专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2005081972A2 MALEIIMIDE ANTI-TUMOR PHOSPHATASE INHIBITORS 审中-公开
标题翻译：抗氧化剂抗肿瘤磷酸酶抑制剂
公开(公告)号：WO2005081972A2
公开(公告)日：2005-09-09
申请号：PCT/US2005/005742
申请日：2005-02-22
申请人： GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by the secretary, DEPARTMENT OF HEALTH AND HUMAN SERVICES , MICHEJDA, Christopher, J. , YAO, Wei , CARR, Brian, I. , KAR, Siddhartha
发明人： MICHEJDA, Christopher, J. , YAO, Wei , CARR, Brian, I. , KAR, Siddhartha
CPC分类号： C07D207/456
摘要： The present invention features maleiimide compounds, pharmaceutical compositions of maleiimide compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more maleiimide compounds of the invention.
摘要翻译：本发明的特征在于马来酰亚胺化合物，马来酰亚胺化合物的药物组合物和治疗患有癌症的患者的方法，所述方法包括向患者施用本发明的一种或多种马来酰亚胺化合物。

2. 发明申请

WO2005032594A3 ALKYLATORS LINKED TO POLYAMIDES AS DNA BINDING AGENTS 审中-公开
公开(公告)号：WO2005032594A3
公开(公告)日：2005-04-14
申请号：PCT/US2004/032617
申请日：2004-10-01
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , SZEKELY, Zoltan , HARIPRAKASHA, Humcha, K. , MICHEJDA, Christopher, J.
发明人： SZEKELY, Zoltan , HARIPRAKASHA, Humcha, K. , MICHEJDA, Christopher, J.
IPC分类号： A61K47/48 , C07D209/12 , C07D209/60 , C07D405/14 , C07D209/94
摘要： The invention provides an alkylator that is an analog of a compound based on 5-oxo-1a,2,3,5-tetrahydro-1H-3-aza-cyclopropa[c]indene-7-carboxylic acid, 9a-chloromethyl-4-oxo-2,4,9,9a-tetrahydro-1H-2-aza-cyclopropa[1,5]cyclopenta[1,2-a]naphthalene-7-carboxylic acid, or 4-oxo-1,2,4,5,8,8a-hexahydrocyclopropa[c]pyrrolo[3,2-e]indole-6-carboxylic acid and conjugates thereof.

3. 发明申请

WO2003072754A2 CONJUGATES OF LIGAND, LINKER AND CYTOTOXIC AGENT AND RELATED COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：配体，连接体和细胞毒性剂的结合及相关组合物及使用方法
公开(公告)号：WO2003072754A2
公开(公告)日：2003-09-04
申请号：PCT/US2003/006344
申请日：2003-02-27
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTAN D HUMAN SERVICES , TARASOVA, Nadya, I. , MICHEJDA, Christopher, J. , DYBA, Marcin , COHRAN, Carolyn
发明人： TARASOVA, Nadya, I. , MICHEJDA, Christopher, J. , DYBA, Marcin , COHRAN, Carolyn
IPC分类号： C12N
CPC分类号： C07K14/595 , A61K38/00 , A61K47/64 , C07K5/0205 , C07K5/06078 , C07K7/02 , C07K7/06 , C07K2319/00
摘要： A conjugate comprising a ligand, a linker, and a cytotoxic agent, in which the linker is FALA, VLALA, ALAL, ALALA, ChaLALA, ChaChaLAL, NalChaLAL or NalLALA; a composition thereof; a method of delivering a cytotoxic agent in a cell-specific manner; and a method of treating cancer in a mammal.
摘要翻译：包含配体，接头和细胞毒性剂的缀合物，其中接头是FALA，VLALA，ALAL，ALALA，ChaLALA，ChaChaLAL，NalChaLAL或NalLALA; 其组成; 以细胞特异性方式递送细胞毒性剂的方法; 以及在哺乳动物中治疗癌症的方法。

4. 发明申请

WO2003072058A3 DNA-BINDING POLYAMIDE DRUG CONJUGATES 审中-公开
公开(公告)号：WO2003072058A3
公开(公告)日：2003-09-04
申请号：PCT/US2003/006006
申请日：2003-02-27
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, representated by THE SECRETARY, DEPARMENT OF HEALTH AND HUMAN SERVICES , SZEKELY, Zoltan , HARIPRAKASHA, Humcha, Krishnamurthy , CHOLODY, Marek, W. , MICHEJDA, Christopher, J.
发明人： SZEKELY, Zoltan , HARIPRAKASHA, Humcha, Krishnamurthy , CHOLODY, Marek, W. , MICHEJDA, Christopher, J.
IPC分类号： A61K38/00
摘要： A conjugate of formula: V-(Y) a -Z-T: (I), T-X-B-(Y) a -Z-T': (II), V-(Y) a Z-(Y') a V': (III), T-X-B-(Y) a -Z-(Y') a -X'-B'-T': (IV), V-(Y) a -Z-(Y') a -X-B-T : (V), V-(Y) a -Z-X-B-Z'-(Y') a -(V') b : (VI), or (W) a -(Y) b -[(Z) c -(Y') d -(X-B) e -(Y") f -(Z') g ] h -(Y ...) i -(W') j : (VII), in which W and W' are independently a DNA intercalator or terminal subunit, V and V' are independently a DNA intercalator, X and X' are independently a DNA alkylator, B and B' are the same or different and each is a heteroaromatic residue that is attached to the Nterminus of an alkylator subunit (X or X'), Y, Y', Y" and Y"' are independently a linker, T and T' are independently terminal subunits, Z and Z' are independently a polyamide group that binds to the minor groove of DNA, a, b, c, d, f, g, i, and j are independently 0 to 5, and e and h are independently 1 to 5, a composition comprising a conjugate of any of formulae (I)-(VII) and a carrier, and a method for treating cancer in a mammal comprising administering an effective amount of a conjugate of any of formulae (I)-(VII) or a composition comprising same.

5. 发明申请

WO02059123A2 BENZOYLALKYLINDOLEPYRIDINIUM COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS 审中-公开
标题翻译：苯甲酰基二烯丙基化合物和包含这些化合物的药物组合物
公开(公告)号：WO02059123A2
公开(公告)日：2002-08-01
申请号：PCT/US0148311
申请日：2001-12-13
申请人： US GOV HEALTH & HUMAN SERV , RICE WILLIAM G , HUANG MINGJUN , BUCKHEIT ROBERT W JR , COVELL DAVID G , CZERWINSKI GRZEGORZ , MICHEJDA CHRISTOPHER J
发明人： RICE WILLIAM G , HUANG MINGJUN , BUCKHEIT ROBERT W JR , COVELL DAVID G , CZERWINSKI GRZEGORZ , MICHEJDA CHRISTOPHER J
IPC分类号： A61P31/12 , C07D471/04 , C07D519/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The design, synthesis and antiviral activity of novel benzoylalkylindole-pyridiniums are disclosed. These compounds inhibit the reverse transcriptase enzymes of several retroviruses, including human immunodeficiency virus types 1 and 2, and simian immunodeficiency virus, and effectively inhibit viral replication thereby. Most of these compounds satisfy formula (1) where R1 is independently selected from the group consisting of lower alkyl; N1 is a nitrogen in a ring and is bonded to C1 by either a single bond or a double bond; C1 is a carbon atom in a ring, is bonded to N1 by either a single bond or a double bond, and is bonded to C2 by either a single bond or a double bond; C2 is a carbon atom in a ring and is bonded to C1 by either a single bond or a double bond, and is bonded by either a single bond or a double bond to C3; and R2 is selected from the group consisting of hydrogen, lower alkyl, lower alkyl amide, and formula (2). Compositions comprising effective amounts of such compounds are also described. These compounds and compositions can be used in a method for inhibiting the replication of retroviruses in a subject comprising administering an effective amount of the compound(s) or composition(s) comprising the compound, to a subject to inhibit retroviral replication.
摘要翻译：公开了新型苯甲酰基吲哚 - 吡啶的设计，合成和抗病毒活性。这些化合物抑制几种逆转录病毒的逆转录酶，包括1型和2型人类免疫缺陷病毒和猿猴免疫缺陷病毒，从而有效地抑制病毒复制。这些化合物中的大多数满足式（1），其中R 1独立地选自低级烷基; N1是环中的氮，并且通过单键或双键与C1键合; C1是环中的碳原子，通过单键或双键与N1键合，并且通过单键或双键与C2键合; C2是环中的碳原子，并且通过单键或双键与C1键合，并且通过单键或双键与C3键合; 并且R 2选自氢，低级烷基，低级烷基酰胺和式（2）。还描述了包含有效量的这种化合物的组合物。这些化合物和组合物可用于抑制受试者中逆转录病毒复制的方法，包括向受试者施用有效量的包含该化合物的化合物或组合物以抑制逆转录病毒复制。

6. 发明申请

WO1997038999A1 ACRIDONE-DERIVED COMPOUNDS USEFUL AS ANTINEOPLASTIC AND ANTIRETROVIRAL AGENTS 审中-公开
标题翻译：作为抗肿瘤药物和抗逆转录病毒剂的阿司匹林衍生化合物有用
公开(公告)号：WO1997038999A1
公开(公告)日：1997-10-23
申请号：PCT/US1997007070
申请日：1997-04-09
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , MICHEJDA, Christopher, J. , CHOLODY, Marek, W. , RICE, William, G. , TURPIN, James, A.
发明人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
IPC分类号： C07D471/06
CPC分类号： C07D471/06
摘要： The present invention relates to several novel acridone-derived compounds of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as Human Immunodeficiency Virus. In addition, these compounds are anti-neoplastic agents useful in the treatment of various forms of cancer. In said formula (I) or (II) R1 and R2 are independently -H, -OH, amino, alkylamino, dialkylamino, alkoxy, alkyl, haloalkyl or halogen; n is 2 to 6, X and X' are independently -N or -NO2; Y and Y' are independently -N or -CH, or -H; and the double-slash represents a double bond or no bond.
摘要翻译：本发明涉及几种新的吖啶酮衍生的式（I）或（II）化合物。这些化合物是有效的抗病毒剂，可用于治疗病毒性疾病，例如人类免疫缺陷病毒。此外，这些化合物是可用于治疗各种形式的癌症的抗肿瘤剂。在所述式（I）或（II）中，R 1和R 2独立地为-H，-OH，氨基，烷基氨基，二烷基氨基，烷氧基，烷基，卤代烷基或卤素; n为2至6，X和X'独立地为-N或-NO 2; Y和Y'独立地是-N或-CH或-H; 双斜线代表双键或无键。

7. 发明申请

WO2002059123A3 BENZOYLALKYLINDOLEPYRIDINIUM COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS 审中-公开
公开(公告)号：WO2002059123A3
公开(公告)日：2002-08-01
申请号：PCT/US2001/048311
申请日：2001-12-13
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , RICE, William, G. , HUANG, Mingjun , BUCKHEIT, Robert, W., Jr. , COVELL, David, G. , CZERWINSKI, Grzegorz , MICHEJDA, Christopher, J.
发明人： RICE, William, G. , HUANG, Mingjun , BUCKHEIT, Robert, W., Jr. , COVELL, David, G. , CZERWINSKI, Grzegorz , MICHEJDA, Christopher, J.
IPC分类号： C07D471/04
摘要： The design, synthesis and antiviral activity of novel benzoylalkylindole-pyridiniums are disclosed. These compounds inhibit the reverse transcriptase enzymes of several retroviruses, including human immunodeficiency virus types 1 and 2, and simian immunodeficiency virus, and effectively inhibit viral replication thereby. Most of these compounds satisfy formula (1) where R 1 is independently selected from the group consisting of lower alkyl; N 1 is a nitrogen in a ring and is bonded to C 1 by either a single bond or a double bond; C 1 is a carbon atom in a ring, is bonded to N 1 by either a single bond or a double bond, and is bonded to C 2 by either a single bond or a double bond; C 2 is a carbon atom in a ring and is bonded to C 1 by either a single bond or a double bond, and is bonded by either a single bond or a double bond to C 3 ; and R 2 is selected from the group consisting of hydrogen, lower alkyl, lower alkyl amide, and formula (2). Compositions comprising effective amounts of such compounds are also described. These compounds and compositions can be used in a method for inhibiting the replication of retroviruses in a subject comprising administering an effective amount of the compound(s) or composition(s) comprising the compound, to a subject to inhibit retroviral replication.

8. 发明申请

WO2008058125A2 SELF-ASSEMBLING NANOPARTICLES COMPOSED OF TRANSMEMBRANE PEPTIDES AND THEIR APPLICATION FOR SPECIFIC INTRA-TUMOR DELIVERY OF ANTI-CANCER DRUGS 审中-公开
标题翻译：自组装转氨酶的纳米颗粒及其用于特异性肿瘤输送抗癌药物的应用
公开(公告)号：WO2008058125A2
公开(公告)日：2008-05-15
申请号：PCT/US2007/083772
申请日：2007-11-06
申请人： GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , TARASOVA, Nadya I. , TARASOV, Sergey G. , MICHEJDA, Christopher J.
发明人： TARASOVA, Nadya I. , TARASOV, Sergey G. , MICHEJDA, Christopher J.
CPC分类号： A61K9/5169
摘要： The invention provides a method of handling a hydrophobic agent, which method comprises (a) combining in an aqueous solution (i) a hydrophobic agent and (ii) an isolated peptide that is a structural analog of a transmembrane domain of an integral membrane protein, wherein one terminus of the peptide has one or more negatively charged residues, and (b) allowing the peptide to self-assemble into nanoparticles, wherein the nanoparticles comprise the hydrophobic agent.
摘要翻译：本发明提供了一种处理疏水剂的方法，该方法包括（a）在水溶液（i）疏水剂和（ii）作为整合膜蛋白的跨膜结构域的结构类似物的分离肽组合，其中肽的一个末端具有一个或多个带负电荷的残基，和（b）允许肽自组装成纳米颗粒，其中纳米颗粒包含疏水剂。

9. 发明申请

WO2003072058A2 DNA-BINDING POLYAMIDE DRUG CONJUGATES 审中-公开
标题翻译： DNA结合聚酰胺药物结合
公开(公告)号：WO2003072058A2
公开(公告)日：2003-09-04
申请号：PCT/US2003/006006
申请日：2003-02-27
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, representated by THE SECRETARY, DEPARMENT OF HEALTH AND HUMAN SERVICES , SZEKELY, Zoltan , HARIPRAKASHA, Humcha, Krishnamurthy , CHOLODY, Marek, W. , MICHEJDA, Christopher, J.
发明人： SZEKELY, Zoltan , HARIPRAKASHA, Humcha, Krishnamurthy , CHOLODY, Marek, W. , MICHEJDA, Christopher, J.
IPC分类号： A61K
CPC分类号： A61K47/645
摘要： A conjugate of formula: V-(Y) a -Z-T: (I), T-X-B-(Y) a -Z-T': (II), V-(Y) a Z-(Y') a V': (III), T-X-B-(Y) a -Z-(Y') a -X'-B'-T': (IV), V-(Y) a -Z-(Y') a -X-B-T : (V), V-(Y) a -Z-X-B-Z'-(Y') a -(V') b : (VI), or (W) a -(Y) b -[(Z) c -(Y') d -(X-B) e -(Y") f -(Z') g ] h -(Y ...) i -(W') j : (VII), in which W and W' are independently a DNA intercalator or terminal subunit, V and V' are independently a DNA intercalator, X and X' are independently a DNA alkylator, B and B' are the same or different and each is a heteroaromatic residue that is attached to the Nterminus of an alkylator subunit (X or X'), Y, Y', Y" and Y"' are independently a linker, T and T' are independently terminal subunits, Z and Z' are independently a polyamide group that binds to the minor groove of DNA, a, b, c, d, f, g, i, and j are independently 0 to 5, and e and h are independently 1 to 5, a composition comprising a conjugate of any of formulae (I)-(VII) and a carrier, and a method for treating cancer in a mammal comprising administering an effective amount of a conjugate of any of formulae (I)-(VII) or a composition comprising same.
摘要翻译：式（V）（Y）aZT：（I），TXB-（Y）aZ-T'：（II），V-（Y）a Z-（Y'）a V' TXB-（Y）aZ-（Y'）a-X'-B'-T'：（IV），V-（Y）aZ-（Y'）aXBT：（V），V-（Y）aZXB- Z' - （Y'）a-（V'）b：（VI）或（W）a-（Y）b - [（Z）c-（Y'）d-（XB）e-（Y“ ）f-（Z'）g] h-（Y ...）i-（W'）j：（VII），其中W和W'独立地是DNA嵌入剂或末端亚单元，V和V' DNA嵌入剂X和X'独立地是DNA烷基化剂，B和B'相同或不同，并且各自是连接到烷基化子亚单位（X或X'），Y，Y'的N末端的杂芳族残基，，Y“和Y”'独立地是连接体，T和T'独立地是末端亚单元，Z和Z'独立地是结合DNA的小沟的聚酰胺基团，a，b，c，d，f，g i和j独立地为0〜5，e和h独立地为1〜5，包含式（I） - （VII）中任一式的结合物和载体的组合物，以及哺乳动物的癌症治疗方法包括施用有效的（I） - （VII）中任一项的缀合物或包含其的组合物。

10. 发明申请

WO0136477A3 INHIBITION OF ABC TRANSPORTERS BY TRANSMEMBRANE DOMAIN ANALOGS 审中-公开
标题翻译：通过跨膜域模拟抑制ABC运输机
公开(公告)号：WO0136477A3
公开(公告)日：2002-07-18
申请号：PCT/US0031817
申请日：2000-11-17
申请人： US GOV HEALTH & HUMAN SERV , TARASOVA NADYA I , MICHEJDA CHRISTOPHER J , GOTTESMAN MICHAEL M , HRYCYNA CHRISTINE
发明人： TARASOVA NADYA I , MICHEJDA CHRISTOPHER J , GOTTESMAN MICHAEL M , HRYCYNA CHRISTINE
IPC分类号： A61K38/00 , C07K14/705 , A61K38/17 , C12N5/10 , C12N15/12
CPC分类号： C07K14/705 , A61K38/00
摘要： ATP-binding cassette (ABC) transporters generally contain a number of transmembrane helices. The present invention provides synthetic peptides derived from these transmembrane helices. The peptides inhibit ABC transporter function, presumably by disrupting the structure of the ABC transporter. Negatively charged residues are added at the extracellular terminus to promote correct orientation of the peptide in the membrane, and residues considered to aid solubility may be added at that terminus to increase solubility. Exemplary ABC transporters that can be inhibited by these peptides include MDR1, MRP1, MRP2, and BCRP. The invention further provides nucleic acids encoding the peptides, expression cassettes comprising the nucleic acids, and host cells expressing the expression cassettes. The invention further provides a simple and inexpensive assay for determining whether a potential chemotherapeutic agent can inhibit the activity of P-glycoprotein.
摘要翻译： ATP结合盒（ABC）转运蛋白通常含有许多跨膜螺旋。本发明提供了衍生自这些跨膜螺旋的合成肽。这些肽抑制ABC转运蛋白功能，大概是通过破坏ABC转运蛋白的结构。在细胞外末端添加负电荷残基以促进肽在膜中的正确取向，并且可以在该末端添加被认为有助于溶解性的残基以增加溶解度。可以被这些肽抑制的ABC转运蛋白的实例包括MDR1，MRP1，MRP2和BCRP。本发明还提供了编码肽的核酸，包含核酸的表达盒和表达表达盒的宿主细胞。本发明进一步提供了用于确定潜在化学治疗剂是否能抑制P-糖蛋白活性的简单和便宜的测定法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式