a useful medicament for therapy of a S1P2-mediated disease such as a disease resulting from vascular constriction, fibrosis and respiratory disease. The compound represented by the general formula (I), wherein all the symbols have the same meanings as described in the specification, has a halogen atom or a haloalkyl group and a phenoxy group at certain substitution sites, and thus has strong human S1P2 antagonistic activity. Therefore, the compound can be a therapeutic agent for a S1P2-mediated disease, such as a disease resulting from vascular constriction, fibrosis and respiratory disease.

Abstract translation: 本发明的目的是提供具有强人S1P2拮抗活性的化合物，以便开发用于治疗S1P2介导的疾病如由血管收缩，纤维化和呼吸系统疾病引起的疾病的有用药物。 由通式（I）表示的化合物，其中所有符号具有与说明书中所述相同的含义，在某些取代位置具有卤素原子或卤代烷基和苯氧基，因此具有强的人S1P2拮抗活性 。 因此，该化合物可以是S1P2介导的疾病的治疗剂，例如由血管收缩，纤维化和呼吸道疾病引起的疾病。