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1. 发明申请

WO2004043347A2 CALCITONIN DRUG-OLIGOMER CONJUGATES, AND USES THEREOF 审中-公开
标题翻译：降钙素药物 - 低聚物缀合物及其用途
公开(公告)号：WO2004043347A2
公开(公告)日：2004-05-27
申请号：PCT/US2003/033618
申请日：2003-10-24
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri, N. , RADHAKRISHNAN, Balasingam
发明人： EKWURIBE, Nnochiri, N. , RADHAKRISHNAN, Balasingam
IPC分类号： A61K
CPC分类号： C07K14/585 , A61K47/60
摘要： Calcitonin drug-oligomer conjugates that include a calcitonin drug coupled to an oligomer including a single polyalkylene glycol moiety consisting of between 4 and 10 polyalkylene glycol subunits are disclosed. Pharmaceutical compositions including such conjugates and methods of treating bone disorders by administering such conjugates are also disclosed.
摘要翻译：包括降钙素药物的降钙素药物 - 寡聚物缀合物被偶联到包含由4和10个聚亚烷基二醇亚单元组成的单个聚亚烷基二醇部分的寡聚物上。还公开了包含这种缀合物的药物组合物和通过施用这样的缀合物来治疗骨疾病的方法。

2. 发明申请

WO2003022208A2 PHARMACEUTICAL COMPOSITIONS OF INSULIN DRUG-OLIGOMER CONJUGATES AND METHODS OF TREATING DISEASES THEREWITH 审中-公开
标题翻译：胰高血糖素联合药物的药物组合物及其治疗方法
公开(公告)号：WO2003022208A2
公开(公告)日：2003-03-20
申请号：PCT/US2002/028429
申请日：2002-09-06
申请人： NOBEX CORPORATION , SOLTERO, Richard , RADHAKRISHNAN, Balasingham , EKWURIBE, Nnochiri, N. , REHLAENDER, Bruce , HICKEY, Anthony , BOVET, Li, Li
发明人： SOLTERO, Richard , RADHAKRISHNAN, Balasingham , EKWURIBE, Nnochiri, N. , 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 an insulin drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The insulin 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 an insulin deficiency 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：描述了包括胰岛素药物 - 低聚物缀合物，脂肪酸组分和胆汁盐组分的药物组合物。胰岛素药物与低聚部分共价偶联。脂肪酸组分和胆汁盐组分以1:5至5:1的重量比重存在。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胰岛素缺乏症的方法，以及提供这种药物组合物的方法。

3. 发明申请

WO2006014549A3 SYNTHESIS OF AZO BONDED IMMUNOREGULATORY COMPOUNDS 审中-公开
公开(公告)号：WO2006014549A3
公开(公告)日：2006-02-09
申请号：PCT/US2005/024109
申请日：2005-07-07
申请人： NOBEX CORPORATION , SAUTHIER, Jennifer, A., Riggs , EKWURIBE, Nnochiri, N.
发明人： SAUTHIER, Jennifer, A., Riggs , EKWURIBE, Nnochiri, N.
IPC分类号： C07D207/09 , C07D207/10 , A61K31/4025
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.

4. 发明申请

WO2005116655A3 NATRIURETIC COMPOUNDS, CONJUGATES, AND USES THEREOF 审中-公开
公开(公告)号：WO2005116655A3
公开(公告)日：2005-12-08
申请号：PCT/US2005/019249
申请日：2005-05-26
申请人： NOBEX CORPORATION , JAMES, Kenneth, D. , RADHAKRISHNAN, Balasingam , MALKAR, Navdeep, B. , MILLER, Mark, A. , EKWURIBE, Nnochiri, N.
发明人： JAMES, Kenneth, D. , RADHAKRISHNAN, Balasingam , MALKAR, Navdeep, B. , MILLER, Mark, A. , EKWURIBE, Nnochiri, N.
IPC分类号： A61K38/00
摘要： Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.

5. 发明申请

WO2004043396A2 MODIFIED CARBAMATE-CONTAINING PRODRUGS AND METHODS OF SYNTHESIZING SAME 审中-公开
标题翻译：改性含碳酸酯的制剂及其合成方法
公开(公告)号：WO2004043396A2
公开(公告)日：2004-05-27
申请号：PCT/US2003/035995
申请日：2003-11-07
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri, N. , RIGGS-SAUTHIER, Jennifer , DYAKONOV, Tatyana
发明人： EKWURIBE, Nnochiri, N. , RIGGS-SAUTHIER, Jennifer , DYAKONOV, Tatyana
IPC分类号： A61K
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：公开了具有可水解氨基甲酸酯部分的前药，包含前药的组合物，制备前体药物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，R是修饰生物活性剂的各种性质的部分。生物活性剂还包括官能团，例如酰胺，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。相对于常规氨基甲酸酯基团，另外的羰基或磺酰基的存在使得氨基甲酸酯基团更易于水解。前药在某些环境中比生物活性剂更稳定，并且可以允许药物口服给药，在那些其中生物活性剂必须通过注射或静脉内给药施用的那些实施方案中。

6. 发明申请

WO2002098949A1 METHODS OF SYNTHESIZING SUBSTANTIALLY MONODISPERSED MIXTURES OF POLYMERS HAVING POLYETHYLENE GLYCOL MOIETIES 审中-公开
标题翻译：合成具有聚乙二醇纤维素的聚合物的主要单体混合物的方法
公开(公告)号：WO2002098949A1
公开(公告)日：2002-12-12
申请号：PCT/US2002/017619
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： C08G65/00
CPC分类号： C08G65/334 , C08L71/02 , C08L71/00
摘要： Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R 1 (OC 2 H 4 )n-O - X + (I) wherein R 1 is H or a lipophilic moiety; n is from 1 to 25; and X + is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R 2 (OC 2 H 4 ) m -OMs (II) wherein R 2 is H or a lipophilic moiety; and m is from 1 to 25,under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R 2 (OC 2 H 4 ) m+n -OR 1 (III).
摘要翻译：合成基本上单分散的包含聚乙二醇部分的聚合物的混合物的方法包括：使具有式I结构的化合物的基本上单分散的混合物：R 1（OC 2 H 4）n O X +（I） 1>是H或亲脂性部分; n为1至25; 并且X +是具有式II结构的化合物的基本上单分散的混合物：R 2（OC 2 H 4）m-OM（II）其中R 2是H或亲油部分; 并且m为1至25，在足以提供包含聚乙二醇部分并且具有式III结构的基本单分散混合物的条件下：R 2（OC 2 H 4）m + n -OR 1（III）。

7. 发明申请

WO2002088070A1 METHODS OF SYNTHESIZING ACYLANILIDES INCLUDING BICALUTAMIDE AND DERIVATIVES THEREOF 审中-公开
标题翻译：合成亚胺嘧啶的方法，其中包括苯甲酰胺及其衍生物
公开(公告)号：WO2002088070A1
公开(公告)日：2002-11-07
申请号：PCT/US2002/013591
申请日：2002-05-02
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri, N. , JAMES, Kenneth, D.
发明人： EKWURIBE, Nnochiri, N. , JAMES, Kenneth, D.
IPC分类号： C07C255/50
CPC分类号： C07C253/30 , C07C315/04 , C07C317/46 , C07C255/60
摘要： Methods of synthesizing an acylanilide include contacting a compound having the structure of Formula I with a compound having the structure of Formula II under conditions sufficient to provide a compound having the structure of Formula III and treating the compound of Formula III under conditions sufficient to provide an acylanilide. The compound of Formula III may be addition reacted with a compound having the structure of Formula IV: under conditions sufficient to provide an acylanilide having the structure of Formula V.
摘要翻译：合成酰基酰苯胺的方法包括使具有式I结构的化合物与具有式II结构的化合物在足以提供具有式III结构的化合物的条件下接触，并在足以提供 N-酰基苯胺。式III的化合物可以与具有式IV结构的化合物反应：在足以提供具有式V结构的酰基酰苯胺的条件下。

8. 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。

9. 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。

10. 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。

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