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1. 发明授权

US07378423B2 Pyrimidine compound and medical use thereof 有权
标题翻译：嘧啶化合物及其医疗用途
公开(公告)号：US07378423B2
公开(公告)日：2008-05-27
申请号：US11150792
申请日：2005-06-10
申请人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
发明人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
IPC分类号： A61K31/519 , C07D487/04 , C07D413/10 , C07D413/12 , A61P35/00 , A61P31/5355
CPC分类号： C07D471/04 , A61K31/519 , C07C275/30 , C07C275/50 , C07C2601/16 , C07D239/545 , C07D239/553 , C07D239/62 , C07D471/16 , C07D487/04 , C07F9/53
摘要： The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.
摘要翻译：本发明涉及由下式[I]表示的嘧啶化合物或其药学上可接受的盐，其中每个符号如说明书中所定义，以及治疗或预防性治疗不期望的细胞增殖的方法，包括施用这种化合物。本发明的化合物在抑制不期望的细胞增殖，特别是抗肿瘤活性方面具有优异的活性，可用作预防或治疗癌症，风湿病等的抗肿瘤剂。此外，当与其它抗肿瘤剂如烷化剂或代谢拮抗剂组合使用时，本发明的化合物可以是更有效的抗肿瘤剂。

2. 发明申请

US20100240613A1 PYRIMIDINE COMPOUND AND MEDICAL USE THEREOF 有权
标题翻译：吡嗪类化合物及其医疗用途
公开(公告)号：US20100240613A1
公开(公告)日：2010-09-23
申请号：US12626443
申请日：2009-11-25
申请人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
发明人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
IPC分类号： A61K31/675 , C07D471/04 , A61K31/519 , C07F9/53 , A61K31/5377 , C07D487/04 , C07C275/30 , C07C275/50 , C07D239/545 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04 , A61K31/519 , C07C275/30 , C07C275/50 , C07C2601/16 , C07D239/545 , C07D239/553 , C07D239/62 , C07D471/16 , C07D487/04 , C07F9/53
摘要： The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.
摘要翻译：本发明涉及由下式[I]表示的嘧啶化合物或其药学上可接受的盐，其中每个符号如说明书中所定义，以及治疗或预防性治疗不期望的细胞增殖的方法，包括施用这种化合物。本发明的化合物在抑制不期望的细胞增殖，特别是抗肿瘤活性方面具有优异的活性，可用作预防或治疗癌症，风湿病等的抗肿瘤剂。此外，当与其它抗肿瘤剂如烷化剂或代谢拮抗剂组合使用时，本发明的化合物可以是更有效的抗肿瘤剂。

3. 发明申请

US20060014768A1 Pyrimidine compound and medical use thereof 有权
标题翻译：嘧啶化合物及其医疗用途
公开(公告)号：US20060014768A1
公开(公告)日：2006-01-19
申请号：US11150792
申请日：2005-06-10
申请人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
发明人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
IPC分类号： A61K31/513 , C07D405/02
CPC分类号： C07D471/04 , A61K31/519 , C07C275/30 , C07C275/50 , C07C2601/16 , C07D239/545 , C07D239/553 , C07D239/62 , C07D471/16 , C07D487/04 , C07F9/53
摘要： The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.
摘要翻译：本发明涉及由下式[I]表示的嘧啶化合物或其药学上可接受的盐，其中每个符号如说明书中所定义，以及治疗或预防性治疗不期望的细胞增殖的方法，包括施用这种化合物。本发明的化合物在抑制不期望的细胞增殖，特别是抗肿瘤活性方面具有优异的活性，可用作预防或治疗癌症，风湿病等的抗肿瘤剂。此外，当与其它抗肿瘤剂如烷化剂或代谢拮抗剂组合使用时，本发明的化合物可以是更有效的抗肿瘤剂。

4. 发明申请

US20080312228A1 PYRIMIDINE COMPOUND AND MEDICAL USE THEREOF 审中-公开
标题翻译：吡嗪类化合物及其医疗用途
公开(公告)号：US20080312228A1
公开(公告)日：2008-12-18
申请号：US12053133
申请日：2008-03-21
申请人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
发明人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/496 , A61P35/00
CPC分类号： C07D471/04 , A61K31/519 , C07C275/30 , C07C275/50 , C07C2601/16 , C07D239/545 , C07D239/553 , C07D239/62 , C07D471/16 , C07D487/04 , C07F9/53
摘要： The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.
摘要翻译：本发明涉及由下式[I]表示的嘧啶化合物或其药学上可接受的盐，其中每个符号如说明书中所定义，以及治疗或预防性治疗不期望的细胞增殖的方法，包括施用这种化合物。本发明的化合物在抑制不期望的细胞增殖，特别是抗肿瘤活性方面具有优异的活性，可用作预防或治疗癌症，风湿病等的抗肿瘤剂。此外，当与其它抗肿瘤剂如烷化剂或代谢拮抗剂组合使用时，本发明的化合物可以是更有效的抗肿瘤剂。

5. 发明授权

US5332734A Oxazinone derivative 失效
标题翻译：恶嗪酮衍生物
公开(公告)号：US5332734A
公开(公告)日：1994-07-26
申请号：US956029
申请日：1992-12-10
申请人： Koji Kobayashi , Shunichi Manabe , Yoshihiro Watanabe , Kazuhide Hayakawa , Itsuo Uchida
发明人： Koji Kobayashi , Shunichi Manabe , Yoshihiro Watanabe , Kazuhide Hayakawa , Itsuo Uchida
IPC分类号： C07D265/22 , C07D413/12 , C07D417/12 , C07D471/04 , C07D239/95 , A61K31/535 , A61K31/54 , C07D239/72
CPC分类号： C07D265/22 , C07D413/10 , C07D417/12 , C07D471/04
摘要： Disclosed is a novel oxazinone derivative represented by formula (I) given below or a pharmaceutically acceptable acid-addition salt thereof, which is useful as an anti-inflammatory agent, an agent for suppressing neutrophil infiltration and as a serine protease inhibitor: ##STR1## where A includes, for example, ##STR2## in which W is --O--, --S--, --CH.dbd.CH-- or --NR.sup.9 -- or means that (CH.sub.2).sub.n is directly bonded to (CH.sub.2).sub.n,V.sup.2 is .dbd.CR.sup.12 -- or .dbd.N--, andD is 5 to 7-membered carbon ring or hetero ring;X is --O--, --S--, --CO--, or --NR.sup.15 or means that A is directly bonded to (CH.sub.2).sub.l ;Y is --O--, --CH.dbd.CH-- or --NR.sup.16 -- or means that (CH.sub.2).sub.l is directly bonded to Z;Z is --CH.sub.2 -- or --CO--; andl is an integer of 0 to 4.Further, R and R.sup.1 to R.sup.16 are hydrogen atom, lower alkyl group, etc.
摘要翻译： PCT No.PCT / JP92 / 00444 Sec。 371日期：1992年12月10日 102（e）日期1992年12月10日PCT提交1992年4月9日PCT公布。出版物WO92 / 18488 日期：1992年10月29日。公开是由下述式（I）表示的新型恶嗪酮衍生物或其药学上可接受的酸加成盐，其可用作抗炎剂，抑制嗜中性粒细胞浸润的药剂丝氨酸蛋白酶抑制剂：其中A包括例如其中W是-O - ， - S - ， - CH = CH-或-NR 9 - 的，或意味着（CH 2）n直接键合到（CH 2）n，V 2是= CR 12 - 或= N-，D是5至7元碳环或杂环; X是-O - ， - S - ， - CO-或-NR 15或意指A直接键合到（CH 2）l; Y是-O - ， - CH = CH-或-NR 16 - 或意指（CH 2）l直接键合到Z上; Z是-CH 2 - 或-CO-; l为0〜4的整数。另外，R和R 1〜R 16为氢原子，低级烷基等。

6. 发明授权

US08835443B2 Pyrimidine compound and medical use thereof 有权
标题翻译：嘧啶化合物及其医疗用途
公开(公告)号：US08835443B2
公开(公告)日：2014-09-16
申请号：US12626443
申请日：2009-11-25
申请人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
发明人： Hisashi Kawasaki , Hiroyuki Abe , Kazuhide Hayakawa , Tetsuya Iida , Shinichi Kikuchi , Takayuki Yamaguchi , Toyomichi Nanayama , Hironori Kurachi , Masahiro Tamaru , Yoshikazu Hori , Mitsuru Takahashi , Takayuki Yoshida , Toshiyuki Sakai
IPC分类号： A61K31/519 , C07D239/545 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , A61K31/519 , C07C275/30 , C07C275/50 , C07C2601/16 , C07D239/545 , C07D239/553 , C07D239/62 , C07D471/16 , C07D487/04 , C07F9/53
摘要： The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.
摘要翻译：本发明涉及由下式[I]表示的嘧啶化合物或其药学上可接受的盐，其中每个符号如说明书中所定义，以及治疗或预防性治疗不期望的细胞增殖的方法，包括施用这种化合物。本发明的化合物在抑制不期望的细胞增殖，特别是抗肿瘤活性方面具有优异的活性，可用作预防或治疗癌症，风湿病等的抗肿瘤剂。此外，当与其它抗肿瘤剂如烷化剂或代谢拮抗剂组合使用时，本发明的化合物可以是更有效的抗肿瘤剂。

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