公开(公告)号：US20050119303A1

公开(公告)日：2005-06-02

申请号：US10504676

申请日：2003-03-04

Applicant: Toshiaki Wakabayashi ,  Naoto Ono ,  Taro Semba ,  Toru Haneda

Inventor： Toshiaki Wakabayashi ,  Naoto Ono ,  Taro Semba ,  Toru Haneda

IPC: A61K31/403 ,  A61K31/404 ,  A61K31/427 ,  A61K31/47 ,  A61K31/502 ,  A61K31/517 ,  A61K45/06 ,  A61P35/00 ,  A61P43/00 ,  A61K31/405

CPC classification number: A61K45/06 ,  A61K31/403 ,  A61K31/404 ,  A61K31/427 ,  A61K31/47 ,  A61K31/502 ,  A61K31/517 ,  A61K2300/00

Abstract: The present invention provides a composition and a kit for treating tumors, which permits a sulfonamide-containing heterocyclic compound to exhibit its angiogenesis inhibitory activity and antitumor activity more effectively. According to the present invention, the sulfonamide-containing heterocyclic compound can be used in treating cancers more effectively by combination with a VEGF inhibitor/FGF inhibitor.

Abstract translation: 本发明提供用于治疗肿瘤的组合物和试剂盒，其允许含磺酰胺的杂环化合物更有效地表现出其血管生成抑制活性和抗肿瘤活性。 根据本发明，通过与VEGF抑制剂/ FGF抑制剂组合，可以更有效地使用含磺酰胺的杂环化合物来治疗癌症。

公开(公告)号：US5846969A

公开(公告)日：1998-12-08

申请号：US873033

申请日：1997-06-11

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 ,  A61K31/55 ,  A61K31/505 ,  C07D487/00 ,  C07D471/00

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: 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 O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; 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).

Abstract translation: （I）表示的磺酰胺衍生物或磺酸酯衍生物：（I）{G表示芳香族5-或6-元环; L表示O或-N（R 1） - （R 1表示氢或低级烷基）; （D）环A和B各自表示不饱和的5-或6-元环; 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）。

公开(公告)号：US20090062348A1

公开(公告)日：2009-03-05

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: C07D401/12 ,  C07D409/12 ,  C07D407/12 ,  A61K31/4436 ,  A61K31/443 ,  A61K31/4439 ,  A61P31/10

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：US07253286B2

公开(公告)日：2007-08-07

申请号：US10420466

申请日：2003-04-18

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: A61K31/47 ,  C07D215/16

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A为任选取代的5至14元杂环基等; X-O是-O - ， - S-等; Y是任选取代的C 6-14芳基，任选取代的5至14元杂环基等; 并且T 1是由以下通式表示的基团：其中E是单键或-N（R 2）2 - R 1，G 1和R 2各自独立地表示氢原子，任选取代的C 1-6烷基等，Z

公开(公告)号：US06673787B2

公开(公告)日：2004-01-06

申请号：US10098420

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: A61K3133

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其水合物。在式中，R 1表示氢原子，卤素原子或氰基; R 2和R 3各自表示氢原子，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：US07612092B2

公开(公告)日：2009-11-03

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

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

IPC: A61K31/47

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。

公开(公告)号：US20090269352A1

公开(公告)日：2009-10-29

申请号：US12498303

申请日：2009-07-06

Applicant: Toshiaki WAKABAYASHI ,  Naoto Ono ,  Taro Semba ,  Toru Haneda

Inventor： Toshiaki WAKABAYASHI ,  Naoto Ono ,  Taro Semba ,  Toru Haneda

IPC: A61K39/395 ,  A61K31/404 ,  A61K31/47 ,  A61P35/00

CPC classification number: A61K45/06 ,  A61K31/403 ,  A61K31/404 ,  A61K31/427 ,  A61K31/47 ,  A61K31/502 ,  A61K31/517 ,  A61K2300/00

Abstract: The present invention provides a composition and a kit for treating tumors, which permits a sulfonamide-containing heterocyclic compound to exhibit its angiogenesis inhibitory activity and antitumor activity more effectively. According to the present invention, the sulfonamide-containing heterocyclic compound can be used in treating cancers more effectively by combination with a VEGF inhibitor/FGF inhibitor.

Abstract translation: 本发明提供用于治疗肿瘤的组合物和试剂盒，其允许含磺酰胺的杂环化合物更有效地表现出其血管生成抑制活性和抗肿瘤活性。 根据本发明，通过与VEGF抑制剂/ FGF抑制剂组合，可以更有效地使用含磺酰胺的杂环化合物来治疗癌症。

公开(公告)号：US20050176712A1

公开(公告)日：2005-08-11

申请号：US11097218

申请日：2005-04-04

Applicant: Toshiaki Wakabayashi ,  Yasuhiro Funahashi ,  Naoko Hata ,  Taro Semba ,  Yuji Yamamoto ,  Toru Haneda ,  Takashi Owa ,  Akihiko Tsuruoka ,  Junichi Kamata ,  Tadashi Okabe ,  Keiko Takahashi ,  Kazumasa Nara ,  Shinichi Hamaoka ,  Norihiro Ueda

Inventor： Toshiaki Wakabayashi ,  Yasuhiro Funahashi ,  Naoko Hata ,  Taro Semba ,  Yuji Yamamoto ,  Toru Haneda ,  Takashi Owa ,  Akihiko Tsuruoka ,  Junichi Kamata ,  Tadashi Okabe ,  Keiko Takahashi ,  Kazumasa Nara ,  Shinichi Hamaoka ,  Norihiro Ueda

IPC: A61K45/06 ,  A61K31/00 ,  A61K31/145 ,  A61K31/18 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/506 ,  A61P7/02 ,  A61P9/10 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P35/00 ,  A61P35/04 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D215/38 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D311/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D411/12 ,  C07D417/12 ,  C07D471/04 ,  A61K31/53 ,  A61K31/47 ,  A61K31/517 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/00 ,  A61K31/18 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/4439 ,  A61K31/506 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D215/38 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D311/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D411/12 ,  C07D417/12

Abstract: The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, wherein in the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, —CH═CH— or —(CR4bR5b)mb— (wherein R4b and R5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mb means an integer of 1 or 2); R1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or —CO—NH—; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

Abstract translation: 本发明提供一种整联蛋白表达抑制剂，以及基于整联蛋白抑制作用的治疗动脉硬化，银屑病，癌症，视网膜血管生成，糖尿病性视网膜病变或炎性疾病，抗凝血剂或癌转移抑制剂的药剂。 即，提供一种整联蛋白表达抑制剂，其包含作为活性成分的下式（I）表示的磺酰胺化合物，其药理学上可接受的盐或其水合物，其中，式中，B表示C6〜C10芳基 环或6至10元杂芳基环，其可以具有取代基，并且其中一部分环可以饱和; K表示单键，-CH-CH-或 - （CR 4b）R b） （其中R 4b和R 5b彼此相同或不同，并且各自表示氢原子或C 1 -C 4烷基;且m b， / SUP>表示1或2的整数）; R 1表示氢原子或C 1 -C 6烷基; Z表示单键或-CO-NH-; 并且R表示可以分别具有取代基并且其中一部分环可以饱和的C 6 -C 10芳基环或6至10元杂芳基环。

公开(公告)号：US06787534B2

公开(公告)日：2004-09-07

申请号：US10149253

申请日：2002-06-10

Applicant: Toru Haneda ,  Akihiko Tsuruoka ,  Junichi Kamata ,  Tadashi Okabe ,  Keiko Takahashi ,  Kazumasa Nara ,  Shinichi Hamaoka ,  Norihiro Ueda ,  Toshiaki Wakabayashi ,  Yasuhiro Funahashi ,  Taro Semba ,  Naoko Hata ,  Yuji Yamamoto ,  Yoichi Ozawa ,  Naoko Tsukahara ,  Takashi Owa

Inventor： Toru Haneda ,  Akihiko Tsuruoka ,  Junichi Kamata ,  Tadashi Okabe ,  Keiko Takahashi ,  Kazumasa Nara ,  Shinichi Hamaoka ,  Norihiro Ueda ,  Toshiaki Wakabayashi ,  Yasuhiro Funahashi ,  Taro Semba ,  Naoko Hata ,  Yuji Yamamoto ,  Yoichi Ozawa ,  Naoko Tsukahara ,  Takashi Owa

IPC: A61K3133

CPC classification number: C07D215/38 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D311/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. In the formula, A is hydrogen atom, a halogen atom, a C1-C4 alkyl or alkoxy group which may be substituted with a halogen atom, or cyano group; B is an optionally substituted aryl group or monocyclic heteroaryl group, or: (wherein, the ring Q is an aromatic ring which may have nitrogen atom; and the ring M is a ring sharing a double bond with the ring Q, which ring may have a heteroatom; and the rings Q and M may share nitrogen atom); K is a single bond; T, W, X and Y are the same as or different from each other and each is ═C(D)— (wherein, D is hydrogen or a halogen atom) or nitrogen atom; U and V are the same as or different from each other and each is ═C(D)—, nitrogen atom, —CH2—, oxygen atom or —CO—; Z is a single bond or —CO—NH—; and R1 is hydrogen atom, etc.

Abstract translation: 本发明提供了含磺酰胺或磺酰脲的杂环化合物。 具体地说，它提供由式（I）表示的杂环化合物，其药理学上可接受的盐或它们的水合物。在该式中，A是氢原子，卤素原子，可以是C 1 -C 4烷基或烷氧基的 被卤素原子或氰基取代; B是任选取代的芳基或单环杂芳基，或者：（其中，环Q是可以具有氮原子的芳环;环M是与环Q共享双键的环，该环可以具有 杂原子;并且环Q和M可以共享氮原子）; K是单键; T，W，X和Y彼此相同或不同，并且各自为= C（D） - （其中，D为氢或卤素原子）或氮原子; U和V彼此相同或不同，并且各自为= C（D） - ，氮原子，-CH 2 - ，氧原子或-CO-; Z是单键或-CO-NH-; R1为氢原子等

公开(公告)号：US06469043B1

公开(公告)日：2002-10-22

申请号：US09647215

申请日：2000-09-28

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: A61K31404

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其水合物。在该式中，R1表示氢原子，卤素原子或氰基; R2和R3相同或不同，各自表示氢原子，C1〜C4低级烷基或卤原子; R4表示氢原子或C1〜C4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，条件是所有的R 1，R 2和R 3均为氢原子，其中R 2和R 3均为氢原子或 环A为氨基磺酰基，R1和R2均为卤素原子。 此外，当环A为氰基苯基，2-氨基-5-吡啶基或2-卤代-5-吡啶基并且R 1为氰基或卤素原子时，R 2和R 3中的至少一个不应为氢 原子。