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1. 发明申请

WO1996002659A1 IT-62-B SUBSTANCE AND MEDICINAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译： IT-62-B物质和药物组合物
公开(公告)号：WO1996002659A1
公开(公告)日：1996-02-01
申请号：PCT/JP1995001384
申请日：1995-07-12
申请人： TAIHO PHARMACEUTICAL CO., LTD. , KAWAUCHI, Takashi , SASAKI, Toru , MATSUMOTO, Hiroshi , OTANI, Toshio , CHEN, Ru-Xian , HUANG, Ming-Yu , YOSHIDA, Ken-ichiro
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C12P19/56
CPC分类号： C07H15/252 , C07H17/00 , C12P19/56
摘要： An IT-62-B substance represented by formula (1), a process for producing the same, a medicinal composition containing the same as the active ingredient, and a method of treating bacterium-induced infectious diseases and tumors by administering the same. The compound has antibacterial activities against gram-positive bacteria and part of gram-negative bacteria and also has an excellent antitumor activity against, for example, human nasopharyngeal cancer, thus being useful as a medicine.
摘要翻译：由式（1）表示的IT-62-B物质，其制备方法，含有该活性成分的药物组合物和通过施用该细菌诱导的传染病和肿瘤的方法。该化合物对革兰氏阳性细菌和革兰氏阴性细菌的一部分具有抗菌活性，并且对例如人鼻咽癌具有优异的抗肿瘤活性，因此可用作药物。

2. 发明申请

WO1997031122A1 SUBSTANCE FA-70D, PROCESS FOR PRODUCING THE SAME, AND USES THEREOF 审中-公开
标题翻译：物质FA-70D，其生产方法及其用途
公开(公告)号：WO1997031122A1
公开(公告)日：1997-08-28
申请号：PCT/JP1997000472
申请日：1997-02-20
申请人： TAIHO PHARMACEUTICAL CO., LTD. , KITANO, Shizuo , SASAKI, Toru , YOSHIDA, Kenichiro , OTANI, Toshio , YU, Lei , WU, Yun , KATSUNUMA, Nobuhiko
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C12P21/02
CPC分类号： C07K5/06095 , A61K38/00 , C12P21/02
摘要： Substance FA-70D represented by formula (1) or salts thereof; a medicinal composition comprising the compound as the active ingredient; a method of treatment for osteoporosis, comprising administering the compound; the use of the compound in drugs; and a microorganism capable of yielding this substance. The compound has a specific inhibitory activity against cathepsin proteases, and is useful as a drug for the treatment of various diseases wherein these enzymes participate, in particular osteoporosis.
摘要翻译：由式（1）表示的物质FA-70D或其盐; 包含该化合物作为活性成分的药物组合物; 一种治疗骨质疏松症的方法，包括给予所述化合物; 药物中使用该化合物; 和能够产生该物质的微生物。该化合物对组织蛋白酶蛋白酶具有特异性抑制活性，并且可用作治疗其中这些酶参与的各种疾病，特别是骨质疏松症的药物。

3. 发明申请

WO1997026242A1 3-(BIS-SUBSTITUTED-PHENYLMETHYLENE)OXINDOLE DERIVATIVES 审中-公开
标题翻译： 3-（双 - 取代 - 苯基甲基）氧化衍生物
公开(公告)号：WO1997026242A1
公开(公告)日：1997-07-24
申请号：PCT/JP1997000066
申请日：1997-01-16
申请人： TAIHO PHARMACEUTICAL CO., LTD. , SATO, Atsushi , ASAO, Tetsuji , HAGIWARA, Yuichi , KITADE, Makoto , YAMAZAKI, Yasundo
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D209/34
CPC分类号： C07D401/06 , C07D209/34 , C07D401/14 , C07D471/04
摘要： Oxindole derivatives represented by general formula (1) and drugs containing the same, wherein R represents methyl or methoxy. Because of having excellent effects of inhibiting granulation with little hepatic toxicity, these compounds are useful as drugs and usable in the prevention and treatmeent of articular rheumatism, arterial sclerosis, hepatic cirrhosis, arthrosis deformans, psoriasis, gout, nephritis, angiitis, inflammatory enteral diseases (ulcerative colitis, Crohn's disease), bronchitis, arthritis, chronic granulomatous disease, etc.
摘要翻译：由通式（1）表示的羟吲哚衍生物和含有它们的药物，其中R表示甲基或甲氧基。由于具有抑制肉毒毒性极小的效果，这些化合物可用作药物，可用于预防和治疗关节风湿病，动脉硬化，肝硬化，变形性关节炎，牛皮癣，痛风，肾炎，血管炎，炎性肠内疾病（溃疡性结肠炎，克罗恩病），支气管炎，关节炎，慢性肉芽肿病等

4. 发明申请

WO1997006145A1 FUSED INDAN DERIVATIVES AND SALTS THEREOF 审中-公开
标题翻译：熔融印度衍生物及其销售
公开(公告)号：WO1997006145A1
公开(公告)日：1997-02-20
申请号：PCT/JP1996002195
申请日：1996-08-02
申请人： TAIHO PHARMACEUTICAL CO., LTD. , OKAZAKI, Shinji , ASAO, Tetsuji , UTSUGI, Teruhiro , YAMADA, Yuji
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D221/18
CPC分类号： C07D401/04 , C07D221/18
摘要： Fused indan derivatives represented by general formula (1), salts thereof and medicinal uses of the same, wherein the ring A represents an optionally substituted benzene ring or a benzene ring having lower alkylenedioxy; the ring B represents an optionally substituted benzene ring or a benzene ring having lower alkylenedioxy; and R represents -NR1R2, an optionally substituted nitrogen-containing heterocycle, -OR3 or -SR4, wherein R1 and R2 are the same or different and each represent hydrogen, phenyl, an optionally substituted nitrogen-containing heterocycle, or lower alkyl optionally substituted by optionally substituted amino, lower alkoxy, phenyl, a nitrogen-containing heterocycle or hydroxy; and R3 and R4 represent each lower alkyl optionally substituted by substituted amino, excluding the case where the rings A and B are both unsubstituted benzene rings or the case where R is -NHCH3.
摘要翻译：由通式（1）表示的稠合茚满衍生物，其盐及其药用用途，其中环A表示任选取代的苯环或具有低亚烷基二氧基的苯环; 环B表示任选取代的苯环或具有低亚烷基二氧基的苯环; 并且R表示-NR1R2，任选取代的含氮杂环，-OR 3或-SR 4，其中R 1和R 2相同或不同，各自表示氢，苯基，任选取代的含氮杂环或任选被任选取代的氨基，低级烷氧基，苯基，含氮杂环或羟基; R 3和R 4代表任选被取代的氨基取代的低级烷基，不包括环A和B都是未取代的苯环的情况，或者R是-NHCH 3的情况。

5. 发明申请

WO1996020217A1 MONOCLONAL ANTIBODY 审中-公开
标题翻译：单克隆抗体
公开(公告)号：WO1996020217A1
公开(公告)日：1996-07-04
申请号：PCT/JP1995002661
申请日：1995-12-25
申请人： TAIHO PHARMACEUTICAL CO., LTD. , MIYADERA, Kazutaka , YAMADA, Yuji , TAKEBAYASHI, Yuji , AKIYAMA, Shin-ichi
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07K16/18
CPC分类号： C07K16/40 , C07K16/22 , Y10S435/96
摘要： A monoclonal antibody against a peptide which occurs in human thymidine phosphorylase and vascular endothelial cell growth factor originating in human platelets and contains amino acid sequences of SEQ ID NOS: 1 and 2; and a method of immunoassay of human thymidine phosphorylase and/or vascular endothelial cell growth factor originating in human platelet by using this monoclonal antibody. The monoclonal antibody recognizes human thymidine phosphorylase and vascular endothelial cell growth factor originating in human platelet and is useful in the diagnosis and treatment of various tumors, metastasis thereof, diseases accompanied by abnormal vascularization, etc.
摘要翻译：一种针对人胸腺嘧啶磷酸化酶和源自人血小板并含有SEQ ID NO：1和2的氨基酸序列的血管内皮细胞生长因子中的肽的单克隆抗体; 以及通过使用该单克隆抗体免疫测定人胸苷磷酸化酶和/或起源于人血小板的血管内皮细胞生长因子的方法。单克隆抗体识别起源于人血小板的人胸苷磷酸化酶和血管内皮细胞生长因子，可用于诊断和治疗各种肿瘤，其转移，伴有异常血管化的疾病等。

6. 发明申请

WO1996006835A1 PROCESS FOR PRODUCING 1-AMINO-1,2,3-TRIAZOLE 审中-公开
标题翻译： 1-氨基-1,2,3-三唑的制备方法
公开(公告)号：WO1996006835A1
公开(公告)日：1996-03-07
申请号：PCT/JP1995001727
申请日：1995-08-30
申请人： TAIHO PHARMACEUTICAL CO., LTD. , SHIGENO, Kazuhiko , ONO, Tomoyasu , TANAKA, Motoaki , YAMADA, Syozo , ASAO, Tetsuji
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D249/04
CPC分类号： C07D249/04
摘要： An industrial process for producing 1-amino-1,2,3-triazole represented by formula (III), safely and readily at a low cost, which comprises cyclizing glyoxal bishydrazone represented by formula (I), through the reaction thereof with hydrogen peroxide solution or manganese dioxide in the presence of a catalytic amount of a transition metal oxide represented by the general formula (II): MmOn, wherein M represents a transition metal atom; and m and n represent each independently an integer of 1 to 5.
摘要翻译：一种以式（III）代表的1-氨基-1,2,3-三唑生产工业方法，其成本低廉，包括使式（I）代表的乙二醛双腙环通过与过氧化氢反应溶液或二氧化锰在催化量的由通式（II）表示的过渡金属氧化物的存在下反应：MmOn，其中M表示过渡金属原子; m和n分别独立地表示1〜5的整数。

7. 发明申请

WO1995011879A1 PROCESS FOR PRODUCING ACID-ADDITION SALT OF Z-ISOMER OF TRIPHENYLETHYLENE COMPOUND 审中-公开
标题翻译：生产三苯乙烯化合物的Z-异构体酸的添加剂的方法
公开(公告)号：WO1995011879A1
公开(公告)日：1995-05-04
申请号：PCT/JP1994001782
申请日：1994-10-25
申请人： TAIHO PHARMACEUTICAL CO., LTD. , SHINOZAKI, Fumihiko , NAGASAWA, Hiroshi , MARUHASHI, Kazuo
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C217/18
CPC分类号： C07C217/18 , C07C213/08
摘要： A process for producing an acid-addition salt of a Z-isomer of a compound represented by general formula (I) (wherein R and R represent each lower alkyl, or are combined together with the nitrogen atom to which they are bonded to thereby form a nitrogenous heterocyclic group which may bear other heteroatom(s); R and R represent each hydrogen, lower alkyl, hydroxy, lower alkoxy, lower alkylcarbonyloxy, arylcarbonyloxy wherein the benzene ring may be substituted by one or two groups selected from among lower alkyl, lower alkoxy, halogen and cyano, benzylcarbonyloxy, mono- or di(lower alkyl)aminocarbonyloxy, or mono- or di(aryl)aminocarbonyloxy; R represents lower alkyl or halogen; and n represents 1 to 6), which process comprises heating an E-isomer of a compound represented by general formula (I) or an acid-addition salt thereof, either alone or as a mixture thereof with a Z-isomer of a comound represented by general formula (I) or an acid-addition salt thereof, in an organic solvent containing hydrobromic acid.
摘要翻译：一种制备通式（I）表示的化合物的Z-异构体的酸加成盐的方法（其中R 1和R 2代表每个低级烷基，或与氮原子相结合它们被键合从而形成可含有其它杂原子的含氮杂环基; R 3和R 4代表各自的氢，低级烷基，羟基，低级烷氧基，低级烷基羰基氧基，芳基羰基氧基，其中苯环可以是被一个或两个选自低级烷基，低级烷氧基，卤素和氰基的基团取代，苄基羰基氧基，一或二（低级烷基）氨基羰基氧基或一或二（芳基）氨基羰基氧基; R 5表示低级烷基或卤素 ; n表示1至6），该方法包括将通式（I）表示的化合物的E-异构体或其酸加成盐单独或作为其与组合的Z-异构体的混合物由通式（I）表示的化合物或其酸加成盐含有氢溴酸的厌氧溶剂。

8. 发明申请

WO1994006767A1 OPTICALLY ACTIVE 1-PHENYLPYRROLIDONE DERIVATIVE, INTERMEDIATE FOR PRODUCING THE SAME, AND PROCESS FOR PRODUCING BOTH 审中-公开
标题翻译：光学活性的1-苯基吡咯烷酮衍生物，用于生产其的中间体，以及生产两者的方法
公开(公告)号：WO1994006767A1
公开(公告)日：1994-03-31
申请号：PCT/JP1993001274
申请日：1993-09-08
申请人： TAIHO PHARMACEUTICAL CO., LTD. , YANO, Shingo , OHNO, Tomoyasu , OGAWA, Kazuo , SHIRASAKA, Tetsuhiko
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/26
CPC分类号： C07D207/26
摘要： An optically active 1-phenylpyrrolidone derivative represented by general formula (I), wherein R represents an optically active (alpha)-phenylethylamino group which may be substituted; a 1-phenylpyrrolidone derivative represented by general formula (I-a), and a process for producing 1-phenylpyrrolidone derivatives represented by these formulae.
摘要翻译：由通式（I）表示的光学活性1-苯基吡咯烷酮衍生物，其中R表示可被取代的光学活性（α） - 苯基乙基氨基; 由通式（I-a）表示的1-苯基吡咯烷酮衍生物以及由这些式表示的1-苯基吡咯烷酮衍生物的制备方法。

9. 发明申请

WO1996032384A1 NOVEL 4,6-DIARYLPYRIMIDINE DERIVATIVES AND SALTS THEREOF 审中-公开
标题翻译：新的4,6-二氨基嘧啶衍生物及其盐
公开(公告)号：WO1996032384A1
公开(公告)日：1996-10-17
申请号：PCT/JP1996001022
申请日：1996-04-12
申请人： TAIHO PHARMACEUTICAL CO., LTD. , KONNO, Yasuo , NOZAKI, Kenji , YAMADA, Shozo , ASAO, Tetsuji , SUZUKI, Takashi , KIMURA, Masayasu
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D403/12 , C07D417/04 , C07F9/6512
摘要： Novel 4,6-diarylpyrimidine derivatives represented by general formula (1), salts thereof, a process for producing the same, and a drug comprising the same as the active ingredient, wherein R represents a heterocycle or amino optionally substituted by one to four lower alkyl groups; and Ar represents phenyl, naphthyl or an aromatic heterocycle optionally having one to four substituents. The compounds have an excellent effect of inhibiting neovascularization and are useful as a remedy for solid tumor, rheumatism, diabetic retinopathy and psoriasis.
摘要翻译：由通式（1）表示的新颖的4,6-二芳基嘧啶衍生物，其盐，其制备方法和含有该活性成分的药物，其中R表示任选被1-4个低级烷基取代的杂环或氨基烷基; 并且Ar表示苯基，萘基或任选具有一至四个取代基的芳族杂环。该化合物具有优异的抑制新血管形成的作用，可用作实体瘤，风湿病，糖尿病性视网膜病和银屑病的治疗方法。

10. 发明申请

WO1996011681A1 PREVENTIVE AND REMEDY FOR DIARRHEA 审中-公开
标题翻译：防治艾滋病的预防和救济
公开(公告)号：WO1996011681A1
公开(公告)日：1996-04-25
申请号：PCT/JP1995002107
申请日：1995-10-13
申请人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI , TAIHO PHARMACEUTICAL CO., LTD. , KANEGAFUCHI KAGAKU KOGYO KABUSHIKI KAISHA , ISHIZUKA, Masaaki , MAEDA, Kenji , TAKEUCHI, Tomio , TOKO, Toshiyuki , SHIRAISHI, Tadayoshi
发明人： ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI , TAIHO PHARMACEUTICAL CO., LTD. , KANEGAFUCHI KAGAKU KOGYO KABUSHIKI KAISHA
IPC分类号： A61K31/195
CPC分类号： A61K31/475 , A61K31/198 , A61K31/505 , A61K31/675 , Y10S514/867 , A61K31/195 , A61K2300/00
摘要： A preventive and remedy for diarrhea containing conagenin or a salt thereof as the active ingredient, capable of intensely suppressing particularly a diarrheic symptom accompanying the administration of cancer chemotherapeutics to thereby permit perennial cancer chemotherapy, and capable of preventing exhaustion of the physical strength of a patient to thereby enhance the therapeutic effect.
摘要翻译：作为活性成分的含有络合蛋白或其盐的腹泻的预防和补救措施，能够特别强烈地抑制伴随癌症化学治疗剂的施用的腹泻症状，从而允许多年生癌症化学疗法，并且能够防止患者身体的疲劳疲劳从而提高治疗效果。

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