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1. 发明申请

WO2004099131A3 COMPOUNDS HAVING A FUSED, BICYCLIC MOIETY FOR BINDING TO THE MINOR GROOVE OF DSDNA 审中-公开
标题翻译：具有融合的双链体系的化合物用于与DSDNA的小型细胞结合
公开(公告)号：WO2004099131A3
公开(公告)日：2005-02-17
申请号：PCT/US2004013285
申请日：2004-04-29
申请人： PHARMACIA CORP , PHILLION DENNIS P , BASHKIN JAMES K
发明人： PHILLION DENNIS P , BASHKIN JAMES K
IPC分类号： C07D20060101 , C07D235/04 , C07D401/00 , C07D403/02 , C07H19/04 , C07H21/04 , C12Q1/68
CPC分类号： C07D417/14 , C07D403/14 , C07D471/04 , C07H19/04 , C07H21/04
摘要： The present invention is directed to the means by which to alter the binding affinity and/or specificity of a compound with a sequence of DNA in the minor groove of a double-strand thereof. More particularly, the present invention is directed to a synthetic and/or non-naturally occurring compound (e.g., an analog of a polyamide oligomer or polymer) which contains at least one hydrogen bond donor moiety and at least one hydrogen bond acceptor moiety, wherein the latter moiety or "building block" has a fused, bicyclic structure which is heteroaromatic, said structure having a heteroatom therein which acts as a hydrogen bond acceptor to bind guanine in the minor groove of the dsDNA sequence, and which is incapable of forming a tautomer. In one particular embodiment of the synthetic and/or non-naturally occurring compound, the fused, bicyclic structure occupies an initial or first terminal position within the compound.
摘要翻译：本发明涉及在双链的小槽中改变化合物与DNA序列的结合亲和力和/或特异性的方法。更具体地，本发明涉及含有至少一个氢键供体部分和至少一个氢键受体部分的合成和/或非天然存在的化合物（例如，聚酰胺低聚物或聚合物的类似物），其中后一部分或“构建块”具有杂芳族化合物的稠合双环结构，所述结构在其中具有杂原子，其作为氢键受体以在dsDNA序列的小沟中结合鸟嘌呤，并且不能形成互变异构体。在合成和/或非天然存在的化合物的一个具体实施方案中，稠合双环结构占据化合物内的初始或第一末端位置。

2. 发明申请

WO2003040337A3 POLYAMIDE MODULATORS OF COX2 TRANSCRIPTION 审中-公开
公开(公告)号：WO2003040337A3
公开(公告)日：2003-05-15
申请号：PCT/US2002/035718
申请日：2002-11-07
申请人： PHARMACIA CORPORATION , PHILLION, Dennis, P. , CROWLEY, Kathleen, S. , BASHKIN, James, K. , SCHWEITZER, Barbara, A. , BURNETTE, Barry, L. , WOODARD, Scott, S.
发明人： PHILLION, Dennis, P. , CROWLEY, Kathleen, S. , BASHKIN, James, K. , SCHWEITZER, Barbara, A. , BURNETTE, Barry, L. , WOODARD, Scott, S.
IPC分类号： C07D231/02
摘要： Processes and compositions are provided for regulating COX2 gene expression in a cell. The process includes selecting a polyamide composition comprising N-methyl pyrrole (Py) and N-methyl imidazole (Im) to provide specific binding to DNA at a COX2 gene target site in a cell. The polyamide is then combined with the cell containing the COX2 gene, wherein the polyamide binds to the COX2 gene promoter target site and regulates transcription of the COX2 gene.

3. 发明申请

WO03041128A2 METHODS OF PROMOTING UPTAKE AND NUCLEAR ACCUMULATION OF POLYAMIDES IN EUKARYOTIC CELLS 审中-公开
标题翻译：促肾上腺皮质激素摄取和核聚集的方法
公开(公告)号：WO03041128A2
公开(公告)日：2003-05-15
申请号：PCT/US0235587
申请日：2002-11-07
申请人： PHARMACIA CORP , CROWLEY KATHLEEN S , BASHKIN JAMES K , SCHWEITZER BARBARA A , PHILLION DENNIS P
发明人： CROWLEY KATHLEEN S , BASHKIN JAMES K , SCHWEITZER BARBARA A , PHILLION DENNIS P
IPC分类号： C12N1/00 , A61K31/275 , A61K31/40 , A61K31/495 , A61K38/00 , A61K45/00 , A61K48/00 , A61P43/00 , C12N15/63 , H01L
CPC分类号： C12N15/63 , A61K31/275 , A61K31/40 , A61K31/495
摘要： A method for enhancing cellular uptake and redistributing gene regulating polyamides from the extranuclear areas in eukaryotic cells to the nucleus thereof. The method consists of administering to the eukaryotic cells a molecular trafficking compound. The administered molecular trafficking compound affects cellular pathways and mechanisms that accumulate polyamides in cytoplasmic vessicles and/or efflux polyamides from the intracellular regions of cell. The method also includes modifying polyamides to contain negatively-charged or acidic moieties wherein the moieties inhibit the accumulation of polyamides in cellular lysosomes. By affecting the cellular pathways and mechanisms, the polyamides are redistributed throughout the cell, whereby nuclear accumulation of the polyamides is enhanced.
摘要翻译：一种用于增强细胞摄取并将基因调节聚酰胺从真核细胞的核外区重新分布到其核的方法。该方法包括向真核细胞施用分子运输化合物。所施用的分子运输化合物影响细胞途径和机制，其在细胞质容器中积聚聚酰胺和/或从细胞的细胞内区域流出聚酰胺。该方法还包括改性聚酰胺以含有带负电荷或酸性部分，其中所述部分抑制聚酰胺在细胞溶酶体中的积聚。通过影响细胞途径和机制，聚酰胺在整个细胞中重新分布，从而增强了聚酰胺的核聚集。

4. 发明申请

WO2003020684A1 (ALPHA)-HALOENAMINE REAGENTS 审中-公开
标题翻译：（ALPHA）-HALOENAMINE试剂
公开(公告)号：WO2003020684A1
公开(公告)日：2003-03-13
申请号：PCT/US2002/025609
申请日：2002-08-13
申请人： PHARMACIA CORPORATION , PHILLION, Dennis, P.
发明人： PHILLION, Dennis, P.
IPC分类号： C07C211/24
CPC分类号： C07D403/14 , C07B2200/11 , C07C17/16 , C07C205/57 , C07C209/74 , C07C269/06 , C07C303/02 , C07D207/34 , C07D233/90 , C07D307/68 , C07F9/12 , C07F9/1406 , C07F9/4015 , C07F9/4075 , C07F9/42 , C07F9/4465 , C08F8/30 , C07C211/24 , C07C271/22 , C07C309/86
摘要： The present invention describes immobilized haloenamine reagents, immobilized tertiary amides, methods for their preparation, and methods of use.
摘要翻译：本发明描述了固定的卤代胺试剂，固定的叔酰胺，其制备方法和使用方法。

5. 发明申请

WO2005033282A2 POLYAMIDE COMPOSITIONS AND THERAPEUTIC METHODS FOR TREATMENT OF HUMAN PAPILLOMA VIRUS 审中-公开
标题翻译：聚酰胺组合物和治疗人类斑马鱼病毒的治疗方法
公开(公告)号：WO2005033282A2
公开(公告)日：2005-04-14
申请号：PCT/US2004/032138
申请日：2004-09-30
申请人： PHARMACIA & UPJOHN COMPANY LLC , FISHER, Chris , BASHKIN, James, K. , CROWLEY, Kathleen, S. , SVERDRUP, Francis, M. , GARNER-HAMRICK, Peggy, A. , PHILLION, Dennis, P.
发明人： FISHER, Chris , BASHKIN, James, K. , CROWLEY, Kathleen, S. , SVERDRUP, Francis, M. , GARNER-HAMRICK, Peggy, A. , PHILLION, Dennis, P.
IPC分类号： C12N
CPC分类号： A61K31/785 , A61K9/0014 , A61K9/0034 , C12N2710/20011
摘要： Processes and compositions are provided for regulating replication in a human papilloma virus. The process includes selecting a polyamide composition comprising N-methyl pyrrole (Py) and either des-amino-N-methyl imidazole ( d Im) or a fused, non-tautomerizing heteroaromatic bicyclic structure (L) that contains at least one hydrogen bond acceptor moiety, to provide specific binding to DNA at the E1 binding site in a human papilloma virus episome. The polyamide is then combined with the cell containing a human papilloma virus, wherein the polyamide binds to the human papilloma virus E1 binding site and regulates replication of the human papilloma virus.
摘要翻译：提供了用于调节人乳头状瘤病毒复制的方法和组合物。该方法包括选择包含N-甲基吡咯（Py）和去氨基-N-甲基咪唑（dm1）的聚酰胺组合物或包含至少一个氢的稠合的，非互变异构的杂芳族双环结构（L）键受体部分，以在人乳头状瘤病毒附加体中的E1结合位点提供与DNA的特异性结合。然后将聚酰胺与含有人乳头瘤病毒的细胞组合，其中聚酰胺结合人乳头状瘤病毒E1结合位点并调节人乳头状瘤病毒的复制。

6. 发明申请

WO03018552A3 AROMATIC AND HETEROAROMATIC ACID HALIDES FOR SYNTHESIZING POLYAMIDES 审中-公开
标题翻译：芳香和杂芳酸用于合成聚酰胺
公开(公告)号：WO03018552A3
公开(公告)日：2003-05-30
申请号：PCT/US0227953
申请日：2002-08-30
申请人： PHARMACIA CORP , PHILLION DENNIS P
发明人： PHILLION DENNIS P
IPC分类号： C07C17/16 , C07C17/18 , C07C19/01 , C07C23/08 , C07C51/56 , C07C53/40 , C07C53/42 , C07C63/10 , C07C65/03 , C07C65/05 , C07C201/14 , C07C205/57 , C07C209/00 , C07C209/74 , C07C211/24 , C07C211/29 , C07C269/06 , C07C271/22 , C07C303/02 , C07C303/38 , C07C309/86 , C07C311/16 , C07D207/34 , C07D207/416 , C07D233/90 , C07D307/68 , C07D309/10 , C07D403/14 , C07F7/12 , C07F7/18 , C07F9/12 , C07F9/14 , C07F9/40 , C07F9/42 , C07F9/44 , C08F8/30
CPC分类号： C07D403/14 , C07B2200/11 , C07C17/16 , C07C205/57 , C07C209/74 , C07C269/06 , C07C303/02 , C07D207/34 , C07D233/90 , C07D307/68 , C07F9/12 , C07F9/1406 , C07F9/4015 , C07F9/4075 , C07F9/42 , C07F9/4465 , C08F8/30 , C07C211/24 , C07C271/22 , C07C309/86
摘要： The present invention is directed to protected amino acid halide monomers and oligomers, and to their use in the efficient sythesis of polyamides. The present invention is further directed to the use of -haloenamine reagents, which may optionally be immobilized, for the preparation of the amino acid halides.
摘要翻译：本发明涉及被保护的氨基酸卤化物单体和低聚物，并涉及它们在聚酰胺的有效合成中的用途。本发明进一步涉及可任选地固定化的N-卤代苯胺试剂用于制备氨基酸卤化物的用途。

7. 发明申请

WO2003041128A3 METHODS OF PROMOTING UPTAKE AND NUCLEAR ACCUMULATION OF POLYAMIDES IN EUKARYOTIC CELLS 审中-公开
公开(公告)号：WO2003041128A3
公开(公告)日：2003-05-15
申请号：PCT/US2002/035587
申请日：2002-11-07
申请人： PHARMACIA CORPORATION , CROWLEY, Kathleen, S. , BASHKIN, James, K. , SCHWEITZER, Barbara, A. , PHILLION, Dennis, P.
发明人： CROWLEY, Kathleen, S. , BASHKIN, James, K. , SCHWEITZER, Barbara, A. , PHILLION, Dennis, P.
IPC分类号： A61K38/00
摘要： A method for enhancing cellular uptake and redistributing gene regulating polyamides from the extranuclear areas in eukaryotic cells to the nucleus thereof. The method consists of administering to the eukaryotic cells a molecular trafficking compound. The administered molecular trafficking compound affects cellular pathways and mechanisms that accumulate polyamides in cytoplasmic vessicles and/or efflux polyamides from the intracellular regions of cell. The method also includes modifying polyamides to contain negatively-charged or acidic moieties wherein the moieties inhibit the accumulation of polyamides in cellular lysosomes. By affecting the cellular pathways and mechanisms, the polyamides are redistributed throughout the cell, whereby nuclear accumulation of the polyamides is enhanced.

8. 发明申请

WO2003040337A2 POLYAMIDE MODULATORS OF COX2 TRANSCRIPTION 审中-公开
标题翻译： COX2转录酶的多胺调节剂
公开(公告)号：WO2003040337A2
公开(公告)日：2003-05-15
申请号：PCT/US2002/035718
申请日：2002-11-07
申请人： PHARMACIA CORPORATION , PHILLION, Dennis, P. , CROWLEY, Kathleen, S. , BASHKIN, James, K. , SCHWEITZER, Barbara, A. , BURNETT, Barry, L. , WOODARD, Scott, S.
发明人： PHILLION, Dennis, P. , CROWLEY, Kathleen, S. , BASHKIN, James, K. , SCHWEITZER, Barbara, A. , BURNETT, Barry, L. , WOODARD, Scott, S.
IPC分类号： C12N
CPC分类号： C12N15/635 , C07K14/575
摘要： Processes and compositions are provided for regulating COX2 gene expression in a cell. The process includes selecting a polyamide composition comprising N-methyl pyrrole (Py) and N-methyl imidazole (Im) to provide specific binding to DNA at a COX2 gene target site in a cell. The polyamide is then combined with the cell containing the COX2 gene, wherein the polyamide binds to the COX2 gene promoter target site and regulates transcription of the COX2 gene.
摘要翻译：提供用于调节细胞中COX2基因表达的方法和组合物。该方法包括选择包含N-甲基吡咯（Py）和N-甲基咪唑（Im）的聚酰胺组合物以在细胞中COX2基因靶位点提供与DNA的特异性结合。然后将聚酰胺与含有COX2基因的细胞组合，其中聚酰胺与COX2基因启动子靶位点结合并调节COX2基因的转录。

9. 发明申请

WO2005033282A3 POLYAMIDE COMPOSITIONS AND THERAPEUTIC METHODS FOR TREATMENT OF HUMAN PAPILLOMA VIRUS 审中-公开
标题翻译：聚酰胺组合物和治疗人类斑马鱼病毒的治疗方法
公开(公告)号：WO2005033282A3
公开(公告)日：2009-04-09
申请号：PCT/US2004032138
申请日：2004-09-30
申请人： PHARMACIA & UPJOHN CO LLC , FISHER CHRIS , BASHKIN JAMES K , CROWLEY KATHLEEN S , SVERDRUP FRANCIS M , GARNER-HAMRICK PEGGY A , PHILLION DENNIS P
发明人： FISHER CHRIS , BASHKIN JAMES K , CROWLEY KATHLEEN S , SVERDRUP FRANCIS M , GARNER-HAMRICK PEGGY A , PHILLION DENNIS P
IPC分类号： C07D207/04 , C12N20060101
CPC分类号： A61K31/785 , A61K9/0014 , A61K9/0034 , C12N2710/20011
摘要： Processes and compositions are provided for regulating replication in a human papilloma virus. The process includes selecting a polyamide composition comprising N-methyl pyrrole (Py) and either des-amino-N-methyl imidazole (dIm) or a fused, non-tautomerizing heteroaromatic bicyclic structure (L) that contains at least one hydrogen bond acceptor moiety, to provide specific binding to DNA at the E1 binding site in a human papilloma virus episome. The polyamide is then combined with the cell containing a human papilloma virus, wherein the polyamide binds to the human papilloma virus E1 binding site and regulates replication of the human papilloma virus.
摘要翻译：提供了用于调节人乳头状瘤病毒复制的方法和组合物。该方法包括选择包含N-甲基吡咯（Py）和去氨基-N-甲基咪唑（dIm）的聚酰胺组合物或包含至少一个氢键受体部分的融合的，非互变异构的杂芳族双环结构（L），以在人乳头状瘤病毒附加体中的E1结合位点提供与DNA的特异性结合。然后将聚酰胺与含有人乳头瘤病毒的细胞组合，其中聚酰胺结合人乳头状瘤病毒E1结合位点并调节人乳头状瘤病毒的复制。

10. 发明申请

WO2004099131A2 COMPOUNDS HAVING A FUSED, BICYCLIC MOIETY FOR BINDING TO THE MINOR GROOVE OF DSDNA 审中-公开
标题翻译：具有融合的双链体系的化合物用于与DSDNA的小型细菌结合
公开(公告)号：WO2004099131A2
公开(公告)日：2004-11-18
申请号：PCT/US2004/013285
申请日：2004-04-29
申请人： PHARMACIA CORPORATION , PHILLION, Dennis, P. , BASHKIN, James, K.
发明人： PHILLION, Dennis, P. , BASHKIN, James, K.
IPC分类号： C07D
CPC分类号： C07D417/14 , C07D403/14 , C07D471/04 , C07H19/04 , C07H21/04
摘要： The present invention is directed to the means by which to alter the binding affinity and/or specificity of a compound with a sequence of DNA in the minor groove of a double-strand thereof. More particularly, the present invention is directed to a synthetic and/or non-naturally occurring compound (e.g., an analog of a polyamide oligomer or polymer) which contains at least one hydrogen bond donor moiety and at least one hydrogen bond acceptor moiety, wherein the latter moiety or "building block" has a fused, bicyclic structure which is heteroaromatic, said structure having a heteroatom therein which acts as a hydrogen bond acceptor to bind guanine in the minor groove of the dsDNA sequence, and which is incapable of forming a tautomer. In one particular embodiment of the synthetic and/or non-naturally occurring compound, the fused, bicyclic structure occupies an initial or first terminal position within the compound.
摘要翻译：本发明涉及在双链的小槽中改变化合物与DNA序列的结合亲和性和/或特异性的方法。更具体地，本发明涉及含有至少一个氢键供体部分和至少一个氢键受体部分的合成和/或非天然存在的化合物（例如，聚酰胺低聚物或聚合物的类似物），其中后一部分或“结构单元”具有杂芳族的稠合双环结构，所述结构具有其中的杂原子，其作为氢键受体以在dsDNA序列的小沟中结合鸟嘌呤，并且其不能形成互变异构体。在合成和/或非天然存在的化合物的一个具体实施方案中，稠合双环结构占据化合物内的初始或第一末端位置。

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