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公开(公告)号：EP1308441B1
公开(公告)日：2009-10-07
申请号：EP01955633.1
申请日：2001-08-09
发明人： HARADA, Hitoshi , ASANO, Osamu , MIYAZAWA, Shuhei , UEDA, Masato , YASUDA, Masahiro , YASUDA, Nobuyuki
IPC分类号： A61K31/443 , A61K31/444 , A61K31/455 , A61P1/10 , C07D405/14 , C07D213/85 , C07D409/14 , C07D213/82
CPC分类号： C07D213/80 , A61K31/4409 , A61K31/443 , A61K31/4436 , A61K31/444 , A61K31/455 , C07D213/82 , C07D213/85 , C07D405/04 , C07D405/14 , C07D409/14
摘要： 2-Aminopyridine compounds of the general formula (I) and salts thereof, exhibiting excellent adenosine receptor (A1, A2a, or A2b receptor) antagonism wherein R1 is cyano, carboxyl, or optionally substituted carbamoyl; R2 is hydrogen, hydroxyl, optionally substituted C¿1-6? alkoxy, an optionally substituted C6-14 aromatic carbocyclic group, or an optionally substituted 5- to 14-membered aromatic heterocyclic group; and R?3 and R4¿ are each independently an optionally substituted C¿6-14? aromatic carbocyclic group, a 5- to 14-membered nonaromatic heterocyclic group, a 5- to 14-membered aromatic heterocyclic group, or the like.
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2.发明公开4-(3-BENZOYLAMINOPHENYL)-6,7-DIMETHOXY-2- METHYLAMINOQUINAZOLINE DERIVATIVE 有权4-（3-苯甲酰氨基苯基）-6,7-二甲氧基-2- METHYLAMINOCHINAZOLINDERIVAT
公开(公告)号：EP1992622A1
公开(公告)日：2008-11-19
申请号：EP07714569.6
申请日：2007-02-20
发明人： MIYAZAKI, Kazuki , KUSANO, Kazutomi , TAKASE, Yasutaka , ASANO, Osamu , SHIRATO, Manabu , WAKITA, Hisashi , ISHII, Naoto , SAEKI, Takao
IPC分类号： C07D239/84 , A61K31/517 , A61P17/00 , A61P17/04 , A61P37/08
CPC分类号： C07D239/84
摘要： A compound represented by the following formula (I), salt thereof, or hydrate thereof, can effectively relieve itch caused by atopic disease or the like:
wherein R represents hydroxyl, C 1-6 alkoxy optionally substituted with C 1-6 alkoxy, or amino optionally substituted with C 1-6 alkyl.摘要翻译： 由下式（I）表示的化合物或其盐或其水合物可有效缓解由特应性疾病等引起的瘙痒：其中R表示羟基，任选被C 1-6烷氧基取代的C 1-6烷氧基或 任选被C 1-6烷基取代的氨基。
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公开(公告)号：EP1439175B1
公开(公告)日：2011-04-27
申请号：EP02802050.1
申请日：2002-10-22
发明人： HARADA, Hitoshi , ASANO, Osamu , UEDA, Masato , MIYAZAWA, Shuhei , KOTAKE, Yoshihiko , KABASAWA, Yasuhiro , YASUDA, Masahiro , YASUDA, Nobuyuki , IIDA, Daisuke , NAGAKAWA, Junichi , HIROTA, Kazuo , NAKAGAWA, Makoto
IPC分类号： C07D401/04 , C07D405/14 , C07D409/14 , A61K31/506 , A61P1/00 , A61P1/10 , A61P3/04 , A61P3/10 , A61P9/12 , A61P11/06 , A61P13/02 , A61P19/10 , A61P25/16 , A61P25/28 , A61P43/00
CPC分类号： C07D405/14 , A61K31/506 , C07D401/04 , C07D409/14
摘要： A novel pyrimidine compound having an excellent antagonistic activity against adenosine receptors (A1, A2A, and A2B receptors). Specifically, it is a compound represented by the following formula, a salt of the compound, or a solvate of either. (I) In the formula, R1 and R2 are the same or different and each represents hydrogen, optionally substituted C1-6 alkyl, etc.; R3 represents hydrogen, halogeno, etc.; R4 represents an optionally substituted C6-14 aromatic hydrocarbon ring group, optionally substituted 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond, etc.; and R5 represents an optionally substituted C6-14 aromatic hydrocarbon ring group or optionally substituted 5- to 14-membered aromatic heterocyclic group.
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4.发明授权4-(3-BENZOYLAMINOPHENYL)-6,7-DIMETHOXY-2- METHYLAMINOQUINAZOLINE DERIVATIVE 有权4-（3-苯甲酰氨基苯基）-6,7-二甲氧基-2- METHYLAMINOCHINAZOLINDERIVAT
公开(公告)号：EP1992622B1
公开(公告)日：2011-07-27
申请号：EP07714569.6
申请日：2007-02-20
发明人： MIYAZAKI, Kazuki , KUSANO, Kazutomi , TAKASE, Yasutaka , ASANO, Osamu , SHIRATO, Manabu , WAKITA, Hisashi , ISHII, Naoto , SAEKI, Takao
IPC分类号： C07D239/84 , A61K31/517 , A61P17/00 , A61P17/04 , A61P37/08
CPC分类号： C07D239/84
摘要： A compound represented by the formula (I) below, a salt thereof or a hydrate of any of them is capable of effectively suppressing itch of atopic diseases and the like. (I) [In the formula, R represents a hydroxyl group, a C1-6 alkoxy group which may be substituted by a C1-6 alkoxy group, or an amino group which may be substituted by a C1-6 alkyl group.]
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5.发明公开CRYSTAL, AMORPHOUS FORM AND SALT OF METHYL N-Ý3-(6,7-DIMETHOXY- 2-METHYLAMINOQUINAZOLIN-4-YL)PHENYL¨TEREPHTHALAMIC ACID 审中-公开KRISTALL，AMORPHE FORM UND盐酸N- [3-（6,7-二甲氧基-2-甲基氨基氧杂环己烷-4-YL）苯基]十二烷基硫酸钠
公开(公告)号：EP2123641A1
公开(公告)日：2009-11-25
申请号：EP08711290.0
申请日：2008-02-14
IPC分类号： C07D239/84
CPC分类号： C07D239/84
摘要： Crystals, amorphous substances, salts, and hydrates of salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid have PDE4 inhibitory action and are useful for treating allergic diseases such as atopic dermatitis.
摘要翻译： N- [3-（6,7-二甲氧基-2-甲基氨基喹唑啉-4-基）苯基]苯甲酰甲酸甲酯的晶体，无定形物质，盐和水合物具有PDE4抑制作用，可用于治疗过敏性疾病如 特应性皮炎。
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公开(公告)号：EP2202231A1
公开(公告)日：2010-06-30
申请号：EP08832347.2
申请日：2008-09-19
发明人： CLARK, Richard , TAKEMURA, Atsushi , WATANABE, Nobuhisa , ASANO, Osamu , NAGAKURA, Tadashi , TABATA, Kimiyo
IPC分类号： C07D401/12 , A61K31/4196 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/506 , A61P7/02 , A61P9/10 , A61P9/14 , A61P11/00 , A61P35/00 , A61P43/00 , C07D209/44 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D417/14 , C07D209/44 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation.
[wherein R 1 represents hydrogen, R 2 represents optionally substituted phenyl, etc., R 3 represents optionally substituted C6-10 aryl, etc.]摘要翻译： 由下述通式（1）表示的化合物或其盐具有丝氨酸蛋白酶抑制活性，特别是对凝血因子VIIa的抑制活性特别优异。 该化合物或其盐可用作与血栓形成有关的疾病的治疗剂和/或预防剂。 [其中R 1表示氢，R 2表示任选取代的苯基等，R 3表示任选取代的C 6-10芳基等]
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公开(公告)号：EP1439176B1
公开(公告)日：2007-03-21
申请号：EP02802051.9
申请日：2002-10-22
发明人： HARADA, Hitoshi , ASANO, Osamu , UEDA, Masato , MIYAZAWA, Shuhei , KOTAKE, Yoshihiko , KABASAWA, Yasuhiro , YASUDA, Masahiro , YASUDA, Nobuyuki
IPC分类号： C07D401/04 , C07D405/14 , C07D409/14 , A61K31/513 , A61P1/04 , A61P1/10 , A61P3/04 , A61P3/10 , A61P7/10 , A61P9/12 , A61P11/06 , A61P19/10 , A61P25/16 , A61P25/28 , A61P27/02 , A61P43/00
CPC分类号： C07D239/34 , A61K31/513
摘要： The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (I), salts thereof, or solvates of both: (I) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).
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