公开(公告)号：US07473694B2

公开(公告)日：2009-01-06

申请号：US11377363

申请日：2006-03-17

申请人： Gen Unoki ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi

发明人： Gen Unoki ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： C07D471/14 ,  C07D487/14

摘要： A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth.

摘要翻译： 由式（1）表示的吡唑并嘧啶衍生物及其药学上可接受的盐对MAPKAP-K2具有优异的抑制活性。 因此，含有该化合物作为活性成分的药物预期对于治疗由MAPKAP-K2介导的疾病例如炎症性疾病，自身免疫疾病，破坏性骨病，癌症和/或肿瘤生长是有效的。

公开(公告)号：US20060189632A1

公开(公告)日：2006-08-24

申请号：US10547080

申请日：2004-03-01

申请人： Kenichiro Kataoka ,  Naotaka Suzuki ,  Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Aiko Fujino ,  Yasuhiro Oue ,  Yuko Yamakoshi ,  Satoshi Sugiura ,  Robert Mitchell ,  James Simpson ,  John Harris ,  Joelle Le

发明人： Kenichiro Kataoka ,  Naotaka Suzuki ,  Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Aiko Fujino ,  Yasuhiro Oue ,  Yuko Yamakoshi ,  Satoshi Sugiura ,  Robert Mitchell ,  James Simpson ,  John Harris ,  Joelle Le

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.

公开(公告)号：US06589984B1

公开(公告)日：2003-07-08

申请号：US09646005

申请日：2000-09-11

申请人： Yoshimitsu Naniwa ,  Hiroshi Imai ,  Tomohide Ida ,  Emiko Muratani ,  Kazuo Kitai ,  Yoshinori Sugimoto ,  Tomomi Kosugi ,  Akiko Takeuchi ,  Kunihito Watanabe ,  Takami Tomiyama ,  Tomio Takeuchi ,  Masa Hamada

发明人： Yoshimitsu Naniwa ,  Hiroshi Imai ,  Tomohide Ida ,  Emiko Muratani ,  Kazuo Kitai ,  Yoshinori Sugimoto ,  Tomomi Kosugi ,  Akiko Takeuchi ,  Kunihito Watanabe ,  Takami Tomiyama ,  Tomio Takeuchi ,  Masa Hamada

IPC分类号： C07D30932

CPC分类号： C07D405/14 ,  C07D407/04 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04

摘要： There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): wherein R1 represents a hydrogen atom or an alkyl group of 1 to 5 carbons; R2 represents hydrogen, —CO—R5 or —SO2R6; R3 represents hydrogen, an alkyl group of 1 to 5 carbons, etc.; and R4 is a substituent attached to the 4-carbon, 5-carbon, 6-carbon or 7 carbon of the benzofuran ring; and their salts. The compounds are useful as therapeutic agent for hypertriglyceridemia, lipid metabolism enhancers, or prophylactic and/or therapeutic agents for arteriosclerosis.

摘要翻译： 提供由以下结构式（I）表示的苯并呋喃基-α-吡喃酮衍生物：其中R1表示氢原子或1〜5个碳原子的烷基; R2表示氢，-CO-R5或-SO2R6; R3表示氢， 1〜5个碳原子的烷基等; 并且R 4是连接到苯并呋喃环的4-碳，5-碳，6-碳或7碳的取代基; 和它们的盐。 该化合物可用作高甘油三酯血症的治疗剂，脂质代谢增强剂，或用于动脉硬化的预防和/或治疗剂。

公开(公告)号：US07528140B2

公开(公告)日：2009-05-05

申请号：US10504583

申请日：2003-02-24

申请人： Kenichiro Kataoka ,  Tomomi Kosugi ,  Toshihiro Ishii ,  Takahiro Takeuchi ,  Takaharu Tsutsumi ,  Akira Nakano ,  Gen Unoki ,  Masanori Yamamoto ,  Yuri Sakai

发明人： Kenichiro Kataoka ,  Tomomi Kosugi ,  Toshihiro Ishii ,  Takahiro Takeuchi ,  Takaharu Tsutsumi ,  Akira Nakano ,  Gen Unoki ,  Masanori Yamamoto ,  Yuri Sakai

IPC分类号： C07D487/04 ,  C07D417/12 ,  C07D417/06 ,  C07D413/12 ,  C07D413/06 ,  C07D519/00 ,  A61K31/519 ,  A61K31/541 ,  A61K31/5355 ,  A61K31/497

CPC分类号： C07D487/04

摘要： The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and are therefore expected to be useful as therapeutic or prophylactic agents for conditions in which GSK-3 is implicated, such as diabetes, diabetes complications, Alzheimer's disease, neurodegenerative diseases, manic depression, traumatic encephalopathy, alopecia, inflammatory diseases, cancer and immune deficiency.

摘要翻译： 本发明提供由式（I）表示的吡咯并[3,2-d]嘧啶衍生物及其医学上可接受的盐。 本发明的化合物显示出GSK-3抑制活性，因此预期其可用作GSK-3涉及的病症的治疗或预防剂，例如糖尿病，糖尿病并发症，阿尔茨海默病，神经变性疾病，躁狂抑郁症，创伤性 脑病，脱发，炎性疾病，癌症和免疫缺陷。

公开(公告)号：US20070173519A1

公开(公告)日：2007-07-26

申请号：US11377363

申请日：2006-03-17

申请人： Gen Unoki ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi

发明人： Gen Unoki ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi

IPC分类号： A61K31/519 ,  C07D487/14

CPC分类号： C07D471/14 ,  C07D487/14

摘要： A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth.

摘要翻译： 由式（1）表示的吡唑并嘧啶衍生物及其药学上可接受的盐对MAPKAP-K2具有优异的抑制活性。 因此，含有该化合物作为活性成分的药物预期对于治疗由MAPKAP-K2介导的疾病例如炎症性疾病，自身免疫疾病，破坏性骨病，癌症和/或肿瘤生长是有效的。

公开(公告)号：US20060205743A1

公开(公告)日：2006-09-14

申请号：US10548668

申请日：2004-03-11

申请人： Kenichiro Kataoka ,  Tomomi Kosugi ,  Minoru Imai ,  Dale Mitchell ,  Donald Simpson ,  Naotaka Suzuki ,  Yuko Yamakoshi

发明人： Kenichiro Kataoka ,  Tomomi Kosugi ,  Minoru Imai ,  Dale Mitchell ,  Donald Simpson ,  Naotaka Suzuki ,  Yuko Yamakoshi

IPC分类号： A61K31/519

CPC分类号： C07D487/04 ,  A61K31/519

摘要： The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.

摘要翻译： 由式I表示的吡唑并[1,5-a]嘧啶衍生物及其药学上可接受的盐表现出优异的激酶抑制活性。 因此，包含化合物作为有效成分的药物预期可用作其中涉及激酶的蛋白激酶介导的病症的治疗或预防剂，例如炎性疾病，自身免疫疾病，破坏性骨病，癌症和/或肿瘤生长。

公开(公告)号：US20050171094A1

公开(公告)日：2005-08-04

申请号：US10505228

申请日：2003-02-24

申请人： Kenichiro Kataoka ,  Tomomi Kosugi ,  Toshihiro Ishii ,  Takahiro Takeuchi ,  Takaharu Tsutsumi ,  Akira Nakano ,  Yoji Yamamoto ,  Noboru Yoshioka

发明人： Kenichiro Kataoka ,  Tomomi Kosugi ,  Toshihiro Ishii ,  Takahiro Takeuchi ,  Takaharu Tsutsumi ,  Akira Nakano ,  Yoji Yamamoto ,  Noboru Yoshioka

IPC分类号： A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P15/00 ,  A61P17/14 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/14 ,  A61K31/551 ,  A61K31/519

CPC分类号： C07D487/14

摘要： A pyrrolo[3,2-d]pyrimidine derivative represented by the formula (I) or a pharamaceutically acceptable salt of the derivative. The derivative or salt is useful as a GSK-3 inhibitor.

摘要翻译： 由式（I）表示的吡咯并[3,2-d]嘧啶衍生物或衍生物的药学上可接受的盐。 衍生物或盐可用作GSK-3抑制剂。

公开(公告)号：US20060135514A1

公开(公告)日：2006-06-22

申请号：US11202035

申请日：2005-08-12

申请人： Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Kenichiro Kataoka ,  Dale Mitchell ,  Donald Simpson ,  Clifford Harris ,  Joelle Le ,  Yuko Yamakoshi

发明人： Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Kenichiro Kataoka ,  Dale Mitchell ,  Donald Simpson ,  Clifford Harris ,  Joelle Le ,  Yuko Yamakoshi

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for MAPKAP-K2 mediated disorder, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.

摘要翻译： 由式I表示的吡唑并[1,5-a]嘧啶衍生物及其药学上可接受的盐表现出优异的MAPKAP-K2抑制活性。 因此，包含化合物作为有效成分的药物预期可用作MAPKAP-K2介导的病症如炎性疾病，自身免疫性疾病，破坏性骨病，癌症和/或肿瘤生长的治疗或预防剂。

公开(公告)号：US07667036B2

公开(公告)日：2010-02-23

申请号：US11202035

申请日：2005-08-12

申请人： Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Kenichiro Kataoka ,  Dale Robert Mitchell ,  Donald James Simpson ,  Clifford John Harris ,  Joelle Le ,  Yuko Yamakoshi

发明人： Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Kenichiro Kataoka ,  Dale Robert Mitchell ,  Donald James Simpson ,  Clifford John Harris ,  Joelle Le ,  Yuko Yamakoshi

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04 ,  A61P25/28

CPC分类号： C07D487/04

摘要： The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for MAPKAP-K2 mediated disorder, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.

摘要翻译： 由式I表示的吡唑并[1,5-a]嘧啶衍生物及其药学上可接受的盐表现出优异的MAPKAP-K2抑制活性。 因此，包含化合物作为有效成分的药物预期可用作MAPKAP-K2介导的病症如炎性疾病，自身免疫性疾病，破坏性骨病，癌症和/或肿瘤生长的治疗或预防剂。

公开(公告)号：US07557110B2

公开(公告)日：2009-07-07

申请号：US10547080

申请日：2004-03-01

申请人： Kenichiro Kataoka ,  Naotaka Suzuki ,  Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Aiko Fujino ,  Yasuhiro Oue ,  Yuko Yamakoshi ,  Satoshi Sugiura ,  Robert Dale Mitchell ,  James Donald Simpson ,  John Clifford Harris ,  Joelle Le

发明人： Kenichiro Kataoka ,  Naotaka Suzuki ,  Tomomi Kosugi ,  Minoru Imai ,  Hiroaki Makino ,  Mika Takakuwa ,  Gen Unoki ,  Aiko Fujino ,  Yasuhiro Oue ,  Yuko Yamakoshi ,  Satoshi Sugiura ,  Robert Dale Mitchell ,  James Donald Simpson ,  John Clifford Harris ,  Joelle Le

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： C07D487/04

摘要： The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent kinase inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for a protein kinase mediated disorder in which kinase is implicated, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.

摘要翻译： 由式I表示的吡唑并[1,5-a]嘧啶衍生物及其药学上可接受的盐表现出优异的激酶抑制活性。 因此，包含化合物作为有效成分的药物预期可用作其中涉及激酶的蛋白激酶介导的病症的治疗或预防剂，例如炎性疾病，自身免疫疾病，破坏性骨病，癌症和/或肿瘤生长。