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：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：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：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：US20070191344A1

公开(公告)日：2007-08-16

申请号：US10572043

申请日：2004-09-15

申请人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltan Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Muller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

发明人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltan Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Muller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

IPC分类号： A61K31/55 ,  A61K31/506 ,  C07D403/02

CPC分类号： C04B35/632 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, and pharmaceutical compositions containing at least one of said 4,6-di substituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said 4,6-disubstituted aminopyrimidine derivatives as inhibitors for a protein kinase and a medium comprising at least one of said 4,6-disubstituted aminopyrimidine derivatives in an immobilized form and the use of said medium for enriching, purifying and/or depleting nucleotide binding proteins which bind to the immobilized 4,6-disubstituted aminopyrimidine derivatives.

摘要翻译： 本发明涉及4,6-二取代的氨基嘧啶衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，朊病毒疾病，免疫学 疾病，自身免疫疾病，双相和临床疾病，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病和中风，以及含有所述4,6-二取代氨基嘧啶衍生物和 /或其药学上可接受的盐。 此外，本发明涉及所述4,6-二取代氨基嘧啶衍生物作为蛋白激酶的抑制剂和包含至少一种固定化形式的所述4,6-二取代氨基嘧啶衍生物的介质和使用所述培养基 用于富集，纯化和/或消除与固定的4,6-二取代氨基嘧啶衍生物结合的核苷酸结合蛋白。

公开(公告)号：US08084457B2

公开(公告)日：2011-12-27

申请号：US10572043

申请日：2004-09-15

申请人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltán Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Müller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

发明人： Axel Choidas ,  Alexander Backes ,  Matt Cotten ,  Ola Engkvist ,  Beatrice Felber ,  Achim Freisleben ,  Klaus Godl ,  Zoltán Greff ,  Peter Habenberger ,  Doris Hafenbradl ,  Christian Hartung ,  Thomas Herget ,  Edmund Hoppe ,  Bert Klebl ,  Andrea Missio ,  Gerhard Müller ,  Wilfried Schwab ,  Birgit Zech ,  Jose Bravo ,  John Harris ,  Joelle Le ,  Jackie Macritchie ,  Vladimir Savic ,  Brad Sherborne ,  Don Simpson

IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04 ,  C07D239/00 ,  C07D239/02

CPC分类号： C04B35/632 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, and pharmaceutical compositions containing at least one of said 4,6-di substituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said 4,6-disubstituted aminopyrimidine derivatives as inhibitors for a protein kinase and a medium comprising at least one of said 4,6-disubstituted aminopyrimidine derivatives in an immobilized form and the use of said medium for enriching, purifying and/or depleting nucleotide binding proteins which bind to the immobilized 4,6-disubstituted aminopyrimidine derivatives.

摘要翻译： 本发明涉及4,6-二取代的氨基嘧啶衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，朊病毒疾病，免疫学 疾病，自身免疫疾病，双相和临床疾病，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病和中风，以及含有所述4,6-二取代氨基嘧啶衍生物和 /或其药学上可接受的盐。 此外，本发明涉及所述4,6-二取代氨基嘧啶衍生物作为蛋白激酶的抑制剂和包含至少一种固定化形式的所述4,6-二取代氨基嘧啶衍生物的介质和使用所述培养基 用于富集，纯化和/或消除与固定的4,6-二取代氨基嘧啶衍生物结合的核苷酸结合蛋白。

公开(公告)号：US08586590B2

公开(公告)日：2013-11-19

申请号：US13633320

申请日：2012-10-02

申请人： Julie Nicole Hamblin ,  Paul Spencer Jones ,  Suzanne Elaine Keeling ,  Joelle Le ,  Nigel James Parr

发明人： Julie Nicole Hamblin ,  Paul Spencer Jones ,  Suzanne Elaine Keeling ,  Joelle Le ,  Nigel James Parr

IPC分类号： A61K31/497 ,  C07D413/14

CPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/497 ,  A61K31/535 ,  A61K45/06 ,  C07B2200/13 ,  C07D413/14 ,  Y02A50/409

摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

摘要翻译： 本发明涉及某些新化合物。 具体地，本发明涉及式（I）的化合物及其盐。 本发明的化合物是激酶活性的抑制剂，特别是PI3-激酶活性。

公开(公告)号：US20130203772A1

公开(公告)日：2013-08-08

申请号：US13879667

申请日：2011-10-25

申请人： Julie Nicole Hamblin ,  Paul Spencer Jones ,  Suzanne Elaine Keeling ,  Joelle Le ,  Nigel James Parr ,  Robert David Willacy

发明人： Julie Nicole Hamblin ,  Paul Spencer Jones ,  Suzanne Elaine Keeling ,  Joelle Le ,  Nigel James Parr ,  Robert David Willacy

IPC分类号： C07D413/14

CPC分类号： C07D413/14

摘要： The present invention is directed to a polymorph of a compound and salts of a compound and polymorphs thereof, which compound is an inhibitor of kinase activity.

摘要翻译： 本发明涉及一种化合物和化合物的盐及其多晶型物的多晶型物，该化合物是激酶活性的抑制剂。

公开(公告)号：US08163743B2

公开(公告)日：2012-04-24

申请号：US12994246

申请日：2009-06-03

申请人： Ian Robert Baldwin ,  Kenneth David Down ,  Paul Faulder ,  Simon Gaines ,  Julie Nicole Hamblin ,  Katherine Louise Jones ,  Joelle Le ,  Christopher James Lunniss ,  Nigel James Parr ,  Timothy John Ritchie ,  Christian Alan Paul Smethurst ,  Yoshiaki Washio

发明人： Ian Robert Baldwin ,  Kenneth David Down ,  Paul Faulder ,  Simon Gaines ,  Julie Nicole Hamblin ,  Katherine Louise Jones ,  Joelle Le ,  Christopher James Lunniss ,  Nigel James Parr ,  Timothy John Ritchie ,  Christian Alan Paul Smethurst ,  Yoshiaki Washio

IPC分类号： C07D231/56 ,  C07D401/04 ,  A61K31/416 ,  A61K31/4439 ,  A61P11/00

CPC分类号： C07D231/56

摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.

摘要翻译： 本发明涉及某些新化合物。 具体地，本发明涉及式（I）的化合物及其盐。 本发明的化合物是P13-激酶活性的抑制剂。

公开(公告)号：US08993576B2

公开(公告)日：2015-03-31

申请号：US13879667

申请日：2011-10-25

申请人： Julie Nicole Hamblin ,  Paul Spencer Jones ,  Suzanne Elaine Keeling ,  Joelle Le ,  Nigel James Parr ,  Robert David Willacy

发明人： Julie Nicole Hamblin ,  Paul Spencer Jones ,  Suzanne Elaine Keeling ,  Joelle Le ,  Nigel James Parr ,  Robert David Willacy

IPC分类号： A61K31/496 ,  C07D413/14

CPC分类号： C07D413/14

摘要： The present invention is directed to a polymorph of a compound and salts of a compound and polymorphs thereof, which compound is an inhibitor of kinase activity.

摘要翻译： 本发明涉及一种化合物和化合物的盐及其多晶型物的多晶型物，该化合物是激酶活性的抑制剂。