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1. 发明申请

WO2010133318A1 METHODS FOR THE IDENTIFICATION OF PHOSPHATIDYLINOSITOL KINASE INTERACTING MOLECULES AND FOR THE PURIFICATION OF PHOSPHATIDYLINOSITOL KINASE PROTEINS 审中-公开
标题翻译：磷脂酰肌氨酸激酶相互作用分子鉴定方法和磷脂酰肌氨酸激酶蛋白的纯化方法
公开(公告)号：WO2010133318A1
公开(公告)日：2010-11-25
申请号：PCT/EP2010/002987
申请日：2010-05-14
申请人： CELLZOME AG , BELL, Kathryn , RAMSDEN, Nigel , BERGAMINI, Giovanna , NEUBAUER, Gitte
发明人： BELL, Kathryn , RAMSDEN, Nigel , BERGAMINI, Giovanna , NEUBAUER, Gitte
IPC分类号： C07D471/04 , C12N11/06 , C12Q1/48
CPC分类号： C07D471/04 , B01J20/3212 , B01J20/3255 , C12N9/1205 , C12N11/06 , C12Q1/485 , G01N2500/02
摘要： The present invention relates to immobilization compounds of formula (I), immobilization products and preparations thereof as well as methods and uses for the identification of phosphatidylinositol kinase interacting compounds or for the purification or identification of phosphatidylinositol kinase proteins.
摘要翻译：本发明涉及式（I）的固定化合物，其固定产物及其制备方法以及用于鉴定磷脂酰肌醇激酶相互作用化合物或用于纯化或鉴定磷脂酰肌醇激酶蛋白的方法和用途。

2. 发明申请

WO2009068482A1 AMINO TRIAZOLES AS PI3K INHIBITORS 审中-公开
标题翻译： AMINO TRIAZOLES作为PI3K抑制剂
公开(公告)号：WO2009068482A1
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066001
申请日：2008-11-21
申请人： Cellzome Limited , RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , NEUBAUER, Gitte
发明人： RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , NEUBAUER, Gitte
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) Said compounds are useful as protein kinase inhibitors, especially inhibitors of P13K, 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）化合物。所述化合物可用作蛋白激酶抑制剂，特别是P13K抑制剂，用于治疗或预防免疫学，炎症，自身免疫性或过敏性疾病。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制备和用作药物。

3. 发明申请

WO2008015013A1 METHODS FOR THE IDENTIFICATION OF PI3K INTERACTING MOLECULES AND FOR THE PURIFICATION OF PI3K 审中-公开
标题翻译： PI3K相互作用分子鉴定方法和PI3K纯化方法
公开(公告)号：WO2008015013A1
公开(公告)日：2008-02-07
申请号：PCT/EP2007/006887
申请日：2007-08-03
申请人： CELLZOME AG , BERGAMINI MOORE, Giovanna , CANSFIELD, Andrew , RAMSDEN, Nigel , NEUBAUER, Gitte
发明人： BERGAMINI MOORE, Giovanna , CANSFIELD, Andrew , RAMSDEN, Nigel , NEUBAUER, Gitte
IPC分类号： G01N33/573 , C12Q1/48
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 PI3 K 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 realtes 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).
摘要翻译：本发明涉及一种鉴定PI3K相互作用化合物的方法，包括以下步骤：a）提供含有PI3K的蛋白质制剂，b）使蛋白制备物与固定在固相载体上的苯基噻唑配体1接触，苯基噻唑配体1-PI3K复合物，c）将苯基噻唑配体1-PI3K复合物与给定化合物一起孵育，以及d）测定该化合物是否能够从固定的苯基噻唑配体1分离PI3K。此外，本发明涉及用于鉴定PI3K相互作用化合物的方法，包括以下步骤：a）提供含有PI3K的蛋白质制剂，b）使所述蛋白质制剂与固定在固体支持物上的苯基噻唑配体1和给定化合物在允许形成苯基噻唑配体1-PI3K复合物，和c）检测苯基噻唑配体1-PI3K互补 x在步骤b）中形成。此外，本发明涉及用于鉴定PI3K相互作用化合物的方法，包括以下步骤：a）提供含有PI3K的蛋白质制剂的两个等分试样，b）使一个等分试样与固定在固体支持物上的苯基噻唑配体1接触在允许形成苯基噻唑配体1-PI3K复合物的条件下，c）使其他等分试样与固定在固体载体上的苯基噻唑配体1和允许形成苯基噻唑配体1-PI3K复合物的条件下与给定化合物接触，以及 d）测定步骤b）和c）中形成的苯基噻唑配体1-PI3K复合物的量。此外，本发明涉及用于鉴定PI3K相互作用化合物的方法，其包括以下步骤：a）提供两个等分试样，其包含每个至少一个含有PI3K的细胞，b）将一个等分试样与给定化合物一起孵育，c）每个等分试样的细胞，d）裂解细胞以获得蛋白质制剂，e）在允许形成苯基噻唑配体1-PI3K复合物的条件下，使蛋白质制剂与固定在固体支持物上的苯基噻唑配体1接触，以及f）测定在步骤e）中在每个等分试样中形成的苯基噻唑配体1-PI3K复合物的量。

4. 发明申请

WO2013041407A1 HYDROXAMIC ACIDS AS HDAC6 INHIBITORS 审中-公开
标题翻译：羟基酸作为HDAC6抑制剂
公开(公告)号：WO2013041407A1
公开(公告)日：2013-03-28
申请号：PCT/EP2012/067721
申请日：2012-09-11
申请人： CELLZOME AG , CELLZOME LIMITED , RAMSDEN, Nigel , BELL, Kathryn
发明人： RAMSDEN, Nigel , BELL, Kathryn
IPC分类号： A61K31/166 , C07D209/18 , C07D215/14 , A61P37/00
CPC分类号： A61K31/166 , C07C259/06 , C07C311/08 , C07C311/13 , C07C311/17 , C07D209/08 , C07D209/18 , C07D217/04
摘要： A hydroxamic acid of formula (I) or a pharmaceutically acceptable salt thereof for use in a method for treating or preventing an immunological, inflammatory, autoimmune or allergic disorder or disease, or a transplant rejection, or a graft-versus host disease, or a neurogenerative disease, or neuron injury, where the symbols in formula (I) have the following meanings: X is aryl, heteroaryl, cycloalkyl or heterocyclyl, any of which is unsubstituted or substituted, or H; L is C 1 -C 14 saturated alkylene or C 2 -C 8 -alkenylene, wherein the alkylene or alkenylene is unsubstituted or substituted, wherein one or two of the carbon atoms of the alkylene or alkenylene is replaced by NR', R' being hydrogen, alkyl, acyl, hydrogen, arylalkyl or, together with R, is (C 1 -C 3 )-alkylene, and wherein one or two of the carbon atoms of the alkylene or alkenylene is optionally replaced with O, S, S(O), S(O)2 or C(O); and R is H or, together with R', (C 1 -C 3 )-alkylene.
摘要翻译：用于治疗或预防免疫，炎症，自身免疫或过敏性疾病或疾病或移植排斥或移植物抗宿主病的方法中的式（I）的异羟肟酸或其药学上可接受的盐，或神经元损伤，其中式（I）中的符号具有以下含义：X是芳基，杂芳基，环烷基或杂环基，其中任何一个是未取代或取代的，或H; L是C1-C14饱和亚烷基或C2-C8-亚烯基，其中亚烷基或亚烯基是未取代或取代的，其中亚烷基或亚烯基的一个或两个碳原子被NR'取代，R'是氢，烷基，酰基，氢，芳基烷基或与R一起为（C 1 -C 3） - 亚烷基，并且其中亚烷基或亚烯基的一个或两个碳原子任选被O，S，S（O），S（O ）2或C（O）; 并且R是H或与R'，（C 1 -C 3） - 亚烷基一起。

5. 发明申请

WO2010007100A1 7-SUBSTITUTED AMINO TRIAZOLES AS PI3K INHIBITORS 审中-公开
标题翻译： 7-取代的氨基三唑作为PI3K抑制剂
公开(公告)号：WO2010007100A1
公开(公告)日：2010-01-21
申请号：PCT/EP2009/059076
申请日：2009-07-15
申请人： CELLZOME LTD , RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
发明人： RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein T 1 and R 1 to R 3 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）化合物，其中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制备和用作药物。

6. 发明申请

WO2010007099A1 2-AMINOIMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的2-氨基咪唑并[1,2-B]吡啶衍生物
公开(公告)号：WO2010007099A1
公开(公告)日：2010-01-21
申请号：PCT/EP2009/059075
申请日：2009-07-15
申请人： CELLZOME LIMITED , RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David
发明人： RAMSDEN, Nigel , BELL, Kathryn , CANSFIELD, Andrew , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David
IPC分类号： A61P35/00 , A61P29/00 , A61P37/00 , A61P9/00 , A61K31/5025 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of formula (I) wherein T 1 and R 1 to R 3 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）化合物，其中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制备和用作药物。

7. 发明申请

WO2012022681A2 HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS SELECTIVE JAK INHIBITORS 审中-公开
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：WO2012022681A2
公开(公告)日：2012-02-23
申请号：PCT/EP2011/063905
申请日：2011-08-12
申请人： CELLZOME LIMITED , BELL, Kathryn , PITON, Nelly , DAGOSTIN, Claudio , BOUSSARD, Cyrille , RATCLIFFE, Andrew , RAMSDEN, Nigel
发明人： BELL, Kathryn , PITON, Nelly , DAGOSTIN, Claudio , BOUSSARD, Cyrille , RATCLIFFE, Andrew , RAMSDEN, Nigel
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 X 1 to X 5 , Y, Z 1 to Z 3 , 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。

8. 发明申请

WO2011048082A1 HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS 审中-公开
标题翻译：作为JAK抑制剂的异喹啉基吡嗪类似物
公开(公告)号：WO2011048082A1
公开(公告)日：2011-04-28
申请号：PCT/EP2010/065700
申请日：2010-10-19
申请人： CELLZOME LIMITED , RAMSDEN, Nigel , HARRISON, Richard John , OXENFORD, Sally , BELL, Kathryn , PITON, Nelly , DAGOSTIN, Claudio , BOUSSARD, Cyrille , RATCLIFFE, Andrew
发明人： RAMSDEN, Nigel , HARRISON, Richard John , OXENFORD, Sally , BELL, Kathryn , PITON, Nelly , DAGOSTIN, Claudio , BOUSSARD, Cyrille , RATCLIFFE, Andrew
IPC分类号： C07D487/04 , A61K31/505 , A61P35/00 , A61P37/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I) wherein X 1 to X 5 , Y, Z 1 to Z 3 , 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：本发明涉及式（I）化合物，其中X 1至X 5，Y，Z 1至Z 3和R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JAK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

WO2010092015A1 UREA TRIAZOLOLO [1, 5-A] PYRIDINE DERIVATIVES AS PI3K INHIBITORS 审中-公开
标题翻译：尿素三唑醇[1,5-A]吡啶衍生物作为PI3K抑制剂
公开(公告)号：WO2010092015A1
公开(公告)日：2010-08-19
申请号：PCT/EP2010/051462
申请日：2010-02-08
申请人： CELLZOME LIMITED , RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
发明人： RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P9/00 , A61P35/00 , A61P31/00 , A61P25/00
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I) wherein X 1 ,R and R 1 to R 4 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）化合物，其中X 1，R 2和R 1至R 4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制备和用作药物。

10. 发明申请

WO2010057877A1 7-PYRIDINYL- OR PHENYL- SUBSTITUTED TRIAZOLO [1, 5 -A] PYRIDINES AS PI3K INHIBITORS 审中-公开
标题翻译：作为PI3K抑制剂的7-吡啶基或苯基取代的三唑并[1,5-A]吡啶
公开(公告)号：WO2010057877A1
公开(公告)日：2010-05-27
申请号：PCT/EP2009/065292
申请日：2009-11-17
申请人： CELLZOME LIMITED , RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
发明人： RAMSDEN, Nigel , BELL, Kathryn , TAYLOR, Jess , SUNOSE, Mihiro , MIDDLEMISS, David , ELLARD, Katie
IPC分类号： C07D471/04 , A61P37/08 , A61P35/00 , A61P3/00 , A61P29/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I), wherein X, X 1 , R and R 1 to R 4 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）化合物，其中X，X1，R和R1至R4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制备和用作药物。

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