公开(公告)号：US20040266747A1

公开(公告)日：2004-12-30

申请号：US10494441

申请日：2004-05-04

发明人： Hans R. Pfaendler ,  Alexander Klingl

IPC分类号： C07F015/00 ,  A61K031/513 ,  A61K031/555

CPC分类号： C07D239/553 ,  A61K47/54 ,  A61K47/555 ,  C07F15/0093

摘要： Novel tumour selective anti-neoplastic agents are characterized, in that to customary antineoplastic agents are attached one or two very specific unbranched null-hydroxyalkyl, (null-hydroxy)alkenyl, null-(2,3-dihydroxypropyloxy)alkyl or an (null-(2,3-dihydroxypropyloxy))alkenyl groups R2 and R3 with 5 to 30 carbon atoms, forming a tumour selective conjugate as exemplified with the compounds of formulae I, II and III nullnull wherein R1 is a customary pharmaceutically acceptable inorganic or organic leaving group and A is 1,2-dimethylene, 1,3-trim ethylene, 1,2-cyclopentylene or 1,2-cyclohexylene. These compounds as well as their pharmaceutically acceptable salts, ester and prodrug derivatives are valuable chemotherapeutics 1

摘要翻译： 其特征在于新型肿瘤选择性抗肿瘤剂的特征在于，对于常规的抗肿瘤药物，其连接有一个或两个非特异性非支链的ω-羟基烷基（ω-羟基）烯基，ω-（2,3-二羟基丙氧基）烷基或（ω- （2,3-二羟基丙氧基））烯基R 2和R 3具有5至30个碳原子，形成肿瘤选择性缀合物，如式I，II和III []化合物所例举，其中R 1， 是常规的药学上可接受的无机或有机离去基团，A是1,2-二亚甲基，1,3-修饰的乙烯，1,2-亚环戊基或1,2-亚环己基。 这些化合物及其药学上可接受的盐，酯和前药衍生物是有价值的化学治疗剂

公开(公告)号：US20040208875A1

公开(公告)日：2004-10-21

申请号：US10777926

申请日：2004-02-11

申请人： Queen's University at Kingston

发明人： Robert Kisilevsky ,  Walter Szarek ,  Donald Weaver

IPC分类号： A61K039/395 ,  A61K038/16

CPC分类号： C07H15/04 ,  A61K31/095 ,  A61K31/185 ,  A61K31/255 ,  A61K31/34 ,  A61K31/41 ,  A61K31/70 ,  A61K47/51 ,  A61K47/549 ,  A61K47/55 ,  A61K47/555 ,  A61K47/58 ,  C07C305/10 ,  C07C309/05 ,  C07D491/04 ,  C07H11/00

摘要： Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.

摘要翻译： 描述了用于抑制受试者中淀粉样蛋白沉积的治疗化合物和方法，无论其临床情况如何。 通过给予受试者有效量的包含阴离子基团和载体分子或其药学上可接受的盐的治疗化合物或其淀粉样蛋白形成蛋白质与基底膜成分之间的相互作用被抑制来抑制淀粉样蛋白沉积。 优选的阴离子基团是磺酸盐和硫酸盐。 优选的载体分子包括碳水化合物，聚合物，肽，肽衍生物，脂族基团，脂环族基团，杂环基团，芳族基团及其组合。

公开(公告)号：US20040204434A1

公开(公告)日：2004-10-14

申请号：US10800898

申请日：2004-03-15

申请人： Controlled Chemicals Inc.

发明人： Jules A. Shafer ,  Vladislav V. Telyatnikov ,  Zhiwei Guo

IPC分类号： A61K031/485

CPC分类号： C07D489/08 ,  A61K47/555 ,  A61K47/60

摘要： The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.

摘要翻译： 降低生物可利用药物如鸦片止痛剂的滥用潜力，并且通过在制剂前将其转化为不良吸收的酯前药或其它前药衍生物来延长其作用时间。 与活性药物的许多现有持续释放制剂不同，其中通过咀嚼，破碎或以其它方式破坏含有活性药剂的片剂或胶囊珠可以释放活性药剂，这种包含本发明前药的片剂或胶囊珠粒的机械加工 既不释放活性药物也不妥协药物对药物的受控转化。 此外，含有本发明前药或其他药物的片剂和胶囊珠可以用足量的增稠剂如羟丙基甲基纤维素或羧甲基纤维素配制，以阻止对这些给药模式未注明的制剂的不适当的静脉内和鼻内施用。

公开(公告)号：US20040198820A1

公开(公告)日：2004-10-07

申请号：US10829896

申请日：2004-04-21

发明人： Kenneth C. Cundy ,  Mark A. Gallop

IPC分类号： A61K031/19 ,  A61K031/13

CPC分类号： C07C201/12 ,  A61K31/19 ,  A61K31/197 ,  A61K31/22 ,  A61K31/27 ,  A61K31/341 ,  A61K47/54 ,  A61K47/555 ,  C07C271/22 ,  C07C323/58 ,  C07C2601/14 ,  C07D213/79 ,  C07D213/80 ,  C07D267/06 ,  C07D307/33 ,  C07D307/58 ,  C07D307/60 ,  C07D317/32 ,  C07D317/40 ,  C07C205/43

摘要： The present invention provides an extended release oral dosage form of prodrugs of gabapentin and other GABA analogs, which dosage forms exhibit reduced toxicity. The dosage forms are particularly useful in administering those prodrugs of gabapentin and other GABA analogs that are metabolized to form an aldehyde. The dosage forms of the invention are useful for treating or preventing diseases and/or disorders for which the parent gabapentin or other GABA analog are known to be therapeutically effective.

摘要翻译： 本发明提供加巴喷丁和其他GABA类似物的前药的延长释放口服剂型，其剂型显示降低的毒性。 剂型特别可用于给予加巴喷丁和其它代谢形成醛的GABA类似物的前药。 本发明的剂型可用于治疗或预防已知母本加巴喷丁或其他GABA类似物在治疗上有效的疾病和/或病症。

公开(公告)号：US20040192578A1

公开(公告)日：2004-09-30

申请号：US10766575

申请日：2004-01-27

发明人： Evan Harris Walker ,  Eduardo Palomino ,  Steven L. Blumenthal

IPC分类号： A61K031/00

CPC分类号： C07D409/04 ,  A61K31/382 ,  A61K31/385 ,  A61K47/54 ,  A61K47/545 ,  A61K47/555 ,  C07D335/16 ,  C07D409/12

摘要： A process for producing new anticancer drugs such that the drugs can be administered in a nontoxic, proto-drug form and, subsequent to a time delay which allows for differential concentration in the targer cancer or invasive tissues or cells, the non-toxic drug is then modified by an activation drug to selectively provide toxic levels of a pharmacologically active agent to the target issue.

摘要翻译： 一种生产新的抗癌药物的方法，使得药物可以以无毒的原始药物形式施用，并且在允许在较大癌症或侵入性组织或细胞中不同浓度的时间延迟之后，无毒药物是 然后通过活化药物修饰以选择性地向目标问题提供毒性水平的药理学活性剂。

公开(公告)号：US20040162351A1

公开(公告)日：2004-08-19

申请号：US10734631

申请日：2003-12-11

发明人： Mark A. Gallop

IPC分类号： A61K031/195

CPC分类号： A61K47/555 ,  A61K47/54

摘要： The present invention provides an extended release oral dosage form of prodrugs of fused GABA analogs of reduced toxicity. The dosage forms are particularly useful in administering those fused GABA analogs that are metabolized to form an aldehyde. The dosage forms of the invention are useful for treating or preventing diseases and/or disorders for which fused GABA analog are known to be therapeutically effective.

摘要翻译： 本发明提供了具有降低毒性的融合GABA类似物的前药的延长释放口服剂型。 剂型特别可用于施用代谢形成醛的融合GABA类似物。 本发明的剂型可用于治疗或预防已知融合的GABA类似物具有治疗有效性的疾病和/或病症。

公开(公告)号：US20040087664A1

公开(公告)日：2004-05-06

申请号：US10639972

申请日：2003-08-13

发明人： Dennis Michael Marcus ,  Chung Kwang Chu

IPC分类号： A61K031/12 ,  A61K031/015

CPC分类号： A61K31/56 ,  A61K9/0019 ,  A61K31/015 ,  A61K31/07 ,  A61K31/12 ,  A61K31/35 ,  A61K31/40 ,  A61K31/405 ,  A61K31/44 ,  A61K31/497 ,  A61K47/54 ,  A61K47/551 ,  A61K47/555 ,  Y10S514/914

摘要： The present invention describes linking a therapeutic agent to a compound which is known to be naturally concentrated in a tissue affected by, or that is causing, a disease, to create a prodrug for treatment of the disease. Embodiments of the present invention include a new class of carotenoid-linked drugs to treat such blinding retinal disease such as age-related macular degeneration, retinoblastoma, and diabetic macular edema. For example, the present invention comprises a method for the treatment of a disorder of the eye comprising linking a therapeutic agent to a xanthophyll carotenoid to create a prodrug, and administering a therapeutically effective amount of the prodrug to an individual in need of treatment. Provided are prodrugs for treatment of retinoblastoma, cystoid macular edema (CME), exudative age-related macular degeneration (AMD), diabetic retinopathy, diabetic macular edema, or inflammatory disorders.

摘要翻译： 本发明描述了将治疗剂与已知天然浓缩在受疾病或正在引起疾病的组织中的化合物连接以产生用于治疗疾病的前体药物。 本发明的实施方案包括一类新的类胡萝卜素相关药物来治疗这种致盲性视网膜疾病如年龄相关性黄斑变性，视网膜母细胞瘤和糖尿病性黄斑水肿。 例如，本发明包括用于治疗眼病的方法，包括将治疗剂与叶黄素类胡萝卜素连接以产生前药，以及将治疗有效量的前药施用于需要治疗的个体。 提供用于治疗视网膜母细胞瘤，囊性黄斑水肿（CME），渗出性年龄相关性黄斑变性（AMD），糖尿病性视网膜病变，糖尿病性黄斑水肿或炎症性疾病的前药。

公开(公告)号：US06656966B2

公开(公告)日：2003-12-02

申请号：US09886494

申请日：2001-06-22

申请人： David S. Garvey ,  L. Gordon Letts ,  Chia-En Lin ,  Stewart K. Richardson ,  Tiansheng Wang

发明人： David S. Garvey ,  L. Gordon Letts ,  Chia-En Lin ,  Stewart K. Richardson ,  Tiansheng Wang

IPC分类号： A61K31337

CPC分类号： C07D409/12 ,  A61K31/335 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/555 ,  B82Y5/00 ,  C07D305/14 ,  Y10S977/775 ,  Y10S977/907 ,  Y10S977/915 ,  Y10S977/926 ,  A61K2300/00

摘要： The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The present invention also provides novel compositions comprising at least one taxane and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The compounds and compositions of the present invention can also be bound to a matrix. The present invention also provides methods for treating or preventing cardiovascular diseases and disorders, autoimmune diseases, pathological conditions resulting from abnormal cell proliferation, polycystic kidney disease, inflammatory disease, preserving organs and/or tissues or to inhibit wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis, by administering nitrosated and/or nitrosylated taxane or parent taxanes in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.

公开(公告)号：US06624317B1

公开(公告)日：2003-09-23

申请号：US09669156

申请日：2000-09-25

申请人： Kuo-Hsiung Lee ,  Qian Shi ,  Kenneth F. Bastow ,  Hui-Kang Wang

发明人： Kuo-Hsiung Lee ,  Qian Shi ,  Kenneth F. Bastow ,  Hui-Kang Wang

IPC分类号： C07D30500

CPC分类号： C07D405/12 ,  A61K47/55 ,  A61K47/552 ,  A61K47/555 ,  C07D305/14 ,  C07D471/04 ,  C07D493/04 ,  C07H15/26 ,  C07H17/02

摘要： Compounds according to formula I: T1—L—T2   (I), wherein T1 is a taxoid group, preferably of Formula II: wherein R1 is C6H5; R2 is O; L is a linking group; and T2 is a substituent selected from the group consisting of epipodophyllotoxin, amsacrine, ellipticine, anthracycline antibiotic, mitoxantrone, and colchicine groups, and pharmaceutically acceptable salts thereof, are provided herein. The compounds are useful in, among other things, treating tumors or cancer in subjects in need thereof, inducing cellular differentiation, and inhibiting cellular mitosis.

摘要翻译： 根据式I的化合物：其中T1是紫杉烷基，优选式II：其中R1是C6H5; R2是O; L是连接基团; 并且T2是选自表鬼臼毒素，amsacrine，玫瑰树碱，蒽环类抗生素，米托蒽醌和秋水仙素基团的取代基及其药学上可接受的盐。 除其他外，该化合物可用于治疗有需要的受试者的肿瘤或癌症，诱导细胞分化和抑制细胞有丝分裂。

公开(公告)号：US20030109697A1

公开(公告)日：2003-06-12

申请号：US10119927

申请日：2002-04-09

发明人： H. Michael Shepard ,  Andrew Rein Vaino ,  Danielle M. Lehsten

IPC分类号： C07H019/048 ,  C07H019/10 ,  A61K031/7072

CPC分类号： B82Y5/00 ,  A61K47/54 ,  A61K47/555 ,  A61K47/556 ,  A61K47/67 ,  C07F9/6512 ,  C07H19/06 ,  C07H19/10 ,  C07H19/20

摘要： This invention provides compounds, compositions and methods for treating cancer, infectious disease, an autoimmune disorder or an inflammatory condition. Therapeutic compounds useful in the methods of this invention are 5null-phosphoramidatyl, 1,5-substituted pyrimidine compounds, derivatives, analogs and pharmaceutically acceptable salts thereof

摘要翻译： 本发明提供了治疗癌症，感染性疾病，自身免疫性疾病或炎性病症的化合物，组合物和方法。 可用于本发明方法的治疗化合物是5'-氨基磷酰基，1,5-取代的嘧啶化合物，其衍生物，类似物和药学上可接受的盐