公开(公告)号：US20080058347A1

公开(公告)日：2008-03-06

申请号：US11897272

申请日：2007-08-29

申请人： Yoshikuzu Iwasawa ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Kouta Masutani ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

发明人： Yoshikuzu Iwasawa ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Kouta Masutani ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

IPC分类号： A61K31/497 ,  A61K31/443 ,  A61K31/4436 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D413/14 ,  C07D401/14 ,  A61P35/00 ,  A61K31/4439

CPC分类号： C07D413/14 ,  A61K45/06 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1′ is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及式I化合物：其中：R 1是氢原子，F，CN等; R 1是氢原子或可被取代的低级烷基; R 2是O，S，SO，SO 2等; R 3是可被取代的苯基; X 1，X 2，X 3和X 3各自独立地为CH，N等。但是，X 1， / SUB>，X 2和X 3，氮的数目为0或1; W是以下残基：其中：W 1，W 2和W 3各自独立地是CH，N等，或药学上 可接受的盐或酯。

公开(公告)号：US20100016335A1

公开(公告)日：2010-01-21

申请号：US12310307

申请日：2007-08-29

申请人： Yoshikazu Iwasawa ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Kouta Masutani ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

发明人： Yoshikazu Iwasawa ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Kouta Masutani ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

IPC分类号： A61K31/497 ,  C07D413/14 ,  A61K31/4439 ,  C07D417/14 ,  A61K31/506 ,  C07D403/04

CPC分类号： C07D413/14 ,  A61K45/06 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1′ is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及式I化合物：其中：R1是氢原子，F，CN等; R1'是氢原子或可被取代的低级烷基; R2是O，S，SO，SO2等; R3是可被取代的苯基; X1，X2和X3各自独立地为CH，N等，但X1，X2和X3之间的氮数为0或1。 W是以下残基：其中：W1，W2和W3各自独立地为CH，N等，或其药学上可接受的盐或酯。

公开(公告)号：US07915263B2

公开(公告)日：2011-03-29

申请号：US11897272

申请日：2007-08-29

申请人： Yoshikazu Iwasawa ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Kouta Masutani ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

发明人： Yoshikazu Iwasawa ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Kouta Masutani ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

IPC分类号： C07D401/12 ,  A61K31/4439

CPC分类号： C07D413/14 ,  A61K45/06 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1′ is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及式I化合物：其中：R1是氢原子，F，CN等; R1'是氢原子或可被取代的低级烷基; R2是O，S，SO，SO2等; R3是可被取代的苯基; X1，X2和X3各自独立地为CH，N等，但X1，X2和X3之间的氮数为0或1。 W是以下残基：其中：W1，W2和W3各自独立地为CH，N等，或其药学上可接受的盐或酯。

公开(公告)号：US20110003833A1

公开(公告)日：2011-01-06

申请号：US12866955

申请日：2009-02-18

申请人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

发明人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

IPC分类号： A61K31/506 ,  C07D417/14 ,  A61K31/4545 ,  A61P35/00 ,  C07D401/14

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D413/14

摘要： The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R2 is CO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及式I化合物：其中：R1是氢原子，F，CN等; R2是CO，SO2等; R3是可被取代的苯基; X1，X2和X3各自独立地为CH，N等，但X1，X2和X3之间的氮数为0或1。 W是以下残基：其中：W1，W2和W3各自独立地为CH，N等，或其药学上可接受的盐或酯。

公开(公告)号：US08101621B2

公开(公告)日：2012-01-24

申请号：US12226639

申请日：2007-04-25

申请人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Keita Nagai ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

发明人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Keita Nagai ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

IPC分类号： C07D239/42 ,  C07D239/02 ,  C07D403/14

CPC分类号： C07D487/08

摘要： The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1′, (ii) either one of Ra2 and Ra2′, (iii) either one of Rb1 and Rb1′, and (iv) either one of Rb2 and Rb2′, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1′, Ra2, Ra2′, Rb1, Rb1′, Rb2 and Rb2′, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及通式I的化合物：其中：n1和n2相同或不同，为0或1; R是芳基，杂芳基等; Re为氢原子或低级烷基; 选自由（i）Ra1和Ra1'中的任一个组成的四组中的两个基团，（ii）Ra2和Ra2'中的任一个，（iii）Rb1和Rb1'中的任一个，以及（iv）Rb2和 Rb2'组合形成 - （CH 2）n - ，其中n为1,2或3; 在Ra1，Ra1'，Ra2，Ra2'，Rb1，Rb1'，Rb2和Rb2'之间，不形成 - （CH2）n-的基团各自独立地为氢原子等; X1，X2，X3和X4各自独立地为CH，N等; Y1，Y2，Y3和Y4相同或不同，为CH或N等; W是5元芳杂环基或其药学上可接受的盐或酯。

公开(公告)号：US20090192174A1

公开(公告)日：2009-07-30

申请号：US12226639

申请日：2007-04-25

申请人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Keita Nagai ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

发明人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Keita Nagai ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

IPC分类号： A61K31/506 ,  C07D487/04

CPC分类号： C07D487/08

摘要： The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of Ra1 and Ra1′, (ii) either one of Ra2 and Ra2′, (iii) either one of Rb1 and Rb1′, and (iv) either one of Rb2 and Rb2′, are combined to form —(CH2)n— where n is 1, 2 or 3; and among Ra1, Ra1′, Ra2, Ra2′, Rb1, Rb1′, Rb2 and Rb2′, the groups which do not form —(CH2)n— are each independently hydrogen atom, etc.; X1, X2, X3 and X4 are each independently CH, N, etc.; Y1, Y2, Y3 and Y4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group, or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及通式I的化合物：其中：n1和n2相同或不同，为0或1; R是芳基，杂芳基等; Re为氢原子或低级烷基; 选自由（i）Ra1和Ra1'中的任一个组成的四组中的两个基团，（ii）Ra2和Ra2'中的任一个，（iii）Rb1和Rb1'中的任一个，以及（iv）Rb2和 Rb2'组合形成 - （CH 2）n - ，其中n为1,2或3; 在Ra1，Ra1'，Ra2，Ra2'，Rb1，Rb1'，Rb2和Rb2'之间，不形成 - （CH2）n-的基团各自独立地为氢原子等; X1，X2，X3和X4各自独立地为CH，N等; Y1，Y2，Y3和Y4相同或不同，为CH或N等; W是5元芳杂环基或其药学上可接受的盐或酯。

公开(公告)号：US08519136B2

公开(公告)日：2013-08-27

申请号：US12866955

申请日：2009-02-18

申请人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

发明人： Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Katsumasa Nonoshita ,  Mitsuru Ohkubo

IPC分类号： C07D413/14 ,  C07D401/14 ,  A61K31/4525 ,  A61K31/454

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D413/14

摘要： The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R2 is CO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及式I化合物：其中：R1是氢原子，F，CN等; R2是CO，SO2等; R3是可被取代的苯基; X1，X2和X3各自独立地为CH，N等，但X1，X2和X3之间的氮数为0或1。 W是以下残基：其中：W1，W2和W3各自独立地为CH，N等，或其药学上可接受的盐或酯。

公开(公告)号：US07491720B2

公开(公告)日：2009-02-17

申请号：US11258447

申请日：2005-10-25

申请人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

发明人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

IPC分类号： C07D241/00 ,  C07D241/02 ,  A01N43/58 ,  A61K31/50

CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D417/14

摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).

摘要翻译： 本发明涉及由通式（I）表示的化合物：其中m1和m2为1,2或3; n1和n2为0或1; 我是1到m1中任何一个的整数; j为1〜m2的整数， R是芳基，杂芳基或环烷基，其中任一个可以被取代; Rai和Rai'是氢原子等，Rbj和Rbj'是氢原子等; Rc，Rd和Re为氢原子等; X1是CH，CX1a或N; X2是CH，N等; X3是CH，N等; X4是CH或N; Y1，Y2和Y3各自独立地为CH或N; Z1和Z2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。

公开(公告)号：US20080027042A1

公开(公告)日：2008-01-31

申请号：US11666531

申请日：2005-10-25

申请人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

发明人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

IPC分类号： A61K31/496 ,  A61K31/425 ,  A61K31/497 ,  A61K31/5513 ,  C07D211/72 ,  C07D243/14 ,  C07D295/00 ,  C07D277/04 ,  C07D241/04 ,  A61P43/00 ,  A61K31/5355 ,  A61K31/44

CPC分类号： A61K38/21 ,  A61K31/282 ,  A61K31/337 ,  A61K31/407 ,  A61K31/4745 ,  A61K31/475 ,  A61K31/496 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  A61K31/52 ,  A61K31/675 ,  A61K31/704 ,  A61K31/7048 ,  A61K31/7068 ,  A61K31/7076 ,  A61K33/24 ,  A61K45/06 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  A61K2300/00

摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).

摘要翻译： 本发明涉及由通式（I）表示的化合物：其中m 1和m 2是1,2或3; n 1和n 2是0或1; i是1〜m1的任一个的整数; j为1〜m 2的整数; R是芳基，杂芳基或环烷基，其中任一个可以被取代; R a a和R a'是氢原子等，R bj和R b'是氢原子 等等 R c，R d和R e是氢原子等; X 1是CH，CX 1a，或N; X 2是CH，N等; X 3是CH，N等; X 4是CH或N; Y 1，Y 2和Y 3各自独立地为CH或N; Z 1和Z 2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。

公开(公告)号：US07834018B2

公开(公告)日：2010-11-16

申请号：US12315425

申请日：2008-12-03

申请人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

发明人： Mitsuru Ohkubo ,  Tetsuya Kato ,  Nobuhiko Kawanishi ,  Takashi Mita ,  Toshiyasu Shimomura

IPC分类号： A61K31/497 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D417/14

摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).

摘要翻译： 本发明涉及由通式（I）表示的化合物：其中m1和m2为1,2或3; n1和n2为0或1; 我是1到m1中任何一个的整数; j为1〜m2的整数， R是芳基，杂芳基或环烷基，其中任一个可以被取代; Rai和Rai'是氢原子等，Rbj和Rbj'是氢原子等; Rc，Rd和Re为氢原子等; X1是CH，CX1a或N; X2是CH，N等; X3是CH，N等; X4是CH或N; Y1，Y2和Y3各自独立地为CH或N; Z1和Z2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。