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21. 发明申请

WO2011025980A1 MODIFIED LUCIFERASES AND USES THEREOF 审中-公开
标题翻译：改性的润滑剂及其用途
公开(公告)号：WO2011025980A1
公开(公告)日：2011-03-03
申请号：PCT/US2010/047033
申请日：2010-08-27
申请人： TARGETING SYSTEMS , WALIA, Rampyari, R.
发明人： WALIA, Rampyari, R.
IPC分类号： C12Q1/66 , C07H21/04
CPC分类号： C12N9/0069 , C12Q1/66 , C12Y113/12007
摘要： The present invention encompasses modified luciferases, methods for making modified luciferases, and assays utilizing modified luciferases. Modified luciferases of the invention show increased activity over wildtype luciferases and also show increased stability of signal. The present invention also encompasses multiplex assays utilizing multiple luciferases with different emission spectra.
摘要翻译：本发明包括修饰的荧光素酶，用于制备修饰的荧光素酶的方法和利用修饰的荧光素酶的测定。本发明的修饰的荧光素酶显示出比野生型萤光素酶增加的活性，并且还显示增加的信号稳定性。本发明还包括利用具有不同发射光谱的多个荧光素酶的多重测定。

22. 发明申请

WO2009108806A1 CONJUGATED FACTOR VIII MOLECULES 审中-公开
标题翻译：结合因子VIII分子
公开(公告)号：WO2009108806A1
公开(公告)日：2009-09-03
申请号：PCT/US2009/035339
申请日：2009-02-26
申请人： NOVO NORDISK A/S , DEFREES, Shawn
发明人： DEFREES, Shawn
IPC分类号： A61K47/48 , A61P7/04
CPC分类号： C12N9/96 , A61K38/00 , A61K47/26 , A61K47/60 , C07K14/755
摘要： The present invention relates to B-domain truncated Factor VIII molecules with a modified circulatory half life, said molecule being covalently conjugated with a hydrophilic polymer. The invention furthermore relates to methods for obtaining such molecules as well as use of such molecules.
摘要翻译：本发明涉及具有修饰的循环半衰期的B结构域截短的因子VIII分子，所述分子与亲水性聚合物共价共轭。本发明还涉及获得这种分子的方法以及这种分子的使用。

23. 发明申请

WO2009075778A3 NONPEPTIDIC INHIBITORS OF CRUZAIN 审中-公开
公开(公告)号：WO2009075778A3
公开(公告)日：2009-06-18
申请号：PCT/US2008/013400
申请日：2008-12-05
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , ELLMAN, Jonathan, A. , BRAK, Katrien
发明人： ELLMAN, Jonathan, A. , BRAK, Katrien
IPC分类号： C07D249/10 , C07D249/12
摘要： Cruzain is the major cysteine protease of T. cruzi , which is the causative agent of Chagas' disease and is a promising target for the development of new chemotherapy. With the goal of developing potent nonpeptidic inhibitors of cruzain, the Substrate Activity Screening (SAS) method was used to screen a library of protease substrates initially designed to target the homologous human protease cathepsin S. Structure-based design was next used to further improve substrate cleavage efficiency by introducing additional binding interactions in the S3 pocket of cruzain. The optimized substrates were then converted to inhibitors by the introduction of cysteine protease mechanism-based pharmacophores. Inhibitor (38) was determined to be reversible even though it incorporated the vinyl sulfone pharmacophore that is well documented to give irreversible cruzain inhibition for peptidic inhibitors. The previously unexplored β-chloro vinyl sulfone pharmacophore provided mechanistic insight that led to the development of potent irreversible acyl- and aryl- oxymethyl ketone cruzain inhibitors. For these inhibitors, potency did not solely depend on leaving group pTa, with 2,3,5,6-tetrafluorophenoxy methyl ketone (54) identified as one of the most potent inhibitors with a second order inactivation constant of 147,000 s -1 M -1 . This inhibitor completely eradicated the T. cruzi parasite from mammalian cell cultures and consequently has the potential to lead to new chemo therapeutics for Chagas' disease.

24. 发明申请

WO2009020814A2 FUSED HETEROCYCLES 审中-公开
标题翻译：融合的杂项
公开(公告)号：WO2009020814A2
公开(公告)日：2009-02-12
申请号：PCT/US2008/071642
申请日：2008-07-30
申请人： SEPRACOR INC. , HEFFERNAN, Michele, L.R. , DORSEY, James, M. , FANG, Qun, Kevin , FOGLESONG, Robert, J. , HOPKINS, Seth, C. , OGBU, Cyprian, O. , SOUKRI, Mustapha , SPEAR, Kerry, L.
发明人： HEFFERNAN, Michele, L.R. , DORSEY, James, M. , FANG, Qun, Kevin , FOGLESONG, Robert, J. , HOPKINS, Seth, C. , OGBU, Cyprian, O. , SOUKRI, Mustapha , SPEAR, Kerry, L.
IPC分类号： A61K31/407
CPC分类号： A61K31/407 , C07D491/04 , C07D495/04
摘要： This invention provides fused heterocycles having the formula: in which R 1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R 2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R 3 is a member selected from the group consisting of H 1 C 1 -C 6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R 4 is a member selected from OH and O - X + , in which X + is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4. Formulae A, B.
摘要翻译：本发明提供具有下式的稠合杂环：其中R 1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R 2是选自由H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基组成的组中的成员。 R 3是选自下组的成员：H 1 -C 1 -C 6取代或未取代的烷基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基。 R 4是选自OH和O - + X - +的成员，其中X + +是正离子，其中是选自有机正离子和无机正离子的成员。取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。索引n是从1到4的整数。公式A，B。

25. 发明申请

WO2008057683A3 METHODS FOR THE PURIFICATION OF POLYPEPTIDE CONJUGATES 审中-公开
公开(公告)号：WO2008057683A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/080353
申请日：2007-10-03
申请人： NEOSE TECHNOLOGIES, INC. , DEFREES, Shawn , KINEALY, Kyle
发明人： DEFREES, Shawn , KINEALY, Kyle
IPC分类号： C07K1/10 , C07K1/18 , C07K1/20 , C07K14/51
摘要： The present invention provides processes for the manufacturing of polypeptide conjugates. In particular, the invention provides methods for the purification of polypeptide conjugates, which include at least one polymeric modifying groups, such as a poly(alkylene oxide) moiety. Exemplary poly(alkylene oxide) moieties include poly(ethylene glycol) (PEG) and poly(propylene glycol). In an exemplary process, hydrophobic interaction chromatography (HIC) is used to resolve different glycoforms of glycoPEGylated polypeptides.

26. 发明申请

WO2008019196A2 CARBOMETALLATION OF ALKYNES AND IMPROVED SYNTHSIS OF UBIQUINONES 审中-公开
标题翻译：烷基碳原子的加成反应及对泛基葡聚糖的合成
公开(公告)号：WO2008019196A2
公开(公告)日：2008-02-14
申请号：PCT/US2007/071411
申请日：2007-06-15
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , LIPSHUTZ, Bruce, H.
发明人： LIPSHUTZ, Bruce, H.
IPC分类号： C07F5/06
CPC分类号： C07D213/69
摘要： Methods for the carbometallation of alkynes are presented. Those are useful for the synthesis of CoQ 10 and other ubiquinones as well as for the synthesis of ubiquinol analogs.
摘要翻译：介绍了炔烃金属化的方法。这些对于合成辅酶Q10和其他泛醌以及合成泛醌类似物是有用的。

27. 发明申请

WO2006105426A2 MANUFACTURING PROCESS FOR THE PRODUCTION OF PEPTIDES GROWN IN INSECT CELL LINES 审中-公开
标题翻译：在细胞系中生产肽的制造工艺
公开(公告)号：WO2006105426A2
公开(公告)日：2006-10-05
申请号：PCT/US2006/012013
申请日：2006-03-30
申请人： NEOSE TECHNOLOGIES, INC. , KANG, Yun , WILLETT, Walter, Scott , KLIMEK, Thomas, J. , CAMPBELL, Basil, Amir , CINO, Paul, M. , THOMAS, Bradley , BERMEL, John, V. , CHEN, Chun-Chiang
发明人： KANG, Yun , WILLETT, Walter, Scott , KLIMEK, Thomas, J. , CAMPBELL, Basil, Amir , CINO, Paul, M. , THOMAS, Bradley , BERMEL, John, V. , CHEN, Chun-Chiang
IPC分类号： C12P21/06 , C12N9/24 , C12N5/06 , C07K14/53 , C07K14/51
CPC分类号： C07K14/535 , C07K1/20 , C07K14/505 , C07K14/51 , C07K14/53 , C12N9/1081 , C12P21/02 , C12Y204/99003
摘要： The present invention provides a manufacturing method for the production of peptides that are grown in insect cell lines. The peptides are grown in insect cell cultures that are infected with baculovirus particles in a culture supplemented with a lipid mixture. The peptides are then isolated from the insect cell culture using a method that employs a tangential flow filtration cascade. The isolated peptides are glycopeptides having an insect specific glycosylation pattern. The glycopeptides may then be conjugated to a modifying group via linkage through a glycosyl linking group interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from glycosylated peptides by the action of a glycosyltransferase.
摘要翻译：本发明提供了生产在昆虫细胞系中生长的肽的制备方法。这些肽在补充有脂质混合物的培养物中被杆状病毒颗粒感染的昆虫细胞培养物中生长。然后使用采用切向流过滤级联的方法从昆虫细胞培养物中分离肽。分离的肽是具有昆虫特异性糖基化模式的糖肽。然后可以通过插入在肽和修饰基团之间并且共价连接到肽和修饰基团上的糖基连接基团通过连接将糖肽与修饰基团缀合。通过糖基转移酶的作用由糖基化肽形成缀合物。

28. 发明申请

WO2006081384A2 HETEROGENEOUS COPPER CATALYSTS 审中-公开
标题翻译：异构铜催化剂
公开(公告)号：WO2006081384A2
公开(公告)日：2006-08-03
申请号：PCT/US2006/002854
申请日：2006-01-26
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , LIPSHUTZ, Bruce, H.
发明人： LIPSHUTZ, Bruce, H.
IPC分类号： C01B25/26
CPC分类号： B01J37/06 , B01J21/18 , B01J23/72 , B01J31/1616 , B01J31/24 , B01J37/0201 , B01J2231/32 , B01J2231/34 , B01J2531/16
摘要： The present invention provides a class of heterogeneous copper catalysts that catalyze the addition of various species across an unsaturated system (e.g., C-C and C-heteroatom systems), the additions occurring in a 1,2- or 1,4-manner. Also provided are methods of using the catalysts to perform the additions and methods of making the catalysts themselves.
摘要翻译：本发明提供了一类异种铜催化剂，其催化跨越不饱和体系（例如C-C和C - 杂原子体系）添加各种物质，添加物以1,2-或1,4-方式存在。还提供了使用催化剂进行添加的方法和制备催化剂本身的方法。

29. 发明申请

WO2005014779A3 CYCLODEXTRIN AFFINITY PURIFICATION 审中-公开
公开(公告)号：WO2005014779A3
公开(公告)日：2005-02-17
申请号：PCT/US2004/013841
申请日：2004-05-05
申请人： NEOSE TECHNOLOGIES, INC. , VILLAFRANCA, Joseph, John , HAKES, David, James , JOHNSON, Karl, Frank , WILLET, Walter, Scott, Jr. , MEYERS, Chester, A.
发明人： VILLAFRANCA, Joseph, John , HAKES, David, James , JOHNSON, Karl, Frank , WILLET, Walter, Scott, Jr. , MEYERS, Chester, A.
IPC分类号： C12P21/06
摘要： A method of immobilizing a molecular species that include a starch-binding domain is provided. There also is provided a material upon which the molecular species is immobilized, and a material that is capable of immobilizing the species The method includes binding the species to a solid support, e.g., membranes, chromatographic supports and the like. The immobilized species is optionally purified by the method of the invention. Alternatively, the immobilized species is use in another method, such as in a synthesis as a synthetic reagent, or to purify another species that has an affinity for the immobilized species. Exemplary immobilized molecular species include bioactive agents, and biomolecules.

30. 发明申请

WO2004103275A3 COMPOSITIONS AND METHODS FOR THE PREPARATION OF HUMAN GROWTH HORMONE GLYCOSYLATION MUTANTS 审中-公开
公开(公告)号：WO2004103275A3
公开(公告)日：2004-12-02
申请号：PCT/US2004/014254
申请日：2004-05-07
申请人： NEOSE TECHNOLOGIES, INC. , DEFREES, Shawn , CLAUSEN, Henrik
发明人： DEFREES, Shawn , CLAUSEN, Henrik
IPC分类号： A61K38/18 , C07K14/475 , C12N5/10 , C12N15/18 , C12N15/63
摘要： The present invention relates to mutants of human growth hormone, which contain newly introduced N-linked or O-linked glycosylation site(s), such that these recombinantly produced polypeptides have glycosylation patterns distinctly different from that of the naturally occurring human growth hormone. The polynucleotide coding sequences for the mutants, expression cassettes comprising the coding sequences, cells expressing the mutants, and methods for producing the mutants are also disclosed. Further disclosed are pharmaceutical compositions comprising the mutants and method for using the mutants.

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