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1. 发明申请

US20100004238A1 FUSED HETEROCYCLIC COMPOUND 审中-公开
标题翻译：熔融杂环化合物
公开(公告)号：US20100004238A1
公开(公告)日：2010-01-07
申请号：US12518596
申请日：2007-12-11
申请人： Tomoyasu Ishikawa , Hiroshi Banno , Youichi Kawakita , Tomohiro Ohashi , Osamu Kurasawa
发明人： Tomoyasu Ishikawa , Hiroshi Banno , Youichi Kawakita , Tomohiro Ohashi , Osamu Kurasawa
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/519 , A61K31/4985
CPC分类号： C07D487/04
摘要： The present invention provides a fused heterocyclic compound having a tyrosine kinase inhibitory action, which is represented by the formula: wherein R1 is a hydrogen atom, a halogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom; R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, or R1 and R2, or R2 and R3 are optionally bonded to each other to form an optionally substituted ring structure; R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 is optionally bonded to the carbon atom on ring A to form an optionally substituted ring structure; ring A is an optionally substituted benzene ring; and ring B is (i) an optionally substituted fused ring, or (ii) a pyridine ring having optionally substituted carbamoyl (the pyridine ring is optionally further substituted).
摘要翻译：本发明提供具有酪氨酸激酶抑制作用的稠合杂环化合物，其由下式表示：其中R1是氢原子，卤原子或经由碳原子，氮原子或氧键键合的任意取代的基团原子; R2是氢原子，或通过碳原子或硫原子键合的任选取代的基团，或者R 1和R 2，或R 2和R 3相互结合形成任选取代的环结构; R3是氢原子或任选取代的脂族烃基，或R3任选地键合到环A上的碳原子上以形成任选取代的环结构; 环A是任选取代的苯环; 和环B是（i）任选取代的稠合环，或（ii）具有任选取代的氨基甲酰基的吡啶环（吡啶环任选进一步被取代）。

2. 发明申请

US20100216788A1 FUSED HETEROCYCLIC COMPOUND 审中-公开
标题翻译：熔融杂环化合物
公开(公告)号：US20100216788A1
公开(公告)日：2010-08-26
申请号：US12095543
申请日：2006-12-01
申请人： Tomoyasu Ishikawa , Kazuhiro Miwa , Masaki Seto , Hiroshi Banno , Youichi Kawakita
发明人： Tomoyasu Ishikawa , Kazuhiro Miwa , Masaki Seto , Hiroshi Banno , Youichi Kawakita
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/519 , C07D413/14 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides a compound represented by the formula: wherein R1a is a hydrogen atom, R2a is a C1-6 alkyl group substituted by a group represented by —NR6a—CO—(CH2)n—SO2— optionally halogenated C1-4 alkyl wherein n is an integer of 1 to 4, R6a is a hydrogen atom or a C1-4 alkyl group, and —(CH2)n— is optionally substituted by C1-4 alkyl, R3a is a hydrogen atom or a C1-6 alkyl group, R4a is a halogen atom or a C1-6 alkyl group, R5a is a halogen atom or a C1-6 alkyl group, and Xa is a hydrogen atom or a halogen atom, or a salt thereof. The compound of the present invention has a superior tyrosine kinase inhibitory action, is highly safe, and is sufficiently satisfactory as a pharmaceutical product.
摘要翻译：本发明提供由下式表示的化合物：其中R1a是氢原子，R2a是被-NR6a-CO-（CH2）n-SO2-代表的基团取代的C1-6烷基，任选被卤代的C 1-4烷基其中n为1〜4的整数，R6a为氢原子或C1-4烷基， - （CH2）n-为C1-4烷基，R3a为氢原子或C1-6烷基基团，R 4a是卤素原子或C 1-6烷基，R 5a是卤素原子或C 1-6烷基，X a是氢原子或卤素原子或其盐。本发明的化合物具有优异的酪氨酸激酶抑制作用，是高度安全的，并且作为药物产品足够令人满意。

3. 发明申请

US20080269238A1 Thiazolopyrimidine Derivative 审中-公开
标题翻译：噻唑并嘧啶衍生物
公开(公告)号：US20080269238A1
公开(公告)日：2008-10-30
申请号：US11547493
申请日：2005-03-31
申请人： Yoshihiro Sugihara , Youichi Kawakita
发明人： Yoshihiro Sugihara , Youichi Kawakita
IPC分类号： A61K31/519 , C07D513/04 , A61K31/496 , A61P35/00
CPC分类号： C07D513/04
摘要： The present invention provides a compound represented by the following Formula: wherein A is an aryl group or a heteroaryl group, each of which may be substituted; R1 is a group which is bonded through carbon; R2 is hydrogen or an aliphatic hydrocarbon group; and X is —NR3—, —O—, —S—, —SO—, —SO2—, or —CHR3— (wherein R3 is hydrogen or an aliphatic hydrocarbon group), or a salt thereof, or a prodrug thereof, which has growth factor receptor tyrosine kinase inhibitory activity and low toxicity, and is useful for prevention and treatment of cancer, and thus can be sufficiently used as a medicine.
摘要翻译：本发明提供由下式表示的化合物：其中A是可以被取代的芳基或杂芳基; R 1是通过碳键合的基团; R 2是氢或脂族烃基; 和X是-NR 3 - ， - O - ， - S - ， - SO - ， - SO 2 - 或-CHR 3 - - （其中R 3是氢或脂族烃基）或其盐或其前药，其具有生长因子受体酪氨酸激酶抑制活性和低毒性，并且可用于预防和治疗癌症，因此可以充分地用作药物。

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