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21.发明申请公开(公告)号：US20200000816A1
公开(公告)日：2020-01-02
申请号：US16484399
申请日：2018-02-07
IPC分类号： A61K31/5377 , A61K31/4545 , C07D401/14 , C07D405/14 , C07D413/14 , A61K47/38 , A61K47/12 , A61K47/02
摘要： A somatostatin receptor subtype 2 agonist represented by the general formula (I): wherein all symbols have the same meanings as described in the specification, or a salt thereof, which can be easily administered and can alleviate pain accompanied by the therapy of patients.
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公开(公告)号：US20190307761A1
公开(公告)日：2019-10-10
申请号：US16339201
申请日：2018-06-29
IPC分类号： A61K31/5377 , A61K31/216 , A61K45/06 , A61P35/04
摘要： The inventors found that postsurgical recurrence and/or metastasis of cancer is suppressed by administering a beta-blocker to a cancer patient during a perioperative period of cancer surgery. Accordingly, the disclosure provides an agent for suppressing recurrence and/or metastasis of cancer, comprising a beta-blocker and being administered during a perioperative period of cancer surgery.
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公开(公告)号：US20190135785A1
公开(公告)日：2019-05-09
申请号：US16237275
申请日：2018-12-31
发明人： Takayuki Inukai , Jun Takeuchi , Tomoko Yasuhiro
IPC分类号： C07D401/14 , C07D215/54 , C07D401/12
摘要： A compound represented by general formula (I) has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases
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24.发明申请公开(公告)号：US20190099413A1
公开(公告)日：2019-04-04
申请号：US16079823
申请日：2017-02-24
发明人： Kohei TANAKA , Tomoko YASUHIRO
IPC分类号： A61K31/4709 , A61K31/519 , A61P35/00 , C07K16/28
摘要： A drug for cancer therapy characterized in that an Axl inhibitor and an immune checkpoint inhibitor (for example, an anti-PD-1 antibody) are administered in combination, wherein the Axl inhibitor is a compound represented by the general formula (I): (wherein in the formula, all of the symbols have the same meanings as defined in the specification), a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, and the combination exhibits a strong anti-tumor effect and, therefore, is useful for cancer therapy.
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公开(公告)号：US20190054091A1
公开(公告)日：2019-02-21
申请号：US16167835
申请日：2018-10-23
发明人： Toshio YOSHIZAWA , Ryohei KOZAKI
IPC分类号： A61K31/522 , A61K45/06 , C07D473/34
CPC分类号： A61K31/522 , A61K45/06 , A61P35/00 , C07D473/34
摘要： To provide a medicament which shows more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-CLBCL) than the existing Btk inhibitor, and is excellent in safety. The present compound exhibits more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-DLBCL) patients, inter alia, ABC-DLBCL patients having CD79B wild-type gene background than the existing Btk inhibitor, and therefore, it can attain the object of the present invention.
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公开(公告)号：US10201520B2
公开(公告)日：2019-02-12
申请号：US15852493
申请日：2017-12-22
发明人： Tohru Kambe , Toru Maruyama , Shinsaku Yamane , Satoshi Nakayama , Kousuke Tani
IPC分类号： A61K31/335 , A61K31/4427 , A61K31/558 , C07D313/06 , C07D401/06 , C07D417/04 , C07D407/12 , C07D405/06 , A61K9/00
摘要： Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
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公开(公告)号：US20190031605A1
公开(公告)日：2019-01-31
申请号：US16073620
申请日：2017-01-27
IPC分类号： 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
摘要： 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.
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公开(公告)号：US20180346422A1
公开(公告)日：2018-12-06
申请号：US16059270
申请日：2018-08-09
IPC分类号： C07D213/61 , C07D307/52 , A61K31/17 , C07D213/40 , C07D209/30 , C07D277/28 , C07D271/06 , C07C233/29 , C07C233/26 , C07D241/12 , C07D413/06 , C07D239/26 , C07D233/64 , C07D333/28 , C07D333/20 , C07C275/40 , C07C275/32 , C07D309/04 , C07D213/74 , A61K31/505 , A61K31/4965 , A61K31/4545 , A61K31/435 , A61K31/426 , A61K31/4245 , A61K31/422 , A61K31/417 , A61K31/4045 , A61K31/381 , A61K31/351 , A61K31/341
摘要： The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.
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公开(公告)号：US10137129B2
公开(公告)日：2018-11-27
申请号：US15208998
申请日：2016-07-13
发明人： Toshio Yoshizawa , Ryohei Kozaki
IPC分类号： C07D473/34 , A61K31/522 , A61K45/06
摘要： To provide a medicament which shows more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-CLBCL) than the existing Btk inhibitor, and is excellent in safety. The present compound exhibits more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-DLBCL) patients, inter alia, ABC-DLBCL patients having CD79B wild-type gene background than the existing Btk inhibitor, and therefore, it can attain the object of the present invention.
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公开(公告)号：US20180334458A1
公开(公告)日：2018-11-22
申请号：US16050266
申请日：2018-07-31
发明人： Motoyuki TANAKA , Takashi KONDO , Yasuo HIROOKA , Taihei NISHIYAMA , Atsushi HIRAMATSU , Tomoyuki KODA , Sho KOUYAMA
IPC分类号： C07D471/04 , C07D487/04 , A61K31/519 , A61P43/00 , A61K9/20 , A61K31/444
CPC分类号： C07D471/04 , A61K9/20 , A61K31/444 , A61K31/519 , A61P43/00 , C07D487/04
摘要： 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.
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