公开(公告)号：EP2326180B1

公开(公告)日：2013-10-16

申请号：EP09806946.1

申请日：2009-08-10

Applicant: Merck Sharp & Dohme Corp. ,  Scynexis, Inc.

Inventor： GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  SPERBECK, Donald ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L., Jr. ,  MAMAI, Ahmed

IPC: A01N43/64 ,  A61K31/21 ,  A61K31/41

CPC classification number: A61K31/21 ,  A61K31/41 ,  C07D405/04

公开(公告)号：EP2007396B1

公开(公告)日：2013-02-13

申请号：EP07754382.5

申请日：2007-03-29

Applicant: Merck Sharp & Dohme Corp. ,  Scynexis, Inc.

Inventor： 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: A61K31/58 ,  C07J71/00 ,  A61P31/10

CPC classification number: C07J71/0005

公开(公告)号：EP2326181A1

公开(公告)日：2011-06-01

申请号：EP09806945.3

申请日：2009-08-07

Applicant: Merck Sharp & Dohme Corp. ,  Scynexis, Inc.

Inventor： GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  SPERBECK, Donald ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L. Jr. ,  PACOFSKY, Gregory, James ,  HEASLEY, Brian, Haid ,  MAMAI, Ahmed ,  NELSON, Kingsley

IPC: A01N43/64 ,  A61K31/21 ,  A61K31/41

CPC classification number: A61K31/343 ,  A01N43/653 ,  A61K31/21 ,  A61K31/41 ,  C07D493/08 ,  C07D519/00

Abstract: 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)-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.

Abstract translation: 本文公开了enfumafungin的新衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含此类化合物的组合物，制备此类化合物的方法以及使用此类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。 公开的化合物，它们的药学上可接受的盐，水合物和前药以及包含此类化合物，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：EP2326180A1

公开(公告)日：2011-06-01

申请号：EP09806946.1

申请日：2009-08-10

Applicant: Merck Sharp & Dohme Corp. ,  Scynexis, Inc.

Inventor： GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  SPERBECK, Donald ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L., Jr. ,  MAMAI, Ahmed

IPC: A01N43/64 ,  A61K31/21 ,  A61K31/41

CPC classification number: A61K31/21 ,  A61K31/41 ,  C07D405/04

Abstract: 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 (l,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.

公开(公告)号：EP1943224B1

公开(公告)日：2011-07-27

申请号：EP06849833.6

申请日：2006-09-29

Applicant: Merck Sharp & Dohme Corp.

Inventor： GREENLEE, Mark, L. ,  MENG, Dongfang ,  PARKER, Dann, L., Jr. ,  SUN, Wanying ,  WILDONGER, Kenneth, J. ,  WILKENING, Robert, R.

IPC: C07D231/00 ,  A61K31/416 ,  A61K31/4192 ,  C07D249/16

CPC classification number: C07D249/16 ,  C07D231/54 ,  C07D235/02 ,  C07D405/04 ,  C07D413/04

Abstract: 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.

公开(公告)号：EP1827421B1

公开(公告)日：2017-09-27

申请号：EP05852923.1

申请日：2005-12-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： GREENLEE, Mark, L. ,  MENG, Dongfang ,  SPERBECK, Donald, M. ,  WILDONGER, Kenneth, J.

IPC: C07D249/16 ,  A61K31/4192 ,  A61P5/30 ,  A61P5/32

CPC classification number: C07D249/16

公开(公告)号：EP1883624B1

公开(公告)日：2010-04-07

申请号：EP06770329.8

申请日：2006-05-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： TAYLOR, Gayle, E. ,  MEISSNER, Robert, S. ,  MCVEAN, Carol, A. ,  GREENLEE, Mark, L. ,  ALI, Amjad

IPC: C07C261/00 ,  C07J63/00 ,  A61K31/56

CPC classification number: C07J63/008

公开(公告)号：EP2326172A1

公开(公告)日：2011-06-01

申请号：EP09806944.6

申请日：2009-08-07

Applicant: Merck Sharp & Dohme Corp.

Inventor： GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L, Jr.

IPC: A01N37/18

CPC classification number: A01N43/653 ,  A61K31/4196 ,  C07J71/0005

Abstract: 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)-
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.

Abstract translation: 本文公开了enfumafungin的新衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含此类化合物的组合物，制备此类化合物的方法以及使用此类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。 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：EP2326172B1

公开(公告)日：2014-10-22

申请号：EP09806944.6

申请日：2009-08-07

Applicant: Scynexis, Inc.

Inventor： GREENLEE, Mark, L. ,  WILKENING, Robert ,  APGAR, James ,  WILDONGER, Kenneth, James ,  MENG, Dongfang ,  PARKER, Dann, L, Jr.

IPC: A01N37/18

CPC classification number: A01N43/653 ,  A61K31/4196 ,  C07J71/0005

公开(公告)号：EP2007396A1

公开(公告)日：2008-12-31

申请号：EP07754382.5

申请日：2007-03-29

Applicant: Merck and Co., Inc. ,  Scynexis, Inc.

Inventor： 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: A61K31/58 ,  C07J71/00 ,  A61P31/10

CPC classification number: C07J71/0005

Abstract: 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)-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.