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31. 发明申请

WO0009073A3 BLOOD-BRAIN BARRIER THERAPEUTICS 审中-公开
标题翻译：血脑屏障治疗法
公开(公告)号：WO0009073A3
公开(公告)日：2000-06-29
申请号：PCT/US9918248
申请日：1999-08-12
申请人： PROTEIN DELIVERY INC , EKWURIBE NNOCHIRI N , RADHAKRISHNAN BALASINGAM , PRICE CHRISTOPHER H , ANDERSON WESLEY R JR , AUSARI ASLAM M
发明人： EKWURIBE NNOCHIRI N , RADHAKRISHNAN BALASINGAM , PRICE CHRISTOPHER H , ANDERSON WESLEY R JR , AUSARI ASLAM M
IPC分类号： A61K38/00 , A61K38/04 , A61K38/11 , A61K38/21 , A61K38/22 , A61K38/26 , A61K38/27 , A61K38/36 , A61K38/46 , A61K38/48 , A61K39/395 , A61K45/00 , A61K47/48 , A61P5/02 , A61P5/10 , A61P5/14 , A61P5/18 , A61P29/00 , A61P43/00 , C07K14/70 , C07K17/00 , A61K31/705
CPC分类号： A61K47/60
摘要： The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier and to methods of making and using such conjugates. Amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.
摘要翻译：本发明涉及能够穿过血脑屏障的两亲性药物 - 寡聚体缀合物以及制备和使用这种缀合物的方法。两亲性药物 - 寡聚物缀合物包含缀合至寡聚体的治疗性化合物，其中寡聚体包含偶联至亲水性部分的亲脂性部分。本发明的缀合物进一步包含与两亲低聚物化学偶联的治疗剂，例如蛋白质，肽，核苷，核苷酸，抗病毒剂，抗肿瘤剂，抗生素等，以及其前体药物，前体，衍生物和中间体。

32. 发明申请

WO2006014549A8 SYNTHESIS OF AZO BONDED IMMUNOREGULATORY COMPOUNDS 审中-公开
标题翻译： AZO结合免疫化合物的合成
公开(公告)号：WO2006014549A8
公开(公告)日：2007-02-22
申请号：PCT/US2005024109
申请日：2005-07-07
申请人： NOBEX CORP , SAUTHIER JENNIFER A RIGGS , EKWURIBE NNOCHIRI N
发明人： SAUTHIER JENNIFER A RIGGS , EKWURIBE NNOCHIRI N
IPC分类号： C07D207/09 , A61K31/4025 , C07D207/10
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R 1 , R 3 , and R 4 are independently hydrogen or C 1 to C 4 alkyl, and R 2 is: where R 5 is selected from the group consisting of hydrogen and C 1 to C 4 alkyl, or where R 6 , R 7 and R 8 are independently hydrogen or C 1 to C 4 alkyl; or the esters or pharmacologically acceptable salts thereof.. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.
摘要翻译：公开了制备式I化合物的方法：其中R 1，...，R 3，...和R 4是独立地是氢或C 1至C 4烷基，R 2是：其中R 5选自由C 1〜C 4烷基构成的氢和C 1〜4的基团，或者R 6，R 6， >和R 8独立地是氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。该方法可以包括将适当官能化的苯胺化合物转化为重氮盐（可以首先通过还原硝基苯形成苯胺化合物）并将重氮盐与适当官能化的苯化合物偶联。适当官能化的苯胺化合物包括伯醇或醛基，然后将其氧化成羧酸基团，或包括被水解成羧酸基团的腈或酰胺基团。所述方法还可以涉及适当官能化的硝基苯的直接偶联（通过还原硝基以形成偶氮键）。化合物及其代谢物可用于治疗或预防各种疾病，特别是胃肠道的炎性病症。

33. 发明申请

WO2005094448A3 METHODS AND COMPOSITIONS EMPLOYING 4-AMINOPHENYLACETIC ACID COMPOUNDS 审中-公开
标题翻译：使用4-氨基苯乙酸化合物的方法和组合物
公开(公告)号：WO2005094448A3
公开(公告)日：2006-08-17
申请号：PCT/US2005009325
申请日：2005-03-22
申请人： NOBEX CORP , EKWURIBE NNOCHIRI N , LIDDLE RODGER
发明人： EKWURIBE NNOCHIRI N , LIDDLE RODGER
IPC分类号： A61K31/606 , A61K31/192 , A61K31/194 , A61K31/196
CPC分类号： A61K31/192 , A61K2300/00
摘要： The invention provides compositions comprising 4-APAA compounds and methods for treating disorders involving inflammation of the digestive system and/or mucosal tissues, such as inflammatory bowel disease. The methods and compositions of the invention also include combinations of 4-APAA compounds and 5-ASA compounds for treatment of such disorders.
摘要翻译：本发明提供了包含4-APAA化合物的组合物和用于治疗涉及消化系统和/或粘膜组织炎症的疾病例如炎症性肠病的方法。本发明的方法和组合物还包括用于治疗这些病症的4-APAA化合物和5-ASA化合物的组合。

34. 发明申请

WO2004083234A3 INSULIN POLYPEPTIDE-OLIGOMER CONJUGATES, PROINSULIN POLYPEPTIDE-OLIGOMER CONJUGATES AND METHODS OF SYNTHESIZING SAME 审中-公开
标题翻译：胰岛素多肽 - 寡聚体，蛋白多肽 - 低聚物结合体及其合成方法
公开(公告)号：WO2004083234A3
公开(公告)日：2005-08-04
申请号：PCT/US2004007310
申请日：2004-03-11
申请人： NOBEX CORP , EKWURIBE NNOCHIRI N , RADHAKRISHNAN BALASINGAM , SOLTERO RICHARD , PUSKAS MONICA , SANGAL DITI
发明人： EKWURIBE NNOCHIRI N , RADHAKRISHNAN BALASINGAM , SOLTERO RICHARD , PUSKAS MONICA , SANGAL DITI
IPC分类号： A61K38/28 , A61K47/48 , C07K20060101 , C07K14/62
CPC分类号： C07K14/62 , A61K47/60
摘要： Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.
摘要翻译：描述了用于合成胰岛素原多肽的方法，其包括通过能够被切割的肽键将包含与一个或多个肽偶联的胰岛素原多肽与足够使寡聚物与胰岛素原多肽的胰岛素多肽部分，并提供胰岛素原多肽 - 低聚物缀合物，并切割来自胰岛素原多肽 - 低聚物缀合物的一种或多种肽，以提供胰岛素多肽 - 低聚物缀合物。还提供了合成胰岛素原多肽 - 低聚物缀合物的方法，胰岛素原多肽 - 低聚物缀合物。还提供了合成C-肽多肽 - 低聚物缀合物和其它前 - 多肽 - 低聚物缀合物的方法。

35. 发明申请

WO2004083234A2 INSULIN POLYPEPTIDE-OLIGOMER CONJUGATES, PROINSULIN POLYPEPTIDE-OLIGOMER CONJUGATES AND METHODS OF SYNTHESIZING SAME 审中-公开
标题翻译：胰岛素多肽 - 寡聚体，蛋白多肽 - 低聚物结合体及其合成方法
公开(公告)号：WO2004083234A2
公开(公告)日：2004-09-30
申请号：PCT/US2004/007310
申请日：2004-03-11
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri N. , RADHAKRISHNAN, Balasingam , SOLTERO, Richard , PUSKAS, Monica , SANGAL, Diti
发明人： EKWURIBE, Nnochiri N. , RADHAKRISHNAN, Balasingam , SOLTERO, Richard , PUSKAS, Monica , SANGAL, Diti
IPC分类号： C07K
CPC分类号： C07K14/62 , A61K47/60
摘要： Methods for synthesizing proinsulin polypeptides are described that include contacting a proinsulin polypeptide including an insulin polypeptide coupled to one or more peptides by peptide bond(s) capable of being cleaved to yield the insulin polypeptide with an oligomer under conditions sufficient to couple the oligomer to the insulin polypeptide portion of the proinsulin polypeptide and provide a proinsulin polypeptide-oligomer conjugate, and cleaving the one or more peptides from the proinsulin polypeptide-oligomer conjugate to provide the insulin polypeptide-oligomer conjugate. Methods of synthesizing proinsulin polypeptide-oligomer conjugates are also provided as are proinsulin polypeptide-oligomer conjugates. Methods of synthesizing C-peptide polypeptide-oligomer conjugates and other pro-polypeptide-oligomer conjugates are also provided.
摘要翻译：描述了用于合成胰岛素原多肽的方法，其包括通过能够被切割的肽键将包含与一个或多个肽偶联的胰岛素原多肽与足够使寡聚物与胰岛素原多肽的胰岛素多肽部分，并提供胰岛素原多肽 - 低聚物缀合物，并切割来自胰岛素原多肽 - 低聚物缀合物的一种或多种肽，以提供胰岛素多肽 - 低聚物缀合物。还提供了合成胰岛素原多肽 - 低聚物缀合物的方法，胰岛素原多肽 - 低聚物缀合物。还提供了合成C-肽多肽 - 低聚物缀合物和其它前 - 多肽 - 低聚物缀合物的方法。

36. 发明申请

WO2004043396A3 MODIFIED CARBAMATE-CONTAINING PRODRUGS AND METHODS OF SYNTHESIZING SAME 审中-公开
标题翻译：含有改性的氨基甲酸酯的前躯体及其合成方法
公开(公告)号：WO2004043396A3
公开(公告)日：2004-08-12
申请号：PCT/US0335995
申请日：2003-11-07
申请人： NOBEX CORP , EKWURIBE NNOCHIRI N , RIGGS-SAUTHIER JENNIFER , DYAKONOV TATYANA
发明人： EKWURIBE NNOCHIRI N , RIGGS-SAUTHIER JENNIFER , DYAKONOV TATYANA
IPC分类号： A61K31/16 , A61K31/325 , A61K31/66 , A61K47/48 , C07K7/04 , A61K37/24 , C07K37/43
CPC分类号： A61K31/325 , A61K47/54 , A61K47/58 , A61K47/60 , A61K47/61
摘要： Prodrugs having a hydrolyzable carbamate moiety, compositions including the prodrugs, methods of preparing the prodrugs and methods of treatment using the prodrugs are disclosed. The prodrug has the formula DC(X)XR, where D is a biologically active agent, X is O, S or NR , and R is a moiety that modifies various properties of the biologically active agent. The biologically active agent either includes a functional group such as an amide, thioamide, imide, thioimide, urea, thiourea, carbamate, thiocarbamate, sulfonamide, or sulfonimide group, or includes a hydroxy, amine, carboxylic acid or thiol group that is modified to include such a group. An NH group from the biologically active agent can be coupled to an activated form the C(X)XR moiety to form the prodrugs described herein. Relative to a conventional carbamate group, the presence of the additional carbonyl or sulfonyl group makes the carbamate group more susceptible to hydrolysis. The prodrugs are more stable in certain environments than the biologically active agent, and can permit the drugs to be administered orally, in those embodiments where the biologically active agent must otherwise be administered by injection or intraveneous administration.
摘要翻译：公开了具有可水解的氨基甲酸酯部分的前药，包括前药的组合物，制备前药的方法和使用前药的治疗方法。前药具有式DC（X）XR，其中D是生物活性剂，X是O，S或NR，并且R是改变生物活性剂的各种性质的部分。生物活性剂包括官能团如酰胺，硫代酰胺，酰亚胺，硫代酰亚胺，脲，硫脲，氨基甲酸酯，硫代氨基甲酸酯，磺酰胺或磺酰亚胺基团，或包括羟基，胺，羧酸或硫醇基，包括这样一个组。来自生物活性剂的NH基团可以与C（X）XR部分的活化形式偶联以形成本文所述的前药。相对于常规的氨基甲酸酯基团而言，额外的羰基或磺酰基团的存在使得氨基甲酸酯基团更易于水解。前药在某些环境下比生物活性剂更稳定，并且可以允许药物以口服方式施用，其中生物活性剂必须以其他方式通过注射或静脉内施用施用。

37. 发明申请

WO2003022210A2 PHARMACEUTICAL COMPOSITIONS OF DRUG-OLIGOMER CONJUGATES AND METHODS OF TREATING DISEASES THEREWITH 审中-公开
标题翻译：药物低聚物共轭物的药物组合物和治疗疾病的方法
公开(公告)号：WO2003022210A2
公开(公告)日：2003-03-20
申请号：PCT/US2002/028536
申请日：2002-09-06
申请人： NOBEX CORPORATION , SOLTERO, Richard , EKWURIBE, Nnochiri, N. , OPAWALE, Foyeke , REHLAENDER, Bruce , HICKEY, Anthony , BOVET, Li, Li
发明人： SOLTERO, Richard , EKWURIBE, Nnochiri, N. , OPAWALE, Foyeke , REHLAENDER, Bruce , HICKEY, Anthony , BOVET, Li, Li
IPC分类号： A61K
CPC分类号： A61K47/554 , A61K47/542 , A61K47/60 , Y10S514/808
摘要： Pharmaceutical compositions that include a drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating diseases in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.
摘要翻译：描述了包含药物 - 寡聚物缀合物，脂肪酸组分和胆汁盐组分的药物组合物。药物共价偶联到寡聚部分。脂肪酸组分和胆汁盐组分以1：5至5：1的重量比存在。还提供了使用这种药物组合物治疗需要这种治疗的受试者的疾病的方法，以及提供这种药物组合物的方法。

38. 发明申请

WO2002098452A1 MIXTURES OF GROWTH HORMONE DRUG-OLIGOMER CONJUGATES COMPROMISING POLYALKYLENE GLYCOL, USES THEREOF, AND METHODS OF MAKING SAME 审中-公开
标题翻译：含有聚乙烯甘油的生长激素混合物 - 低聚物的混合物及其制备方法
公开(公告)号：WO2002098452A1
公开(公告)日：2002-12-12
申请号：PCT/US2002/017504
申请日：2002-06-04
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri, N. , PRICE, Christopher, H. , ANSARI, Aslam, M. , ODENBAUGH, Amy, L.
发明人： EKWURIBE, Nnochiri, N. , PRICE, Christopher, H. , ANSARI, Aslam, M. , ODENBAUGH, Amy, L.
IPC分类号： A61K38/27
CPC分类号： C07K14/61 , A61K38/27 , A61K47/60
摘要： A mixture of conjugates in which each conjugate in the mixture comprises a growth hormone drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed.
摘要翻译：公开了混合物的混合物，其中混合物中的每个缀合物包含与包含聚亚烷基二醇部分的低聚物偶联的生长激素药物。

39. 发明申请

WO2002098451A1 MIXTURES OF CALCITONIN DRUG-OLIGOMER CONJUGATES COMPRISING POLYALKYLENE GLYCOL, USES THEREOF, AND METHODS OF MAKING SAME 审中-公开
标题翻译：包含聚乙烯甘露醇的钙依诺礼酸低聚物混合物的混合物及其制备方法
公开(公告)号：WO2002098451A1
公开(公告)日：2002-12-12
申请号：PCT/US2002/017575
申请日：2002-06-04
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri, N. , PRICE, Christopher, H. , ANSARI, Aslam, M. , ODENBAUGH, Amy, L.
发明人： EKWURIBE, Nnochiri, N. , PRICE, Christopher, H. , ANSARI, Aslam, M. , ODENBAUGH, Amy, L.
IPC分类号： A61K38/23
CPC分类号： C07K14/585 , A61K47/60
摘要： A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin.
摘要翻译：公开了混合物的混合物，其中混合物中的每个缀合物包含与包含聚亚烷基二醇部分的低聚物偶联的降钙素药物。该混合物可使受试者中的血清钙水平降低10,15或甚至20％或更多。此外，混合物在存活肠内消化的体外模型方面比非共轭降钙素更有效。此外，该混合物可能表现出比非共轭降钙素更高的生物利用度。

40. 发明申请

WO2002098232A1 MIXTURES OF INSULIN DRUG-OLIGOMER CONJUGATES COMPRISING POLYALKYLENE GLYCOL, USES THEREOF, AND METHODS OF MAKING SAME 审中-公开
标题翻译：包含聚乙烯甘露糖的胰岛素药物 - 低聚物混合物的混合物及其制备方法
公开(公告)号：WO2002098232A1
公开(公告)日：2002-12-12
申请号：PCT/US2002/017574
申请日：2002-06-04
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri, N. , PRICE, Christopher, H. , ANSARI, Aslam, M. , ODENBAUGH, Amy, L. , RADHAKRISHNAN, Balasingam
发明人： EKWURIBE, Nnochiri, N. , PRICE, Christopher, H. , ANSARI, Aslam, M. , ODENBAUGH, Amy, L. , RADHAKRISHNAN, Balasingam
IPC分类号： A01N61/00
CPC分类号： A61K38/28 , A61K45/06 , A61K47/60
摘要： A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may also result in less inter-subject variability than polydispersed mixtures of similar conjugates.
摘要翻译：公开了混合物的混合物，其中混合物中的每个缀合物包含与包含聚亚烷基二醇部分的低聚物偶联的胰岛素药物。该混合物可以表现出比类似共轭物的多分散混合物更高的体内活性。与类似共轭物的多分散混合物相比，混合物在存活肠内消化的体外模型时也可能更有效。与相似缀合物的多分散混合物相比，混合物还可导致较少的受试者间变异性。

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