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1. 发明申请

US20100227800A1 TRIAZOLE DERIVATIVES AS KINASE INHIBITORS 有权
标题翻译：三唑衍生物作为激酶抑制剂
公开(公告)号：US20100227800A1
公开(公告)日：2010-09-09
申请号：US12438662
申请日：2007-08-30
申请人： Francis Wilson , Nigel Ramsden , Kathryn Bell , Andrew Cansfield , Svenja Burckhardt , Jess Taylor , Mihiro Sunose , David Middlemiss
发明人： Francis Wilson , Nigel Ramsden , Kathryn Bell , Andrew Cansfield , Svenja Burckhardt , Jess Taylor , Mihiro Sunose , David Middlemiss
IPC分类号： A61K38/13 , C07D471/04 , A61K31/437 , A61P11/02 , A61P3/10 , A61P17/06 , A61P37/06 , A61P29/00 , A61P19/02 , A61P1/04 , A61K31/506 , A61K31/56 , A61K31/436
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I); wherein X and R1 to R5 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）化合物; 其中X和R 1至R 5具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是Itk或PI3K的抑制剂，用于治疗或预防免疫学，炎症或过敏性疾病。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及生产和用作药物。

2. 发明授权

US08883820B2 Triazole derivatives as kinase inhibitors 有权
标题翻译：三唑衍生物作为激酶抑制剂
公开(公告)号：US08883820B2
公开(公告)日：2014-11-11
申请号：US12438662
申请日：2007-08-30
申请人： Francis Wilson , Nigel Ramsden , Kathryn Bell , Andrew Cansfield , Svenja Burckhardt , Jess Taylor , Mihiro Sunose , David Middlemiss
发明人： Francis Wilson , Nigel Ramsden , Kathryn Bell , Andrew Cansfield , Svenja Burckhardt , Jess Taylor , Mihiro Sunose , David Middlemiss
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I); wherein X and R1 to R5 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）化合物; 其中X和R 1至R 5具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是Itk或PI3K的抑制剂，用于治疗或预防免疫学，炎症或过敏性疾病。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及生产和用作药物。

3. 发明授权

US08865699B2 Amino triazoles as PI3K inhibitors 有权
标题翻译：氨基三唑作为PI3K抑制剂
公开(公告)号：US08865699B2
公开(公告)日：2014-10-21
申请号：US12744940
申请日：2008-11-21
申请人： Nigel Ramsden , Kathryn Bell , Andrew David Cansfield , Jess Taylor , Mihiro Sunose , David Middlemiss , Gitte Neubauer
发明人： Nigel Ramsden , Kathryn Bell , Andrew David Cansfield , Jess Taylor , Mihiro Sunose , David Middlemiss , Gitte Neubauer
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein X, T1 and R1 to R3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）的化合物，其中X，T1和R1至R3具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是用于治疗或预防免疫学，炎症，自身免疫或过敏性疾病的PI3K抑制剂。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及生产和用作药物。

4. 发明申请

US20110021497A1 AMINO TRIAZOLES AS PI3K INHIBITORS 有权
标题翻译： AMINO TRIAZOLES作为PI3K抑制剂
公开(公告)号：US20110021497A1
公开(公告)日：2011-01-27
申请号：US12744940
申请日：2008-11-21
申请人： Nigel Ramsden , Kathryn Bell , Andrew David Cansfield , Jess Taylor , Mihiro Sunose , David Middlemiss , Gitte Neubauer
发明人： Nigel Ramsden , Kathryn Bell , Andrew David Cansfield , Jess Taylor , Mihiro Sunose , David Middlemiss , Gitte Neubauer
IPC分类号： A61K31/437 , C07D471/04 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K31/506 , A61P37/00 , A61P29/00 , A61P37/08 , A61P37/06 , A61P1/18 , A61P17/00 , A61P17/06 , A61P19/02 , A61P1/00 , A61P3/10 , A61P11/06 , A61P35/00 , A61P25/28 , A61P9/00 , A61P3/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein X, T1 and R1 to R3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.
摘要翻译：本发明涉及式（I）的化合物，其中X，T1和R1至R3具有在说明书和权利要求书中引用的含义。所述化合物可用作蛋白激酶抑制剂，特别是用于治疗或预防免疫学，炎症，自身免疫或过敏性疾病的PI3K抑制剂。本发明还涉及药物组合物，包括所述化合物，这些化合物的制备以及生产和用作药物。

5. 发明申请

US20120142667A1 PYRIMIDINE DERIVATIVES AS ZAP-70 INHIBITORS 审中-公开
标题翻译：吡嗪衍生物作为ZAP-70抑制剂
公开(公告)号：US20120142667A1
公开(公告)日：2012-06-07
申请号：US13377550
申请日：2010-06-10
申请人： Nigel Ramsden , Jeremy Major , Adeline Morel , Mihiro Sunose , Nelly Piton
发明人： Nigel Ramsden , Jeremy Major , Adeline Morel , Mihiro Sunose , Nelly Piton
IPC分类号： A61K31/506 , C07D239/48 , A61P29/00 , C07D405/12 , A61P37/08 , A61P37/00 , A61K31/505 , C07D401/12
CPC分类号： C07D239/48
摘要： The invention relates to compounds of formula (I) wherein R1 to R5, X and X1 to X3 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 5，X和X 1至X 3具有如在说明书和权利要求书中引用的含义。所述化合物可用作ZAP-70的抑制剂，用于治疗或预防免疫学，炎性，自身免疫性，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

6. 发明申请

US20100055711A1 METHODS FOR THE IDENTIFICATION OF PI3K INTERACTING MOLECULES AND FOR THE PURIFICATION OF PI3K 失效
公开(公告)号：US20100055711A1
公开(公告)日：2010-03-04
申请号：US12375979
申请日：2007-08-03
申请人： Giovanna Bergamini Moore , Andrew Cansfield , Nigel Ramsden , Gitte Neubauer
发明人： Giovanna Bergamini Moore , Andrew Cansfield , Nigel Ramsden , Gitte Neubauer
IPC分类号： G01N33/53
CPC分类号： C12Q1/485 , G01N2500/02
摘要： The present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing a protein preparation containing PI3K, b) contacting the protein preparation with phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, c) incubating the phenylthiazole ligand 1-PI3K complex with a given compound, and d) determining whether the compound is able to separate PI3K from the immobilized phenylthiazole ligand 1. Furthermore, the present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing a protein preparation containing PI3K, b) contacting the protein preparation with phenylthiazole ligand 1 immobilized on a solid support and with a given compound under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, and c) detecting the phenylthiazole ligand 1-PI3K complex formed in step b). Furthermore, the present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing two aliquots of a protein preparation containing PI3K, b) contacting one aliquot with the phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, c) contacting the other aliquot with the phenylthiazole ligand 1 immobilized on a solid support and with a given compound under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, and d) determining the amount of the phenylthiazole ligand 1-PI3K complex formed in steps b) and c). Furthermore, the present invention relates to a method for the identification of a PI3K interacting compound, comprising the steps of a) providing two aliquots comprising each at least one cell containing PI3K, b) incubating one aliquot with a given compound, c) harvesting the cells of each aliquot, d) lysing the cells in order to obtain protein preparations, e) contacting the protein preparations with the phenylthiazole ligand 1 immobilized on a solid support under conditions allowing the formation of a phenylthiazole ligand 1-PI3K complex, and f) determining the amount of the phenylthiazole ligand 1-PI3K complex formed in each aliquot in step e).

7. 发明授权

US08153389B2 Methods for the identification of PI3K interacting molecules and for the purification of PI3K 失效
标题翻译：用于鉴定PI3K相互作用分子和纯化PI3K的方法
公开(公告)号：US08153389B2
公开(公告)日：2012-04-10
申请号：US12375979
申请日：2007-08-03
申请人： Giovanna Bergamini Moore , Andrew Cansfield , Nigel Ramsden , Gitte Neubauer
发明人： Giovanna Bergamini Moore , Andrew Cansfield , Nigel Ramsden , Gitte Neubauer
IPC分类号： C12Q1/48
CPC分类号： C12Q1/485 , G01N2500/02
摘要： The present invention relates to methods for the identification of a PI3K interacting compound using phenylthiazole ligand 1.
摘要翻译：本发明涉及使用苯基噻唑配体1鉴定PI3K相互作用化合物的方法。

8. 发明申请

US20110028405A1 SULFAMIDES AS ZAP-70 INHIBITORS 审中-公开
标题翻译： SULFAMIDES作为ZAP-70抑制剂
公开(公告)号：US20110028405A1
公开(公告)日：2011-02-03
申请号：US12809585
申请日：2008-12-17
申请人： Richard John Harrison , Jeremy Major , David Middlemiss , Nigel Ramsden , Ulrich Kruse , Gerard Drewes
发明人： Richard John Harrison , Jeremy Major , David Middlemiss , Nigel Ramsden , Ulrich Kruse , Gerard Drewes
IPC分类号： A61K31/505 , C07D239/48 , A61K31/56 , A61K38/13 , A61P37/00 , A61P29/00 , A61P37/08 , A61P37/06 , A61P11/06
CPC分类号： C07D239/48 , C07D403/14
摘要： The invention relates to compounds of formula (I) wherein X, R1, R2, R3, R8, R9 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中X，R 1，R 2，R 3，R 8，R 9具有在说明书和权利要求书中引用的含义。所述化合物可用作ZAP-70的抑制剂，用于治疗或预防免疫学，炎性，自身免疫性，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

9. 发明申请

US20110098288A1 SULFONAMIDES AS ZAP-70 INHIBITORS 审中-公开
标题翻译：磺酰胺作为ZAP-70抑制剂
公开(公告)号：US20110098288A1
公开(公告)日：2011-04-28
申请号：US12922163
申请日：2009-03-10
申请人： Jeremy Major , Richard John Harrison , Nigel Ramsden , David Middlemiss , Ulrich Kruse , Gerard Drewes
发明人： Jeremy Major , Richard John Harrison , Nigel Ramsden , David Middlemiss , Ulrich Kruse , Gerard Drewes
IPC分类号： A61K31/505 , C07D239/48 , C07D405/12 , C07D417/12 , C07D413/12 , C07D401/12 , C07D403/12 , A61K31/538 , A61K31/5377 , A61K31/506 , A61P37/00 , A61P29/00 , A61P37/08 , A61P19/02 , A61P25/00 , A61P17/06 , A61P1/00 , A61P1/04 , A61P11/06 , A61P11/00
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of formula (I) wherein R1 to R9 and R4a have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 9和R 4a具有在说明书和权利要求书中引用的含义。所述化合物可用作ZAP-70的抑制剂，用于治疗或预防免疫学，炎性，自身免疫性，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

10. 发明申请

US20130190292A1 HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS SELECTIVE JAK INHIBITORS 有权
标题翻译：作为选择性JAK抑制剂的杂环基亚氨基嘧啶类似物
公开(公告)号：US20130190292A1
公开(公告)日：2013-07-25
申请号：US13816555
申请日：2011-08-12
申请人： Kathryn Bell , Nelly Piton , Claudio Dagostin , Cyrille Boussard , Andrew Ratcliffe , Nigel Ramsden
发明人： Kathryn Bell , Nelly Piton , Claudio Dagostin , Cyrille Boussard , Andrew Ratcliffe , Nigel Ramsden
IPC分类号： C07D487/04 , C07D491/107 , C07D498/08
CPC分类号： C07D487/04 , A61K31/519 , C07D491/107 , C07D498/08 , C07D519/00
摘要： The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
摘要翻译：本发明涉及其中X1至X5，Y，Z1至Z3和R具有在说明书和权利要求书中引用的含义的式（I）化合物。所述化合物可用作JAK抑制剂，用于治疗或预防免疫学，炎症，自身免疫，过敏性疾病和免疫介导的疾病。本发明还涉及包含所述化合物的药物组合物，这些化合物的制备以及作为药物的用途。

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