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1.发明公开
公开(公告)号：EP1080069A1
公开(公告)日：2001-03-07
申请号：EP99913686.4
申请日：1999-04-15
发明人： OKU, Teruo , SAWADA, Kozo , KURODA, Akio , INOUE, Takayuki , KAYAKIRI, Natsuko , SAWADA, Yuki , MIZUTANI, Tsuyoshi
IPC分类号： C07C237/28 , A61K31/165
CPC分类号： C07D213/40 , C07C227/30 , C07C227/32 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D207/48 , C07D211/58 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D307/22 , C07D317/58 , C07D333/20
摘要： Compounds of formula (I) wherein R1 is hydrogen or halogen; R2 is electron withdrawing group; R3 is hydrogen, hydroxy, lower alkoxy, cycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted, unsaturated heterocycle; A is lower alkylene; R4 is lower alkoxy, substituted or unsubstituted, saturated or unsaturated heterocycle, substituted or unsubstituted amino, -CH¿2?-R?5, -CR6R7R8¿ wherein R?6 and R7¿ are each independently carboxy, protected carboxy, substituted or unsubstituted carbamoyl, or substituted or unsubstituted lower alkyl, or R?6 and R7¿ together with the carbon atom to which they are attached may form substituted or unsubstituted, saturated carbocycle, or substituted or unsubstituted, unsaturated carbocycle, and R8 is hydrogen, lower alkoxy, or substituted or unsubstituted lower alkyl; provided that when R?4 is -CR6R7R8¿ wherein R?6 and R7¿ are each independently substituted or unsubstituted lower alkyl, and R8 is hydrogen or lower alkyl, or when R4 is -CH¿2?-R?5, R3¿ should be hydrogen, hydroxy or cycloalkyl.
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2.发明公开BENZIMIDAZOLONE DERIVATIVES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS 审中-公开苯并咪唑酮衍生物及其作为磷酸二酯酶抑制剂的使用
公开(公告)号：EP1196391A1
公开(公告)日：2002-04-17
申请号：EP00944421.7
申请日：2000-07-12
IPC分类号： C07D235/26 , C07D235/28 , C07D471/04 , C07D403/04 , C07D405/04 , C07D401/04 , C07D405/12 , C07D401/12 , A61K31/4184 , A61K31/437 , A61P15/10
CPC分类号： C07D401/04 , C07D235/26 , C07D235/28 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/12 , C07D471/04
摘要： Compounds of formula (Ia) wherein Xa is CH or nitrogen, Ya is oxygen or sulfur, R?1a and R2a¿ are specific substituents, R?3a, R4a and R5a¿ are the same or different, hydrogen, halogen, cyano, lower alkoxy or lower-alkoxy-substituted aralkyl; or two of R?3a, R4a and R5a¿ may combine together to form lower alkylenedioxy, and m is 1 or 2, are useful as cGMP-PDE inhibitors.
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3.发明公开SULFONAMIDE COMPOUNDS AND MEDICINAL USE THEREOF 失效SULFONAMIDVERBINDUNGEN UND IHRE MEDISINISCHE VERWENDUNG
公开(公告)号：EP0995742A1
公开(公告)日：2000-04-26
申请号：EP98929715.5
申请日：1998-06-24
发明人： KAYAKIRI, Hiroshi , ABE, Yoshito , HAMASHIMA, Hitoshi , SAWADA, Hitoshi , MIZUTANI, Tsuyoshi , YAMASAKI, Noritsugu , ONOMURA, Osamu , NISHIKAWA, Masahiro , HIRAMURA, Takahiro , OKU, Teruo , IMOTO, Takafumi
IPC分类号： C07D215/48 , C07D231/56 , C07D235/26 , C07D239/96 , C07D241/52 , C07D249/18 , C07D307/79 , C07D333/56 , C07D333/54 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , A61K31/34 , A61K31/38 , A61K31/415 , A61K31/47 , A61K31/495 , A61K31/505
CPC分类号： C07D241/52 , C07D215/48 , C07D231/56 , C07D239/96 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A sulfonamide compound of the formula (I):
R 1 -SO 2 NHCO-A-X-R 2 (I)
wherein R 1 is alkyl, alkenyl, alkynyl and the like; A is an optionally substituted heteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyl and 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R 2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.摘要翻译： 式（I）的磺酰胺化合物：R 1 -SO 2 NHCO-A-X-R 2其中R 1是烷基，烯基，炔基等; A是任选取代的杂多环基团，除了苯并咪唑基，吲哚基，4,7-二氢苯并咪唑基和2,3-二氢苯并恶嗪基; X是亚烷基，氧杂，氧杂（低级）亚烷基等; R 2是任选取代的芳基，取代的联苯基等，其盐和包含它们的药物组合物。 磺胺类化合物基于其血糖抑制活性，cGMP-PDE（特别是PDE-V）抑制活性，平滑肌松弛活性，支气管扩张活性，血管舒张活性，平滑肌细胞抑制活性，对于可治疗的疾病是有效的，以及 抗过敏活性。
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公开(公告)号：EP0879233B1
公开(公告)日：2003-08-13
申请号：EP97901799.3
申请日：1997-01-31
IPC分类号： C07D401/12 , A61K31/395 , C07D401/14 , C07D409/14
CPC分类号： C07D401/14 , C07D401/12 , C07D409/14
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公开(公告)号：EP0879233A1
公开(公告)日：1998-11-25
申请号：EP97901799.0
申请日：1997-01-31
CPC分类号： C07D401/14 , C07D401/12 , C07D409/14
摘要： This invention relates to a compound of formula (1) wherein R1 is halogen, etc., R2 is halogen, etc., R3 is amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, etc., R4 is heterocyclic (lower)alkyl, R5 is lower alkyl, and A1 is lower alkylene, and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of hypertension or the like.
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公开(公告)号：EP0861243B1
公开(公告)日：2003-11-12
申请号：EP96931226.3
申请日：1996-09-18
IPC分类号： C07D401/12 , A61K31/395 , C07D401/14 , C07D471/04 , C07D215/26 , C07D409/12 , C07D409/14
CPC分类号： C07D231/12 , C07D215/26 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D471/04
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7.发明授权ANTHRANILIC ACID DERIVATIVES AS INHIBITORS OF THE CGMP-PHOSPHODIESTERASE 有权ANTHRANILSAUREDERIVATE ALS INHIBITOREN DER C-GMP-PHOSPHODIESTERASE
公开(公告)号：EP1080069B1
公开(公告)日：2003-03-19
申请号：EP99913686.4
申请日：1999-04-15
发明人： OKU, Teruo , SAWADA, Kozo , KURODA, Akio , INOUE, Takayuki , KAYAKIRI, Natsuko , SAWADA, Yuki , MIZUTANI, Tsuyoshi
IPC分类号： C07C237/28 , A61K31/165
CPC分类号： C07D213/40 , C07C227/30 , C07C227/32 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D207/48 , C07D211/58 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D307/22 , C07D317/58 , C07D333/20
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公开(公告)号：EP0861243A1
公开(公告)日：1998-09-02
申请号：EP96931226.0
申请日：1996-09-18
IPC分类号： A61K31 , A61P29 , A61P37 , A61P43 , C07D215 , C07D401 , C07D403 , C07D405 , C07D409 , C07D413 , C07D471 , C07D521
CPC分类号： C07D231/12 , C07D215/26 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D471/04
摘要： This invention relates to a compound of formula (I) wherein A1 is lower alkylene, R1 is substituted quinolyl, etc., R2 is hydrogen, halogen or lower alkyl, R3 is halogen or lower alkyl, and R4 is a group of the formula: -Q-A2-R5, etc., in which R5 is amino, acylamino, etc., A2 is lower alkylene or a single bond, and Q is a group of formula (a), and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
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