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1. 发明申请

US20110195110A1 UREA COMPOUNDS USEFUL IN THE TREATMENT OF CANCER 审中-公开
标题翻译： UREA化合物可用于治疗癌症
公开(公告)号：US20110195110A1
公开(公告)日：2011-08-11
申请号：US12095611
申请日：2006-12-01
申请人： Roger Smith , Holia N. Hatoum-Mokdad , Louis David Cantin , Donald E. Bierer , Wenlang Fu , Dhanapalan Nagarathnam , Gaetan Ladouceur , Yamin Wang , Herbert Ogutu , Scot Wilhelm , Ian Taylor , Sanjeeva Reddy , Richard Gedrich , Christopher Carter , Aaron Schmitt , Xiaomei Zhang
发明人： Roger Smith , Holia N. Hatoum-Mokdad , Louis David Cantin , Donald E. Bierer , Wenlang Fu , Dhanapalan Nagarathnam , Gaetan Ladouceur , Yamin Wang , Herbert Ogutu , Scot Wilhelm , Ian Taylor , Sanjeeva Reddy , Richard Gedrich , Christopher Carter , Aaron Schmitt , Xiaomei Zhang
IPC分类号： A61K9/127 , C07D401/12 , C07D401/14 , A61K31/4439 , A61K31/506 , A61K31/444 , A61K31/4375 , A61K31/4535 , A61K38/20 , A61K33/24 , A61K38/21 , A61K33/36 , A61K39/395 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号： C07D401/12 , C07D401/14
摘要： Pyrazole urea compounds, pharmaceutical compositions which contain them and methods for treating cancer using them.
摘要翻译：吡唑脲化合物，含有它们的药物组合物和使用它们治疗癌症的方法。

2. 发明授权

US5925647A Methods for use of cryptolepine analogs with hypoglycemic activity 失效
标题翻译：使用具有降血糖活性的隐性类固醇的方法
公开(公告)号：US5925647A
公开(公告)日：1999-07-20
申请号：US955320
申请日：1997-10-20
申请人： Donald E. Bierer
发明人： Donald E. Bierer
IPC分类号： A61K31/475 , A61K31/64 , C07D471/16 , C07D491/048 , A61K31/44
CPC分类号： A61K31/7004 , A61K31/475 , A61K31/64 , C07D471/16 , Y10S514/866 , Y10S514/884
摘要： Novel cryptolepine analogs useful as hypoglycemic agents and methods for their use as hypoglycemic agents, for example, in the treatment of diabetes, and a method for their synthesis are described. As hypoglycemic agents, the novel cryptolepine analogs are useful for the treatment of insulin-dependent diabetes mellitus (IDDM or Type I) and non-insulin dependent diabetes mellitus (NIDDM or Type II).
摘要翻译：描述了作为降血糖药物使用的新型隐黑血素类似物及其作为降血糖药物使用的方法，例如治疗糖尿病及其合成方法。作为降血糖药，该新型隐黑血糖类似物可用于治疗胰岛素依赖性糖尿病（IDDM或I型）和非胰岛素依赖性糖尿病（NIDDM或II型）。

3. 发明授权

US5917052A Hypoglycemic agent from cryptolepis 失效
标题翻译：来自密类的低血糖药
公开(公告)号：US5917052A
公开(公告)日：1999-06-29
申请号：US314188
申请日：1994-09-28
申请人： Donald E. Bierer , Diana M. Fort
发明人： Donald E. Bierer , Diana M. Fort
IPC分类号： A61K31/4745 , A61K31/475 , A61K31/64 , A61K31/715 , A61K36/27 , A61K38/28 , C07D471/04 , C07D471/16 , C07D209/80
CPC分类号： A61K31/475 , A61K31/4745 , A61K31/64 , A61K31/7004 , A61K31/715 , A61K36/27 , A61K38/28 , C07D471/04 , Y10S514/866 , Y10S514/884
摘要： The use of extracts from Cryptolepis sp. or quindoline alkaloids such quindoline and cryptolepine contained therein as hypoglycemic agents, as well as methods for obtaining the hypoglycemic agents are described. According to a preferred embodiment, the extracts are derived from Cryptolepis sanguinolenta. As hypoglycemic agents, the extracts or quindoline alkaloids such as quindoline or cryptolepine are useful for treating insulin-dependent (type I) and non-insulin-dependent (type II) diabetes.
摘要翻译：使用Cryptolepis sp。提取物或喹啉生物碱，如其中含有作为降血糖剂的喹啉和隐树灵，以及获得降血糖剂的方法。根据一个优选的实施方案，提取物衍生自海参甘油三角菌。作为降血糖药，提取物或喹啉生物碱如喹啉或隐高血糖可用于治疗胰岛素依赖型（I型）和非胰岛素依赖型（II型）糖尿病。

4. 发明授权

US5753790A Hypoglycemic agent from cryptolepis 失效
标题翻译：来自密类的低血糖药
公开(公告)号：US5753790A
公开(公告)日：1998-05-19
申请号：US472020
申请日：1995-06-06
申请人： Donald E. Bierer
发明人： Donald E. Bierer
IPC分类号： A61K31/4745 , A61K31/475 , A61K31/64 , A61K31/715 , A61K36/27 , A61K38/28 , C07D471/04 , C07D471/16 , C07D209/80 , C09B7/00
CPC分类号： A61K31/475 , A61K31/4745 , A61K31/64 , A61K31/7004 , A61K31/715 , A61K36/27 , A61K38/28 , C07D471/04 , Y10S514/866 , Y10S514/884
摘要： The use of extracts from Cryptolepis sp. or quinodoline alkaloids such quindoline and cryptolepine contained therein as hypoglycemic agents, as well as methods for obtaining the hypoglycemic agents are described. According to a preferred embodiment, the extracts are derived from Cryptolepis sanguinolenta. As hypoglycemic agents, the extracts or quindoline alkaloids such as quindoline or cryptolepine are useful for treating insulin-dependent (type I) and non-insulin-dependent (type II) diabetes.
摘要翻译：使用Cryptolepis sp。提取物或喹诺酮类生物碱，如其中含有作为降血糖剂的喹诺福尔和隐斜甘油，以及获得降血糖剂的方法。根据一个优选的实施方案，提取物衍生自海参甘油三角菌。作为降血糖药，提取物或喹啉生物碱如喹啉或隐高血糖可用于治疗胰岛素依赖型（I型）和非胰岛素依赖型（II型）糖尿病。

5. 发明授权

US5629319A Hypoglycemic agent from cryptolepis 失效
标题翻译：来自密类的低血糖药
公开(公告)号：US5629319A
公开(公告)日：1997-05-13
申请号：US472036
申请日：1995-06-06
申请人： Jian Luo , Diana M. Fort , Donald E. Bierer , Reimar C. Bruening
发明人： Jian Luo , Diana M. Fort , Donald E. Bierer , Reimar C. Bruening
IPC分类号： A61K31/4745 , A61K31/475 , A61K31/64 , A61K31/715 , A61K36/27 , A61K38/28 , C07D471/04 , C07D471/16 , A61K31/44 , A61K31/40
CPC分类号： A61K31/475 , A61K31/4745 , A61K31/64 , A61K31/7004 , A61K31/715 , A61K36/27 , A61K38/28 , C07D471/04 , Y10S514/866 , Y10S514/884
摘要： The use of extracts from Cryptolepis sp. or quindoline alkaloids such quindoline and cryptolepine contained therein as hypoglycemic agents, as well as methods for obtaining the hypoglycemic agents are described. According to a preferred embodiment, the extracts are derived from Cryptolepis sanguinolenta. As hypoglycemic agents, the extracts or quindoline alkaloids such as quindoline or cryptolepine are useful for treating insulin-dependent (type I) and non-insulin-dependent (type II) diabetes.
摘要翻译：使用Cryptolepis sp。提取物或喹啉生物碱，如其中含有作为降血糖剂的喹啉和隐树灵，以及获得降血糖剂的方法。根据一个优选的实施方案，提取物衍生自海参甘蓝三角菌。作为降血糖药，提取物或喹啉生物碱如喹啉或隐高血糖可用于治疗胰岛素依赖型（I型）和非胰岛素依赖型（II型）糖尿病。

6. 发明授权

US5811568A Process for the preparation of mono- and bis(phosphocholine) derivatives which have antifungal activity 失效
标题翻译：具有抗真菌活性的单和双（磷酸胆碱）衍生物的制备方法
公开(公告)号：US5811568A
公开(公告)日：1998-09-22
申请号：US234483
申请日：1994-04-28
申请人： Donald E. Bierer , Jeffrey M. Dener , Thien V. Truong
发明人： Donald E. Bierer , Jeffrey M. Dener , Thien V. Truong
IPC分类号： A01N57/14 , A01N57/16 , A61K31/66 , A61K31/70 , A61K31/7028 , A61K36/18 , A61K47/24 , A61P31/04 , A61P31/10 , C07F9/09 , C07F9/10 , C07F9/655 , C07G3/00 , C07H15/04 , C07H15/18 , C07F9/02
CPC分类号： A01N57/14 , A01N57/16 , A61K31/685 , A61K31/688 , A61K31/70 , A61K47/24 , C07F9/093 , C07F9/10 , C07H15/04 , C07H15/18
摘要： This invention pertains to a synthetic process for obtaining a unique phosphocholine derivative which has been isolated from the leaves of the plant Irbachia alata, identified to be 1,22-bis�2-(trimethylammonium)ethylphosphatyl! docosane is disclosed. Also disclosed is a synthetic process for obtaining a novel class of mono- and bis(phosphocholine) derivatives which are useful as antiinfective agents. The compounds are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus.
摘要翻译：本发明涉及一种用于获得已鉴定为1,22-双[2-（三甲基铵）乙基磷酰基]二十二烷的植物Irbachia alata的叶分离的独特的磷酸胆碱衍生物的合成方法。还公开了一种用于获得可用作抗感染剂的新型单 - 和双（磷酸胆碱）衍生物的合成方法。这些化合物特别有效地治疗真菌感染，特别是由白色念珠菌，新型隐球菌和烟曲霉引起的真菌感染。

7. 发明授权

US5681829A Class of phosphocholine derivatives having antifungal activity 失效
标题翻译：具有抗真菌活性的磷酸胆碱衍生物类
公开(公告)号：US5681829A
公开(公告)日：1997-10-28
申请号：US411709
申请日：1995-04-05
申请人： Michael Tempesta , Shivanand D. Jolad , Steven King , Guohua Mao , Reimar C. Bruening , John E. Kuo , Thien V. Troung , Donald E. Bierer , Jeffrey M. Dener
发明人： Michael Tempesta , Shivanand D. Jolad , Steven King , Guohua Mao , Reimar C. Bruening , John E. Kuo , Thien V. Troung , Donald E. Bierer , Jeffrey M. Dener
IPC分类号： A01N57/14 , A01N57/16 , A61K31/66 , A61K31/70 , A61K31/7028 , A61K36/18 , A61K47/24 , A61P31/04 , A61P31/10 , C07F9/09 , C07F9/10 , C07F9/655 , C07G3/00 , C07H15/04 , C07H15/18 , C07F9/02
CPC分类号： A01N57/14 , A01N57/16 , A61K31/685 , A61K31/688 , A61K31/70 , A61K47/24 , C07F9/093 , C07F9/10 , C07H15/04 , C07H15/18
摘要： Certain phosphocholine derivatives having substantial antifungal therapeutic activity are disclosed. The phosphocholine derivatives may be chemically synthesized, enzymatically prepared or extracted from the plant Irlbachia alata. The phosphocholine derivatives are useful in treating fungal infections including those which are dermatophytic, systemic, ophthalmic and vaginal.
摘要翻译： PCT No.PCT / US93 / 09623 Sec。 371日期1995年04月5日 102（e）日期1995年4月5日PCT提交1993年10月8日PCT公布。出版物WO94 / 08563 日期：1994年4月28日公开了具有大量抗真菌治疗活性的磷酸胆碱衍生物。磷酸胆碱衍生物可以从植物Irlbachia alata化学合成，酶促制备或提取。磷酸胆碱衍生物可用于治疗真菌感染，包括皮肤真菌，全身性，眼睛和阴道的真菌感染。

8. 发明授权

US06849638B2 4-AMINO-5,6-SUBSTITUTED THIOPHENO [2,3-D] PYRIMIDINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND THEIR USE IN THE TREATMENT OR PREVENTION OF PDE7B-MEDIATED DISEASES AND CONDITIONS 失效
标题翻译： 4-氨基-5,6-取代的噻吩并[2,3-D]嘧啶，含有它们的药物组合物及其在治疗或预防PDE7B介导的疾病和病症中的用途
公开(公告)号：US06849638B2
公开(公告)日：2005-02-01
申请号：US10136575
申请日：2002-04-29
申请人： Andreas Stolle , Donald E. Bierer , Yuanwei Chen , Dongping Fan , Barry Hart , Mary Katherine Monahan , William J. Scott
发明人： Andreas Stolle , Donald E. Bierer , Yuanwei Chen , Dongping Fan , Barry Hart , Mary Katherine Monahan , William J. Scott
IPC分类号： A61K31/4365 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P1/04 , A61P1/18 , A61P3/10 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/08 , A61P25/24 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D495/04 , C07D495/14 , C07D521/00
CPC分类号： C07D231/12 , A61K31/4365 , A61K31/519 , A61K31/5377 , A61K31/541 , C07D233/56 , C07D249/08 , C07D495/04 , C07D495/14
摘要： The invention relates to 4-amino-5,6-substituted thiopheno [2,3-d] pyrimidines, pharmaceutical compositions containing the same and their use to treat or prevent diseases and conditions mediated by the phosphodiesterase enzyme 7B (PDE7B). Diseases and conditions mediated by PDE7B include osteoporosis, osteopenia and asthma.
摘要翻译：本发明涉及4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶，含有它们的药物组合物及其用于治疗或预防由磷酸二酯酶7B（PDE7B）介导的疾病和病症的用途。 PDE7B介导的疾病和病症包括骨质疏松症，骨质减少和哮喘。

9. 发明授权

US5648354A 1,2-dithiins having antifungal activity 失效
标题翻译：具有抗真菌活性的1,2-二硫辛酸
公开(公告)号：US5648354A
公开(公告)日：1997-07-15
申请号：US395777
申请日：1995-02-28
申请人： Donald E. Bierer , Jeffrey M. Dener , Joane Litvak , Larisa G. Dubenko
发明人： Donald E. Bierer , Jeffrey M. Dener , Joane Litvak , Larisa G. Dubenko
IPC分类号： C07D339/08 , C07D409/06 , C07D409/12 , C07D409/14 , C07D521/00 , C07F7/18 , A61K31/385
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D339/08 , C07D409/06 , C07D409/12 , C07D409/14 , C07F7/1856
摘要： Novel 1,2-dithiin compounds useful as antifungal or anti-infective agents, as well as methods for their use as such, are described. The 1,2-dithiin compounds are particularly effective in treating infections, especially those caused by Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Candida krusei, Candida parapsilosis, Candida tropicalis, Trichophyton rubrum, Epidermophyton species, Microsporum species, Sporothrix species, Blastomyces dermatitidis, Coccidiodes immiitis, Histoplasma capsulatum, Herpes virus, Influenza virus, Cytomegalovirus, human immunodeficiency virus, retrovirus, Adenovirus, Papillomavirus, Paravirus, Arenavirus, Bunyavirus, Coronavirus, Paramyxovirus, Picornavirus, Rhabdovirus, Togavirus, Hepadnavirus, Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Enterobacter aerogenes, Klebsiella pneumoniae, Staphylococcus epidermis, Zanthomonus maltrophilia, Acinetobacter, Enterobacter cloacae, Serratia marscens, Listeria, Monocytogenes, Enterococcus faecalis, Streptococcus pyogenes; Streptococcus pneumonia, Viridans streptococci, Haemophilus influenzae, Proteus mirabills, Proteus vulgaris and Bacterioides fragilis.
摘要翻译：描述了可用作抗真菌剂或抗感染剂的新颖的1,2-二硫素化合物，以及它们如此使用的方法。 1,2-二硫素化合物特别有效地治疗感染，特别是由白色念珠菌，新型隐球菌，烟曲霉，卡尼酵母，热带假丝酵母，热带假丝酵母，红色毛癣菌，表皮癣菌属，微孢子虫种，孢子虫属，皮肤真菌，球孢子虫疫霉菌，耻垢球菌，疱疹病毒，流感病毒，巨细胞病毒，人类免疫缺陷病毒，逆转录病毒，腺病毒，乳头瘤病毒，副病毒，瘟病毒，布尼亚病毒，冠状病毒，副粘病毒，小RNA病毒，犀牛病毒，披头丝病毒，肝炎病毒，金黄色葡萄球菌，粪便链球菌大肠杆菌，铜绿假单胞菌，产气肠杆菌，肺炎克雷伯杆菌，表皮葡萄球菌，嗜麦芽寡糖杆菌，不动杆菌，阴沟肠杆菌，沙雷氏菌，李斯特菌，单核细胞增多症，粪肠球菌，化脓链球菌; 肺炎链球菌，维生素链球菌，流感嗜血杆菌，变形杆菌，普通变形杆菌和脆弱杆菌。

10. 发明授权

US5583235A Preparation of symmetrical and unsymmetrical 3,6-disubstituted-1,2-dithiins having antifungal activity 失效
标题翻译：具有抗真菌活性的对称和不对称3,6-二取代-1,2-二硫辛的制备
公开(公告)号：US5583235A
公开(公告)日：1996-12-10
申请号：US212096
申请日：1994-03-11
申请人： Donald E. Bierer , Jeffrey M. Dener , Thien V. Truong
发明人： Donald E. Bierer , Jeffrey M. Dener , Thien V. Truong
IPC分类号： C07D339/08 , C07D409/06 , C07D409/12 , C07D409/14 , C07D521/00 , C07F7/18
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D339/08 , C07D409/06 , C07D409/12 , C07D409/14 , C07F7/1856
摘要： The present invention provides an improved procedure for the preparation of 3,6-disubstituted-1,2-dithiin derivatives, especially unsymmetrical 1,2-dithiins. In addition, the process offers significant process, scaleup, and safety advantages over the previously reported synthetic processes. The compounds synthesized by this new process and described herein are particularly effective in treating fungal infections, especially those caused by Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton rubrum, Candida parapsilosis, Candida tropicalis, or Candida krusei.
摘要翻译：本发明提供了制备3,6-二取代-1,2-二硫素衍生物，特别是不对称1,2-二硫辛烷的改进方法。此外，该方法比以前报道的合成方法提供了重要的过程，放大和安全优势。通过这种新方法合成并在本文中描述的化合物在治疗真菌感染，特别是由白色念珠菌，新型隐球酵母，烟曲霉，红色毛癣菌，热带假丝酵母，热带假丝酵母或克罗斯假丝酵母引起的真菌感染中特别有效。

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