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1. 发明专利

JP2005325031A 1-cinnamylpiperidine derivative 审中-公开
标题翻译： 1-CINNAMYLPIPERIDINE DERIVATIVE
公开(公告)号：JP2005325031A
公开(公告)日：2005-11-24
申请号：JP2004142185
申请日：2004-05-12
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： KAKU HIDETAKA , IWASAKI SHIRO , IIKUBO KAZUHIKO , MORITOMO HIROYUKI , KIMURA TAIJI , SUWA AKIRA
IPC分类号： C07D211/58 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/55 , A61P3/04 , A61P43/00 , C07D401/12
摘要： PROBLEM TO BE SOLVED: To provide a compound useful as a preventing and treating agent of diseases to which a melanin-agglutinating hormone receptor inhibitor is effective, especially obesity, since it has a good ingestion-inhibiting activity based on the melanin-agglutinating hormone receptor-inhibiting effect.
SOLUTION: This 4-benzoylamino-1-cinnamylpiperidine derivative is provided by joining a nitrogen-containing saturated heterocyclic ring such as piperidine, etc., on the benzene ring of cinnamyl group through a linker.
COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供一种可用作黑色素凝集素激素受体抑制剂有效的疾病的预防和治疗剂的化合物，特别是肥胖症，因为其具有基于黑色素的凝集素抑制活性，凝集素激素受体抑制作用。解决方案：该4-苯甲酰基氨基-1-肉桂基哌啶衍生物通过连接物在肉桂基的苯环上连接含氮饱和杂环如哌啶等而提供。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

JP2010037198A Quinolone derivative or its pharmaceutically acceptable salt 审中-公开
标题翻译：喹诺酮衍生物或其药物可接受的盐
公开(公告)号：JP2010037198A
公开(公告)日：2010-02-18
申请号：JP2006316188
申请日：2006-11-22
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： KOGA YUJI , KAMIKUBO TAKASHI , OKUDA TAKAO , KAGEYAMA MICHITO , MORITOMO HIROYUKI
IPC分类号： C07D215/56 , A61K31/4709 , A61P7/02 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
CPC分类号： C07D215/56 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12
摘要： PROBLEM TO BE SOLVED: To provide a compound useful as a medicine having a P2Y12-inhibiting action, especially a platelet aggregation inhibitor. SOLUTION: As a result of zealous examination of P2Y12 inhibitors, there are found that a quinolone derivative having a substituted carbamoyl group at the 3-position wherein the substituent on the carbamoyl group is -(polymethylene substituted on a carbon atom adjacent to the carbamoyl group)-CO 2 R (R is -H or a lower alkyl) has an excellent platelet aggregation-inhibiting action, and improves in vivo dynamics. The compound is useful as a platelet aggregation inhibitor, because of having an excellent P2Y12-inhibiting action and an excellent platelet aggregation-inhibiting action. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用作具有P2Y12抑制作用的药物的化合物，特别是血小板聚集抑制剂。解决方案：作为对P2Y12抑制剂的热烈检查的结果，发现在3-位上具有取代的氨基甲酰基的喹诺酮衍生物是氨基甲酰基上的取代基是 - （在与...相邻的碳原子上取代的聚亚甲基氨基甲酰基）-CO 2 SBR（R为-H或低级烷基）具有优异的血小板聚集抑制作用，并改善体内动力学。由于具有优异的P2Y12抑制作用和优异的血小板聚集抑制作用，该化合物可用作血小板聚集抑制剂。版权所有（C）2010，JPO＆INPIT

3. 发明专利

JP2013107880A N-thienyl benzamide derivative 审中-公开
标题翻译： N-苯基苯甲酰衍生物
公开(公告)号：JP2013107880A
公开(公告)日：2013-06-06
申请号：JP2012236135
申请日：2012-10-25
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： MIURA MICHINORI , YATANI SHUNICHIRO , KAGA DAISUKE , WATANUKI SUSUMU , OKUDA TAKAO , OKU MAKOTO , IMAMURA YOSHIMASA , FUJIYASU JIRO , SUZUKI DAISUKE , MORITOMO HIROYUKI , KATO KOJI , SATO IPPEI , ISOMURA MAI , KUROSAWA KAZUO , YOSHIMITSU TATSUYA , MARUYAMA TATSUYA , YOSHIHARA KOSEI , TERAI KAZUHIRO , TERADA HIROSHI
IPC分类号： C07D333/50 , A61K31/381 , A61K31/4025 , A61K31/439 , A61K31/4436 , A61K31/4535 , A61K31/496 , A61K31/5377 , A61K31/67 , A61P3/12 , A61P13/12 , A61P43/00 , C07D333/68 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D453/02 , C07D495/04
CPC分类号： C07D409/12 , C07D333/68 , C07D333/78 , C07D333/80 , C07D409/14 , C07D413/12 , C07D417/12 , C07D453/02 , C07D495/04
摘要： PROBLEM TO BE SOLVED: To provide a compound that has the inhibitory action of an intestinal tract phosphate transporter (NPT-IIb), and is useful for the active ingredient of the therapeutic agent and/or the prophylactic agent of high phosphorus blood syndrome.SOLUTION: The creation of a compound that has an NPT-IIb inhibitory action and is useful as the active ingredient of the therapeutic agent and/or the prophylactic agent of a high phosphorus blood syndrome is examined. As a result, an N-thienyl benzamide derivative that has an NPT-IIb inhibitory action is found. The N-thienyl benzamide derivative has the NPT-IIb inhibitory action, and can be used as the prevention and/or therapeutic agent of a high phosphorus blood syndrome.
摘要翻译：待解决的问题：提供具有肠道磷酸转运蛋白（NPT-IIb）抑制作用的化合物，并且可用于高磷血液的治疗剂和/或预防剂的活性成分综合征解决方案：检查具有NPT-IIb抑制作用并可用作治疗剂和/或高磷血症综合征预防剂的活性成分的化合物的产生。结果发现具有NPT-IIb抑制作用的N-噻吩基苯甲酰胺衍生物。 N-噻吩基苯甲酰胺衍生物具有NPT-IIb抑制作用，可用作高磷血症综合征的预防和/或治疗剂。版权所有（C）2013，JPO＆INPIT

4. 发明专利

JP2010174027A Diaminopyrimidine carboxamide derivative 有权
标题翻译：二氨基嘧啶羧酰胺衍生物
公开(公告)号：JP2010174027A
公开(公告)日：2010-08-12
申请号：JP2010057853
申请日：2010-03-15
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： NAGASHIMA SHINYA , OSADA HIROSHI , IWATA MASAHIRO , YOKOTA MASAKI , MORITOMO HIROYUKI , NAKAI HIDEKAZU , KUROMITSU SADAO , OGA KEIKO , TAKEUCHI MAKOTO
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/553 , A61K31/7064 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/08 , C07D471/10 , C07D487/08 , C07H15/26 , C12N15/09
CPC分类号： C07D403/12 , C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/04 , C07D453/02 , C07D471/10 , C07D487/08
摘要： PROBLEM TO BE SOLVED: To provide a compound usable for the prevention and treatment of respiratory diseases in which STAT6 is concerned, especially asthma and chronic obstructive pulmonary disease and the like. SOLUTION: This diaminopyrimidine carboxamide derivative is a diaminopyrimidine-5-carboxamide derivative having an arylamino or an arylethylamino group which may be substituted with a specific substituent at the 2-position, an amino group which is substituted with a cycloalkylmethyl group, an arylalkyl or the like at the 4-position, and a carbamoyl group which may be substituted with an alkyl group or the like at the 5-position, or salts thereof and they have strong and selective STAT6 inhibiting action and pharmacodynamic action based thereon. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用于预防和治疗其中涉及STAT6的呼吸系统疾病的化合物，特别是哮喘和慢性阻塞性肺病等。解决方案：该二氨基嘧啶羧酰胺衍生物是具有可被2-位上的特定取代基取代的芳氨基或芳乙氨基的二氨基嘧啶-5-甲酰胺衍生物，被环烷基甲基取代的氨基， 4-位上的芳基烷基等，以及可以被5位上的烷基等取代的氨基甲酰基或其盐，并且它们具有强的和选择性的STAT6抑制作用和基于其的药效学作用。版权所有（C）2010，JPO＆INPIT

5. 发明专利

JP2006166823A Method for screening therapeutic medicine for sex hormone disorder 审中-公开
标题翻译：用于筛选性激素治疗药物的方法
公开(公告)号：JP2006166823A
公开(公告)日：2006-06-29
申请号：JP2004365181
申请日：2004-12-17
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： MATSUMOTO SHUNICHIRO , HIYAMA HIDEKI , ORITA MASAYA , MORITOMO HIROYUKI
IPC分类号： C12Q1/02 , C12N15/09 , G01N33/15 , G01N33/50
摘要： PROBLEM TO BE SOLVED: To provide a new and simple method for screening therapeutic medicines for sex hormone disorders. SOLUTION: The present inventors prepared a knockout mouse of GPRg2 gene and analyzed a phenotype and found that testis which is a tissue for secreting testosterone which is an exacerbation factor for androgenic disorders notably shrinks in the knockout mouse, compared with that of a wild type mouse. These inventors further found that ovary which is a tissue for secreting estrogen causing female hormone disorder remarkably shrinks in the knockout mouse, compared with that of a wild type mouse. These inventors provided GPRg2 polypeptide and a cell expressing the polypeptide as a screening tool for therapeutic medicines for sex hormone disorder by these knowledge. These inventors, further, built a system for screening therapeutic medicines for sex hormone disorders using the GPRg2 polypeptide to complete the present invention. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：提供一种用于筛选性激素障碍治疗药物的新型简单方法。解决方案：本发明人制备了GPRg2基因的敲除小鼠并分析了表型，发现作为分泌睾丸激素的组织的睾丸是雄激素障碍的加重因子，特别是与敲除小鼠相比，在敲除小鼠中收缩野生型鼠标。这些发明人进一步发现，与野生型小鼠相比，在敲除小鼠中，作为分泌雌激素导致雌激素紊乱的组织的卵巢显着收缩。这些发明人通过这些知识，提供GPRg2多肽和表达多肽的细胞作为性激素障碍治疗药物的筛选工具。此外，这些发明人还构建了一种使用GPRg2多肽筛选用于性激素障碍的治疗药物来完成本发明的系统。版权所有（C）2006，JPO＆NCIPI

6. 发明公开

KR20180032585A 피페라진 유도체 审中-公开
标题翻译：哌嗪衍生物
公开(公告)号：KR20180032585A
公开(公告)日：2018-03-30
申请号：KR20187003183
申请日：2016-08-02
申请人： ASTELLAS PHARMA INC
发明人： SUGANE TAKASHI , MAKINO TAKUYA , YAMASHITA DAISUKE , YONETOKU YASUHIRO , TANABE DAISUKE , MIHARA HISASHI , ASAI NORIO , OSODA KAZUHIKO , SHIMIZU TAKAFUMI , MORITOMO HIROYUKI , SUGASAWA KEIZO , MAENO KYOICHI , HOSOGAI NAOMI
IPC分类号： C07D405/14 , A61K31/496 , A61K31/501 , A61P13/02 , A61P13/10 , C07D403/06 , C07D409/14
CPC分类号： A61K31/496 , A61K31/501 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： [과제] MC수용체아고니스트로서사용할수 있는화합물을제공한다. [해결수단] 본발명자들은, MC수용체아고니스트에관해검토하여, 피페라진유도체가작용을갖는것을확인하여, 본발명을완성하였다. 즉, 본발명의피페라진유도체는 MC수용체아고니스트작용을가지고, 방광·요로계질환, 특히, 저활동방광, 저긴장성방광, 무수축방광, 배뇨근저활동, 신경인성방광, 요도이완부전, 배뇨근-외요도괄약근협조부전및 전립선비대증에있어서의배뇨장해의예방및/또는치료제로서사용할수 있다.
摘要翻译： [问题]提供可以用作MC受体激动剂的化合物。 [解决问题的手段]本发明人已经研究和MC受体激动剂，确认具有作用的哌嗪衍生物，并完成了本发明。即，本发明的哌嗪衍生物具有MC受体激动剂作用，膀胱，泌尿道障碍，特别是，低活性膀胱，低张力膀胱，非收缩膀胱，逼尿肌的活性低，神经原性膀胱，尿道松弛失败，逼尿肌 - 更尿道括约肌可以用作预防和/或治疗剂，以用于协作失败和良性前列腺增生症的排尿困难。

7. 发明专利

JP2006225378A MEDICINAL COMPOSITION COMPRISING QUINOLONE DERIVATIVE AS ACTIVE INGREDIENT 审中-公开
公开(公告)号：JP2006225378A
公开(公告)日：2006-08-31
申请号：JP2006009349
申请日：2006-01-18
申请人： ASTELLAS PHARMA INC
发明人： WATANUKI SUSUMU , KOGA YUJI , MORITOMO HIROYUKI , TSUKAMOTO KAZUNARI , KAGA DAISUKE , OKUDA TAKAO , HIRAYAMA FUKUSHI , MORITANI YUMIKO , TAKASAKI ATSUSHI
IPC分类号： C07D215/56 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4745 , A61K31/496 , A61K31/502 , A61K31/55 , A61K31/706 , A61P7/04 , C07D237/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D417/12 , C07D455/04 , C07D471/04 , C07H7/033
摘要： PROBLEM TO BE SOLVED: To provide a medicinal composition having excellent inhibitory actions on platelet aggregation. SOLUTION: A quinolone derivative having an amide group at the 3-position and a substituted amino group substituted with a substituent having a cyclic structure at the 7-position or a pharmaceutically acceptable salt thereof has excellent inhibitory actions on P2Y12. The quinolone derivative has the excellent inhibitory actions on the platelet aggregation. A medicinal composition comprising the quinolone derivative or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier as active ingredients is useful as an inhibitor of the platelet aggregation. COPYRIGHT: (C)2006,JPO&NCIPI

8. 发明专利

JP2006225379A METHOD FOR PRODUCING QUINOLONE DERIVATIVE OR SALT THEREOF 审中-公开
公开(公告)号：JP2006225379A
公开(公告)日：2006-08-31
申请号：JP2006009367
申请日：2006-01-18
申请人： ASTELLAS PHARMA INC
发明人： WATANUKI SUSUMU , KOGA YUJI , MORITOMO HIROYUKI , TSUKAMOTO KAZUNARI , KAGA DAISUKE , OKUDA TAKAO , HIRAYAMA FUKUSHI , MORITANI YUMIKO , TAKASAKI ATSUSHI
IPC分类号： C07D215/56 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/661 , A61P7/02 , C07D237/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/06 , C07D417/12 , C07D471/04 , C07F9/60
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a quinolone derivative or a salt thereof useful as an inhibitor of platelet aggregation and having inhibitory actions on P2Y12. SOLUTION: The quinolone derivative or pharmaceutically acceptable salt thereof having an amide group at the 3-position and an amino group substituted with a substituent having a cyclic structure at the 7-position has the excellent inhibitory actions on the P2Y12. Thereby, the quinolone derivative or pharmaceutically acceptable salt thereof is useful as the inhibitor of the platelet aggregation. The quinolone derivative or pharmaceutically acceptable salt thereof can be produced by condensing a carboxylic acid derivative with an amine compound or condensing a quinolone derivative having a leaving group at the 7-position with an amine compound. COPYRIGHT: (C)2006,JPO&NCIPI

9. 发明公开

EP1806347A4 AROMATIC-RING-FUSED PYRIMIDINE DERIVATIVE 审中-公开
标题翻译：与芳环缩合的嘧啶衍生物
公开(公告)号：EP1806347A4
公开(公告)日：2009-07-01
申请号：EP05790537
申请日：2005-10-05
申请人： ASTELLAS PHARMA INC
发明人： YONETOKU YASUHIRO , NEGORO KENJI , ONDA KENICHI , HAYAKAWA MASAHIKO , SASUGA DAISUKE , NIGAWARA TAKAHIRO , IIKUBO KAZUHIKO , MORITOMO HIROYUKI , YOSHIDA SHIGERU , OHISHI TAKAHIDE
IPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , A61K31/54 , A61K31/55 , A61P3/10 , A61P5/50 , A61P43/00 , C07D495/04 , C07D513/04
CPC分类号： C07D471/04 , C07D495/04 , C07D513/04
摘要： A novel pyrimidine derivative in which pyrimidine has been fused with an aromatic heterocycle selected among thiophene, thiazole, and pyridine or a pharmaceutically acceptable salt of the derivative; and a medicinal composition containing the compound or salt as an active ingredient. These compounds have excellent activity in accelerating insulin secretion and excellent activity in inhibiting the increase of a blood sugar level. Therefore, the medicinal composition containing the compound or salt as an active ingredient is useful, based on these activities, for the treatment and/or prevention of insulin-dependent diabetes mellitus (type 1 diabetes), noninsulin-dependent diabetes mellitus (type 2 diabetes), insulin-resistant diseases, and obesity.

10. 发明公开

EP2821402A4 NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND 有权转让
标题翻译：芳香族杂环CONNECTION含氮
公开(公告)号：EP2821402A4
公开(公告)日：2015-08-19
申请号：EP13754501
申请日：2013-02-26
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAMEDA MINORU , KURIWAKI IKUMI , IIKUBO KAZUHIKO , HISAMICHI HIROYUKI , KAWAMOTO YUICHIRO , MORITOMO HIROYUKI , SUZUKI TOMOYUKI , FUTAMI TAKASHI , SUZUKI ATSUSHI , TSUNOYAMA KAZUHISA , ASAUMI MAKOTO , TOMIYAMA HIROSHI , NODA ATSUSHI , IWAI YOSHINORI , TOKUZAKI KAZUO , OKADA HARUKI , MIYASAKA KOZO
IPC分类号： C07D239/42 , A61K31/4545 , A61K31/506 , A61P35/00 , A61P43/00 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/12 , C07D471/10 , C07D487/20
CPC分类号： C07D239/47 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D451/02 , C07D451/04 , C07D453/02 , C07D471/08 , C07D471/10 , C07D487/10 , C07D491/107
摘要： Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

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