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1. 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。

2. 发明申请

WO1997043295A1 D-PENTOFURANOSE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译： D-吡喃葡萄糖苷衍生物及其制备方法
公开(公告)号：WO1997043295A1
公开(公告)日：1997-11-20
申请号：PCT/JP1997001427
申请日：1997-04-24
申请人： TAIHO PHARMACEUTICAL CO., LTD. , NOMURA, Makoto , KAZUNO, Hideki , SATO, Tsutomu , WASHINOSU, Masato , TANAKA, Motoaki , MATSUDA, Akira , ASAO, Tetsuji
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07H13/06
CPC分类号： C07H9/04 , C07H13/04 , C07H19/04
摘要： D-Pentofuranose derivatives represented by general formulae (1) to (4) and a process for the preparation of compounds of general formula (2) by oxidizing compounds of general formula (1) with a hypochlorite in the presence of a catalytic amount of a 2,2,6,6-tetramethylpiperidinoxy compound (wherein A is 4-chlorobenzoyl; R is hydrogen, aliphatic lower acyl or optionally substituted benzoyl; X and Y are each lower alkyl; Z is ethynyl or tri(lower alkyl)silylethynyl; and the sugar moiety of general formula (1) is xylose and those of general formulae (3) and (4) are each ribose). These compounds are useful as intermediates for the synthesis of 3'-C-substituted ribonucleoside derivatives having an excellent antitumor activity.
摘要翻译：在通式（1）〜（4）表示的D-戊聚糖衍生物和通式（2）的化合物的制备方法中，在催化剂量的存在下，用次氯酸盐氧化通式（1）的化合物 2,2,6,6-四甲基哌啶氧基化合物（其中A为4-氯苯甲酰基; R 1为氢，脂族低级酰基或任选取代的苯甲酰基; X和Y为低级烷基; Z为乙炔基或三（低级烷基）甲硅烷基乙炔基;通式（1）的糖部分为木糖，通式（3）和（4）的糖部分为核糖）。这些化合物可用作合成具有优异抗肿瘤活性的3'-C-取代核糖核苷衍生物的中间体。

3. 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。

4. 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

5. 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。

6. 发明申请

WO1997025986A1 INTIMAL THICKENING INHIBITORS 审中-公开
标题翻译：最终增稠抑制剂
公开(公告)号：WO1997025986A1
公开(公告)日：1997-07-24
申请号：PCT/JP1997000065
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： A61K31/40
CPC分类号： C07D401/06 , C07D209/34 , C07D401/14 , C07D471/04
摘要： Intimal thickening inhibitors containing as the active ingredient oxyindole derivatives represented by general formula (1) or salts thereof (wherein R represents hydrogen, phenyl optionally substituted by lower alkyl, lower alkoxy, lower alkylaminoalkoxy, hydroxy, amino, lower alkylamino or halogeno, or pyridyl optionally substituted by lower alkyl, lower alkoxy, lower alkylaminoalkoxy, hydroxy, amino, lower alkylamino, halogeno, lower alkoxycarbonyl or carboxy; R represents optionally substituted phenyl, or pyridyl optionally substituted by lower alkyl, lower alkoxy, lower alkylamino-alkoxy, hydroxy, amino, lower alkylamino, halogeno, lower alkoxycarbonyl or carboxy; R represents hydrogen, optionally substituted lower alkyl, benzyl or benzenesulfonyl, or acyl; R represents hydrogen, lower alkoxy, halogeno, amino, lower alkylamino, carboxy, lower alkoxycarbonyl, optionally substituted phenylcarbamoyl, or trifluoromethyl; X represents CH or N; n represents the number of the substituents ranging from 0 to 4; and the double line composed of dotted and solid lines means that this bond is either a single or a double bond). These drugs show excellent effects of inhibiting intimal thickening and thus useful in preventing, treating and relieving proliferative vascular lesions such as vascular reconstriction after percutaneous transluminal coronary recanalization, arterial sclerosis, peripheral embolism and angiitis.
摘要翻译：含有作为活性成分的由通式（1）表示的氧吲哚衍生物或其盐（其中R 1表示氢，任选被低级烷基，低级烷氧基，低级烷基氨基烷氧基，羟基，氨基，低级烷基氨基或卤素取代的苯基）的内增稠抑制剂或任选被低级烷基，低级烷氧基，低级烷基氨基烷氧基，羟基，氨基，低级烷基氨基，卤代，低级烷氧基羰基或羧基取代的吡啶基; R 2表示任选取代的苯基，或任选被低级烷基，低级烷氧基，低级烷基氨基 - 烷氧基，羟基，氨基，低级烷基氨基，卤代，低级烷氧基羰基或羧基; R 3表示氢，任选取代的低级烷基，苄基或苯磺酰基或酰基; R 4表示氢，低级烷氧基，，低级烷基氨基，羧基，低级烷氧基羰基，任选取代的苯基氨基甲酰基或三氟甲基; X表示CH或N; n表示取代基为0至4; 并且由虚线和实线组成的双线意味着该键是单键或双键）。这些药物显示出优异的抑制内膜增厚的效果，因此可用于预防，治疗和缓解经皮冠状动脉冠状动脉再通，动脉硬化，周围栓塞和血管炎等增殖性血管病变如血管再狭窄。

7. 发明申请

WO1996030346A1 URACIL DERIVATIVES, AND ANTITUMOR EFFECT POTENTIATOR AND ANTITUMOR AGENT CONTAINING THE SAME 审中-公开
标题翻译：尿嘧啶衍生物和抗肿瘤效应物质和含有其的抗肿瘤剂
公开(公告)号：WO1996030346A1
公开(公告)日：1996-10-03
申请号：PCT/JP1996000828
申请日：1996-03-28
申请人： TAIHO PHARMACEUTICAL CO., LTD. , YANO, Shingo , TADA, Yukio , KAZUNO Hideki , SATO, Tsutomu , YAMASHITA, Junichi , SUZUKI, Norihiko , EMURA, Tomohiro , FUKUSHIMA, Masakazu , ASAO, Tetsuji
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D239/54
CPC分类号： C07D239/54 , C07D231/12 , C07D233/56 , C07D239/553 , C07D249/08 , C07D403/06 , C07D403/12
摘要： Uracil derivatives represented by general formula (1) or salts thereof, wherein R represents chloro, bromo, iodo, cyano or lower alkyl; and R represents a 4- to 8-membered heterocycle optionally substituted by lower alkyl, imino, hydroxy, hydroxymethyl, methanesulfonyloxy, amino or nitro and having one to three nitrogen atoms, amidinothio wherein hydrogen on nitrogen is optionally substituted by lower alkyl, guanidino wherein hydrogen on nitrogen is optionally substituted by lower alkyl or cyano, lower alkylamidino, amino wherein hydrogen on nitrogen is optionally substituted by lower alkyl, -CH2N(R )R (wherein R and R are the same or different and each represents hydrogen or lower alkyl, or R and R together with the nitrogen atom to which they are bonded may form pyrrolidine), -NH-(CH2)m-Z (wherein Z represents amino wherein hydrogen on nitrogen is optionally substituted by lower alkyl, or cyano; and m is an integer of 0 to 3), -NR (CH2)m-OH (wherein R represents hydrogen or lower alkyl; and n is a natural number of 1 to 4), -X-Y (wherein X represents S or NH; and Y represents 2-imidazolin-2-yl, 2-imidazolyl, 1-methylimidazol-2-yl, 1,2,4-triasol-3-yl, 2-pyrimidyl or 2-benzimidazolyl optionally substituted by lower alkyl), or ureido or thioureido wherein hydrogen on nitrogen is optionally substituted by lower alkyl; and drugs containing the same, such as antitumor effect potentiators and antitumor agents.
摘要翻译：由通式（1）表示的尿嘧啶衍生物或其盐，其中R 1表示氯，溴，碘，氰基或低级烷基; 并且R 2表示任选被低级烷基，亚氨基，羟基，羟甲基，甲磺酰氧基，氨基或硝基取代且具有一至三个氮原子的4-至8-元杂环，其中氮上的氢任选被低级烷基取代胍基，其中氮上的氢任选被低级烷基或氰基取代，低级烷基脒基，氨基，其中氮上的氢任选被低级烷基，-CH 2 N（R a）R b取代（其中R a和R b）相同或不同，各自表示氢或低级烷基，或R a和R b与它们所键合的氮原子一起形成吡咯烷），-NH-（CH2）mZ（其中 Z表示氨基，其中氮上的氢任选被低级烷基或氰基取代;且m为0至3的整数），-NR c（CH 2）m -OH（其中R c表示氢或低级烷基 ; n为1至4的自然数），-XY（其中X表示S或NH; Y表示2-咪唑啉-2-基任选被低级烷基取代的2-嘧啶基或2-苯并咪唑基，或脲基或硫脲基，其中氮原子上的氢是任选的被低级烷基取代; 和含有相同药物的药物，如抗肿瘤作用增强剂和抗肿瘤剂。

8. 发明申请

WO1995032187A1 NOVEL FUSED INDAN DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：新型熔融衍生物和药物接受盐
公开(公告)号：WO1995032187A1
公开(公告)日：1995-11-30
申请号：PCT/JP1995000944
申请日：1995-05-18
申请人： TAIHO PHARMACEUTICAL CO., LTD. , OKAZAKI, Shinji , ASAO, Tetsuji , WAKIDA, Motoji , ISHIDA, Keisuke , WASHINOSU, Masato , UTSUGI, Teruhiro , YAMADA, Yuji
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D221/18
CPC分类号： C07D231/12 , C07D221/18 , C07D233/56 , C07D249/08 , C07D401/12 , C07D491/04
摘要： A fused indan derivative represented by general formula (1), a pharmaceutically acceptable salt thereof, and an antitumor drug, wherein ring A represents an optionally substituted benzene or naphtalene ring, or a benzene ring having a lower alkylenedioxy group; ring B represents a benzene ring which may be substituted or has a lower alkylenedioxy group; Y represents -N=CR- or -CR=N-; R represents -NR1R2, -OR3 or an optionally substituted nitrogenous heterocyclic group; R1 and R2 are the same or different from each other and each represents hydrogen, phenyl, an optionally substituted nitrogenous heterocyclic group, or a lower alkyl group which may be substituted by at least one substituent selected from the group consisting of optionally substituted amino, lower alkoxy, phenyl, a nitrogenous heterocyclic group, an amine oxide group substituted by lower alkyl, and hydroxy; and R3 represents lower alkyl which may be substituted by substituted amino, provided the case where R represents an optionally substituted nitrogenous heterocyclic group and rings A and B represent each an unsubstituted benzene ring, is excluded.
摘要翻译：或通式（1）表示的稠合茚满衍生物，其药学上可接受的盐和抗肿瘤药物，其中环A表示任选取代的苯或萘环或具有低亚烷基二氧基的苯环; 环B表示可以被取代或具有低亚烷基二氧基的苯环; Y表示-N = CR-或-CR = N-; R表示-NR1R2，-OR3或任选取代的含氮杂环基; R1和R2彼此相同或不同，各自表示氢，苯基，任选取代的含氮杂环基或可被至少一个选自以下的取代基取代的低级烷基：任选取代的氨基，低级烷氧基，苯基，含氮杂环基，被低级烷基取代的氧化胺基和羟基; 并且R 3表示可以被取代的氨基取代的低级烷基，只要其中R表示任选取代的含氮杂环基并且环A和B表示各自为未取代的苯环的情况即可。

9. 发明申请

WO1997021694A1 EPOXYSUCCINAMIDE DERIVATIVES OR SALTS THEREOF, AND DRUGS CONTAINING THE SAME 审中-公开
标题翻译： EPOXYSUCCINAMIDE衍生物或其盐，以及含有它们的药物
公开(公告)号：WO1997021694A1
公开(公告)日：1997-06-19
申请号：PCT/JP1996003603
申请日：1996-12-10
申请人： TAIHO PHARMACEUTICAL CO., LTD. , YAMASHITA, Tomohiro , SUDA, Yoshimitsu , TADA, Yukio , KATSUNUMA, Nobuhiko , ASAO, Tetsuji
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07D303/48
CPC分类号： C07D303/48
摘要： Epoxysuccinamide derivatives represented by general formula (1) or salts thereof and drugs comprising the same as the active ingredient, wherein R and R are the same or different and each represents H or optionally substituted aromatic hydrocarbyl or aralkyl, or R and R may form a nitrogenous heterocycle in cooperation with the adjacent nitrogen atom; R represents H or acyl; R represents H or aralkyl; and R represents optionally substituted aromatic hydrocarbyl or aralkyl or may form an optionally protected amino acid residue in cooperation with the adjacent nitrogen atom. These compounds have a cathepsin inhibitory activity, in particular a specific inhibitory activity against cathepsin L, and are hence effective in the prophylaxis and therapy of bone diseases such as osteoporosis.
摘要翻译：由通式（1）表示的环氧琥珀酰胺衍生物或其盐和包含与活性成分相同的药物，其中R 1和R 2相同或不同，各自表示H或任选取代的芳族烃基或芳烷基，或 R 1和R 2可以与相邻的氮原子一起形成含氮杂环; R 3表示H或酰基; R 4表示H或芳烷基; R 5表示任选取代的芳族烃基或芳烷基，或者可以与相邻的氮原子一起形成任选被保护的氨基酸残基。这些化合物具有组织蛋白酶抑制活性，特别是针对组织蛋白酶L的特异性抑制活性，因此有效预防和治疗骨疾病如骨质疏松症。

10. 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。

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