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1. 发明申请

WO1995022329A1 AGENT FOR PROPHYLAXIS AND TREATMENT OF THROMBOXANE A2-MEDIATED DISEASES 审中-公开
标题翻译：丙型肝炎治疗和治疗甲硫氨酸A2介导性疾病
公开(公告)号：WO1995022329A1
公开(公告)日：1995-08-24
申请号：PCT/JP1995000244
申请日：1995-02-20
申请人： THE GREEN CROSS CORPORATION , NISSAN CHEMICAL INDUSTRIES, LTD. , IKEGAWA, Ruriko , IMADA, Teruaki , NAKAMURA, Norifumi , TANIKAWA, Keizo , TSURUZOE, Nobutomo
发明人： THE GREEN CROSS CORPORATION , NISSAN CHEMICAL INDUSTRIES, LTD.
IPC分类号： A61K31/50
CPC分类号： A61K31/501 , A61K31/50
摘要： An agent for the prophylaxis or treatment of TXA2-mediated diseases, particularly, a TXA2 synthetase inhibitor, which comprises a pyridazinone compound of formula (I), wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof as an active ingredient. The pyridazinone compound (I) and pharmacologically acceptable salts thereof used in the present invention have prophylactic and therapeutic activities against TXA2-mediated diseases, particularly a TXA2 synthetase inhibitory action and are useful as an agent for the prophylaxis or treatment of TXA2-mediated diseases, particularly as TXA2 synthetase inhibitors.
摘要翻译：用于预防或治疗TXA2介导的疾病的药剂，特别是TXA2合成酶抑制剂，其包含式（I）的哒嗪酮化合物，其中每个符号如说明书中所定义，或其药理学上可接受的盐作为活性物质成分。用于本发明的哒嗪酮化合物（I）及其药理学上可接受的盐具有抗TXA2介导的疾病，特别是TXA2合成酶抑制作用的预防和治疗活性，可用作预防或治疗TXA2介导的疾病，特别是作为TXA2合成酶抑制剂。

2. 发明申请

WO1995033720A1 NOVEL FUSED-RING CARBOXYLIC ACID COMPOUND OR SALT THEREOF, AND MEDICINAL USE THEREOF 审中-公开
标题翻译：新颖的环氧化羧酸化合物或其盐，以及药物使用
公开(公告)号：WO1995033720A1
公开(公告)日：1995-12-14
申请号：PCT/JP1995001119
申请日：1995-06-06
申请人： THE GREEN CROSS CORPORATION , ONO, Shinichiro , YOSHIDA, Tomohiro , ASHIMORI, Atsuyuki , KOSAKA, Keigo , OKADA, Takehiro , MAEDA, Kazuhiro , EDA, Masahiro , MORI, Fumio , INOUE, Yoshihisa , EBISU, Hajime , IMADA, Teruaki , IKEGAWA, Ruriko , WANG, Feng , NAKAMURA, Norifumi
发明人： THE GREEN CROSS CORPORATION
IPC分类号： C07D209/42
CPC分类号： C07D491/04 , C07D209/42 , C07D307/84 , C07D307/85 , C07D333/62 , C07D333/68
摘要： A novel fused-ring carboxylic acid compound represented by general formula (I) or a pharmacologically acceptable salt thereof; a medicinal composition thereof; and a medicinal use thereof, wherein each symbol is as defined in the specification. The compound and salt have an excellent GPIIb/IIIa antagonism against mammals including humans, can be administered orally, have a long life in blood and a low toxicity, and are reduced in side effects, thus being very useful for preventing or treating thrombotic diseases.
摘要翻译：一种由通式（I）表示的新型稠环羧酸化合物或其药学上可接受的盐; 其药用组合物; 及其医疗用途，其中每个符号如说明书中所定义。该化合物和盐对包括人在内的哺乳动物具有优异的GPIIb / IIIa拮抗作用，可口服给药，血液中的使用寿命长，毒性低，并且副作用减少，因此对预防或治疗血栓性疾病非常有用。

3. 发明申请

WO1998018794A1 NOVEL HETEROCYCLIC AMIDE COMPOUNDS AND MEDICINAL USES THEREOF 审中-公开
标题翻译：新型杂环化合物及其药物用途
公开(公告)号：WO1998018794A1
公开(公告)日：1998-05-07
申请号：PCT/JP1997003839
申请日：1997-10-22
申请人： THE GREEN CROSS CORPORATION , AKAHOSHI, Fumihiko , ASHIMORI, Atsuyuki , YOSHIMURA, Takuya , EDA, Masahiro , SAKASHITA, Hiroshi , NAKAJIMA, Masahide , IMADA, Teruaki
发明人： THE GREEN CROSS CORPORATION
IPC分类号： C07D413/12
CPC分类号： C07K5/06139 , A61K38/00
摘要： Heterocyclic amide compounds represented by general formula (I) or pharmacologically acceptable salts thereof; medicinal compositions thereof; and medicinal uses of the same wherein each symbol is as defined in the specification. These compounds and pharmacologically acceptable salts thereof have excellent effects of inhibiting chymases on mammals including human being and can be administered orally or parenterally. Thus, they are useful as chymase inhibitors in preventing and treating various diseases caused by chymases typified by those caused by angiotensin II.
摘要翻译：由通式（I）表示的杂环酰胺化合物或其药学上可接受的盐; 其药用组合物; 和其药物用途，其中每个符号如说明书中所定义。这些化合物及其药理学上可接受的盐具有抑制糜酶对包括人在内的哺乳动物的优异效果，并且可以口服或肠胃外给药。因此，它们作为胃促胰酶抑制剂可用于预防和治疗由血管紧张素II引起的糜肠炎引起的各种疾病。

4. 发明申请

WO1996033974A1 HETEROCYCLIC AMIDE COMPOUNDS AND MEDICINAL USE OF THE SAME 审中-公开
标题翻译：杂环酰胺化合物及其药物用途
公开(公告)号：WO1996033974A1
公开(公告)日：1996-10-31
申请号：PCT/JP1996001171
申请日：1996-04-26
申请人： THE GREEN CROSS CORPORATION , AKAHOSHI, Fumihiko , YOSHIMURA, Takuya , EDA, Masahiro , ASHIMORI, Atsuyuki , FUKUYAMA, Hajime , NAKAJIMA, Masahide , IMADA, Teruaki , OKUNISHI, Hideki , MIYAZAKI, Mizuo
发明人： THE GREEN CROSS CORPORATION
IPC分类号： C07D213/64
CPC分类号： C07D213/73 , C07D213/75 , C07D239/47
摘要： Heterocyclic compounds represented by general formula (I) or pharmacologically acceptable salts of the same and a medicinal composition comprising the same, wherein each symbol has the meaning as defined in the specification. The heterocyclic amide compounds and pharmacologically acceptable salt thereof have excellent effects of inhibiting chymases on mammals including human being and can be orally or parenterally administered. Thus they are useful as a chymase inhibitor and can be used in the prevention and treatment of various diseases caused by chymases such as those caused by angiotensin II.
摘要翻译：由通式（I）表示的杂环化合物或其药理学上可接受的盐及包含其的药用组合物，其中每个符号具有说明书中定义的含义。杂环酰胺化合物及其药理学上可接受的盐具有抑制糜烂酶对包括人在内的哺乳动物的口服或肠胃外给药的优异效果。因此，它们可用作胃促胰酶抑制剂，并且可用于预防和治疗由糜酶如由血管紧张素II引起的各种疾病引起的各种疾病。

5. 发明申请

WO1997001533A1 THIOCARBAMIC ACID DERIVATIVES 审中-公开
标题翻译：甲硫氨酸衍生物
公开(公告)号：WO1997001533A1
公开(公告)日：1997-01-16
申请号：PCT/JP1996001776
申请日：1996-06-27
申请人： THE GREEN CROSS CORPORATION , TOSOH CORPORATION , ISHIDA, Naomichi , GODA, Maki , YAMAURA, Yasunari , INOUE, Yoshihisa , NAKAMURA, Norifumi , TOKUNAGA, Takumi , HAGA, Kenichi , TOKUHISA, Kenji , KATSUURA, Kimio , HANASAKI, Yasuaki
发明人： THE GREEN CROSS CORPORATION , TOSOH CORPORATION
IPC分类号： C07C333/04
CPC分类号： C07D207/323 , C07C333/04 , C07C333/08 , C07D277/42 , C07D333/36 , C07D333/38
摘要： Thiocarbamic acid derivatives represented by general formula (I) and salts thereof, wherein m is 0 or 1; A is 4,4-dimethyl-2-pentynyl or the like; R and R are each hydrogen, formyl or lower alkyl; Z is nitrogen or CH; R is hydrogen, lower alkyl, lower acyl or like; R is a phenyl group having an arbitrary substituent or a 5- or 6-membered heterocycle containing at least one atom of oxygen, nitrogen or sulfur or a combination of two or more of them, the heterocycle being optionally substituted by an arbitrary group. They provide an antihypercholesterolemic agent, an antihyperlipemic agent, and a remedy or preventive for arteriosclerosis, each being safer than conventional drugs and exhibiting excellent anticholesterol activity.
摘要翻译：由通式（I）表示的硫代氨基甲酸衍生物及其盐，其中m为0或1; A是4,4-二甲基-2-戊炔基等; R 1和R 3各自为氢，甲酰基或低级烷基; Z是氮或CH; R 2是氢，低级烷基，低级酰基等; R 4是具有任意取代基的苯基或含有至少一个氧原子，氮原子或硫原子的5或6元杂环或其两个或多个的组合，该杂环任选被任意取代组。它们提供抗高胆固醇血症药，抗高血脂药，以及用于动脉硬化的治疗或预防药物，每种药物比常规药物更安全，并显示出优异的抗胆固醇活性。

6. 发明申请

WO1998008514A1 PREVENTIVES/REMEDIES FOR MUSCLE TISSUE DEGENERATIONS 审中-公开
标题翻译：肌肉组织变性的预防/补救措施
公开(公告)号：WO1998008514A1
公开(公告)日：1998-03-05
申请号：PCT/JP1997002992
申请日：1997-08-27
申请人： THE GREEN CROSS CORPORATION , ASAHI GLASS CO., LTD. , NAKAMURA, Norifumi , KOYAMA, Mamoru , MIYAZAKI, Mizuo
发明人： THE GREEN CROSS CORPORATION , ASAHI GLASS CO., LTD.
IPC分类号： A61K31/47
CPC分类号： C07D471/04 , Y10S514/907
摘要： Preventives/remedies for muscle tissue degenerations containing as the active ingredient quinoline compounds represented by general formula (I) or pharmaceutically acceptable salts thereof. The preventives/remedies exert remarkable inhibitory and improving effects on muscle tissue degenerations such as necrosis, fibrosis or calcification. Thus, they are useful in the prevention and treatment of, in particular, cardiomyopathy, muscular dystrophy, pulmonary fibrosis, etc.
摘要翻译：含有作为活性成分的通式（I）表示的喹啉化合物或其药学上可接受的盐的肌肉组织变性的预防/治疗。预防措施/补救措施对肌肉组织变性如坏死，纤维化或钙化具有显着的抑制和改善作用。因此，它们可用于预防和治疗特别是心肌病，肌营养不良症，肺纤维化等。

7. 发明申请

WO1994023721A1 NOVEL MEDICINAL USE OF DIHYDROPYRIDINE DERIVATIVE 审中-公开
标题翻译：二氢吡啶衍生物的新药物使用
公开(公告)号：WO1994023721A1
公开(公告)日：1994-10-27
申请号：PCT/JP1994000460
申请日：1994-03-22
申请人： THE GREEN CROSS CORPORATION , NAKAJIMA, Masahide , NAKAMURA, Norifumi , WANG, Feng , YAMANOUCHI, Koichi , HAYASHI, Kazutaka , KIDO, Hideaki , KUBO, Yoshiji , OKITA, Minori , UCHIDA, Takeshi , WATANABE, Masahiro , YAMANAGA, Katsumi , SHINYAMA, Hiroshi , KAWAMURA, Toru , NARITA, Yuji
发明人： THE GREEN CROSS CORPORATION
IPC分类号： A61K31/455
CPC分类号： A61K31/44 , A61K31/495 , Y10S514/824 , Y10S514/87 , Y10S514/925 , Y10S514/929
摘要： Novel medicinal uses of a dihydropyridine derivative represented by general formula (I) or an acid-addition salt thereof for promoting PGI2 production and preventing or treating hyperlipemia, arteriosclerosis and brain diseases. In said formula (I), R1, R2 and R3 represent each independently alkyl, etc.; R4 represents hydrogen, etc.; R5 represents nitro, haloalkyl, cyano, etc.; X represents vinylene or azomethine; A represents alkylene; and B represents -NR6R7 or a group (a) wherein R6 and R7 represent each independently alkyl, aralkyl, aryl, etc.; R8 and Ar represent each aryl, etc.; and n represents 0, 1 or 2.
摘要翻译：用于促进PGI 2产生和预防或治疗高脂血症，动脉硬化和脑疾病的由通式（I）表示的二氢吡啶衍生物或其酸加成盐的新药物用途。在所述式（I）中，R 1，R 2和R 3各自独立地表示烷基等。 R4代表氢等; R5代表硝基，卤代烷基，氰基等; X表示亚乙烯基或偶氮甲碱; A表示亚烷基; 和B代表-NR6R7或（a）其中R6和R7各自表示烷基，芳烷基，芳基等; R8和Ar表示各芳基等; n表示0,1或2。

8. 发明申请

WO1993019060A1 ISOINDAZOLE COMPOUND 审中-公开
标题翻译： ISOINDAZOLE化合物
公开(公告)号：WO1993019060A1
公开(公告)日：1993-09-30
申请号：PCT/JP1993000354
申请日：1993-03-25
申请人： THE GREEN CROSS CORPORATION , ASAHI GLASS CO., LTD. , INOUE, Yoshihisa , EBISU, Hajime , NAKAMURA, Norifumi , MORIZAWA, Yoshitomi , OKAZOE, Takashi , YASUDA, Arata
发明人： THE GREEN CROSS CORPORATION , ASAHI GLASS CO., LTD.
IPC分类号： C07D403/06
CPC分类号： C07D473/00 , C07D403/06 , C07D471/04
摘要： An isoindazole compound represented by general formula (1) or a salt thereof, a process for producing the same, and a pharmaceutical use thereof, in particular, as an angiotensin II antagonist and a prophylactic and/or therapeutic agent for circulatory organ diseases such as hypertension and cardiac insufficiency, wherein Q represents a heterocyclic group represented by general formula (2) or (3), and other symbols are each as defined in the specification. The above compound and salt have an excellent angiotensin II antagonism and reduced toxicity, thus being useful as an angiotensin II antagonist for treating or preventing various diseases mediated by angiotensin II, such as circulatory organ diseases, for example, hypertensions including essential and renal ones, cardiac insufficiency, and so forth.
摘要翻译：由通式（1）表示的异吲唑化合物或其盐，其制备方法及其药物用途，特别是作为血管紧张素II拮抗剂和循环器官疾病的预防和/或治疗剂，例如高血压和心功能不全，其中Q表示由通式（2）或（3）表示的杂环基，其它符号各自如说明书中所定义。上述化合物和盐具有优异的血管紧张素II拮抗作用和毒性降低，因此可用作血管紧张素II拮抗剂，用于治疗或预防由血管紧张素II介导的各种疾病，例如循环器官疾病，例如包括必需和肾脏的高血压，心功能不全等。

9. 发明申请

WO1998018492A1 METHOD OF INHIBITING DRUG PRECIPITATION 审中-公开
标题翻译：抑制药物降解的方法
公开(公告)号：WO1998018492A1
公开(公告)日：1998-05-07
申请号：PCT/JP1997003859
申请日：1997-10-23
申请人： THE GREEN CROSS CORPORATION , KODAIRA, Hideto , KIDO, Takae , NAWA, Yoshihito , MUNECHIKA, Koji , UEDA, Yasuo
发明人： THE GREEN CROSS CORPORATION
IPC分类号： A61K47/14
CPC分类号： A61K9/127 , A61K9/0019 , A61K9/1075 , A61K47/14 , A61K47/24
摘要： A method of inhibiting the precipitation of an acidic or basic drug which is liable to cause precipitation in aqueous solutions, such as a transfusion, by blending the drug with at least one ingredient selected among phospholipids, glycerides and synthetic surfactants, whereby it is possible to inhibit the precipitation of the drug liable to cause precipitation as a result of solubility lowering due to a pH change. Accordingly, it is possible to administer such a drug to a patient under the physiological pH conditions by mixing the drug with a transfusion having such an electrolyte composition as to fit the condition of the patient.
摘要翻译：通过将药物与选自磷脂，甘油酯和合成表面活性剂中的至少一种成分混合，抑制易于在水溶液中析出的酸性或碱性药物的沉淀的方法，例如输血，由此可以抑制由于pH变化引起的溶解性降低的结果，容易引起沉淀的药物的沉淀。因此，通过将药物与具有适合患者状况的电解质组成的输液混合，可以在生理pH条件下向患者施用这种药物。

10. 发明申请

WO1996003503A1 PROCESS FOR PRODUCING URINARY TRYPSIN INHIBITOR AND DOMAINS THEREOF, NOVEL POLYPEPTIDE RELATED TO THE BOTH, AND PROCESS FOR PRODUCING THE POLYPEPTIDE 审中-公开
标题翻译：用于生产尿素抑制剂及其领域的方法，与两相关的新型多肽，以及生产多肽的方法
公开(公告)号：WO1996003503A1
公开(公告)日：1996-02-08
申请号：PCT/JP1995001449
申请日：1995-07-21
申请人： THE GREEN CROSS CORPORATION , IDENO, Shoji , GOTO, Takashi , HORII, Hajime
发明人： THE GREEN CROSS CORPORATION
IPC分类号： C12N15/12
CPC分类号： C07K14/8103 , A61K38/00
摘要： A process for producing a urinary human trypsin inhibitor (UTI) and domains thereof by using a yeast of the genus Pichia as the host cell; an expression system related thereto; a novel polypeptide at least having the amino acid sequence represented by formula (I) in the specification; a DNA coding for the same; an expression vector containing the DNA; a transformant containing the vector; and a process for producing the polypeptide. The above UTI, expression system of each domain thereof, and process for producing the UTI and domains thereof enable UTI and domains thereof to be mass-produced readily and efficiently. The use of the expression system facilitates the preparation of variants or derivatives of UTI and so forth and contributes to the development of novel medicines such as a protease inhibitor. The invention also provides a novel useful polypeptide which is more excellent in elastase inhibitory activity than natural UTI and can be mass-produced.
摘要翻译：通过使用毕赤酵母属的酵母作为宿主细胞来制备尿胰蛋白酶抑制剂（UTI）及其结构域的方法; 与此有关的表达制度; 至少具有说明书中由式（I）表示的氨基酸序列的新型多肽; 编码相同的DNA; 含有DNA的表达载体; 含有载体的转化体以及产生该多肽的方法。上述UTI，其每个结构域的表达系统，以及UTI及其结构域的制备方法使得UTI及其结构域容易且有效地批量生产。表达系统的使用促进了UTI等变体或衍生物的制备，并有助于新型药物如蛋白酶抑制剂的开发。本发明还提供了一种与天然UTI相比弹性蛋白酶抑制活性更优异的新型有用多肽，可以批量生产。

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