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1. 发明申请

US20100113439A1 Antifungal agents 有权
标题翻译：抗真菌剂
公开(公告)号：US20100113439A1
公开(公告)日：2010-05-06
申请号：US12461318
申请日：2009-08-07
申请人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, JR. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
发明人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, JR. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
IPC分类号： A61K31/5377 , C07D405/04 , C07D405/14 , C07D413/14 , A61P31/10 , C07D417/14 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/454 , A61K31/427 , A61K31/4192 , A61K31/4196
CPC分类号： A61K31/343 , A01N43/653 , A61K31/21 , A61K31/41 , C07D493/08 , C07D519/00
摘要： Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译：本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

2. 发明授权

US08722727B2 Antifungal agents 有权
标题翻译：抗真菌剂
公开(公告)号：US08722727B2
公开(公告)日：2014-05-13
申请号：US13058227
申请日：2009-08-10
申请人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, Jr. , Ahmed Mamai
发明人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, Jr. , Ahmed Mamai
IPC分类号： A61K31/35 , C07D311/78
CPC分类号： A61K31/21 , A61K31/41 , C07D405/04
摘要： Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译：本文公开了enfumafungin的新型衍生物以及“其药学上可接受的盐，水合物和前药”。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

3. 发明授权

US08188085B2 Antifungal agents 有权
标题翻译：抗真菌剂
公开(公告)号：US08188085B2
公开(公告)日：2012-05-29
申请号：US12461318
申请日：2009-08-07
申请人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, Jr. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
发明人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, Jr. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
IPC分类号： A61K31/41 , A61K31/445 , A61K31/501 , C07D231/02 , C07D249/08 , C07D401/00 , C07D401/02 , C07D405/02 , C07D405/14
CPC分类号： A61K31/343 , A01N43/653 , A61K31/21 , A61K31/41 , C07D493/08 , C07D519/00
摘要： Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译：本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

4. 发明申请

US20110224228A1 ANTIFUNGAL AGENTS 有权
标题翻译：反真菌药
公开(公告)号：US20110224228A1
公开(公告)日：2011-09-15
申请号：US13058227
申请日：2009-08-10
申请人： Mark L Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, JR. , Ahmed Mamai
发明人： Mark L Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, JR. , Ahmed Mamai
IPC分类号： A61K31/496 , C07D405/08 , C07D405/14 , C07D409/14 , A61K31/41 , A61K31/454 , A61P31/10
CPC分类号： A61K31/21 , A61K31/41 , C07D405/04
摘要： Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译：本文公开了enfumafungin的新型衍生物以及“其药学上可接受的盐，水合物和前药”。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

5. 发明申请

US20070265318A1 Estrogen Receptor Modulators 有权
标题翻译：雌激素受体调节剂
公开(公告)号：US20070265318A1
公开(公告)日：2007-11-15
申请号：US11792729
申请日：2005-12-05
申请人： Mark Greenlee , Dongfang Meng , Donald Sperbeck , Kenneth Wildonger
发明人： Mark Greenlee , Dongfang Meng , Donald Sperbeck , Kenneth Wildonger
IPC分类号： A61K31/4192 , A61P19/08 , C07D249/16
CPC分类号： C07D249/16
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病，软骨变性，子宫内膜异位症，子宫肌瘤疾病，潮热，LDL胆固醇水平升高，心血管疾病，认知功能障碍，年龄相关性轻度认知障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增生，肥胖，失禁，炎症，炎症性肠病，肠易激综合征，性功能障碍，高血压，视网膜变性和癌症，特别是乳腺，子宫和前列腺。

6. 发明申请

US20050090502A1 5-Substituted 1,1-dioxo-'1,2,5!thiazolidine-3-one derivatives as ptpase 1b inhibitors 有权
标题翻译： 5-取代的1,1-二氧代-1,2,5'噻唑烷-3-酮衍生物作为ptpase 1b抑制剂
公开(公告)号：US20050090502A1
公开(公告)日：2005-04-28
申请号：US10510026
申请日：2003-04-02
申请人： Gary Coppola , John Davies , Charles Jewell Jr , Yu-Chin Li , James Wareing , Donald Sperbeck , Travis Stams , Sidney Topiol , Isidoros Vlattas
发明人： Gary Coppola , John Davies , Charles Jewell Jr , Yu-Chin Li , James Wareing , Donald Sperbeck , Travis Stams , Sidney Topiol , Isidoros Vlattas
IPC分类号： A61K31/433 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/5513 , A61K38/55 , A61K45/00 , A61P1/00 , A61P1/18 , A61P3/06 , A61P3/08 , A61P3/10 , A61P5/50 , A61P9/00 , A61P9/10 , A61P9/12 , A61P19/10 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D285/10 , C07D285/14 , C07D417/02 , C07D417/06 , C07D417/10
CPC分类号： C07D285/10 , C07D417/06 , C07D417/10 , C07K5/06078
摘要： Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of conditions that accompany Type 2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物提供作为PTPase抑制剂的药理学试剂，特别是式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。本发明的化合物也可用于抑制具有磷酸酪氨酸结合区的其它酶，例如SH2结构域。因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，糖尿病，高血压和大血管和小血管缺血性疾病相关的胰岛素抵抗。本发明的化合物还可用于治疗，预防或控制伴随2型糖尿病的多种病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞瘤和癌。作为脂肪肉瘤，血脂异常和其他指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

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