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11. 发明申请

WO1990012809A1 NOVEL PHYSIOLOGICALLY ACTIVE PEPTIDE AND CALCIUM METABOLISM-REGULATING AGENT COMPRISING SAID PEPTIDE AS EFFECTIVE INGREDIENT 审中-公开
标题翻译：新型生理活性肽和钙代谢调节剂包含作为有效成分的肽
公开(公告)号：WO1990012809A1
公开(公告)日：1990-11-01
申请号：PCT/US1990002143
申请日：1990-04-19
申请人： TSUMURA & CO. , ORLOWSKI, Ronald, C. , HANAMURA, Satoshi , MARUMOTO, Masahiko , SAKAMOTO, Kenji , WAKI, Yoshihiro
发明人： TSUMURA & CO.
IPC分类号： C07K07/10
CPC分类号： C07K14/585 , A61K38/00
摘要： A novel physiologically active peptide having the amino acid sequence (I) wherein X1 stands for Ser-Thr or Thr-Ser, X2 stands for Met, Gly, Ala, Val, n-Val, Pro, Leu, n-Leu, Ile, Phe or alpha -aminolactic acid, X3 stands for Asp or Glu, X4 stands for Leu-Gln-Thr, Gln-Thr, Leu or Gly-Gln-Thr, X5 stands for Val-Gly-Ala or Ser-Gly-Thr, R stands for H, NH2, N-acyl or N-aklyl, X6 sands for CO-NH or NH-CO, X7 stands for an amino acid sequence at the 2- to 6-positions of native calcitonin, or a substitution, deletion or addition derivative thereof, having 0 to 6 amino acids, X8 stands for an amino acid sequence at the 8- to 32-positions of native calcitonin, or a substitution, deletion or addition derivative thereof, and each of n1 and n2 is an integer or 1 to 19 and n1 + n2 is 2 to 20, or a pharmacologically acceptable salt thereof, and a calcium metabolism-regulating agent comprising, as an effective ingredient, the above-mentioned peptide or salt.
摘要翻译：具有氨基酸序列（I）的新型生理活性肽，其中X1表示Ser-Thr或Thr-Ser，X2表示Met，Gly，Ala，Val，n-Val，Pro，Leu，n-Leu，Ile， Phe或α-氨基乳酸，X3代表Asp或Glu，X4代表Leu-Gln-Thr，Gln-Thr，Leu或Gly-Gln-Thr，X5代表Val-Gly-Ala或Ser-Gly-Thr， R代表H，NH2，N-酰基或N-甲基，对于CO-NH或NH-CO的X6砂，X7代表天然降钙素2-至6-位的氨基酸序列，或取代，缺失或其加成衍生物，其具有0至6个氨基酸，X8表示天然降钙素的8至32位的氨基酸序列或其取代，缺失或加成衍生物，n1和n2均为整数或1〜19，n1 + n2为2〜20，或其药理学上可接受的盐，以及含有上述肽或盐的有效成分的钙代谢调节剂。

12. 发明申请

WO1997000068A1 CORNEAL CLOUDING INHIBITOR 审中-公开
公开(公告)号：WO1997000068A1
公开(公告)日：1997-01-03
申请号：PCT/JP1996001636
申请日：1996-06-14
申请人： SENJU PHARMACEUTICAL CO., LTD. , TSUMURA & CO. , TAKEDA, Masakazu , KIGAWA, Masaharu , WATANABE, Noriko , UMEGAKI, Yasuko , OKUMURA, Yasushi
发明人： SENJU PHARMACEUTICAL CO., LTD. , TSUMURA & CO.
IPC分类号： A61K31/34
CPC分类号： C07D207/34
摘要： A corneal clouding inhibitor which comprises a compound represented by general formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are the same or different and each represents hydrogen or optionally substituted hydroxy; R11 and R12 are the same or different and each represents hydrogen, alkyl or optionally esterified carboxy; R13 represents hydrogen, hydroxy, (optionally substituted aromatic carbon ring)-alkyl or (optionally substituted heterocycle)-alkyl; and X represents oxygen or nitrogen, provided that R13 represents an unshared electron pair, when X is oxygen.
摘要翻译：一种角膜混浊抑制剂，其包含通式（I）表示的化合物或其盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10相同或不同，各自表示氢或任选取代的羟基; R11和R12相同或不同，各自表示氢，烷基或任意酯化的羧基; R 13表示氢，羟基，（任选取代的芳族碳环） - 烷基或（任选取代的杂环） - 烷基; 并且X表示氧或氮，条件是当X为氧时，R 13表示非共享电子对。

13. 发明申请

WO1996038412A1 NOVEL COMPOUNDS AND ANTI-DERMATITIS DRUG 审中-公开
标题翻译：新型化合物和抗真菌药物
公开(公告)号：WO1996038412A1
公开(公告)日：1996-12-05
申请号：PCT/JP1996001458
申请日：1996-05-30
申请人： TSUMURA & CO. , TAKEDA, Masakazu , YAMAZAKI, Yuko , KIGAWA, Masaharu
发明人： TSUMURA & CO.
IPC分类号： C07D207/333
CPC分类号： C07D207/333 , C07D207/34 , C07D307/42 , C07D307/68 , C07D333/16
摘要： Compounds represented by general formula (1), 2,5-diphenylpyrrole compounds, 2,5-diphenylthiophene compounds and pharmaceutically acceptable salts thereof, wherein R11 represents hydrogen, hydroxy, C1-2 alkoxy, acetoxy or benzyloxy; R12 represents hydrogen, hydroxy, C1-2 alkoxy or benzyloxy; R13 represents hydrogen, hydroxy, C1-2 alkoxy, acetoxy or benzyloxy; and R14 represents hydrogen, hydroxy or benzyloxy. Because of having antiinflammatory effects, the above compounds (1), 2,5-diphenylpyrrole compounds and 2,5-diphenylthiophene compounds are useful in the treatment of dermatitis.
摘要翻译：由通式（1）表示的化合物，2,5-二苯基吡咯化合物，2,5-二苯基噻吩化合物及其药学上可接受的盐，其中R 11表示氢，羟基，C 1-2烷氧基，乙酰氧基或苄氧基; R 12表示氢，羟基，C 1-2烷氧基或苄氧基; R 13表示氢，羟基，C 1-2烷氧基，乙酰氧基或苄氧基; R 14表示氢，羟基或苄氧基。由于具有抗炎作用，上述化合物（1），2,5-二苯基吡咯化合物和2,5-二苯基噻吩化合物可用于治疗皮炎。

14. 发明申请

WO1996004002A1 REMEDY FOR CORNEAL DISEASES 审中-公开
标题翻译：治疗角膜疾病
公开(公告)号：WO1996004002A1
公开(公告)日：1996-02-15
申请号：PCT/JP1995001549
申请日：1995-08-04
申请人： TSUMURA & CO. , OKAMOTO, Sinseiro , AMAGAYA, Sakae , SAKAMOTO, Kenji , KANITANI, Masanao
发明人： TSUMURA & CO.
IPC分类号： A61K38/07
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1019 , C07K7/02 , Y10S514/912 , Y10S514/914
摘要： A remedy for corneal diseases containing at least one member selected from among hexapeptides represented by the following general formula (I): A-B-Pro-C-D-E and pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. In said formula (I) A represents arginine or lysine with the terminal amino group thereof removed, alkylated or acylated; B represents arginine, lysine or histidine; Pro represents proline; C represents tyrosine, tryptophan or phenylalanine; D represents valine, isoleucine or leucine; and E represents valine, isoleucine or leucine with the terminal carboxyl group thereof substituted by -COOR, -CH2OR or CONHR, wherein R represents hydrogen or C1-C4 alkyl.
摘要翻译：一种治疗角膜疾病的方法，所述角膜疾病含有选自以下通式（I）表示的六肽中的至少一种：A-B-Pro-C-D-E及其药学上可接受的盐和药学上可接受的载体。在所述式（I）中，A表示精氨酸或赖氨酸，其末端氨基被除去，烷基化或酰化; B代表精氨酸，赖氨酸或组氨酸; Pro代表脯氨酸; C代表酪氨酸，色氨酸或苯丙氨酸; D代表缬氨酸，异亮氨酸或亮氨酸; E表示缬氨酸，异亮氨酸或其末端羧基被-COOR，-CH 2 OR或CONHR取代的亮氨酸，其中R表示氢或C1-C4烷基。

15. 发明申请

WO1994004697A1 NOVEL ELAFIN DERIVATIVE 审中-公开
标题翻译：新的ELAFIN DERIVATIVE
公开(公告)号：WO1994004697A1
公开(公告)日：1994-03-03
申请号：PCT/JP1993001133
申请日：1993-08-11
申请人： TSUMURA & CO. , ISHIMA, Yoshiaki , OKAWA, Noriyuki , YOSHIDA, Masaya , AMAGAYA, Sakae , KAJI, Akira
发明人： TSUMURA & CO.
IPC分类号： C12P21/02
CPC分类号： C07K14/811 , A61K38/00
摘要： A novel elafin derivative having the amino acid sequence represented by formula (I): Ala-Gln-Glu-Pro-Val-Lys-Gly-Pro-Val-Ser-Thr-Lys-Pro-Gly-Ser-Cys-Pro-Ile-Ile-Leu-Ile-Arg-Cys-Ala- X -Leu-Asn-Pro-Pro-Asn-Arg-Cys-Leu-Lys-Asp-Thr-Asp-Cys-Pro-Gly-Ile-Lys-Lys-Cys-Cys-Glu-Gly-Ser-Cys-Gly-Met-Ala-Cys-Phe-Val-Pro-Gln or other amino acid sequence homologous thereto, wherein X represents leucine, isoleucine or valine. This derivative has an oxidation stability superior to that of natural elafin and hence can be utilized as a medicine such as an elastase inhibitor.
摘要翻译：具有式（I）表示的氨基酸序列的新颖的埃拉芬衍生物：Ala-Gln-Glu-Pro-Val-Lys-Gly-Pro-Val-Ser-Thr-Lys-Pro-Gly-Ser-Cys-Pro- Ile-Ile-Leu-Ile-Arg-Cys-Ala- X -Leu-Asn-Pro-Pro-Asn-Arg-Cys-Leu-Lys-Asp-Thr-Asp-Cys-Pro-Gly-Ile-Lys- Lys-Cys-Cys-Glu-Gly-Ser-Cys-Gly-Met-Ala-Cys-Phe-Val-Pro-Gln或与其同源的其它氨基酸序列，其中X表示亮氨酸，异亮氨酸或缬氨酸。该衍生物的氧化稳定性优于天然elafin，因此可用作药物如弹性蛋白酶抑制剂。

16. 发明申请

WO1993002684A1 'beta'-GLUCURONIDASE INHIBITOR 审中-公开
标题翻译： β-GLUCURONIDASE抑制剂
公开(公告)号：WO1993002684A1
公开(公告)日：1993-02-18
申请号：PCT/JP1992000988
申请日：1992-08-03
申请人： TSUMURA & CO. , KAMATAKI, Tetsuya
发明人： TSUMURA & CO.
IPC分类号： A61K31/70
CPC分类号： C07H17/00 , A61K31/70 , A61K36/538 , A61K36/539 , A61K2300/00
摘要： A $(b)-glucuronidase inhibitor comprising at least one compound selected among baïcalin, oroxylin A-7-O-glucuronide and luteolin-3'-glucuronide, an extract from scutellaria root and/or schizonepeta herb, or a Chinese medicine containing scutellaria root and/or schizonepeta herb as the crude drug ingredient. It can relieve side effects caused by the administration of a compound represented by formula (I), in particular, diarrhea.

17. 发明申请

WO1992015543A1 NOVEL ALLYL ALCOHOL DERIVATIVE 审中-公开
标题翻译：新款ALLYL酒精衍生物
公开(公告)号：WO1992015543A1
公开(公告)日：1992-09-17
申请号：PCT/JP1992000262
申请日：1992-03-05
申请人： TSUMURA & CO. , TAKEDA, Shuichi , ABURADA, Masaki , ASAMI, Akitoshi , ISHIHARA, Kazuhisa , FUJIWARA, Tadami , ICHIKAWA, Yukinobu
发明人： TSUMURA & CO.
IPC分类号： C07C43/23
CPC分类号： C07C43/23
摘要： A novel allyl alcohol derivative represented by formula (I), which is useful for treating hepatic diseases, psoriasis, cancer, arteriosclerosis, thrombosis and ache.

18. 发明申请

WO1998011086A1 CHROMONE DERIVATIVES AND NERVE CELL DEATH INHIBITORS CONTAINING THE SAME 审中-公开
标题翻译：色酮衍生物和含有其的神经细胞死亡抑制剂
公开(公告)号：WO1998011086A1
公开(公告)日：1998-03-19
申请号：PCT/JP1997002402
申请日：1997-07-10
申请人： TSUMURA & CO. , IGARASHI, Yasushi , TANAKA, Masahide , YANAGISAWA, Erika , YAMAGUCHI, Takuji
发明人： TSUMURA & CO.
IPC分类号： C07D311/54
CPC分类号： C07D311/54
摘要： Chromone derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and nerve cells death inhibitors containing the same as the active ingredient wherein R represents carboxyalkyl, carboxyalkenyl, alkoxyalkyl, alkoxycarbonyl, alkylthioalkyl, alkylsulfinyl-alkyl, alkylsulfonylalkyl, alkylsulfonyl, alkylcarbonyloxy-alkyl, alkoxycarbonylalkyl, alkoxycarbonylalkenyl, branched alkyl, aliphatic acyl, alkoxycarbonyl, optionally substituted carbamoyl, optionally substituted thiocarbamoyl, optionally substituted 1-piperidinylcarbonyl, optionally substituted 1-pyrrolidinylcarbonyl, optionally substituted 1-piperazinyl-carbonyl, optionally substituted morpholinocarbonyl, optionally substituted benzenesulfonyl, alkenyl, 2-acetoxy-2-methylpropionyl, benzoyl, alkoxybenzoyl, nitrobenzoyl, acetoxybenzoyl, aminobenzoyl, morpholinomethylbenzoyl, thiophenecarbonyl, furoyl, pyridinecarbonyl, phenoxycarbonyl or diphenoxyphosphoryl.
摘要翻译：由通式（I）表示的色酮衍生物或其药学上可接受的盐和含有与活性成分相同的神经细胞死亡抑制剂，其中R表示羧基烷基，羧基烯基，烷氧基烷基，烷氧基羰基，烷硫基烷基，烷基亚磺酰基 - 烷基，烷基磺酰基烷基，烷基磺酰基，烷基羰氧基 - 烷基任选取代的1-哌啶基羰基，任选取代的1-吡咯烷基羰基，任选取代的1-哌嗪基羰基，任选取代的吗啉代羰基，任选取代的苯磺酰基，烯基，2-乙酰氧基-2-甲基丙酰基，苯甲酰基，烷氧基苯甲酰基，硝基苯甲酰基，乙酰氧基苯甲酰基，氨基苯甲酰基，吗啉代甲基苯甲酰基，噻吩羰基，糠酰基，吡啶羰基，苯氧基羰基或二苯氧基磷酰基。

19. 发明申请

WO1996002528A1 METHOD OF SEPARATING AND RECOVERING FLAVONE COMPOUND HAVING GLYCOSIDE STRUCTURE AND FLAVONE COMPOUND NOT HAVING GLYCOSIDE STRUCTURE 审中-公开
标题翻译：分离和回收具有糖苷结构的FLAVONE化合物的方法和不具有糖苷结构的FLAVONE化合物
公开(公告)号：WO1996002528A1
公开(公告)日：1996-02-01
申请号：PCT/JP1995001400
申请日：1995-07-13
申请人： TSUMURA & CO. , INOUE, Katsutoshi , YOSHIZUKA, Kazuharu , KITAZAKI, Hironori , ISHIMARU, Masayuki
发明人： TSUMURA & CO.
IPC分类号： C07D311/40
CPC分类号： C07D311/30 , C07D311/40
摘要： A flavone compound having a glycoside structure, such as baicalin, is separated from a flavone compound not having a glycoside structure, such as baicalein, by treating an aqueous solution containing both compounds with a solvent containing compounds represented by following general formulae (I), (II) and (III) as the extractant, wherein R1 to R9 represent each independently optionally aryl-terminated, linear or branched C3-C20 alkyl, alkoxy or aryl, provided one or two of R7, R8 and R9 may be hydrogen. This method permits baicalein to be directly separated from scutellaria roots, a crude drug, by solvent extraction, and a mixture of baicalin with baicalein to be separated readily in a short time by solvent extraction.
摘要翻译：通过用含有下述通式（I）表示的化合物的溶剂处理含有两种化合物的水溶液，将不具有糖苷结构的黄酮化合物如黄芩苷从黄酮化合物中分离出黄酮苷，（II）和（III）），其中R 1至R 9各自独立地表示任选芳基封端的直链或支链C 3 -C 20烷基，烷氧基或芳基，其中R 7，R 8和R 9中的一个或两个可以是氢。该方法允许黄芩素通过溶剂萃取与黄芩根，生药，黄芩苷与黄芩苷的混合物直接分离，通过溶剂萃取在短时间内容易分离。

20. 发明申请

WO1995026753A1 PROCESS FOR PRODUCING SUSTAINED-RELEASE TABLETS AND ENTERIC TABLETS 审中-公开
标题翻译：生产持续释放片和肠道片的方法
公开(公告)号：WO1995026753A1
公开(公告)日：1995-10-12
申请号：PCT/JP1995000577
申请日：1995-03-28
申请人： TSUMURA & CO. , NAKAI, Yoichiro , NAKAI, Yoshinobu
发明人： TSUMURA & CO.
IPC分类号： A61K47/38
CPC分类号： A61K9/2013 , A61K9/2054 , A61K9/2095
摘要： A process for producing sustained-release tablets which comprises tableting a mixture of water-insoluble cellulose or a derivative thereof, a drug and a wax and heat-treating the obtained tablets; and a process for producing sustained-release tablets and enteric tablets which comprises heat-treating a mixture of water-insoluble cellulose or a derivative thereof, a drug and a wax and tableting the mixture thus treated. The above processes can provide sustained-release tablets from which the drug is sustainedly released at a nearly constant of arbitrary rate and which can retain the drug activity for long and enteric tablets from which the drug is released not in the stomach but in the intestine.
摘要翻译：一种缓释片剂的制造方法，其特征在于，将水不溶性纤维素或其衍生物，药物和蜡的混合物压片，并对所得片剂进行热处理。以及生产缓释片和肠溶片剂的方法，其包括热处理水不溶性纤维素或其衍生物，药物和蜡的混合物，并将如此处理的混合物压片。上述方法可以提供持续释放片剂，药物以几乎恒定的任意速率被持续释放，并且可以保持长期和肠溶片剂的药物活性，药物不会在胃中而不是在肠中释放。

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