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2. 发明公开

EP3315492A1 PYRAZOLE DERIVATIVE, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 有权
标题翻译：吡唑衍生物，或药物可接受的盐
公开(公告)号：EP3315492A1
公开(公告)日：2018-05-02
申请号：EP16814372.5
申请日：2016-06-22
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： HIRASAWA, Hideaki , TANADA, Fumiya , MUTAI, Yousuke , FUSHIMI, Nobuhiko , KOBAYASHI, Junichi , KIJIMA, Yoshiro
IPC分类号： C07D231/12 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/427 , A61K31/436 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61P11/02
摘要： [Problem]
The present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof.
[Solution]
The present invention provides a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which has TRPM8 inhibitory effects:

wherein ring A is C 6-10 aryl or the like; X is CR 4a or the like; R 1 and R 2 are a hydrogen atom or the like; R 3 is a hydrogen atom or the like; R 4 is a hydrogen atom or the like; ring B is C 6-10 aryl or the like; R 5 is a hydrogen atom or the like; R 6a is a hydrogen atom or the like; R 7a is a hydrogen atom or the like; R 7b is a hydrogen atom or the like; R 6b is a hydrogen atom or the like; R 8 is a hydrogen atom or the like; n is 0, 1 or 2. Therefore, the compound represented by the formula (I) of the present invention or a pharmaceutically acceptable salt thereof is useful as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.
摘要翻译：本发明提供新的吡唑衍生物或其药学上可接受的盐，含有其的药物组合物及其药物用途。本发明提供具有TRPM8抑制效果的式（I）所示的化合物或其药学上可接受的盐，其中环A为C 6-10芳基等; X是CR4a等; R1和R2是氢原子等; R3是氢原子等; R4是氢原子等; 环B是C 6-10芳基等; R5是氢原子等; R6a是氢原子等; R7a是氢原子等; R7b是氢原子等; R6b是氢原子等; R8是氢原子等; n为0,1或2.因此，由本发明的式（I）表示的化合物或其药学上可接受的盐可用作用于治疗或预防由传入神经元的兴奋过度或病症引起的疾病或症状的药剂。

3. 发明授权

EP3067349B1 CARBOXYMETHYL PIPERIDINE DERIVATIVE 有权
标题翻译：羧甲基哌啶衍生物
公开(公告)号：EP3067349B1
公开(公告)日：2018-02-28
申请号：EP14860761.7
申请日：2014-11-06
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： SHIMIZU, Kazuo , MIYAGI, Takashi , OHNO, Kohsuke , UENO, Yasunori , ONDA, Yusuke , SUZUKI, Hikaru
IPC分类号： C07D401/04 , A61K31/4545 , A61P1/08 , A61P35/00 , A61P43/00 , C12N15/09
CPC分类号： C07D401/04 , C07D413/14
摘要： The present invention provides a new compound which has NK 1 receptor antagonist activity ,whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R 1 is C 1-6 alkyl or C 1-6 alkoxy; R 2 and R 3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5. Formula (I):

4. 发明公开

EP2930175A4 NOVEL OCTAHYDROPYRIDOQUINAZOLINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USES FOR SAID DERIVATIVE AND COMPOSITION 审中-公开
标题翻译：新型OCTAHYDROPYRIDOCHINAZOLINDERIVAT，药物组合物所述衍生物与成分使用
公开(公告)号：EP2930175A4
公开(公告)日：2016-12-21
申请号：EP13862652
申请日：2013-12-06
申请人： KISSEI PHARMACEUTICAL
发明人： NISHIMURA TOSHIHIRO , UENO YASUNORI , KASAI KIYOSHI , YOSHIDA MASAKO
IPC分类号： C07D471/04 , A61K31/519 , A61K31/55 , A61K31/553 , A61K45/00 , A61P5/06 , A61P25/16 , A61P25/28 , A61P43/00 , C12N15/09
CPC分类号： A61K31/519 , A61K31/13 , A61K31/198 , A61K31/423 , A61K31/55 , A61K45/06 , C07D471/04 , C12N15/09 , A61K2300/00

5. 发明公开

EP2979697A4 ORAL ADMINISTRATION PREPARATION WITH MASKED BITTERNESS OF SILODOSIN 审中-公开
标题翻译：法制备西洛多辛掩蔽的苦涩ORAL
公开(公告)号：EP2979697A4
公开(公告)日：2016-11-30
申请号：EP14776456
申请日：2014-03-25
申请人： KISSEI PHARMACEUTICAL
发明人： SHIBATA YUSUKE , ISSHIKI NOBUYUKI , KIMURA SHIN-ICHIRO
IPC分类号： A61K31/404 , A61K9/14 , A61K9/16 , A61K9/50 , A61K9/62 , A61K31/4045 , A61K47/10 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61P13/02 , A61P13/08
CPC分类号： A61K9/5026 , A61K9/1635 , A61K9/1652 , A61K9/5042 , A61K9/5047 , A61K9/5089 , A61K31/404 , A61K31/4045
摘要： The present invention provides a novel oral administration preparation that enables administration of silodosin, which is a drug with extremely strong bitterness, without a foreign-body sensation even without water, and has dissolution properties of being able to reproduce an effective blood concentration for the treatment of dysuria associated with benign prostatic hyperplasia or the like. The present invention relates to a masked particle and a novel oral administration preparation comprising the masked particle or the like, wherein the masked particle obtained by granulating or coating a drug particle comprising a fine powder of silodosin with a coating agent comprising a non-enteric polymer, and a content of the non-enteric polymer is 80 parts by mass to 400 parts by mass relative to 100 parts by mass of silodosin.

6. 发明授权

EP1782828B1 PROGRESSION INHIBITOR FOR DISEASE ATTRIBUTED TO ABNORMAL ACCUMULATION OF LIVER FAT 有权
标题翻译： PROGRESSION抑制剂与肝脂异常积累有关的疾病
公开(公告)号：EP1782828B1
公开(公告)日：2016-06-29
申请号：EP05762058.5
申请日：2005-07-19
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： KATSUNO, Kenji , FUJIMORI, Yoshikazu , ISAJI, Masayuki
IPC分类号： A61K45/00 , A61K31/155 , A61K31/4427 , A61K31/57 , A61K31/7028 , A61K31/7036 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P35/00 , A61P43/00
CPC分类号： A61K31/7028 , A61K31/155 , A61K31/4427 , A61K31/57 , A61K31/7036

7. 发明公开

EP2848254A1 PYRAZOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 有权
标题翻译：吡唑及其用途为医疗目的
公开(公告)号：EP2848254A1
公开(公告)日：2015-03-18
申请号：EP13787714.8
申请日：2013-05-02
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： ISAJI, Masayuki , TAKEMURA, Masaaki , ISAWA, Hidetoshi , HOTEI, Yukihiko , MIYASHITA, Itaru
IPC分类号： A61K31/7056 , A61P1/10
CPC分类号： A61K31/7056 , C07H17/02
摘要： The present invention provides pyrazole derivatives, uses thereof for for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.

8. 发明公开

EP2749562A1 FUSED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：秘密药剂师联合会在西班牙药剂师VERWENDUNG
公开(公告)号：EP2749562A1
公开(公告)日：2014-07-02
申请号：EP12825645.0
申请日：2012-08-23
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： SHIMIZU, Kazuo , ONDA, Yusuke , IIZUKA, Masato
IPC分类号： C07D491/048 , A61K31/407 , A61P13/12 , A61P19/06 , A61P43/00 , C07D495/04
CPC分类号： C07D495/04 , C07D333/24 , C07D491/048
摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like.
The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, or prodrugs thereof, or pharmaceutically acceptable salts thereof.
In the formula (I), ring U represents C 6-10 aryl or the like; R 1 independently represents a hydrogen atom, a hydroxy group, C 1-6 alkyl or the like; m represents an integral number from 1 to 2; ring Q represents 5-membered heteroaryl; n represents an integral number from 1 to 3; R 2 independently represents a hydrogen atom, a halogen atom, C 1-6 alkyl or the like.
摘要翻译：本发明提供可用作预防或治疗与血清尿酸水平异常等有关的疾病的药剂的化合物。本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠合杂环衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病或其前药或药学上可接受的盐它们。在式（I）中，环U表示C 6-10芳基等; R 1独立地表示氢原子，羟基，C 1-6烷基等; m表示1〜2的整数; 环Q表示5元杂芳基; n表示1〜3的整数; R 2独立地表示氢原子，卤素原子，C 1-6烷基等。

9. 发明公开

EP2669285A4 PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：其PYRAZOLOPYRIDINDERIVAT或药学上可接受的盐
公开(公告)号：EP2669285A4
公开(公告)日：2014-06-18
申请号：EP12739093
申请日：2012-01-25
申请人： KYORIN SEIYAKU KK , KISSEI PHARMACEUTICAL
发明人： SETO SHIGEKI , UMEI KENTARO , NISHIGAYA YOSUKE , TANIOKA ASAO , KONDO TATSUHIRO , KONDO ATSUSHI , TATANI KAZUYA , KAWAMURA NAOHIRO
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/5377 , A61P13/02 , A61P43/00
CPC分类号： C07D471/04

10. 发明公开

EP2228378A4 MONOSEBACATE OF PYRAZOLE DERIVATIVE 有权
标题翻译： PYRAZOLDERIVAT-MONOSEBACAT
公开(公告)号：EP2228378A4
公开(公告)日：2014-05-28
申请号：EP08867231
申请日：2008-12-24
申请人： KISSEI PHARMACEUTICAL
发明人： TAKEUCHI HIDEKI , TSURU EIJI
IPC分类号： C07H17/02 , A61K31/7056 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P7/10 , A61P9/04 , A61P9/10 , A61P9/12 , A61P19/06 , A61P43/00
CPC分类号： C07H17/02

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