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1. 发明授权

US06958401B2 Method for synthesizing epothilones and epothilone analogs 失效
公开(公告)号：US06958401B2
公开(公告)日：2005-10-25
申请号：US10352340
申请日：2003-01-27
申请人： James David White , Rich Garrett Carter , Kurt Frederick Sundermann
发明人： James David White , Rich Garrett Carter , Kurt Frederick Sundermann
IPC分类号： C07D277/20 , C07D417/06 , C07D277/22 , A61P35/00
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.

2. 发明授权

US06596875B2 Method for synthesizing epothilones and epothilone analogs 失效
公开(公告)号：US06596875B2
公开(公告)日：2003-07-22
申请号：US09846154
申请日：2001-04-30
申请人： James David White , Rich Garrett Carter , Kurt Frederick Sundermann
发明人： James David White , Rich Garrett Carter , Kurt Frederick Sundermann
IPC分类号： C07D49304
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.

3. 发明授权

US07145018B2 Method for synthesizing epothilones and epothilone analogs 失效
标题翻译：合成埃坡霉素和埃坡霉素类似物的方法
公开(公告)号：US07145018B2
公开(公告)日：2006-12-05
申请号：US11123530
申请日：2005-05-05
申请人： James David White , Rich Garrett Carter , Kurt Frederick Sundermann
发明人： James David White , Rich Garrett Carter , Kurt Frederick Sundermann
IPC分类号： C07D277/22
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B
摘要翻译：描述了制备埃坡霉素和埃坡霉素类似物的方法，以及通过该方法制备的新型化合物。该方法的一个实施方案用于通过收敛方法合成埃坡霉素B，其使得衍生自溴化鏻的内鎓盐与醛的Wittig偶联。前者由炔丙醇通过九步路径制备，其安装了具有清洁Z构型的三取代双键。得到的仲酸的大环内酯化得到以下的中间体二烯雌二醇类似物。选择性饱和的9,10-烯烃和随后的环氧化提供埃坡霉素B

4. 发明授权

US06906188B2 Method for synthesizing epothilones and epothilone analogs 失效
标题翻译：合成埃坡霉素和埃坡霉素类似物的方法
公开(公告)号：US06906188B2
公开(公告)日：2005-06-14
申请号：US10354694
申请日：2003-01-29
申请人： James David White , Kurt Frederick Sundermann , Rich Garrett Carter
发明人： James David White , Kurt Frederick Sundermann , Rich Garrett Carter
IPC分类号： C07D277/20 , C07D417/06 , C07D225/02 , C07D321/00 , C07D327/02 , C07D411/06
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. Exemplary novel compounds include those according to the formula: With respect the formula, G is selected from the group consisting of R2 substituents independently are selected from the group consisting of H and lower alkyl groups; Z is selected from the group consisting of the halogens and —CN; M is selected from the group consisting of O and NR3; R3 is selected from the group consisting of H, lower alkyl, R4CO, R4OCO, and R4SO2; R4 is selected from the group consisting of H, lower alkyl, and aryl; T is selected from the group consisting of CH2, CO, HCOH and protected derivatives thereof; W is H or OR; and X and Y independently are selected from the group consisting of O, NH, S, CO, and C. Embodiments of the method provide convenient access to analogs of the epothilones, such as those having alternate stereochemistry and those containing an ester, amide, thioester, or alkyne moieties in the macrocycle.
摘要翻译：描述了制备埃坡霉素和埃坡霉素类似物的方法，以及通过该方法制备的新型化合物。示例性的新化合物包括根据下式的化合物：关于式，G选自R 2 2取代基，独立地选自H和低级烷基; Z选自卤素和-CN; M选自O和NR 3; R 3选自H，低级烷基，R 4 CO，R 4 OCO和R 4， / SO 2 SO 2; R 4选自H，低级烷基和芳基; T选自CH 2 CO，HCOH及其被保护的衍生物; W为H或OR; X和Y独立地选自O，NH，S，CO和C.这些方法的实施方案提供方便地获得埃坡霉素的类似物，例如具有交替立体化学的那些类似物，以及含有酯，酰胺，硫代酯或炔烃部分。

5. 发明申请

US20120190725A1 INHIBITOR(S) OF TRANSPORTERS OR UPTAKE OF MONOAMINERGIC NEUROTRANSMITTERS 有权
标题翻译：运输商抑制剂或单宁神经递质的摄取
公开(公告)号：US20120190725A1
公开(公告)日：2012-07-26
申请号：US13355371
申请日：2012-01-20
申请人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
发明人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
IPC分类号： A61K31/381 , C07D333/20 , C07D333/16 , A61P25/24 , A61P25/22 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/08 , A61P25/18 , A61P13/00 , A61P25/06 , A61P3/04 , A61P3/00 , A61P25/30 , A61P25/32 , A61P25/36 , A61P25/34 , C07D333/24
CPC分类号： A61K31/381 , C07D333/16 , C07D333/20 , C07D333/24
摘要： The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R1-R4 is a heterocycle, at least one of R1-R4 is an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R1-R4 is an amide, and any and all combinations thereof. Remaining R1-R4 substituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.
摘要翻译：本公开涉及具有下式的化合物或其药学上可接受的盐：其中R 1 -R 4中的至少一个是杂环，R 1 -R 4中的至少一个是通过连接原子与环连接的芳基，官能团或其它部分，或者其中没有R 1 -R 4是酰胺，以及其任何和所有组合。残留的R 1 -R 4取代基独立地是脂族，取代的脂族，胺，取代的胺，芳基，取代的芳基，环状，取代的环状，卤素，杂芳基，取代的杂芳基，杂环，取代的杂环，氢或羟基。还提供了治疗受试者的方法，其包括向受试者施用公开的化合物或化合物，或将其转化为所公开的化合物或化合物的前体药物或包含其化合物，化合物或前药的组合物。还提供了制备公开化合物的方法。

6. 发明授权

US08772330B2 Inhibitor(s) of transporters or uptake of monoaminergic neurotransmitters 有权
标题翻译：转运蛋白的抑制剂或单胺能神经递质的摄取
公开(公告)号：US08772330B2
公开(公告)日：2014-07-08
申请号：US13355371
申请日：2012-01-20
申请人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
发明人： James David White , David T. Wong , David B. Chan , Jongtae Yang , Rajan Juniku
IPC分类号： A61K31/381 , C07D333/16
CPC分类号： A61K31/381 , C07D333/16 , C07D333/20 , C07D333/24
摘要： The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R1-R4 is a heterocycle, at least one of R1-R4 is an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R1-R4 is an amide, and any and all combinations thereof. Remaining R1-R4 substituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.
摘要翻译：本公开涉及具有下式的化合物或其药学上可接受的盐：其中R 1 -R 4中的至少一个是杂环，R 1 -R 4中的至少一个是通过连接原子与环偶联的芳基，官能团或其它部分，或者其中没有R 1 -R 4是酰胺，以及其任何和所有组合。残留的R 1 -R 4取代基独立地是脂族，取代的脂族，胺，取代的胺，芳基，取代的芳基，环状，取代的环状，卤素，杂芳基，取代的杂芳基，杂环，取代的杂环，氢或羟基。还提供了治疗受试者的方法，其包括向受试者施用公开的化合物或化合物，或将其转化为所公开的化合物或化合物的前体药物或包含其化合物，化合物或前药的组合物。还提供了制备公开化合物的方法。

7. 发明申请

US20160059363A1 PORTABLE COMPUTER NUMERICALLY CONTROLLED CUTTING MACHINE WITH FOLDING ARM 审中-公开
标题翻译：便携式计算机数字控制切割机与折叠ARM
公开(公告)号：US20160059363A1
公开(公告)日：2016-03-03
申请号：US14749576
申请日：2015-06-24
申请人： William Scott Ardisson , Anthony Olivieri , Michael Farmer , James David White
发明人： William Scott Ardisson , Anthony Olivieri , Michael Farmer , James David White
IPC分类号： B23K37/02 , B23K26/38 , B23K26/06 , B23K26/00 , B23K26/08 , B23K26/70 , B23K37/00 , B23K10/00 , B23K26/03
CPC分类号： B23K37/0288 , B23K26/0096 , B23K26/032 , B23K26/0648 , B23K26/0876 , B23K26/38 , B23K26/702 , B23K37/0235
摘要： A portable computer numerically controlled non-contact cutting apparatus is provided comprising a housing, and an arm having a base portion attached to the housing and movable along a longitudinal axis of the housing. The arm may comprise a head assembly adapted to receive a cutting device, the head assembly may be movable along a longitudinal axis of the arm, and the arm may be rotatable about the base portion relative to the longitudinal axis of the housing from a retracted position to an extended position. Further, the arm may be adapted to be releasably held in the extended position.
摘要翻译：提供一种便携式计算机数字控制的非接触切割装置，其包括壳体和臂，其具有附接到壳体并可沿着壳体的纵向轴线移动的基部。臂可以包括适于接收切割装置的头部组件，头部组件可以沿着臂的纵向轴线移动，并且臂可以相对于壳体的纵向轴线从缩回位置围绕基部旋转到一个延伸的位置。此外，臂可以适于可释放地保持在延伸位置。

8. 发明授权

US06494942B1 Dye-based ink jet compositions having improved stability and light fastness 有权
标题翻译：具有改善的稳定性和耐光性的染料型喷墨组合物
公开(公告)号：US06494942B1
公开(公告)日：2002-12-17
申请号：US09662950
申请日：2000-09-15
申请人： Larrie A Deardurff , James David White , Christopher Lincoln
发明人： Larrie A Deardurff , James David White , Christopher Lincoln
IPC分类号： C09D1102
CPC分类号： C09D11/32 , C09D11/328
摘要： An aqueous ink jet ink is disclosed which comprises an effective amount of an azomethine dye having at least one water solubilizing functional group covalently attached thereto. The water solubilizing functional group can either be directly attached to the azomethine dye and/or can be attached to the azomethine dye through an electrophilic coupling moiety. If an organic spacer group is used to separate the water solubilizing functional group from azomethine dye or the electrophilic coupling moiety, then straight and branched chained alkyl groups having from about 1 to 10 carbon atoms is preferred. Preferred azomethine dyes can be pyrazolone azomethines, pyrazolotriazole azomethines, and combinations thereof. Additionally, an aqueous ink jet ink is disclosed comprising an effective amount of a dye-based colorant and an essentially water soluble spiroindane additive for improving light fastness and stability of the dye-based colorant.
摘要翻译：公开了一种含水喷墨油墨，其包含有效量的具有至少一个与其共价连接的水溶性官能团的偶氮甲碱染料。水溶性官能团可以直接连接到偶氮甲碱染料和/或可以通过亲电子偶联部分连接到偶氮甲碱染料。如果使用有机间隔基团从水杨酸染料或亲电偶联部分分离水溶性官能团，则优选具有约1至10个碳原子的直链和支链链烷基。优选的偶氮甲碱染料可以是吡唑啉酮偶氮甲碱，吡唑并三唑偶氮甲碱及其组合。此外，公开了一种含水喷墨油墨，其包含有效量的染料基着色剂和基本上水溶性的螺环茚添加剂，用于改善染料基着色剂的耐光性和稳定性。

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