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1. 发明申请

WO2011011543A1 OLIGOMER-OPIOID AGONIST CONJUGATES 审中-公开
标题翻译：低分子阿片受体激动剂
公开(公告)号：WO2011011543A1
公开(公告)日：2011-01-27
申请号：PCT/US2010/042792
申请日：2010-07-21
申请人： NEKTAR THERAPEUTICS , RIGGS-SAUTHIER, Jennifer , DENG, Bo-Liang , RILEY, Timothy, A.
发明人： RIGGS-SAUTHIER, Jennifer , DENG, Bo-Liang , RILEY, Timothy, A.
IPC分类号： A61K47/48 , A61P25/04 , A61P25/36
CPC分类号： A61K47/60
摘要： The invention provides conjugates wherein the opioid agonists, hydroxycodone (oxycodone) and hydrocodone (dihydrocodeiπone) are covalently attached to poly(ethylene glycol) oligomers. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the opioid agonist not attached to the PEG oligomers.
摘要翻译：本发明提供了缀合物，其中阿片样物质激动剂羟考酮（羟考酮）和氢可酮（氢可待因酮）共价连接到聚（乙二醇）低聚物上。本发明的缀合物当通过多种施用途径中的任一种施用时，表现出与不连接到PEG低聚物的阿片样物质激动剂不同的特征。

2. 发明申请

WO2010120387A1 OLIGOMER-PROTEIN TYROSINE KINASE INHIBITOR CONJUGATES 审中-公开
标题翻译：低聚物蛋白酪氨酸激酶抑制剂共轭物
公开(公告)号：WO2010120387A1
公开(公告)日：2010-10-21
申请号：PCT/US2010/001163
申请日：2010-04-19
申请人： NEKTAR THERAPEUTICS , RIGGS-SAUTHIER, Jennifer , ZHANG, Wen
发明人： RIGGS-SAUTHIER, Jennifer , ZHANG, Wen
IPC分类号： A61K47/48
CPC分类号： A61K47/60
摘要： The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.
摘要翻译：本发明涉及（除其他之外）低聚物-PTK抑制剂缀合物和相关化合物。当通过多种给药途径中的任一种给药时，本发明的化合物显示出优于缺乏水溶性非肽类低聚物的PTK抑制剂化合物的优点。

3. 发明申请

WO2008112286A3 DE NOVO SYNTHESIS OF CONJUGATES 审中-公开
标题翻译：合并的合并
公开(公告)号：WO2008112286A3
公开(公告)日：2009-11-19
申请号：PCT/US2008003351
申请日：2008-03-12
申请人： NEKTAR THERAPEUTICS , RIGGS-SAUTHIER JENNIFER , DENG BO-LIANG , REN ZHONGXU , ZHANG WEN , GU XUYUAN , DUARTE FRANCO J
发明人： RIGGS-SAUTHIER JENNIFER , DENG BO-LIANG , REN ZHONGXU , ZHANG WEN , GU XUYUAN , DUARTE FRANCO J
IPC分类号： A61K47/48
CPC分类号： C08G65/3315 , A61K47/60 , C08G65/33306 , C08G65/33337 , C08G65/33368 , C08G65/33389 , C08L2203/02
摘要： The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.
摘要翻译：本发明提供了通过共价连接由水溶性低聚物组合物获得的水溶性低聚物进行化学修饰的小分子药物的制备方法。通过修饰合成途径产生这样的药物，以将低聚物连接到中间体化合物，然后完成合成路径。

4. 发明申请

WO2009131695A1 OLIGOMER-BIS-CHROMONYL COMPOUND CONJUGATES 审中-公开
标题翻译：低聚物双官能团化合物
公开(公告)号：WO2009131695A1
公开(公告)日：2009-10-29
申请号：PCT/US2009/002525
申请日：2009-04-23
申请人： NEKTAR THERAPEUTICS , RIGGS-SAUTHIER, Jennifer , DENG, Bo-liang
发明人： RIGGS-SAUTHIER, Jennifer , DENG, Bo-liang
IPC分类号： A61K47/48 , A61P11/06
CPC分类号： A61K47/48215 , A61K31/353 , A61K47/60
摘要： The invention provides oligomer-bis-chromonyl compound conjugates. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
摘要翻译：本发明提供低聚物 - 双 - 色酮化合物共轭物。当通过任何多种施用途径施用时，本发明的缀合物显示出优于先前给予的化合物的优点。

5. 发明申请

WO2009054916A2 OLIGOMER CONJUGATES OF LIDOCAINE AND ITS DERIVATIVES 审中-公开
标题翻译： LIDOCAINE及其衍生物的低聚物
公开(公告)号：WO2009054916A2
公开(公告)日：2009-04-30
申请号：PCT/US2008/011880
申请日：2008-10-17
申请人： NEKTAR THERAPEUTICS AL, CORPORATION , RIGGS-SAUTHIER, Jennifer , DENG, Bo-liang
发明人： RIGGS-SAUTHIER, Jennifer , DENG, Bo-liang
IPC分类号： A61K47/48 , A61K31/167 , A61K31/138 , C07C237/04 , C07C217/18
CPC分类号： C07C237/04 , A61K47/55 , A61K47/60 , C07C217/18
摘要： The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.
摘要翻译：本发明提供通过共价连接水溶性低聚物进行化学修饰的小分子药物。

6. 发明申请

WO2009045539A3 PEG-CORTICOSTEROID CONJUGATES 审中-公开
公开(公告)号：WO2009045539A3
公开(公告)日：2009-04-09
申请号：PCT/US2008/011523
申请日：2008-10-03
申请人： NEKTAR THERAPEUTICS , ZHANG, Wen , RIGGS-SAUTHIER, Jennifer , HARRIS, J., Milton , BENTLEY, Michael, D.
发明人： ZHANG, Wen , RIGGS-SAUTHIER, Jennifer , HARRIS, J., Milton , BENTLEY, Michael, D.
IPC分类号： A61K47/48
摘要： The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.

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

WO0218324A3 IMMUNOREGULATORY COMPOUNDS, DERIVATIVES THEREOF AND THEIR USE 审中-公开
标题翻译：免疫测定化合物，其衍生物及其用途
公开(公告)号：WO0218324A3
公开(公告)日：2002-08-29
申请号：PCT/US0126697
申请日：2001-08-28
申请人： NOBEX CORP , EKWURIBE NNOCHIRI N , RIGGS-SAUTHIER JENNIFER
发明人： EKWURIBE NNOCHIRI N , RIGGS-SAUTHIER JENNIFER
IPC分类号： A61P1/04 , A61K31/194 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/606 , A61P1/00 , A61P29/00 , A61P43/00 , C07C245/08 , A61K31/655
CPC分类号： A61K31/195 , A61K31/196 , A61K31/215 , A61K31/24 , C07C229/42 , C07C245/08 , A61K2300/00
摘要： Compounds are disclosed having the structure of Formula (I), where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is (II), where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or (III), where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed (IV), where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and -C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.
摘要翻译：公开了具有式（I）结构的化合物，其中R 1，R 3和R 4独立地为氢或C 1至C 4烷基，R 2为（II），其中R 5选自氢和C 1至C 4烷基或（III），其中R 6，R 7和R 8独立地为氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。这些化合物可用于预防或治疗各种疾病，特别是GI道的炎性病症。还公开了使用具有下式的化合物治疗胃肠道炎症性疾病如炎症性肠病的方法（Ⅳ），其中R9，R10和R11独立地选自氢和C1至C4烷基，R12 选自氢和-C（O）R 13，其中R 13是C 1至C 6烷基或芳基。

9. 发明申请

WO2012166555A1 WATER - SOLUBLE POLYMER - LINKED BINDING MOIETY AND DRUG COMPOUNDS 审中-公开
标题翻译：水 - 可溶聚合物 - 连接的结合剂和药物化合物
公开(公告)号：WO2012166555A1
公开(公告)日：2012-12-06
申请号：PCT/US2012/039453
申请日：2012-05-24
申请人： NEKTAR THERAPEUTICS , RIGGS-SAUTHIER, Jennifer , CHARYCH, Deborah, H. , EID, Clark, Norman, Jr. , FRY, Dennis, G. , KONAKOVA, Marina , LOEHRLEIN, Christine, Frances
发明人： RIGGS-SAUTHIER, Jennifer , CHARYCH, Deborah, H. , EID, Clark, Norman, Jr. , FRY, Dennis, G. , KONAKOVA, Marina , LOEHRLEIN, Christine, Frances
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/48215 , A61K47/60 , A61K47/6855
摘要： Compounds comprising a binding moiety, water-soluble, non-peptidic polymer, and drug are provided. Also provided are methods preparing such compounds, compositions comprising such compounds and methods for administering and using such compounds and compositions.
摘要翻译：提供了包含结合部分，水溶性，非肽聚合物和药物的化合物。还提供了制备这种化合物的方法，包含这些化合物的组合物以及用于施用和使用这些化合物和组合物的方法。

10. 发明申请

WO2012088506A1 POLYMER-SEMAXANIB MOIETY CONJUGATES 审中-公开
公开(公告)号：WO2012088506A1
公开(公告)日：2012-06-28
申请号：PCT/US2011/067175
申请日：2011-12-23
申请人： NEKTAR THERAPEUTICS , RIGGS-SAUTHIER, Jennifer , ALLUMS-DONALD, Stephanie , CULBERTSON, Sean, M.
发明人： RIGGS-SAUTHIER, Jennifer , ALLUMS-DONALD, Stephanie , CULBERTSON, Sean, M.
IPC分类号： A61K47/48 , A61P35/00
CPC分类号： A61K47/545 , A61K31/404 , A61K47/60 , C07D209/34
摘要： The invention relates to (among other things) polymer-semaxanib moiety conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over the semaxanib moiety in unconjugated form.
摘要翻译：本发明涉及（尤其是）聚合物 - 半卡尼部分缀合物和相关化合物。本发明的化合物当通过任何多种施用途径施用时，以非共轭形式显示优于semaxanib部分的优点。

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