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1. 发明申请

WO2009042013A1 PROCESS FOR THE SYNTHESIS OF E1 ACTIVATING ENZYME INHIBITORS 审中-公开
标题翻译：合成E1活化酶抑制剂的方法
公开(公告)号：WO2009042013A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/009338
申请日：2008-08-01
申请人： MILLENNIUM PHARMACEUTICALS, INC. , ARMITAGE, Ian , ELLIOT, Eric, L. , LANGSTON, Marianne , LANGSTON, Steven, P. , MCCUBBIN, Quentin, J. , MIZUTANI, Hirotake , STIRLING, Matthew , ZHU, Lei
发明人： ARMITAGE, Ian , ELLIOT, Eric, L. , LANGSTON, Marianne , LANGSTON, Steven, P. , MCCUBBIN, Quentin, J. , MIZUTANI, Hirotake , STIRLING, Matthew , ZHU, Lei
IPC分类号： C07D487/04 , C07C215/44 , C07C217/52 , C07C219/24
CPC分类号： C07D487/04 , C07C215/44 , C07C217/52 , C07C219/24 , C07C315/04 , C07C317/50 , C07C2601/08 , C07D211/96 , C07D213/89 , C07D241/50 , C07D295/22 , C07D305/08 , C07D471/08 , Y02P20/55
摘要： The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2/3-d]pyrimidin-7- yl}cyclopentyl)methyl sulfamates, which are El activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with El activity.
摘要翻译：本发明提供合成4-取代的（（1S，2S，4R）-2-羟基-4- {7H-吡咯并[2,3-d]嘧啶-7-基}环戊基）甲基的方法和合成中间体氨基磺酸盐，其是E1活化酶抑制剂，并且可用于治疗细胞增殖，特别是癌症和与El活性相关的其它病症的病症。

2. 发明申请

WO2006046062A1 PROCESS FOR THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES 审中-公开
标题翻译：去除强化基底的方法
公开(公告)号：WO2006046062A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004179
申请日：2005-10-27
申请人： AVECIA PHARMACEUTICALS LIMITED , BLACKER, Andrew, John , STIRLING, Matthew, John
发明人： BLACKER, Andrew, John , STIRLING, Matthew, John
IPC分类号： C07B55/00 , C07B31/00 , C07C29/145
CPC分类号： C07B55/00 , C07B2200/07 , C07C29/00 , C07C33/22
摘要： There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group VI heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or disatereomer in the product composition being greater than the ratio of second to first enantiomer or disatereomer in the enantiomerically enriched composition. Preferred substrates include compounds of Formula (1) wherein: X represents O, S; R 1 , R 2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R 1 & R 2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R 1 and R 2 are selected such that * is a chiral centre. In a preferred process a compound of Formula : (2) wherein: X represents O, S; R 1 , R 2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R 1 & R 2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R1 and R2 are different, may be obtained.
摘要翻译：提供了对富含对映体的组合物进行去富集的方法，该方法包括使包含至少第一对映异构体或包含碳 - 杂原子键的底物的非对映异构体的对映异构体富集的组合物反应，其中碳是手性中心，杂原子是 VI族杂原子，在催化剂体系和任选的反应促进剂的存在下，得到包含具有碳 - 杂原子键的底物的第一和第二对映异构体或非对映异构体的产物组合物，第二对映异构体或二聚异构体的比例产物组成大于对映异构体富集组合物中第二至第一对映异构体或二聚异构体的比例。优选的底物包括式（1）的化合物，其中：X表示O，S; R 1，R 2各自独立地表示任选取代的烃基，全卤代烃基，任选取代的杂环基; 或R 1和R 2任选地以使得形成任选取代的环的方式连接; 条件是选择R 1和R 2以使得*是手性中心。在优选的方法中，式（2）的化合物其中：X表示O，S; R 1，R 2各自独立地表示任选取代的烃基，全卤代烃基，任选取代的杂环基; 或R 1和R 2任选地以使得形成任选取代的环的方式连接; 只要R1和R2不同，就可以得到。

3. 发明申请

WO2006046059A1 CATALYST COMPOSITIONS AND THEIR USE IN THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES 审中-公开
标题翻译：催化剂组合物及其在完全充分增强底物中的应用
公开(公告)号：WO2006046059A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004176
申请日：2005-10-27
申请人： AVECIA PHARMACEUTICALS LIMITED , BLACKER, Andrew, John , STIRLING, Matthew, John
发明人： BLACKER, Andrew, John , STIRLING, Matthew, John
IPC分类号： C07B55/00
CPC分类号： C07B55/00
摘要： There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group V heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or disatereomer in the product composition being greater than the ratio of second to first enantiomer or disatereomer in the enantiomerically enriched composition. Preferred catalyst systems include transition metal halide complex of the formula M n X p Y r wherein M is a transition metal; X is a halide; Y is a neutral optionally substituted hydrocarbyl complexing group, a neutral optionally substituted perhalogenated hydrocarbyl complexing group, or an optionally substituted cyclopentadienyl complexing group; and n, p and r are integers. The reaction promoter is preferably a halide salt.
摘要翻译：提供了对富含对映体的组合物进行去富集的方法，该方法包括使包含至少第一对映异构体或包含碳 - 杂原子键的底物的非对映异构体的对映异构体富集的组合物反应，其中碳是手性中心，杂原子是 V族杂原子，在催化剂体系和任选的反应促进剂的存在下，得到包含具有碳 - 杂原子键的基材的第一和第二对映异构体或非对映异构体的产物组合物，第二对映异构体或二聚异构体的比例在产物组成大于对映异构体富集组合物中第二至第一对映异构体或二聚异构体的比例。优选的催化剂体系包括式M的过渡金属卤化物络合物，其中M是过渡金属; X是卤化物; Y是中性任选取代的烃基络合基团，中性任选取代的全卤代烃基络合基团或任选取代的环戊二烯基络合基团; 并且n，p和r是整数。反应促进剂优选为卤化物盐。

4. 发明申请

WO2013028832A2 INHIBITORS OF NEDD8-ACTIVATING ENZYME 审中-公开
标题翻译： NEDD8激活酶的抑制剂
公开(公告)号：WO2013028832A2
公开(公告)日：2013-02-28
申请号：PCT/US2012/052007
申请日：2012-08-23
申请人： MILLENNIUM PHARMACEUTICALS, INC. , MCCARRON, Ashley, Sue , SELLS, Todd, B. , STIRLING, Matthew , STROUD, Stephen, G.
发明人： MCCARRON, Ashley, Sue , SELLS, Todd, B. , STIRLING, Matthew , STROUD, Stephen, G.
IPC分类号： C07D487/04 , C07D487/02 , A61K31/519 , A61K31/505 , A61P35/00
CPC分类号： C07D239/47 , C07D239/46 , C07D473/02
摘要： Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyciopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.
摘要翻译：公开了作为Nedd8激活酶（NAE）抑制剂的化学实体，即化合物{（1S，2S，4R）-4 - [（6 - {[（1R，2S） -5-氯-2-甲氧基-2,3-二氢-1H-茚-1-基]氨基}嘧啶-4-基）氧基] -2-羟基环戊基}甲基氨基磺酸酯及其药学上可接受的盐; 其固态形式; 及其前药。还公开了使用化学实体来治疗诸如癌症的疾病的方法。

5. 发明申请

WO2006041773A3 LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006041773A3
公开(公告)日：2006-04-20
申请号：PCT/US2005/035458
申请日：2005-10-03
申请人： MILLENNIUM PHARMACEUTICALS, INC. , BLACKBURN, Christopher , CLAIBORNE, Christopher, F. , CULLIS, Courtney, A. , DALES, Natalie, A. , PATANE, Michael, A. , STIRLING, Matthew , STRADELLA, Omar, G. , WEATHERHEAD, Gabriel, S.
发明人： BLACKBURN, Christopher , CLAIBORNE, Christopher, F. , CULLIS, Courtney, A. , DALES, Natalie, A. , PATANE, Michael, A. , STIRLING, Matthew , STRADELLA, Omar, G. , WEATHERHEAD, Gabriel, S.
IPC分类号： C07D487/04 , A61K31/55
摘要： The present invention provides novel compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A, R e , R b , R c , R d , G 1 , Y 1 , and Y 2 have the meaning as given in the claims useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

6. 发明申请

WO2013028832A3 INHIBITORS OF NEDD8-ACTIVATING ENZYME 审中-公开
标题翻译： NEDD8激活酶的抑制剂
公开(公告)号：WO2013028832A3
公开(公告)日：2013-05-02
申请号：PCT/US2012052007
申请日：2012-08-23
申请人： MILLENNIUM PHARM INC , MCCARRON ASHLEY SUE , SELLS TODD B , STIRLING MATTHEW , STROUD STEPHEN G
发明人： MCCARRON ASHLEY SUE , SELLS TODD B , STIRLING MATTHEW , STROUD STEPHEN G
IPC分类号： C07D487/04 , A61K31/505 , A61K31/519 , A61P35/00 , C07D487/02
CPC分类号： C07D239/47 , C07D239/46 , C07D473/02
摘要： Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyciopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.
摘要翻译：公开了作为Nedd8活化酶（NAE）抑制剂的化学实体，即化合物{（1S，2S，4R）-4 - [（6 - {[（1R，2S）-5-氯-2-甲氧基 -2,3-二氢-1H-茚-1-基]氨基}嘧啶-4-基）氧基] -2-羟基环戊基}甲基氨基磺酸酯及其药学上可接受的盐; 其固态形式; 及其前体药物。还公开了使用化学实体来治疗诸如癌症的疾病的方法。

7. 发明申请

WO2006046056A1 PROCESS FOR THE TRANSFER HYDROGENATION OF AN ORGANIC COMPOUND IN THE PRESENCE OF A CATALYST REGENERATOR 审中-公开
标题翻译：有机化合物在催化剂再生器存在下的转移加氢方法
公开(公告)号：WO2006046056A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004171
申请日：2005-10-27
申请人： AVECIA PHARMACEUTICALS LIMITED , HODGES, George, Robert , STIRLING, Matthew, John
发明人： HODGES, George, Robert , STIRLING, Matthew, John
IPC分类号： C07B31/00 , C07C29/145
CPC分类号： C07C29/143 , C07B31/00 , Y02P20/584 , C07C33/22 , C07C33/46
摘要： There is provided a process for the transfer hydrogenation of an organic compound having a carbon-carbon or carbon-heteroatom double bond wherein an organic compound of formula (I): wherein: X represents CR 3 R 4 , NR 5 , (NR 5 R 6 ) + Q - , O or S; Q - represents an anion; R 1 , R 2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl or an optionally substituted heterocyclyl group; R 3 , R 4 , and R 6 each independently represents a hydrogen atom, an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl or an optionally substituted heterocyclyl group; R 5 independently represents a hydrogen atom, an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group or a removable group; or one or more of R 1 & R 2 , R 1 & R 3 , R 2 & R 4 , R 3 & R 4 , R 1 & R 5 , R 2 & R 6 and R 5 & R 6 optionally being linked in such a way as to form an optionally substituted ring(s), is reacted with a hydrogen donor in the presence of a transfer hydrogenation catalyst, and substantially in the presence of a catalyst regenerator. Catalyst regenerators include oxidants, for example KMnO 4 , oxygen and oxygen/inert gas mixtures.
摘要翻译：提供了具有碳 - 碳或碳 - 杂原子双键的有机化合物的转移氢化方法，其中式（I）的有机化合物：其中：X表示CR 3 R SUP > 4 ，NR 5，（NR 5 R 6）6 - ，O或S; Q 表示阴离子; R 1，R 2各自独立地表示任选取代的烃基，全卤代烃基或任选取代的杂环基; R 3，R 4和R 6各自独立地表示氢原子，任选取代的烃基，全卤代烃基或任选取代的杂环基组; R 5独立地表示氢原子，任选取代的烃基，全卤代烃基，任选取代的杂环基或可除去的基团; 或R 1，R 2，R 2，R 3和R 3中的一个或多个， R＆lt; 3＆gt;＆lt; 4＆gt;，＆lt; 1＆gt;＆lt; 5＆gt; 任选地在这样的一个或多个连接在一起的第二个和第六个和第六个和第六个和第六个在形成任选取代的环的方式与氢供体在转移氢化催化剂的存在下，基本上在催化剂再生器的存在下反应。催化剂再生器包括氧化剂，例如KMnO 4，氧和氧/惰性气体混合物。

8. 发明申请

WO2006041773A2 LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： LACTAM化合物作为蛋白激酶抑制剂有用
公开(公告)号：WO2006041773A2
公开(公告)日：2006-04-20
申请号：PCT/US2005035458
申请日：2005-10-03
申请人： MILLENNIUM PHARM INC , BLACKBURN CHRISTOPHER , CLAIBORNE CHRISTOPHER F , CULLIS COURTNEY A , DALES NATALIE A , PATANE MICHAEL A , STIRLING MATTHEW , STRADELLA OMAR G , WEATHERHEAD GABRIEL S
发明人： BLACKBURN CHRISTOPHER , CLAIBORNE CHRISTOPHER F , CULLIS COURTNEY A , DALES NATALIE A , PATANE MICHAEL A , STIRLING MATTHEW , STRADELLA OMAR G , WEATHERHEAD GABRIEL S
IPC分类号： C07D487/04 , A61K31/55
CPC分类号： C07D491/14 , C07D471/14 , C07D487/04 , C07D495/14
摘要： The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译：本发明提供了可用作蛋白激酶抑制剂的新化合物。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。

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