公开(公告)号：US20140187577A1

公开(公告)日：2014-07-03

申请号：US14122339

申请日：2012-05-31

Applicant: Yasuhiro Funahashi ,  Tadashi Kadowaki ,  Junji Matsui ,  Jason S. Simon ,  Lucy Xu

Inventor： Yasuhiro Funahashi ,  Tadashi Kadowaki ,  Junji Matsui ,  Jason S. Simon ,  Lucy Xu

IPC: G01N33/574 ,  A61K31/47 ,  C12Q1/68

CPC classification number: G01N33/57407 ,  A61K31/47 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156 ,  G01N33/57438

Abstract: Biomarkers are provided that are predictive of a subject's responsiveness to a therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate). The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having cancer (e.g., thyroid cancer, kidney cancer), suspected of having cancer, or at risk of developing cancer.

Abstract translation: 提供了可预测受试者对包含联苯卡因或其药学上可接受的盐（例如甲磺酸伦伐他汀）的疗法的反应性的生物标志物。 本文描述的生物标志物，组合物和方法可用于为具有癌症（例如甲状腺癌，肾癌），疑似患有癌症或具有发展癌症风险的受试者选择适当的治疗方式。

公开(公告)号：US07662919B2

公开(公告)日：2010-02-16

申请号：US11114962

申请日：2005-04-26

Applicant: Jan Kitajewski ,  Carrie Shawber ,  Yasuhiro Funahashi

Inventor： Jan Kitajewski ,  Carrie Shawber ,  Yasuhiro Funahashi

IPC: C07K14/00 ,  C07K17/00 ,  A61K38/00 ,  A61K39/00

CPC classification number: A61K48/00 ,  A61K9/0019 ,  A61K38/00 ,  C07K14/705 ,  C07K2319/30 ,  C07K2319/32

Abstract: This invention provides a method for treating a subject having a tumor and a method for inhibiting angiogenesis in a subject, both comprising administering to the subject an effective amount of a composition of matter comprising the extracellular domain of a Notch receptor protein operably affixed to a half-life-increasing moiety. This invention also provides a composition of matter comprising the extracellular domain of Notch4 receptor protein operably affixed to a half-life-increasing moiety. This invention further provides an article of manufacture. Finally, this invention provides a replicable vector which encodes a polypeptide comprising the extracellular domain of a Notch receptor protein operably affixed to a half-life-increasing moiety, a host vector system which comprises such replicable vector and a method of producing such polypeptide.

Abstract translation: 本发明提供了治疗患有肿瘤的受试者的方法和用于抑制受试者血管生成的方法，所述方法包括向受试者施用有效量的包含Notch受体蛋白的细胞外结构域的物质组合物， 生命增加部分。 本发明还提供了包含Notch4受体蛋白的细胞外结构域的物质组合物，其可操作地附着于半衰期增加的部分。 本发明还提供了一种制造品。 最后，本发明提供了可复制载体，其编码包含可操作地附着于半衰期增加部分的Notch受体蛋白的细胞外结构域的多肽，包含该可复制载体的宿主载体系统和产生该多肽的方法。

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：US20060030694A1

公开(公告)日：2006-02-09

申请号：US11114962

申请日：2005-04-26

Applicant: Jan Kitajewski ,  Carrie Shawber ,  Yasuhiro Funahashi

Inventor： Jan Kitajewski ,  Carrie Shawber ,  Yasuhiro Funahashi

IPC: C07K14/705 ,  C07K16/46 ,  A61K38/17

CPC classification number: A61K48/00 ,  A61K9/0019 ,  A61K38/00 ,  C07K14/705 ,  C07K2319/30 ,  C07K2319/32

Abstract: This invention provides a method for treating a subject having a tumor and a method for inhibiting angiogenesis in a subject, both comprising administering to the subject an effective amount of a composition of matter comprising the extracellular domain of a Notch receptor protein operably affixed to a half-life-increasing moiety. This invention also provides a composition of matter comprising the extracellular domain of Notch4 receptor protein operably affixed to a half-life-increasing moiety. This invention further provides an article of manufacture. Finally, this invention provides a replicable vector which encodes a polypeptide comprising the extracellular domain of a Notch receptor protein operably affixed to a half-life-increasing moiety, a host vector system which comprises such replicable vector and a method of producing such polypeptide.

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：US5612681A

公开(公告)日：1997-03-18

申请号：US277744

申请日：1994-07-20

Applicant: Yasuhiro Funahashi ,  Kazunori Ikami ,  Osamu Nishimura ,  Yuji Kiyohara ,  Yoshihiko Hibino ,  Yuichi Yasutomo

Inventor： Yasuhiro Funahashi ,  Kazunori Ikami ,  Osamu Nishimura ,  Yuji Kiyohara ,  Yoshihiko Hibino ,  Yuichi Yasutomo

IPC: H04N7/14 ,  H04J3/06 ,  H04L12/40 ,  H04N21/437 ,  H04N21/647 ,  H04L7/00

CPC classification number: H04L7/0008 ,  H04N7/17318

Abstract: The clock demodulator 25 continually demodulates the clock signal of the control CPU 7 transmitted from the clock modulator 10 of the center S. The terminal control CPU 23 performs processes such as transmission and reception of data with the demodulated clock signal as a reference clock. The time required to synchronize the clocks of the CPUs 7 and 23 is eliminated. Transmission and reception of data is executed quickly as soon as right of transmission is transferred to a terminal.

Abstract translation: 时钟解调器25连续地解调从中心S的时钟调制器10发送的控制CPU7的时钟信号。终端控制CPU 23以解调的时钟信号作为参考时钟执行诸如发送和接收数据的处理。 消除了CPU7和23的时钟同步所需的时间。 一旦传输权转移到终端，数据的传输和接收就会快速执行。

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。

公开(公告)号：US20110118470A1

公开(公告)日：2011-05-19

申请号：US12986638

申请日：2011-01-07

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: C07D213/74 ,  C07D401/04 ,  C07D401/14 ,  C07D417/12

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，任意取代的C 1-6烷基等， Zg表示C1-8烷基，C3-8脂环族烃基，C6-14芳基等），其盐或上述的水合物。

公开(公告)号：US07834049B2

公开(公告)日：2010-11-16

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: A61K31/405

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 - （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

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: A61K31/505 ,  A61K31/24 ,  A61K31/405 ,  A61K31/44 ,  A61K31/50 ,  A61P19/10 ,  A61P7/02

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 - （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。