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1. 发明专利

AU2002319535B2 The treatment of lipodystrophy 未知
公开(公告)号：AU2002319535B2
公开(公告)日：2005-01-06
申请号：AU2002319535
申请日：2002-08-07
申请人： ARK THERAPEUTICS LTD
发明人： MARTIN JOHN FRANCIS , ERUSALIMSKY JORGE D , MONTGOMERY HUGH EDWARD
IPC分类号： A61K45/00 , A61K31/00 , A61K31/55 , A61K31/551 , A61K31/675 , A61K38/55 , A61P3/00 , A61P3/06 , A61P3/10 , A61K031/00 , A61K031/223 , A61K031/519 , A61K031/422 , A61P003/00 , A61K031/401 , A61K031/403 , A61K031/472 , A61K031/675 , A61K031/417 , A61K031/4178 , A61K031/4184 , A61K031/55 , A61K031/551 , A61K031/554
摘要： An inhibitor of the renin-angiotensin system is useful for the treatment or prevention of the lipodystrophy syndrome, e.g. in AIDS patients also receiving anti-retroviral therapy.

2. 发明申请

US20020193416A1 Synergistic tumorcidal response induced by histamine 审中-公开
标题翻译：组胺引起的协同杀肿瘤反应
公开(公告)号：US20020193416A1
公开(公告)日：2002-12-19
申请号：US10217254
申请日：2002-08-09
发明人： Kurt R. Gehlsen , Kristoffer Hellstrand , Svante Hermodsson
IPC分类号： A61K039/395 , A61K031/417
CPC分类号： A61K41/0038 , A61K31/417 , A61K39/395 , A61K31/415 , A61K2300/00
摘要： The present invention relates to methods of treating cancer in which histamine is administered in conjunction with other cancer therapies. The cancer therapy includes surgery, radiation, immunotherapy, the administration of an agent which enhances the humoral immune response of the patient or any combination thereof.
摘要翻译：本发明涉及治疗癌症的方法，其中组胺与其它癌症疗法结合使用。癌症治疗包括手术，放射线，免疫治疗，给予增强患者体液免疫应答的药物或其任何组合。

3. 发明申请

US20020143044A1 Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands 失效
标题翻译：某些4-氨基甲基-2-取代的咪唑衍生物和2-氨基甲基-4-取代的咪唑衍生物; 新类型的多巴胺受体亚型特异性配体
公开(公告)号：US20020143044A1
公开(公告)日：2002-10-03
申请号：US10100691
申请日：2002-03-18
申请人： Neurogen Corporation
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： A61K031/4178 , A61K031/417 , C07D403/02 , C07D233/64 , C07D233/22
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula: 1 wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

4. 发明申请

US20020182175A1 Methods and compositions for promoting the maturation of monocytes 有权
公开(公告)号：US20020182175A1
公开(公告)日：2002-12-05
申请号：US10160368
申请日：2002-05-30
发明人： Kristoffer Hellstrand , Svante H. Hermodsson , Kurt R. Gehlsen
IPC分类号： A61K038/19 , A61K038/20 , A61K038/21 , A61K031/417
CPC分类号： A61K39/39 , A61K38/191 , A61K38/193 , A61K38/20 , A61K38/44 , A61K2039/55511 , A61K2039/55522 , C12N5/0645 , C12N2501/22 , C12N2501/82 , Y02A50/41 , Y02A50/412 , Y02A50/423 , Y02A50/467 , A61K2300/00
摘要： Disclosed is a method of promoting the maturation of monocytes comprising the administration of a reactive oxygen species (ROS) inhibitor or scavenger and at least one monocyte maturation-promoting agent. A composition for promoting the maturation of monocytes is likewise disclosed. The pharmaceutical composition includes a compound effective to promote the maturation of monocytes and a ROS inhibitor or scavenger combined in a pharmaceutically acceptable carrier.

5. 发明申请

US20020103156A1 Gene delivery compositions and methods 失效
公开(公告)号：US20020103156A1
公开(公告)日：2002-08-01
申请号：US10092184
申请日：2002-03-05
申请人： Johns Hopkins University of Baltimore, Maryland
发明人： John H. Lawrence III , J. Kevin Donahue
IPC分类号： A61K048/00 , A61K038/17 , A61K038/18 , A61K038/20 , A61K031/405 , A61K031/417 , A61K031/5575 , A61K031/198
CPC分类号： A61K48/0083 , A61K48/00 , C12N15/88
摘要： The present provides methods and compositions that enable effective delivery of nucleic acids to desired cells, including to a solid organ such as a mammalian heart. The methods and compositions enable effective gene transfer and subsequent expression to a majority of cells throughout a solid organ such as the heart. Methods and compositions of the invention preferably provide enhanced vascular permeability that enables increased gene transfer to targeted cells, but without significant degradation or injury to endothelial cell layers. Global delivery of nucleic acid to an intact heart has been achieved with as little as 2 minutes of intracoronary exposure to the administered nucleic acid.

6. 发明申请

US20020098224A1 Ophthalmic histamine compositions and uses thereof 失效
标题翻译：眼组织胺组合物及其用途
公开(公告)号：US20020098224A1
公开(公告)日：2002-07-25
申请号：US10000462
申请日：2001-11-30
发明人： Kurt R. Gehlsen
IPC分类号： A61K031/407 , A61K031/417
CPC分类号： A61K9/0048 , A61K31/4045 , A61K31/417
摘要： An ophthalmic composition for use in reducing ocular irritation comprising histamine, at a concentration of between about 0.01 and 1.0% by weight, in a pharmaceutically acceptable carrier, adapted for ophthalmic administration.
摘要翻译：一种用于减少眼睛刺激的眼用组合物，其包含浓度为约0.01至1.0重量％的组胺，其在药学上可接受的载体中适用于眼部给药。

7. 发明申请

US20020091146A1 Compositions and methods for treating glomerular disorders 审中-公开
标题翻译：治疗肾小球疾病的组合物和方法
公开(公告)号：US20020091146A1
公开(公告)日：2002-07-11
申请号：US10059763
申请日：2002-01-29
发明人： Sudhir V. Shah , Radhakrishna Ballga
IPC分类号： A61K031/426 , A61K031/417 , A61K031/343 , A61K031/27
CPC分类号： A61K31/4525 , A61K31/325 , A61K31/4164 , A61K31/426
摘要： Compositions and methods comprising an agent that reduces proteinuria in an individual are disclosed. Compositions and methods comprise an agent that reduces availability of a catalytic iron source in glomeruli. Agents of the invention include inhibitors of members of the cytochrome P450 (CYP) superfamily. In a particularly preferred embodiment, compositions and methods comprise an agent that inhibits ability of a CYP superfamily member to serve as a glomerular catalytic iron source, thereby reducing proteinuria in an individual afflicted with a glomerular disease.
摘要翻译：公开了包含降低个体中的蛋白尿的药剂的组合物和方法。组合物和方法包括降低肾小球中催化铁源的可利用性的试剂。本发明的药剂包括细胞色素P450（CYP）超家族成员的抑制剂。在一个特别优选的实施方案中，组合物和方法包括抑制CYP超家族成员作为肾小球催化铁源的能力的试剂，由此减轻患有肾小球疾病的个体中的蛋白尿。

8. 发明申请

US20030105095A1 4'-Methanesulfonyl-biphenyl derivatives as a highly selective cyclooxygenase-2 inhibitor 有权
标题翻译： 4'-甲磺酰基 - 联苯衍生物作为高选择性环加氧酶-2抑制剂
公开(公告)号：US20030105095A1
公开(公告)日：2003-06-05
申请号：US10264113
申请日：2002-10-03
申请人： CHEIL JEDANG Corporation
发明人： Il Hwan Cho , Jee Woong Lim , Ji Young Noh , Jong Hoon Kim , Sang Wook Park , Hyung Chul Ryu , Je Hak Kim , Hyung Ok Chun , So Young Wang , Eun Young Lee
IPC分类号： A61K031/54 , A61K031/537 , A61K031/496 , A61K031/426 , A61K031/421 , A61K031/417 , A61K031/10
CPC分类号： C07C317/22 , C07C2601/02 , C07C2601/08
摘要： The present invention relates to a novel 4null-methanesulfonyl-biphenyl derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor. 1 Wherein, R1 and R2 are defined in this specification respectively.
摘要翻译：本发明涉及具有式1结构的新型4'-甲磺酰基 - 联苯衍生物及其药学上可接受的盐作为高选择性环加氧酶-2抑制剂。其中R1和R2分别在本说明书中定义。

9. 发明申请

US20030036557A1 Heterocyclo-substituted imidazoles for the treatment of inflammation 失效
标题翻译：杂环取代的咪唑用于治疗炎症
公开(公告)号：US20030036557A1
公开(公告)日：2003-02-20
申请号：US10004944
申请日：2001-12-05
申请人： G.D. Searle & Co.
发明人： Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
IPC分类号： A61K031/655 , A61K031/4178 , A61K031/417 , C07D43/02 , C07D233/54
CPC分类号： C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by Formula V: 1 wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类咪唑基化合物用于治疗炎症。特别感兴趣的化合物由式V定义：其中R3是选自氢，烷基，卤代烷基，芳烷基，杂环烷基，杂芳烷基，酰基，氰基，烷氧基，烷硫基，烷硫基烷基，烷基磺酰基，环烷硫基，环烷硫基烷基，环烷基磺酰基，环烷基磺酰基烷基，卤代烷基磺酰基，芳基磺酰基，卤素，羟基烷基，烷氧基烷基，烷基羰基，芳基羰基，芳烷基羰基，杂环羰基，氰基烷基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-烷基-N-芳基氨基烷基，羧基烷基，烷氧基羰基烷基，烷氧基羰基，卤代烷基羰基，羧基，氨基羰基，烷基氨基羰基，烷基氨基羰基烷基杂芳基烷氧基，杂芳基硫基，杂芳烷氧基，杂芳烷硫基，杂芳基烷硫基烷基，杂芳氧基，杂芳硫基，芳硫基烷基，芳氧基烷基，芳硫基，芳氧基，芳烷硫基烷基，芳烷氧基烷基，芳基和杂芳基; 其中R4是选自氢，烷基和卤素的基团; 并且其中R 13和R 14独立地选自芳基和杂环，其中R 13和R 14在可取代的位置任选被一个或多个独立地选自烷基磺酰基，氨基磺酰基，卤素，烷硫基，烷基，氰基，羧基，烷氧基羰基，卤代烷基，羟基，烷氧基，羟基烷基，烷氧基烷基，卤代烷氧基，氨基，烷基氨基，芳基氨基和硝基; 提供R13和R14中的至少一个是被烷基磺酰基或氨基磺酰基取代的芳基; 或其药学上可接受的盐。

10. 发明申请

US20020137785A1 Inflammatory mechanism modulator composition and methods with anti-asthmatic properties 审中-公开
标题翻译：炎症机制调节剂组成及方法具有抗哮喘特性
公开(公告)号：US20020137785A1
公开(公告)日：2002-09-26
申请号：US10106625
申请日：2002-03-26
发明人： George Kindness , Brooke Schumm III , F. Timothy Guilford
IPC分类号： A61K031/496 , A61K031/47 , A61K031/433 , A61K031/417 , A61K031/341 , A61K031/198
CPC分类号： A61K31/433 , A61K31/198 , A61K31/341 , A61K31/417 , A61K31/47 , A61K31/496 , A61K2300/00
摘要： The invention proposes the use of a leukotriene antagonist, particularly a montelukast sodium compound such as SINGULAIR, in combination with cystine to combat inflammatory disease and hopefully reduce the necessary use of SINGULAIR. Combination with other anti-inflammatory agents and anti-asthmatic agents is proposed. Selenium to assure glutathione pathway benefit is suggested. The addition of a selective COX-2 inhibitor is suggested.
摘要翻译：本发明提出使用白细胞三烯拮抗剂，特别是孟鲁司特钠化合物如SINGULAIR，与胱氨酸组合以抵抗炎性疾病，并希望减少SINGULAIR的必要用途。提出与其他抗炎剂和抗哮喘药物的组合。建议硒以确保谷胱甘肽途径的益处。建议添加选择性COX-2抑制剂。

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