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1. 发明授权

EP1010699B1 5-SUBSTITUTED-3-OXADIAZOLYL-1,6-NAPHTHYRIDIN-2(1H)-ONE DERIVATIVES 失效
标题翻译： IN 5-取代的3-恶二唑基-1,6-萘啶-2（1H） - 酮衍生物
公开(公告)号：EP1010699B1
公开(公告)日：2005-06-15
申请号：EP98931076.8
申请日：1998-07-14
申请人： DAINIPPON PHARMACEUTICAL CO., LTD.
发明人： OHNO, Kazunori , ODAI, Osamu , MASUMOTO, Kaoru , FURUKAWA, Kiyoshi , OKA, Makoto
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： Novel 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives represented by general formula (I) wherein Het represents oxadiazolyl; R1 represents H, lower alkyl, lower cycloalkyl, lower alkenyl, lower alkoxy, optionally substituted aryl, optionally substituted heteroaryl, etc.; and R2 represents H, lower alkyl, lower cycloalkyl, optionally substituted aryl, etc. Because of having high affinities selectively with benzodiazepine receptors, these compounds are useful as benzodiazepine receptor agonists, in particular, inverse agonists thereof, for example, brain activators and remedies for memory disorders associating senile dementia, Alzheimer's disease, etc.

2. 发明授权

EP1040830B1 REMEDY FOR NEURODEGENERATIVE DISEASES 有权
标题翻译：救济神经退行性疾病
公开(公告)号：EP1040830B1
公开(公告)日：2005-06-08
申请号：EP98961430.0
申请日：1998-12-21
申请人： Dainippon Pharmaceutical Co., Ltd.
发明人： MASUDA, Yoshinobu , OCHI, Yoshiaki
IPC分类号： A61K31/42 , C07D261/20 , A61K31/423 , A61P25/16 , A61P25/28
CPC分类号： A61K31/423 , A61K31/42 , Y10S514/878 , Y10S514/879
摘要： A remedy for neurodegenerative diseases containing zonisamide or an alkali metal salt thereof as the active ingredient and usable for preventing and remedying mammalian (including human) neurodegenerative diseases such as Parkinson's disease, Huntington's disease, choreic syndrome and dystonic syndrome.

3. 发明授权

EP1033132B1 RAPIDLY SOLUBLE DRUG COMPOSITION COMPRISING MICRONIZED AS-3201 有权
标题翻译： FAST性药物成分含微粉化AS-3201
公开(公告)号：EP1033132B1
公开(公告)日：2005-05-25
申请号：EP98947883.9
申请日：1998-10-15
申请人： Dainippon Pharmaceutical Co., Ltd.
发明人： OHASHI, Mamoru , OGASAWARA, Kazuyoshi , SHIRAI, Yoshimi , FUJIOKA, Hiroshi
IPC分类号： A61K31/495 , A61K9/20 , A61K47/12
CPC分类号： A61K9/2054 , A61K9/2013 , A61K31/499 , A61K47/02 , A61K47/12 , Y10S514/951 , Y10S514/96
摘要： A rapidly soluble drug composition containing pulverized (R)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3'-pyrrolidine-1,2',3,5'-tetraone (AS-3201). It is improve d in dissolution and has a good bioavailability.

4. 发明授权

EP0748869B1 ECTOINE SYNTHETASE GENE 失效
标题翻译： ECTOINE合成酶基因
公开(公告)号：EP0748869B1
公开(公告)日：2005-01-26
申请号：EP94931196.3
申请日：1994-11-01
申请人： DAINIPPON PHARMACEUTICAL CO., LTD.
发明人： TAKANO, Mitsuo , ONO, Hisayo , YAMADA, Hiroyuki , YAMATOYA, Kazuhiko
IPC分类号： C12N15/00
CPC分类号： C12N15/8273 , C07K14/215 , C12N9/00
摘要： The base sequence of a DNA coding for an ectoine synthetase has been determined by isolating a gene coding for an enzyme participating in ectoine synthesis in the form of a DNA with about 4.2 kilobase pairs obtained by cleaving a Halomonas KS-3 strain gene DNA with restriction enzymes Eco RI and Sal I. By introducing the obtained gene DNA into Escherichia coli , it is possible to impart the capability of synthesizing ectoine and the character of high osmotic pressure resistance, thus permitting the development of an efficient fermentation technique utilizing the resultant transformant and the creation of drought-resistant plants.
摘要翻译：已经通过分离编码参与ectoine合成的酶的基因的DNA碱基序列来确定，所述DNA以具有约4.2千碱基对的DNA形式通过用限制性切割盐生哈尔纳萨姆KS-3菌株基因DNA 酶EcoRI和SalI。通过将获得的基因DNA导入大肠杆菌中，可以赋予合成ectoine的能力和高渗透压性的特性，从而允许开发利用所得转化体和产生抗旱植物的有效发酵技术。

5. 发明公开

EP1491896A1 METHOD OF JUDGING CARDIOTOXICITY OF ANTHRACYCLINE-TYPE ANTICANCER CHEMICAL THERAPEUTIC BY DETECTING HUMAN H-FABP AND REAGENT THEREFOR 审中-公开
标题翻译：评估方法的心脏毒性抗癌从检测到人H-FABP和试剂的THEREFOR的化疗蒽环类TYPE
公开(公告)号：EP1491896A1
公开(公告)日：2004-12-29
申请号：EP03715565.2
申请日：2003-03-28
申请人： Dainippon Pharmaceutical Co., Ltd.
发明人： KITAYAMA, Hitoshi , OHKARU, Yasuhiko
IPC分类号： G01N33/68 , G01N33/53 , G01N33/15
CPC分类号： G01N33/92 , G01N33/5014
摘要： The present invention provides a method of determining toxicity to the heart of an anthracycline-type anticancer chemotherapeutic agent such as adriamycin etc., which comprises detecting human H-FABP (Human Heart-type Fatty Acid-Binding Protein) in the blood separated from human, a reagent therefor, a kit therefor and the like.
摘要翻译：蒽环型抗癌剂确定性采矿心脏毒性的方法包括检测人类心脏脂肪酸在人体血液结合蛋白（H-FABP）。因此独立权利要求中包括了的试剂和用于进行上述方法的试剂盒。

6. 发明公开

EP1473302A1 HETEROCYCLIC COMPOUNDS HAVING ELASTASE−INHIBITING ACTIVITY AND INTERMEDIATES THEREOF 审中-公开
标题翻译：兽医学家VERBINDUNGEN MIT ELASTASEHEMMENDER WIRKUNG UND ZWISCHENPRODUKTEDAFÜR
公开(公告)号：EP1473302A1
公开(公告)日：2004-11-03
申请号：EP03737491.5
申请日：2003-02-05
申请人： Dainippon Pharmaceutical Co., Ltd.
发明人： SATO, Fuminori , DEGUCHI, Takashi , SHIRATAKE, Ryotaro , OKAZAKI, Hiroshi , KUROMIYA, Akemi
IPC分类号： C07K5/083 , C12N9/99 , A61K38/55 , A61P11/00 , A61P43/00
CPC分类号： C07K5/06191 , A61K38/00
摘要： Heterocyclic compounds represented by the general formula (I) and having elastase inhibiting activity; and intermediates for the synthesis thereof: (I) wherein R 1 is a heterocyclic group represented by the general formula (II): (II) [wherein A represents the presence or absence of a benzene ring; X is oxygen, sulfur or NH; and Y is nitrogen or CH], and the heterocyclic group may be substituted with one to three substituents which may be the same or different and are selected from the group consisting of lower alkyl, lower alkoxy, and phenyl which may be substituted with optionally halogenated lower alkyl, lower alkoxy or halogeno; and R 2 and R 3 are each hydrogen or hydroxyl, or R 2 and R 3 may be united to form an oxo group, with the proviso that both are not hydrogen.
摘要翻译：具有通式（I）表示的并具有弹性蛋白酶抑制活性的杂环化合物及其合成中间体：（I）其中R 1为通式（II）表示的杂环基：（Ⅱ）Ä其中A表示苯环的存在或不存在; X是氧，硫或NH; 并且Y是氮或CH，并且杂环基可以被一至三个可以相同或不同并且选自低级烷基，低级烷氧基和可被任选卤代低级取代的苯基的取代基取代烷基，低级烷氧基或卤代; R 2和R 3各自为氢或羟基，或者R 2和R 3可以一起形成氧代基，条件是两者都不是氢。

7. 发明公开

EP1403235A1 N-ARYLPHENYLACETAMIDE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：正丁基苯甲酸氨基甲酸酯在食品包装中的应用ZUSAMMENSETZUNGEN
公开(公告)号：EP1403235A1
公开(公告)日：2004-03-31
申请号：EP02733338.4
申请日：2002-06-06
申请人： Dainippon Pharmaceutical Co., Ltd.
发明人： MORIE, Toshiya , ADACHI, Keiji , NIIDOME, Kazumi , KAWASHIMA, Katsuyoshi , SHIMIZU, Isao , ISHII, Daisuke
IPC分类号： C07C1/00
CPC分类号： A61K31/4164 , A61K31/167 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/385 , A61K31/40 , A61K31/404 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/4453 , A61K31/451 , A61K31/47 , A61K31/505 , A61K31/5375 , A61K31/55 , C07C235/38 , C07C311/08 , C07C311/46 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2603/18 , C07C2603/74 , C07D333/20
摘要： N-Arylphenylacetamide derivatives represented by the following formula [I]:
(wherein R 1 is C 1-6 alkoxy, etc.; R 2 is hydrogen, -(CH 2 ) m -N(R 6 )(R 7 ) (m is an integer of from 1 to 4; R 6 is hydrogen, C 1-4 alkyl, etc., R 7 is hydrogen, etc.), etc.; R 3 is hydrogen, halogen, etc.; R 4 is C 6-10 alkyl, -Y-R 8 (Y is a single bond, C 1-6 alkylene, C 2-6 alkenylene, C 2-6 alkynylene, etc., R 8 is aryl, C 3-8 cycloalkyl, C 6-15 polycycloalkyl, etc.), etc.; R 5 is hydrogen, etc.; and X 1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.
摘要翻译： N-芳基苯乙酰胺衍生物（I）是新的。式（I）的N-芳基苯基乙酰胺衍生物及其盐，水合物和溶剂化物是新的。 R 1OAlk，OH，卤素，NO 2，NH 2，NHAlk，N（Alk）2，NHSO 2 Al或NHSO 2r; Alk：1-6C烷基; Ar：芳基; R 2H，COAlk，COAr，（CH 2）mNR 6R 7，（CH 2）mOH或（CH 2）qCOOH; m：0-2; q：1-4; R 6Alk 1,2或3C羟烷基，2或3C氨基烷基，CHO，COAlk 1，1-4C烷氧基羰基，COAr或COOAlk 1Ar; R 7H，Alk 1,2或3C羟烷基或2或3C氨基烷基; R 3H，卤素，Alk，1-4C烷氧基，Ar或CHO; Alk 11-3C烷基; R 46-10C烷基，YR 8或哌啶-1-基，吗啉-4-基或硫代吗啉-4-基，其全部任选被1或2个Alk，Cyc，卤素，CF 3，1-4C烷氧基羰基，Ar，AlkAr ，OAlk 1或OH或螺环; Y：键，1-3C亚烷基，2或3个亚烷基，2或3个亚烷基，CO（CH 2）p，2或3C亚烷基羰基，O，O（CH 2）2，O（CH 2）3或CONH 2）p; p：0-3; 环：3-7C环烷基; R 8Ar 1（任选被1-3个卤素，Alk，Cyc，2-6C烯基，2-6C炔基，CF 3，三氟乙基，Ar，AlkAr，OAlk，OCF 3，OCCl，OAr，OAlk 1Ar，COOAlk，COCyc ，CHO，NO 2，NH 2，N（Alk）2，CN，OH，SAlk 1，1-4C烷氧基羰基1-3C烷基，Alk 1COOH，1-4C烷氧基羰基，COOAlk 1Ar，COOH或SO 2 NH 2） 5-7C环烯基（任选被1-4个Alk，Cyc，卤素，CF 3，1-4C烷氧基羰基，Ar，AlkAr，OAlk 1或OH取代）或式（i）的基团; 任选含有1-3个N，O或S的Ar 15或6元单环或多环芳基; R a-R dH，Alk，Cyc，卤素，CF 3，1-4C烷氧基羰基，Ar，AlkAr，OAlk 1或OH; 或R a + R b O或S; 或R c + R dspiro环; 或R a + R b + R c6-15C多环烷基; n：1-6; R 5H，卤素，Alk，CF 3，OAlk 1，OCF 3，CN，NH 2，NO 2，OH，COOH，CH 2 OCOAlk或Ar; 或R 4 + R 5稠合的四氢萘酮或吲哚环，其任选被1-8C烷基，1-8C烯基（sic），Alk1Ar，Alk1Cyc，SO2-2，1-8C亚烷基（任选被Ar或Cyc取代）或1- 8C亚链烯基（sic）; 条件是当R 4para-YR 8和Y = 1-3C亚烷基或2或3亚烷基时，R 8不是任选被NH 2，Alk，Ar或SAlk 1取代的吡咯基，吡唑基，咪唑基，三唑基或嘧啶基。活性：止痛; 躁狂; 抗过敏; 抗炎; 抗关节炎; 抗风湿; Uropathic; 脑保护; 平喘; 皮肤; 眼科; 抗溃疡; 厌食。在ddY小鼠中的苯基-1,4-苯醌诱导的扭体试验中，N-（3-环己基苯基）-4-羟基-3-甲氧基苯乙酰胺（Ia）的ED 5 0值为0.014mg / kg。相比之下，1.15 mg / kg s.c. 为辣椒素。作用机制：香草素拮抗剂。

8. 发明授权

EP0913159B1 DRUG DELIVERY SYSTEM USING GALACTOXYLOGLUCAN 失效
标题翻译：药监系统使用galactoxyloglucan
公开(公告)号：EP0913159B1
公开(公告)日：2002-09-25
申请号：EP97902673.9
申请日：1997-02-13
申请人： DAINIPPON PHARMACEUTICAL CO., LTD.
发明人： MIYAZAKI, Shozo , SHIRAKAWA, Mayumi , YAMATOYA, Kazuhiko
IPC分类号： A61K47/36 , A61K9/22
CPC分类号： A61K9/02 , A61K9/205 , A61K47/36 , Y10S514/964
摘要： A sustained release preparation of a drug and a method for the sustained release of a drug by using a degradation product of the galactose moiety of galactoxyloglucan as the sustained release ingredient. In the above preparation and method, more particularly, it is intended to achieve the sustained release of a drug by using the reversible heat-responding gelation of a degradation product of the galactose moiety of galactoxyloglucan obtained by partly eliminating the side chain galactose therefrom with the use of an enzyme.

9. 发明公开

EP1236721A1 5-CHLORO-6-PHENYL-2-(4-TRIFLUOROMETHYLPHENYL)-4-PYRIMIDINYLAMINO]ACETAMIDE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATE OF THESE COMPOUNDS 审中-公开
标题翻译： 5-氯-6-苯基-2-（4-三氟甲基苯基）-4-嘧啶基氨基乙酰胺衍生物，含有该医药制剂和中间体，这些化合物
公开(公告)号：EP1236721A1
公开(公告)日：2002-09-04
申请号：EP00974834.4
申请日：2000-11-09
申请人： Dainippon Pharmaceutical Co., Ltd.
发明人： Murata, Teruya , Ohno, Kazunori , Tanaka, Masayasu , Itoh, Mari
IPC分类号： C07D239/42 , A61K31/505 , A61P29/00 , A61P37/06
CPC分类号： C07D239/42
摘要： A [5-chloro-6-phenyl-2-(4-trifluoromethylphenyl)-4-pyrimidinylamino]acetamide derivative of the formula (I):
wherein R 1 is a methyl group or a cyclopropyl group, and a pharmaceutical composition containing the same. Said compounds exhibit a potent anti-rheumatoid activity and show low toxicity, and hence, they are useful as an agent for prophylaxis or treatment of immuno inflammatory diseases such as rheumatoid diseases (e.g., rheumatoid arthritis, Behçet disease, ankylosing spondylitis, etc.) and autoimmune diseases (e.g., multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, etc.).
摘要翻译：甲AE5氯-6-苯基-2-（4-三氟甲基苯基）的式（I）-4-pyrimidinylaminoÜacet酰胺衍生物： worin - [R <1>是甲基或环丙基，和药物组合物含有相同。所述的化合物表现出有效的抗风湿活性，并显示低毒性，并因此，它们作为用于免疫炎性疾病的预防或治疗剂是有用的：例如类风湿疾病（例如，类风湿关节炎，贝切特病，强直性脊柱炎，等等）（例如综合征，多发性硬化，系统性红斑狼疮，SJ |舍格伦等）和自身免疫性疾病。

10. 发明公开

EP1235801A2 SOLID PHARMACEUTICAL PREPARATION 审中-公开
标题翻译： FIXED药物配制
公开(公告)号：EP1235801A2
公开(公告)日：2002-09-04
申请号：EP00977904.2
申请日：2000-11-24
申请人： Dainippon Pharmaceutical Co., Ltd.
发明人： IWATA, Motokazu , KURIYAMA, Teruaki , FUJITA, Megumi , FUJIWARA, Keiichi216, Suncity-Katsurazaka-Royal , KATO, Shiro , HARADA, Hiroshi , FUJII, Akihito , ODAI, Osamu , KAWASHIMA, Hitoshi
IPC分类号： C07D209/16 , A61K31/404 , A61P3/04
CPC分类号： C07D209/16
摘要： The present invention provides a solid preparation comprising a crystal of [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid (Compound A), especially a crystal of Compound A having a particle size of not larger than 100 νm at the cumulative weight distribution value of 50 %, and not larger than 200 νm at the cumulative weight distribution value of 95 %, preferably a solid preparation having the excellent stability and the content uniformity of Compound A, which is prepared by preparing granules of the crystal of Compound A with fillers, disintegrants and binders, and then followed by mixing said granules with external excipients.

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