公开(公告)号：US06413995B1

公开(公告)日：2002-07-02

申请号：US09856419

申请日：2001-05-21

申请人： Yoshihiro Hasegawa ,  Shouichirou Shindou ,  Tomohisa Hattori ,  Tatsuhiro Obata ,  Fumiko Horiuchi ,  Hiroyuki Hayakawa ,  Hiroaki Kumazawa

发明人： Yoshihiro Hasegawa ,  Shouichirou Shindou ,  Tomohisa Hattori ,  Tatsuhiro Obata ,  Fumiko Horiuchi ,  Hiroyuki Hayakawa ,  Hiroaki Kumazawa

IPC分类号： C07D21340

CPC分类号： C07D213/40

摘要： The invention relates to cinnamamide derivatives having the following formula wherein R1 represents a hydroxyl group, a C1-6-alkoxy group, an arylalkoxy group or a substituted or unsubstituted amino group; R2 and R3 are same or different, each of which represents a hydrogen atom, a halogen atom or a C1-4-alkyl group; R4 represents a hydrogen atom or a C1-6-alkyl group; R5 represents a hydrogen atom, a C1-6-alkyl group or an aryl group; R6 represents a hydrogen atom, a C1-6-alkyl group, a cyano group or a C1-6-alkoxy-carbonyl group; W represents an oxygen atom, a sulfur atom, an imino group, a methylene group, a hydroxymethylene group or a carbonyl group; X and Y are same or different, each of which represents an oxygen atom or a sulfur atom; m represents an integer of 0 to 2; n represents an integer of 1 to 3; and when m is 0, a group: —C(R2)(R3)—W— may represent a vinylene group; or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition containing the above compound, in particular, an immunomodulatory agent and a prophylactic or therapeutic agent for nephrotic syndrome, circulatory disorders or respiratory diseases.

摘要翻译： 本发明涉及具有下列化学式的肉桂酰胺衍生物：R1表示羟基，C1-6-烷氧基，芳基烷氧基或取代或未取代的氨基; R2和R3相同或不同，各自表示氢原子， 卤素原子或C 1-4 - 烷基; R 4表示氢原子或C 1-6 - 烷基; R 5表示氢原子，C 1-6 - 烷基或芳基; R 6表示氢原子， C 1-6 - 烷基，氰基或C 1-6 - 烷氧基 - 羰基; W表示氧原子，硫原子，亚氨基，亚甲基，羟基亚甲基或羰基; X和 Y相同或不同，各自表示氧原子或硫原子; m表示0〜2的整数，n表示1〜3的整数， 并且当m为0时，基团-C（R 2）（R 3）-W-可以表示亚乙烯基;或其药学上可接受的盐; 以及含有上述化合物，特别是免疫调节剂，肾病综合征，循环障碍或呼吸系统疾病的预防或治疗剂的药物组合物。

公开(公告)号：US06313153B1

公开(公告)日：2001-11-06

申请号：US09463511

申请日：2000-01-21

申请人： Yoshihiro Hasegawa ,  Shouichirou Shindou ,  Tomohisa Hattori ,  Yousuke Yamazaki ,  Tatsuhiro Obata ,  Fumiko Horiuchi ,  Hiroyuki Hayakawa ,  Hiroaki Kumazawa

发明人： Yoshihiro Hasegawa ,  Shouichirou Shindou ,  Tomohisa Hattori ,  Yousuke Yamazaki ,  Tatsuhiro Obata ,  Fumiko Horiuchi ,  Hiroyuki Hayakawa ,  Hiroaki Kumazawa

IPC分类号： C07D21342

CPC分类号： C07D213/56

摘要： The present invention relates to an agent for treating nephritis and a TGF-&bgr; inhibiting agent comprising as an effective ingredient a pyridylacrylamide derivative represented by the following formula (I): wherein Ar1 is a substituted or unsubstituted pyridyl group, Ar2 is a substituted or unsubstituted phenyl group, R1 is a hydrogen atom, an alkyl group or an aryl group, R2 is a hydrogen atom, an alkyl group, a cyano group or an alkoxycarbonyl group, R3 is a hydrogen atom or an optionally substituted alkyl group, X is an oxygen or sulfur atom, A and B are same or different and each represent a hydrogen atom, a hydroxyl group, an alkoxy group or an alkylthio group, or A and B together form an oxo or thioxo group, or a group represented by the formula: ═N—Y in which Y is a dialkylamino, hydroxyl, aralkyloxy or alkoxy group, or a group represented by the formula: —Z1—M—Z2— which Z1 and Z2 are same or different and each represent an oxygen or sulfur atom or an imino group optionally substituted by an alkyl group, and M is an alkylene group or a 1,2-phenylene group, or A is a hydroxyl group and B is a 1-alkylimidazol-2-yl group, and n is an integer of 1 to 3, or a pharmaceutically acceptable salt thereof; as well as the pyridylacrylamide derivatives.

摘要翻译： 本发明涉及治疗肾炎的药剂和TGF-β抑制剂，其包含作为有效成分的下式（I）表示的吡啶基丙烯酰胺衍生物：其中Ar1为取代或未取代的吡啶基，Ar2为取代或未取代的 苯基，R 1为氢原子，烷基或芳基，R 2为氢原子，烷基，氰基或烷氧基羰基，R 3为氢原子或任选取代的烷基，X为 氧或硫原子，A和B相同或不同，各自表示氢原子，羟基，烷氧基或烷硫基，或A和B一起形成氧代或硫代基，或由式 ：= NY，其中Y是二烷基氨基，羟基，芳烷氧基或烷氧基，或由式-Z1-M-Z2-表示的基团，其中Z1和Z2相同或不同，各自表示氧或硫原子或 亚胺基可选择地 由烷基取代，M为亚烷基或1,2-亚苯基，或A为羟基，B为1-烷基咪唑-2-基，n为1〜3的整数， 或其药学上可接受的盐; 以及吡啶基丙烯酰胺衍生物。