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51. 发明授权

US06828271B2 Chiral ligands, transition-metal complexes thereof and uses thereof in asymmetric reactions 有权
标题翻译：手性配体，其过渡金属络合物及其在不对称反应中的用途
公开(公告)号：US06828271B2
公开(公告)日：2004-12-07
申请号：US10319093
申请日：2002-12-13
申请人： Xumu Zhang , Dengming Xiao
发明人： Xumu Zhang , Dengming Xiao
IPC分类号： B01J3118
CPC分类号： C07C45/505 , B01J31/2419 , B01J2231/643 , B01J2531/0266 , B01J2531/46 , B01J2531/56 , B01J2531/66 , B01J2531/72 , B01J2531/74 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/847 , C07B53/00 , C07C39/17 , C07C45/69 , C07C45/72 , C07C209/52 , C07D213/04 , C07F9/005 , C07F9/5027 , C07F9/58 , C07F9/60 , C07F9/65683 , C07F11/005 , C07F13/005 , C07F15/0033 , C07F15/004 , C07F15/0046 , C07F15/0053 , C07F15/006 , C07F15/0066 , C07F15/0073 , C07F15/008 , C07F15/0086 , C07F15/0093 , C07F17/02
摘要： Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include phospholanes, P,N ligands, N,N ligands, biphenols, and chelating phosphines. The ferrocene-based irridium (R,R)-f-binaphane complex reduces imines to the corresponding amines with 95-99.6% enantioselectivity and reduces &bgr;-substituted-&agr;-arylenamides with 95% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation of imines, asymmetric hydride transfer reactions, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.
摘要翻译：公开了基于用于不对称催化的这种手性配体的手性配体和过渡金属配合物。手性配体包括磷脂，P，N配体，N，N配体，联苯酚和螯合膦。基于二茂铁的铱（R，R）-f-联吡啶络合物将亚胺还原为具有95-99.6％对映选择性的相应胺，并且减少具有95％对映选择性的β-取代-α-亚芳基酰胺。手性配体的过渡金属络合物是可用于不对称反应，如亚胺的不对称氢化，不对称氢化物转移反应，氢化硅烷化，氢化，加氢乙烯化，加氢甲酰化，烯丙基烷基化，环丙烷化，Diels-Alder反应，Heck反应，异构化，醛醇反应，迈克尔加成和环氧化反应。

52. 发明授权

US06770651B2 A2B adenosine receptor antagonists 失效
标题翻译： A2B腺苷受体拮抗剂
公开(公告)号：US06770651B2
公开(公告)日：2004-08-03
申请号：US10184494
申请日：2002-06-27
申请人： Venkata Palle , Vaibhav Varkhedkar , Jeff Zablocki , Dengming Xiao
发明人： Venkata Palle , Vaibhav Varkhedkar , Jeff Zablocki , Dengming Xiao
IPC分类号： C07D47316
CPC分类号： C07D473/16
摘要： Disclosed are novel A2B adenosine receptor antagonists of Formula I: A compound of the formula: wherein: R1 is optionally substituted alkyl or a group —Y—Z, in which Y is a covalent bond or optionally substituted alkylene, and Z is optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted alkenyl or optionally substituted alkynyl, with the proviso that when Y is a covalent bond Z cannot be alkenyl or alkynyl; and X is oxygen, sulfur, or NH—, or a pharmaceutically acceptable salt, ester, or prodrug thereof. The compounds are particularly useful for treating asthma and diabetic retinopathy.
摘要翻译：公开了式I的新型A2B腺苷受体拮抗剂：下式化合物：其中：R 1为任选取代的烷基或基团-YZ，其中Y为共价键或任选取代的亚烷基，Z为任选取代的环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的杂环基，任选取代的烯基或任选取代的炔基，条件是当Y为共价键时，Z不能为烯基或炔基; 和X是氧，硫或NH-，或其药学上可接受的盐，酯或前药。该化合物特别可用于治疗哮喘和糖尿病性视网膜病变。

53. 发明授权

US06525210B1 Chiral ligands, transition-metal complexes thereof and uses thereof in asymmetric reactions 有权
标题翻译：手性配体，其过渡金属络合物及其在不对称反应中的用途
公开(公告)号：US06525210B1
公开(公告)日：2003-02-25
申请号：US09643434
申请日：2000-08-22
申请人： Xumu Zhang , Dengming Xiao
发明人： Xumu Zhang , Dengming Xiao
IPC分类号： C07F950
CPC分类号： C07C45/505 , B01J31/2419 , B01J2231/643 , B01J2531/0266 , B01J2531/46 , B01J2531/56 , B01J2531/66 , B01J2531/72 , B01J2531/74 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/847 , C07B53/00 , C07C39/17 , C07C45/69 , C07C45/72 , C07C209/52 , C07D213/04 , C07F9/005 , C07F9/5027 , C07F9/58 , C07F9/60 , C07F9/65683 , C07F11/005 , C07F13/005 , C07F15/0033 , C07F15/004 , C07F15/0046 , C07F15/0053 , C07F15/006 , C07F15/0066 , C07F15/0073 , C07F15/008 , C07F15/0086 , C07F15/0093 , C07F17/02
摘要： Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include phospholanes, P,N ligands, N,N ligands, biphenols, and chelating phosphines. The ferrocene-based irridium (R,R)-f-binaphane complex reduces imines to the corresponding amines with 95-99.6% enantioselectivity and reduces &bgr;-substituted-&agr;-arylenamides with 95% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation of imines, asymmetric hydride transfer reactions, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.
摘要翻译：公开了基于用于不对称催化的这种手性配体的手性配体和过渡金属配合物。手性配体包括磷脂，P，N配体，N，N配体，联苯酚和螯合膦。二茂铁基的铱（R，R）-f-联吡啶络合物将亚胺还原为具有95-99.6％对映体选择性的相应的胺，并减少具有95％对映选择性的β-取代的α-亚芳基酰胺。手性配体的过渡金属络合物可用于不对称反应，如亚胺的不对称氢化，不对称氢化物转移反应，氢化硅烷化，氢化，氢化，加氢甲酰化，烯丙基烷基化，环丙烷化，狄尔斯 - 阿尔德反应，Heck反应，异构化，醛醇反应，迈克尔加成和环氧化反应。

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