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1. 发明申请

WO2008156758A1 BIFUNCTIONAL SYNTHETIC MOLECULES 审中-公开
标题翻译：双功能合成分子
公开(公告)号：WO2008156758A1
公开(公告)日：2008-12-24
申请号：PCT/US2008/007536
申请日：2008-06-17
申请人： BIOCHEMICS, INC. , CARTER, Stephen, G. , PATEL, Kanu , ZHU, Zhen , QIAO, Lixin
发明人： CARTER, Stephen, G. , PATEL, Kanu , ZHU, Zhen , QIAO, Lixin
IPC分类号： A61K31/74 , A01N61/00
CPC分类号： C07D213/80 , C07C69/612 , C07C233/87 , C07C2601/14 , C07D207/16 , C07D217/26 , C07D233/06 , C07D233/24 , C07D233/50 , C07D417/04
摘要： The synthesis and use of bifunctional molecules to improve the topical and transdermal delivery efficiency of various types of therapeutic agents or agents designed to promote the transdermal delivery of those therapeutic agents either into the skin tissue or into the systemic circulation. Three major classes of molecules are covalently joined as bifunctional substances; chemical vasodilators, passive dermal penetration enhancers and therapeutic or diagnostic drugs. Chemical vasodilators may be delivered into the skin to increasing the blood flow in a tissue that has compromised circulation or they may be used as part of a delivery vehicle to promote the delivery of the drug. Passive dermal penetration enhancers are those chemicals that promote the passive penetration of drugs and other chemicals through the stratum corneum and epidermis of the skin tissue. Drugs and diagnostic agents are the third group of chemicals that are candidates for the linkage of molecules.
摘要翻译：双功能分子的合成和使用以改善各种类型治疗剂或试剂的局部和透皮递送效率，所述治疗剂或试剂旨在促进将这些治疗剂透皮递送至皮肤组织或进入体循环。三大类分子共价连接成双功能物质; 化学血管扩张剂，被动皮肤渗透增强剂和治疗或诊断药物。化学血管扩张剂可以被递送到皮肤中以增加已经损害循环的组织中的血液流动，或者它们可以用作递送载体的一部分以促进药物的递送。被动皮肤渗透增强剂是促进药物和其他化学物质通过角质层和皮肤组织表皮的被动穿透的化学物质。药物和诊断剂是作为分子连接的候选物的第三组化学品。

2. 发明申请

WO2011090760A1 HETEROARYL COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：异喹啉化合物及其用途
公开(公告)号：WO2011090760A1
公开(公告)日：2011-07-28
申请号：PCT/US2010/062432
申请日：2010-12-29
申请人： AVILA THERAPEUTICS, INC. , SINGH, Juswinder , PETTER, Russell , TESTER, Richland, Wayne , KLUGE, Arthur, F. , MAZDIYASNI, Hormoz , WESTLIN, III, William, Frederick , NIU, Deqiang , QIAO, Lixin
发明人： SINGH, Juswinder , PETTER, Russell , TESTER, Richland, Wayne , KLUGE, Arthur, F. , MAZDIYASNI, Hormoz , WESTLIN, III, William, Frederick , NIU, Deqiang , QIAO, Lixin
IPC分类号： A61K31/33
CPC分类号： A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K45/06 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/18 , C07D495/04
摘要： The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
摘要翻译：本发明提供化合物，其药学上可接受的组合物及其使用方法。

3. 发明申请

WO2011002808A1 HCV PROTEASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： HCV蛋白酶抑制剂及其用途
公开(公告)号：WO2011002808A1
公开(公告)日：2011-01-06
申请号：PCT/US2010/040474
申请日：2010-06-29
申请人： AVILA THERAPEUTICS, INC. , NIU, Deqiang , PETTER, Rusell, C. , SINGH, Juswinder , KLUGE, Arthur, F. , QIAO, Lixin
发明人： NIU, Deqiang , PETTER, Rusell, C. , SINGH, Juswinder , KLUGE, Arthur, F. , QIAO, Lixin
IPC分类号： C07D487/00 , A61K31/40
CPC分类号： C07K5/081 , A61K38/00 , C07K5/0202 , C07K5/06165 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/0821 , C12N9/506 , C12N9/96 , C12N9/99
摘要： The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
摘要翻译：本发明提供了化合物，其药学上可接受的组合物及其使用方法。

4. 发明申请

WO2012122383A2 PI3 KINASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： PI3激酶抑制剂及其用途
公开(公告)号：WO2012122383A2
公开(公告)日：2012-09-13
申请号：PCT/US2012/028293
申请日：2012-03-08
申请人： AVILA THERAPEUTICS, INC. , QIAO, Lixin , NIU, Deqiang , PETTER, Russell, C. , ZHU, Zhendong
发明人： QIAO, Lixin , NIU, Deqiang , PETTER, Russell, C. , ZHU, Zhendong
IPC分类号： A61K39/395
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention provides compounds, compositions thereof, and methods of using the same.
摘要翻译：本发明提供化合物，其组合物及其使用方法。

5. 发明申请

WO2011031896A3 PI3 KINASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： PI3激酶抑制剂及其用途
公开(公告)号：WO2011031896A3
公开(公告)日：2011-03-17
申请号：PCT/US2010/048317
申请日：2010-09-09
申请人： AVILA THERAPEUTICS, INC. , NIU, Deqiang , PETTER, Russell, C. , SINGH, Juswinder , KLUGE, Arthur, F. , MAZDIYASNI, Hormoz , ZHU, Zhendong , QIAO, Lixin , KUNTZ, Kevin
发明人： NIU, Deqiang , PETTER, Russell, C. , SINGH, Juswinder , KLUGE, Arthur, F. , MAZDIYASNI, Hormoz , ZHU, Zhendong , QIAO, Lixin , KUNTZ, Kevin
IPC分类号： A61K38/00
摘要： The present invention provides compounds, compositions thereof, and methods of using the same.
摘要翻译：本发明提供了化合物，其组合物及其使用方法。

6. 发明申请

WO2010117787A2 INHIBITING EPH B-3 KINASE 审中-公开
标题翻译：抑制EPH B-3激酶
公开(公告)号：WO2010117787A2
公开(公告)日：2010-10-14
申请号：PCT/US2010/029209
申请日：2010-03-30
申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC. , DUKE UNIVERSITY , QIAO, Lixin , GLICKSMAN, Marcie , GAINER, Thomas , LO, Donald C. , STEIN, Ross L. , CHOI, Sungwoon , CUNY, Gregory D.
发明人： QIAO, Lixin , GLICKSMAN, Marcie , GAINER, Thomas , LO, Donald C. , STEIN, Ross L. , CHOI, Sungwoon , CUNY, Gregory D.
IPC分类号： C07D487/04 , C07D487/02 , A61K31/437 , A61P25/00
CPC分类号： A61K31/437 , A61K31/00
摘要： EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke.
摘要翻译：包括某些吡唑并[1,5-a]吡啶和咪唑并[1,2-a]吡啶化合物的EphB3激酶抑制剂化合物抑制EphB3激酶。与通用激酶抑制剂相比，EphB3激酶抑制剂化合物对EphB3激酶的抑制作用可能更大。还提供了包含EphB3激酶抑制剂化合物的药物组合物，例如神经保护剂。 EphB3激酶抑制剂化合物和药物组合物可用于例如在缺血事件（例如中风）期间损伤的神经元组织的神经保护和/或修复。

7. 发明申请

WO2002096897A1 PHOSPHINYLMETHYL AND PHOSPHORYLMETHYL SUCCINIC AND GLUTARIC ACID ANALOGS AS β-SECRETASE INHIBITORS 审中-公开
标题翻译：磷酸二甲酯和磷酸二甲酯与胰蛋白酶类似物作为β-巯基抑制剂
公开(公告)号：WO2002096897A1
公开(公告)日：2002-12-05
申请号：PCT/US2002/016917
申请日：2002-05-30
申请人： NEUROLOGIC, INC. , QIAO, Lixin , ETCHEBERRIGARAY, Rene
发明人： QIAO, Lixin , ETCHEBERRIGARAY, Rene
IPC分类号： C07D295/205
CPC分类号： C07D295/205 , C07F9/650958
摘要： The invention provides a compound of formula (I), or salts or hydrates thereof, useful as beta-secretase inhibitors. The invention further relates to a method of reducing plaque formation, particularly useful in the treatment of Alzheimer's disease.
摘要翻译：本发明提供了可用作β-分泌酶抑制剂的式（I）化合物或其盐或水合物。本发明还涉及减少斑块形成的方法，特别可用于治疗阿尔茨海默氏病。

8. 发明申请

WO2011082285A1 LIGAND-DIRECTED COVALENT MODIFICATION OF PROTEIN 审中-公开
标题翻译：蛋白质的配体指导性共价修饰
公开(公告)号：WO2011082285A1
公开(公告)日：2011-07-07
申请号：PCT/US2010/062473
申请日：2010-12-30
申请人： AVILA THERAPEUTICS, INC. , PETTER, Russell C. , JEWELL, Charles F. , LEE, Kwangho , MEDIKONDA, Aravind Prasad , NIU, Deqiang , QIAO, Lixin , SINGH, Juswinder , ZHU, Zhendong
发明人： PETTER, Russell C. , JEWELL, Charles F. , LEE, Kwangho , MEDIKONDA, Aravind Prasad , NIU, Deqiang , QIAO, Lixin , SINGH, Juswinder , ZHU, Zhendong
IPC分类号： C40B30/04
CPC分类号： C12N9/96 , C07D207/16 , C07D239/49 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/06 , C07D417/14 , C07D487/04 , C07D491/08 , C07D493/04 , C07D495/04 , C07D513/04 , C07D519/00 , C12N9/12 , C12N9/506 , C12N9/93 , C12Q1/25 , C12Q1/37 , C12Q1/485 , C12Y207/11001 , C12Y304/21098 , C12Y603/02 , G01N33/68 , G06F19/16 , G06F19/706
摘要： The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.
摘要翻译：本发明涉及酶抑制剂。更具体地，本发明涉及蛋白质的配体定向共价修饰; 设计方法药物制剂相同; 和使用方法。

9. 发明申请

WO2011034907A2 PROTEIN KINASE CONJUGATES AND INHIBITORS 审中-公开
标题翻译：蛋白激酶结合和抑制剂
公开(公告)号：WO2011034907A2
公开(公告)日：2011-03-24
申请号：PCT/US2010/048916
申请日：2010-09-15
申请人： AVILA THERAPEUTICS, INC. , SINGH, Juswinder , PETTER, Russell Colyn , NIU, Deqiang , QIAO, Lixin , KLUGE, Arthur , LOBB, Roy , GHOSH, Shomir , ZHU, Zhendong
发明人： SINGH, Juswinder , PETTER, Russell Colyn , NIU, Deqiang , QIAO, Lixin , KLUGE, Arthur , LOBB, Roy , GHOSH, Shomir , ZHU, Zhendong
IPC分类号： A61K31/519 , C12N9/12
CPC分类号： C07D487/04 , A61K47/545 , A61K47/62 , C07D213/72 , C07D213/74 , C07D213/81 , C07D213/82 , C07D215/22 , C07D231/12 , C07D239/42 , C07D239/48 , C07D333/68 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D495/04 , C07D498/04 , C12N9/1205 , C12N9/96
摘要： The invention relates to protein conjugates that contain a protein kinase containgn a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.
摘要翻译：本发明涉及蛋白质缀合物，其含有包含ATP结合位点中的半胱氨酸残基的蛋白激酶和与所述半胱氨酸残基共价和不可逆地结合的抑制剂，使得蛋白激酶的活性不可逆地被抑制。本发明还涉及不可逆地抑制蛋白激酶的化合物。

10. 发明申请

WO2009082697A1 HCV PROTEASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译： HCV蛋白酶抑制剂及其用途
公开(公告)号：WO2009082697A1
公开(公告)日：2009-07-02
申请号：PCT/US2008/087725
申请日：2008-12-19
申请人： AVILA THERAPEUTICS, INC. , PETTER, Russell , SINGH, Juswinder , KLUGE, Arthur, F. , NIU, Deqiang , QIAO, Lixin , GHOSH, Shomir
发明人： PETTER, Russell , SINGH, Juswinder , KLUGE, Arthur, F. , NIU, Deqiang , QIAO, Lixin , GHOSH, Shomir
IPC分类号： A01N43/36 , A61K31/40
CPC分类号： A61K38/06 , A61K38/00 , A61K38/05 , A61K38/12 , C07K5/06165 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0827 , C07K5/12
摘要： The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
摘要翻译：本发明提供化合物，其药学上可接受的组合物及其使用方法。

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