公开(公告)号：US5688800A

公开(公告)日：1997-11-18

申请号：US413100

申请日：1995-03-29

Applicant: Hiroaki Nomura ,  Toru Haneda ,  Yoshihiko Kotake ,  Norihiro Ueda ,  Kyosuke Kitoh

Inventor： Hiroaki Nomura ,  Toru Haneda ,  Yoshihiko Kotake ,  Norihiro Ueda ,  Kyosuke Kitoh

IPC: C07D239/70 ,  C07D487/04 ,  A61K31/505

CPC classification number: C07D487/04 ,  C07D239/70

Abstract: A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a hydroxyl or amino group; R.sup.2 represents a phenylene, pyridinediyl, thiendiyl furandiyl or thlazoldiyl group --CO.sub.2 R.sup.5 and --CO.sub.2 R.sup.6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part ##STR2## A represents an oxygen atom, a group represented by the formula: ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R.sup.3 and R.sup.4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: ##STR4## (wherein R.sup.70 represents a hydrogen atom or a hydrocarbon group), and n is an integer of 1 to 3, provided that the compound in which R.sup.1 represents oxygen, and hydrogen is attached to nitrogen at 3-position is included in the above shown definition, a process for preparation the same, and an antitumor drug containing the same.

Abstract translation: 一种具有优异抗肿瘤活性的新型嘧啶衍生物，其由下列通式（I）表示或其药理学上可接受的盐：其中R 1表示羟基或氨基; R2表示亚苯基，吡啶二基，噻二烷基呋喃基或噻唑烷基-CO 2 R 5和-CO 2 R 6可以彼此相同或不同，并且各自表示羧基或羧酸酯，部分 A表示氧 原子，由下式表示的基团：彼此不同且各自表示氢或卤素原子或可被取代的烃基，或者R3和R4可以一起形成可被取代的亚烷基）或 以下式表示的基团：其中R 70表示氢原子或烃基，n为1〜3的整数，条件是其中R1表示氧，氮与氮连接的化合物为3 位置包括在上述定义中，其制备方法和含有该定义的抗肿瘤药物。

公开(公告)号：US5554615A

公开(公告)日：1996-09-10

申请号：US300564

申请日：1994-09-06

Applicant: Hiroaki Nomura ,  Toru Haneda ,  Yoshihiko Kotake ,  Norihiro Ueda ,  Kyosuke Kitoh

Inventor： Hiroaki Nomura ,  Toru Haneda ,  Yoshihiko Kotake ,  Norihiro Ueda ,  Kyosuke Kitoh

IPC: C07D239/70 ,  C07D487/04 ,  A61K31/505

CPC classification number: C07D487/04 ,  C07D239/70

Abstract: A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a hydroxyl or amino group; R.sup.2 represents a phenylene, pyridinediyl, thiendiyl, furandiyl or thiazoldiyl group, --CO.sub.2 R.sup.5 and --CO.sub.2 R.sup.6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part ##STR2## A represents an oxygen atom, a group represented by the formula: ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R.sup.3 and R.sup.4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: ##STR4## (wherein R.sup.70 represents a hydrogen atom or a hydrocarbon group), and n is an integer of 1 to 3, provided that the compound in which R.sup.1 represents oxygen, and hydrogen is attached to nitrogen at 3-position is included in the above shown definition, a process for preparation the same, and an antitumor drug containing the same.

Abstract translation: 一种具有优异抗肿瘤活性的新型嘧啶衍生物，其由下列通式（I）表示或其药理学上可接受的盐：其中R 1表示羟基或氨基; R2代表亚苯基，吡啶二基，噻二基，呋喃二基或噻二唑基，-CO 2 R 5和-CO 2 R 6可以相同或不同，各自表示羧基或羧酸酯，部分 氧原子，由下式表示的基团：彼此不同，各自表示氢或卤素原子或可被取代的烃基，或者R3和R4可以相互结合形成可被取代的亚烷基） 或由下式表示的基团：其中R 70表示氢原子或烃基，n为1〜3的整数，条件是其中R1表示氧，氮与氮连接的化合物 在上述定义中包括3-位，其制备方法和含有该定义的抗肿瘤药物。

公开(公告)号：US20110195999A1

公开(公告)日：2011-08-11

申请号：US13047447

申请日：2011-03-14

Applicant: Kazutaka NAKAMOTO ,  Itaru Tsukada ,  Keigo Tanaka ,  Masayuki Matsukura ,  Toru Haneda ,  Satoshi Inoue ,  Norihiro Ueda ,  Shinya Abe ,  Katsura Hata ,  Naoaki Watanabe

Inventor： Kazutaka NAKAMOTO ,  Itaru Tsukada ,  Keigo Tanaka ,  Masayuki Matsukura ,  Toru Haneda ,  Satoshi Inoue ,  Norihiro Ueda ,  Shinya Abe ,  Katsura Hata ,  Naoaki Watanabe

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07829585B2

公开(公告)日：2010-11-09

申请号：US11887249

申请日：2006-03-29

Applicant: Kazutaka Nakamoto ,  Satoshi Inoue ,  Keigo Tanaka ,  Toru Haneda

Inventor： Kazutaka Nakamoto ,  Satoshi Inoue ,  Keigo Tanaka ,  Toru Haneda

IPC: A61K31/443 ,  C07D405/12

CPC classification number: C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12

Abstract: The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or —NH—, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.

Abstract translation: 本发明提供了具有优异的抗真菌作用的抗真菌剂，并且在物理性质，安全性和代谢稳定性方面也优异。 本发明公开了式（I）表示的化合物：其中X表示氧原子，硫原子或-NH-，R1表示氢原子，卤原子，氰基，氨基或取代基 ，R2和R3独立地表示氢原子，卤素原子，羟基或取代基，除了R2和R3都是氢原子的情况）和含有上述化合物的抗真菌剂。

公开(公告)号：US20090227799A1

公开(公告)日：2009-09-10

申请号：US11658901

申请日：2005-08-08

Applicant: Kazutaka Nakamoto ,  Masayuki Matsukura ,  Keigo Tanaka ,  Satoshi Inoue ,  Itaru Tsukada ,  Toru Haneda ,  Norihiro Ueda ,  Shinya Abe ,  Koji Sagane

Inventor： Kazutaka Nakamoto ,  Masayuki Matsukura ,  Keigo Tanaka ,  Satoshi Inoue ,  Itaru Tsukada ,  Toru Haneda ,  Norihiro Ueda ,  Shinya Abe ,  Koji Sagane

IPC: C07D409/12

CPC classification number: C07D405/12 ,  C07D409/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20060247259A1

公开(公告)日：2006-11-02

申请号：US11293785

申请日：2005-12-02

Applicant: Yasuhiro Funahashi ,  Akihiko Tsuruoka ,  Masayuki Matsukura ,  Toru Haneda ,  Yoshio Fukuda ,  Junichi Kamata ,  Keiko Takahashi ,  Tomohiro Matsushima ,  Kazuki Miyazaki ,  Ken-ichi Nomoto ,  Tatsuo Watanabe ,  Hiroshi Obaishi ,  Atsumi Yamaguchi ,  Sachi Suzuki ,  Katsuji Nakamura ,  Fusayo Mimura ,  Yuji Yamamoto ,  Junji Matsui ,  Kenji Matsui ,  Takako Yoshiba ,  Yasuyuki Suzuki ,  Itaru Arimoto

Inventor： Yasuhiro Funahashi ,  Akihiko Tsuruoka ,  Masayuki Matsukura ,  Toru Haneda ,  Yoshio Fukuda ,  Junichi Kamata ,  Keiko Takahashi ,  Tomohiro Matsushima ,  Kazuki Miyazaki ,  Ken-ichi Nomoto ,  Tatsuo Watanabe ,  Hiroshi Obaishi ,  Atsumi Yamaguchi ,  Sachi Suzuki ,  Katsuji Nakamura ,  Fusayo Mimura ,  Yuji Yamamoto ,  Junji Matsui ,  Kenji Matsui ,  Takako Yoshiba ,  Yasuyuki Suzuki ,  Itaru Arimoto

IPC: A61K31/519 ,  A61K31/517 ,  A61K31/4745 ,  A61K31/4706 ,  C07D487/02 ,  C07D471/02

CPC classification number: C07D213/73 ,  A61K31/4706 ,  A61K31/4745 ,  A61K31/517 ,  A61K31/519 ,  C07D207/34 ,  C07D213/26 ,  C07D213/68 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D215/18 ,  C07D215/233 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/88 ,  C07D249/04 ,  C07D261/14 ,  C07D277/48 ,  C07D307/68 ,  C07D319/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: Compounds represented by the following general formula: [wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—, Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.

公开(公告)号：US06638964B2

公开(公告)日：2003-10-28

申请号：US10098421

申请日：2002-03-18

Applicant: 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

Inventor： 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: A61K31405

CPC classification number: C07D401/12 ,  C07D209/04 ,  C07D209/30 ,  C07D209/42 ,  C07D403/12 ,  C07D409/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5854274A

公开(公告)日：1998-12-29

申请号：US760738

申请日：1996-12-05

Applicant: Hiroshi Yoshino ,  Norihiro Ueda ,  Jun Niijima ,  Toru Haneda ,  Yoshihiko Kotake ,  Kentaro Yoshimatsu ,  Tatsuo Watanabe ,  Takeshi Nagasu ,  Naoko Tsukahara ,  Nozomu Koyanagi ,  Kyosuke Kitoh

Inventor： Hiroshi Yoshino ,  Norihiro Ueda ,  Jun Niijima ,  Toru Haneda ,  Yoshihiko Kotake ,  Kentaro Yoshimatsu ,  Tatsuo Watanabe ,  Takeshi Nagasu ,  Naoko Tsukahara ,  Nozomu Koyanagi ,  Kyosuke Kitoh

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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

Applicant: Hiroshi Yoshino ,  Norihiro Ueda ,  Jun Niijima ,  Toru Haneda ,  Yoshihiko Kotake ,  Kentaro Yoshimatsu ,  Tatsuo Watanabe ,  Takeshi Nagasu ,  Naoko Tsukahara ,  Nozomu Koyanagi ,  Kyosuke Kitoh

Inventor： Hiroshi Yoshino ,  Norihiro Ueda ,  Jun Niijima ,  Toru Haneda ,  Yoshihiko Kotake ,  Kentaro Yoshimatsu ,  Tatsuo Watanabe ,  Takeshi Nagasu ,  Naoko Tsukahara ,  Nozomu Koyanagi ,  Kyosuke Kitoh

IPC: 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 classification number: 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

Abstract: 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.)!}

Abstract translation: 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：US07973160B2

公开(公告)日：2011-07-05

申请号：US12244227

申请日：2008-10-02

Applicant: Yasuhiro Funahashi ,  Toru Haneda ,  Junichi Kamata ,  Tatsuo Watanabe ,  Hiroshi Obaishi ,  Junji Matsui

Inventor： Yasuhiro Funahashi ,  Toru Haneda ,  Junichi Kamata ,  Tatsuo Watanabe ,  Hiroshi Obaishi ,  Junji Matsui

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/47 ,  C07D215/16 ,  A61P9/10 ,  A61P35/04

CPC classification number: C07D213/73 ,  A61K31/4706 ,  A61K31/4745 ,  A61K31/517 ,  A61K31/519 ,  C07D207/34 ,  C07D213/26 ,  C07D213/68 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D215/18 ,  C07D215/233 ,  C07D215/36 ,  C07D215/38 ,  C07D215/48 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/88 ,  C07D249/04 ,  C07D261/14 ,  C07D277/48 ,  C07D307/68 ,  C07D319/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

Abstract: Compounds represented by the following general formula: [wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—, Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.

Abstract translation: 由以下通式表示的化合物：其中Ag是任选取代的5至14元杂环基等; Xg为-O-，-S-等; Yg是任选取代的C 6-14芳基，任选取代的5至14元杂环基等; Tg1为下列通式表示的基团：（其中Eg为单键或-N（Rg2） - ，Rg1和Rg2各自独立地表示氢原子，可以具有取代基的C1-6烷基等，Zg 表示C 1-8烷基，C 3-8脂环族烃基，C 6-14芳基等）]，其盐或前述的水合物。