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1. 发明申请

US20050026996A1 Taxane prodrugs 审中-公开
标题翻译：紫杉烷前药
公开(公告)号：US20050026996A1
公开(公告)日：2005-02-03
申请号：US10870505
申请日：2004-06-17
申请人： Nnochiri Ekwuribe , Christopher Price , Gary Bartley
发明人： Nnochiri Ekwuribe , Christopher Price , Gary Bartley
IPC分类号： A61K9/08 , A61K9/10 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/24 , A61K31/337 , A61K31/704 , A61K33/24 , A61K45/06 , A61K47/48 , A61P13/12 , A61P33/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07D305/14 , C07
CPC分类号： A61K31/704 , A61K31/335 , A61K31/70 , A61K33/24 , A61K45/06 , A61K47/60 , Y02A50/411 , A61K2300/00
摘要： Taxane prodrugs comprise a taxane joined by a hydrolyzable bond to one or more oligomers that comprise a polyethylene glycol moiety. The oligomer preferably further comprises a salt-forming moiety.
摘要翻译：紫杉烷前药包含通过可水解键与包含聚乙二醇部分的一种或多种低聚物连接的紫杉烷。低聚物优选还包含形成盐的部分。

2. 发明申请

US20050059799A1 Substantiallymonodispersed mixtures of polymers having polyethylene glycol moieties 有权
标题翻译：具有聚乙二醇部分的聚合物的主要单分散混合物
公开(公告)号：US20050059799A1
公开(公告)日：2005-03-17
申请号：US10977973
申请日：2004-10-29
申请人： Nnochiri Ekwuribe , Christopher Price , Aslam Ansari , Amy Odenbaugh
发明人： Nnochiri Ekwuribe , Christopher Price , Aslam Ansari , Amy Odenbaugh
IPC分类号： C07C41/16 , C07C43/13 , C08G65/08 , C08G65/334 , C08L71/02 , C12N5/00
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: R1(OC2H4)b—O−X+ (I) wherein R1 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: R2(OC2H4)m—OMs (II) wherein R2 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: R2(OC2H4)m+n—OR1 (III). Substantially monodispersed mixtures of polymers comprising polyethylene glycol moieties are also disclosed.
摘要翻译：合成包含聚乙二醇部分的聚合物的基本上单分散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）b 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）。还公开了包含聚乙二醇部分的聚合物的基本上单分散的混合物。

3. 发明申请

US20070213262A1 Mixtures Of Calcitonin Drug-Oligomer Conjugates And Methods Of Use In Pain Treatment 审中-公开
标题翻译：降钙素药物低聚物缀合物的混合物及其在疼痛治疗中的应用
公开(公告)号：US20070213262A1
公开(公告)日：2007-09-13
申请号：US10562478
申请日：2004-05-27
申请人： Gordana Kosutic , Nnochiri Ekwuribe , Christopher H. Price , Christopher Price , Aslam Andsari , Amy Odenbaugh
发明人： Gordana Kosutic , Nnochiri Ekwuribe , Christopher H. Price , Christopher Price , Aslam Andsari , Amy Odenbaugh
IPC分类号： A61K38/17
CPC分类号： A61K38/23 , A61K51/02 , A61K51/0402 , A61K51/0406 , A61K51/0489 , A61K51/0491 , A61K51/10 , A61K51/1241
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. The compositions of this invention are useful in the treatment of various bone disorders and pain.
摘要翻译：公开了混合物的混合物，其中混合物中的每个偶联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时可能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。本发明的组合物可用于治疗各种骨病和疼痛。

4. 发明申请

US20060293219A1 METHODS OF TREATING DIABETES MELLITUS 有权
标题翻译：治疗糖尿病的方法
公开(公告)号：US20060293219A1
公开(公告)日：2006-12-28
申请号：US11424295
申请日：2006-06-15
申请人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy Odenbaugh , Balasingam Radhakrishnan
发明人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy Odenbaugh , Balasingam Radhakrishnan
IPC分类号： A61K38/28
CPC分类号： C07K14/62 , A61K38/28 , A61K47/542 , A61K47/60
摘要： Methods of treating diabetes mellitus in a patient in need of such treatment include administering an effective amount of an insulin drug to the patient in order to treat diabetes mellitus in the patient. Methods according to the present invention may “activate” the liver, potentially restoring normal glucose homeostasis to individuals suffering from diabetes mellitus.
摘要翻译：在需要这种治疗的患者中治疗糖尿病的方法包括向患者施用有效量的胰岛素药物以治疗患者的糖尿病。根据本发明的方法可以“激活”肝脏，潜在地恢复患有糖尿病的个体的正常葡萄糖体内平衡。

5. 发明申请

US20060199759A1 Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same 有权
公开(公告)号：US20060199759A1
公开(公告)日：2006-09-07
申请号：US11417586
申请日：2006-05-04
申请人： Nnochiri Ekwuribe , Christopher Price , Aslam Ansari , Balasingam Radhakrishnan , Amy Odenbaugh
发明人： Nnochiri Ekwuribe , Christopher Price , Aslam Ansari , Balasingam Radhakrishnan , Amy Odenbaugh
IPC分类号： A61K38/28 , C07K14/62
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.

6. 发明申请

US20060100137A1 Methods of treating diabetes mellitus 有权
公开(公告)号：US20060100137A1
公开(公告)日：2006-05-11
申请号：US11314309
申请日：2005-12-21
申请人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy Odenbaugh , Balasingam Radhakrishnan
发明人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy Odenbaugh , Balasingam Radhakrishnan
IPC分类号： A61K38/28 , C07K14/62
CPC分类号： C07K14/62 , A61K38/28 , A61K47/542 , A61K47/60
摘要： Methods of treating diabetes mellitus in a patient in need of such treatment include administering an effective amount of an insulin drug to the patient in order to treat diabetes mellitus in the patient. Methods according to the present invention may “activate” the liver, potentially restoring normal glucose homeostasis to individuals suffering from diabetes mellitus.

7. 发明申请

US20080033153A1 Synthesis of Azo Bonded Immunoregulatory Compounds 有权
标题翻译：偶氮键合的免疫调节化合物的合成
公开(公告)号：US20080033153A1
公开(公告)日：2008-02-07
申请号：US11631582
申请日：2005-07-07
申请人： Jennifer Riggs-Sauthier , Nnochiri Ekwuribe
发明人： Jennifer Riggs-Sauthier , Nnochiri Ekwuribe
IPC分类号： C07C245/08
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 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独立地是氢或C 1 C 1至C 4烷基，R 2是：其中R 5选自氢和C _{C 1至C 4烷基，或其中R 6，R 7和R 8是独立地是氢或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。}

8. 发明申请

US20110319267A1 AROMATIC CARBOXYLIC ACID DERIVATIVES FOR TREATMENT AND PROPHYLAXIS OF GASTROINTESTINAL DISEASES INCLUDING COLON CANCERS 失效
标题翻译：用于治疗和预防胃肠疾病的芳香羧酸衍生物，包括结肠癌
公开(公告)号：US20110319267A1
公开(公告)日：2011-12-29
申请号：US13063445
申请日：2009-09-10
申请人： Nnochiri Ekwuribe
发明人： Nnochiri Ekwuribe
IPC分类号： A01N47/30 , C07C309/24 , C07C245/06 , C07D311/68 , A61K31/655 , A61K31/196 , A61K31/185 , A61K31/353 , A01N41/06 , A01N41/04 , A01N43/16 , A61P1/00 , A61P31/12 , A61P31/04 , A61P31/10 , A61P29/00 , A61P1/04 , A61P35/00 , A61P1/14 , A01P7/04 , A01P13/00 , A01P3/00 , A61P31/00 , A61P37/02 , A61K31/56 , C07C245/08
CPC分类号： A61K31/655 , A01N41/04 , A01N41/06 , A01N41/08 , A61K45/06 , C07C245/06 , C07C245/08 , C07C309/15 , C07C309/24 , C07C311/46 , C07C311/49 , C07C311/54 , C07D311/54 , C07D311/68
摘要： Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.
摘要翻译：公开了在结肠部位代谢为5-ASA或其类似物的前体化合物及其牛磺酸或其类似物。还公开了包括该化合物的药物组合物和使用该化合物的治疗方法。这些化合物可用于治疗或预防胃肠道疾病，包括结肠癌，溃疡性结肠炎和克罗恩氏病。

9. 发明申请

US20070004800A1 IMMUNOREGULATORY COMPOUNDS AND DERIVATIVES AND METHODS OF TREATING DISEASES THEREWITH 有权
标题翻译：免疫组化化合物及其衍生物及其治疗疾病的方法
公开(公告)号：US20070004800A1
公开(公告)日：2007-01-04
申请号：US11470655
申请日：2006-09-07
申请人： Nnochiri Ekwuribe , Jennifer Riggs-Sauthier
发明人： Nnochiri Ekwuribe , Jennifer Riggs-Sauthier
IPC分类号： A61K31/24 , A61K31/195
CPC分类号： A61K31/195 , A61K31/196 , A61K31/215 , A61K31/24 , C07C229/42 , C07C245/08 , Y02A50/475 , Y02A50/481 , 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: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or 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: 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独立地是氢或C 1 C 1至C 4烷基，R 2是：其中R 5选自氢和C _{C 1至C 4烷基，或其中R 6，R 7和R 8是独立地是氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。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：其中R 9，R 10和R 11 独立地选自氢和C 1至C 4烷基，R 12选自基团由氢和-C（O）R 13组成，其中R 13是C 1至C 6 - 烷基或芳基。}

10. 发明申请

US20050054735A1 6-Methoxy-2-naphthylacetic acid prodrugs 审中-公开
标题翻译： 6-甲氧基-2-萘基乙酸前药
公开(公告)号：US20050054735A1
公开(公告)日：2005-03-10
申请号：US10970571
申请日：2004-10-21
申请人： Nnochiri Ekwuribe , Tatyana Dyakonov
发明人： Nnochiri Ekwuribe , Tatyana Dyakonov
IPC分类号： A61P29/00 , A61K31/085 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/21 , A61K31/216 , A61K31/222 , A61K31/235 , A61K31/265 , C07C43/23 , A61K31/445 , A61K31/075 , A61K31/12
CPC分类号： A61K31/16 , A61K31/085 , A61K31/167 , A61K31/21 , A61K31/216 , A61K31/235 , A61K31/265
摘要： The present invention provides therapeutically effective amounts of 6MNA prodrugs. The pharmaceutical composition comprises wherein R is H or COR′, wherein R′ is selected from the group consisting of C1 to C6 alkyl, (CH2)m O(CH2)n, (CH2)m(OC2H4)p O(CH2)n, (CH2)m(OC2H4)p, (OCH2H4)p ONO2 and (OCH2H4)p O(CH2)n wherein m is an integer from 2 to 4, and n and p are integers from 1 to 4. Alternatively, R is a therapeutic moiety.
摘要翻译：本发明提供治疗有效量的6MNA前药。该药物组合物包含其中R是H或COR'，其中R'选自C1-C6烷基，（CH2）m O（CH2）n，（CH2）m（OC2H4）pO（CH2）n ，（CH 2）m（OC 2 H 4）p，（OCH 2 H 4）p ONO 2和（OCH 2 H 4）p O（CH 2）n，其中m是2至4的整数，n和p是1至4的整数。治疗部分。

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