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    Small-Molecule HSP90 Inhibitors
    2.
    发明申请
    Small-Molecule HSP90 Inhibitors 有权
    小分子HSP90抑制剂

    公开(公告)号：US20110104054A1

    公开(公告)日：2011-05-05

    申请号：US12939807

    申请日：2010-11-04

    申请人： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-bufi ,  Joungnam Kim ,  Steven M. Larson ,  Peter Smith-Jones

    发明人： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-bufi ,  Joungnam Kim ,  Steven M. Larson ,  Peter Smith-Jones

    IPC分类号： A61K31/52 ,  C07D473/34 ,  A61P35/00 ,  A61K51/00 ,  A61P43/00 ,  C12N5/02

    CPC分类号： C07D473/34 ,  A61K51/0459 ,  C07D491/056 ,  G01N33/60

    摘要： Hsp90 inhibitors having are provided having the formula: with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

    摘要翻译： 提供具有下式的Hsp90抑制剂：右侧芳基部分具有2'，4'，5'-取代模式。 X1表示在芳基的4'和5'位置上可以相同或不同的两个取代基，其中X 1选自卤素，烷基，烷氧基，卤代烷氧基，羟基烷基，吡咯基，任选取代的芳氧基，烷基氨基 ，二烷基氨基，氨基甲酰基，酰氨基，烷基酰氨基二烷基酰氨基，酰基氨基，烷基磺酰氨基，三卤甲氧基，三卤代烷基，硫代烷基，SO2-烷基，COO-烷基，KH 2，OH，CN，SO 2 X 5，NO 2，NO，C≡SR2 NSO 2 X 5，C = OR 2，其中 X5是F，NH2，烷基或H，R2是烷基，NH2，NH-烷基或O-烷基，C1-C6烷基或烷氧基; 或其中X 1具有式-O-（CH 2）n -O-，其中n是0至2的整数，优选1或2，并且其中一个氧键在5'-位上而另一个在 芳基环的4'-位。 该化合物可用于癌症治疗和放射成像配体。

    Small-molecule Hsp90 inhibitors
    3.
    发明授权
    Small-molecule Hsp90 inhibitors 有权
    小分子Hsp90抑制剂

    公开(公告)号：US07834181B2

    公开(公告)日：2010-11-16

    申请号：US11814506

    申请日：2006-02-01

    申请人： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-Bufi ,  Joungnam Kim ,  Steve M. Larson ,  Peter Smith-Jones

    发明人： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-Bufi ,  Joungnam Kim ,  Steve M. Larson ,  Peter Smith-Jones

    IPC分类号： C07D473/34 ,  C07D473/40 ,  A61K31/52 ,  A61P35/00

    CPC分类号： C07D473/34 ,  A61K51/0459 ,  C07D491/056 ,  G01N33/60

    摘要： Hsp90 inhibitors are provided having the formula: with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2−alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygen is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

    摘要翻译： 提供具有下式的Hsp90抑制剂：右侧芳基部分具有2'，4'，5'-取代模式。 X1表示在芳基的4'和5'位置上可以相同或不同的两个取代基，其中X 1选自卤素，烷基，烷氧基，卤代烷氧基，羟基烷基，吡咯基，任选取代的芳氧基，烷基氨基 ，二烷基氨基，氨基甲酰基，酰氨基，烷基酰氨基二烷基酰氨基，酰基氨基，烷基磺酰氨基，三卤甲氧基，三卤代烷基，硫代烷基，SO2-烷基，COO-烷基，KH 2，OH，CN，SO 2 X 5，NO 2，NO，C≡SR2 NSO 2 X 5，C = OR 2，其中 X5是F，NH2，烷基或H，R2是烷基，NH2，NH-烷基或O-烷基，C1-C6烷基或烷氧基; 或其中X 1具有式-O-（CH 2）n -O-的化合物，其中n为0至2的整数，优选1或2，并且一个氧键在5'位置而另一个在 芳基环的4'-位。 该化合物可用于癌症治疗和放射成像配体。

    Small-Molecule Hsp90 Inhibitors
    4.
    发明申请
    Small-Molecule Hsp90 Inhibitors 有权
    小分子Hsp90抑制剂

    公开(公告)号：US20080253965A1

    公开(公告)日：2008-10-16

    申请号：US11814506

    申请日：2006-02-01

    申请人： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-Bufi ,  Joungnam Kim ,  Steve M. Larson ,  Peter Smith-Jones

    发明人： Gabriela Chiosis ,  Huazhong He ,  Laura Llauger-Bufi ,  Joungnam Kim ,  Steve M. Larson ,  Peter Smith-Jones

    IPC分类号： A61K51/04 ,  C07D473/00 ,  A61P35/00 ,  A61K31/52

    CPC分类号： C07D473/34 ,  A61K51/0459 ,  C07D491/056 ,  G01N33/60

    摘要： Hsp90 inhibitors are provided having the formula: with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2. alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C═SR2 NSO2X5, C═OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5′-position and the other at the 4′-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

    摘要翻译： 提供具有下式的Hsp90抑制剂：右侧芳基部分具有2'，4'，5'-取代模式。 X1表示在芳基的4'和5'位置上可以相同或不同的两个取代基，其中X 1选自卤素，烷基，烷氧基，卤代烷氧基，羟基烷基，吡咯基，任选取代的芳氧基，烷基氨基 ，二烷基氨基，氨基甲酰基，酰胺基，烷基酰氨基二烷基酰氨基，酰基氨基，烷基磺酰基氨基，三卤甲氧基，三卤代烃，硫代烷基，SO 2。 烷基，COO-烷基，KH 2，OH，CN，SO 2 X 5，NO 2，NO ，C-SR 2 NSO 2 X 5，C-OR 2，其中X 5 < NH 2，烷基或H，R 2是烷基，NH 2，NH-烷基或O-烷基，C 1〜 C 1 -C 6烷基或烷氧基; 或其中X 1具有式-O-（CH 2 CH 2）n -O-，其中n是0至2的整数， 优选1或2个，并且一个氧键在芳环的5'-位而另一个位于4'-位。 该化合物可用于癌症治疗和放射成像配体。

    High-torque ratchet wrench
    6.
    发明授权
    High-torque ratchet wrench 有权

    公开(公告)号：US11491613B2

    公开(公告)日：2022-11-08

    申请号：US16611779

    申请日：2018-02-09

    申请人： Huazhong He

    发明人： Huazhong He

    IPC分类号： B25B13/46

    摘要： A high-torque ratchet wrench including a wrench body having a driving aperture and a handle, and a drive member is disposed in the driving aperture and an axial position-limiting mechanism is disposed between the driving aperture and the drive member to limit the relative axial displacement. The external side wall of the drive member and the internal aperture side of the driving aperture form two cylindrical drive faces nested, wherein a first cylindrical drive face is provided with a pin recess, a pin is rotatably mounted in the pin recess, a relief is disposed on the side face of pin, the pin is connected with a resilient reset member, the pin is rotated with the resilience of a resilient reset member, and a relief is driven to stand out of the pin recess and contacts a second drive face.

    Method of preparing pentaerythritol
    7.
    发明授权
    Method of preparing pentaerythritol 失效
    制备季戊四醇的方法

    公开(公告)号：US08293950B2

    公开(公告)日：2012-10-23

    申请号：US11993843

    申请日：2006-03-31

    申请人： Yuanhua Jiang ,  Xiaoqin Yang ,  Pingguan Bian ,  Jiaxin Feng ,  Jinjun Dong ,  Huazhong He ,  Yuanhai Li ,  Yexiang Zhang ,  Leguan Huang

    发明人： Yuanhua Jiang ,  Xiaoqin Yang ,  Pingguan Bian ,  Jiaxin Feng ,  Jinjun Dong ,  Huazhong He ,  Yuanhai Li ,  Yexiang Zhang ,  Leguan Huang

    IPC分类号： C07C29/38 ,  C07C31/18 ,  C07C31/24

    CPC分类号： C07C29/38 ,  C07C29/78 ,  C07C31/245

    摘要： A method of preparing monopentaerythritol, dipentaerthritol, and sodium formate through high temperature condensation and cascade recrystallization is disclosed. The method lowers the energy consumption dramatically and improves the cost-effectiveness by carrying out the reaction in a non-low-temperature zone, and thereby avoiding the requirement for refrigeration. The method alleviates the difficulty of separation and improves the product quality by means of cascade separation process, and thereby avoiding the low purity from a single separation. In addition, the mother liquor obtained after each separation step is recycled to the previous step as the recycling liquor, which avoids discharging waste, increases the product yield and lowers raw materials consumption.

    摘要翻译： 公开了通过高温冷凝和级联重结晶制备单季戊四醇，二季戊四醇和甲酸钠的方法。 该方法显着降低了能量消耗，通过在非低温区域进行反应提高了成本效益，从而避免了制冷的需要。 该方法减轻了分离的难度，通过级联分离方法提高了产品质量，从而避免了单一分离的低纯度。 此外，在每个分离步骤之后获得的母液被再循环至前一步骤，作为避免排放废物的再循环液体，增加了产品产率并降低了原料消耗。

    METHOD OF PREPARING PENTAERYTHRITOL
    8.
    发明申请
    METHOD OF PREPARING PENTAERYTHRITOL 失效
    辛伐他汀的制备方法

    公开(公告)号：US20100152500A1

    公开(公告)日：2010-06-17

    申请号：US11993843

    申请日：2006-03-31

    申请人： Yuanhua Jiang ,  Xiaoquin Yang ,  Pingguan Bian ,  Jiaxin Feng ,  Jinjun Dong ,  Huazhong He ,  Yuanhai Li ,  Yexiang Zhang ,  Leguan Huang

    发明人： Yuanhua Jiang ,  Xiaoquin Yang ,  Pingguan Bian ,  Jiaxin Feng ,  Jinjun Dong ,  Huazhong He ,  Yuanhai Li ,  Yexiang Zhang ,  Leguan Huang

    IPC分类号： C07C31/24

    CPC分类号： C07C29/38 ,  C07C29/78 ,  C07C31/245

    摘要： A method of preparing monopentaerythritol, dipentaerthritol, and sodium formate through high temperature condensation and cascade recrystallization is disclosed. The method lowers the energy consumption dramatically and improves the cost-effectiveness by carrying out the reaction in a non-low-temperature zone, and thereby avoiding the requirement for refrigeration. The method alleviates the difficulty of separation and improves the product quality by means of cascade separation process, and thereby avoiding the low purity from a single separation. In addition, the mother liquor obtained after each separation step is recycled to the previous step as the recycling liquor, which avoids discharging waste, increases the product yield and lowers raw materials consumption.

    摘要翻译： 公开了通过高温冷凝和级联重结晶制备单季戊四醇，二季戊四醇和甲酸钠的方法。 该方法显着降低了能量消耗，通过在非低温区域进行反应提高了成本效益，从而避免了制冷的需要。 该方法减轻了分离的难度，通过级联分离方法提高了产品质量，从而避免了单一分离的低纯度。 此外，在每个分离步骤之后获得的母液被再循环至前一步骤，作为避免排放废物的再循环液体，增加了产品产率并降低了原料消耗。