公开(公告)号：US20080009504A1

公开(公告)日：2008-01-10

申请号：US11727927

申请日：2007-03-29

申请人： James Balkovec ,  Frances Bouffard ,  Bruno Tse ,  James Dropinski ,  Dongfang Meng ,  Mark Greenlee ,  Michael Peel ,  Weiming Fan ,  Ahmed Mamai ,  Hao Liu ,  Keqaing Li

发明人： James Balkovec ,  Frances Bouffard ,  Bruno Tse ,  James Dropinski ,  Dongfang Meng ,  Mark Greenlee ,  Michael Peel ,  Weiming Fan ,  Ahmed Mamai ,  Hao Liu ,  Keqaing Li

IPC分类号： A61K31/495 ,  A61K31/35 ,  A61K31/4196 ,  A61P31/00 ,  C07D239/02 ,  C07D277/02 ,  C07D311/02 ,  C07D295/00 ,  C07D249/08 ,  C07D207/00 ,  A61K31/496 ,  A61K31/426

CPC分类号： C07J71/0005

摘要： The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (1,3)-β-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.

摘要翻译： 本发明涉及式I的新型烯虫腈衍生物及其药学上可接受的盐，其合成及其作为（1,3）-β-D-葡聚糖合酶抑制剂的用途。 本发明化合物及其药学上可接受的盐以及包含本发明化合物及其药学上可接受的盐的药物组合物可用于治疗或预防抗真菌感染和相关疾病和病症。

公开(公告)号：US07863465B2

公开(公告)日：2011-01-04

申请号：US11727927

申请日：2007-03-29

申请人： James M. Balkovec ,  Frances Aileen Bouffard ,  Bruno Tse ,  James Dropinski ,  Dongfang Meng ,  Mark L. Greenlee ,  Michael Peel ,  Weiming Fan ,  Ahmed Mamai ,  Hao Liu ,  Keqaing Li

发明人： James M. Balkovec ,  Frances Aileen Bouffard ,  Bruno Tse ,  James Dropinski ,  Dongfang Meng ,  Mark L. Greenlee ,  Michael Peel ,  Weiming Fan ,  Ahmed Mamai ,  Hao Liu ,  Keqaing Li

IPC分类号： C07D311/00 ,  C07D315/00

CPC分类号： C07J71/0005

摘要： The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (1,3)-β-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.

摘要翻译： 本发明涉及式I的新型烯虫腈衍生物及其药学上可接受的盐，它们的合成及其作为（1,3） - β-葡聚糖合酶抑制剂的用途。 本发明化合物及其药学上可接受的盐以及包含本发明化合物及其药学上可接受的盐的药物组合物可用于治疗或预防抗真菌感染和相关疾病和病症。

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。

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。

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。

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。

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。

公开(公告)号：US20180030036A1

公开(公告)日：2018-02-01

申请号：US15534029

申请日：2015-12-07

申请人： Ting ZHANG ,  Yi-Heng CHEN ,  Liangqin GUO ,  Alan HARUZA ,  Tianying JIAN ,  Bing LI ,  Dongfang MENG ,  Dann L. PARKER, JR. ,  Edward C. SHERER ,  Harold B. WOOD ,  Isao SAKURADA ,  MERCK SHARP & DOHME CORP. ,  MOCHIDA PHARMACEUTICAL CO., LTD

发明人： Ting Zhang ,  Yi-Heng Chen ,  Liangqin Guo ,  Alan Hruza ,  Tianying Jian ,  Bing Li ,  Dongfang Meng ,  Dann L. Parker ,  Edward C. Sherer ,  Harold B. Wood ,  Isao Sakurada

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D471/04

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

摘要： The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.

公开(公告)号：US20110263663A1

公开(公告)日：2011-10-27

申请号：US13040211

申请日：2011-03-03

申请人： Samuel J. Danishefsky ,  Peter Bertinato ,  Dai-shi Su ,  Dongfang Meng ,  Ting-Chao Chou ,  Ted Kamenecka ,  Erik J. Sorensen ,  Aaron Balog ,  Kenneth A. Savin

发明人： Samuel J. Danishefsky ,  Peter Bertinato ,  Dai-shi Su ,  Dongfang Meng ,  Ting-Chao Chou ,  Ted Kamenecka ,  Erik J. Sorensen ,  Aaron Balog ,  Kenneth A. Savin

IPC分类号： A61K31/427 ,  A61P35/00

CPC分类号： A61K31/704 ,  A61K31/335 ,  A61K31/337 ,  A61K31/425 ,  A61K31/475 ,  A61K31/70 ,  A61K45/06 ,  C07C69/007 ,  C07D277/24 ,  C07D313/00 ,  C07D417/06 ,  C07D417/14 ,  C07D493/04 ,  C07F7/1804 ,  A61K2300/00

摘要： The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

摘要翻译： 本发明提供用于制备埃坡霉素A和B，脱氧头孢菌素A和B及其类似物的收敛方法。 还提供了与埃坡霉素A和B相关的类似物以及可用于制备它的中间体。 本发明还提供了基于埃坡霉素类似物的新型组合物和治疗癌症和癌症的方法，其已经开发出多药耐药表型。

公开(公告)号：USRE41990E1

公开(公告)日：2010-12-07

申请号：US11649750

申请日：2007-01-04

申请人： Samuel J. Danishefsky ,  Peter Bertinato ,  Dai-Shi Su ,  Dongfang Meng ,  Ting-Chao Chou ,  Ted Kamenecka ,  Erik J. Sorensen ,  Aaron Balog ,  Kenneth A. Savin

发明人： Samuel J. Danishefsky ,  Peter Bertinato ,  Dai-Shi Su ,  Dongfang Meng ,  Ting-Chao Chou ,  Ted Kamenecka ,  Erik J. Sorensen ,  Aaron Balog ,  Kenneth A. Savin

IPC分类号： A61K31/365 ,  A61K31/427 ,  C07D277/22 ,  C07D313/00

CPC分类号： A61K31/704 ,  A61K31/335 ,  A61K31/337 ,  A61K31/425 ,  A61K31/475 ,  A61K31/70 ,  A61K45/06 ,  C07C69/007 ,  C07D277/24 ,  C07D313/00 ,  C07D417/06 ,  C07D417/14 ,  C07D493/04 ,  C07F7/1804 ,  A61K2300/00

摘要： The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.