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11. 发明专利

AU7175094A Inhibition of interferon-gamma with oligonucleotides 未知
公开(公告)号：AU7175094A
公开(公告)日：1995-01-17
申请号：AU7175094
申请日：1994-06-17
申请人： PHARMAGENICS INC
发明人： COPPOLA GEORGE R , BEUTEL BRUCE A , BERTELSEN ARTHUR H
IPC分类号： C12N15/113 , C07H21/02 , C07H21/04 , C12Q1/68 , G01N33/50

12. 发明专利

CA2153057A1 NOVEL OLIGONUCLEOTIDES MODIFIED WITH NON-NUCLEOTIDE BRIDGING GROUPS 未知
公开(公告)号：CA2153057A1
公开(公告)日：1994-07-21
申请号：CA2153057
申请日：1994-01-13
申请人： PHARMAGENICS INC
发明人： COOK ALAN F , COHEN JACK S , GAO HETIAN
IPC分类号： C07H21/00 , A61K31/70 , A61K48/00
摘要： An oligonucleotide having a structural formula selected from the group consisting of (a) and (b). S1, S2, S3, S4, and S5 are oligonucleotide strands, and each of X1 and X2 is a bridging moiety which may be a nucleotide strand or a non-nucleotide bridging moiety. Each of X1 and X2 may be the same or different, with the proviso that when one of X1 and X2 is a nucleotide strand, the other of X1 and X2 is a non-nucleotide bridging moiety. Each of X1 and X2 independently is a bridging moiety having first and second termini that each binds independently with a nucleotide phosphate moiety or a nucleotide hydroxyl moiety. Such oligonucleotides are designed to have increased resistance to exonucleases and endonucleases, greater thermal stabilities, improved cellular uptake, and improved binding to target proteins and nucleic acids.

13. 发明专利

AU1753297A Non-nucleotide phosphorous ester oligomers 未知
公开(公告)号：AU1753297A
公开(公告)日：1997-08-22
申请号：AU1753297
申请日：1997-01-22
申请人： PHARMAGENICS INC
发明人： GENTLES ROBERT G , COOK ALAN F , RUDOLPH MORRIS J , FATHI REZA
IPC分类号： C07F9/08 , A61K31/66 , A61K31/661 , A61K31/6615 , C07B61/00 , C07F9/141 , C07F9/143 , C07F9/145 , C07F9/24 , C07F9/572 , C07F9/58 , C07F9/6506 , C07F9/6509 , C07F9/6512 , C07F9/6539 , C07F9/655 , C07F9/6561

14. 发明专利

GR3022473T3 Sequence specific DNA binding by P53 未知
公开(公告)号：GR3022473T3
公开(公告)日：1997-05-31
申请号：GR970400120
申请日：1997-02-05
申请人： UNIV JOHNS HOPKINS , PHARMAGENICS INC
发明人： VOGELSTEIN BERT , KINZLER KENNETH W , SHERMAN MICHAEL I
IPC分类号： A61B10/00 , C07K14/47 , C12N15/09 , C12P21/08 , C12Q1/02 , C12Q1/68 , G01N33/50 , G01N33/53 , G01N33/574 , G01N33/577 , G01N33/68 , A61K48/00 , C07H21/04 , C12Q1/70
摘要： Specific sequences in the human genome are the sites of strong binding of wild-type p53 protein, but not mutant forms of the protein. These sequences are used diagnostically to detect cells in which the These sequences are used diagnostically to detect cells in which the amount of wild-type p53 is diminished. The sequences can also be used to screen for agents which correct for loss of wild-type p53 to DNA in cancer cells.

15. 发明专利

CA2155930A1 VECTORS AND VECTOR SYSTEMS INCLUDING GENES ENCODING TUMOR SUPPRESSOR PROTEINS AND PRODUCER CELLS TRANSFORMED THEREBY 未知
公开(公告)号：CA2155930A1
公开(公告)日：1995-06-22
申请号：CA2155930
申请日：1994-12-09
申请人： PHARMAGENICS INC , GENZYME CORP
发明人： BEAUDRY GARY A , BERTELSEN ARTHUR H , SHERMAN MICHAEL I , VOGELSTEIN BERT
IPC分类号： C07K14/47 , C12N15/86 , A61K48/00 , C12N5/10 , C12N15/11
摘要： Vectors and vector systems are embodied that include a gene encoding a tumor suppressor protein. In one embodiment, the vector includes a gene encoding a tumor suppressor protein and an inducible promoter controlling the gene encoding a tumor suppressor protein. The tumor suppressor protein may be p53 protein. In another embodiment, there is provided a vector system which comprises a first vector including a gene encoding a tumor suppressor protein, and a second vector containing a nucleic acid sequence encoding an antisense sequence complementary to all or a portion of the gene encoding a tumor suppressor protein. In yet another embodiment, there is provided a vector system which comprises a first vector including a gene encoding a tumor suppressor protein, and a second vector containing a gene which encodes a protein which binds to, and thereby inhibits, the tumor suppressor protein. Such vectors and vector systems enable cells transformed thereby to continue to proliferate such that adequate amounts of infectious viral particles, generated from viral vectors including a gene encoding a tumor suppressor protein, can be harvested for administration to patients.

16. 发明专利

AU7717094A Methods for isolation of most abundant oligonucleotides from complex mixtures 未知
公开(公告)号：AU7717094A
公开(公告)日：1995-03-22
申请号：AU7717094
申请日：1994-08-26
申请人： PHARMAGENICS INC
发明人： BEUTEL BRUCE A , COPPOLA GEORGE R , SHERMAN MICHAEL I , COOK ALAN F , FATHI REZA , GAO HETIAN , RUDOLPH M JONATHAN , BERTELSEN ARTHUR H
IPC分类号： C07H21/00 , C12Q1/68 , C12Q1/6811 , C12Q1/6813 , C07H21/02 , C07H21/04

17. 发明申请

WO1997028168A1 NON-NUCLEOTIDE PHOSPHOROUS ESTER OLIGOMERS 审中-公开
标题翻译：非核苷酸磷酸酯低聚物
公开(公告)号：WO1997028168A1
公开(公告)日：1997-08-07
申请号：PCT/US1997001060
申请日：1997-01-22
申请人： PHARMAGENICS, INC.
发明人： PHARMAGENICS, INC. , GENTLES, Robert, G. , COOK, Alan, F. , RUDOLPH, Morris, J. , FATHI, Reza
IPC分类号： C07F09/58
CPC分类号： C07F9/65616 , C07F9/1411 , C07F9/143 , C07F9/145 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/5728 , C07F9/58 , C07F9/6506 , C07F9/650952 , C07F9/6539 , C07F9/65515 , C07F9/6561 , C40B40/00 , Y02P20/55
摘要： A phosphorus ester oligomer having structure (I) wherein A can be the same or different in each monomeric unit and each is independently selected from the group consisting of oxygen, sulfur, lower alkyl, substituted or unsubstituted alkylamino, substituted or unsubstituted arylamino and aminoalkyl; B1 and B2 can be the same or different and each is independently selected from hydrogen, lower alkyl, a labelling group, a protecting group, a phosphoramidate or a phosphomonoester; R1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R1 is independently selected from the group consisting of a condensation product of (i) a non-vicinal diol attached to a hydrogen bond donor functionality; (ii) a hydrogen bond acceptor selected from an ether, a purine or pyrimidine substituted 1,2-diol or a disubstituted heterocycle; (iii) a non-vicinal diol attached to a hydrophobic functionality or a vicinal diol attached to an aliphatic or alicyclic hydrophobic functionality; (iv) a diol attached to a ring substituted anionic functionality and (v) a cationic moiety attached to a non-vicinal or alicyclic diol, any of which can further include a detectable label, and n is at least one. Preferred R1 moieties include condensation products of heterocyclic diols, alicyclic diols, and polycyclic diols. Also the non-nucleotide monomers thereof, combinatorial library mixtures of the oligomers and the use of the oligomers as selective target-binding compounds.
摘要翻译：具有结构（I）的磷酯低聚物，其中A在每个单体单元中可以相同或不同，并且各自独立地选自氧，硫，低级烷基，取代或未取代的烷基氨基，取代或未取代的芳基氨基和氨基烷基; B1和B2可以相同或不同，各自独立地选自氢，低级烷基，标记基团，保护基，氨基磷酸酯或磷酸酯酯; R 1可以在每个单体单元中相同或不同，并且在至少一个非核苷酸单体单元中，R 1独立地选自以下组中的缩合产物：（i）连接于氢的非连位二醇债券供体功能; （ii）选自醚，嘌呤或嘧啶取代的1,2-二醇或二取代杂环的氢键受体; （iii）连接到疏水官能团的非连位二醇或连接到脂族或脂环族疏水官能团的连位二醇; （iv）连接到环取代的阴离子官能团的二醇和（v）连接到非邻位或脂环族二醇上的阳离子部分，其中任何一个可以进一步包括可检测标记，并且n是至少一个。优选的R1部分包括杂环二醇，脂环族二醇和多环二醇的缩合产物。还有其非核苷酸单体，低聚物的组合文库混合物以及低聚物作为选择性靶结合化合物的用途。

18. 发明申请

WO1995027072A1 DETERMINATION AND IDENTIFICATION OF ACTIVE COMPOUNDS IN A COMPOUND LIBRARY 审中-公开
标题翻译：活性化合物在化合物库中的测定和鉴定
公开(公告)号：WO1995027072A1
公开(公告)日：1995-10-12
申请号：PCT/US1995004098
申请日：1995-04-03
申请人： PHARMAGENICS, INC.
发明人： PHARMAGENICS, INC. , BEUTEL, Bruce, A.
IPC分类号： C12P19/34
CPC分类号： C07K1/047 , C07H21/00 , Y10S435/962
摘要： Libraries of compounds such as nucleic acids or peptides are contacted with a target molecule and libraries that have at least one compound that binds with at least a minimum activity are determined by a reiterative process in which a change in the rate of recorvery (elimination) of compounds that bind to the target indicates that the library contains such a compound. The procedure may also be used to determine indirectly the sequence of such compound by employing sublibraries, each of which has a known entity at a known position of the compound.
摘要翻译：诸如核酸或肽的化合物的文库与目标分子接触，并且具有至少一种与至少最低活性结合的化合物的文库通过重复方法来确定，其中，修复（消除）结合靶标的化合物表明文库含有这种化合物。该方法还可以用于间接地通过使用亚文库来确定这种化合物的序列，其中每一个在化合物的已知位置具有已知的实体。

19. 发明申请

WO1994029479A1 OLIGONUCLEOTIDES WHICH INHIBIT HIV PROTEASE FUNCTION 审中-公开
标题翻译：抑制艾滋病病毒功能的寡核苷酸
公开(公告)号：WO1994029479A1
公开(公告)日：1994-12-22
申请号：PCT/US1994006456
申请日：1994-06-09
申请人： PHARMAGENICS, INC. , BEUTEL, Bruce, A. , SHERMAN, Michael, I. , COPPOLA, George, R.
发明人： PHARMAGENICS, INC.
IPC分类号： C12Q01/00
CPC分类号： C07H21/00 , C07K14/00
摘要： A method of inhibiting HIV protease function which comprises administering to a host an effective amount of an oligonucleotide which inhibits HIV protease function. Preferred oligonucleotides are RNA oligonucleotides which include at least one of the following oligonucleotide sequences: (a) 5' - GGAAAGUGGAC - 3'; (b) 5' - AANGU - 3'; and (c) 5' - ANUGGA - 3'; (d) 5' - GGAAAGUGGACRRR - 3'; (e) 5' - RGUGAGUGUGGGCR - 3'; (f) 5' - RGUGAGUGUGGGGCR - 3'; (g) 5' - AGUGUG - 3'; (h) 5' - UNGAUNY - 3'; (i) 5' - CCUC - 3'; and (j) 5' - GGUGNA - 3', wherein A is modified or unmodified adenine, C is modified or unmodified cytosine, G is modified or unmodified guanine, U is modified or unmodified uracil, R is modified or unmodified purine, Y is modified or unmodified pyrimidine, and N is modified or unmodified adenine, cytosine, guanine, or uracil. The oligonucleotide may include a looped region bounded by a base-paired stem region, and at least a portion of at least one of sequences (a) through (j) is contained in the looped region. Such oligonucleotides bind to HIV protease, thereby inhibiting HIV protease function and preventing HIV maturation.
摘要翻译：一种抑制HIV蛋白酶功能的方法，其包括向宿主施用有效量的抑制HIV蛋白酶功能的寡核苷酸。优选的寡核苷酸是RNA寡核苷酸，其包括以下寡核苷酸序列中的至少一个：（a）5'-GGAAAGUGGAC-3'; （b）5' - AANGU - 3'; 和（c）5' - ANUGGA-3'; （d）5' - GGAAAGUGGACRRR-3'; （e）5' - RGUGAGUGUGGGCR-3'; （f）5' - RGUGAGUGUGGGGCR-3'; （g）5' - AGUGUG - 3'; （h）5' - UNGAUNY - 3'; （i）5'-CCCUC-3'; 和（j）5'-GGUGNA-3'，其中A是修饰或未修饰的腺嘌呤，C是修饰的或未修饰的胞嘧啶，G是修饰的或未修饰的鸟嘌呤，U是修饰的或未修饰的尿嘧啶，R是修饰的或未修饰的嘌呤，Y是修饰或未修饰的嘧啶，N是修饰的或未修饰的腺嘌呤，胞嘧啶，鸟嘌呤或尿嘧啶。寡核苷酸可以包括由碱基配对的茎区限定的环状区域，并且在环状区域中包含序列（a）至（j）中的至少一个序列的至少一部分。这样的寡核苷酸结合HIV蛋白酶，从而抑制HIV蛋白酶功能并防止HIV成熟。

20. 发明申请

WO1995000528A1 INHIBITION OF BASIC FIBROBLAST GROWTH FACTOR WITH OLIGONCULEOTIDES 审中-公开
标题翻译：基础成纤维细胞生长因子与寡核苷酸的抑制作用
公开(公告)号：WO1995000528A1
公开(公告)日：1995-01-05
申请号：PCT/US1994006884
申请日：1994-06-17
申请人： PHARMAGENICS, INC.
发明人： PHARMAGENICS, INC. , BEUTEL, Bruce, A. , JOESTEN, Michael, E.
IPC分类号： C07H21/02
CPC分类号： C12N15/1136 , C12N2310/13 , C12N2310/321
摘要： Oligonucleotides and analogs thereof that bind to and modulate the activity of basic fibroblast growth factor and methods for their use, including therapeutic and diagnostic methods.
摘要翻译：结合并调节碱性成纤维细胞生长因子的活性的寡核苷酸及其类似物及其使用方法，包括治疗和诊断方法。

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