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1. 发明申请

US20080319044A1 Compounds and Methods of Use Thereof 审中-公开
标题翻译：化合物及其使用方法
公开(公告)号：US20080319044A1
公开(公告)日：2008-12-25
申请号：US11718286
申请日：2005-10-27
申请人： John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , Jan J. Scicinski , David Middlemiss
发明人： John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , Jan J. Scicinski , David Middlemiss
IPC分类号： A61K31/404 , C07D209/04 , A61P1/00 , A61P19/02 , A61P17/06 , A61P25/28 , A61P9/00 , A61P3/10 , A61P35/00 , A61P9/12 , A61P15/10
CPC分类号： C07D491/04 , C07D209/08 , C07F5/025
摘要： Indole boronic acid compounds, and analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要翻译：描述了吲哚硼酸化合物及其类似物和药物制剂，以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法。

2. 发明申请

US20090005344A1 Compounds and Methods of Use Thereof 审中-公开
标题翻译：化合物及其使用方法
公开(公告)号：US20090005344A1
公开(公告)日：2009-01-01
申请号：US11718277
申请日：2005-10-27
申请人： James F. Burns , Leonardo A. Cabana , Glenn C. Collupy , John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
发明人： James F. Burns , Leonardo A. Cabana , Glenn C. Collupy , John R. Didsbury , Tatyana A. Dyakonov , Simon N. Haydar , Michael L. Jones , Francine F. Li , Christopher J. Markworth , Jessymol Mathew , Frank J. Schoenen , David S. Van Vliet , David Middlemiss
IPC分类号： A61K31/4184 , A61K31/381 , A61P43/00 , A61P29/00 , A61P19/02 , A61P17/06 , A61P19/08 , A61P11/06
CPC分类号： C07F5/025 , C07D235/18 , C07D417/04
摘要： Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof.
摘要翻译：描述了咪唑和苯并咪唑硼酸化合物，其类似物和药物制剂，以及其用于抑制有需要的受试者中的炎性细胞因子如肿瘤坏死因子α（TNF-α）的方法。

3. 发明授权

US06481442B1 Smoking article including a filter for selectively removing carbonyls 失效
标题翻译：吸烟制品包括用于选择性除去羰基的过滤器
公开(公告)号：US06481442B1
公开(公告)日：2002-11-19
申请号：US09723842
申请日：2000-11-28
申请人： Alexander J. Dyakonov , David A. Grider , Tatyana A. Dyakonov
发明人： Alexander J. Dyakonov , David A. Grider , Tatyana A. Dyakonov
IPC分类号： A24D104
CPC分类号： A24D3/166 , A24D3/08 , A24D3/14 , A24D3/163
摘要： A smoking article including a wrapper surrounding a tobacco column and a selective filter element is disclosed. The selective filter element includes at least one carrier having a developed structure and a plurality of moieties capable of the nucleophilic attack of carbonyl-containing combustion products of the smoking article supported by the at least one carrier. The selective filter element may include at least one additional filter element such as cellulose acetate. The developed structure of the at least one carrier encourages the interaction of the carbonyl-containing combustion products and the plurality of moieties capable of the nucleophilic attack. Carries include polymers, which may have branch, such as partially oxidized cellulose and polyaniline. Carries may also be a zeolite or an inorganic oxide such as aluminum, of silicon, of aluminum and silicon, and combinations thereof. In yet another carrier is an activated carbon. A moiety capable of the nucleophillic attack includes a nitrogen and hydrogen containing group such as a hydrazide—(e.g., —NH—NH2), a hydrazone—(e.g., —HC═N—NH2), a semicarbazide—(e.g., —C(═O)—NH2), an imino—(e.g., —HC═NH), and an amino—(—NH2). Preferably, the nitrogen is a primary nitrogen such as a primary amino. A spacer may be used to attach the moiety to a carrier. Examples of spacers include at least one of a —CO— group, —CO—[CH2]n—CO— group with n=1 through 4 and more.
摘要翻译：公开了一种包括围绕烟草柱和选择性过滤元件的包装物的吸烟制品。选择性过滤元件包括具有显影结构的至少一个载体和能够由至少一个载体支撑的吸烟制品的含羰基燃烧产物的亲核攻击的多个部分。选择性过滤元件可以包括至少一种额外的过滤元件，例如醋酸纤维素。所述至少一种载体的显影结构促进了含羰基燃烧产物和能够进行亲核攻击的多个部分的相互作用。载体包括可以具有分支的聚合物，例如部分氧化的纤维素和聚苯胺。携带物也可以是沸石或无机氧化物如铝，硅，铝和硅及其组合。在另一载体中是活性炭。能够进行嗜盐性攻击的部分包括含氮和氢的基团，例如酰肼 - （例如-NH-NH 2），腙 - （例如-HC = N-NH 2），氨基脲 - （例如-C （= O）-NH 2），亚氨基 - （例如-HC = NH）和氨基 - （ - NH 2）。优选地，氮是初级氮，例如伯氨基。可以使用间隔物将部分连接到载体上。间隔基的实例包括具有n = 1至4以上的-CO-基团，-CO- [CH 2] n -CO-基团中的至少一个。

4. 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。

5. 发明授权

US06713454B1 Prodrugs of etoposide and etoposide analogs 失效
标题翻译：依托泊苷和依托泊苷类似物的前药
公开(公告)号：US06713454B1
公开(公告)日：2004-03-30
申请号：US09474915
申请日：1999-12-31
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： A61K31704
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。

6. 发明授权

US06525098B1 6-methoxy-2-naphthylacetic acid prodrugs 失效
标题翻译： 6-甲氧基-2-萘基乙酸前药
公开(公告)号：US06525098B1
公开(公告)日：2003-02-25
申请号：US09697795
申请日：2000-10-27
申请人： Nnochiri Nkem Ekwuribe , Tatyana A. Dyakonov
发明人： Nnochiri Nkem Ekwuribe , Tatyana A. Dyakonov
IPC分类号： A61K3119
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。药物组合物包含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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