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：US07932272B2

公开(公告)日：2011-04-26

申请号：US10573890

申请日：2004-09-27

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: A61K31/4436 ,  C07D409/12

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：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。

公开(公告)号：US20100197911A1

公开(公告)日：2010-08-05

申请号：US12244227

申请日：2008-10-02

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: C07D487/04 ,  C07F7/08

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：US20070105943A1

公开(公告)日：2007-05-10

申请号：US10573890

申请日：2004-09-27

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: A01N43/02

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: 本发明提供一种由下式表示的抗真菌剂：其中A 1表示可具有取代基的3-吡啶基，可具有取代基的喹啉基等; X 1表示由式-NH-C（-O） - 表示的基团，由式-C（ - ） - 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A 1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：US20060160832A1

公开(公告)日：2006-07-20

申请号：US11347749

申请日：2006-02-03

Applicant: Yosuhiro 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： Yosuhiro 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: A61K31/517 ,  A61K31/47 ,  C07D239/72 ,  C07D215/02

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.

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