公开(公告)号：US06861428B2

公开(公告)日：2005-03-01

申请号：US10396726

申请日：2003-03-26

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/14 ,  C07D237/24 ,  A61K31/51 ,  C07D237/04 ,  C07D403/06

CPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/14 ,  C07D237/24

摘要： Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represents a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represents a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to pharmaceutical compositions containing them. These compounds have inhibitory activity against IL-1β production, high water solubility and good oral absorbability.

摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子或烷基，羟基烷基，二羟基烷基或炔基，或R 2 >和R 3可以与相邻的氮原子一起形成取代或未取代的含氮饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子或 n，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。

公开(公告)号：US06869954B2

公开(公告)日：2005-03-22

申请号：US10253523

申请日：2002-09-25

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  A61P1/04 ,  A61P9/00 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P37/02 ,  A61P43/00 ,  C07D237/24 ,  A61K31/51 ,  C07D237/04 ,  C07D403/06

CPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  C07D237/24

摘要： Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1β production, high water solubility and good oral absorbability.

摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子或烷基，羟烷基，二羟基烷基或炔基，或R 2 >和R 3可以与相邻的氮原子一起形成取代或未取代的含氮饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子或 n，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。

公开(公告)号：US07211577B2

公开(公告)日：2007-05-01

申请号：US10544881

申请日：2004-03-16

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： C07D237/04 ,  C07D403/06 ,  A61K31/50 ,  A61K31/51

CPC分类号： A61K31/501 ,  A61K31/50 ,  C07D237/14

摘要： A phenylpyridazine derivative represented by the formula (1): Wherein, R1, R2, R3, X, Y, Z and n have the same meaning as defined in the specification; or a salt thereof, or a medicine containing the compound. The present invention provides water-soluble phenylpyridazine derivatives and medicines containing them, which have excellent inhibitory activity against interleukin-β production, high water solubility and high oral absorbability.

摘要翻译： 由式（1）表示的苯基哒嗪衍生物：其中R1，R2，R3，X，Y，Z和n与说明书中定义相同; 或其盐，或含有该化合物的药物。 本发明提供水溶性苯基哒嗪衍生物和含有它们的药物，其对白细胞介素-β产生具有优异的抑制活性，高水溶性和高口服吸收性。

公开(公告)号：US07087606B2

公开(公告)日：2006-08-08

申请号：US10960993

申请日：2004-10-12

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： A01N43/58 ,  A61K31/50

CPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  C07D237/24

摘要： Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1β production, high water solubility and good oral absorbability.

摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子 或烷基，羟基烷基，二羟基烷基或炔基或R 2和R 3可以与相邻的氮原子一起形成取代或未取代的含氮的 饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子等，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。

公开(公告)号：US20060142292A1

公开(公告)日：2006-06-29

申请号：US10544881

申请日：2004-03-16

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： A61K31/501 ,  C07D403/02 ,  A61K31/50

CPC分类号： A61K31/501 ,  A61K31/50 ,  C07D237/14

摘要： A phenylpyridazine derivative represented by the formula (1): Wherein, R1, R2, R3, X, Y, Z and n have the same meaning as defined in the specification; or a salt thereof, or a medicine containing the compound. The present invention provides water-soluble phenylpyridazine derivatives and medicines containing them, which have excellent inhibitory activity against interleukin-β production, high water solubility and high oral absorbability.

摘要翻译： 由式（1）表示的苯基哒嗪衍生物：其中R1，R2，R3，X，Y，Z和n与说明书中定义相同; 或其盐，或含有该化合物的药物。 本发明提供水溶性苯基哒嗪衍生物和含有它们的药物，其对白细胞介素-β产生具有优异的抑制活性，高水溶性和高口服吸收性。

公开(公告)号：US07314877B2

公开(公告)日：2008-01-01

申请号：US10547779

申请日：2004-03-03

申请人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Natsuyo Kumai ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

发明人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Natsuyo Kumai ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

IPC分类号： C07D405/04 ,  A61K31/501

CPC分类号： C07D405/04

摘要： The present invention is directed to a compound represented by formula (1): (wherein R1 represents an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and each of R2 and R3 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a dihydroxyalkyl group, or an alkynyl group, or R2 and R3 form, together with the nitrogen atom adjacent thereto, a nitrogen-containing saturated heterocyclic group which may have a substituent) and a drug composition containing the compound. The compound exhibits tumor necrosis factor (TNF-α) production inhibitory effect and improved absorption upon oral administration.

摘要翻译： 本发明涉及由式（1）表示的化合物：其中R 1表示可以具有取代基的烷基或可具有取代基的烯基; R 1， SO 2和R 3表示氢原子，烷基，羟基烷基，二羟基烷基或炔基，或R 2和 R 3形式与与其相邻的氮原子，可以具有取代基的含氮饱和杂环基）和含有该化合物的药物组合物。 该化合物表现出肿瘤坏死因子（TNF-α）产生抑制作用和口服给药改善吸收。

公开(公告)号：US20060189621A1

公开(公告)日：2006-08-24

申请号：US10547779

申请日：2004-03-03

申请人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

发明人： Seiichi Sato ,  Tomoyuki Koshi ,  Toshimi Mizoguchi ,  Kyoko Yasuoka ,  Junko Totsuka ,  Masahiro Tamura ,  Masao Ohkuchi

IPC分类号： A61K31/501 ,  C07D405/02

CPC分类号： C07D405/04

摘要： The present invention is directed to a compound represented by formula (1): (wherein R1 represents an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and each of R2 and R3 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a dihydroxyalkyl group, or an alkynyl group, or R2 and R3 form, together with the nitrogen atom adjacent thereto, a nitrogen-containing saturated heterocyclic group which may have a substituent) and a drug composition containing the compound. The compound exhibits tumor necrosis factor (TNF-α) production inhibitory effect and improved absorption upon oral administration.

摘要翻译： 本发明涉及由式（1）表示的化合物：其中R 1表示可以具有取代基的烷基或可具有取代基的烯基; R 1， SO 2和R 3表示氢原子，烷基，羟基烷基，二羟基烷基或炔基，或R 2和 R 3形式与与其相邻的氮原子，可以具有取代基的含氮饱和杂环基）和含有该化合物的药物组合物。 该化合物表现出肿瘤坏死因子（TNF-α）产生抑制作用和口服给药改善吸收。

公开(公告)号：US20050085480A1

公开(公告)日：2005-04-21

申请号：US10960993

申请日：2004-10-12

申请人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

发明人： Yoshinori Kyotani ,  Tomoyuki Koshi ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Takahiro Kitamura ,  Shunji Takemura ,  Kyoko Yasuoka ,  Junko Totsuka ,  Seiichi Sato

IPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  A61P1/04 ,  A61P9/00 ,  A61P19/02 ,  A61P19/10 ,  A61P29/00 ,  A61P31/04 ,  A61P37/02 ,  A61P43/00 ,  C07D237/24 ,  C07D43/02

CPC分类号： C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  C07D237/24

摘要： Compounds having the formula (1): wherein R1 represents an alkyl or alkenyl group, R2 and R3 each independently represent a hydrogen atom or an alkyl, hydroxyalkyl, dihydroxyalkyl or alkynyl group, or R2 and R3 may be fused together with the adjacent nitrogen atom to form a substituted or unsubstituted, nitrogen-containing, saturated heterocyclic group, X, Y and Z each independently represent a hydrogen atom, an alkyl group, a halogen atom or the like, and n stands for an integer of from 1 to 5; and also to medicinal compositions containing them. These compounds have inhibitory activity against IL-1β production, high water solubility and good oral absorbability.

摘要翻译： 具有式（1）的化合物：其中R 1表示烷基或烯基，R 2和R 3各自独立地表示氢原子 或烷基，羟基烷基，二羟基烷基或炔基或R 2和R 3可以与相邻的氮原子一起形成取代或未取代的含氮的 饱和杂环基，X，Y和Z各自独立地表示氢原子，烷基，卤素原子等，n表示1〜5的整数， 以及含有它们的药物组合物。 这些化合物对IL-1β生产具有抑制活性，水溶性高，口服吸收性好。