公开(公告)号：US20070270421A1

公开(公告)日：2007-11-22

申请号：US10577065

申请日：2005-02-25

申请人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi

发明人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi

IPC分类号： A61K31/44 ,  A61K31/445 ,  A61K31/497 ,  A61K31/505 ,  A61K31/535 ,  A61P35/04 ,  C07D211/68 ,  C07D239/02 ,  C07D239/42 ,  C07D413/02

CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

摘要： A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents C1-6 alkyl or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents C1-6 alkyl or the like; V1 represents oxygen or the like; V2 represents oxygen or sulfur; W represents —NH— or the like; X represents —CH═, nitrogen or the like; and Y represents oxygen or the like.]

摘要翻译： 由下式表示的化合物，其盐或其水合物具有优异的肝细胞生长因子受体（HGFR）抑制活性，具有抗肿瘤活性，血管生成抑制活性和癌转移抑制活性。 [R 1] 1表示C 1-6烷基等; R 2和R 3代表氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢 卤素，C 1-6烷基等; R 8表示氢等; R 9表示C 1-6烷基等; V 1表示氧等; V 2表示氧或硫; W表示-NH-等; X表示-CH-，氮等; Y表示氧等。]

公开(公告)号：US20100075944A1

公开(公告)日：2010-03-25

申请号：US12558982

申请日：2009-09-14

申请人： Tomohiro MATSUSHIMA ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi ,  Shuji Shirotori

发明人： Tomohiro MATSUSHIMA ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi ,  Shuji Shirotori

IPC分类号： A61K31/4545 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/397 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D213/75 ,  C07D239/47 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen or the like.

摘要翻译： 由下式表示的化合物或其盐或前述的水合物具有优异的肝细胞生长因子受体（HGFR）抑制活性，具有抗肿瘤活性，血管生成抑制活性和癌转移抑制活性。 R1表示3〜10元非芳族杂环基等， R2和R3表示氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢，卤素，C 1-6烷基等; R8表示氢等; R9表示3〜10元非芳香族杂环基等， n表示1或2的整数; X表示-CH =，氮等。

公开(公告)号：US20080319188A1

公开(公告)日：2008-12-25

申请号：US11508322

申请日：2006-08-23

申请人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi ,  Shuji Shirotori

发明人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi ,  Shuji Shirotori

IPC分类号： C07D213/72 ,  C07D239/47 ,  C07D403/02 ,  C07D413/02 ,  C07D417/02 ,  C07D401/02

CPC分类号： C07D401/12 ,  C07D213/75 ,  C07D239/47 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen or the like.]

摘要翻译： 由下式表示的化合物，其盐或其水合物具有优异的肝细胞生长因子受体（HGFR）抑制活性，具有抗肿瘤活性，血管生成抑制活性和癌转移抑制活性。 [R 1表示3〜10元非芳香族杂环基等， R2和R3表示氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢，卤素，C 1-6烷基等; R8表示氢等; R9表示3〜10元非芳香族杂环基等， n表示1或2的整数; X表示-CH-，氮等。]

公开(公告)号：US08288538B2

公开(公告)日：2012-10-16

申请号：US12558982

申请日：2009-09-14

申请人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi ,  Shuji Shirotori

发明人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi ,  Shuji Shirotori

IPC分类号： C07D213/75 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

CPC分类号： C07D401/12 ,  C07D213/75 ,  C07D239/47 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen or the like.

摘要翻译： 由下式表示的化合物或其盐或前述的水合物具有优异的肝细胞生长因子受体（HGFR）抑制活性，具有抗肿瘤活性，血管生成抑制活性和癌转移抑制活性。 R1表示3〜10元非芳族杂环基等， R2和R3表示氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢，卤素，C 1-6烷基等; R8表示氢等; R9表示3〜10元非芳香族杂环基等， n表示1或2的整数; X表示-CH =，氮等。

公开(公告)号：US20120232049A1

公开(公告)日：2012-09-13

申请号：US12527633

申请日：2008-02-22

申请人： Hiroshi Obaishi ,  Takayuki Nakagawa ,  Tomohiro Matsushima ,  Setsuo Funasaka ,  Shuji Shirotori ,  Keiko Takahashi

发明人： Hiroshi Obaishi ,  Takayuki Nakagawa ,  Tomohiro Matsushima ,  Setsuo Funasaka ,  Shuji Shirotori ,  Keiko Takahashi

IPC分类号： A61K31/4427 ,  C12Q1/68 ,  C07D401/12 ,  A61K31/4545 ,  A61K31/496 ,  A61P35/00 ,  A61K31/4439 ,  A61K31/506 ,  C07D413/12 ,  A61K31/5377 ,  C07D213/75 ,  A61K31/44 ,  G01N33/573 ,  C07D401/14

CPC分类号： C07D213/75 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C12Q1/6886 ,  C12Q2600/136 ,  G01N33/5011 ,  G01N2333/4753

摘要： A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen.

摘要翻译： 由式（I）表示的吡啶或嘧啶衍生物具有优异的HGFR抑制活性，对具有扩增的HGFR基因的癌细胞系表现出强的细胞增殖抑制作用和抗肿瘤效果。 其中R1表示3至10元非芳族杂环基等; R2和R3表示氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢，卤素，C 1-6烷基等; R8表示氢等; R9表示3〜10元非芳香族杂环基等， n表示1或2的整数; X表示-CH =，氮。

公开(公告)号：US07531532B2

公开(公告)日：2009-05-12

申请号：US11065631

申请日：2005-02-25

申请人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi

发明人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi

IPC分类号： C07D213/75 ,  C07D239/48 ,  C07D239/47 ,  A61K31/44

CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

摘要： A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents C1-6 alkyl or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents C1-6 alkyl or the like; V1 represents oxygen or the like; V2 represents oxygen or sulfur; W represents —NH— or the like; X represents —CH═, nitrogen or the like; and Y represents oxygen or the like.]

摘要翻译： 由下式表示的化合物，其盐或其水合物具有优异的肝细胞生长因子受体（HGFR）抑制活性，具有抗肿瘤活性，血管生成抑制活性和癌转移抑制活性。 [R1表示C1-6烷基等; R2和R3表示氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢，卤素，C 1-6烷基等; R8表示氢等; R 9表示C 1-6烷基等; V1表示氧等; V2表示氧或硫; W表示-NH-等; X表示-CH-，氮等; Y表示氧等。]

公开(公告)号：US20050277652A1

公开(公告)日：2005-12-15

申请号：US11065631

申请日：2005-02-25

申请人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi

发明人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Hiroshi Obaishi

IPC分类号： A61K31/44 ,  A61K31/4409 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/18 ,  A61P9/00 ,  A61P11/00 ,  A61P13/08 ,  A61P13/12 ,  A61P15/00 ,  A61P25/00 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07D213/73 ,  C07D213/75 ,  C07D239/46 ,  C07D239/47 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D487/08

CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

摘要： A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents C1-6 alkyl or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents C1-6 alkyl or the like; V1 represents oxygen or the like; V2 represents oxygen or sulfur; W represents —NH— or the like; X represents —CH═, nitrogen or the like; and Y represents oxygen or the like.]

摘要翻译： 由下式表示的化合物，其盐或其水合物具有优异的肝细胞生长因子受体（HGFR）抑制活性，具有抗肿瘤活性，血管生成抑制活性和癌转移抑制活性。 [R 1] 1表示C 1-6烷基等; R 2和R 3代表氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢 卤素，C 1-6烷基等; R 8表示氢等; R 9表示C 1-6烷基等; V 1表示氧等; V 2表示氧或硫; W表示-NH-等; X表示-CH-，氮等; Y表示氧等。]

公开(公告)号：US07855290B2

公开(公告)日：2010-12-21

申请号：US11508322

申请日：2006-08-23

申请人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Shuji Shirotori

发明人： Tomohiro Matsushima ,  Keiko Takahashi ,  Setsuo Funasaka ,  Shuji Shirotori

IPC分类号： C07D213/75 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

CPC分类号： C07D401/12 ,  C07D213/75 ,  C07D239/47 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH═, nitrogen or the like.]

摘要翻译： 由下式表示的化合物，其盐或其水合物具有优异的肝细胞生长因子受体（HGFR）抑制活性，具有抗肿瘤活性，血管生成抑制活性和癌转移抑制活性。 [R 1表示3〜10元非芳香族杂环基等， R2和R3表示氢; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢，卤素，C 1-6烷基等; R8表示氢等; R9表示3〜10元非芳香族杂环基等， n表示1或2的整数; X表示-CH =，氮等。]