公开(公告)号：US20030148967A1

公开(公告)日：2003-08-07

申请号：US10257855

申请日：2002-10-17

发明人： Christopher McGuigan ,  Jan Balzarini

IPC分类号： A61K031/7052 ,  A61K031/519 ,  A61K031/517 ,  C07D491/02 ,  C07D487/02 ,  C07D45/02 ,  C07H019/22

CPC分类号： C07H19/24 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/706 ,  C07D403/02 ,  C07D405/04 ,  C07D487/04 ,  C07D491/04 ,  C07D498/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/23

摘要： A compound having the formula (I) wherein Ar is an, optionally substituted, aromatic ring system, the aromatic ring system comprising one six-membered aromatic ring or two fused six-membered aromatic rings; R8 and R9 are each independently selected form the group comprising hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, aryl; Q is selected from the group comprising O, S and CY2, where Y may be the same or different and is selected from H, alkyl and halogens; X is selected from the group comprising O, NH, S, N-alkyl, (CH2)m where m is 1 to 10, and CY2 where Y may be the same or different and is selected from hydrogen, alkyl and halogens; Z is selected from the group comprising O, S, NH, and N-alkyl; Unull is H and Unull is selected from H and CH2T, or Unull and Unull are joined so as to form a ring moiety including Q wherein UnullnullUnull together is respectively selected from the group comprising nullCTHnullCTnullTnull- and nullCTnullCT- and nullCTnullnullCTnull-, so as to provide ring moieties selected from the group comprising (a), (b) wherein: T is selected from the group comprising OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2 and N3; Tnull is selected from the group comprising H and halogens and, where more than one Tnull is present, they may be the same or different; Tnull is selected from the group comprising H and halogens; and W is selected from the group comprising H, a phosphate group and a pharmacologically acceptable salt, derivative or pro-drug thereof; with the proviso that when T is OAc and Tnull and Tnull are present and are H, Ar is not 4-(2-benzoxazolyl)phenyl. C1 to C10 alkyl and alkoxy substituents on the aromatic ring system of Ar are preferred. Compounds show anti-viral activity, for example with respect to varicella zoster virus.

公开(公告)号：US20030148966A1

公开(公告)日：2003-08-07

申请号：US10347990

申请日：2003-01-20

发明人： Hiremagalur Jayaram ,  Georg Krupitza ,  Thomas Szekeres ,  Michael Grusch

IPC分类号： A61K031/7076 ,  A61K031/7052

CPC分类号： A61K31/7052 ,  A61K31/7076 ,  A61K2300/00

摘要： There is provided a composition including an ATP-inducing compound or ATP and an effective amount of cell death-inducing drug. Also provided is the method of inducing apoptosis in apoptosis-inducible cells by administering to the apoptosis inducible cells a composition including an effective amount of a cell death-inducing compound and an ATP-inducing compound or ATP. The present invention also provides a method of suppressing necrosis in cells by administering an effective amount of an ATP-inducing compound or ATP to a cell population, thereby inhibiting necrosis.

摘要翻译： 提供了包含ATP诱导化合物或ATP和有效量的细胞死亡诱导药物的组合物。 还提供了通过向凋亡诱导细胞施用包含有效量的细胞死亡诱导化合物和ATP诱导化合物或ATP的组合物来诱导凋亡诱导型细胞凋亡的方法。 本发明还提供了通过向细胞群施用有效量的ATP诱导化合物或ATP，从而抑制坏死来抑制细胞坏死的方法。

公开(公告)号：US20030119760A1

公开(公告)日：2003-06-26

申请号：US10286389

申请日：2002-11-01

发明人： Javed Hussain ,  Pankaj Khapra ,  Arun S. Gosavi

IPC分类号： A61K031/7052 ,  A61K031/7048 ,  A61K009/22

CPC分类号： A61K9/1652 ,  A61K9/2009 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/7048 ,  A61K31/7052

摘要： The present invention provides a controlled release pharmaceutical composition of an acid labile, poorly soluble drug having pH dependent solubility profile in aqueous environment. In a preferred embodiment the drug is combined with a practically water insoluble polymer an optimizing agent and optional additives to produce a controlled release of therapeutic agent when compositions is exposed to aqueous environment.

摘要翻译： 本发明提供了一种在水性环境中具有pH依赖性溶解度曲线的酸不稳定，难溶性药物的控释药物组合物。 在优选的实施方案中，药物与实际上不溶于水的聚合物结合，优选剂和任选的添加剂，以在组合物暴露于水性环境时产生治疗剂的受控释放。

公开(公告)号：US20030114390A1

公开(公告)日：2003-06-19

申请号：US10264410

申请日：2002-10-04

发明人： William N. Washburn ,  Bruce Ellsworth ,  Wei Meng ,  Gang Wu ,  Philip M. Sher

IPC分类号： A61K031/70 ,  A61K031/7052

CPC分类号： A61K45/06 ,  A61K31/70 ,  A61K31/7052 ,  A61K2300/00

摘要： A method is provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of a compound of the formula 1 alone or in combination with one or more other antidiabetic agent(s) or other therapeutic agent(s).

摘要翻译： 提供了一种用于治疗糖尿病和相关疾病的方法，其使用抑制SGLT2的量的单独的化合物或与一种或多种其它抗糖尿病剂或其它治疗剂组合。

公开(公告)号：US20030087842A1

公开(公告)日：2003-05-08

申请号：US10057260

申请日：2001-10-29

申请人： Advanced Life Sciences, Inc.

发明人： David E. Zembower ,  Yongping Xie ,  Yasheen Zhou

IPC分类号： A61K031/7052 ,  C07H019/22

CPC分类号： C07H19/04 ,  C07H19/044

摘要： The present invention relates to anti-tumor compounds, compositions and methods. In particular, the invention relates to indolocarbazole analogues of the following general formulas that inhibit topoisomerase I activity. 1

摘要翻译： 本发明涉及抗肿瘤化合物，组合物和方法。 特别地，本发明涉及抑制拓扑异构酶I活性的以下通式的吲哚咔唑类似物。

公开(公告)号：US20030021816A1

公开(公告)日：2003-01-30

申请号：US10167040

申请日：2002-06-06

发明人： Sewon Kang ,  John J. Voorhees ,  Gary J. Fisher

IPC分类号： A61K038/13 ,  A61K031/7052 ,  A61K031/7048 ,  A61K031/4745 ,  A61K031/366 ,  A61K031/353

CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/353 ,  A61K31/366 ,  A61K31/4745 ,  A61K31/7048 ,  A61K31/7052 ,  A61K38/13 ,  A61K2300/00

摘要： Acne-affected skin has been found to be accompanied by the presence of matrix-degrading enzymes such as MMPs and neutrophil elastase, induction of neutrophils, and a reduction in procollagen biosynthesis. This invention treats scarring and inflammation accompanying acne by administering, topically or systemically, at least one of (i) an inhibitor of the matrix degrading enzymes and (ii) a cytokine inhibitor that alleviates inflammation and thus also alleviate neutrophil infiltration. Alleviating the matrix degradation and renormalizing procollagen biosynthesis allows for reduced inflammation and better natural repair of acne-affected skin. Inhibiting cytokines alleviates induction of MMPs in resident skin cells, and also alleviates inflammation with its concommitant induction of neutrophils from the blood stream bringing MMPs and elastase into the acne lesion. Dimishing the presence of matrix-degrading enzymes in the acne lesion reduces imperfect repair of the skin and thus decreases scarring in acne-affected skin.

摘要翻译： 已经发现受痤疮影响的皮肤伴随着基质降解酶如MMP和嗜中性粒细胞弹性蛋白酶的存在，嗜中性粒细胞的诱导和前胶原生物合成的减少。 本发明通过局部或全身地施用（i）基质降解酶的抑制剂和（ii）减轻炎症并因此也减轻嗜中性粒细胞浸润的细胞因子抑制剂中的至少一种来治疗伴随痤疮的瘢痕形成和炎症。 减轻基质降解和重塑原胶原生物合成可以减少炎症和更好的天然修复受痤疮影响的皮肤。 抑制细胞因子减轻常驻皮肤细胞中MMPs的诱导，并且还可以缓解炎症，同时从血液中诱导嗜中性粒细胞，使MMP和弹性蛋白酶进入痤疮病变。 减少痤疮病变中基质降解酶的存在降低皮肤的不完美修复，从而减少痤疮影响的皮肤中的瘢痕形成。

公开(公告)号：US20020132784A1

公开(公告)日：2002-09-19

申请号：US10136745

申请日：2002-04-29

发明人： Robert Tam ,  Guangyi Wang ,  Devron Averett ,  Kandasamy Ramasamy

IPC分类号： A61K031/7052 ,  A61K031/4196

CPC分类号： A61K31/675

摘要： Nucleosides and other compounds to selectively modulate Th1 and Th2 responses relative to each other in the treatment of disease. In one aspect of the invention, administration of a nucleoside or other compound reduces the dosage at which a primary drug is administered. In another aspect of the invention, an abnormality reflected in increased response in one group of cytokines is treated by administering a nucleoside or other compound that increases response in another group of cytokines. In yet another aspect of the invention, a patient is prophylactically treated by administering a nucleoside or other compound that selectively reduces Th1 activity without significantly reducing Th2 activity. In yet another aspect of the invention, a nucleoside or other compound is administered to a patient at a dose that reduces the patient's GTP pool to a degree that selectively reduces one of the Th1 or Th2 responses without significantly reducing the other response. Controlled release dosage forms are particularly contemplated to achieve that result.

摘要翻译： 核苷和其他化合物，用于在疾病治疗中相对于彼此选择性调节Th1和Th2应答。 在本发明的一个方面，核苷或其他化合物的施用降低了施用初次药物的剂量。 在本发明的另一方面，通过施用增加另一组细胞因子中的反应的核苷或其它化合物来治疗反映在一组细胞因子中的增加的反应中的异常。 在本发明的另一方面，通过施用选择性降低Th1活性但不显着降低Th2活性的核苷或其它化合物来预防性地治疗患者。 在本发明的又一方面中，将核苷或其它化合物以一定剂量给予患者，剂量可将患者的GTP池降低到选择性降低Th1或Th2反应之一而不显着降低其他反应的程度。 特别考虑到控制释放剂型以实现该结果。

公开(公告)号：US20020019353A1

公开(公告)日：2002-02-14

申请号：US09829672

申请日：2001-04-10

发明人： Peter Connor Canning ,  Wayne Alan Boettner

IPC分类号： A61K031/7052

CPC分类号： C07H17/08 ,  A61K31/7052 ,  A61K45/06 ,  A61K2300/00

摘要： Methods for treating or preventing bacterial or protozoal infections in mammals by administering a single dose of an antibiotic composition comprising a mixture of azalide isomers and a pharmaceutically acceptable vehicle are disclosed. Methods for increasing acute or chronic injection-site toleration in mammals by administering a single dose of antibiotic compositions comprising a mixture of azalide isomers and a pharmaceutically acceptable vehicle are also disclosed. A combination comprising: an antibiotic composition comprising a mixture of azalide isomers, a pharmaceutically acceptable carrier, and instructions for use in a single-dose administration is also disclosed.

摘要翻译： 公开了通过施用单剂量的包含氮杂异构体混合物和药学上可接受的载体的抗生素组合来治疗或预防哺乳动物细菌或原生动物感染的方法。 还公开了通过施用包含氮杂异构体混合物和药学上可接受的载体的单剂量抗生素组合物来增加哺乳动物的急性或慢性注射部位耐受性的方法。 还公开了包含：包含氮杂异构体混合物的抗生素组合物，药学上可接受的载体和用于单剂量给药的说明书。

公开(公告)号：US20040209826A1

公开(公告)日：2004-10-21

申请号：US10840529

申请日：2004-05-06

发明人： Robert J. Rafka ,  Colman B. Ragan ,  Douglas J.M. Allen

IPC分类号： A61K031/7052 ,  C07H017/08

CPC分类号： C07H17/08 ,  C07H17/00

摘要： This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-nullnull2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-null(propylamino)methylnull-null-L-ribo-hexopryanosylnulloxynull-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-nullnull3,4,6-trideoxy-3-(dimethylamino)-null-D-xylo-hexopyranosylnulloxynull-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.

摘要翻译： 本发明涉及（2R，3S，4R，5R，8R，10R，11R，12S，13S，14R）-13 - [[2,6-二脱氧-3-C-甲基-3- O-甲基-4-C - [（丙基氨基）甲基]-α-L-核 - 六羟基甲硅烷基]氧基] -2-乙基-3,4,10-三羟基-3,5,8,10,12,14- 六甲基-11 - [[3,4,6-三脱氧-3-（二甲基氨基） - D-xylo-hexopyranosyl]氧基] -1-氧杂-6-氮杂环十五烷-15-可用作抗细菌和抗原生动物 哺乳动物代理。 本发明还涉及含有二磷酸盐的游离碱的药物组合物和通过向需要这种治疗的哺乳动物施用二磷酸的游离碱来治疗哺乳动物的细菌和原生动物感染的方法。 本发明的二磷酸盐的游离碱在通过胃肠外施用于哺乳动物时具有针对各种细菌和原生动物感染的有效活性。

公开(公告)号：US20040198675A1

公开(公告)日：2004-10-07

申请号：US10416802

申请日：2003-07-10

发明人： Masao Sugamata

IPC分类号： A61K031/7052

CPC分类号： C07H17/08 ,  A61K31/7048

摘要： A drug effective for prevention and therapy of endometriosis and hysteromyoma is disclosed. The drug for prevention and/or therapy of endometriosis and/or hysteromyoma according to the present invention comprises as an effective ingredient a macrolide antibiotic.

摘要翻译： 公开了一种有效预防和治疗子宫内膜异位症和子宫肌瘤的药物。 根据本发明的用于预防和/或治疗子宫内膜异位症和/或子宫肌瘤的药物包含大环内酯抗生素作为有效成分。