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21. 发明专利

NZ524974A Aliphatic nitrogen-containing 5-membered ring compound 未知
公开(公告)号：NZ524974A
公开(公告)日：2005-10-28
申请号：NZ52497401
申请日：2001-10-05
申请人： TANABE SEIYAKU CO
发明人： YASUDA KOSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKOTA MASATAKA , MATSUMOTO TAKESHI , ARAKAWA KENJI
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , C07D405/14 , C07D495/04 , C07D409/12 , A61K31/4439 , A61K31/506 , A61K31/501 , A61K31/497 , A61K31/5377 , A61K31/428 , A61K31/423 , A61K31/498 , A61K31/519 , A61K31/401 , A61K31/4709 , A61K31/454 , A61K31/4025 , A61K31/327 , A61K31/433 , A61K31/55 , A61K31/541 , A61K31/437 , A61K31/4725 , A61K31/4365 , A61K31/4035 , A61K31/41 , A61K31/4155 , C07D277/06 , C07D277/42 , C07D277/82
摘要： Disclosed are aliphatic nitrogen-containing 5-memebered ring compounds of formula (I), wherein: A is -CH2- or -S-, R1 is H, lower alkyl, hydroxy lower alkyl, or lower alkoxy lower alkyl, X is -N(R3)-, -O- or -CO-, and the remaining substituents are defined herein. The compounds are used in the manufacture of medicaments for the treatment of diseases mediated by inhibiting dipeptidylpeptidase IV activity.

22. 发明专利

AU2001294197B2 Aliphatic nitrogenous five-membered ring compounds 未知
公开(公告)号：AU2001294197B2
公开(公告)日：2004-09-16
申请号：AU2001294197
申请日：2001-10-05
申请人： TANABE SEIYAKU CO
发明人： ARAKAWA KENJI , MATSUMOTO TAKESHI , HIKOTA MASATAKA , KAWANAMI SABURO , MORIMOTO HIROSHI , YASUDA KOSUKE
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61P003/10 , A61P043/00 , C07D277/82 , C07D277/42 , C07D277/06 , A61K031/4155 , A61K031/41 , A61K031/4035 , A61K031/4365 , A61K031/4725 , A61K031/437 , A61K031/541 , A61K031/55 , A61K031/433 , A61K031/327 , A61K031/4025 , A61K031/454 , A61K031/4709 , A61K031/401 , A61K031/519 , A61K031/498 , A61K031/423 , A61K031/428 , A61K031/5377 , A61K031/497 , A61K031/501 , A61K031/506 , A61K031/4439 , C07D409/12 , C07D495/04 , C07D405/14
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula ÄIÜ : wherein symbols in the formula have the following meanings; A: -CH2- or -S-, B: CH or N, R : H, a lower alkyl group, etc., X: a single bonding arm, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, etc., R : hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R : (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is -CO-, then B is N, or a pharmaceutically acceptable salt thereof.

23. 发明专利

JP2005200427A A nitrogen-containing five-membered ring compound 审中-公开
标题翻译：含氮的五元环化合物
公开(公告)号：JP2005200427A
公开(公告)日：2005-07-28
申请号：JP2005105732
申请日：2005-04-01
申请人： Tanabe Seiyaku Co Ltd , 田辺製薬株式会社
发明人： YASUDA KOUSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKODA MASAKATSU , MATSUMOTO TAKESHI , ARAKAWA KENJI
IPC分类号： C07D401/12 , A61K31/40 , A61K31/4015 , A61K31/4035 , A61K31/4155 , A61K31/422 , A61K31/423 , A61K31/427 , A61K31/4365 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P19/02 , A61P19/10 , A61P31/18 , A61P37/02 , A61P43/00 , C07D207/16 , C07D207/333 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： PROBLEM TO BE SOLVED: To provide a new aliphatic nitrogen-containing five-membered ring compound having excellent DPPIV (dipeptidyl peptidase IV) inhibitory action. SOLUTION: The aliphatic nitrogen-containing five-membered ring compound is represented by formula [I], [wherein, A is CH 2 or S; B is CH or N; R 1 is H, a lower alkyl or the like; X is a single bond, CO, Alk-CO, COCH 2 , Alk-O, O-CH 2 , SO 2 , S, COO, CON(R 3 ), Alk-CON(R 3 ), CON(R 3 )CH 2 , NHCH 2 or the like; R 3 is H or a lower alkyl; Alk is a lower alkylene; R 2 is (1) a (substituted) cyclic group, (2) a (substituted) amino group or the like; and, if X is CO, B is N]. And pharmacologically permissible salts thereof and a method for producing the compound are also provided. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：提供具有优异DPPIV（二肽基肽酶IV）抑制作用的新型脂族含氮五元环化合物。解决方案：脂肪族含氮五元环化合物由式[I]表示，[其中A是CH 2 或S; B是CH或N; R 1 是H，低级烷基等; X是单键，CO，Alk-CO，COCH 2 ，Alk-O，O-CH 2 ，SO 2 COO，CON（R 3 ），Alk-CON（R SP 3），CON（R 3 SP 3）CH SB 2 >，NHCH 2 等; R 3是H或低级烷基; Alk是低级亚烷基; R 2是（1）（取代的）环状基团，（2）（取代的）氨基等; 并且如果X是CO，B是N]。还提供了其药学上允许的盐及其制备方法。版权所有（C）2005，JPO＆NCIPI

24. 发明专利

JP2002356472A NITROGEN-CONTAINING FIVE-MEMBERED RING COMPOUND 审中-公开
公开(公告)号：JP2002356472A
公开(公告)日：2002-12-13
申请号：JP2001309559
申请日：2001-10-05
申请人： TANABE SEIYAKU CO
发明人： YASUDA KOUSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKODA MASAKATSU , MATSUMOTO TAKESHI , ARAKAWA KENJI
IPC分类号： C07D401/12 , A61K31/341 , A61K31/4025 , A61K31/4035 , A61K31/422 , A61K31/423 , A61K31/437 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P13/12 , A61P25/00 , A61P43/00 , C07D207/16 , C07D207/40 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D513/04
摘要： PROBLEM TO BE SOLVED: To provide a new aliphatic nitrogen-containing five-membered ring compound having excellent DPPIV inhibitory action. SOLUTION: This compound is an aliphatic nitrogen-containing five-membered ring compound represented by the formula [I] [wherein, A is CH2 or S; B is CH or N; R is H, a lower alkyl or the like; X is a single direct bond, CO, Alk-CO, COCH2 , Alk-O, O-CH2 , SO2 , S, COO, CON(R ), Alk-CON(R ), CON(R ) CH2 , NHCH2 or the like; R is H or a lower alkyl; Alk is a lower alkylene; R is (1) a (substituted)cyclic group or (2) a (substituted)amino group or the like; and, if X is CO, B is N.] or a pharmacologically permissible salt of the compound, and the method for producing the compound is also provided.

25. 发明专利

JPH11130677A INTRACELLULAR CALCIUM INDUCTIVE CALCIUM RELEASE CHANNEL ACTIVITY REGULATOR 失效
公开(公告)号：JPH11130677A
公开(公告)日：1999-05-18
申请号：JP29378697
申请日：1997-10-27
申请人： TANABE SEIYAKU CO
发明人： MATSUMOTO TAKESHI , KOO ICHIRO , OOGIKU NORIKO , SAEKI KAZUHIKO
IPC分类号： C07D471/04 , A61K31/47 , A61P9/00 , A61P9/10 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain a regulator which inhibits the increase of the intracellulor calcium concentration due to the opening of intracellular calcium inductive calcium release channel caused by caffeine and, as a result, is effective in the prevention and the treatment of ischemic heart disease and the like by formulating a specific ellipticine derivative as an active ingredient. SOLUTION: This regulator includes an ellipticine derivative with a skeleton of formula I or its pharmacologically permissible salt, suitably an ellipticine derivative of formula II (R is H, a lower alkyl, etc.; R is H and a lower alkyl) or the like as an active ingredient. It is preferable that the above-stated derivative is 9-hydroxyellipticine or a compound convertible to 9-hydroxyellipticine in vivo. For example, 9-hydroxyellipticine may be reacted with a carboxylic acid derivative in a solvent in the presence of a condensing agent or a deacidification agent and then submitted to the deprotection reaction.

26. 发明专利

JPH06160376A EVALUATING METHOD FOR TRANSFUSION 失效
公开(公告)号：JPH06160376A
公开(公告)日：1994-06-07
申请号：JP31253292
申请日：1992-11-24
申请人： TANABE SEIYAKU CO
发明人： KISHI TETSUYA , IWAZAWA YASURO , MATSUMOTO TAKESHI , MORITA MOTOYO
IPC分类号： G01N33/15
摘要： PURPOSE:To sharply and accurately evaluate nutrition by measuring a concentration of a rapid turnover protein in blood collected from a mammal in which transfusion is administered. CONSTITUTION:When sodium chloride injection (fresh group) and high calorie transfusion (AMZ group) are injected in a plurality of rats, variations in weights of the rats during injection period are examined, bloods are collected, and concentrations of rapid turnover proteins in plasmas are measured by a sandwich type enzyme immunity measuring method, the weights of the rats of the fresh group containing no amino acid and no sugar are reduced with day, the weights of the rats of the AMZ group are increased with day, and it is understood that nutrient state of the AMZ group is high. Concentrations of transthiolation, retinol-binding protein of the fresh group in bloods are reduced with day, and those of the AMZ group are all rapidly increased. From these results, it is clear that the protein is varied in response to the nutrient state and it is understood that it is excellent as an evaluation index of the transfusion.

27. 发明专利

JP2004035574A Aliphatic nitrogenous five-membered ring compound 审中-公开
公开(公告)号：JP2004035574A
公开(公告)日：2004-02-05
申请号：JP2003368572
申请日：2003-10-29
申请人： Tanabe Seiyaku Co Ltd , 田辺製薬株式会社
发明人： YASUDA KOUSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKODA MASAKATSU , MATSUMOTO TAKESHI , ARAKAWA KENJI
IPC分类号： C07D277/06 , A61K31/40 , A61K31/4025 , A61K31/4045 , A61K31/41 , A61K31/423 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/4365 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P3/04 , A61P3/06 , A61P3/10 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/18 , A61P37/06 , A61P43/00 , C07D207/16 , C07D277/20 , C07D277/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： PROBLEM TO BE SOLVED: To provide a new aliphatic nitrogenous five-membered ring compound having excellent dipeptidyl peptidase IV (DPPIV) inhibitory action and its pharmacologically permissible salts, and to provide a method for producing the compound. SOLUTION: The aliphatic nitrogenous five-membered ring compound is represented by formula [1] [wherein, A is CH 2 or S; R 1 is H, a lower alkyl, a hydroxy lower alkyl or a lower alkoxy lower alkyl; X is N(R 3 ) or O; R 3 is H or a lower alkyl; and R 2 is (1) a (substituted) cyclic group or (2) a (substituted) amino]. COPYRIGHT: (C)2004,JPO

28. 发明专利

JPH04352720A AMINO ACID PREPARATION FOR CANCER PATIENT 失效
公开(公告)号：JPH04352720A
公开(公告)日：1992-12-07
申请号：JP22818091
申请日：1991-05-30
申请人： TANABE SEIYAKU CO
发明人： SATO TADASHI , KISHI TETSUYA , MATSUMOTO TAKESHI , SHIRAI HIROKI
IPC分类号： A61K31/195 , A61K31/198 , A61K31/405 , A61P3/00 , A61P3/12 , A61P35/00
摘要： PURPOSE:To provide an amino acid preparation capable of sufficiently supplying nutrients for a host living body but selectively inhibiting only the growth of a malignant tumor and used for cancer patients by replacing L-phenylalanine, L-tryptophan, and L-lysine with substitutes. CONSTITUTION:In an amino acid preparation containing L-phenylalanine, L- tryptophan and L-lysine, at least one of the amino acids is replaced with 3-phenyl lactic acid (for the L-phenylalanine), 3-indole lactic acid (for the L-tryptophan) or Nepsilon-methyl-L-lysine (for the L-lysine). The substitutes become the substitutes for the respective amino acids in normal cells, but do not exhibit the substitution actions of the amino acids in malignant tumor cells to inhibit the multiplication of the tumor cells. A preferable example of the preparation is an amino acid infusion solution for patients having the amino acid composition in the table.

29. 发明专利

JPS61112023A Novel method for preparation of substance having cytotoxic activity to cancer cell 失效
标题翻译：用于制备具有对癌细胞的细胞活性的物质的新方法
公开(公告)号：JPS61112023A
公开(公告)日：1986-05-30
申请号：JP23385784
申请日：1984-11-05
申请人： Tanabe Seiyaku Co Ltd
发明人： KATO JOJI , YAMAMOTO KOZO , KOMATSUBARA SABURO , TAKAGI TSUTOMU , MATSUMOTO TAKESHI , SUGITA NAOHISA , KASHIDA TATSUO
IPC分类号： C07K14/195 , A61K35/12 , A61K38/16 , A61P35/00 , C07K14/005 , C07K14/37 , C07K14/41 , C07K14/42 , C07K14/52 , C07K14/525
摘要： PURPOSE: To obtain a substance having cytotoxic activity to cancer cells and extremely high safety, by using a water-soluble peptide glucomannan originated from microorganisms.
CONSTITUTION: A substance having cytotoxic activity to cancer cell can be produced by treating a mammal or a mammal-originated monocytic cell with a water-soluble peptide glucomannan originated from microorganism (e.g. SPGM- I, etc. obtained from beer yeast belonging to Saccharomyces genus) and culturing the cell, or treating the above mammal cell first with a reticuloendothelial system-activating substance (e.g. Gram-positive bacteria, cell of protozoan) and then with a water-soluble peptide glucomannan, and culturing the product. The concentrations of the reticuloendothelial system-activating substance and the water-soluble peptide glucomannan in the medium are 1ngW1,000μg/ml and 1W1,000μg/ml, respectively. The cultivation is carried out aerobically at 30W40°C in an atmosphere composed of e.g. 5% CO
2 gas and 95% air.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过使用源于微生物的水溶性肽葡甘露聚糖，获得对癌细胞具有细胞毒活性的物质和极高的安全性。构成：可以通过用源自微生物的水溶性肽葡甘露聚糖（例如从属于酵母属的啤酒酵母获得的SPGM-1）处理哺乳动物或哺乳动物来源的单核细胞来产生对癌细胞具有细胞毒性活性的物质）并培养细胞，或首先用网状内皮系统活化物质（例如革兰氏阳性菌，原生动物细胞）处理上述哺乳动物细胞，然后用水溶性肽葡甘露聚糖处理，并培养该产物。培养基中网状内皮系统活化物质和水溶性肽葡甘露聚糖的浓度分别为1ng-1,000mug / ml和1-1,000mug / ml。培养在30-40℃的有氧气氛中， 5％CO2气体和95％空气。

30. 发明专利

JP2004002368A Pharmaceutical composition 有权
公开(公告)号：JP2004002368A
公开(公告)日：2004-01-08
申请号：JP2003101362
申请日：2003-04-04
申请人： Tanabe Seiyaku Co Ltd , 田辺製薬株式会社
发明人： YASUDA KOUSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKODA MASAKATSU , MATSUMOTO TAKESHI , ARAKAWA KENJI
IPC分类号： C07D401/12 , A61K31/401 , A61K31/4025 , A61K31/4035 , A61K31/4155 , A61K31/422 , A61K31/423 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/48 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P31/18 , A61P37/02 , A61P37/06 , A61P43/00 , C07D207/16 , C07D207/404 , C07D207/416 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition comprising, as an effective ingredient, a novel aliphatic, nitrogen-containing, five-membered cyclic compound having an excellent DPPIV inhibiting action. SOLUTION: The pharmaceutical composition comprises:, as an effective ingredient, an aliphatic, nitrogen-containing, five-membered cyclic compound represented by general formula [I'] (wherein A is -CH 2 - or -S-; B is CH or N; R 1 is H, a lower alkyl group or the like; X is a single bond, -CO, -Alk-CO-, -COCH 2 -, -Alk-O-, -O-CH 2 -, -SO 2 -, -S-, -COO-, -CON(R 3 )-, -Alk-CON(R 3 )-, -CON(R 3 )CH 2 -, -NHCH 2 - or the like; R 3 is a hydrogen atom or a lower alkyl group; Alk is a lower alkylene group; R 2 is (1) an optionally substituted cyclic group or (2) a substituted amino group or the like; and when X is -CO-, B is N); or a pharmacologically acceptable salt thereof. COPYRIGHT: (C)2004,JPO

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