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1. 发明申请

US20030162761A1 Formulations comprising selective androgen receptor modulators 有权
标题翻译：包含选择性雄激素受体调节剂的制剂
公开(公告)号：US20030162761A1
公开(公告)日：2003-08-28
申请号：US10270232
申请日：2002-10-15
发明人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller
IPC分类号： A61K031/555 , A61K031/4706 , A61K031/404 , A61K031/325 , A61K031/27 , A61K031/277 , A61K031/165
CPC分类号： A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D215/227 , C07D271/12 , G01N30/7233 , G01N33/5438 , G01N33/74 , G01N2030/8813
摘要： The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.
摘要翻译：本发明涉及包含新型雄激素受体靶向剂（ARTA）的药物组合物和制剂，其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血，肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防慢性肌肉消瘦; 和/或e）降低前列腺癌的发生率，停止或导致消退。本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

2. 发明申请

US20020137792A1 Use of an LTB4 antagonist for the treatment or prevention of diseases caused by increased expression of mucin genes 有权
标题翻译：使用LTB4拮抗剂治疗或预防由粘蛋白基因表达增加引起的疾病
公开(公告)号：US20020137792A1
公开(公告)日：2002-09-26
申请号：US10050409
申请日：2002-01-16
发明人： Ralf Anderskewitz , Christopher J. Montague Meade , Franz Birke , Hans Michael Jennewein , Birgit Jung
IPC分类号： A61K031/27
CPC分类号： A61K45/06 , A61K31/155 , A61K31/27 , Y02A50/475 , Y10S514/851 , A61K2300/00
摘要： Medicaments and pharmaceutical kits comprising an LTB4 antagonist of formula (I) 1 a tautomer thereof or a pharmaceutically acceptable salt thereof, and methods of treating or preventing cystic fibrosis, diseases caused by increased expression of mucin genes in the bronchial or gastrointestinal epithelium, or hyperplasia of goblet cells induced by toxins of products of pathogenic bacteria in a patient in need of such treatment, the method comprising administering to the patient a therapeutically effective amount of an LTB4 antagonist of formula (I).
摘要翻译：包含式（I）的LTB4拮抗剂及其互变异构体或其药学上可接受的盐的药物和药物试剂盒，以及治疗或预防囊性纤维化的方法，由支气管或胃肠上皮中粘蛋白基因表达增加引起的疾病或增生在需要这种治疗的患者中由致病细菌产物的毒素诱导的杯状细胞，所述方法包括向患者施用治疗有效量的式（I）的LTB4拮抗剂。

3. 发明申请

US20020107283A1 Carbamate compounds for use in preventing or treating neuropathic pain and cluster and migraine headache-associated pain 审中-公开
标题翻译：用于预防或治疗神经性疼痛和集束型和偏头痛头痛相关疼痛的氨基甲酸酯化合物
公开(公告)号：US20020107283A1
公开(公告)日：2002-08-08
申请号：US09906251
申请日：2001-07-16
发明人： Ellen E. Codd , Richard P. Shank , Katherine E. Rogers , Carlos R. Plata-Salaman , Boyu Zhao
IPC分类号： A61K031/27
CPC分类号： A61K31/27
摘要： This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain comprising administering to a subject in need thereof a therapeutically effective amount of an enantiomer of Formula (I) substantially free of other enantiomers or an enantiomeric mixture wherein an enantiomer of Formula (I) predominates: 1 wherein phenyl is substituted at X with one to five halogen atoms independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).
摘要翻译：本发明涉及一种用于预防或治疗神经性疼痛和集束型和偏头痛性头痛相关疼痛的方法，包括向有需要的受试者施用治疗有效量的基本上不含其它对映异构体或对映体混合物的式（I）对映异构体其中式（I）的对映异构体占主导地位：其中苯基在X上被一至五个独立地选自氟，氯，溴和碘的卤素原子取代; 和; R 1和R 2独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基的取代基取代）。

4. 发明申请

US20020065247A1 Chemical compounds having ion channel blocking activity for the treatment of immune dysfunction 失效
标题翻译：具有离子通道阻断活性的化合物用于治疗免疫功能障碍
公开(公告)号：US20020065247A1
公开(公告)日：2002-05-30
申请号：US09986725
申请日：2001-11-09
发明人： Bo Skaaning Jensen , Soren Peter Olsen , Palle Christophersen
IPC分类号： A61K031/695 , A61K031/66 , A61K031/27 , A61K031/28
CPC分类号： A61K45/06 , A61K31/00 , A61K31/045 , A61K31/12 , A61K31/4453 , Y02A50/409
摘要： The present invention relates to chemical compounds having inhibitory activity on an intermediate conductance Ca2null activated potassium channel (IKCa), and the use of such compounds for the treatment or alleviation of diseases or conditions relating to immune dysfunction.
摘要翻译：本发明涉及对中等电导Ca 2+活化钾通道（IKCa）具有抑制活性的化合物，以及这些化合物用于治疗或减轻与免疫功能障碍有关的疾病或病症的用途。

5. 发明申请

US20030203025A1 Sustained release oral formulations 审中-公开
公开(公告)号：US20030203025A1
公开(公告)日：2003-10-30
申请号：US10403146
申请日：2003-03-31
发明人： Jorg Ogorka , Oskar Kalb , Rajen Shah , Satish Chandra Khanna
IPC分类号： A61K031/325 , A61K031/717 , A61K009/22 , A61K031/27
CPC分类号： A61K9/5084 , A61K9/2077 , A61K9/2866 , A61K9/2886 , A61K9/5078 , A61K31/27
摘要： Pharmaceutical composition capable of releasing a therapeutically effective dose of active agent, e.g., rivastigamine, in a time-controlled manner.

6. 发明申请

US20030166715A1 Use of vitaletheine modulators in the prophylaxis and treatment of disease 审中-公开
标题翻译：使用依托沙星调节剂预防和治疗疾病
公开(公告)号：US20030166715A1
公开(公告)日：2003-09-04
申请号：US10006798
申请日：2001-12-04
发明人： Galen D. Knight , Terence J. Scallen
IPC分类号： A61K031/27 , A61K031/17 , A61K031/155
CPC分类号： C07C323/41 , C12N1/36
摘要： Sulfur-containing derivatives of carboxy-amino-amides are provided for use, inter alia, in treating diseases or disorders.
摘要翻译：提供了羧基 - 氨基 - 酰胺的含硫衍生物，尤其用于治疗疾病或病症。

7. 发明申请

US20030069305A1 Pharmaceutical uses and synthesis of benzobicyclooctanes 失效
标题翻译：苯并双环辛烷的药用和合成
公开(公告)号：US20030069305A1
公开(公告)日：2003-04-10
申请号：US10015828
申请日：2001-12-11
申请人： Celltech R & D, Inc.
发明人： Randy W. Jackson , Ihab Darwish , Ted A. Baughman , J. Jeffry Howbert
IPC分类号： A61K031/27 , A61K031/216 , A61K031/17 , A61K031/165
CPC分类号： C07F7/081
摘要： Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-null and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
摘要翻译：苯并双环辛烷化合物，其用于抑制涉及TNF-α和IL-8的细胞事件，以及一般治疗炎症事件; 多元双环辛烷的组合文库及其作为文库和单独化合物合成的方法。

8. 发明申请

US20020045573A1 POLYDITHIOCARBAMATE-CONTAINING NON-TARGETING MACROMOLECULES AND THE USE THEREOF FOR THERAPEUTIC AND DIAGNOSTIC APPLICATIONS 失效
标题翻译：含聚异戊二酰胺的非靶向大分子及其用于治疗和诊断应用的用途
公开(公告)号：US20020045573A1
公开(公告)日：2002-04-18
申请号：US09409645
申请日：1999-10-01
发明人： CHING-SAN LAI
IPC分类号： A61K038/16 , A61K031/415 , C07H021/00 , A61K031/715 , A01N043/04 , A61K031/70 , C07H001/00 , C08H001/00 , C07K017/00 , A01N043/56 , A61K031/27 , A01N047/10
CPC分类号： C07C333/20
摘要： In accordance with the present invention, there is provided a new class of drugs for therapeutic treatment of such indications as cerebral stroke and other ischemia/reperfusion injury. Thus, in accordance with the present invention, dithiocarbamates are linked to the surface of a non-immunogenic, non-targeting macromolecule other than an antibody (e.g., albumin protein) either by using cross-linking reagents or by nonspecific binding to produce polydithiocarbamate-macromolecule-containing compositions, which represent a new class of drugs for therapeutic treatment of such indications as cerebral stroke and other ischemia/reperfusion injury. In accordance with another aspect of the present invention, combinational therapeutic methods have been developed for the in vivo inactivation or inhibition of formation (either directly or indirectly) of species which induce the expression of inducible nitric oxide synthase, as well as reducing nitric oxide levels produced as a result of .NO synthase expression. In accordance with yet another aspect of the present invention, magnetic resonance imaging methods have been developed for the measurement of cerebral and cardiac blood flow and infarct volume in ischemic stroke or heart attack situations. Such methods employ iron-containing complexes of a composition comprising a dithiocarbamate and a non-immunogenic, non-targeting macromolecule other than an antibody as contrast agents.
摘要翻译：根据本发明，提供了一类用于治疗性治疗诸如脑中风和其他缺血/再灌注损伤的适应症的药物。因此，根据本发明，通过使用交联试剂或通过非特异性结合将二硫代氨基甲酸酯与除抗体（例如白蛋白蛋白）之外的非免疫原性非靶向大分子的表面连接以产生聚二硫代氨基甲酸盐 - 其代表用于治疗性治疗脑卒中和其他缺血/再灌注损伤的新一类药物。根据本发明的另一方面，已经开发出组合治疗方法用于体内失活或抑制诱导一氧化氮合酶表达的物种的形成（直接或间接），以及还原一氧化氮水平作为.NO合酶表达的结果产生。根据本发明的另一方面，已经开发了用于测量缺血性卒中或心脏病发作情况下的脑和心脏血流量和梗死体积的磁共振成像方法。这样的方法使用包含二硫代氨基甲酸盐和除抗体之外的非免疫原性非靶向大分子作为造影剂的组合物的含铁络合物。

9. 发明申请

US20010002403A1 N-chlorophenylcarbamate and N-chlorophenylthiocarbamate compositions 失效
标题翻译： N-氯苯基氨基甲酸酯和N-氯苯硫基氨基甲酸酯组合物
公开(公告)号：US20010002403A1
公开(公告)日：2001-05-31
申请号：US09748652
申请日：2000-12-22
申请人： The Procter & Gamble Company
发明人： James Berger Camden
IPC分类号： A61K031/27 , A01N047/10
CPC分类号： A61K31/415 , A61K31/27 , A61K45/06 , A61K2300/00
摘要： Methods for the treatment of cancers or viral infections in mammals are disclosed that include administration of an N-chlorophenylcarbamate, or an N-chlorophenylthiocarbamate, or a salt thereof. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
摘要翻译：公开了用于治疗哺乳动物中的癌症或病毒感染的方法，包括施用N-氯苯基氨基甲酸酯或N-氯苯基硫代氨基甲酸酯或其盐。这样的化合物可以与化疗剂和/或增效剂组合使用。

10. 发明申请

US20040132809A1 Cell adhesion inhibitors 失效
标题翻译：细胞粘附抑制剂
公开(公告)号：US20040132809A1
公开(公告)日：2004-07-08
申请号：US10677756
申请日：2003-10-03
申请人： Biogen, Inc.
发明人： Daniel Scott , Wen-Cherng Lee , Russell C. Petter , Mark Cornebise
IPC分类号： A61K031/27 , A61K031/22 , A61K031/17 , A61K031/18 , A61K031/16
CPC分类号： C07D401/06 , A61K38/00 , C07D205/04 , C07D207/16 , C07D207/48 , C07D209/42 , C07D211/32 , C07D265/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07K5/0215 , C07K5/06165 , C07K5/06191
摘要： A cell adhesion inhibitor of the general formula: R3nullLnullLnullnullR1 is disclosed. An inhibitor of the present invention interacts with VLA-4 molecules and inhibits VLA-4 dependent cell adhesion. Also disclosed are methods for preparing and using such a cell adhesion inhibitor, as well as pharmaceutical compositions containing the same.
摘要翻译：公开了通式为R 3 -L-L'-R 1的细胞粘附抑制剂。本发明的抑制剂与VLA-4分子相互作用并抑制VLA-4依赖性细胞粘附。还公开了制备和使用这种细胞粘附抑制剂的方法以及含有该细胞粘附抑制剂的药物组合物。

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