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21. 发明授权

US08569466B2 Aromatic carboxylic acid derivatives for treatment and prophylaxis of gastrointestinal diseases including colon cancers 失效
公开(公告)号：US08569466B2
公开(公告)日：2013-10-29
申请号：US13063445
申请日：2009-09-10
申请人： Nnochiri Ekwuribe
发明人： Nnochiri Ekwuribe
IPC分类号： C07C309/24 , C07C245/06 , C07C245/08 , A61K31/185 , A61K31/353 , A61K31/655
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.

22. 发明申请

US20070060552A1 Methods and compositions employing 4-aminophenylacetic acid compounds 有权
标题翻译：采用4-氨基苯乙酸化合物的方法和组合物
公开(公告)号：US20070060552A1
公开(公告)日：2007-03-15
申请号：US10594046
申请日：2005-03-22
申请人： Nnochiri Ekwuribe , Rodger Liddle
发明人： Nnochiri Ekwuribe , Rodger Liddle
IPC分类号： A61K31/655 , A61K31/56 , A61K31/195
CPC分类号： A61K45/06 , A61K31/195 , A61K31/56 , A61K31/655 , 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炎症和/或粘膜组织如炎性肠病的疾病的方法。本发明的方法和组合物还包括用于治疗这种疾病的4-APAA化合物和5-ASA化合物的组合。

23. 发明申请

US20060172933A1 Natriuretic compounds, conjugates, and uses thereof 失效
标题翻译：利尿钠化合物，缀合物及其用途
公开(公告)号：US20060172933A1
公开(公告)日：2006-08-03
申请号：US10999761
申请日：2004-11-30
申请人： Kenneth James , Balasingham Radhakrishnan , Navdeep Malkar , Mark Miller , Nnochiri Ekwuribe
发明人： Kenneth James , Balasingham Radhakrishnan , Navdeep Malkar , Mark Miller , Nnochiri Ekwuribe
IPC分类号： A61K38/17 , C07K14/47
CPC分类号： C07K14/58 , A61K38/00 , A61K47/60 , C07K14/72 , C07K16/26
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.
摘要翻译：本发明公开了改良的利尿钠化合物及其缀合物。特别地，提供了缀合形式的hBNP，其包括与其连接的至少一个修饰部分。修饰的利尿钠化合物缀合物保留刺激cGMP产生，结合NPR-A受体的活性，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。还公开了利尿钠化合物的类似物，其具有不同于天然序列的氨基酸序列。

24. 发明申请

US20060074009A1 Natriuretic compounds, conjugates, and uses thereof 审中-公开
公开(公告)号：US20060074009A1
公开(公告)日：2006-04-06
申请号：US11138194
申请日：2005-05-26
申请人： Kenneth James , Balasingham Radhakrishnan , Navdeep Malkar , Mark Miller , Nnochiri Ekwuribe
发明人： Kenneth James , Balasingham Radhakrishnan , Navdeep Malkar , Mark Miller , Nnochiri Ekwuribe
IPC分类号： A61K38/17 , C07K14/47
CPC分类号： C07K14/58 , A61K38/00 , A61K47/60 , C07K14/72 , C07K16/26
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.

25. 发明申请

US20050181976A1 Amphiphilic oligomers 审中-公开
标题翻译：两亲低聚物
公开(公告)号：US20050181976A1
公开(公告)日：2005-08-18
申请号：US10977849
申请日：2004-10-29
申请人： Nnochiri Ekwuribe
发明人： Nnochiri Ekwuribe
IPC分类号： A61K9/107 , A61K9/48 , A61K38/00 , A61K38/28 , A61K38/46 , A61K47/48 , A61K49/00 , B29C59/00 , B60R21/20 , B60R21/215 , C07K1/107 , C07K14/62 , C12N9/96 , A61K38/17 , C07K14/47
CPC分类号： A61K38/465 , A61K9/1075 , A61K9/4858 , A61K38/28 , A61K47/56 , A61K47/60 , B29C59/007 , B29C2793/009 , B29L2031/3038 , B60R21/2165 , C07K1/1077 , C07K14/62 , C12N9/96 , C12Y301/03001
摘要： A therapeutic formulation comprising a microemulsion of a therapeutic agent in free and/or conjugatively coupled form, wherein the microemulsion comprises a water-in-oil (w/o) microemulsion including a lipophilic phase and a hydrophilic phase, and has a hydrophilic and lipophilic balance (HLB) value between 3 and 7, wherein the therapeutic agent may for example be selected from the group consisting of insulin, calcitonin, ACTH, glucagon, somatostatin, somatotropin, somatomedin, parathyroid honnone, erythropoietin, hypothalamic releasing factors, prolactin, thyroid stimulating hormones, endorphins, enkephalins, vasopressin, non-naturally occurring opioids, superoxide dismutase, interferon, asparaginase, arginase, arginine deaminease, adenosine deaminase, ribonuclease, trypsin, chymotrypsin, papain, Ara-A (Arabinofuranosyladenine), Acylguanosine, Nordeoxyguanosine, Azidothym id ine, Didesoxyadenosine, Dideoxycytidine, Dideoxyinosine Floxuridine, 6-Mercaptopurine, Doxorubicin, Daunorubicin, or I-darubicin, Erythromycin, Vancomycin, oleandomycin, Ampicillin; Quinidine and Heparin. In a particular aspect, the invention comprises an insulin composition suitable for parenteral as well as non-parenteral administration, preferably oral or parenteral administration, comprising insulin covalently coupled with a polymer including (i) a linear polyalkylene glycol moiety and (ii) a lipophilic moiety, wherein the insulin, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the insulin in the composition has an enhanced in vivo resistance to enzymatic degradation, relative to insulin alone. The microemulsion compositions of the invention are usefully employed in therapeutic as well as non-therapeutic, e.g., diagnostic, applications.
摘要翻译：一种包含游离和/或共轭偶联形式的治疗剂的微乳液的治疗剂型，其中所述微乳液包括包含亲油相和亲水相的油包水（w / o）微乳液，并具有亲水和亲脂性平衡（HLB）值在3和7之间，其中治疗剂可以例如选自胰岛素，降钙素，ACTH，胰高血糖素，生长抑素，生长激素，生长因子，甲状旁腺激素，促红细胞生成素，下丘脑释放因子，催乳素，甲状腺刺激激素，内啡肽，脑啡肽，加压素，非天然存在的阿片样物质，超氧化物歧化酶，干扰素，天冬酰胺酶，精氨酸酶，精氨酸脱胺酶，腺苷脱氨酶，核糖核酸酶，胰蛋白酶，糜蛋白酶，木瓜蛋白酶，Ara-A（阿拉伯呋喃糖基腺嘌呤），酰基鸟苷， idede，Didesoxyadenosine，Dideoxycytidine，Dideoxyinosine Flouuridine，6-Mercaptopurine，Doxorubicin，Daunorubici n或I-dorubicin，红霉素，万古霉素，oleandomycin，氨苄青霉素; 奎尼丁和肝素。在一个特定方面，本发明包括适于肠胃外和非肠胃外给药的胰岛素组合物，优选口服或非肠道给药，其包含与聚合物共价偶联的胰岛素，所述聚合物包括（i）线性聚亚烷基二醇部分和（ii）亲脂性部分，其中胰岛素，线性聚亚烷基二醇部分和亲脂性部分相对于彼此构象地排列，使得组合物中的胰岛素相对于单独的胰岛素具有增强的体内抗酶降解性。本发明的微乳液组合物可用于治疗以及非治疗性，例如诊断性应用。

26. 发明申请

US20050054728A1 Immunoregulatory compounds and derivatives and methods of treating diseases therewith 有权
标题翻译：免疫调节化合物及其治疗疾病的衍生物和方法
公开(公告)号：US20050054728A1
公开(公告)日：2005-03-10
申请号：US10967736
申请日：2004-10-18
申请人： Nnochiri Ekwuribe , Jennifer Riggs-Sauthier
发明人： Nnochiri Ekwuribe , Jennifer Riggs-Sauthier
IPC分类号： A61P1/04 , A61K31/194 , A61K31/195 , A61K31/196 , A61K31/215 , A61K31/606 , A61P1/00 , A61P29/00 , A61P43/00 , C07C245/08
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至C 4烷基，R 2是：其中R 5选自由氢和C 1至C 4烷基组成的组，或其中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状况如炎性肠病的方法：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选自氢和-C（O）R 13，其中R 13为C 1至C 6烷基或芳基。

27. 发明授权

US07625995B2 Aryl carbamate oligomers for hydrolyzable prodrugs and prodrugs comprising same 有权
标题翻译：用于可水解前药的芳基氨基甲酸酯低聚物和包含其的前体药物
公开(公告)号：US07625995B2
公开(公告)日：2009-12-01
申请号：US12037445
申请日：2008-02-26
申请人： Nnochiri Ekwuribe , Amy L. Odenbaugh
发明人： Nnochiri Ekwuribe , Amy L. Odenbaugh
IPC分类号： A61K38/00 , C07K14/00
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: where R1 is selected from the group consisting of alkyl, CH2(OC2H4)OCH3, and —(OC2H4)OCH3; n is 0-4; Olig is an oligomer having a formula: -L-O-PAGR.R2]q where L is a optional linker moiety selected from the group consisting of —CH2O—, —CH2OX—, —OX—, —C(O)—, —C(O)X, —NH—, —NHC(O)—, —XNHC(O)—, —NHC(O)X—, —C(O)NH—, —C(O)NHX—, and where X is alky1-6 or is not present, Y is N or O or is not present, and R3 is alkyl1-6; PAG is a linear or branched polyalkylene glycol moiety; R2 is an alkyl1-22 capping moiety if X is present or alkyl2-22 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：本发明提供具有下式的化合物：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是具有下式的低聚物：-LO-PAGR.R2] q其中L是选自-CH 2 O-，-CH 2 OX - ， - O - ， - C（O） - ， - C （O）X，-NH-，-NHC（O） - ， - N-NH（O） - ， - NHC（O）X - ， - C（O）NH-， - （O）NHX-，其中X 是烷基-16或不存在，Y是N或O或不存在，并且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R2是烷基-22封端部分，如果X不存在，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。

28. 发明授权

US07119074B2 Treatment of cancers, tumors and malignancies using amphiphilic prodrugs 失效
标题翻译：使用两亲前体药物治疗癌症，肿瘤和恶性肿瘤
公开(公告)号：US07119074B2
公开(公告)日：2006-10-10
申请号：US10808044
申请日：2004-03-24
申请人： Nnochiri Ekwuribe , Christopher H. Price , Tatyana A. Dyakonov
发明人： Nnochiri Ekwuribe , Christopher H. Price , Tatyana A. Dyakonov
IPC分类号： A61K31/704
CPC分类号： A61K47/60
摘要： The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.
摘要翻译：本发明提供了包含与PEG-低聚物/聚合物缀合的治疗化合物的两亲前药，以及使用所述前体药物以使药物能够穿过血脑屏障进入中枢神经系统的口服药物递送和/或递送的方法。

29. 发明申请

US20060153801A1 Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same 审中-公开
公开(公告)号：US20060153801A1
公开(公告)日：2006-07-13
申请号：US11364061
申请日：2006-02-28
申请人： Nnochiri Ekwuribe
发明人： Nnochiri Ekwuribe
IPC分类号： A61K38/22 , A61K38/19 , A61K38/16
CPC分类号： A61K39/385 , A61K47/60 , A61K2039/6093 , C07K1/1077
摘要： A non-polydispersed mixture of conjugates in which each conjugate in the mixture comprises a 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 be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may result in less inter-subject variability than polydispersed mixtures of similar conjugates.

30. 发明申请

US20060008850A1 Combinatorial synthesis of PEG oligomer libraries 有权
标题翻译： PEG寡聚体文库的组合合成
公开(公告)号：US20060008850A1
公开(公告)日：2006-01-12
申请号：US11174938
申请日：2005-07-05
申请人： Jennifer Riggs-Sauthier , Nnochiri Ekwuribe
发明人： Jennifer Riggs-Sauthier , Nnochiri Ekwuribe
IPC分类号： C07C41/03 , G01N33/53
CPC分类号： C07C43/11 , C07C69/28
摘要： A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
摘要翻译：建立了一种简单的扩链方法，用于单保护单分散PEG二醇材料的放大。 THP-（OCH 2 CH 2 CH 2）n -OMs（n = 4,8,12）与大量可商购的反应在碱性条件下，H（OCH 2 CH 2 CH 2）n -OH（n = 1-4）导致THP-（OCH _{2 H 2 -OH（n = 5-15）。类似地，Me-（OCH 2 CH 2 CH 2）n -OH（n = 4-11,13）由Me-（OCH （n = 3，7，11）n -OMs（n = 3,7,11）。对于链延伸步骤，通过萃取纯化获得40-80％的产率。通过烷基化或酰化THP-（OCH 2 CH 2 CH 2）n H 2生成PEG低聚物文库I和II，其总产率为50-95％ -OH（n = 1-15），随后脱保护。使用X-（CH}

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