公开(公告)号：EP3533449A1

公开(公告)日：2019-09-04

申请号：EP17864975.2

申请日：2017-10-13

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： MIYADERA, Kazutaka ,  AOYAGI, Yoshimi ,  HASAKO, Shinichi

IPC分类号： A61K31/519 ,  A61P35/00

摘要： An antitumor agent comprising a compound selected from the group consisting of Compounds A to D described in the specification, or a salt thereof, for treating a malignant tumor patient expressing EGFR having exon 20 insertion mutation.

公开(公告)号：EP3424505A1

公开(公告)日：2019-01-09

申请号：EP17760187.9

申请日：2017-03-03

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： MIURA, Akihiro ,  SOOTOME, Hiroshi

IPC分类号： A61K31/519 ,  A61K31/337 ,  A61K31/436 ,  A61K31/4375 ,  A61K31/4412 ,  A61K31/513 ,  A61K31/53 ,  A61K31/7068 ,  A61K31/7072 ,  A61K33/24 ,  A61K45/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00

摘要： It is intended to provide a novel method for treating a cancer using an FGFR inhibitor that exhibits a remarkably excellent antitumor effect and has fewer side effects. The present invention provides a combination preparation for the treatment of a malignant tumor comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof, and one or more additional compound(s) having an antitumor effect or pharmaceutically acceptable salt(s) thereof, and a pharmaceutical composition comprising both the active ingredients. The present invention also provides an antitumor effect enhancer, an antitumor agent, a kit for malignant tumor treatment, etc. comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP3070086B1

公开(公告)日：2018-11-21

申请号：EP15746235.9

申请日：2015-02-04

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： NAKAMURA, Masayuki ,  YAMANAKA, Hiroyoshi ,  SHIBATA, Kazuaki ,  MITSUYA, Morihiro ,  HARADA, Takafumi

IPC分类号： C07D471/04 ,  A61K31/437

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/695 ,  C07D471/04

摘要： Provided is a novel compound having a selective JAK3-inhibitory effect and also having excellent oral absorbability. Also provided is a pharmaceutical agent, which is based on a JAK3-inhibitory effect and is useful for preventing and/or treating a disease involving the JAK3, and in particular, rheumatoid arthritis or multiple sclerosis. An azaindole derivative having a cycloalkenyl group, which is represented by the following formula (I), or a salt thereof, and a pharmaceutical composition containing the same: where R 1 to R 4 , m and n have the same meanings as those defined in the description.

公开(公告)号：EP3345907A1

公开(公告)日：2018-07-11

申请号：EP16841868.9

申请日：2016-08-31

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： KAWAI, Yuichi ,  IRIE, Hiroki ,  SAGARA, Takeshi ,  MIYADERA, Kazutaka

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

摘要： To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 inhibitory effect.
The present invention provides a compound of formula (I) wherein X, Y, Z 1 , Z 2 , Z 3 , Z 4 , W, n, R 1 , R 2 , and R 3 have meanings as defined in the present specification, or a salt thereof.

公开(公告)号：EP3315131A1

公开(公告)日：2018-05-02

申请号：EP16814513.4

申请日：2016-06-24

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： FUJIOKA, Akio

IPC分类号： A61K31/47 ,  A61P11/00 ,  C07D215/50

CPC分类号： A61K31/47 ,  A61P11/00 ,  C07D215/50

摘要： Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.

摘要翻译： 本发明提供对纤维化和与纤维化相关的症状发挥优异的预防或治疗效果的治疗剂和药物组合物。 用于纤维化的治疗剂包含4- [2-氟-4 - [[[（2-苯乙酰基）氨基]硫代甲基]氨基]苯氧基] -7-甲氧基-N-甲基-6-喹啉甲酰胺或其盐 有效成分。

公开(公告)号：EP3305779A1

公开(公告)日：2018-04-11

申请号：EP17204730.0

申请日：2014-06-17

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： Kazuno, Hideki ,  Mutsumi, Tomonobu

IPC分类号： C07D403/06 ,  A61K31/506 ,  A61K31/7072 ,  A61P35/00 ,  A61P43/00

CPC分类号： C07D403/06 ,  C07B2200/13

摘要： An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrim idinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-l-yl)methyl-2,4(1H,3H)-pyrim idinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2θ ± 0.1°) in powder X-ray diffraction.

摘要翻译： 本发明的目的是获得5-氯-6-（2-亚氨基吡咯烷-1-基）甲基-2,4（1H，3H） - 嘧啶酮二酮盐酸盐的稳定晶型。 本发明提供了在11.6°，17.2°，17.8°角具有特征峰的5-氯-6-（2-亚氨基吡咯烷-1-基）甲基-2,4（1H，3H） - 嘧啶二酮盐酸盐的晶体 ，23.3°，27.1°和29.3°作为粉末X射线衍射中的衍射角（2θ±0.1°）。

公开(公告)号：EP3290406A1

公开(公告)日：2018-03-07

申请号：EP16789552.3

申请日：2016-04-28

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： FUKUOKA, Masayoshi

IPC分类号： C07D239/54 ,  A61K31/505 ,  A61P35/00 ,  A61P43/00

CPC分类号： C07D239/22 ,  A61P35/00 ,  C07B2200/13 ,  C07D239/54

摘要： The present invention provides a crystal that has preferable oral absorption and can be obtained with particularly preferable reproducibility. Provided is a crystal of (R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamide.

摘要翻译： 本发明提供具有优选的口服吸收且可以特别优选的再现性获得的晶体。 提供了（R）-N-（1-（3-（环戊基氧基）苯基）乙基）-3 - （（2,4-二氧代-3,4-二氢嘧啶-1（2H） - 基）甲氧基） 丙烷-1-磺酰胺。

公开(公告)号：EP3290405A1

公开(公告)日：2018-03-07

申请号：EP16786581.5

申请日：2016-04-28

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： SATO, Ayako

IPC分类号： C07D215/48 ,  A61K31/47 ,  A61P19/10 ,  A61P35/00 ,  A61P43/00

CPC分类号： A61K31/47 ,  A61K9/0053 ,  A61K31/17 ,  A61P35/00 ,  C07B2200/13 ,  C07D215/48

摘要： The purpose of the present invention is to provide a salt of 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, which is useful as an antitumor drug, and crystals of the salt, the salt and crystals being excellent in terms of solubility, stability, and oral absorbability and being capable of mass-production. The present invention relates to a mesylic acid salt of 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide and to the mesylic acid salt including crystals which give an X-ray powder diffraction spectrum having characteristic peaks at given diffraction angles.

摘要翻译： 本发明的目的是提供4-（2-氟-4-（3-（2-苯基乙酰基）硫脲基）苯氧基）-7-甲氧基-N-甲基喹啉-6-甲酰胺的盐， 抗肿瘤药物和盐的晶体，盐和晶体在溶解性，稳定性和口服吸收性方面优异并且能够大量生产。 本发明涉及4-（2-氟-4-（3-（2-苯乙酰基）硫脲基）苯氧基）-7-甲氧基-N-甲基喹啉-6-甲酰胺的甲磺酸盐和甲磺酸盐，包括 给出在给定衍射角下具有特征峰的X射线粉末衍射光谱的晶体。

公开(公告)号：EP3290038A1

公开(公告)日：2018-03-07

申请号：EP16786600.3

申请日：2016-04-28

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： WAKASA, Takeshi

IPC分类号： A61K31/513 ,  A61P1/00 ,  A61P43/00 ,  A61K31/4412 ,  A61K31/519 ,  A61K31/53 ,  A61P35/00

CPC分类号： A61K31/513 ,  A61K31/4412 ,  A61K31/519 ,  A61K31/53 ,  A61K31/7072 ,  A61P1/00 ,  A61P35/00

摘要： Provided is an agent for alleviating side effect of antitumor drug, the agent alleviating side effect of antitumor drug when used in combination with the antitumor drug. Disclosed is an agent for alleviating side effect of antitumor drug, the agent containing a uracil compound represented by the following Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient:

wherein R 1 represents a hydrogen atom or a C1-6 alkyl group; R 2 represents a hydrogen atom or a halogen atom; and R 3 represents a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl) -C1-6 alkyl group, a halogeno-C1-6 alkyl group, or a saturated heterocyclic group.

摘要翻译： 本发明提供一种缓解抗肿瘤药物副作用的药剂，与抗肿瘤药物组合使用时，可以减轻抗肿瘤药物的副作用。 本发明公开了一种缓解抗肿瘤药物副作用的药物，所述药物含有由下式（I）表示的尿嘧啶化合物或其药理学上可接受的盐作为活性成分：其中R 1表示氢原子或C 1-6烷基 ; R2代表氢原子或卤素原子; 并且R 3表示C 1-6烷基，C 2-6烯基，C 3-6环烷基，（C 3-6环烷基）-C 1-6烷基，卤代-C 1-6烷基或饱和 杂环基团。

公开(公告)号：EP2947086B1

公开(公告)日：2018-01-03

申请号：EP14836782.4

申请日：2014-08-11

申请人： Taiho Pharmaceutical Co., Ltd.

发明人： IGUCHI, Satoru ,  HOSOI, Fumihito ,  SAGARA, Takeshi

IPC分类号： C07D519/00 ,  A61K31/519 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519 ,  C07D519/00 ,  C07F5/02

摘要： Provided is a novel compound having BTK inhibitory action and a cell proliferation suppressing effect. Also provided is a medicine useful for the prevention and/or treatment of a disease associated with BTK, particularly cancer, based on BTK inhibitory action. A compound represented by formula (I) [wherein R 1 to R 3 , W, A, Y and Z respectively have the meanings as defined in the specification], or a salt thereof is disclosed.