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1. 发明申请

WO2007126900A3 ANTIFUNGAL AGENTS 审中-公开
标题翻译：反真菌药
公开(公告)号：WO2007126900A3
公开(公告)日：2008-01-03
申请号：PCT/US2007007697
申请日：2007-03-29
申请人： MERCK & CO INC , SCYNEXIS INC , GREENLEE MARK L , MENG DONGFANG , MAMAI AHMED , FAN WEIMING , BALKOVEC JAMES M , PEEL MICHAEL , LI KEQAING
发明人： GREENLEE MARK L , MENG DONGFANG , MAMAI AHMED , FAN WEIMING , BALKOVEC JAMES M , PEEL MICHAEL , LI KEQAING
IPC分类号： A61K31/58 , A61P31/10 , C07J71/00
CPC分类号： C07J71/0005
摘要： The present invention relates to novel enfumafungin derivatives of Formula IV-IA and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitorspf(r,3)-ß-D-glucan synthase. The present compounds and pharmaceutically acceptable salts therpøt, as WeILaS1Sy-pharmaceutical compositions comprising the present compounds and pharmaceuticalty 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IV-IA的新型enfumafungin衍生物及其药学上可接受的盐，其合成及其作为（r，3）-β-D-葡聚糖合酶抑制剂的用途。包含本发明化合物及其药学上可接受的盐的本发明化合物和药学上可接受的盐作为包含本发明化合物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。

2. 发明申请

WO2007127012B1 ANTIFUNGAL AGENTS 审中-公开
标题翻译：反真菌药
公开(公告)号：WO2007127012B1
公开(公告)日：2008-02-21
申请号：PCT/US2007007856
申请日：2007-03-29
申请人： MERCK & CO INC , SCYNEXIS INC , BALKOVEC JAMES M , BOUFFARD FRANCES AILEEN , TSE BRUNO , DROPINSKI JAMES , MENG DONGFANG , GREENLEE MARK L , PEEL MICHAEL , FAN WEIMING , MAMAI AHMED , LIU HAO , LI KEQAING
发明人： BALKOVEC JAMES M , BOUFFARD FRANCES AILEEN , TSE BRUNO , DROPINSKI JAMES , MENG DONGFANG , GREENLEE MARK L , PEEL MICHAEL , FAN WEIMING , MAMAI AHMED , LIU HAO , LI KEQAING
IPC分类号： A61K31/58 , A61P31/10 , C07J71/00
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 (l,3)-ß-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。

3. 发明申请

WO2007089291A3 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2007089291A3
公开(公告)日：2007-11-15
申请号：PCT/US2006038559
申请日：2006-09-29
申请人： MERCK & CO INC , GREENLEE MARK L , MENG DONGFANG , PARKER DANN L JR , SUN WANYING , WILDONGER KENNETH J , WILKENING ROBERT R
发明人： GREENLEE MARK L , MENG DONGFANG , PARKER DANN L JR , SUN WANYING , WILDONGER KENNETH J , WILKENING ROBERT R
IPC分类号： C07D231/00 , A61K31/416 , A61K31/4192
CPC分类号： C07D249/16 , C07D231/54 , C07D235/02 , C07D405/04 , C07D413/04
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, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, 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，子宫肌瘤病，热潮红，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎症性肠病，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。

4. 发明申请

WO2006062876A3 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2006062876A3
公开(公告)日：2006-09-14
申请号：PCT/US2005043859
申请日：2005-12-05
申请人： MERCK & CO INC , GREENLEE MARK L , MENG DONGFANG , SPERBECK DONALD M , WILDONGER KENNETH J
发明人： GREENLEE MARK L , MENG DONGFANG , SPERBECK DONALD M , WILDONGER KENNETH J
IPC分类号： A61K31/41 , C07D403/12
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，子宫肌瘤病，热潮红症，低密度脂蛋白胆固醇水平升高，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。

5. 发明申请

WO2010019203A8 ANTIFUNGAL AGENTS 审中-公开
标题翻译：反真菌药
公开(公告)号：WO2010019203A8
公开(公告)日：2011-03-17
申请号：PCT/US2009004557
申请日：2009-08-07
申请人： MERCK SHARP & DOHME , GREENLEE MARK L , WILKENING ROBERT , APGAR JAMES , WILDONGER KENNETH JAMES , MENG DONGFANG , PARKER DANN L JR
发明人： GREENLEE MARK L , WILKENING ROBERT , APGAR JAMES , WILDONGER KENNETH JAMES , MENG DONGFANG , PARKER DANN L JR
IPC分类号： A01N37/18
CPC分类号： A01N43/653 , A61K31/4196 , C07J71/0005
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 (l,3)-ß-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种化合物作为抗真菌剂和/或（1,3）-β-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。

6. 发明申请

WO2004026887A3 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2004026887A3
公开(公告)日：2005-02-24
申请号：PCT/US0328855
申请日：2003-09-15
申请人： MERCK & CO INC , PARKER DANN LEROY , WILKENING ROBERT R , MENG DONGFANG , RATCLIFFE RONALD W
发明人： PARKER DANN LEROY , WILKENING ROBERT R , MENG DONGFANG , RATCLIFFE RONALD W
IPC分类号： C07C45/28 , C07C45/46 , C07C45/63 , C07C45/67 , C07C45/68 , C07C45/73 , C07C49/747 , C07C49/755 , C07C255/47 , C07C255/56 , C07D307/02 , A61K31/341 , A61K31/381 , C07D333/10
CPC分类号： C07C255/56 , C07C45/28 , C07C45/46 , C07C45/63 , C07C45/676 , C07C45/68 , C07C45/73 , C07C49/747 , C07C49/755 , C07C255/47 , C07C2603/30 , C07C47/575
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, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, 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，子宫肌瘤病，热潮红症，低密度脂蛋白胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖症，失禁和癌症的乳房，子宫和前列腺。

7. 发明申请

WO0241835A3 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO0241835A3
公开(公告)日：2003-01-23
申请号：PCT/US0144010
申请日：2001-11-21
申请人： MERCK & CO INC , WILKENING ROBERT R , PARKER DANN LEROY JR , WILDONGER KENNETH J , MENG DONGFANG , RATCLIFFE RONALD W
发明人： WILKENING ROBERT R , PARKER DANN LEROY JR , WILDONGER KENNETH J , MENG DONGFANG , RATCLIFFE RONALD W
IPC分类号： A61K31/403 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61P3/00 , A61P5/30 , A61P5/32 , A61P13/08 , A61P15/00 , A61P15/12 , A61P17/10 , A61P17/14 , A61P19/08 , A61P19/10 , A61P35/00 , A61P43/00 , C07D209/56 , C07D209/70 , C07D231/54 , C07D231/56 , C07D235/02 , C07D249/16 , C07D401/04 , C07D405/04 , C07D409/04 , A61K31/404 , C07D235/04 , C07D249/18
CPC分类号： C07D405/04 , C07D209/56 , C07D231/56 , C07D235/02 , C07D249/16 , C07D401/04 , C07D409/04
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, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, 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，软骨退化，子宫内膜异位症，子宫肌瘤病，热乳头，子宫和前列腺的LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，乳腺发育不全，血管平滑肌细胞增殖，肥胖症，失禁和癌症。

8. 发明专利

DOP2007000062A AGENTES ANTIFÚNGICOS 未知
公开(公告)号：DOP2007000062A
公开(公告)日：2008-03-31
申请号：DO2007000062
申请日：2007-03-30
申请人： MERCK & CO INC , SCYNEXIS INC
发明人： BALKOVEC JAMES M , MENG DONGFANG , GREENLEE MARK L , PELL MICHAEL , FAN WEIMING , LI KEQAING , MAMAI AHMED
摘要： La presente invención se refiere a nuevos derivados de enfumafungina de la Fórmula IV-1A y sus sales farmacéuticamente aceptables, a su síntesis y a su uso como inhibidores de (1,3)-?-D-glucanosintetasa. Los presentes compuestos y sus sales farmacéuticamente aceptables, además de las composiciones farmacéuticas que comprenden los presentes compuestos y sus sales farmacéuticamente aceptables, son útiles para tratar o prevenir infecciones antifúngicas y enfermedades y condiciones patológicas asociadas.

9. 发明专利

CA2649432A1 ANTIFUNGAL AGENTS 未知
公开(公告)号：CA2649432A1
公开(公告)日：2007-11-08
申请号：CA2649432
申请日：2007-03-29
申请人： MERCK & CO INC , SCYNEXIS INC
发明人： DROPINSKI JAMES , LI KEQAING , GREENLEE MARK L , MENG DONGFANG , BOUFFARD FRANCES AILEEN , FAN WEIMING , LIU HAO , MAMAI AHMED , BALKOVEC JAMES M , PEEL MICHAEL , TSE BRUNO
IPC分类号： A61K31/58 , A61P31/10 , C07J71/00
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)-&bgr;-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.

10. 发明专利

CA2649432C ANTIFUNGAL AGENTS 未知
公开(公告)号：CA2649432C
公开(公告)日：2014-06-03
申请号：CA2649432
申请日：2007-03-29
申请人： MERCK & CO INC , SCYNEXIS INC
发明人： BALKOVEC JAMES M , BOUFFARD FRANCES AILEEN , TSE BRUNO , DROPINSKI JAMES , MENG DONGFANG , GREENLEE MARK L , PEEL MICHAEL , FAN WEIMING , MAMAI AHMED , LIU HAO , LI KEQAING
IPC分类号： C07J71/00 , A61K31/58 , A61P31/10
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 (l,3)-.beta.-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.

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