公开(公告)号：US09662333B2

公开(公告)日：2017-05-30

申请号：US15023894

申请日：2015-05-28

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Kazuhisa Minamiguchi ,  Shigeo Okajima ,  Shinichi Aoki ,  Masanori Asai ,  Takahiro Asai ,  Hiroyoshi Yamanaka ,  Suguru Dohi

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/553 ,  A61P5/28 ,  A61K9/00 ,  A61K31/53

CPC分类号： A61K31/519 ,  A61K9/0019 ,  A61K31/53 ,  A61K31/553 ,  C07D471/04

摘要： A tetrahydropyridopyrimidine compound represented by formula (I) or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition including the tetrahydropyridopyrimidine compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier:

公开(公告)号：US09889136B2

公开(公告)日：2018-02-13

申请号：US15203059

申请日：2016-07-06

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Kazuhisa Minamiguchi ,  Shigeo Okajima ,  Shinichi Aoki ,  Masanori Asai ,  Takahiro Asai ,  Hiroyoshi Yamanaka ,  Suguru Dohi

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/553 ,  A61P5/28 ,  A61P35/00 ,  A61K9/00 ,  A61K31/53

CPC分类号： A61K31/519 ,  A61K9/0019 ,  A61K31/53 ,  A61K31/553 ,  C07D471/04

摘要： A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof

公开(公告)号：US09676773B2

公开(公告)日：2017-06-13

申请号：US15112070

申请日：2015-02-04

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Masayuki Nakamura ,  Hiroyoshi Yamanaka ,  Kazuaki Shibata ,  Morihiro Mitsuya ,  Takafumi Harada

IPC分类号： C07D401/14 ,  A61K31/437 ,  C07D471/04

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/695 ,  C07D471/04

摘要： Provided is a novel compound having a selective JAK3-inhibitory effect and also having excellent oral absorbability. Also provided is a pharmaceutical agent, which is based on a JAK3-inhibitory effect and is useful for preventing and/or treating a disease involving the JAK3, and in particular, rheumatoid arthritis or multiple sclerosis.An azaindole derivative having a cycloalkenyl group, which is represented by the following formula (I), or a salt thereof, and a pharmaceutical composition containing the same: where R1 to R4, m and n have the same meanings as those defined in the description.

公开(公告)号：US10421760B2

公开(公告)日：2019-09-24

申请号：US15746208

申请日：2016-07-29

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Masayuki Nakamura ,  Hiroyoshi Yamanaka ,  Morihiro Mitsuya ,  Takafumi Harada

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/00 ,  A61K47/32 ,  C07D207/30 ,  C07D307/34 ,  A61P29/00

摘要： Provided are a novel compound or a salt thereof, and a pharmaceutical composition comprising the same, which selectively and strongly inhibit JAK3, exhibit an excellent activity for suppressing the growth of human peripheral blood monocytes and an excellent oral absorbability, and exhibits an activity of inhibiting IL-2-induced IFN-γ production in vivo. A compound represented by formula (I) [wherein X represents —CH═CH—, —NH—, a sulfur atom or an oxygen atom; and n represents an integer of 0 to 2], or a salt thereof.

公开(公告)号：US10300067B2

公开(公告)日：2019-05-28

申请号：US15893804

申请日：2018-02-12

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Kazuhisa Minamiguchi ,  Shigeo Okajima ,  Shinichi Aoki ,  Masanori Asai ,  Takahiro Asai ,  Hiroyoshi Yamanaka ,  Suguru Dohi

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/553 ,  A61P5/28 ,  A61K9/00 ,  A61K31/53

摘要： A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof

公开(公告)号：US20160310496A1

公开(公告)日：2016-10-27

申请号：US15203059

申请日：2016-07-06

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Kazuhisa MINAMIGUCHI ,  Shigeo Okajima ,  Shinichi Aoki ,  Masanori Asai ,  Takahiro Asai ,  Hiroyoshi Yamanaka ,  Suguru Dohi

IPC分类号： A61K31/519 ,  A61K31/53 ,  A61K9/00 ,  A61K31/553

CPC分类号： A61K31/519 ,  A61K9/0019 ,  A61K31/53 ,  A61K31/553 ,  C07D471/04

摘要： A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof

公开(公告)号：US09782392B2

公开(公告)日：2017-10-10

申请号：US15404253

申请日：2017-01-12

申请人： TAIHO PHARMACEUTICAL CO., LTD.

发明人： Masayuki Nakamura ,  Hiroyoshi Yamanaka ,  Kazuaki Shibata ,  Morihiro Mitsuya ,  Takafumi Harada

IPC分类号： C07D401/14 ,  A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/695

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61K31/695 ,  C07D471/04

摘要： A method for treating rheumatoid arthritis, multiple sclerosis, or a disease involving JAK3, including administering a compound of the formula (I) or a salt thereof to a subject