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1. 发明申请

WO1995034542A1 TRIAZOLE COMPOUND AND ANTIFUNGAL AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：三唑化合物和含有该成分的抗真菌剂作为活性成分
公开(公告)号：WO1995034542A1
公开(公告)日：1995-12-21
申请号：PCT/JP1995001166
申请日：1995-06-09
申请人： TOKYO TANABE COMPANY LIMITED , TOMARI, Masazumi , SAKUMA, Osamu , OHTO, Hiroyuki , NAGAOKA, Kazuhiko , TSUJI, Michinori
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D249/08
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A triazole compound represented by general formula (I) or a physiologically acceptable salt or hydrate thereof, and an antifungal agent containing the same as the active ingredient, wherein R represents hydrogen or methyl; R represents methyl, 4-methyl-4H-1,2,4-triazol-3-yl or (4-methyl-4H-1,2,4-triazol-3-yl)methyl; R represents hydrogen or methyl; and m and n represent each 0 to 2. These compounds have a remarkably potent antifungal effect and an excellent safety, and are efficacious in treating human or animal superficial or deep-seated mycosis.
摘要翻译：由通式（I）表示的三唑化合物或其生理上可接受的盐或水合物，以及含有与活性成分相同的抗真菌剂，其中R 1表示氢或甲基; R 2表示甲基，4-甲基-4H-1,2,4-三唑-3-基或（4-甲基-4H-1,2,4-三唑-3-基）甲基; R 3表示氢或甲基; m和n分别表示0〜2.这些化合物具有非常有效的抗真菌作用和优异的安全性，并且对于治疗人或动物表面或深层的真菌病有效。

2. 发明申请

WO1995025539A1 NOVEL REMEDY FOR RESPIRATORY-TRACT VIRAL DISEASE 审中-公开
标题翻译：呼吸道病毒性疾病的新措施
公开(公告)号：WO1995025539A1
公开(公告)日：1995-09-28
申请号：PCT/JP1995000513
申请日：1995-03-20
申请人： TOKYO TANABE COMPANY LIMITED , KIDO, Hiroshi , TASHIRO, Masato , SEKIDO, Shozaburo
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： A61K38/57
CPC分类号： C07K14/811 , A61K38/00
摘要： A viral desease remedy or preventive containing antileukoprotease (ALP) as the active ingredient. It can be effectively applied to particularly viral diseases cauded by viruses that can be activated by tryptase clara, i.e., viruses that contain adventitial glycoproteins and cause infection in the respiratory tract to proliferate therein, for example, influenza virus, parainfluenza virus, RS virus, measles virus, or mumps virus.
摘要翻译：一种包含抗白蛋白酶（ALP）作为活性成分的病毒性疾病治疗或预防措施。它可以有效地应用于可以被类胰蛋白酶克拉拉激活的病毒，即含有外膜糖蛋白并引起呼吸道感染的病毒在其中增殖的病毒，例如流感病毒，副流感病毒，RS病毒，麻疹病毒或腮腺炎病毒。

3. 发明申请

WO1995011245A1 INDOLE DERIVATIVE 审中-公开
公开(公告)号：WO1995011245A1
公开(公告)日：1995-04-27
申请号：PCT/JP1994001769
申请日：1994-10-20
申请人： TOKYO TANABE COMPANY LIMITED , TSUCHIYA, Shinji , YASUDA, Noboyuki , FUKUZAKI, Atsushi
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D471/06
CPC分类号： C07D471/16
摘要： An indole derivative represented by general formula (I), each isomer thereof or a mixture of the isomers, a physiologically acceptable salt thereof, and a solvate thereof, wherein R represents (a) or (b); R represents optionally substituted phenyl; and R represents hydrogen, methyl or ethyl. This derivative has a potent and selective antagonism against intestinal 5-HT3 receptors when compared with known 5-HT3 antagonists and can well retain the effect for long, so that it is particularly useful for preventing or treating digestive tract disorders such as irritable bowel syndrome and diarrhea.
摘要翻译：由通式（I）表示的吲哚衍生物，其各异构体或异构体的混合物，其生理学上可接受的盐及其溶剂化物，其中R 1表示（a）或（b）; R 2表示任选取代的苯基; R 3表示氢，甲基或乙基。当与已知的5-HT 3拮抗剂相比时，该衍生物对肠道5-HT 3受体具有有效和选择性的拮抗作用，并且可以很好地保持长期的效果，因此其特别可用于预防或治疗消化道疾病如肠易激综合征和肠易激综合征腹泻。

4. 发明申请

WO1995011223A1 NOVEL ARYLETHANOLAMINO(ARYL)PROPANOL COMPOUND 审中-公开
标题翻译：新亚油酰胺（ARYL）丙二醇化合物
公开(公告)号：WO1995011223A1
公开(公告)日：1995-04-27
申请号：PCT/JP1994001723
申请日：1994-10-13
申请人： TOKYO TANABE COMPANY LIMITED , OHNO, Norio , HIRATSUKA, Kozo , FUKUZAKI, Atsusi , TAKENAWA, Noriko , OSAKA, Kazuya
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07C215/30
CPC分类号： C07C235/34 , C07C215/30 , C07C217/70 , C07C229/36 , C07C255/13 , C07C271/16
摘要： A novel arylethanolamino(aryl)propanol compound represented by general formula (I) and having the activity of regulating intestinal tract movement; a process for producing the compound; an intermediate therefor; and a medicinal composition containing the compound and a salt thereof as the active ingredient, wherein, typically, A represents CH; X represents hydrogen, fluorine or chlorine; Y represents hydrogen, or X and Y are combined together to represent -CH=CH-CH=CH-; Ar represents an aromatic ring, such as benzene or indole, substituted by Z1 and Z2; Z1 represents hydrogen or halogen; Z2 represents -OZ3; and Z3 represents methyl substituted by carbonyl substituted by hydroxy or (C1-C4)alkoxy.
摘要翻译：一种由通式（I）表示的具有调节肠道运动活性的新型芳基乙醇胺基（芳基）丙醇化合物; 一种制备该化合物的方法; 一个中间人以及含有该化合物及其盐作为有效成分的药物组合物，通常A表示CH; X表示氢，氟或氯; Y表示氢，或X和Y组合在一起，表示-CH = CH-CH = CH-; Ar表示被Z1和Z2取代的芳香环，例如苯或吲哚; Z1表示氢或卤素; Z2表示-OZ3; Z 3表示由被羟基或（C 1 -C 4）烷氧基取代的羰基取代的甲基。

5. 发明申请

WO1995010264A1 TABLET CONTAINING ENTERIC GRANULES 审中-公开
标题翻译：包含输入颗粒的片剂
公开(公告)号：WO1995010264A1
公开(公告)日：1995-04-20
申请号：PCT/JP1994001675
申请日：1994-10-06
申请人： TOKYO TANABE COMPANY LIMITED , MATSUSHITA, Tomohisa , HASHIMOTO, Mitsuo
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： A61K09/20
CPC分类号： A61K9/2009 , A61K9/2081
摘要： A tablet containing enteric granules prepared by tableting a mixture of enteric granules containing a basis with at least one member selected from the group consisting of synthetic hydrotalcite, dried aluminum hydroxide gel, a coprecipitate of aluminum hydroxide with sodium hydrogencarbonate, aluminum magnesium hydroxide, synthetic aluminum silicate and dihydroxyaluminum aminoacetate. As compared with the conventional tablets containing coated granules, this tablet has the following advantages: the content of enteric granules is increased by using a specified filler; the basis is rapidly dispersed in the granules; the granules have drug-release ability and acid resistance comparable to those before tableting; damage to the coating is reduced; weight variation during tableting is reduced; and the tablet has a high strength. The technique of preparing a tablet having a high enteric granule content has merits of an improved administrability due to a reduced size of the tablet and the applicability to other drugs.
摘要翻译：一种含有肠溶颗粒的片剂，其通过将含有基础的肠溶颗粒混合物与选自合成水滑石，干燥的氢氧化铝凝胶，氢氧化铝与碳酸氢钠的共沉淀物，氢氧化铝铝，合成铝硅酸盐和二羟基铝氨基乙酸盐。与含有包衣颗粒的常规片剂相比，该片剂具有以下优点：通过使用指定的填充剂增加肠溶颗粒的含量; 基础迅速分散在颗粒中; 颗粒具有与压片前相当的药物释放能力和耐酸性; 对涂层的损伤减少; 压片时的重量变化减小; 并且片剂具有高强度。制备具有高肠溶颗粒含量的片剂的技术由于片剂的尺寸减小和对其它药物的适用性，具有改善的给药能力的优点。

6. 发明申请

WO1993021225A1 SYNTHETIC PEPTIDE, PULMONARY SURFACTANT CONTAINING THE SAME, AND REMEDY FOR RESPIRATORY DISTRESS SYNDROME 审中-公开
标题翻译：合成肽，含有其的脉冲表面活性剂和呼吸道综合征的补救
公开(公告)号：WO1993021225A1
公开(公告)日：1993-10-28
申请号：PCT/JP1993000492
申请日：1993-04-16
申请人： TOKYO TANABE COMPANY LIMITED , TAKEI, Tsunetomo , AIBA, Toshimitsu , SAKAI, Kaoru , FUJIWARA, Tetsuro
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07K07/10
CPC分类号： C07K14/785 , A61K38/00
摘要： A peptide represented by the sequence (I), a pulmonary surfactant comprising the peptide and a lipid mixture, and a remedy for respiratory distress syndrome containing the surfactant as the active ingredient. In sequence (I) Xaa means the absence of any member or represents Cys, Ser or Ala; Xbb represents Cys, Ser or Ala; Xcc represents His or Asn; Xdd represents Leu or Ile; Xee represents Val or Ile; Xff represents Ile, Leu or Val; and Xgg means the absence of any member or represents Leu. The peptide is easy to isolate and purify, can be mass produced in a short time and has a potent surface activity when mixed with a lipid mixture. The pulmonary surfactant has a good suspending activity and a potent surface activity, thus being useful as a remedy for respiratory distress syndrome.
摘要翻译：由序列（I）表示的肽，包含肽和脂质混合物的肺表面活性剂，以及含有表面活性剂作为活性成分的呼吸窘迫综合征的治疗剂。顺序（I）Xaa表示不存在任何成员或表示Cys，Ser或Ala; Xbb表示Cys，Ser或Ala; Xcc代表His或Asn; Xdd表示Leu或Ile; Xee代表Val或Ile; Xff表示Ile，Leu或Val; 而Xgg表示没有任何成员或代表Leu。该肽易于分离和纯化，可在短时间内批量生产，并且与脂质混合物混合时具有强的表面活性。肺表面活性剂具有良好的悬浮活性和有效的表面活性，因此可用作呼吸窘迫综合征的补救剂。

7. 发明申请

WO1997036997A1 NOVEL BILE ACID CONVERTING MICROORGANISM AND PROCESS FOR PREPARING BILE ACID 审中-公开
标题翻译：新型双酸转化微生物及其制备方法
公开(公告)号：WO1997036997A1
公开(公告)日：1997-10-09
申请号：PCT/JP1997000937
申请日：1997-03-21
申请人： TOKYO TANABE COMPANY LIMITED , OKAMURA, Akio , MATSUI, Hiroyuki
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C12N01/14
CPC分类号： C12R1/80 , C12P33/06 , Y10S435/911
摘要： A microorganism having a capability of introducing a 7 beta -hydroxyl group into a 7-unsubstituted bile acid, and a process for preparing a bile acid having a 7 beta -hydroxyl group characterized by bringing the above microorganism into contact with a 7-unsubstituted bile acid to convert the acid to a bile acid having a 7 beta -hydroxyl group. The process permits ursodeoxycholic acid useful as a cholagogue and intermediates therefor to be efficiently prepared.
摘要翻译：具有将7β-羟基引入7-未取代的胆汁酸的能力的微生物，以及制备具有7β-羟基的胆汁酸的方法，其特征在于使上述微生物与7-未取代的胆汁接触酸将酸转化为具有7β-羟基的胆汁酸。该方法允许用作cholagogue的熊去氧胆酸和其中间体以有效地制备。

8. 发明申请

WO1995009167A1 INDOLINE DERIVATIVE AND 5-HT3 RECEPTOR ANTAGONIST CONTAINING THE SAME AS ACTIVE INGREDIENT 审中-公开
标题翻译：含有它们的吲哚衍生物和5-HT3受体拮抗剂作为活性成分
公开(公告)号：WO1995009167A1
公开(公告)日：1995-04-06
申请号：PCT/JP1994001622
申请日：1994-09-29
申请人： TOKYO TANABE COMPANY LIMITED , TSUCHIYA, Shinji , YASUDA, Nobuyuki , FUKUZAKI, Atsushi , KAZAMA, Koichi
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D403/06
CPC分类号： C07D403/06
摘要： An indoline derivative represented by general formula (I); a physiologically acceptable salt thereof; solvates of these compounds; and a 5-HT3 receptor antagonist containing the same as the active ingredient. In said formula, R represents the group (a) ou (b); R represents optionally substituted phenyl or heteroaryl; and R represents hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, carbamoyl or lower alkoxycarbonyl. The derivative has a potent antagonism against 5-HT3 receptors in the intestinal tract as compared with the known 5-HT3 receptor antagonists and is excellent in the persistence of the activity. Hence it is useful for preventing or treating vomiting or nausea induced by chemotherapy or radiation, irritable bowel syndrom and diarrhea.
摘要翻译：由通式（I）表示的二氢吲哚衍生物; 其生理上可接受的盐; 这些化合物的溶剂合物; 和含有与活性成分相同的5-HT 3受体拮抗剂。在所述式中，R 1表示（a）ou（b）; R 2表示任选取代的苯基或杂芳基; R 3表示氢，卤素，低级烷基，羟基，低级烷氧基，氨基甲酰基或低级烷氧基羰基。与已知的5-HT 3受体拮抗剂相比，该衍生物对肠道中的5-HT 3受体具有强烈的拮抗作用，并且活性持久性优异。因此，可用于预防或治疗由化学疗法或放射线引起的呕吐或恶心，肠易激综合征和腹泻。

9. 发明申请

WO1994022896A1 CHOLESTASIS AMELIORANT 审中-公开
标题翻译：美丽的喜悦
公开(公告)号：WO1994022896A1
公开(公告)日：1994-10-13
申请号：PCT/JP1994000282
申请日：1994-02-23
申请人： TOKYO TANABE COMPANY LIMITED , MAEDA, Minoru , KOISO, Kumiko , SEKIDO, Shozaburo
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07J09/00
CPC分类号： C07J41/0061 , A61K31/575
摘要： A cholestasis ameliorant containing as the active ingredient tauroursodeoxycholic acid which is superior to ursodeoxycholic acid in solubility. It is useful as an ameliorant for intrahepatic cholestasis due to drug-induced hepatopathy or viral hepatitis, or cholestasis occurring after the surgical operation for treating obstructive jaundice.
摘要翻译：一种胆固醇改善剂，其含有作为活性成分的葡萄糖脱氧胆酸，其在溶解度方面优于熊去氧胆酸。作为用于治疗阻塞性黄疸的外科手术后发生的由药物诱发的肝病或病毒性肝炎引起的肝内胆汁郁积的改善剂，或胆汁淤积是有用的。

10. 发明申请

WO1994022862A1 INDOLIZINE DERIVATIVE 审中-公开
标题翻译：吲哚衍生物
公开(公告)号：WO1994022862A1
公开(公告)日：1994-10-13
申请号：PCT/JP1994000523
申请日：1994-03-30
申请人： TOKYO TANABE COMPANY LIMITED , TSUCHIYA, Shinji , YASUDA, Nobuyki , FUKUZAKI, Atushi
发明人： TOKYO TANABE COMPANY LIMITED
IPC分类号： C07D471/16
CPC分类号： C07D471/16 , Y02P20/55
摘要： An indolizine derivative represented by general formula (I), a physiologically acceptable salt thereof, and a solvate of each of them (wherein R represents optionally substituted phenyl; R represents a group of (a) or (b); symbol - &cir& _- &cir& _- &cir& _- &cir& _- &cir& _ represents either a single or a double bond; and R represents hydrogen, methyl or ethyl). The derivative has such a remarkably selective and potent antagonism against intestinal 5-HT3 receptors when compared with the conventional 5-HT3 antagonists that it is particularly useful for treating and preventing irritable bowel syndrome, diarrhea and gastrointestinal dysfunction with reduced side effects.
摘要翻译：由通式（I）表示的中氮茚衍生物，其生理学上可接受的盐及其各自的溶剂化物（其中R 1表示任选取代的苯基; R 2表示（a）或（b） ;符号 - ＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_-＆cir＆_表示单键或双键; R 3表示氢，甲基或乙基）。与常规的5-HT3拮抗剂相比，该衍生物具有对肠道5-HT 3受体的显着选择性和有效的拮抗作用，特别适用于治疗和预防肠易激综合征，腹泻和胃肠功能障碍，副作用减轻。

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