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。

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：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：US07417053B2

公开(公告)日：2008-08-26

申请号：US11399484

申请日：2006-04-07

申请人： Gen Unoki ,  Yoshiyuki Matsumoto ,  Yohei Matsueda ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi ,  Motoko Hamada

发明人： Gen Unoki ,  Yoshiyuki Matsumoto ,  Yohei Matsueda ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi ,  Motoko Hamada

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02

CPC分类号： C07D471/04

摘要： A pyrazolo[1,5-a]pyridine derivative represented by formula (I) and salt thereof exhibit excellent MAPKAP-K2 inhibitory activity. Accordingly, medicines comprising this compound as an active ingredient are expected to be valuable for treating or preventing diseases mediated by MAPKAP-K2 such as inflammatory injury, autoimmune diseases, asteropathia destruens, cancer and/or growth of tumor.

摘要翻译： 由式（I）表示的吡唑并[1,5-a]吡啶衍生物及其盐表现出优异的MAPKAP-K2抑制活性。 因此，预期包含该化合物作为活性成分的药物对于治疗或预防由MAPKAP-K2介导的疾病如炎性损伤，自身免疫性疾病，死亡性星状病毒，癌症和/或肿瘤生长是有价值的。

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：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：US20070072898A1

公开(公告)日：2007-03-29

申请号：US11399484

申请日：2006-04-07

申请人： Gen Unoki ,  Yoshiyuki Matsumoto ,  Yohei Matsueda ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi ,  Motoko Hamada

发明人： Gen Unoki ,  Yoshiyuki Matsumoto ,  Yohei Matsueda ,  Tomomi Kosugi ,  Mika Takakuwa ,  Hiroaki Makino ,  Kenichiro Kataoka ,  Yuko Yamakoshi ,  Motoko Hamada

IPC分类号： A61K31/4745 ,  C07D471/02

CPC分类号： C07D471/04

摘要： A pyrazolo[1,5-a]pyridine derivative represented by formula (I) and salt thereof exhibit excellent MAPKAP-K2 inhibitory activity. Accordingly, medicines comprising this compound as an active ingredient are expected to be valuable for treating or preventing diseases mediated by MAPKAP-K2 such as inflammatory injury, autoimmune diseases, asteropathia destruens, cancer and/or growth of tumor.

摘要翻译： 由式（I）表示的吡唑并[1,5-a]吡啶衍生物及其盐表现出优异的MAPKAP-K2抑制活性。 因此，预期包含该化合物作为活性成分的药物对于治疗或预防由MAPKAP-K2介导的疾病如炎性损伤，自身免疫性疾病，死亡性星状病毒，癌症和/或肿瘤生长是有价值的。

公开(公告)号：US09976766B2

公开(公告)日：2018-05-22

申请号：US14391761

申请日：2012-04-26

申请人： Kosuke Tanaka ,  Hiroaki Makino ,  Akinori Sakabe ,  Tadashi Ariyama

发明人： Kosuke Tanaka ,  Hiroaki Makino ,  Akinori Sakabe ,  Tadashi Ariyama

IPC分类号： F24F11/00 ,  F25B49/02 ,  G05B15/02 ,  F25B13/00

CPC分类号： F24F11/30 ,  F24F11/62 ,  F24F11/70 ,  F24F11/83 ,  F24F11/84 ,  F25B13/00 ,  F25B49/02 ,  F25B2313/0314 ,  F25B2600/01 ,  F25B2600/2513 ,  F25B2700/2104 ,  F25B2700/21151 ,  F25B2700/21152 ,  G05B15/02

摘要： An air-conditioning apparatus includes a time constant calculation unit that estimates a response time constant at a time when an opening degree of an expansion device is changed on the basis of specifications of a compressor that forms a refrigeration cycle of the air-conditioning apparatus, specifications of a load side heat exchanger, and an operating state quantity of the air-conditioning apparatus, a control constant calculation means that calculates at least one of a control gain of the opening degree of the expansion device and a control interval on the basis of a calculation result of the time constant calculation means, and a control constant change means that changes a control constant.

公开(公告)号：US20150052922A1

公开(公告)日：2015-02-26

申请号：US14391761

申请日：2012-04-26

申请人： Kosuke Tanaka ,  Hiroaki Makino ,  Akinori Sakabe ,  Tadashi Ariyama

发明人： Kosuke Tanaka ,  Hiroaki Makino ,  Akinori Sakabe ,  Tadashi Ariyama

IPC分类号： F24F11/00

CPC分类号： F24F11/30 ,  F24F11/62 ,  F24F11/70 ,  F24F11/83 ,  F24F11/84 ,  F25B13/00 ,  F25B49/02 ,  F25B2313/0314 ,  F25B2600/01 ,  F25B2600/2513 ,  F25B2700/2104 ,  F25B2700/21151 ,  F25B2700/21152 ,  G05B15/02

摘要： An air-conditioning apparatus includes a time constant calculation unit that estimates a response time constant at a time when an opening degree of an expansion device is changed on the basis of specifications of a compressor that forms a refrigeration cycle of the air-conditioning apparatus, specifications of a load side heat exchanger, and an operating state quantity of the air-conditioning apparatus, a control constant calculation means that calculates at least one of a control gain of the opening degree of the expansion device and a control interval on the basis of a calculation result of the time constant calculation means, and a control constant change means that changes a control constant.

摘要翻译： 一种空调装置，包括时间常数计算单元，其基于形成空调装置的制冷循环的压缩机的规格，来估计膨胀装置的开度变化时的响应时间常数， 负载侧热交换器的规格以及空气调节装置的运转状态量，控制常数计算单元，其基于以下方式计算扩张装置的开度的控制增益和控制间隔中的至少一个： 时间常数计算装置的计算结果和改变控制常数的控制常数改变装置。