公开(公告)号：EP1827421A2

公开(公告)日：2007-09-05

申请号：EP05852923.1

申请日：2005-12-05

申请人： Merck & Co., Inc.

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： 本发明涉及化合物及其衍生物，它们的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有关的多种病症，包括：骨损失，骨折，骨质疏松症，转移性骨疾病，佩吉特氏病，牙周病， 软骨退化，子宫内膜异位，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，年龄相关的轻度认知障碍，脑退行性疾病，再狭窄，男子女性型乳房，血管平滑肌细胞增殖，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，特别是乳房，子宫和前列腺。

公开(公告)号：EP1418900A1

公开(公告)日：2004-05-19

申请号：EP02761314.0

申请日：2002-08-09

申请人： Merck & Co., Inc.

发明人： MENG, Dongfang ,  PARKER, Dann, LeRoy, Jr. ,  RATCLIFFE, Ronald, W. ,  WILKENING, Robert, R.

IPC分类号： A61K31/135 ,  C07C211/00

CPC分类号： C07D295/088 ,  A61K31/135 ,  C07B2200/07 ,  C07C225/22 ,  C07C255/47 ,  C07C255/58 ,  C07C2603/18 ,  C07C2603/86 ,  C07D307/46

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，软骨退化，子宫内膜异位症，子宫肌瘤病，热 特别是乳腺，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，男子乳腺发育症，血管平滑肌细胞增殖，肥胖症，失禁和癌症。

公开(公告)号：EP1339683B1

公开(公告)日：2006-06-14

申请号：EP01995915.4

申请日：2001-11-21

申请人： Merck & Co., Inc.

发明人： WILKENING, Robert, R. ,  PARKER, Dann Leroy, Jr. ,  WILDONGER, Kenneth, J. ,  MENG, Dongfang ,  RATCLIFFE, Ronald, W.

IPC分类号： C07D209/56 ,  C07D235/04 ,  C07D249/18 ,  A61K31/404 ,  A61P5/30

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： 本发明涉及化合物及其衍生物，它们的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有关的各种病症，包括：骨损失，骨折，骨质疏松症，软骨退化，子宫内膜异位症，子宫肌瘤疾病，炎热 闪烁，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，乳腺癌，血管平滑肌细胞增殖，肥胖症，失禁和癌症，特别是乳房，子宫和前列腺。

公开(公告)号：EP1943224A2

公开(公告)日：2008-07-16

申请号：EP06849833.6

申请日：2006-09-29

申请人： Merck & Co., Inc.

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.

公开(公告)号：EP1339683A2

公开(公告)日：2003-09-03

申请号：EP01995915.4

申请日：2001-11-21

申请人： Merck & Co., Inc.

发明人： WILKENING, Robert, R. ,  PARKER, Dann Leroy, Jr. ,  WILDONGER, Kenneth, J. ,  MENG, Dongfang ,  RATCLIFFE, Ronald, W.

IPC分类号： C07D209/56 ,  C07D235/04 ,  C07D249/18 ,  A61K31/404 ,  A61P5/30

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.

公开(公告)号：EP1551820A2

公开(公告)日：2005-07-13

申请号：EP03754563.9

申请日：2003-09-15

申请人： Merck & Co., Inc.

发明人： PARKER, Dann, LeRoy ,  WILKENING, Robert, R. ,  MENG, Dongfang ,  RATCLIFFE, Ronald, W.

IPC分类号： C07D307/02 ,  C07D333/10 ,  A61K31/341 ,  A61K31/381

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： 本发明涉及化合物及其衍生物，它们的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有关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特病，牙周病 ，软骨变性，子宫内膜异位，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，脑退行性疾病，再狭窄，男子女性型乳房，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。