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1. 发明申请

WO2007066784A3 DIARYLETHER DERIVATIVES AS ANTITUMOR AGENTS 审中-公开
标题翻译：二甲苯衍生物作为抗菌剂
公开(公告)号：WO2007066784A3
公开(公告)日：2007-10-25
申请号：PCT/JP2006324610
申请日：2006-12-04
申请人： OTSUKA PHARMA CO LTD , MATSUYAMA HIRONORI , OHNISHI KENJI , NAKAGAWA TAKASHI , TAKASU HIDEKI , SAKAMOTO MAKOTO , HIGUCHI KUMI , MIYAJIMA KEISUKE , YAMADA SATOSHI , MOTOYAMA MASAAKI , KOJIMA YUTAKA , YASUMURA KOICHI , KODAMA TAKESHI , OTSUJI SHUN , KAN KEIZO , SUMIDA TAKUMI
发明人： MATSUYAMA HIRONORI , OHNISHI KENJI , NAKAGAWA TAKASHI , TAKASU HIDEKI , SAKAMOTO MAKOTO , HIGUCHI KUMI , MIYAJIMA KEISUKE , YAMADA SATOSHI , MOTOYAMA MASAAKI , KOJIMA YUTAKA , YASUMURA KOICHI , KODAMA TAKESHI , OTSUJI SHUN , KAN KEIZO , SUMIDA TAKUMI
IPC分类号： A61K31/495 , A61K31/496 , A61P35/00
CPC分类号： A61K31/496 , A61K31/495
摘要： An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X 1 represents a nitrogen atom or a group -CH=, R 1 represents a group -Z-R 6 , in which Z represents a group -CO-, a group -CH(OH)- or the like, R 6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R 2 represents a hydrogen atom or a halogen atom, Y represents a group -O-, a group -CO-, a group -CH(OH)- or a lower alkylene group, and A represents [Formula 2] wherein R 3 represents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, R 4 represents an imidazolyl lower alkyl group or the like.
摘要翻译：本发明的目的在于提供一种抗肿瘤活性大大提高的安全性药物。根据本发明，提供了含有下列通式（1）表示的化合物或其盐作为有效成分的药物：[1]其中X 1代表氮原子或基团-CH =，R 1表示基团-ZR 6，其中Z表示基团-CO-，基团-CH（OH） - 或 R 6表示具有1至4个氮原子，氧原子或硫原子的5至15元单环，二环或三环饱和或不饱和杂环基，R 2， SUP>表示氢原子或卤素原子，Y表示-O-基团，-CO-基团，-CH（OH）基或低级亚烷基，A表示[式2]其中R ^{3 表示氢原子，低级烷氧基等，p表示1或2，R 4表示咪唑基低级烷基等。}

2. 发明申请

WO2009057811A3 HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION THEREOF 审中-公开
标题翻译：杂环化合物及其药物组合物
公开(公告)号：WO2009057811A3
公开(公告)日：2009-07-09
申请号：PCT/JP2008070153
申请日：2008-10-29
申请人： OTSUKA PHARMA CO LTD , SUMIDA TAKUMI , TABUSA FUJIO , SEKIGUCHI KAZUO , KODAMA TAKESHI , YASUMURA KOICHI , KOJIMA YUTAKA , MOTOYAMA MASAAKI , MIYAJIMA KEISUKE , YOSHIDA KENJI , KAN KEIZO , SAKAMOTO MAKOTO , TAKASU HIDEKI , NAKAGAWA TAKASHI , OHI NAOTO , HARADA YASUO , HASHIMOTO NORIKAZU , MATSUYAMA HIRONORI , IIDA MASATOSHI , FUJITA SHIGEKAZU , FUKUSHIMA TAE
发明人： SUMIDA TAKUMI , TABUSA FUJIO , SEKIGUCHI KAZUO , KODAMA TAKESHI , YASUMURA KOICHI , KOJIMA YUTAKA , MOTOYAMA MASAAKI , MIYAJIMA KEISUKE , YOSHIDA KENJI , KAN KEIZO , SAKAMOTO MAKOTO , TAKASU HIDEKI , NAKAGAWA TAKASHI , OHI NAOTO , HARADA YASUO , HASHIMOTO NORIKAZU , MATSUYAMA HIRONORI , IIDA MASATOSHI , FUJITA SHIGEKAZU , FUKUSHIMA TAE
IPC分类号： C07D401/12 , A61K31/444 , A61K31/506 , A61P1/16 , C07D403/12
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5-Z1-, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group -CO-, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.
摘要翻译：本发明提供由通式（1）表示的杂环化合物：其中R1为R5-Z1-基团等，Z1为低级亚烷基等，R5为通式所示的基团。其中R 13为氢原子等，m为1至5的整数; R2是氢原子：Y是CH或N：A1是选自吲哚二基的杂环，其中杂环可以具有至少一个取代基：T是-CO-等：R3是氢原子等：R4是任选被一个或多个羟基取代的低级烷基等：R 3和R 4与它们所结合的氮原子一起可以彼此结合形成5- 10元饱和杂环，其中杂环可以具有至少一个取代基。本发明的杂环化合物具有抑制胶原蛋白的生成和/或治疗肿瘤的优异效果。

3. 发明申请

WO2006014012A3 AROMATIC COMPOUNDS 审中-公开
标题翻译：芳香化合物
公开(公告)号：WO2006014012A3
公开(公告)日：2006-12-07
申请号：PCT/JP2005014611
申请日：2005-08-03
申请人： OTSUKA PHARMA CO LTD , FUKUSHIMA TAE , MATSUMURA SHUJI , TAKEMURA NORIAKI , SATOU HIDEAKI , ITO NOBUAKI , SHITSUTA TAKUYA , TSUTSUI HIRONORI , TANAKA MICHINORI , KAN KEIZO , NAGAO HITOSHI , WATANABE KENJI , TAI KUNINORI , NAKAGAWA TAKASHI , TAKASU HIDEKI , SAKAMOTO MAKOTO , MIYAJIMA KEISUKE , YAMADA SATOSHI , KOJIMA YUTAKA , YASUMURA KOICHI , OHI NAOTO , OKUNO MITSUHIRO , SUGIYAMA KAZUHISA , KIYONO KUNIHIKO , SUZUKI TAKASHI , AKAMATSU SEIJI , KODAMA TAKESHI , YANAGIHARA YASUO , SUMIDA TAKUMI
发明人： FUKUSHIMA TAE , MATSUMURA SHUJI , TAKEMURA NORIAKI , SATOU HIDEAKI , ITO NOBUAKI , SHITSUTA TAKUYA , TSUTSUI HIRONORI , TANAKA MICHINORI , KAN KEIZO , NAGAO HITOSHI , WATANABE KENJI , TAI KUNINORI , NAKAGAWA TAKASHI , TAKASU HIDEKI , SAKAMOTO MAKOTO , MIYAJIMA KEISUKE , YAMADA SATOSHI , KOJIMA YUTAKA , YASUMURA KOICHI , OHI NAOTO , OKUNO MITSUHIRO , SUGIYAMA KAZUHISA , KIYONO KUNIHIKO , SUZUKI TAKASHI , AKAMATSU SEIJI , KODAMA TAKESHI , YANAGIHARA YASUO , SUMIDA TAKUMI
IPC分类号： C07D295/192 , C07C233/67 , C07D211/46 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/75 , C07D239/42 , C07D241/20 , C07D295/185 , C07D317/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14
CPC分类号： C07C229/18 , C07C205/38 , C07C217/90 , C07C233/45 , C07C233/75 , C07C271/58 , C07C275/34 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D211/46 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/75 , C07D239/42 , C07D241/20 , C07D295/185 , C07D295/192 , C07D317/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X 1 represents a nitrogen atom or a group -CH=; R 1 represents a group -Z-R 6 , wherein Z represents a group -CO-, a group -CH(OH)-, or the like, and R 6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R 2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group -O-, a group -CO-, a group -CH(OH)-, a lower alkylene group, or the like; and (A) represents a group or the like, wherein R 3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R 4 represents an imidazolyl lower alkyl group or the like.
摘要翻译：本发明提供了一种新颖的化合物，其具有优异的抑制胶原产生的效果和较少的副作用。本发明的化合物由下列通式（1）表示：其中X 1表示氮原子或基团-CH =; R 1表示基团-ZR 6，其中Z表示-CO-基团，-CH（OH） - 基等基团，R“ 6表示具有1至4个氮原子，氧原子或硫原子的5至15元单环，二环或三环饱和或不饱和杂环基; R 2表示氢原子，卤素原子或低级亚烷基; Y表示基团-O-，基团-CO-，基团-CH（OH） - ，低级亚烷基基团等; 和（A）表示基团等，其中R 3表示氢原子，低级烷氧基等，p表示1或2，R 4 O >表示咪唑基低级烷基等。

4. 发明专利

JPH0881443A EXTRACELLULAR MATRIX METAL PROTEASE INHIBITOR 失效
公开(公告)号：JPH0881443A
公开(公告)日：1996-03-26
申请号：JP21689094
申请日：1994-09-12
申请人： OTSUKA PHARMA CO LTD
发明人： SAKAMOTO MAKOTO , IMAOKA TAKESHI , MOTOYAMA MASAAKI , YAMAMOTO SAKAHITO , TAKASU HIDEKI
IPC分类号： C12N9/99 , A61K31/47 , A61K31/535 , A61P35/00 , A61P43/00 , C07D215/38 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D491/056
摘要： PURPOSE: To obtain a compound useful for treating rheumatoid arthritis disease, having high inhibitory activity against extracellular matrix metal protease, low toxicity, excellent oral absorbability, long duration time, high stability and stability of medicine, shown by a specific formula. CONSTITUTION: This compound of formula I [R is H or AR (A is a lower alkylene; R is H, amino, phthalimide, etc.); R is H or a lower alkyl; R is H, OH, a lower alkoxy (lower alkoxy), etc.; R is H, a halogen, OH, a lower alkoxy, etc.; R is H, benzoyl, etc.; R is a 1-12C alkyl, a lower alkoxy lower alkyl, etc.; (n) is 1 or 2], preferably 3S-[4-(N-hydroxyamino)-2R- isobutylsuccinyl]amino-1-methyl-6,7-methylenedioxy-3,4-dihydroxycarbos tyril, etc. For example, preferably a carboxylic acid of formula II is reacted with an alkylhalocarboxylic acid to give a mixed acid anhydride, which is reacted with an amine of formula III.

5. 发明专利

JPH07157470A CARBOSTYRIL DERIVATIVE 失效
公开(公告)号：JPH07157470A
公开(公告)日：1995-06-20
申请号：JP4822494
申请日：1994-03-18
申请人： OTSUKA PHARMA CO LTD
发明人： SAKAMOTO MAKOTO , IMAOKA TAKESHI , MOTOYAMA MASAAKI , YAMAMOTO SAKAHITO , TAKASU HIDEKI
IPC分类号： C07D215/38 , A61K31/47 , A61P35/00 , A61P43/00 , C07D215/58 , C07D401/12 , C07D409/12
摘要： PURPOSE:To obtain the subject new compound, excellent in inhibiting actions on extracellular matrix metalloproteases, oral absorbability and safety, having low toxicity and a long duration, and useful for preventing and treating metastasis or infiltration of cancerous cells and nephritis, etc. CONSTITUTION:This compound is expressed by formula I [R is H or A-R (A is a lower alkylene; R is H, amino, etc.); R is H or a lower alkyl; R is H, OH, etc.; R is H, a halogen, etc.; R is H, benzoyl, etc.; R is a 1-12C alkyl, a lower alkoxy-lower alkyl, etc.; (n) is l or 2] or its salt, e.g. 3S-[4-(N- hydroxyamino)-2R-isobutylsuccinyl]amino-3,4-dihydrocarbostyril. The compound is obtained by reacting a carboxylic acid expressed by formula II with an amine compound expressed by the formula R ONH2 preferably according to an active ester method, etc. Furthermore, the compound expressed by formula II is prepared by releasing a group R of a compound expressed by formula III (R and R are each a releasable ester), then reacting the prepared product with a compound expressed by formula IV and subsequently deprotecting the resultant product.

6. 发明专利

JPH08325232A CARBOSTYRIL DERIVATIVE 失效
公开(公告)号：JPH08325232A
公开(公告)日：1996-12-10
申请号：JP13654395
申请日：1995-06-02
申请人： OTSUKA PHARMA CO LTD
发明人： SAKAMOTO MAKOTO , TAKASU HIDEKI , MOTOYAMA MASAAKI , KIYONO KUNIHIKO , OTA KAZUHIDE
IPC分类号： C07D215/22 , A61K31/47 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D215/58
摘要： PURPOSE: To obtain a carbostyril derivative having high inhibiting action against extracellular matrix metal protease and useful e.g. as an agent for preventing the metastasis and infiltration of various cancer cells. CONSTITUTION: This carbostyril derivative is a compound of formula I (R is H, a lower alkyl, etc.; R is H or a lower alkylenedioxy; R is H or a phenyl- lower alkyl; R is a lower alkyl), e.g. 3S-[2R-(2,2-dimethyl-4-oxo-1,3-dioxalan-5S- yl)-4-methylentanoyl]amino-1-ethyl-6,7-methylenedioxy-3,4-dihydrocarbo styril. The subject compound of formula I can be produced by the amino bond forming reaction of a carboxylic acid of formula II with an amine compound of formula III.

7. 发明专利

JP2001089450A PYRIDINE DERIVATIVE-CONTAINING MEDICINAL PREPARATION 失效
公开(公告)号：JP2001089450A
公开(公告)日：2001-04-03
申请号：JP26901699
申请日：1999-09-22
申请人： OTSUKA PHARMA CO LTD
发明人： EDAMATSU HIROSHI , NAGAHAMA TAKAO , HAYAKAWA SATOSHI , KOJIMA YUTAKA , SAKAMOTO MAKOTO , YASUMURA KOICHI
IPC分类号： C07D213/64 , A61K31/44 , A61K31/443 , A61P1/16 , C07D213/75 , C07D213/81 , C07D405/12
摘要： PROBLEM TO BE SOLVED: To obtain a medicinal preparation excellent in effect of suppressing the production of collagen. SOLUTION: This pyridine derivative-containing medicinal preparation is obtained by incorporating a pyridine derivative expressed by a general formula (1) [R1 is a halogen atom or a halogen-substituted lower alkyl group; R2, R3 are each H or a halogen atom; V is a group of C=O, NH or the like; and A is a group A1, group A2 or group A3 (groups in A1 to A3 are each H, a lower alkyl group, a lower alkanoyl group, hydroxyl group, benzoyl group, oxo group or the like) or its medicinally permissible salt as an active ingredient.

8. 发明专利

JP2001089412A BENZENE DERIVATIVE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT 失效
公开(公告)号：JP2001089412A
公开(公告)日：2001-04-03
申请号：JP26901599
申请日：1999-09-22
申请人： OTSUKA PHARMA CO LTD
发明人： KOJIMA YUTAKA , SAKAMOTO MAKOTO , YASUMURA KOICHI
IPC分类号： C07D213/75 , A61K31/165 , A61K31/167 , A61K31/505 , A61P1/16 , A61P11/00 , A61P13/12 , A61P27/02 , A61P43/00 , C07C43/29 , C07C49/84 , C07C233/75 , C07C275/36 , C07C317/24 , C07C323/22 , C07C323/42
摘要： PROBLEM TO BE SOLVED: To obtain a new compound excellent in effects on suppression of the collagen production and suitable especially as a therapeutic agent for pulmonary fibrosis and hepatic fibrosis. SOLUTION: This benzene derivative is represented by formula (1) [R1 denotes hydrogen atom or the like; a denotes an integer of 1-5; V denotes a group of NHC(=O) or the like; B denotes formula (2) ; A denotes a group A1 represented by formula (3) (R2 denotes hydrogen atom or the like) or the like; and b denotes an integer of 1-5], specifically represented by, e.g. formula (4) or its pharmaceutically acceptable salt.

9. 发明专利

CA2813153C 4-(METHYLAMINOPHENOXY) PYRDIN-3-YL-BENZAMIDE DERIVATIVES FOR TREATING CANCER 未知
公开(公告)号：CA2813153C
公开(公告)日：2019-01-15
申请号：CA2813153
申请日：2011-10-03
申请人： OTSUKA PHARMA CO LTD
发明人： NAKAGAWA TAKASHI , SAKAMOTO MAKOTO , YAMAGUCHI KAZUYA , TERAUCHI YUKI , SHIRAKURA MASAMICHI , HARADA YASUO , KOJIMA YUTAKA , SUMIDA TAKUMI
IPC分类号： C07D213/75 , A61K31/44 , A61P35/00
摘要： The present invention provides a compound represented by the following general formula (1) (see formula 1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different. The compound may be used to treat cancer.

10. 发明专利

CY1115171T1 ΙΑΤΡΙΚΟ ΦΑΡΜΑΚΟ 未知
公开(公告)号：CY1115171T1
公开(公告)日：2016-12-14
申请号：CY141100316
申请日：2014-05-05
申请人： OTSUKA PHARMA CO LTD
发明人： MATSUYAMA HIRONORI , OHNISHI KENJI , NAKAGAWA TAKASHI , TAKASU HIDEKI , SAKAMOTO MAKOTO , HIGUCHI KUMI , MIYAJIMA KEISUKE , YAMADA SATOSHI , MOTOYAMA MASAAKI , KOJIMA YUTAKA , YASUMURA KOICHI , KODAMA TAKESHI , OTSUJI SHUN , KAN KEIZO , SUMIDA TAKUMI
IPC分类号： A61K31/495 , A61K31/496 , A61P35/00
摘要： Ένααντικείμενοτηςπαρούσαςεφεύρεσηςείναιναπαρέχειιατρικόφάρμακοπολύβελτιωμένοστηδραστικότητακατάτουόγκουκαιεξαιρετικήςασφάλειας. Σύμφωναπροςτηνπαρούσαεφεύρεση, παρέχεταιέναιατρικόφάρμακοπουπεριέχειμίαένωσηπουαντιπροσωπεύεταιαπότονακόλουθογενικότύπο (1) ήάλαςαυτήςωςδραστικόσυστατικό: [Τύπος 1] όπουτοΧ1, αντιπροσωπεύειάτομοαζώτουή μιαομάδα -CH =, το R1 αντιπροσωπεύειμιαομάδα -ZR6, όπουτοΖ αντιπροσωπεύειμίαομάδα -CO-, ομάδα -CH(OH)- ήτιςπαρόμοιες, το R6 αντιπροσωπεύει 5-μελήέως 15-μελήμονοκυκλική, δικυκλικήή τρικυκλικήκορεσμένηή ακόρεστηετεροκυκλικήομάδαέχουσα 1 έως 4 άτομααζώτου, άτομαοξυγόνουή άτομαθείου, το R2 αντιπροσωπεύειάτομουδρογόνουή άτομοαλογόνου, τοΥ αντιπροσωπεύειμίαομάδα -Ο-, μίαομάδα -CO-, μίαομάδα -CH(OH)- ήκατώτερηαλκυλένοομάδακαιτοΑ αντιπροσωπεύει [Τύπος 2] όπουτο R3 αντιπροσωπεύειάτομουδρογόνου, κατώτερηαλκόξυομάδαή τιςπαρόμοιες, το p αντιπροσωπεύει 1 ή 2, το R4 αντιπροσωπεύειιμιδαζολύλκατώτερηαλκύλομάδαή τιςπαρόμοιες.

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