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：US06680316B1

公开(公告)日：2004-01-20

申请号：US09926040

申请日：2001-08-20

申请人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Takayuki Matsuda ,  Kyoko Yasuoka ,  Tomoko Furuyama

发明人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Takayuki Matsuda ,  Kyoko Yasuoka ,  Tomoko Furuyama

IPC分类号： C07D23724

CPC分类号： C07D237/24

摘要： Objects of the invention are to provide compounds having excellent activity against interleukin-1&bgr; production and also medicines comprising them as effective ingredients. Pyridazin-3-one derivatives represented by the following formula (1): wherein Ar1 represents a substituted or unsubstituted aromatic group, Ar2 represents a phenyl group having a substituent at least at the 4-position thereof, R1 represents a linear or branched alkyl group, an alkyl group having a cyclic structure, a substituted or unsubstituted phenyl group or a substituted or unsubstituted phenyl(lower alkyl) group, and R2 represents a cyano group, a carboxyl group, a (lower alkoxy)carbonyl group, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted carbamoyl group, or salts thereof; and medicines comprising them as effective ingredients.

摘要翻译： 本发明的目的是提供对白细胞介素-1β生产具有优异活性的化合物以及包含它们作为有效成分的药物。由下式（1）表示的哒嗪-3-酮衍生物：其中Ar 1表示取代或未取代的 芳基，Ar 2表示至少在其4位具有取代基的苯基，R 1表示直链或支链烷基，具有环状结构的烷基，取代或未取代的苯基或 取代或未取代的苯基（低级烷基），R 2表示氰基，羧基，（低级烷氧基）羰基，取代或未取代的低级烷基或取代或未取代的氨基甲酰基，或盐 的; 和包含它们作为有效成分的药物。

公开(公告)号：US06403586B1

公开(公告)日：2002-06-11

申请号：US09622897

申请日：2000-08-31

申请人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Takayuki Matsuda ,  Soichi Oda ,  Yuriko Habata ,  Kyoko Kotaki

发明人： Masao Ohkuchi ,  Yoshinori Kyotani ,  Hiromichi Shigyo ,  Hideo Yoshizaki ,  Tomoyuki Koshi ,  Takahiro Kitamura ,  Takayuki Matsuda ,  Soichi Oda ,  Yuriko Habata ,  Kyoko Kotaki

IPC分类号： A61K3150

CPC分类号： C07D401/06 ,  C07D237/02 ,  C07D237/04 ,  C07D237/22 ,  C07D237/24 ,  C07D401/12

摘要： This invention relates to pyridazine derivatives represented by the formula (1): wherein R1 represents a lower alkoxyl group, a lower alkylthio group or a halogen atom; R2 represents H, a lower alkoxyl group, a lower alkylthio group or a halogen atom; R3 represents a lower alkyl or lower alkenyl group, which may be substituted by one or more OHs, CNs, lower cycloalkyl groups, (substituted) aromatic groups or (substituted) carbamoyl groups; R4 represents COOH, a lower alkoxycarbonyl group, a (substituted) carbamoyl group, a (substituted) amino group, or a (substituted) ureido group; and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1&bgr; production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.

摘要翻译： 本发明涉及由式（1）表示的哒嗪衍生物：其中R1表示低级烷氧基，低级烷硫基或卤素原子; R2表示H，低级烷氧基，低级烷硫基或卤素原子; R 3表示低级烷基或低级烯基，其可以被一个或多个OH，CN，低级环烷基，（取代的）芳族基团或（取代的）氨基甲酰基取代; R4表示COOH，低级烷氧基羰基，（取代）氨基甲酰基，（取代）氨基或（取代）脲基; 虚线表示4位和5位之间的碳 - 碳键为单键或双键，或其盐; 以及含有它们作为有效成分的药物。 这些化合物对白细胞介素-1β生产具有优异的抑制活性，可用作免疫系统疾病，炎性疾病，缺血性疾病等的预防药物和治疗剂。