公开(公告)号：US07960412B2

公开(公告)日：2011-06-14

申请号：US12544965

申请日：2009-08-20

Applicant: Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

Inventor： Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

IPC: A61K31/445 ,  C07D211/06

CPC classification number: C07C217/22 ,  C07C215/78 ,  C07C217/18 ,  C07C217/78 ,  C07C217/84 ,  C07C219/34 ,  C07C323/25 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/09 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/44 ,  C07D211/14 ,  C07D211/26 ,  C07D211/46 ,  C07D211/58 ,  C07D213/38 ,  C07D213/64 ,  C07D213/73 ,  C07D223/16 ,  C07D243/08 ,  C07D277/66 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D307/14 ,  C07D309/04 ,  C07D309/14 ,  C07D311/58 ,  C07D317/66 ,  C07D333/20 ,  C07D333/58 ,  C07D405/12 ,  C07D451/06 ,  C07D453/02 ,  C07D487/08 ,  C07D491/10 ,  C07F5/025 ,  C07F7/1804 ,  C07F7/2208

Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like;   (I-1) formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Abstract translation: 本发明提供由下式（I）表示的化合物。 [其中T表示单键，可以具有取代基的C1-C4亚烷基等; （I-1）式（I-1）表示单键或双键; A表示单键，可以具有取代基的二价5〜14元杂环基等; Y表示单键等; Z表示亚甲基等; 环G表示可以用5-至6-元环缩合并可具有杂原子的亚苯基等; R a和R b彼此相同或不同，表示氢原子等; W表示单键等; R'表示1〜4个独立的氢原子等; R“表示1〜4个独立的氢原子等]或其盐或其水合物。

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。

公开(公告)号：US20060116364A1

公开(公告)日：2006-06-01

申请号：US11158245

申请日：2005-06-22

Applicant: Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

Inventor： Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

IPC: A61K31/55 ,  A61K31/4439 ,  A61K31/428 ,  A61K31/405 ,  A61K31/4025 ,  C07D417/02 ,  C07D43/02

CPC classification number: C07C217/22 ,  C07C215/78 ,  C07C217/18 ,  C07C217/78 ,  C07C217/84 ,  C07C219/34 ,  C07C323/25 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/09 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/44 ,  C07D211/14 ,  C07D211/26 ,  C07D211/46 ,  C07D211/58 ,  C07D213/38 ,  C07D213/64 ,  C07D213/73 ,  C07D223/16 ,  C07D243/08 ,  C07D277/66 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D307/14 ,  C07D309/04 ,  C07D309/14 ,  C07D311/58 ,  C07D317/66 ,  C07D333/20 ,  C07D333/58 ,  C07D405/12 ,  C07D451/06 ,  C07D453/02 ,  C07D487/08 ,  C07D491/10 ,  C07F5/025 ,  C07F7/1804 ,  C07F7/2208

Abstract: The present invention provides a compound represented by the following formula [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof

Abstract translation: 本发明提供由下式表示的化合物[其中T表示单键，可具有取代基的C 1 -C 4亚烷基等; 式（I-1）表示单键或双键; A表示单键，可以具有取代基的二价5〜14元杂环基等; Y表示单键等; Z表示亚甲基等; 环G表示可以用5-至6-元环缩合并可具有杂原子的亚苯基等; R a和R b彼此相同或不同，表示氢原子等; W代表单键等; R'表示1〜4个独立的氢原子等; R“表示1〜4个独立的氢原子等]或其盐或其水合物

公开(公告)号：US06579881B2

公开(公告)日：2003-06-17

申请号：US09859517

申请日：2001-05-18

Applicant: Noritaka Kitazawa ,  Kohshi Ueno ,  Keiko Takahashi ,  Teiji Kimura ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Makoto Komatsu ,  Manabu Matsunaga ,  Atsuhiko Kubota

Inventor： Noritaka Kitazawa ,  Kohshi Ueno ,  Keiko Takahashi ,  Teiji Kimura ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Makoto Komatsu ,  Manabu Matsunaga ,  Atsuhiko Kubota

IPC: A61K31435

CPC classification number: C07D231/12 ,  C07D211/26 ,  C07D211/74 ,  C07D217/04 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D491/04 ,  C07D513/04

Abstract: A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.

Abstract translation: 由下式表示的1,4-取代环状胺衍生物或其药理学上可接受的盐：其中A，B，C，D，T，Y和Z各自表示次甲基或氮键; R1，R2，R3，R4和R5各自表示取代基; n表示0或1〜3的整数， m表示0或1〜6的整数， p表示1〜3的整数。这些化合物具有5-羟色胺拮抗作用。 因此，它们在临床上可用作药物，特别是用于治疗，改善和预防痉挛性麻痹。 它们也可用作改善肌强直的中枢肌肉松弛剂。

公开(公告)号：US08476301B2

公开(公告)日：2013-07-02

申请号：US13609716

申请日：2012-09-11

Applicant: Ichiro Yoshida ,  Tadashi Okabe ,  Yasunobu Matsumoto ,  Nobuhisa Watanabe ,  Yoshiaki Ohashi ,  Yuji Onizawa ,  Hitoshi Harada

Inventor： Ichiro Yoshida ,  Tadashi Okabe ,  Yasunobu Matsumoto ,  Nobuhisa Watanabe ,  Yoshiaki Ohashi ,  Yuji Onizawa ,  Hitoshi Harada

IPC: A61K31/445 ,  C07D401/12

CPC classification number: A61K31/4025 ,  A61K31/454 ,  C07D401/12 ,  C07D403/12

Abstract: A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: wherein R represents a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, a C3-8 cycloalkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, or a C3-8 cycloalkenyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, X represents a C1-6 alkyl group, Y and Z are the same or different from each other and each represents a halogen atom or a C1-6 alkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group B, n represents 0 or 1, Substituent Group A consists of halogen atoms, and Substituent Group B consists of halogen atoms.

Abstract translation: 由式（1）表示的化合物或其药学上可接受的盐具有抑制作用：其中R表示未取代的或具有1至3个选自取代基组A的取代基的C 1-6烷基，C3- 8个未取代的或具有1〜3个选自取代基组A的取代基的环烷基，或未取代或具有1-3个选自取代基组A的取代基的C 3-8环烯基，X表示C 1-6烷基，Y和Z是 相同或不同，各自表示卤素原子或未取代或具有1〜3个选自取代基组B的取代基的C 1-6烷基，n表示0或1，取代基组A由卤素原子和取代基组B 由卤素原子组成。

公开(公告)号：US08399520B2

公开(公告)日：2013-03-19

申请号：US13048391

申请日：2011-03-15

Applicant: Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

Inventor： Shinichi Hamaoka ,  Noritaka Kitazawa ,  Kazumasa Nara ,  Atsushi Sasaki ,  Atsushi Kamada ,  Tadashi Okabe

IPC: A61K31/137 ,  C07C217/84

CPC classification number: C07C217/22 ,  C07C215/78 ,  C07C217/18 ,  C07C217/78 ,  C07C217/84 ,  C07C219/34 ,  C07C323/25 ,  C07C2602/10 ,  C07D205/04 ,  C07D207/09 ,  C07D209/08 ,  C07D209/14 ,  C07D209/30 ,  C07D209/44 ,  C07D211/14 ,  C07D211/26 ,  C07D211/46 ,  C07D211/58 ,  C07D213/38 ,  C07D213/64 ,  C07D213/73 ,  C07D223/16 ,  C07D243/08 ,  C07D277/66 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D307/14 ,  C07D309/04 ,  C07D309/14 ,  C07D311/58 ,  C07D317/66 ,  C07D333/20 ,  C07D333/58 ,  C07D405/12 ,  C07D451/06 ,  C07D453/02 ,  C07D487/08 ,  C07D491/10 ,  C07F5/025 ,  C07F7/1804 ,  C07F7/2208

Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R′ represents 1 to 4 independent hydrogen atoms and the like; and R″ represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Abstract translation: 本发明提供由下式（I）表示的化合物。 [其中T表示单键，可以具有取代基的C1-C4亚烷基等; 式（I-1）表示单键或双键; A表示单键，可以具有取代基的二价5〜14元杂环基等; Y表示单键等; Z表示亚甲基等; 环G表示可以用5-至6-元环缩合并可具有杂原子的亚苯基等; R a和R b彼此相同或不同，表示氢原子等; W表示单键等; R'表示1〜4个独立的氢原子等; R“表示1〜4个独立的氢原子等]或其盐或其水合物。

公开(公告)号：US07071201B2

公开(公告)日：2006-07-04

申请号：US09846259

申请日：2001-05-02

Applicant: Noritaka Kitazawa ,  Kohshi Ueno ,  Keiko Takahashi ,  Teiji Kimura ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Makoto Komatsu ,  Manabu Matsunaga ,  Atsuhiko Kubota

Inventor： Noritaka Kitazawa ,  Kohshi Ueno ,  Keiko Takahashi ,  Teiji Kimura ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Makoto Komatsu ,  Manabu Matsunaga ,  Atsuhiko Kubota

IPC: A61K31/435 ,  A61K31/55 ,  C07D211/68 ,  C07D401/00

CPC classification number: C07D231/12 ,  C07D211/26 ,  C07D211/74 ,  C07D217/04 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D491/04 ,  C07D513/04

Abstract: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

Abstract translation: 下式的新化合物：其中A，B，C，D，T，Y和Z代表每个次甲基或氮; R 1，R 2，R 3，R 4和R 5， 表示取代基; n表示0或1〜3的整数， m表示0或1〜6的整数， p表示1〜3的整数， 及其药理学上可接受的盐。 该化合物具有5-羟色胺拮抗作用，并且在临床上可用作药物，特别是用于治疗，改善和预防痉挛性麻痹或中枢肌肉松弛剂以改善肌强直。

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：US06790844B2

公开(公告)日：2004-09-14

申请号：US09852850

申请日：2001-05-11

Applicant: Kohshi Ueno ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Noritaka Kitazawa ,  Keiko Takahashi ,  Noboru Yamamoto ,  Yuichi Suzuki ,  Manabu Matsunaga ,  Atsuhiko Kubota

Inventor： Kohshi Ueno ,  Atsushi Sasaki ,  Koki Kawano ,  Tadashi Okabe ,  Noritaka Kitazawa ,  Keiko Takahashi ,  Noboru Yamamoto ,  Yuichi Suzuki ,  Manabu Matsunaga ,  Atsuhiko Kubota

IPC: A61K3133

CPC classification number: C07D401/04 ,  C07D217/22 ,  C07D217/24 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04

Abstract: Condensed pyridine compounds represented by formula (I): wherein: R1 and R3 are, independently, hydrogen, halogen, lower alkyl, or lower alkoxy; R2 represents an amino substituent; ring A is a benzene ring, pyridine ring, thiophene ring, or furan ring; and B represents a substituent containing a ring structure. Also, pharmaceutically acceptable salt and hydrates thereof. These compounds are clinically useful medicaments having; serotonin antagonism, and in particular, for treating, ameliorating, or preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.

Abstract translation: 由式（I）表示的缩合吡啶化合物：其中：R 1和R 3独立地是氢，卤素，低级烷基或低级烷氧基; R 2表示氨基取代基; 环A为苯环，吡啶环，噻吩环或呋喃环; B表示含有环结构的取代基。 此外，其药学上可接受的盐和水合物。 这些化合物是临床有用的药物，具有： 5-羟色胺拮抗作用，特别是用于治疗，改善或预防痉挛性麻痹。 它们也可用作改善肌强直的中枢肌肉松弛剂。