公开(公告)号：EP1339687B1

公开(公告)日：2008-01-23

申请号：EP01991731.9

申请日：2001-11-19

申请人： Bayer HealthCare AG

发明人： MURATA, Toshiki ,  SAKAKIBARA, Sachiko ,  YOSHINO, Takashi ,  IKEGAMI, Yuka ,  MASUDA, Tsutomu ,  SHIMADA, Mitsuyuki ,  SHINTANI, Takuya ,  SHIMAZAKI, Makoto ,  LOWINGER, Timothy, B. ,  ZIEGELBAUER, Karl, B. ,  FUCHIKAMI, Kinji ,  UMEDA, Masaomi ,  KOMURA, Hiroshi ,  YOSHIDA, Nagahiro

IPC分类号： C07D213/85 ,  A61K31/44 ,  A61P29/00 ,  C07D405/12 ,  C07D401/12 ,  C07D401/10 ,  C07D213/73 ,  C07D213/80 ,  C07D213/82 ,  C07D498/04 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377

CPC分类号： C07D213/73 ,  C07D213/80 ,  C07D213/82 ,  C07D213/85 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12

摘要： 4-aryl pyrimidine compounds of general formula and salts thereof:wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C¿1-6? alkoxy, etc.; R?2¿ is hydrogen, halogen, etc.; R3 is hydrogen, hydroxy, halogen, amino, etc.; R4 is hydroxy, amino, carboxy, etc. or R?3 and R4¿ together form a ring; R5 is hydrogen, carbamoyl, cyano, carboxy, C¿1-16? alkoxycarbonyl, etc. and R?6¿ is amino or C¿1-16? alkanoylamino or R?5 and R6¿ together form a ring. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and act as inhibitors of IKK-β and thus inhibit nuclear factor kappa B(NF-¿K?B).

摘要翻译： 通式4-芳基嘧啶化合物及其盐：其中X是CH或N; R 1是氢，卤素，C 1-6烷基，C 1-6 - 烷氧基等; R 2是氢，卤素等; R3是氢，羟基，卤素，氨基等; R4是羟基，氨基，羧基等，或者R3和R4一起形成一个环; R5是氢，氨基甲酰基，氰基，羧基，C1-16- 烷氧基羰基等，R 6是氨基或C 1-16。 烷酰基氨基或R 5和R 6一起形成一个环。 化合物（Ⅰ）或其盐具有优良的抗炎活性，可作为IKK-β的抑制剂，从而抑制核因子κB（NF-κB）。

公开(公告)号：EP1487842B1

公开(公告)日：2007-03-14

申请号：EP03743829.8

申请日：2003-03-03

申请人： Bayer HealthCare AG

发明人： MURATA, Toshiki ,  SAKAKIBARA, Sachiko ,  YOSHINO, Takashi ,  SATO, Hiroki ,  KORIYAMA, Yuji ,  NUNAMI, Noriko ,  YAMAUCHI, Megumi ,  FUKUSHIMA, Keiko ,  GROSSER, Rolf ,  FUCHIKAMI, Kinji ,  BACON, Kevin ,  LOWINGER, Timothy

IPC分类号： C07D498/04 ,  A61K31/5365 ,  A61P29/00

CPC分类号： C07D498/04

摘要： An optically active (-)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido [2,3-d][1,3]oxazin-2-one of the formula (I) or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.

公开(公告)号：EP1487842A1

公开(公告)日：2004-12-22

申请号：EP03743829.8

申请日：2003-03-03

申请人： Bayer HealthCare AG

发明人： MURATA, Toshiki ,  SAKAKIBARA, Sachiko ,  YOSHINO, Takashi ,  SATO, Hiroki ,  KORIYAMA, Yuji ,  NUNAMI, Noriko ,  YAMAUCHI, Megumi ,  FUKUSHIMA, Keiko ,  GROSSER, Rolf ,  FUCHIKAMI, Kinji ,  BACON, Kevin ,  LOWINGER, Timothy

IPC分类号： C07D498/04 ,  A61K31/5365 ,  A61P29/00

CPC分类号： C07D498/04

摘要： An optically active (-)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido [2,3-d][1,3]oxazin-2-one of the formula (I) or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.

公开(公告)号：EP1326856B1

公开(公告)日：2007-12-19

申请号：EP01969704.4

申请日：2001-09-10

申请人： Bayer HealthCare AG

发明人： LOWINGER, Timothy, B. ,  MURATA, Toshiki ,  UMEDA, Masaomi ,  SAKAKIBARA, Sachiko ,  YOSHINO, Takashi ,  SATO, Hiroki ,  MASUDA, Tsutomu ,  KORIYAMA, Yuji ,  SHIMADA, Mitsuyuki ,  SHINTANI, Takuya ,  KADONO, Hiroshi ,  ZIEGELBAUER, Karl, B. ,  FUCHIKAMI, Kinji ,  KOMURA, Hiroshi

IPC分类号： C07D401/04 ,  C07D213/85 ,  C07D401/14 ,  C07D409/14 ,  C07D401/06 ,  C07D413/14 ,  C07D405/14 ,  C07D471/04 ,  A61P17/00 ,  A61P11/06 ,  A61P29/00 ,  A61K31/4427 ,  A61K31/4353 ,  C07D471/18 ,  C07D498/04 ,  C07D213/80 ,  C07D213/73 ,  C07D521/00 ,  C07D513/04

CPC分类号： C07D213/08 ,  C07D213/10 ,  C07D213/73 ,  C07D213/80 ,  C07D213/85 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  C07D513/04 ,  C07D515/04

摘要： Pyridine compounds of general formula (I) wherein -R1 represents, or in which R11 is hydrogen, C¿1-6? alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or -O-(CH2)n-R?111 ; R2¿ represents hydrogen or halogen; R3 represents hydrogen, -CR?31R32R33¿, or -NR?34R35; R4¿ is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C¿1-6? alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.