公开(公告)号：WO2009148887A1

公开(公告)日：2009-12-10

申请号：PCT/US2009/045213

申请日：2009-05-27

Applicant: MERCK & CO., INC. ,  BANYU PHARMACEUTICAL CO., LTD. ,  FURUYAMA, Hidetomo ,  GOTO, Yasuhiro ,  KAWANISHI, Nobuhiko ,  LAYTON, Mark, E. ,  MITA, Takashi ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  ROSSI, Michael, A. ,  SAKAMOTO, Toshihiro ,  SANDERSON, Philip, E. ,  WANG, Jiabing

Inventor： FURUYAMA, Hidetomo ,  GOTO, Yasuhiro ,  KAWANISHI, Nobuhiko ,  LAYTON, Mark, E. ,  MITA, Takashi ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  ROSSI, Michael, A. ,  SAKAMOTO, Toshihiro ,  SANDERSON, Philip, E. ,  WANG, Jiabing

IPC: A01N43/90

CPC classification number: C07D471/14

Abstract: The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.

Abstract translation: 本发明提供了抑制Akt活性的取代的[1,2,4]三唑并[4,3-a] -1,5-二氮杂萘化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型，优选Akt1。 本发明还提供包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法，特别是Akt1。

公开(公告)号：WO0114376A8

公开(公告)日：2001-08-09

申请号：PCT/JP0005427

申请日：2000-08-11

Applicant: BANYU PHARMA CO LTD ,  FUKAMI TAKEHIRO ,  KANATANI AKIO ,  ISHIHARA AKANE ,  ISHII YASUYUKI ,  TAKAHASHI TOSHIYUKI ,  HAGA YUJI ,  SAKAMOTO TOSHIHIRO ,  ITOH TAKAHIRO

Inventor： FUKAMI TAKEHIRO ,  KANATANI AKIO ,  ISHIHARA AKANE ,  ISHII YASUYUKI ,  TAKAHASHI TOSHIYUKI ,  HAGA YUJI ,  SAKAMOTO TOSHIHIRO ,  ITOH TAKAHIRO

IPC: A61K20060101 ,  A61K31/438 ,  A61P20060101 ,  A61P9/00 ,  A61P25/00 ,  C07D20060101 ,  C07D213/61 ,  C07D307/94 ,  C07D405/12 ,  C07D471/10 ,  C07D491/10 ,  C07D491/107 ,  C07D519/00

CPC classification number: C07D405/12 ,  C07D213/61 ,  C07D307/94 ,  C07D471/10 ,  C07D491/10

Abstract: Compounds of formula (I) wherein T, U, V and W represent independently nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or nitrogen; Y represents optionally substituted imino or oxygen atom; and the like. Compounds of the present invention exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY.

Abstract translation: 其中T，U，V和W独立地表示氮原子或任选取代的次甲基的式（I）化合物，其中至少两个表示所述次甲基; X表示次甲基或氮; Y表示任选取代的亚氨基或氧原子; 等等。 本发明化合物表现出NPY拮抗活性，可用作治疗与NPY有关的各种疾病的药剂。

公开(公告)号：WO2009148916A1

公开(公告)日：2009-12-10

申请号：PCT/US2009/045456

申请日：2009-05-28

Applicant: MERCK & CO., INC. ,  BANYU PHARMACEUTICAL CO., LTD. ,  FURUYAMA, Hidetomo ,  GOTO, Yasuhiro ,  KAWANISHI, Nobuhiko ,  LAYTON, Mark, E. ,  MITA, Takashi ,  NAYA, Akira ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  RODZINAK, Kevin, J. ,  SAKAMOTO, Toshihiro ,  SANDERSON, Philip, E. ,  WANG, Jiabing

Inventor： FURUYAMA, Hidetomo ,  GOTO, Yasuhiro ,  KAWANISHI, Nobuhiko ,  LAYTON, Mark, E. ,  MITA, Takashi ,  NAYA, Akira ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  RODZINAK, Kevin, J. ,  SAKAMOTO, Toshihiro ,  SANDERSON, Philip, E. ,  WANG, Jiabing

IPC: A61K31/44 ,  A61K31/52

CPC classification number: C07D471/14

Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer.

Abstract translation: 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型，优选Akt1。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性，尤其是Akt1的方法。

公开(公告)号：WO2007126122A1

公开(公告)日：2007-11-08

申请号：PCT/JP2007/059408

申请日：2007-04-25

Applicant: Banyu Pharmaceutical Co., Ltd. ,  SAKAMOTO, Toshihiro ,  SUNAMI, Satoshi ,  YAMAMOTO, Fuyuki ,  NIIYAMA, Kenji ,  BAMBA, Makoto ,  TAKAHASHI, Keiji ,  FURUYAMA, Hidetomo ,  SAGARA, Takeshi ,  OTSUKI, Sachie ,  NISHIBATA, Toshihide ,  YOSHIZUMI, Takashi ,  HIRAI, Hiroshi

Inventor： SAKAMOTO, Toshihiro ,  SUNAMI, Satoshi ,  YAMAMOTO, Fuyuki ,  NIIYAMA, Kenji ,  BAMBA, Makoto ,  TAKAHASHI, Keiji ,  FURUYAMA, Hidetomo ,  SAGARA, Takeshi ,  OTSUKI, Sachie ,  NISHIBATA, Toshihide ,  YOSHIZUMI, Takashi ,  HIRAI, Hiroshi

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P43/00

CPC classification number: C07D487/04 ,  A61K31/4162 ,  A61K31/519

Abstract: The invention relates to compounds of a general formula (I): wherein A1 is selected from the following formula (aa1); R 1 is a lower alkenyl group or a lower alkynyl group; R 2 is a phenyl, pyridyl or thienyl group; R 5 and R 6 are a hydrogen atom, a lower alkyl group or a hydroxy-lower alkyl group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.

Abstract translation: 本发明涉及通式（I）的化合物：其中A1选自下式（aa1）; R 1是低级烯基或低级炔基; R 2是苯基，吡啶基或噻吩基; R 5和R 6是氢原子，低级烷基或羟基 - 低级烷基等。本发明的化合物具有优异的韦尔激酶抑制作用 因此在药物领域，特别是治疗各种癌症方面是有用的。

公开(公告)号：WO03076443A9

公开(公告)日：2005-01-20

申请号：PCT/JP0302611

申请日：2003-03-05

Applicant: BANYU PHARMA CO LTD ,  FUKAMI TAKEHIRO ,  KANATANI AKIO ,  ISHIHARA AKANE ,  ISHII YASUYUKI ,  TAKAHASHI TOSHIYUKI ,  HAGA YUJI ,  SAKAMOTO TOSHIHIRO ,  ITOH TAKAHIRO ,  CHIBA MASATO

Inventor： FUKAMI TAKEHIRO ,  KANATANI AKIO ,  ISHIHARA AKANE ,  ISHII YASUYUKI ,  TAKAHASHI TOSHIYUKI ,  HAGA YUJI ,  SAKAMOTO TOSHIHIRO ,  ITOH TAKAHIRO ,  CHIBA MASATO

IPC: C07D491/107 ,  A61K31/438 ,  A61P1/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P13/12 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P27/06 ,  A61P29/00 ,  A61P43/00 ,  C07D213/61 ,  C07D307/94 ,  C07D405/12 ,  C07D471/10 ,  C07D491/10 ,  C07D519/00

CPC classification number: C07D213/61 ,  C07D307/94 ,  C07D405/12 ,  C07D471/10 ,  C07D491/10

Abstract: A compound represented by the general formula (I): wherein Ar represents an aryl or heteroaryl which may be substituted, n represents 0 or 1: T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen, and a salt, ester or N-oxide derivative thereof exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like.

Abstract translation: 由通式（I）表示的化合物：其中Ar 1表示可被取代的芳基或杂芳基，n表示0或1：T，U，V和W各自独立地表示氮原子或次甲基， 可以具有选自卤素，低级烷基，羟基和低级烷氧基的取代基，其中至少两个表示所述次甲基; X表示次甲基，羟基取代的次甲基或氮原子; Y表示可被低级烷基或氧取代的亚氨基，其盐，酯或N-氧化物衍生物表现出NPY拮抗活性，可用作治疗与NPY有关的各种疾病的药剂，例如心血管疾病 如高血压，肾病，心脏病，血管痉挛，动脉硬化等。

公开(公告)号：WO2010104933A1

公开(公告)日：2010-09-16

申请号：PCT/US2010/026796

申请日：2010-03-10

Applicant: MERCK SHARP & DOHME CORP. ,  BANYU PHARMACEUTICAL CO., LTD. ,  FAN, Weiming ,  HAXELL, Thomas, F. N. ,  JENKS, Matthew, G. ,  KAWANISHI, Nobuhiko ,  LEE, Shuliang ,  LIU, Hao ,  MALASKA, Michael, J. ,  MOORE, Joseph, A., III ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  PANDI, Bharathi ,  PEEL, Michael, R. ,  SAKAMOTO, Toshihiro ,  SIU, Tony

Inventor： FAN, Weiming ,  HAXELL, Thomas, F. N. ,  JENKS, Matthew, G. ,  KAWANISHI, Nobuhiko ,  LEE, Shuliang ,  LIU, Hao ,  MALASKA, Michael, J. ,  MOORE, Joseph, A., III ,  OGINO, Yoshio ,  ONOZAKI, Yu ,  PANDI, Bharathi ,  PEEL, Michael, R. ,  SAKAMOTO, Toshihiro ,  SIU, Tony

IPC: C07D403/00 ,  C07D413/00

CPC classification number: C07D471/14 ,  C07D487/14 ,  C07D519/00

Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Abstract translation: 本发明提供抑制Akt活性的取代的稠合萘啶衍生物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

公开(公告)号：WO2010067886A1

公开(公告)日：2010-06-17

申请号：PCT/JP2009/070930

申请日：2009-12-09

Applicant: BANYU PHARMACEUTICAL CO.,LTD. ,  BAMBA, Makoto ,  FURUYAMA, Hidetomo ,  SAKAMOTO, Toshihiro ,  SUNAMI, Satoshi ,  TAKAHASHI, Keiji ,  YAMAMOTO, Fuyuki ,  YOSHIZUMI, Takashi

Inventor： BAMBA, Makoto ,  FURUYAMA, Hidetomo ,  SAKAMOTO, Toshihiro ,  SUNAMI, Satoshi ,  TAKAHASHI, Keiji ,  YAMAMOTO, Fuyuki ,  YOSHIZUMI, Takashi

IPC: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K41/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D519/00

CPC classification number: A61K31/519 ,  A61K31/5377 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention relates to a compound of General Formula (I) below, among others. In the Formula, Ar 1 is an optionally substituted aryl or heteroaryl group; R 1 is a hydrogen atom, an optionally substituted C1-C6 alkyl group, or an optionally substituted aryl, aralkyl, or heteroaryl group; R 2 is an optionally substituted aryl, aralkyl, or heteroaryl group; and R 3 is a hydrogen atom or a C1-C6 alkyl group. A compound of the present invention has an excellent Wee1 kinase inhibiting effect, and is therefore useful in the filed of medicine, particularly in various types of cancer therapy.

Abstract translation: 本发明涉及以下通式（I）的化合物等。 在式中，Ar 1是任选取代的芳基或杂芳基; R 1是氢原子，任选取代的C 1 -C 6烷基或任选取代的芳基，芳烷基或杂芳基; R2是任选取代的芳基，芳烷基或杂芳基; 并且R 3是氢原子或C 1 -C 6烷基。 本发明的化合物具有优异的Wee1激酶抑制作用，因此可用于医药领域，特别是在各种类型的癌症治疗中。

公开(公告)号：WO2008133866A1

公开(公告)日：2008-11-06

申请号：PCT/US2008/005155

申请日：2008-04-22

Applicant: MERCK & CO., INC. ,  BANYU PHARMACEUTICAL CO., LTD. ,  KAWASAKI, Masashi ,  MIZUNO, Hiroo ,  SAKAMOTO, Toshihiro ,  SUZUKI, Kimimasa ,  MCKEOWN, Arlene, E.

Inventor： KAWASAKI, Masashi ,  MIZUNO, Hiroo ,  SAKAMOTO, Toshihiro ,  SUZUKI, Kimimasa ,  MCKEOWN, Arlene, E.

IPC: C07D487/04 ,  A61P35/00 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: The present invention relates to the crystalline forms of 2-allyl-l -[6-(I -hydroxy- 1 methylethyl)pyridin-2-yl]-6-{[4-(4-methylpiperazin-l-yl)phenyl]amino}-l,2-dihydro-3H- pyrazolo[3,4-d]pyrirnidin-3-one or a salt thereof, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.

Abstract translation: 本发明涉及2-烯丙基-1- [6-（1-羟基-1-甲基乙基）吡啶-2-基] -6 - {[4-（4-甲基哌嗪-1-基）苯基] 氨基} -1,2-二氢-3H-吡唑并[3,4-d]嘧啶-3-酮或其盐，其可用于治疗作为激酶抑制剂的各种癌症的领域，特别是作为Weel激酶 抑制剂。

公开(公告)号：WO2003076443A1

公开(公告)日：2003-09-18

申请号：PCT/JP2003/002611

申请日：2003-03-05

Applicant: BANYU PHARMACEUTICAL CO., LTD. ,  FUKAMI, Takehiro ,  KANATANI, Akio ,  ISHIHARA, Akane ,  ISHII, Yasuyuki ,  TAKAHASHI, Toshiyuki ,  HAGA, Yuji ,  SAKAMOTO, Toshihiro ,  ITOH, Takahiro ,  CHIBA, Masato

Inventor： FUKAMI, Takehiro ,  KANATANI, Akio ,  ISHIHARA, Akane ,  ISHII, Yasuyuki ,  TAKAHASHI, Toshiyuki ,  HAGA, Yuji ,  SAKAMOTO, Toshihiro ,  ITOH, Takahiro ,  CHIBA, Masato

IPC: C07D491/10

CPC classification number: C07D213/61 ,  C07D307/94 ,  C07D405/12 ,  C07D471/10 ,  C07D491/10

Abstract: A compound represented by the general formula (I): wherein Ar 1 represents an aryl or heteroaryl which may be substituted, n represents 0 or 1: T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen, and a salt, ester or N-oxide derivative thereof exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis and the like.

Abstract translation: 由通式（I）表示的化合物：其中Ar1表示可被取代的n的芳基或杂芳基，表示0或1：T，U，V和W各自独立地表示可以具有取代基的氮原子或次甲基 选自卤素，低级烷基，羟基和低级烷氧基，其中至少两个表示所述次甲基; X表示次甲基，羟基取代的次甲基或氮原子; Y表示可以被低级烷基或氧取代的亚氨基，其盐，酯或N-氧化物衍生物表现出NPY拮抗活性，可用作治疗与NPY有关的各种疾病的药剂，例如心血管疾病 如高血压，肾病，心脏病，血管痉挛，动脉硬化等。