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1. 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。

2. 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。

3. 发明申请

WO2008058125A3 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：自组装跨膜蛋白纳米微粒及其在肿瘤抗肿瘤药物特异性肿瘤给药中的应用
公开(公告)号：WO2008058125A3
公开(公告)日：2008-10-16
申请号：PCT/US2007083772
申请日：2007-11-06
申请人： US GOV HEALTH & HUMAN SERV , TARASOVA NADYA I , TARASOV SERGEY G , MICHEJDA CHRISTOPHER J
发明人： TARASOVA NADYA I , TARASOV SERGEY G , MICHEJDA CHRISTOPHER J
IPC分类号： A61K9/51 , A61K38/00 , A61K47/42 , A61P35/00
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）在水溶液中（i）疏水剂和（ii）分离的肽，其是整合膜蛋白的跨膜结构域的结构类似物，其中所述肽的一个末端具有一个或多个带负电荷的残基，和（b）使所述肽自组装成纳米颗粒，其中所述纳米颗粒包含所述疏水剂。

4. 发明申请

WO2005081972A3 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：WO2005081972A3
公开(公告)日：2006-01-05
申请号：PCT/US2005005742
申请日：2005-02-22
申请人： US GOV HEALTH & HUMAN SERV , MICHEJDA CHRISTOPHER J , YAO WEI , CARR BRIAN I , KAR SIDDHARTHA
发明人： MICHEJDA CHRISTOPHER J , YAO WEI , CARR BRIAN I , KAR SIDDHARTHA
IPC分类号： A61K31/40 , C07D207/12
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。

5. 发明申请

WO2005032594A2 BUILDING BLOCKS FOR DNA BINDING AGENTS 审中-公开
标题翻译：用于DNA绑定代理的建筑块
公开(公告)号：WO2005032594A2
公开(公告)日：2005-04-14
申请号：PCT/US2004032617
申请日：2004-10-01
申请人： US GOV HEALTH & HUMAN SERV , 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 , C07D209/94 , C07D405/14 , C07D487/04
CPC分类号： C07D487/04 , A61K47/54 , C07D209/12 , C07D209/60 , C07D209/94 , C07D405/14
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.
摘要翻译：本发明提供了一种烷基化剂，其是基于5-氧代-1a,2,3,5-四氢-1H-3-氮杂 - 环丙并[c]茚-7-羧酸，9a-氯甲基-4 - 氧代-2,4,9,9a-四氢-1H-2-氮杂 - 环丙[1,5]环戊二烯并[1,2-a]萘-7-羧酸或4-氧代-1,2,4- ，5,8,8a-六氢环丙基[c]吡咯并[3,2-e]吲哚-6-羧酸及其偶联物。

6. 发明申请

WO2008033891A3 AZONAFIDE DERIVED TUMOR AND CANCER TARGETING COMPOUNDS 审中-公开
标题翻译： AZONAFIDE衍生肿瘤和癌靶向化合物
公开(公告)号：WO2008033891A3
公开(公告)日：2008-08-28
申请号：PCT/US2007078233
申请日：2007-09-12
申请人： US GOV HEALTH & HUMAN SERV , MICHEJDA MARIA , TARASOVA NADYA I , DYBA MARCIN
发明人： TARASOVA NADYA I , DYBA MARCIN , MICHEJDA CHRISTOPHER J
IPC分类号： C07D221/18 , A61K31/473 , A61P35/00 , C07D401/12 , C07K7/06
CPC分类号： C07D221/18 , C07D401/12
摘要： An azonafide-based compound of Formula I, a composition comprising the compound, and a method of using the compound to deliver a cytotoxic azonafide derivative to a cell, as well as related compounds and methods for the use thereof to prepare an azonafide-based compound of Formula I.
摘要翻译：式I的以azonafide为基础的化合物，包含该化合物的组合物，以及使用该化合物将细胞毒性偶氮胂衍生物递送至细胞的方法，以及相关化合物及其用于制备以氮鎓化物为基础的化合物式I

7. 发明申请

WO0166545A3 1,8-NAPHTHALIMIDE IMIDAZO[4,5,1-de]ACRIDONES WITH ANTI-TUMOR ACTIVITY 审中-公开
标题翻译：具有抗肿瘤活性的1,8-萘内酰胺咪唑并[4,5,1-二]
公开(公告)号：WO0166545A3
公开(公告)日：2002-02-28
申请号：PCT/US0107087
申请日：2001-03-05
申请人： US HEALTH , CHOLODY WIESLAW M , KOSAKOWSKA CHOLODY TERESA , MICHEJDA CHRISTOPHER J
发明人： CHOLODY WIESLAW M , KOSAKOWSKA-CHOLODY TERESA , MICHEJDA CHRISTOPHER J
IPC分类号： A61K31/4745 , A61K31/496 , A61K31/506 , A61P35/00 , C07D471/06 , A61K31/437
CPC分类号： C07D471/06 , A61K31/4745 , A61K31/496 , A61K31/506
摘要： The invention provides imidazoacridone compounds of general formula (1) which have cytotoxic and anti-tumor activity. The invention also provides methods of preparing the compounds, and methods of using the compounds for the treatment of cancer or other mammalian diseases characterized by undesirably high levels of cell proliferation. The compounds of the invention are also expected to have utility as research tools.
摘要翻译：本发明提供具有细胞毒性和抗肿瘤活性的通式（1）的咪唑并吖啶酮化合物。本发明还提供了制备化合物的方法，以及使用该化合物治疗癌症或以不期望的高水平细胞增殖为特征的其它哺乳动物疾病的方法。本发明的化合物也预期具有作为研究工具的效用。

8. 发明申请

WO9943311A2 CONJUGATED SURAMIN OR DERIVATIVES THEREOF WITH PEG, POLYASPARTATE OR POLYGLUTAMATE FOR CANCER TREATMENT 审中-公开
标题翻译：用PEG，聚天冬氨酸或聚谷氨酸盐共轭的SURAMIN或其衍生物用于癌症治疗
公开(公告)号：WO9943311A2
公开(公告)日：1999-09-02
申请号：PCT/US9904336
申请日：1999-02-26
申请人： US HEALTH , WEBB CRAIG P , JEFFERS MICHAEL E , CZERWINSKI GREGORZ , MICHEJDA CHRISTOPHER J , VANDE WOUDE GEORGE F
发明人： WEBB CRAIG P , JEFFERS MICHAEL E , CZERWINSKI GREGORZ , MICHEJDA CHRISTOPHER J , VANDE WOUDE GEORGE F
IPC分类号： A61K47/48 , C09B69/10 , C12Q1/37 , A61K31/185
CPC分类号： C12Q1/37 , A61K47/60 , A61K47/645 , C09B69/106 , G01N2333/9723
摘要： The present invention provides an assay that identifies compounds which inhibit cleavage of HGF/SF by serum proteases such as uPA, and methods in which such compounds are provided to reaction solutions, to cultured cells in vitro, or to a mammal in vivo, to inhibit cleavage of HGF/SF and to inhibit chemical and biological effects resulting from the activation of c-Met receptor by HGF/SF. The invention also provides methods for modifying suramin and suramin-related polysulfonated compounds that inhibit HGF/SF cleavage, by attaching PEG or polyanions such as polyglutamate or polyaspartate to the compounds to reduce cellular uptake of the compounds, thereby reducing their cytotoxicity. Also provided are a pharmaceutical composition containing at least one polysulfonated HGF/SF cleavage-inhibiting compound other than suramin, and a pharmaceutical composition containing at least one HGF/SF cleavage-inhibiting form of suramin or a suramin-related polysulfonated compound that is modified by conjugation to a chemical moiety that reduces uptake of the compound into cells. The present invention further includes methods wherein such pharmaceutical compositions are administered to a mammal with a tumor that is stimulated to grow by HGF/SF, to inhibit the growth or metastasis of the tumor in the mammal.
摘要翻译：本发明提供了鉴定通过血清蛋白酶如uPA来抑制HGF / SF裂解的化合物的测定法，以及将这些化合物提供给反应溶液，体外培养细胞或体内哺乳动物以提供抑制切割HGF / SF并抑制由HGF / SF激活c-Met受体引起的化学和生物效应。本发明还提供了通过将PEG或聚阴离子如聚谷氨酸盐或聚天冬氨酸连接到化合物以减少化合物的细胞摄取从而减少它们的细胞毒性来修饰抑制HGF / SF切割的苏拉明和苏拉明相关多磺化化合物的方法。还提供了一种药物组合物，其含有至少一种除苏拉明以外的多磺化HGF / SF裂解抑制化合物，以及一种药物组合物，该药物组合物含有至少一种被修饰的苏拉明或苏拉明相关多磺化化合物的HGF / SF切割抑制形式缀合至减少化合物向细胞摄取的化学部分。本发明进一步包括这样的方法，其中将这种药物组合物给予患有被HGF / SF刺激生长的肿瘤的哺乳动物，以抑制哺乳动物中肿瘤的生长或转移。

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