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1. 发明公开

EP1967190A4 NOVEL ARYLAMIDINE DERIVATIVE, SALT THEREOF AND ANTIFUNGAL AGENT CONTAINING THOSE 有权
标题翻译：新芳酰胺衍生物，盐，和那些含有抗真菌剂
公开(公告)号：EP1967190A4
公开(公告)日：2009-08-26
申请号：EP06843443
申请日：2006-12-27
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA
IPC分类号： A61K31/445 , A61P31/10 , C07D211/22
CPC分类号： C07D211/22
摘要： Disclosed is an arylamidine derivative represented by the following general formula: [Chemical formula] (wherein R 1 and R 2 independently represent an optionally substituted C 3-4 alkyl group) or a salt thereof, which is useful as an antifungal agent.

2. 发明公开

EP1481966A4 NOVEL ARYLAMIDINE DERIVATIVE OR SALT THEREOF 有权转让
标题翻译： NEUES ARYLAMIDINDERIVAT BZW. SALZ DAVON
公开(公告)号：EP1481966A4
公开(公告)日：2005-11-23
申请号：EP03743600
申请日：2003-03-04
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 , A61K31/198 , A61K31/445 , A61K31/495 , A61K31/551
CPC分类号： C07D413/06 , C07C257/18 , C07C259/18 , C07C271/64 , C07C323/62 , C07D207/14 , C07D211/22 , C07D211/26 , C07D211/58 , C07D213/78 , C07D213/85 , C07D241/04 , C07D241/08 , C07D243/08 , C07D245/02 , C07D261/12 , C07D295/088 , C07D295/13 , C07D401/06 , Y02P20/55
摘要： An arylamidine derivative represented by the general formula (1) (wherein X means optionally substituted lower alkylene or alkenylene; G1 means oxygen, sulfur, or imino; G2 means carbon or nitrogen; Ra means at least one member selected among hydrogen, halogeno, and optionally substituted alkyl, cycloalkyl, and alkoxy; R1 means optionally protected or substituted amidino; and R2 means substituted amino, substituted cyclic amino, etc.) or a salt of the derivative. The derivative or salt has excellent antifungal activity and is highly safe. It is hence useful as a fungicide with satisfactory behavior in the body.
摘要翻译：由通式（1）表示的芳基脒衍生物（其中X表示任选取代的低级亚烷基或亚烯基; G1表示氧，硫或亚氨基; G2表示碳或氮; Ra表示选自氢，卤素和任选取代的烷基，环烷基和烷氧基; R 1表示任选被保护的或取代的脒基;并且R 2表示取代的氨基，取代的环状氨基等）或该衍生物的盐。该衍生物或盐具有优异的抗真菌活性并且高度安全。因此，它在体内具有令人满意的行为，是一种有效的杀菌剂。

3. 发明公开

EP0882725A4 QUINOLONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF 失效
标题翻译：喹啉二氧化碳衍生物及其盐
公开(公告)号：EP0882725A4
公开(公告)日：1999-05-06
申请号：EP97902618
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
CPC分类号： C07D401/04 , C07F5/025
摘要： Quinolonecarboxylic acid derivatives represented by general formula (I) or salts of these. Preferred are compounds wherein R2 represents optionally substituted cycloalkyl, R3 represents at least one member selected among hydrogen, halogeno, optionally substituted lower alkyl or alkoxy, and optionally protected hydroxy or amino, R4 represents hydrogen or optionally substituted lower alkyl, R?5 and R6¿ 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).

4. 发明公开

EP1767526A4 NOVEL ARYLAMIDINE DERIVATIVE, SALT THEREOF, AND ANTIFUNGAL CONTAINING THESE 有权转让
标题翻译：新ARYLAMIDINDERIVAT，盐，和那些含有杀菌剂
公开(公告)号：EP1767526A4
公开(公告)日：2009-05-06
申请号：EP05765373
申请日：2005-06-28
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , KUNITANI KAZUTO , UEHARA SAYURI , MORITA TEIICHI
IPC分类号： C07D211/22 , A61K31/445 , A61P31/10
CPC分类号： C07D211/22
摘要： An arylamidine derivative represented by the general formula (wherein R1 represents optionally protected or substituted amidino; and R2 and R3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivative and salt have potent activity against fungi including ones having tolerance to azole type drugs and further have high safety and excellent properties in a repeated dose toxicity test. They are hence useful as an excellent antifungal.

5. 发明公开

EP1070713A4 QUINOLONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF 有权
标题翻译：喹诺酮羧酸衍生物或它的盐
公开(公告)号：EP1070713A4
公开(公告)日：2004-09-01
申请号：EP99912111
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
CPC分类号： C07D401/04 , Y02P20/55
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.

6. 发明公开

EP1031569A4 PROCESSES FOR PRODUCING 7-ISOINDOLINEQUINOLONECARBOXYLIC DERIVATIVES AND INTERMEDIATES THEREFOR, SALTS OF 7-ISOINDOLINEQUINOLONECARBOXYLIC ACIDS, HYDRATES THEREOF, AND COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT 有权
标题翻译：用于生产7-ISOINDOLINCHINOLONCARBONSÄUREDERIVATEN和中间产品，第7-ISOINDOLINCHINOLONCARBONSÄURENITS水盐和成分含有这些作为活性成分含
公开(公告)号：EP1031569A4
公开(公告)日：2003-04-23
申请号：EP98950405
申请日：1998-10-27
申请人： TOYAMA CHEMICAL CO LTD
发明人： YAMADA MINORU , HAMAMOTO SHOICHI , HAYASHI KAZUYA , 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 , A61K31/47 , B01J23/44 , B01J31/24 , C07C311/04 , C07C311/17 , C07D215/32 , C07F5/02
CPC分类号： C07D401/04 , A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56 , C07F5/025 , Y02P20/55
摘要： Processes for producing 7-isoindolinequinolonecarboxylic derivatives useful as antibacterials and represented by general formula (1) and intermediates therefor; salts of 7-isoindolinequinolonecarboxylic derivatives represented by formula (1) and hydrates thereof; and compositions containing the same as the active ingredient: (1) wherein R1 represents hydrogen or a carboxyl-protecting group; R2 represents cycloalkyl etc.; R3 represents at least one member selected among hydrogen, halogen, and the like; R4 represents at least one member selected among hydrogen, optionally substituted alkyl, and the like; R5 represents hydrogen, optionally substituted alkyl, etc.; R6 represents hydrogen etc.; and A represents CH or C-R7, wherein R7 represents alkoxy etc.

7. 发明公开

EP0775702A4 NOVEL QUINOLONE- OR NAPHTHYRIDONECARBOXYLIC ACID DERIVATIVE OR SALT THEREOF 失效
标题翻译：新喹诺酮或NAPHTHYRIDONCARBONSÄUREDERIVATE或其盐
公开(公告)号：EP0775702A4
公开(公告)日：1997-11-05
申请号：EP95927967
申请日：1995-08-04
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 , A61K31/435 , A61K31/47
CPC分类号： C07D401/04 , C07D471/04 , C07F7/2212
摘要： A quinolone- or naphthyridonecarboxylic acid derivative having a skeleton represented by general formula (I) at the 7-position and being useful as an antibacterial or a salt thereof, wherein R3 represents at least one group selected from among hydrogen, halogen, optionally substituted lower alkyl, lower alkoxy, lower alkylthio, nitro, cyano, optionally protected hydroxy and optionally protected amino; R4 represents at least one group selected from among hydrogen, optionally substituted lower alkyl, lower alkylidene and a group which forms a cycloalkane ring together with the carbon atom to which R4 is bonded; and R5 represents hydrogen, optionally substituted lower alkyl or cycloalkyl.

8. 发明专利

CY1113266T1 ΠΑΡΑΓΩΓΟ ΑΡΥΛΑΜΙΔΙΝΗΣ, ΑΛΑΣ ΑΥΤΟΥ ΚΑΙ ΑΝΤΙΜΥΚΗΤΙΑΣΙΚΟ ΠΕΡΙΕΧΟΝ ΑΥΤΑ 未知
公开(公告)号：CY1113266T1
公开(公告)日：2016-04-13
申请号：CY121101031
申请日：2012-10-30
申请人： TOYAMA CHEMICAL CO LTD
发明人： HAYASHI KAZUYA , KUNITANI KAZUTO , UEHARA SAYURI , MORITA TEIICHI
IPC分类号： C07D211/22 , A61K31/445 , A61P31/10
摘要： Έναπαράγωγοαρυλαμιδίνηςπουπαριστάνεταιμετογενικότύπο (όπουτο R1 παριστάνειπροαιρετικώςπροστατευμένηή υποκατεστημένηαμιδινο· καιτα R2 και R3 είναιταίδιαή διαφορετικάκαιτοκαθέναπαριστάνειυδρογόνοή αλογόνο) ήέναάλαςτουπαραγώγου. Τοπαράγωγοκαιτοάλαςέχουνισχυρήδραστικότητακατάμυκήτωνσυμπεριλαμβανόμενωναυτώνπουέχουνανοχήσεφάρμακατύπουαζόληςκαιπεραιτέρωέχουνυψηλήασφάλειακαιεξαιρετικέςιδιότητεςσεμιαδοκιμασίατοξικότηταςμεεπαναλαμβανόμενηδόση. Συνεπώςείναιχρήσιμαωςέναεξαιρετικόαντιμυκητιασικό.

9. 发明专利

AT517080T 未知
公开(公告)号：AT517080T
公开(公告)日：2011-08-15
申请号：AT03743600
申请日：2003-03-04
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： C07C257/18 , A61K31/138 , A61K31/155 , A61K31/197 , A61K31/198 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/551 , A61P31/10 , 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
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.

10. 发明专利

AT461186T 未知
公开(公告)号：AT461186T
公开(公告)日：2010-04-15
申请号：AT98950405
申请日：1998-10-27
申请人： TOYAMA CHEMICAL CO LTD
发明人： YAMADA MINORU , HAMAMOTO SHOICHI , HAYASHI KAZUYA , TAKAOKA KAZUKO , MATSUKURA HIROKO , YOTSUJI MINAKO , YONEZAWA KENJI , OJIMA KATSUJI , TAKAMATSU TAMOTSU , TAYA KYOKO , YAMAMOTO HIROHIKO , KIYOTO TARO , KOTSUBO HIRONORI
IPC分类号： C07D401/04 , A61K31/47 , A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56
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.

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