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公开(公告)号：US20110195999A1
公开(公告)日：2011-08-11
申请号：US13047447
申请日：2011-03-14
申请人： Kazutaka NAKAMOTO , Itaru Tsukada , Keigo Tanaka , Masayuki Matsukura , Toru Haneda , Satoshi Inoue , Norihiro Ueda , Shinya Abe , Katsura Hata , Naoaki Watanabe
发明人： Kazutaka NAKAMOTO , Itaru Tsukada , Keigo Tanaka , Masayuki Matsukura , Toru Haneda , Satoshi Inoue , Norihiro Ueda , Shinya Abe , Katsura Hata , Naoaki Watanabe
IPC分类号： A61K31/4375 , C07D405/12 , C07D213/46 , C07D213/78 , C07D401/12 , C07D417/12 , C07D409/12 , C07D471/04 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4427 , A61K31/44 , A61P31/10
CPC分类号： C07D213/82 , A61K31/404 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/435 , A61K31/4355 , A61K31/4365 , A61K31/44 , A61K31/443 , A61K31/455 , A61K31/47 , A61K31/472 , A61K31/4965 , A61K31/498 , A61K31/505 , A61K31/517 , C07D409/12
摘要： The present invention provides an antifungal agent represented by the formula: wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula —NH—C(═O)—, a group represented by the formula —C(═O)—NH—, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents.
摘要翻译： 本发明提供由下式表示的抗真菌剂：其中A1表示可具有取代基的3-吡啶基，可具有取代基的喹啉基等。 X1表示由式-NH-C（= O） - 表示的基团，由式-C（= O）-NH-表示的基团等; E表示呋喃基，噻吩基，吡咯基，苯基，吡啶基，四唑基，噻唑基或吡唑基; 条件是A1可以具有1至3个取代基，并且E具有一个或两个取代基。
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公开(公告)号：US20090227799A1
公开(公告)日：2009-09-10
申请号：US11658901
申请日：2005-08-08
申请人： Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Satoshi Inoue , Itaru Tsukada , Toru Haneda , Norihiro Ueda , Shinya Abe , Koji Sagane
发明人： Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Satoshi Inoue , Itaru Tsukada , Toru Haneda , Norihiro Ueda , Shinya Abe , Koji Sagane
IPC分类号： C07D409/12
CPC分类号： C07D405/12 , C07D409/12
摘要： Disclosed is an antimalarial agent containing a compound represented by the formula: [wherein A1 represents a 3-pyridyl group that may have a substituent, a 6-quinolyl group that may have a substituent, or the like; X1 represents a group represented by the formula —C(═O)—NH— or the like; E represents a furyl group, a thienyl group or a phenyl group; with the proviso that A1 may have one to three substituents, and E has one of two substituents] or a salt thereof or hydrates thereof.
摘要翻译： 公开了含有下式表示的化合物的抗疟剂：[式中，A1表示可具有取代基的3-吡啶基，可具有取代基的6-喹啉基等。 X1表示由式-C（ - ）-NH-等表示的基团; E表示呋喃基，噻吩基或苯基; 条件是A1可以具有一至三个取代基，并且E具有两个取代基之一]或其盐或其水合物。
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公开(公告)号：US20090098636A1
公开(公告)日：2009-04-16
申请号：US12103609
申请日：2008-04-15
申请人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
发明人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
IPC分类号： C12N1/19
CPC分类号： C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要： A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
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公开(公告)号：US20080166765A1
公开(公告)日：2008-07-10
申请号：US11958310
申请日：2007-12-17
申请人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Oba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
发明人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Oba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
CPC分类号： C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要： A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, fungal genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. These genes encode proteins participating in fungal cell wall synthesis. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
摘要翻译： 构建了将GPI锚定蛋白转运至细胞壁的运输过程的记录系统，发现了抑制该过程的化合物。 此外，鉴定了赋予对上述化合物的抗性的真菌基因，并开发了筛选抑制由这些基因编码的蛋白质的活性的化合物的方法。 这些基因编码参与真菌细胞壁合成的蛋白质。 因此，通过本发明，可以实现具有新机理的抗真菌剂，即抑制将GPI锚定蛋白转运到细胞壁的过程。
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公开(公告)号：US06638964B2
公开(公告)日：2003-10-28
申请号：US10098421
申请日：2002-03-18
申请人： Toru Haneda , Akihiko Tsuruoka , Junichi Kamata , Tadashi Okabe , Keiko Takahashi , Kazumasa Nara , Shinichi Hamaoka , Norihiro Ueda , Takashi Owa , Toshiaki Wakabayashi , Yasuhiro Funahashi , Taro Semba , Naoko Hata , Yuji Yamamoto , Yoichi Ozawa , Noako Tsukahara
发明人： Toru Haneda , Akihiko Tsuruoka , Junichi Kamata , Tadashi Okabe , Keiko Takahashi , Kazumasa Nara , Shinichi Hamaoka , Norihiro Ueda , Takashi Owa , Toshiaki Wakabayashi , Yasuhiro Funahashi , Taro Semba , Naoko Hata , Yuji Yamamoto , Yoichi Ozawa , Noako Tsukahara
IPC分类号： A61K31405
CPC分类号： C07D401/12 , C07D209/04 , C07D209/30 , C07D209/42 , C07D403/12 , C07D409/12
摘要： The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof: In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1˜C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1˜C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded. Further, when the ring A is cyanophenyl group, 2-amino-5-pyridyl group or a 2-halo-5-pyridyl group and R1 is cyano group or a halogen atom, at least one of R2 and R3 should not be a hydrogen atom.
摘要翻译： 本发明创造出一种新型抗血管生成剂，并提供与常规抗肿瘤剂相比显示出高安全性的抗肿瘤剂，具有确定的作用并且能够长时间施用。 也就是说，其提供由下式（I）表示的吲哚化合物，其药理学上可接受的盐或水合物：在式中，R 1表示氢原子，卤素原子或氰基; R 2和R 3各自代表氢原子，C 1 -C 4低级烷基或卤素原子; R 4表示氢原子或C 1 -C 4低级烷基; 并且环A表示氰基苯基，氨基磺酰基苯基，氨基吡啶基，氨基嘧啶基，卤代吡啶基或氰基噻吩基，条件是所有R 1，R 2和R 3均为氢原子的情况，其中 R 2和R 3都是氢原子，或者其中环A是氨基磺酰基并且R 1和R 2都是卤素原子。 此外，当环A为氰基苯基，2-氨基-5-吡啶基或2-卤代-5-吡啶基，R 1为氰基或卤素原子时，R 2和 R 3不应该是氢原子。
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公开(公告)号：US5854274A
公开(公告)日：1998-12-29
申请号：US760738
申请日：1996-12-05
申请人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
IPC分类号： C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D498/04 , C07D513/04 , C07F7/18 , A61K31/44 , A61K31/40 , C07D221/06 , C07D209/82
CPC分类号： C07D219/04 , C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D513/04 , C07F7/1856
摘要： Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes for producing the same are provided. The present sulfonamide derivatives or a sulfonic ester derivatives are represented by the following general formula (I): ##STR1## wherein G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- and --R.sup.1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from among the following; ##STR2## rings A and B each represent an unsaturated 5- or 5 -membered ring; X represents N(R.sup.2) wherein R.sup.2 represents hydrogen or lower alkyl, or NHCO; Y represents 0, S(O).sub.n, C(R.sup.3) (R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10) C(O), N.dbd.CR.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.16); and n represents 0, 1 or 2, R.sup.3 to R.sub.13, R.sup.15 and R.sup.16 each represent hydrogen or lower alkyl, and R.sup.14 represents hydrogen, lower alkyl or lower acyl.
摘要翻译： 提供具有优异抗肿瘤活性并由以下通式（I）表示的新型三环杂环磺酰胺衍生物和磺酸酯衍生物及其制备方法。 本发明的磺酰胺衍生物或磺酸酯衍生物由以下通式（I）表示：其中G表示芳族5-或6-元环; L表示0或-N（R1） - ，-R1表示氢或低级烷基; M表示选自以下的三环结构： （a）
（b） （c） （d） （e） （f）环A和B各自表示不饱和5-或5- 环; X表示N（R2），其中R2表示氢或低级烷基或NHCO; Y表示0，S（O）n，C（R3）（R4），C（O），N（R5），CH（R6）CH（R7），C（R8）= C（R9） ）C（O），N = CR 11），OCH（R 12），S（O）n CH（R 13）或N（R 14）CH（R 15）。 Z表示氮或C（R16）; 并且n表示0,1或2，R 3至R 13，R 15和R 16各自表示氢或低级烷基，R 14表示氢，低级烷基或低级酰基。 -
公开(公告)号：US5834462A
公开(公告)日：1998-11-10
申请号：US397254
申请日：1995-03-23
申请人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
发明人： Hiroshi Yoshino , Norihiro Ueda , Jun Niijima , Toru Haneda , Yoshihiko Kotake , Kentaro Yoshimatsu , Tatsuo Watanabe , Takeshi Nagasu , Naoko Tsukahara , Nozomu Koyanagi , Kyosuke Kitoh
IPC分类号： C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D498/04 , C07D513/04 , C07F7/18 , A61K31/40 , A61K31/47
CPC分类号： C07D219/04 , C07C211/55 , C07C229/58 , C07C311/29 , C07D209/88 , C07D219/06 , C07D219/08 , C07D221/12 , C07D223/22 , C07D243/38 , C07D265/38 , C07D267/18 , C07D267/20 , C07D279/20 , C07D281/14 , C07D413/12 , C07D513/04 , C07F7/1856
摘要： Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have each an antitumor action and are represented by the following general formula (I) and processes for producing the same are provided. These compounds have each an excellent antitumor activity. A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alky); and M represents a tricyclic structure selected from among the following ones; ##STR2## �rings A and B represent each an unsaturated 5- or 6-membered ring; X represents N(R.sup.2), (wherein R.sup.2 represents hydrogen or lower alkyl), or NHCO; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.16) (n represents 0, 1 or 2, R.sup.3 to R.sup.13, R.sup.15 and R.sup.16 each represents hydrogen or lower alkyl, and R.sup.14 represents hydrogen, lower alkyl or lowver acyl.)!}
摘要翻译： PCT No.PCT / JP94 / 01231 Sec。 371日期：1995年3月23日 102（e）1995年3月23日PCT PCT 1994年7月26日PCT公布。 出版物WO95 / 03279 日期1995年2月2日提供了具有各自抗肿瘤作用并由以下通式（I）表示的三环杂环磺酰胺衍生物和磺酸酯衍生物及其制备方法。 这些化合物各具有优异的抗肿瘤活性。 由以下通式（I）表示的磺酰胺衍生物或磺酸酯衍生物：元环; L表示0或-N（R1） - （R1表示氢或低级烷基）; M表示选自以下的三环结构： （a）
（b） [环A和B各自表示不饱和的5-或6-元环; X表示N（R2），（其中R2表示氢或低级烷基）或NHCO; Y表示O，S（O）n，C（R3）（R4），C（O），N（R5），CH（R6）CH（R7），C（R8）= C（R9） ）C（O），N = C（R 11），OCH（R 12），S（O）n CH（R 13）或N（R 14）CH（R 15） Z表示氮或C（R16）（n表示0,1或2，R3至R13，R15和R16各自表示氢或低级烷基，R14表示氢，低级烷基或低级酰基）]} -
公开(公告)号：US5075335A
公开(公告)日：1991-12-24
申请号：US495444
申请日：1990-03-16
申请人： Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
发明人： Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
IPC分类号： A61K31/235 , A61K31/245 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/42 , A61K31/421 , A61K31/445 , A61P1/00 , A61P7/02 , A61P7/04 , A61P43/00 , C07C67/00 , C07C313/00 , C07C319/20 , C07C323/20 , C07D207/40 , C07D207/404 , C07D207/408 , C07D209/48 , C07D209/76 , C07D211/76 , C07D211/88 , C07D263/44
CPC分类号： C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44
摘要： A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.
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公开(公告)号：US4801603A
公开(公告)日：1989-01-31
申请号：US946458
申请日：1986-12-24
申请人： Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
发明人： Shigeru Souda , Naoyuki Shimomura , Norihiro Ueda , Shuhei Miyazawa , Takashi Yamanaka , Kaname Miyamoto , Ieharu Hishinuma , Junichi Nagakawa , Naoko Nagaoka , Hidetoshi Kawashima , Tsutomu Kawata , Junsaku Nagaoka , Tsuneo Wakabayashi
IPC分类号： A61K31/235 , A61K31/245 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/42 , A61K31/421 , A61K31/445 , A61P1/00 , A61P7/02 , A61P7/04 , A61P43/00 , C07C67/00 , C07C313/00 , C07C319/20 , C07C323/20 , C07D207/40 , C07D207/404 , C07D207/408 , C07D209/48 , C07D209/76 , C07D211/76 , C07D211/88 , C07D263/44
CPC分类号： C07D207/404 , C07C323/20 , C07D209/48 , C07D263/44
摘要： A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.
摘要翻译： 具有下式的胍基苯甲酸酯衍生物是新颖有效的抑制酶如胰蛋白酶，纤溶酶和凝血酶，可用于治疗胰腺炎和出血性疾病和血栓形成。 其中X表示下式的基团：其中Y是下式的基团： - （CH 2）m - ，m是2或3的整数，
或基团 其中R是氢原子或低级烷基，n表示1〜5的整数。 -
公开(公告)号：US20060234283A1
公开(公告)日：2006-10-19
申请号：US11409453
申请日：2006-04-21
申请人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
发明人： Kappei Tsukahara , Katsura Hata , Koji Sagane , Kazutaka Nakamoto , Mamiko Tsuchiya , Naoaki Watanabe , Fuminori Ohba , Itaru Tsukada , Norihiro Ueda , Keigo Tanaka , Junko Kai
IPC分类号： C12Q1/68 , G01N33/569 , G01N33/53
CPC分类号： C07K14/40 , A61K31/00 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61K38/00 , C07D213/68 , C07D217/18 , C07D217/20 , C07K14/37 , C07K14/38 , C07K14/39 , C07K14/395 , C07K2319/02 , G01N2500/00 , Y10S435/911
摘要： A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.
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