公开(公告)号：EP1027353A1

公开(公告)日：2000-08-16

申请号：EP98950727.2

申请日：1998-09-28

申请人： MERCK & CO., INC.

发明人： DININNO, Frank, P. ,  DYKSTRA, Kevin, D.

IPC分类号： C07D487/04 ,  A61K31/395

CPC分类号： C07D477/14

摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a -Z-CH2 group. The naphthosultam is further substituted with various substituent groups including cationic groups. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.

公开(公告)号：EP1084105A1

公开(公告)日：2001-03-21

申请号：EP99924539.2

申请日：1999-05-28

申请人： MERCK & CO., INC.

发明人： DININNO, Frank, P. ,  DYKSTRA, Kevin, D.

IPC分类号： C07D205/00 ,  A61K31/395

CPC分类号： C07D477/14

摘要： The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6-membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.

公开(公告)号：EP0682667A1

公开(公告)日：1995-11-22

申请号：EP94907775.0

申请日：1994-01-03

申请人： MERCK & CO. INC.

发明人： DININNO, Frank, P. ,  GREENLEE, Mark, L. ,  RANO, Thomas, A. ,  LEE, Wendy

IPC分类号： C07D477 ,  A61K31 ,  A61P31

CPC分类号： C07D477/14

摘要： The present invention relates to antibacterial agents of the carbapenem class, in which the 2-position sidechain is characterized by a phenanthridine moiety, substituted by various neutral substituents.

公开(公告)号：EP1328522A2

公开(公告)日：2003-07-23

申请号：EP01987651.5

申请日：2001-10-15

申请人： Merck & Co., Inc.

发明人： DININNO, Frank, P. ,  KIM, Seongkon ,  WU, Jane, Y.

IPC分类号： C07D401/00

CPC分类号： C07D411/04 ,  A61K31/4535 ,  C07D327/06

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.

公开(公告)号：EP1086104A1

公开(公告)日：2001-03-28

申请号：EP99926080.5

申请日：1999-05-28

申请人： MERCK & CO., INC.

发明人： DININNO, Frank, P. ,  DYKSTRA, Kevin, D.

IPC分类号： C07D477/14 ,  A61K31/40

CPC分类号： C07D477/14

摘要： The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.

公开(公告)号：EP1501819A1

公开(公告)日：2005-02-02

申请号：EP03736470.0

申请日：2003-04-18

申请人： Merck & Co., Inc.

发明人： DININNO, Frank, P. ,  BLIZZARD, Timothy, Allen ,  MORGAN, Jerry, Dwain, II

IPC分类号： C07D327/06 ,  C07D411/10 ,  A61K31/382

CPC分类号： C07D327/06

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, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

公开(公告)号：EP1082325A1

公开(公告)日：2001-03-14

申请号：EP99925849.4

申请日：1999-05-26

申请人： MERCK & CO., INC.

发明人： DININNO, Frank, P.

IPC分类号： C07D499/887 ,  A61K31/43

CPC分类号： C07D499/88

摘要： The present invention relates to penem antibacterial agents in which the penem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明涉及青霉烯类抗菌剂，其中青霉烯核与6元碳环稠合。 该化合物进一步被各种取代基取代，包括至少一个阳离子基团。 该化合物由式（I）表示。 药物组合物和使用方法也包括在内。

公开(公告)号：EP1032384A1

公开(公告)日：2000-09-06

申请号：EP98953737.8

申请日：1998-10-19

申请人： MERCK & CO., INC.

发明人： DININNO, Frank, P. ,  HAMMOND, Milton, L.

IPC分类号： A61K31/40 ,  C07D477/14

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D477/00

摘要： The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.

公开(公告)号：EP1015453A1

公开(公告)日：2000-07-05

申请号：EP98944779.2

申请日：1998-09-04

申请人： MERCK & CO., INC.

发明人： DININNO, Frank, P. ,  DYKSTRA, Kevin, D.

IPC分类号： C07D477/14 ,  A61K31/40

CPC分类号： C07D477/14

摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with an iodo-substituted phenyl linked through a CH2-O- group. The compounds of the invention are represented by formula (I). Salts and hydrates thereof are included. The iodo-substituted phenyl ring is further substituted with various substituent groups including at least one cationic group. Pharmaceutical compositions and methods of treatment are also included.

公开(公告)号：EP1333827A2

公开(公告)日：2003-08-13

申请号：EP01987654.9

申请日：2001-10-15

申请人： Merck & Co., Inc.

发明人： DININNO, Frank, P. ,  CHEN, Helen, Y. ,  KIM, Seongkon ,  WU, Jane, Y.

IPC分类号： A61K31/395 ,  A61K31/55 ,  A61K31/445 ,  A61K31/40 ,  A61P5/00 ,  C07D405/00 ,  C07D409/00 ,  C07D205/00 ,  C07D213/02 ,  C07D411/00

CPC分类号： C07D411/04 ,  C07D327/06 ,  C07D339/08

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.