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1. 发明专利

JP2006219480A Pharmaceutical composition containing acylaminothiazole derivative as active ingredient 有权
标题翻译：含有乙酰胺唑衍生物作为活性成分的药物组合物
公开(公告)号：JP2006219480A
公开(公告)日：2006-08-24
申请号：JP2006003655
申请日：2006-01-11
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： SUGASAWA KEIZOU , KOGA YUJI , KOHITSU KAZUYOSHI , OKUDA TAKAO , HARADA KOICHIRO , KUBOTA HIDEKI , HIRAYAMA FUKUSHI , ABE MASAKI , SUZUKI KENICHI
IPC分类号： A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K31/695 , A61P7/04 , A61P7/06 , C07D417/04 , C07D417/14 , C07D513/14
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition containing a compound, which has excellent thrombocyte increasing activity based on human c-mpl-Ba/F3 cell growth action and megakaryocyte colony formation accelerating action and is useful for treating thrombocytopenia, as an active ingredient. SOLUTION: This pharmaceutical composition contains a new 2-acylaminothiazole derivative expressed by formula (1) (B is a lower alkylene; R 4 is an amino or a cyclic amino of which the each may be substituted; R 5 is thienyl or phenyl of which the each may be substituted; and R 6 is an aromatic heterocyclic, an aryl or a cyclic amino of which the each may be substituted, provided that R 6 does not include phenyl which is not substituted nor indole which may be substituted) or a pharmacologically acceptable salt thereof and a pharmacologically acceptable carrier. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：提供一种含有化合物的药物组合物，其基于人c-mpl-Ba / F3细胞生长作用和巨核细胞集落形成促进作用具有优异的血小板增加活性，并且可用于治疗血小板减少症，如活性成分。解决方案：该药物组合物含有由式（1）表示的新的2-酰基氨基噻唑衍生物（B为低级亚烷基; R 4为每个氨基或环状氨基的氨基或环状氨基） R 6是其中每个可以被取代的噻吩基或苯基;并且R 6是芳族杂环，芳基或环氨基，其各自可以是取代的，条件是R 6不包括未被取代的苯基或可被取代的吲哚）或其药学上可接受的盐和药理学上可接受的载体。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

JP2006219481A Method for producing acylaminothiazole derivative 有权
标题翻译：制备酰氨基噻唑衍生物的方法
公开(公告)号：JP2006219481A
公开(公告)日：2006-08-24
申请号：JP2006003657
申请日：2006-01-11
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： SUGASAWA KEIZOU , KOGA YUJI , KOHITSU KAZUYOSHI , OKUDA TAKAO , HARADA KOICHIRO , KUBOTA HIDEKI , HIRAYAMA FUKUSHI , ABE MASAKI , SUZUKI KENICHI
IPC分类号： C07D417/04 , A61K31/427 , A61K31/4439 , A61K31/4545 , A61P7/04 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a 2-acylaminothiazole derivative or its pharmaceutically allowable salt which has thrombocytosis activity based on excellent human c-mpl-Ba/F3 cell proliferation action and megakaryocyte colony formation acceleration action and is useful for curing thrombocytopenia. SOLUTION: The method produces a 2-acylaminothiazole derivative represented by formula (I) or its pharmaceutically allowable salt. In formula (I), -R 1 is a lower alkyl group or a cycloalkyl group; -A= is -N= or -CH=; -X is a halogen; (a) when -A= is -N=, then -Y- is -NR 3 - and (b) when -A= is -CH=, then -Y- is -O-; -R 2 is a substituted lower alkyl group; and -R 3 is -H or a lower alkyl group; and optionally, R 2 and R 3 may be united with an adjacent nitrogen atom to form a substituted piperidin-1-yl group or a piperazin-1-yl group substituted by an oxo group. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供一种基于优异的人c-mpl-Ba / F3细胞增殖作用和巨核细胞集落形成加速作用产生具有血小板增多活性的2-酰基氨基噻唑衍生物或其药学上允许的盐的方法，并且是可用于治疗血小板减少症。方法：该方法产生由式（I）表示的2-酰基氨基噻唑衍生物或其药学上可允许的盐。在式（I）中，-R SP 1是低级烷基或环烷基; -A = = -N =或-CH =; -X是卤素; （a）当-A =为-N =时，-Y-为-NR 3，和（b）当-A =为-CH =时，-Y-为-O-; -R 2 是取代的低级烷基; 且R 3 = H或低级烷基; 并且任选地，R“SP”2和R“3”可以与相邻的氮原子一起形成取代的哌啶-1-基或被哌嗪-1-基取代的哌嗪-1-基，氧代基团。版权所有（C）2006，JPO＆NCIPI

3. 发明专利

JP2008111001A 2-acylaminothiazole derivative or salt thereof 有权
标题翻译： 2-氨基苯并噻唑衍生物或其盐
公开(公告)号：JP2008111001A
公开(公告)日：2008-05-15
申请号：JP2008023950
申请日：2008-02-04
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： SUGASAWA KEIZOU , WATANUKI SUSUMU , KOGA YUJI , OSADA HIROSHI , KOHITSU KAZUYOSHI , WAKAYAMA RYUTARO , HIRAYAMA FUKUSHI , SUZUKI KENICHI
IPC分类号： C07D417/12 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/5377 , A61K31/55 , A61P7/04 , A61P43/00 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide a 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies, and to provide a compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia. SOLUTION: The invention relates to the platelet-increasing agent comprising 2-acylaminothiazole derivative, which is represented by formula (I), or a pharmaceutically acceptable salt thereof as an active ingredient. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供具有优异的人c-mpl-Ba / F3细胞增殖效果的2-酰基氨基噻唑衍生物或其药学上可接受的盐，并且基于促进形成巨核细胞集落，并提供可用于治疗血小板减少症的化合物或其药学上可接受的盐。解决方案：本发明涉及包含由式（I）表示的2-酰基氨基噻唑衍生物或其药学上可接受的盐作为活性成分的血小板增加剂。版权所有（C）2008，JPO＆INPIT

4. 发明专利

JP2008094720A Prodrug of quinolone derivative or salt of the same 审中-公开
标题翻译：喹诺酮衍生物或其盐的原料
公开(公告)号：JP2008094720A
公开(公告)日：2008-04-24
申请号：JP2005012715
申请日：2005-01-20
申请人： Astellas Pharma Inc , アステラス製薬株式会社
发明人： KOGA YUJI , OKUDA TAKAO , HIRABAYASHI RYOJI , FUJIYASU JIRO , MIYAZAKI TAKEHIRO , WATANUKI SUSUMU , HIRAYAMA FUKUSHI , MORITANI YUMIKO , TAKASAKI ATSUSHI
IPC分类号： C07D215/56 , A61K31/437 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/502 , A61K31/5377 , A61K31/675 , A61K31/706 , A61P7/02 , A61P43/00 , C07D237/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07F9/6561 , C07H15/203
CPC分类号： C07D215/54
摘要： PROBLEM TO BE SOLVED: To provide a compound having an excellent effect in inhibiting platelet aggregation.
SOLUTION: A prodrug of a quinolone derivative represented by formula (I) or its salt is provided. [In the formula, X is C-R
7 or N etc.; Y is C-R
6 or N etc.; R
11 is -H or lower alkyl etc.; R
12 is -H or lower alkyl etc.; R
2 is lower alkyl or cycloalkyl etc.; R
3 is a halogen or lower alkyl etc.; R
4 is cycloalkyl or non-aromatic heterocycle etc.; R
5 is -H or halogen etc.; R
6 is -H or halogen etc.; R
7 is -H or halogen etc.; when Y is C-R
6 , R
2 and R
6 may together form a lower alkylene or a lower alkenylene, provided that 7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carbohydrazide is excluded].
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供抑制血小板聚集的优异效果的化合物。解决方案：提供由式（I）表示的喹诺酮衍生物或其盐的前药。 [式中，X为C-R 7 或N等。 Y是C-R 6 或N等; R 11是H或低级烷基等; R 12是H或低级烷基等; R 2是低级烷基或环烷基等; R 3是卤素或低级烷基等; R 4是环烷基或非芳族杂环等; R 5是-H或卤素等; R 6 = H或卤素等; R 是-H或卤素等; 当Y是CR 6时，R 2 和R SP 6可以一起形成低级亚烷基或低级亚烯基，条件是7-（环己基氨基） -1-乙基-6-氟-4-氧代-1,4-二氢喹啉-3-碳酰肼]。版权所有（C）2008，JPO＆INPIT

5. 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

6. 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

7. 发明公开

EP1647553A4 2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF 审中-公开
标题翻译： 2-ACYLAMINOTHIAZOLDERIVAT ODER SALZ DAVON
公开(公告)号：EP1647553A4
公开(公告)日：2008-12-31
申请号：EP04747829
申请日：2004-07-15
申请人： ASTELLAS PHARMA INC
发明人： SUGASAWA KEIZO , KOGA YUJI , OBITSU KAZUYOSHI , OKUDA TAKAO , HARADA KOICHIRO , KUBOTA HIDEKI , HIRAYAMA FUKUSHI , ABE MASAKI , SUZUKI KEN-ICHI
IPC分类号： C07D417/04 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/4545 , A61K31/55 , A61P7/00 , A61P7/06 , C07D417/14 , C07D513/14
CPC分类号： C07D417/14 , C07D417/04
摘要： It is intended to provide a 2-acylaminothiazole derivative which has an activity of increasing platelets based on excellent effects of proliferating human c-mpl-Ba/F3 cells and promoting megakaryoblast colony formation and is useful in treating thrombopenia.
摘要翻译：旨在提供基于增殖的人c-mpl-Ba / F3细胞的优异作用并促进巨核母细胞集落形成且具有增加血小板活性的2-酰氨基噻唑衍生物，并且可用于治疗血小板减少症。

9. 发明公开

EP1947086A4 BENZENE DERIVATIVE OR SALT THEREOF 审中-公开
标题翻译：苯衍生物或其盐
公开(公告)号：EP1947086A4
公开(公告)日：2012-01-25
申请号：EP06823046
申请日：2006-11-07
申请人： ASTELLAS PHARMA INC
发明人： HIRAYAMA FUKUSHI , FUJIYASU JIRO , KAGA DAISUKE , NEGORO KENJI , SASUGA DAISUKE , SEKI NORIO , SUZUKI KEN-ICHI
IPC分类号： C07D211/74 , A61K31/435 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/553 , A61P7/02 , A61P9/10 , C07D213/64 , C07D213/75 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12
CPC分类号： C07D213/75 , C07D211/76 , C07D213/64 , C07D239/36 , C07D241/18 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14

10. 发明公开

EP2154130A4 PYRIDONE COMPOUND 审中-公开
标题翻译： PYRIDONVERBINDUNG
公开(公告)号：EP2154130A4
公开(公告)日：2011-09-07
申请号：EP08765230
申请日：2008-06-06
申请人： ASTELLAS PHARMA INC
发明人： KAMIKUBO TAKASHI , HIRAYAMA FUKUSHI , MIURA MASANORI , KOMIYA YURIKO , OKUDA TAKAO , MAKI KEISUKE
IPC分类号： C07D213/64 , A61K31/4412 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61P9/00 , C07D213/69 , C07D401/10 , C07D405/12 , C07D409/06 , C07D413/10
CPC分类号： C07D213/64 , C07D213/69 , C07D401/10 , C07D405/12 , C07D409/06 , C07D413/10

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