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1. 发明申请

WO2021240383A1 TABLET COMPRISING OPICAPONE 审中-公开
公开(公告)号：WO2021240383A1
公开(公告)日：2021-12-02
申请号：PCT/IB2021/054574
申请日：2021-05-26
申请人： ONO PHARMACEUTICAL CO., LTD. , BIAL - PORTELA & CA, S.A.
发明人： TANIGUCHI, Koji , SEKIYA, Noboru , VASCONCELOS, Teófilo Cardoso de , LIMA, Ricardo Jorge dos santos
IPC分类号： A61K9/14 , A61K9/20
摘要： The present invention provides a tablet comprising opicapone or a pharmaceutically acceptable salt thereof, having reduced tableting faults during manufacture. It further relates to a tablet comprising opicapone or a pharmaceutically acceptable salt thereof, wherein the tablet comprises particles of opicapone or pharmaceutically acceptable salt thereof having the following particle size, and a manufacturing method thereof:(i) a maximum length D50 value of 45 μm or less, and/or (ii) a maximum length D90 value of 110 μm or less

2. 发明申请

WO2021080015A1 MODULATORS OF TREK (TWIK RELATED K+ CHANNELS) CHANNEL FUNCTION 审中-公开
公开(公告)号：WO2021080015A1
公开(公告)日：2021-04-29
申请号：PCT/JP2020/040001
申请日：2020-10-23
申请人： ONO PHARMACEUTICAL CO., LTD. , VANDERBILT UNIVERSITY
发明人： LINDSLEY, Craig W , ENGERS, Darren W , CHILDRESS, Elizabeth S , BOLLINGER, Sean R , SCHMITT, Joza , GARRISON, Aaron T , PERRY, Charles K , DENTON, Jerod S , TANAKA, Motoyuki
IPC分类号： C07D309/34 , C07D333/10 , C07D307/02 , C07D231/02 , C07D231/56 , A61K31/415 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/55
摘要： Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising 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.

3. 发明申请

WO2021043245A1 HYDANTOIN DERIVATIVE 审中-公开
公开(公告)号：WO2021043245A1
公开(公告)日：2021-03-11
申请号：PCT/CN2020/113408
申请日：2020-09-04
申请人： ONO PHARMACEUTICAL CO., LTD. , PHARMARON BEIJING CO., LTD. (CHINA)
发明人： NISHIOKA, Yota , KURONO, Masakuni , NISHIZAWA, Rena , BANDODKAR, Balachandra , GAO, Xuechao , WAN, Zhilong , LV, Ranran , DOYLE, Kevin , GOLDSMITH, Michael
IPC分类号： C07D401/14 , C07D401/12 , A61K31/4164 , A61P9/00 , A61P25/00 , A61P35/00
摘要： A compound represented by general formula (I-a) : has a strong DDR1 inhibitory activity, and can be a therapeutic agent for DDR1-related diseases, for example, a cancer, a kidney disease, a cardiovascular disease, a central nervous system disease, or fibrosis.

4. 发明申请

WO2021010492A1 COMPOUND HAVING KDM5 INHIBITORY ACTIVITY AND PHARMACEUTICAL USE THEREOF 审中-公开
公开(公告)号：WO2021010492A1
公开(公告)日：2021-01-21
申请号：PCT/JP2020/028771
申请日：2020-07-16
申请人： ONO PHARMACEUTICAL CO., LTD.
发明人： KAKUUCHI, Akito , UMEMURA, Shuhei , SVENSSON, Mats , RAVINSKY, Anatoly , INOYAMA, Daigo , KRILOV, Goran , TAKAHASHI, Hidenori , KONZE, Kyle , VERRAS, Andreas , CRUMPLER, Simon , VALLADE, Maelle , MACLEOD, Calum , SANDERSON, James N. , BULL, Richard J. , GAINES, Simon
IPC分类号： A61P25/28 , A61P35/00 , A61P43/00 , C07D261/08 , C07D471/04 , C07D487/04 , C07D487/10 , C07D498/10 , C07D231/06 , A61K31/415 , A61K31/4178 , A61K31/422 , A61K31/424 , A61K31/5025 , A61K31/519 , A61K31/53
摘要： The present invention provides KDM5 inhibitor. The compound disclosed herein represented by the general formula (Z): wherein all symbols have the same meanings as the definitions described in the specification; or a salt thereof is useful as a prophylactic and/or therapeutic agent for cancer, Huntington's disease, or Alzheimer's disease and the like.

5. 发明申请

WO2017059224A2 COMBINATION OF A BTK INHIBITOR AND A CHECKPOINT INHIBITOR FOR TREATING CANCERS 审中-公开
标题翻译： BTK抑制剂和检查点抑制剂治疗癌症的组合
公开(公告)号：WO2017059224A2
公开(公告)日：2017-04-06
申请号：PCT/US2016/054731
申请日：2016-09-30
申请人： GILEAD SCIENCES, INC. , ONO PHARMACEUTICAL CO., LTD.
发明人： VENKATARAMAN, Sriram , TUMAS, Daniel , TANAKA, Kohei , YASUHIRO, Tomoko , YOSHIZAWA, Toshio
IPC分类号： A61K31/122 , A61K31/351 , A61K31/4748 , A61K31/522 , A61K31/675
CPC分类号： A61K31/522 , A61K31/122 , A61K31/351 , A61K31/4748 , A61K31/675 , A61K2300/00
摘要： Provided herein are methods relating to a therapeutic strategy for treatment of cancer, including hematological malignancies. In particular, the methods include administration of a Btk inhibitor and a checkpoint inhibitor, including combinations in which the Btk inhibitor is 6-amino-9-[(3R)-I-(2-butynoyl)-3- pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, or a pharmaceutically acceptable salt thereof, and the checkpoint inhibitor is selected from inhibitors of PD-1, PD-L1, and CTLA-4.
摘要翻译：本文提供了涉及用于治疗癌症的治疗策略（包括血液恶性肿瘤）的方法。特别地，所述方法包括施用Btk抑制剂和检查点抑制剂，包括其中Btk抑制剂是6-氨基-9 - [（3R）-1-（2-丁炔酰基）-3-吡咯烷基] -7- （4-苯氧基苯基）-7,9-二氢-8H-嘌呤-8-酮或其药学上可接受的盐，检查点抑制剂选自PD-1，PD-L1和CTLA-4的抑制剂。

6. 发明申请

WO2015146159A1 PROPHYLACTIC AGENT AND/OR THERAPEUTIC AGENT FOR DIFFUSE LARGE B-CELL LYMPHOMA 审中-公开
标题翻译：用于免疫大B细胞淋巴瘤的预防剂和/或治疗剂
公开(公告)号：WO2015146159A1
公开(公告)日：2015-10-01
申请号：PCT/JP2015/001676
申请日：2015-03-24
申请人： ONO PHARMACEUTICAL CO., LTD.
发明人： YOSHIZAWA, Toshio , KOZAKI, Ryohei
IPC分类号： A61K31/52 , A61K35/12 , A61K39/395 , A61K45/00 , A61P35/02 , A61P43/00
CPC分类号： A61K31/522 , A61K45/06 , 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.
摘要翻译：提供一种比现有的Btk抑制剂治疗活化的B细胞如弥漫性大B细胞淋巴瘤（ABC-CLBCL）更显着效果的药物，其安全性优异。本发明化合物在治疗活化的B细胞如弥漫性大B细胞淋巴瘤（ABC-DLBCL）患者尤其是具有比现有Btk抑制剂具有CD79B野生型基因背景的ABC-DLBCL患者更显着的效果，因此，可以实现本发明的目的。

7. 发明申请

WO2015067586A2 COMBINATION THERAPY OF AN ANTI CD20 ANTIBODY WITH A BTK INHIBITOR 审中-公开
标题翻译：抗CD20抗体与BTK抑制剂的组合治疗
公开(公告)号：WO2015067586A2
公开(公告)日：2015-05-14
申请号：PCT/EP2014/073640
申请日：2014-11-04
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC. , ONO PHARMACEUTICAL CO., LTD.
发明人： KLEIN, Christian , TOSHIO, Yoshizawa , TOMOKO, Yasuhiro
IPC分类号： C07K16/28
CPC分类号： A61K39/39558 , A61K31/522 , A61K45/06 , A61K2039/505 , C07K16/2887 , C07K2317/24 , A61K2300/00
摘要： The present invention is directed to the combination therapy of an anti-CD20 antibody with a BTK inhibitor for the treatment of cancer, especially to the combination therapy of CD20 expressing cancers with a type I anti-CD20 antibody or an afucosylated humanized B-Lyl antibody and a BTK inhibitor.
摘要翻译：本发明涉及抗CD20抗体与用于治疗癌症的BTK抑制剂的组合疗法，特别是与I型抗CD20抗体或非岩藻糖化的人源化B-Lyl抗体的CD20表达癌症的组合疗法和BTK抑制剂。

8. 发明申请

WO2010001617A1 USE OF AN EFFICACY MARKER FOR OPTIMIZING THERAPEUTIC EFFICACY OF AN ANTI-HUMAN PD-1 ANTIBODY ON CANCERS 审中-公开
标题翻译：使用有效标记来优化抗人PD-1抗体对癌症的治疗效果
公开(公告)号：WO2010001617A1
公开(公告)日：2010-01-07
申请号：PCT/JP2009/003093
申请日：2009-07-03
申请人： ONO PHARMACEUTICAL CO., LTD. , MEDAREX, INC. , SHIBAYAMA, Shiro , YOSHIDA, Takao , HAYASHI, Tamon , HAYASHI, Akio , MURAI, Jun
发明人： SHIBAYAMA, Shiro , YOSHIDA, Takao , HAYASHI, Tamon , HAYASHI, Akio , MURAI, Jun
IPC分类号： A61K39/395 , A61P35/00 , A61P35/02 , G01N33/53
CPC分类号： C07K16/2818 , A61K2039/505 , G01N2800/52
摘要： A purpose of the present invention is to provide a method capable of more effectively prescribing an anti-human PD-1 antibody for anti-cancer therapy, a method for estimating or optimizing therapeutic efficacy thereof, and further an efficacy marker that can be used in methods thereof. The present invention enables selection of the cancer patient in whom the therapeutic efficacy of the anti-human PD-1 antibody can be expected in future, by measuring the change which is more than a certain level of several kinds of efficacy markers in blood after administering the initial dose or doses of the anti-human PD-1 antibody compared to that prior to administering the initial dose, and provides a new prescription of the anti-human PD-1 antibody for anti-cancer therapy.
摘要翻译：本发明的目的是提供一种能够更有效地制备用于抗癌治疗的抗人PD-1抗体的方法，用于估计或优化其治疗功效的方法，以及可用于方法。本发明能够通过测量在施用后多于血液中的几种功效标记物的一定水平的变化来选择将来能够预期抗人PD-1抗体的治疗功效的癌症患者的选择与施用初始剂量之前的抗人PD-1抗体的初始剂量或剂量相比较，并且提供了用于抗癌治疗的抗人PD-1抗体的新处方。

9. 发明申请

WO1996003148A1 METHOD AND DRUG FOR TREATING DIABETES 审中-公开
标题翻译：用于治疗糖尿病的方法和药物
公开(公告)号：WO1996003148A1
公开(公告)日：1996-02-08
申请号：PCT/JP1995001484
申请日：1995-07-26
申请人： ONO PHARMACEUTICAL CO., LTD. , KITAGAWA, Koichiro , HIRANO, Atsushi , OHNO, Hiroyuki
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K45/00
CPC分类号： C07K14/47 , A61K38/00
摘要： A novel protein p82; a method and drug for treating diabetes by tyrosinephosphorylating the protein; a drug for treating diabetes containing a derivative capable of tyrosine-phosphorylating the protein, such as a thiazoline derivative, a benzoquinone derivative, a naphthoquinone derivative or vanadic acid, as the active ingredient; and a method of screening a drug for treating diabetes by using the protein. The tyrosinephosphorylation of protein p82 is an indispensable step for glycogen synthesis and the above treatment method and drug and screening method are useful for the amelioration of hyperglycemia and the prevention, treatement, diagnosis and/or measurement of diabetes, particularly non-insulin-dependent diabetes mellitus.
摘要翻译：一种新型蛋白质p82; 通过酪氨酸磷酸化蛋白质治疗糖尿病的方法和药物; 用于治疗含有能够使酪氨酸磷酸化蛋白质的衍生物（例如噻唑啉衍生物，苯醌衍生物，萘醌衍生物或钒酸）作为活性成分的糖尿病药物; 以及通过使用该蛋白质来筛选用于治疗糖尿病的药物的方法。蛋白质p82的酪氨酸磷酸化是糖原合成不可或缺的一步，上述治疗方法和药物和筛选方法可用于改善高血糖症，预防，治疗，诊断和/或测量糖尿病，特别是非胰岛素依赖性糖尿病糖尿病。

10. 发明申请

WO1990009399A1 NEW NEUROTROPHIC FACTOR 审中-公开
标题翻译：新神经营养因子
公开(公告)号：WO1990009399A1
公开(公告)日：1990-08-23
申请号：PCT/JP1990000154
申请日：1990-02-08
申请人： ONO PHARMACEUTICAL CO., LTD. , KATO, Taiji , TANAKA, Ryo
发明人： ONO PHARMACEUTICAL CO., LTD.
IPC分类号： C07K15/06
CPC分类号： C07K14/475
摘要： This invention relates to a new neurotrophic factor (NTF) isolated and purified from the block of neurofibromata obtained from the patients suffering from the von Recklinghausen disease. The NTF has a polypeptide portion of a molecular weight of 3.000 +/- 500 and is a substance which is thermally stable and sensitive to trypsin and proteinase K. This substance promotes the extension of axons of the neurons of a cerebral cortex in a culture medium of a concentration of 1 to 50 ng/ml.
摘要翻译：本发明涉及从患有冯·雷克灵豪森病的患者获得的神经纤维瘤块中分离和纯化的新的神经营养因子（NTF）。 NTF具有分子量为3.000 +/- 500的多肽部分，并且是对胰蛋白酶和蛋白酶K热稳定和敏感的物质。该物质促进培养基中大脑皮质神经元的轴突的延伸浓度为1至50ng / ml。

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