公开(公告)号：US06645996B1

公开(公告)日：2003-11-11

申请号：US09700680

申请日：2000-11-17

申请人： Toshiaki Wakabayashi ,  Rena Kawase ,  Nobuaki Naruse ,  Masanori Fujita ,  Tomohiro Sameshima ,  Yoshio Watanabe ,  Kazuyuki Dobashi ,  Yasuhiro Funahashi ,  Taro Semba

发明人： Toshiaki Wakabayashi ,  Rena Kawase ,  Nobuaki Naruse ,  Masanori Fujita ,  Tomohiro Sameshima ,  Yoshio Watanabe ,  Kazuyuki Dobashi ,  Yasuhiro Funahashi ,  Taro Semba

IPC分类号： A61K3135

CPC分类号： C07D493/10 ,  C12P17/162

摘要： The present invention provides a novel bioactive substance having an antiangiogenic effect. The chemical compound represented by the formula (1) (wherein, R1 represents hydrogen atom, aldehyde group or a lower acyl group, R2 and R3 are the same as or different from each other and represent hydrogen atom or a lower alkoxy group or are combined to represent oxygen atom, R4 represents a lower alkyl group and R5 represents hydrogen atom or a lower alkyl group, provided that compounds in which R1 is aldehyde group, R2 and R3are different from each other and are hydrogen atom or methoxy group, R4 is ethyl group and R5 is hydrogen atom are excluded), a salt thereof or a hydrate thereof was isolated from the culture broth of genus Streptomyces and the structure thereof was analyzed.

摘要翻译： 本发明提供了具有抗血管生成作用的新型生物活性物质。式（1）表示的化合物（其中，R 1表示氢原子，醛基或低级酰基，R 2和R 3 >彼此相同或不同，表示氢原子或低级烷氧基，或者组合表示氧原子，R 4表示低级烷基，R 5表示氢原子或低级烷基， 条件是其中R 1为醛基，R 2和R 3的化合物彼此不同，为氢原子或甲氧基，R 4为乙基，R 5为氢原子 被除去），其盐或其水合物从链霉菌属的培养肉汤中分离，并分析其结构。

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。

公开(公告)号：US06673787B2

公开(公告)日：2004-01-06

申请号：US10098420

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： A61K3133

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：US07834049B2

公开(公告)日：2010-11-16

申请号：US11097218

申请日：2005-04-04

申请人： 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

发明人： 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分类号： A61K31/405

CPC分类号： 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

摘要： 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.

摘要翻译： 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 - （CR4bR5b）mb-（其中R4b和R5b彼此相同或不同，各自表示氢原子或C1-C4烷基; mb表示整数 1或2）; R1表示氢原子或C1-C6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：US20100267754A1

公开(公告)日：2010-10-21

申请号：US12797806

申请日：2010-06-10

申请人： 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

发明人： 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分类号： A61K31/505 ,  A61K31/24 ,  A61K31/405 ,  A61K31/44 ,  A61K31/50 ,  A61P19/10 ,  A61P7/02

CPC分类号： 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

摘要： 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.

摘要翻译： 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 - （CR4bR5b）mb-（其中R4b和R5b彼此相同或不同，各自表示氢原子或C1-C4烷基; mb表示整数 1或2）; R1表示氢原子或C1-C6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：US20050176712A1

公开(公告)日：2005-08-11

申请号：US11097218

申请日：2005-04-04

申请人： 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

发明人： 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分类号： 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分类号： 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

摘要： 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.

摘要翻译： 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

申请人： 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

发明人： 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分类号： A61K3133

CPC分类号： 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

摘要： 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.

摘要翻译： 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

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： A61K31404

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。

公开(公告)号：US20050119303A1

公开(公告)日：2005-06-02

申请号：US10504676

申请日：2003-03-04

申请人： Toshiaki Wakabayashi ,  Naoto Ono ,  Taro Semba ,  Toru Haneda

发明人： Toshiaki Wakabayashi ,  Naoto Ono ,  Taro Semba ,  Toru Haneda

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

CPC分类号： A61K45/06 ,  A61K31/403 ,  A61K31/404 ,  A61K31/427 ,  A61K31/47 ,  A61K31/502 ,  A61K31/517 ,  A61K2300/00

摘要： 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.

摘要翻译： 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：US20090047278A1

公开(公告)日：2009-02-19

申请号：US11885081

申请日：2006-02-28

申请人： Takashi Owa ,  Yoichi Ozawa ,  Taro Semba ,  Toshiaki Wakabayashi

发明人： Takashi Owa ,  Yoichi Ozawa ,  Taro Semba ,  Toshiaki Wakabayashi

IPC分类号： A61K39/395 ,  A61K31/404 ,  A61K31/18 ,  A61K31/343 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/517

CPC分类号： A61K31/64 ,  A61K31/18 ,  A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/498 ,  A61K31/517 ,  A61K39/39541 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to a pharmaceutical composition, a kit and a method for treating cancer, comprising a sulfonamide compound in combination with a substance having an EGF inhibitory activity.

摘要翻译： 本发明涉及药物组合物，试剂盒和治疗癌症的方法，其包含与具有EGF抑制活性的物质组合的磺酰胺化合物。