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11. 发明专利

DE69933660T2 未知
公开(公告)号：DE69933660T2
公开(公告)日：2007-08-23
申请号：DE69933660
申请日：1999-04-06
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , KITO TOKUNORI , MITSUYAMA JUNICHI , YAMAKAWA TETSUMI , KURODA HIROSHI , KAWAFUCHI HIROYO
IPC分类号： C07D401/04 , A61K31/47
摘要： Novel quinolonecarboxylic acid derivatives represented by general formula (1) which have potent antibacterial effects on gram-positive bacteria, in particular, Propionibacterium acnes, wherein R represents hydrogen or a carboxyl-protective group; R represents optionally substituted cycloalkyl; R represents hydrogen, halogeno, optionally substituted alkyl, alkoxy or alkylthio, optionally protected hydroxy or amino, or nitro; R represents optionally substituted alkyl or alkoxy; Z represents halogeno, optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, amino or pyridin-4-yl or pyridin-3-yl optionally having one or more substituents selected from among optionally substituted hydroxy and amino.

12. 发明专利

NO318813B1 未知
公开(公告)号：NO318813B1
公开(公告)日：2005-05-09
申请号：NO20002125
申请日：2000-04-26
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , YAMADA MINORU , HAMAMOTO SHOICHI , TAKAOKA KAZUKO , MATSUKURA HIROKO , YOTSUJI MINAKO , YONEZAWA KENJI , OJIMA KATSUJI , TAKAMATSU TAMOTSU , TAYA KYOKO , YAMAMOTO HIROHIKO , KIYOTO TARO , KOTSUBO HIRONORI
IPC分类号： A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56 , C07D401/04 , A61P31/04
摘要： This invention relates to processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula Ä1Ü which is useful as an antibacterial agent, and an intermediate thereof: wherein R represents a hydrogen atom or a carboxyl-protecting group; R represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio groups, nitro group, cyano group, acyl groups, protected or unprotected hydroxyl groups and protected or unprotected or substituted or unsubstituted amino groups; R represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio groups, protected or unprotected hydroxyl or imino groups, protected or unprotected or substituted or unsubstituted amino groups, alkylidene groups, oxo group and groups each forming a cycloalkane group together with the carbon atom to which R bonds; R represents a hydrogen atom, an amino-protecting group, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group; R represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl or amino group or a nitro group; and A represents CH or C-R in which R represents a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group, and to a salt of a 7-isoindoline-quinolonecarboxylic acid represented by the general formula Ä1Ü, a hydrate thereof and a composition comprising them as an active ingredient.

13. 发明专利

NO20043914L 未知
公开(公告)号：NO20043914L
公开(公告)日：2004-09-20
申请号：NO20043914
申请日：2004-09-20
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , OJIMA KATSUJI , HORI KOZO , OKUJO NORIYUKI , MITSUYAMA JUNICHI , KUNITANI KAZUTO , TOHDO KEISUKE
IPC分类号： A61K31/138 , A61K31/44 , A61P31/10 , C07C257/18 , C07C259/18 , C07C271/64 , C07C323/62 , C07D207/14 , C07D211/22 , C07D211/26 , C07D211/58 , C07D213/62 , C07D213/78 , C07D213/85 , C07D241/04 , C07D241/08 , C07D243/08 , C07D245/02 , C07D261/12 , C07D295/092 , C07D295/13 , C07D401/06 , C07D413/06 , A61K31/155 , A61K31/197
摘要： Arylamide derivatives (I) are new. Arylamide derivatives of formula (I) and their salts are new. [Image] X : optionally substituted lower alkylene or alkenylene; G 1O, S or NH; G 2C or N; R aH, halo or optionally substituted alkyl, cycloalkyl or alkoxy; R 1optionally protected or substituted amidino; R 2NR 3R 4, NR 5YNR 6R 7 or a group of formula (i); R 3H, amino protecting group, a group of formula (ii) or optionally substituted cycloalkyl or alkenyl; W : a bond or optionally substituted alkylene; Y coptionally substituted 2-4C alkylene; Y c1optionally substituted 1-4C alkylene; R 7bH, amino protecting group, a group of formula (iii) or optionally substituted alkyl, cycloalkyl or alkenyl; Z : optionally substituted lower alkylene or alkenylene; G 3O, S, NH or bond; G 5C or N; R bH, halo or optionally substituted alkyl, cycloalkyl or alkoxy; R 8para or meta to G 3 and is optionally protected or substituted amidino; R 4-R 6H, amino protecting group or optionally substituted alkyl, cycloalkyl or alkenyl; Y : optionally substituted 2-6C alkyelene or 3-6C alkenylene; R 7R 4 or (iii); Y aoptionally substituted 2-4C alkylene; Y boptionally substituted 1-4C alkylene; G 4C or N; R 7aalkyl (optionally substituted by at least one CN, NO 2, halo, sulfo, phosphoryl, lower alkenyl, lower alkoxy, heterocyclyl, cycloalkyl, lower alkylidene, SH, amidinophenylaryloxy, aryloxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower alkylcarbamoyl, lower alkylsulfonylamino, lower alkylaminosulfonyl, lower carboxylalkenyl, lower alkoxyimino or optionally protected hydroxyl, amino, carbamoyl, hydrocarbamoyl, aminosulfonyl, cyclic amino or lower alkylamino), (iii) or optionally substituted phenyl, cycloalkyl or alkenyl, provided that when G 1 = NH, then X = optionally substituted 3-6C alkylene or alkenylene. [Image] ACTIVITY : Fungicide. In cytotoxicity assays, 4-[2-[1-(3-[4-[amino(imino)methyl]phenoxy]propyl)-4-piperidinyl]ethoxy]benzamidine hydrochloride (Ia) had an IC 50 value for Candida albicans TIMM1623 of 0.0039 mu g/ml. MECHANISM OF ACTION : None given.

14. 发明专利

ES2188890T3 未知
公开(公告)号：ES2188890T3
公开(公告)日：2003-07-01
申请号：ES97902618
申请日：1997-02-07
申请人： TOYAMA CHEMICAL CO LTD
发明人： TODO YOZO , HAYASHI KAZUYA , TAKAHATA MASAHIRO , WATANABE YASUO , NARITA HIROKAZU
IPC分类号： C07D401/04 , C07F5/02 , A61K31/475
摘要： Quinolonecaboxylic acid derivatives represented by general formula (I) or salts of these. Preferred are compounds wherein R represents optionally substituted cycloalkyl, R represents at least one member selected among hydrogen, halogeno, optionally substituted lower alkyl or alkoxy, and optionally protected hydroxy or amino, R represents hydrogen or optionally substituted lower alkyl, R and R each represents hydrogen, and A represents C-Y (where Y represents halogeno, lower alkyl or alkoxy each optionally substituted by halogeno, or optionally protected hydroxy).

15. 发明专利

DE69717970D1 未知
公开(公告)号：DE69717970D1
公开(公告)日：2003-01-30
申请号：DE69717970
申请日：1997-02-07
申请人： TOYAMA CHEMICAL CO LTD
发明人： TODO YOZO , HAYASHI KAZUYA , TAKAHATA MASAHIRO , WATANABE YASUO , NARITA HIROKAZU
IPC分类号： C07D401/04 , C07F5/02 , A61K31/475
摘要： Quinolonecaboxylic acid derivatives represented by general formula (I) or salts of these. Preferred are compounds wherein R represents optionally substituted cycloalkyl, R represents at least one member selected among hydrogen, halogeno, optionally substituted lower alkyl or alkoxy, and optionally protected hydroxy or amino, R represents hydrogen or optionally substituted lower alkyl, R and R each represents hydrogen, and A represents C-Y (where Y represents halogeno, lower alkyl or alkoxy each optionally substituted by halogeno, or optionally protected hydroxy).

16. 发明专利

NO312032B1 未知
公开(公告)号：NO312032B1
公开(公告)日：2002-03-04
申请号：NO970622
申请日：1997-02-11
申请人： TOYAMA CHEMICAL CO LTD
发明人： TODO YOZO , HAYASHI KAZUYA , TAKAHATA MASAHIRO , WATANABE YASUO , NARITA HIROKAZU
IPC分类号： C07D401/04 , C07D471/04 , C07D498/06 , C07F7/22 , A61K31/4709 , A61P31/04
摘要： This invention relates to a novel quinolone- or naphthyridone-carboxylic acid derivative or its salt useful as an antibacterial agent, said derivative has a substituent represented by the following formula at the 7 position: wherein preferably R represents at least one member selected from the group consisting of a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl, lower alkoxy or lower alkylthio group, a nitro group, a cyano group, a protected or unprotected hydroxyl group and a protected or unprotected amino group; R represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkylidene group and a group forming a cycloalkane ring together with the carbon atom to which R is bonded; and R represents a hydrogen atom or a substituted or unsubstituted lower alkyl or cycloalkyl group.

17. 发明专利

NO20042109L 未知
公开(公告)号：NO20042109L
公开(公告)日：2000-06-07
申请号：NO20042109
申请日：2004-05-21
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , YAMADA MINORU , HAMAMOTO SHOICHI , TAKAOKA KAZUKO , MATSUKURA HIROKO , YOTSUJI MINAKO , YONEZAWA KENJI , OJIMA KATSUJI , TAKAMATSU TAMOTSU , TAYA KYOKO , YAMAMOTO HIROHIKO , KIYOTO TARO , KOTSUBO HIRONORI
IPC分类号： A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56 , C07D401/04 , C07F5/02
摘要： This invention relates to processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula Ä1Ü which is useful as an antibacterial agent, and an intermediate thereof: wherein R represents a hydrogen atom or a carboxyl-protecting group; R represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio groups, nitro group, cyano group, acyl groups, protected or unprotected hydroxyl groups and protected or unprotected or substituted or unsubstituted amino groups; R represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio groups, protected or unprotected hydroxyl or imino groups, protected or unprotected or substituted or unsubstituted amino groups, alkylidene groups, oxo group and groups each forming a cycloalkane group together with the carbon atom to which R bonds; R represents a hydrogen atom, an amino-protecting group, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group; R represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl or amino group or a nitro group; and A represents CH or C-R in which R represents a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group, and to a salt of a 7-isoindoline-quinolonecarboxylic acid represented by the general formula Ä1Ü, a hydrate thereof and a composition comprising them as an active ingredient.

18. 发明专利

NZ336499A Isoindoline boron compounds and their use in preparing quinolonecarboxylic acids 未知
公开(公告)号：NZ336499A
公开(公告)日：1999-11-29
申请号：NZ33649997
申请日：1997-02-07
申请人： TOYAMA CHEMICAL CO LTD
发明人： TAKAHATA MASAHIRO , TODO YOZO , HAYASHI KAZUYA , WATANABE YASUO , NARITA HIROKAZU
IPC分类号： A61K31/475 , C07D401/04 , C07F5/02
摘要： An isoindoline boron compound of the formula (I). The variables are as defined in the specification. These compounds are used in the preparation of quinolonecarboxylic acid derivatives.

19. 发明专利

CA2327328A1 QUINOLONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF 未知
公开(公告)号：CA2327328A1
公开(公告)日：1999-10-14
申请号：CA2327328
申请日：1999-04-06
申请人： TOYAMA CHEMICAL CO LTD
发明人： KAWAFUCHI HIROYO , KURODA HIROSHI , HAYASHI KAZUYA , YAMAKAWA TETSUMI , KITO TOKUNORI , MITSUYAMA JUNICHI
IPC分类号： C07D401/04 , A61K31/47
摘要： Novel quinolonecarboxylic acid derivatives represented by general formula (1 ) which have potent antibacterial effects on gram-positive bacteria, in particular, Propionibacterium acnes, wherein R1 represents hydrogen or a carboxyl-protective group; R2 represents optionally substituted cycloalkyl; R3 represents hydrogen, halogeno, optionally substituted alkyl, alkoxy or alkylthio, optionally protected hydroxy or amino, or nitro; R4 represents optionally substituted alkyl or alkoxy; Z represents halogeno, optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, amino or pyridin- 4- yl or pyridin-3-yl optionally having one or more substituents selected from among optionally substituted hydroxy and amino.

20. 发明专利

HU9901966A2 QUINOLONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF 未知
公开(公告)号：HU9901966A2
公开(公告)日：1999-09-28
申请号：HU9901966
申请日：1997-02-07
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , NARITA HIROKAZU , TAKAHATA MASAHIRO , TODO YOZO , WATANABE YASUO
IPC分类号： C07D401/04 , C07F5/02 , A61K31/475
摘要： Quinolonecaboxylic acid derivatives represented by general formula (I) or salts of these. Preferred are compounds wherein R represents optionally substituted cycloalkyl, R represents at least one member selected among hydrogen, halogeno, optionally substituted lower alkyl or alkoxy, and optionally protected hydroxy or amino, R represents hydrogen or optionally substituted lower alkyl, R and R each represents hydrogen, and A represents C-Y (where Y represents halogeno, lower alkyl or alkoxy each optionally substituted by halogeno, or optionally protected hydroxy).

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