公开(公告)号：US5539112A

公开(公告)日：1996-07-23

申请号：US464093

申请日：1995-06-05

申请人： Tsutomu Akama ,  Shun-ichi Ikeda ,  Yasushi Shida ,  Masaji Kasai ,  Hiroyuki Ishida ,  Uichiro Kimura ,  Katsushige Gomi ,  Hiromitsu Saito ,  Kimihisa Ueno

发明人： Tsutomu Akama ,  Shun-ichi Ikeda ,  Yasushi Shida ,  Masaji Kasai ,  Hiroyuki Ishida ,  Uichiro Kimura ,  Katsushige Gomi ,  Hiromitsu Saito ,  Kimihisa Ueno

IPC分类号： C07D311/30 ,  C07D413/12

CPC分类号： C07D311/30

摘要： 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.6 are taken together to form a heterocyclic group containing the nitrogen atom in the ring), lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, lower alkoxycarbonyl, lower alkanoyl, adizo, cyano, substituted or unsubstituted carbamoyl or lower alkylthiothiocarbonyl: or pharmaceutically acceptable salts thereof.

摘要翻译： 由式（I）表示的5-氨基黄酮衍生物：其中R 1，R 2，R 3和R 4相同或不同，表示氢，取代或未取代的低级烷基，低级烯基，卤素取代或未取代的低级 烷酰基或低级烷氧基羰基，X 1，X 2，Y 1和Y 2相同或不同，表示氢，卤素或低级烷基，X 1和X 2中的至少一个表示卤素或低级烷基，X 3表示氢，取代或未取代的低级烷基，低级 烯基，低级炔基，卤素，羟基，取代或未取代的低级烷氧基，NR5R6（其中R5和R6相同或不同，代表氢，或取代或未取代的低级烷基，或R5和R6一起形成含有 环中的氮原子），低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，羧基，低级烷氧基羰基，低级烷酰基，二唑基，氰基，取代或未取代的氨基甲酰基或低级烷硫基硫代 辛基或其药学上可接受的盐。

公开(公告)号：US5952355A

公开(公告)日：1999-09-14

申请号：US757080

申请日：1996-11-26

申请人： Shun-Ichi Ikeda ,  Uichiro Kimura ,  Tadashi Ashizawa ,  Katsushige Gomi ,  Hiromitsu Saito ,  Masaji Kasai ,  Junji Kanazawa ,  Kimihito Sasaki ,  Etsuko Nukui ,  Masami Okabe ,  Soichiro Sato

发明人： Shun-Ichi Ikeda ,  Uichiro Kimura ,  Tadashi Ashizawa ,  Katsushige Gomi ,  Hiromitsu Saito ,  Masaji Kasai ,  Junji Kanazawa ,  Kimihito Sasaki ,  Etsuko Nukui ,  Masami Okabe ,  Soichiro Sato

IPC分类号： C07D209/12 ,  C07D209/30 ,  C07D401/06 ,  C07D405/06 ,  C07F7/08 ,  C07H15/24 ,  A61K31/40 ,  A61K31/44 ,  C07D209/32 ,  C07D209/40

CPC分类号： C07D401/06 ,  C07D209/12 ,  C07D209/30 ,  C07D405/06 ,  C07F7/0812 ,  C07H15/24

摘要： The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR.sup.5 (wherein Y represents S or O; and R.sup.5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R.sup.2 and R.sup.3 are combined to form substituted or unsubstituted methylene or ethylene; R.sup.4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及由下式（I）表示的丙烯酮衍生物：其中R1表示氢，取代或未取代的低级烷基，取代或未取代的芳基或YR5（其中Y表示S或O; R5表示取代或未取代的低级烷基 取代或未取代的芳基，取代或未取代的杂芳基，或取代或未取代的环醚残基）; R2和R3独立地表示氢，低级烷基或取代或未取代的芳烷基，或者R2和R3组合形成取代或未取代的亚甲基或亚乙基; R4表示氢，羟基，低级烷基，取代或未取代的芳烷基，低级烷氧基，取代或未取代的芳烷氧基或卤素; X表示取代或未取代的吲哚基; 或其药学上可接受的盐。