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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

WO2003105768A3 METHODS OF REDUCING HYPOGLYCEMIC EPISODES IN THE TREATMENT OF DIABETES MELLITUS 审中-公开
公开(公告)号：WO2003105768A3
公开(公告)日：2003-12-24
申请号：PCT/US2003/018763
申请日：2003-06-13
申请人： NOBEX CORPORATION , STILL, James, Gordon , KOSUTIC, Gordana
发明人： STILL, James, Gordon , KOSUTIC, Gordana
IPC分类号： A61K38/28
摘要： The present invention provides compositions and methods for reducing hypoglycemic episodes experienced by a subject in need of treatment for diabetes mellitus, said method comprising orally administering an amount of an insulin polypeptide-oligomer conjugate to the subject, wherein: i) the amount of the insulin polypeptide-oligomer conjugate reduces the number and/or severity of hypoglycemic episodes experienced by the subject during a given time period when compared with the number and/or severity of hypoglycemic episodes that would have been experienced during a similar time period by the subject or by subjects in a control group parenterally administered insulin or an insulin analog in an amount that provides a substantially equivalent level of glycemic control; and ii) the oligomer of the insulin polypeptide-oligomer conjugate comprises a hydrophilic moiety and a lipophilic moiety.

3. 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。

4. 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.

5. 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.

6. 发明申请

WO2005016240A2 ARYL CARBAMATE OLIGOMERS FOR HYDROLYZABLE PRODRUGS AND PRODRUGS COMPRISING SAME 审中-公开
标题翻译：用于可水解产品的ARYL碳酸酯低聚物和包含其的原料
公开(公告)号：WO2005016240A2
公开(公告)日：2005-02-24
申请号：PCT/US2004/015004
申请日：2004-05-06
申请人： NOBEX CORPORATION , EKWURIBE, Nnochiri N. , ODENBAUGH, Amy L.
发明人： EKWURIBE, Nnochiri N. , ODENBAUGH, Amy L.
IPC分类号： A61K
CPC分类号： C07C235/48 , C07C41/16 , C07C41/26 , C07C43/23 , C07C45/673 , C07C45/71 , C07C47/575 , C07C49/84 , C07C271/22 , C07C271/28 , C07K7/02 , C07K7/06 , C07C43/2055
摘要： The present invention provides a compound having a formula: (I) where R 1 is selected from the group consisting of alkyl, -CH 2 (OC 2 H4)OCH 3 , and -(OC 2 H 4 )OCH 3 ; n is 0-4; Olig is an oligomer having a formula (I) where L is a optional linker moiety selected from the group consisting of CH 2 O , CH 2 OX , OX , C(O) , C(O)X, NH , NHC(O) , XNHC(O) , NHC(O)X , C(O)NH , C(O)NHX , and (I), where X is alkyl 1-6 or is not present, Y is N or O or is not present, and R 3 is alkyl 1-6 ; PAG is a linear or branched polyalkylene glycol moiety; R 2 is an alkyl 1-22 capping moiety if X is present or alkyl 2-22 if X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5.
摘要翻译：本发明提供具有式（I）的化合物，其中R 1选自烷基，-CH 2（OC 2 H 4）OCH 3和 - （OC 2 H 4）OCH 3; n为0-4; Olig是具有式（I）的低聚物，其中L是选自CH 2 O，CH 2 OX，OX，C（O），C（O）X，NH，NHC（O），XNHC（O）），NHC（O）X，C（O）NH，C（O）NHX和（I），其中X是烷基1-6或不存在，Y是N或O或不存在，R 3 >是烷基1-6; PAG是直链或支链的聚亚烷基二醇部分; 如果X存在，则R 2为烷基-22封端部分，如果不存在X则为烷基2-22; q是PAG上从1到最大分支数的数字; m为1-5。

7. 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。

8. 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）。

9. 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。

10. 发明申请

WO2006076471A2 BNP CONJUGATES AND METHODS OF USE 审中-公开
标题翻译： BNP联合使用和使用方法
公开(公告)号：WO2006076471A2
公开(公告)日：2006-07-20
申请号：PCT/US2006/001049
申请日：2006-01-12
申请人： NOBEX CORPORATION , JAMES, Kenneth
发明人： JAMES, Kenneth
CPC分类号： C07K14/58 , A61K38/00
摘要： Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of liBNP 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, decreasing arterial blood pressure 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 hBNP compound are also disclosed, having an amino acid sequence that is other than the native sequence.
摘要翻译：本发明公开了改进的利尿钠化合物及其缀合物。特别地，提供了缀合形式的liBNP，其包括与其连接的至少一个修饰部分。修饰的利钠化合物缀合物保留刺激cGMP产生，结合NPR-A受体，降低动脉血压的活性，并且在一些实施方案中，与未修饰的对应利钠化合物相比，循环中的半衰期改善。口服，胃肠外，肠内，皮下，肺和静脉内形式的化合物和缀合物可以制备为用于心脏状况的治疗和/或治疗，特别是充血性心力衰竭。还公开了包含具有各种长度和构型的寡聚结构的修饰部分。还公开了具有不同于天然序列的氨基酸序列的hBNP化合物的类似物。

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