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1. 发明申请

WO1993005778A1 BLOOD LIPID METABOLISM AMELIORANT 审中-公开
标题翻译：血液脂肪代谢物
公开(公告)号：WO1993005778A1
公开(公告)日：1993-04-01
申请号：PCT/JP1992001173
申请日：1992-09-14
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , MASUDA, Yoshinobu , MINATO, Hisao , IKENO, Akihisa , TAKEYAMA, Kunihiko , HOSOKI, Kanoo
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/38
CPC分类号： A61K31/495 , C07D337/12
摘要： A blood lipid metabolism ameliorant, in particular, a hyperlipemia inhibitor and an atherosclerosis inhibitor, containing N-(6,11-dihydrobenzo[b,e]thiepin-11-yl)-4-(4-fluorophenyl)-1-piperazin ebutanamide or a physiologically acceptable salt thereof as an active ingredient.
摘要翻译：含有N-（6,11-二氢苯并[b，e]硫杂-11-基）-4-（4-氟苯基）-1-哌嗪基丁酰胺的血脂代谢改善剂，特别是高脂血症抑制剂和动脉粥样硬化抑制剂或其生理学上可接受的盐作为活性成分。

2. 发明申请

WO1987005014A1 TRICYCLIC COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND MEDICINAL COMPOSITION CONTAINING THEM 审中-公开
标题翻译：三氯化合物，其制备方法和含有它们的药物组合物
公开(公告)号：WO1987005014A1
公开(公告)日：1987-08-27
申请号：PCT/JP1987000085
申请日：1987-02-10
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , UNO, Hitoshi , KUROKAWA, Mikio , SATO, Fuminori , NARUTO, Shunsuke , HOSOKI, Kanoo , TAKEYAMA, Kunihiko
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C07C83/10
CPC分类号： C07D409/12 , C07D213/38 , C07D307/14 , C07D307/52 , C07D309/04 , C07D333/20 , C07D333/76 , C07D337/12 , C07D409/14
摘要： Compounds represented by general formula (I), (wherein Y-Z represents (II), -CH=CH- or -CH2CH2-, R1 and R2 each represents a substituent, R3 represents hydrogen, alkyl or alkoxy, R4 represents hydrogen, alkyl, optionally substituted alkenyl, alkynyl, optionally substituted cycloalkyl, phenyl, monocyclic heteroaryl or substituted alkyl, R5 represents phenyl, substituted phenyl or monocyclic heteroaryl, W represents alkylene, X represents a single bond, optionally substituted alkylene, or alkylene interrupted by a group selected from among -O-, -S-, (III) and -CH=CH- or bound to R5 through one of these groups, and a represents an integer of 0 to 2), salts thereof, a process for their preparation, and a medicinal composition containing them. The compounds and the salts show such a strong calcium-antagonistic effect that they are useful for prophylaxis and/or treatment of hypertensive and/or ischemic heart diseases.
摘要翻译：由通式（I）表示的化合物（其中YZ表示（II），-CH = CH-或-CH2CH2-，R1和R2各自表示取代基，R3表示氢，烷基或烷氧基，R4表示氢，烷基，取代的烯基，炔基，任选取代的环烷基，苯基，单环杂芳基或取代的烷基，R 5表示苯基，取代的苯基或单环杂芳基，W表示亚烷基，X表示单键，任选取代的亚烷基或被选自 -O - ， - S - ，（III）和-CH = CH-或通过这些基团之一与R5结合，a表示0至2的整数），其盐，其制备方法和药用包含它们的组合。化合物和盐显示出如此强的钙拮抗作用，它们可用于预防和/或治疗高血压和/或缺血性心脏病。

3. 发明申请

WO1992004339A1 NOVEL PROSTAGLANDIN I2 DERIVATIVES 审中-公开
标题翻译：新型PROSTAGLANDIN I2衍生物
公开(公告)号：WO1992004339A1
公开(公告)日：1992-03-19
申请号：PCT/JP1991001185
申请日：1991-09-05
申请人： ASAHI GLASS COMPANY LTD. , DAINIPPON PHARMACEUTICAL CO., LTD. , ASAI, Tomoyuki , MORIZAWA, Yoshitomi , YASUDA, Arata , YAMAMOTO, Taku , FUJITANI, Buichi , HOSOKI, Kanoo
发明人： ASAHI GLASS COMPANY LTD. , DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C07D307/937
CPC分类号： C07D307/937
摘要： A novel prostaglandin I2 derivative selected from a prostaglandin I2 having a halogen atom on the carbon atom corresponding to the 7-position of natural prostaglandin I2 and having a cycloalkylene group in the α-chain, and its esters and salts.

4. 发明申请

WO1989006129A1 AGENT FOR TREATING ISCHEMIC BRAIN TROUBLE 审中-公开
标题翻译：用于治疗脑缺血的药物
公开(公告)号：WO1989006129A1
公开(公告)日：1989-07-13
申请号：PCT/JP1988001335
申请日：1988-12-27
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , MASUDA, Yoshinobu , KADOKAWA, Toshiaki , KUROKAWA, Mikio , ZUSHI, Kayoko , OCHI, Yoshiaki
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/42
CPC分类号： A61K31/42 , C07D261/20
摘要： An agent for treating ischemic brain troubles which contains 3-sulfamoylmethyl-1,2-benzisoxazole or its alkali metal salt as the active ingredient. This agent can be used for prophylaxis and treatment of intracranial diseases of mammals (including human beings) induced by brain ischemia or various diseases accompanying them.

5. 发明申请

WO1997035963A1 NOVEL BETA-2 ADRENERGIC RECEPTOR SUBTYPE AND USE THEREOF 审中-公开
标题翻译：新型β-2 ADRENERGIC受体亚型及其用途
公开(公告)号：WO1997035963A1
公开(公告)日：1997-10-02
申请号：PCT/JP1997000982
申请日：1997-03-24
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , NOMURA, Akinori , KAWASHIMA, Hitoshi , YANO, Kaori , FUJII, Kaori , FURUTANI, Yasuji
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C12N15/00
CPC分类号： C07K14/70571 , A01K2217/05 , A61K38/00
摘要： A novel beta-2 adrenergic receptor subtype; a DNA coding for the same; a recombinant vector having said DNA; a host cell transformed by said vector; a process for producing said beta-2 adrenergic receptor subtype by culturing said host cell; a method and kit for screening agonists and/or antagonists of said beta-2 adrenergic receptor subtype; and a method of assaying the expression of said beta-2 adrenergic receptor subtype in the cells or tissues. The method of screening agonists of the novel beta-2 adrenergic receptor subtype is useful for the development of remedies for a certain type of asthmatic disease. Recombinant animals genetically engineered with the DNA coding for the beta-2 adrenergic receptor subtype provide useful means for studying the relationship between beta-2 adrenergic receptors and asthmatic diseases.
摘要翻译：一种新型的β-2肾上腺素能受体亚型; 编码相同的DNA; 具有所述DNA的重组载体; 由所述载体转化的宿主细胞; 通过培养所述宿主细胞来产生所述β-2肾上腺素能受体亚型的方法; 用于筛选所述β-2肾上腺素能受体亚型的激动剂和/或拮抗剂的方法和试剂盒; 以及测定细胞或组织中所述β-2肾上腺素能受体亚型的表达的方法。筛选新型β-2肾上腺素能受体亚型的激动剂的方法可用于开发某种类型的哮喘病的药物。用编码β-2肾上腺素能受体亚型的DNA进行遗传工程改造的重组动物为研究β-2肾上腺素能受体与哮喘病之间的关系提供了有用的手段。

6. 发明申请

WO1996020186A1 CARBOXYLIC ACID DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：羧酸衍生物，其制备方法和含有其的药物组合物
公开(公告)号：WO1996020186A1
公开(公告)日：1996-07-04
申请号：PCT/JP1995002686
申请日：1995-12-26
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , MURATA, Makoto , NEGORO, Toshiyuki , UEDA, Shozo , FUJITANI, Buichi , ONO, Yoshiyuki
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C07D311/22
CPC分类号： C07D311/22 , C07D335/06
摘要： A carboxylic acid derivative represented by the following general formula (I): R-CH2COOH, salts thereof, a compound that can be converted into the above compound (I) in vivo, a process for producing these compounds, and a medicinal composition containing the same, wherein R represents a group represented by formula [A] or [B], wherein X represents oxygen or methylene. As these compounds have a potent aldose reductase inhibitory effect, they are useful as a remedy for diabetic complications.
摘要翻译：由以下通式（I）表示的羧酸衍生物：R-CH 2 COOH，其盐，可以在体内转化为上述化合物（I）的化合物，这些化合物的制备方法和含有相同，其中R表示由式[A]或[B]表示的基团，其中X表示氧或亚甲基。由于这些化合物具有强效的醛糖还原酶抑制作用，因此它们可用作糖尿病并发症的治疗方法。

7. 发明申请

WO1996016038A1 2-[2-(INDOL-3-YL)ETHYLAMINO]-1-PHENYLETHANOL DERIVATIVE 审中-公开
标题翻译： 2- [2-（吲哚-3-基）乙酰胺基] -1-苯基乙醇衍生物
公开(公告)号：WO1996016038A1
公开(公告)日：1996-05-30
申请号：PCT/JP1994001941
申请日：1994-11-17
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , KATO, Shiro , HARADA, Hiroshi , MORIE, Toshiya , HIROKAWA, Yoshimi , YOSHIDA, Naoyuki
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C07D209/14
CPC分类号： C07D209/16
摘要： A 2-[2-(indol-3-yl)ethylamino]-1-phenylethanol derivative represented by general formula (I) and a pharmaceutically acceptable acid-addition salt thereof, wherein R1 stands for halogen or trifluoromethyl; R2 stands for hydrogen, lower alkyl or fluorinated lower alkyl; and R3 stands for hydrogen, halogen, trifluoromethyl, nitro or cyano. This compound has a highly selective activity of stimulating beta 3 adrenaline receptors and is usable for treating or preventing diabetes, obesity, irritable bowel syndrome, acute or chronic diarrhea and so forth, and also for ameliorating syndromes accompanying peptic ulcer, acute or chronic gastritis, and so forth, such as abdominal pain, nausea, vomiting and epigastric discomfort.
摘要翻译：由通式（I）表示的2- [2-（吲哚-3-基）乙基氨基] -1-苯基乙醇衍生物及其药学上可接受的酸加成盐，其中R1代表卤素或三氟甲基; R2代表氢，低级烷基或氟化低级烷基; R3代表氢，卤素，三氟甲基，硝基或氰基。该化合物具有刺激β3肾上腺素受体的高选择性活性，可用于治疗或预防糖尿病，肥胖症，肠易激综合征，急性或慢性腹泻等，以及用于改善伴随消化性溃疡，急性或慢性胃炎的综合征，等等，如腹痛，恶心，呕吐和上腹部不适。

8. 发明申请

WO1992019737A1 PROCESS FOR PRODUCING A MONOCYTE CHEMOTACTIC FACTOR POLYPEPTIDE AND A STRAIN FOR THE PRODUCTION THEREOF 审中-公开
标题翻译：生产单体化学因子多肽的方法及其生产菌株
公开(公告)号：WO1992019737A1
公开(公告)日：1992-11-12
申请号：PCT/JP1992000550
申请日：1992-04-27
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , YAMAGISHI, Junichi , MATSUO, Noriyuki , FUKUI, Toshikazu , YAMADA, Masaaki
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C12N15/19
CPC分类号： C07K14/523 , C12N15/71
摘要： A process for producing a monocyte chemotactic factor which comprises constructing an expression plasmid in which has been inserted DNA encoding a monocyte chemotactic factor consisting of 76 amino acids or a polypeptide which has truncated N-terminal amino acids thereof and having a terminator sequence inserted downstream of said DNA, introducing the expression plasmid into a selected E. coli such as an E. coli LE392 strain or the like to transform said E. coli, and cultivating the transformed E. coli.
摘要翻译：一种生产单核细胞趋化因子的方法，其包括构建其中已插入编码由76个氨基酸组成的单核细胞趋化因子的DNA的表达质粒或其截短的N-末端氨基酸的多肽，并且具有插入到所述DNA将表达质粒导入到选择的大肠杆菌如大肠杆菌LE392菌株等中以转化所述大肠杆菌，并培养转化的大肠杆菌。

9. 发明申请

WO1998042701A1 3-OXADIAZOLYLQUINOXALINE DERIVATIVES 审中-公开
标题翻译： 3-氧代二氢喹啉衍生物
公开(公告)号：WO1998042701A1
公开(公告)日：1998-10-01
申请号：PCT/JP1998000827
申请日：1998-02-27
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , OHNO, Kazunori , ODAI, Osamu , FURUKAWA, Kiyoshi , OKA, Makoto
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C07D413/04
CPC分类号： C07D413/04
摘要： Novel 3-oxadiazolylquinoxaline derivatives represented by general formula (I), wherein Het is oxadiazolyl; R is hydrogen, lower alkyl, trifluoromethyl, lower cycloalkyl, lower alkenyl, lower alkynyl, optionally substituted aryl, optionally substituted heteroaryl, or lower alkoxy; R is hydrogen, lower alkyl, trifluoromethyl, lower cycloalkyl, halogeno, hydroxy, lower alkoxy, cyano, nitro, acyl, optionally substituted benzoyl, amino, lower mono- or dialkylamino, lower alkoxycarbonylmethyloxy, lower mono- or dialkylaminocarbonylmethyloxy, or optionally substituted benzyloxy; and R is hydrogen, lower alkyl, lower cycloalkyl, halogeno, or lower alkoxy, which are useful as a medicine, in particular, which have a selective affinity for benzodiazepine receptors and are useful as a brain activator and a remedy for senile dementia and Alzheimer's disease.
摘要翻译：由通式（I）表示的新型3-恶二唑基喹喔啉衍生物，其中Het是恶二唑基; R 1是氢，低级烷基，三氟甲基，低级环烷基，低级烯基，低级炔基，任选取代的芳基，任选取代的杂芳基或低级烷氧基; R 2是氢，低级烷基，三氟甲基，低级环烷基，卤代，羟基，低级烷氧基，氰基，硝基，酰基，任选取代的苯甲酰基，氨基，低级单烷基氨基或二烷基氨基，低级烷氧基羰基甲氧基，低级单或二烷基氨基羰基甲氧基，或任选取代的苄氧基; R 3为氢，低级烷基，低级环烷基，卤代或低级烷氧基，其可用作药物，特别是对苯并二氮杂受体具有选择性亲和力，可用作脑活化剂和老年化疗法痴呆和阿尔茨海默病。

10. 发明申请

WO1998016519A1 ['omega'-(2,3-DIHYDRO-1-BENZOXEPIN-4-YL)ALKYL]AMINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, AND MEDICINAL COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译： [ω-（2,3-二氢-1H-苯并[4-YL]烷基]胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：WO1998016519A1
公开(公告)日：1998-04-23
申请号：PCT/JP1997003672
申请日：1997-10-14
申请人： DAINIPPON PHARMACEUTICAL CO., LTD. , MORIE, Toshiya , KANEHIRA, Aki , KAI, Naoki , HINO, Katsuhiko , KAWASHIMA, Katsuyoshi , SHIMIZU, Isao , AKIYAMA, Kazuhisa
发明人： DAINIPPON PHARMACEUTICAL CO., LTD.
IPC分类号： C07D313/08
CPC分类号： C07D313/08
摘要： [ omega -(2,3-Dihydro-1-benzoxepin-4-yl)alkyl]amine derivatives represented by general formula (I), and salts and N-oxide derivatives thereof; a process for the preparation of them; and medicinal compositions containing the same as formula (I) (wherein R and R are each hydrogen, halogeno, alkyl, alkoxy or the like, or alternatively R and R may be united to form ethyleneoxy, trimethylene or the like; R is hydrogen, alkyl or the like; R is hydrogen, alkyl, acyl or the like, and R is cycloalkyl, or alternatively R and R may form together with the adjacent nitrogen atom a cyclic amino group; and p is an integer of 2 to 6). The compounds exhibit a potent inhibitory activity against micturition reflex, being useful as remedies for pollakiuria and urinary incontinence.
摘要翻译：由通式（I）表示的[ω-（2,3-二氢-1-苯并氧杂-4-基）烷基]胺衍生物及其盐和N-氧化物衍生物; 它们的制备过程; 和含有与式（I）相同的药物组合物（其中R 1和R 2各自为氢，卤代，烷基，烷氧基等，或者R 1和R 2可以相互结合形成亚乙氧基，三亚甲基等; R 3是氢，烷基等; R 4是氢，烷基，酰基等，R 5是环烷基，或者R 4和R <5>可以与相邻的氮原子一起形成环状氨基，p为2〜6的整数。该化合物对排尿反射表现出有效的抑制活性，可用作尿频尿失禁和尿失禁的补救措施。

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