专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明申请

WO1998011108A1 CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴因抗菌化合物，含有这些化合物的组合物和处理方法
公开(公告)号：WO1998011108A1
公开(公告)日：1998-03-19
申请号：PCT/US1997015831
申请日：1997-09-08
申请人： MERCK & CO., INC. , CAMA, Lovji, D. , WILKENING, Robert, R. , RATCLIFFE, Ronald, W. , BLIZZARD, Timothy, A.
发明人： MERCK & CO., INC.
IPC分类号： C07D487/04
CPC分类号： C07D477/14 , Y02P20/55
摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a sulfonamide containing ring system linked to the carbapenem nucleus through a CH2 group. The compounds are represented by formula (I) including pharmaceutically acceptable salts thereof, wherein: R represents H or methyl; CO2M represents a carboxylic acid, a carboxylate anion, a pharmaceutically acceptable ester group or a carboxylic acid protected by a protecting group; P represents hydrogen, hydroxyl, F or hydroxyl protected by a hydroxyl-protecting group; X and X represent hydrogen or X and X taken together represent a carbonyl group; and one of AB, BC and CD represents a fused aryl, heteroaryl or heteroarylium ring, and the other variables represent R, said fused aryl, heteroaryl or heteroarylium ring being substituted with from 1-4 R groups. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯细胞核在2-位被具有通过CH2基连接到碳青霉烯核的含磺酰胺的环系统取代。化合物由式（I）表示，包括其药学上可接受的盐，其中：R 1表示H或甲基; CO 2 M表示羧酸，羧酸根阴离子，药学上可接受的酯基或被保护基保护的羧酸; P表示氢，羟基，F或被羟基保护基保护的羟基; X 1和X 2代表氢或X 1和X 2一起代表羰基; 并且AB，BC和CD之一代表稠合芳基，杂芳基或杂芳基环，其它变量表示R，所述稠合芳基，杂芳基或杂芳基环被1-4个R基团取代。还包括药物组合物和使用方法。

3. 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。

4. 发明申请

WO1997040048A1 CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴因抗菌化合物，含有这些化合物的组合物和处理方法
公开(公告)号：WO1997040048A1
公开(公告)日：1997-10-30
申请号：PCT/US1997006626
申请日：1997-04-21
申请人： MERCK & CO., INC. , WILKENING, Robert, R. , RATCLIFFE, Ronald, W. , BLIZZARD, Timothy, A.
发明人： MERCK & CO., INC.
IPC分类号： C07D477/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14 , Y02P20/55
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 CH2 group. The naphthosultam 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：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯核在2-位被用CH2链连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式（I）表示。还包括药物组合物和使用方法。

5. 发明申请

WO1996004282A1 CARBAPENEM COMPOUNDS, COMPOSITIONS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴辛化合物，组合物和治疗方法
公开(公告)号：WO1996004282A1
公开(公告)日：1996-02-15
申请号：PCT/US1995010029
申请日：1995-07-25
申请人： MERCK & CO., INC. , WADDELL, Sherman, T. , RATCLIFFE, Ronald, W. , BLIZZARD, Timothy, A. , WILDONGER, Kenneth, J. , WILKENING, Robert, R. , SZUMILOSKI, Sandra, P.
发明人： MERCK & CO., INC.
IPC分类号： C07D487/04
CPC分类号： C07D477/20 , Y02P20/55
摘要： Carbapenems of formula (I) are disclosed as MRSA active agents. R represents hydrogen or methyl; CO2M represents a carboxylic acid, a carboxylate anion with or without a pharmaceutically acceptable counterion, a pharmaceutically acceptable ester group or a carboxylic acid protected by a protecting group; P* represents hydrogen or a hydroxyl protecting group; Het represents a heterocyclic group which is uncharged or positively charged, containing no more than three positively charged atoms, and is selected from the group consisting of: (a) and (b) wherein represents the point of attachment to S; A represents O or S; and X, Y and Z independently represent CR, N or N R .
摘要翻译：公开了式（I）的碳青霉烯作为MRSA活性剂。 R 1表示氢或甲基; CO 2 M表示羧酸，具有或不具有药学上可接受的抗衡离子的羧酸根阴离子，药学上可接受的酯基或被保护基保护的羧酸; P *表示氢或羟基保护基; Het表示不带电荷或带正电荷的杂环基，其含有不多于三个带正电荷的原子，并且选自：（a）和（b）其中表示与S的连接点; A代表O或S; X，Y和Z独立地表示CR，N或N + R a。

6. 发明申请

WO9912552A8 9a-AZALIDES AS VETERINARY ANTIMICROBIAL AGENTS 审中-公开
标题翻译： 9a-AZALIDES作为兽医抗真菌剂
公开(公告)号：WO9912552A8
公开(公告)日：2013-07-04
申请号：PCT/US9818579
申请日：1998-09-04
申请人： MERCK & CO INC , KROPP HELMUT , FARRINGTON DANIEL O , CLARK JEFFREY N , RATCLIFFE RONALD W , WILKENING ROBERT D
发明人： KROPP HELMUT , FARRINGTON DANIEL O , CLARK JEFFREY N , RATCLIFFE RONALD W , WILKENING ROBERT D
IPC分类号： A61K31/70 , C07H17/00 , A61K31/7042 , A61K31/7052 , A61P31/04
CPC分类号： A61K31/7052
摘要： 9a-Azalides are useful in the treatment and prevention of bacterial respiratory and enteric infections in livestock animals, particularly in cattle and swine.
摘要翻译： 9a-Azalides可用于治疗和预防牲畜，特别是牛和猪中的细菌性呼吸道和肠道感染。

7. 发明申请

WO2004026887A2 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2004026887A2
公开(公告)日：2004-04-01
申请号：PCT/US2003/028855
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： C07H
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。

8. 发明申请

WO02053522A3 NOVEL ESTROGEN RECEPTOR LIGANDS AND METHODS I 审中-公开
标题翻译：新颖的雌激素受体配体和方法I
公开(公告)号：WO02053522A3
公开(公告)日：2004-01-08
申请号：PCT/EP0115230
申请日：2001-12-24
申请人： KAROBIO AB , MERCK & CO INC , KOEHLER KONRAD , HENSSEN CECILIA , NILSSON MARITA , GILLNER MIKAEL , LIU YE , SANIN ANDREI , WILKENING ROBERT R , RATCLIFFE RONALD W , WENSBO DAVID
发明人： KOEHLER KONRAD , HENSSEN CECILIA , NILSSON MARITA , GILLNER MIKAEL , LIU YE , SANIN ANDREI , WILKENING ROBERT R , RATCLIFFE RONALD W , WENSBO DAVID
IPC分类号： A61K31/343 , A61K31/05 , A61K31/10 , A61K31/122 , A61K31/15 , A61K31/352 , A61K31/357 , A61K31/385 , A61P3/02 , A61P3/04 , A61P3/06 , A61P5/30 , A61P9/00 , A61P9/10 , A61P15/08 , A61P19/00 , A61P19/08 , A61P19/10 , A61P25/28 , A61P35/00 , A61P37/02 , A61P43/00 , C07C35/37 , C07C35/44 , C07C39/17 , C07C39/42 , C07C49/727 , C07C49/737 , C07C49/747 , C07C251/44 , C07C323/17 , C07D307/94 , C07D311/96 , C07D317/72 , C07D339/06 , C07D339/08 , A61K31/045 , A61K31/39 , A61K31/557 , C07C43/315
CPC分类号： C07D317/72 , C07C39/17 , C07C39/42 , C07C49/747 , C07C251/44 , C07C323/17 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/16 , C07C2603/26 , C07C2603/96 , C07D307/94 , C07D311/96 , C07D339/06 , 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 inventive 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, gynecomastia, autoimmune disease, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer of the lung, colon, 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，潮热，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，男子女性生殖症，自身免疫性疾病，血管平滑肌细胞增殖，肥胖症，失禁和肺癌，结肠癌，乳腺癌，子宫癌和前列腺癌。

9. 发明申请

WO2003015761A1 SELECTIVE ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：选择性雌激素受体调节剂
公开(公告)号：WO2003015761A1
公开(公告)日：2003-02-27
申请号：PCT/US2002/025377
申请日：2002-08-09
申请人： MERCK & CO., INC. , MENG, Dongfang , PARKER, Dann, LeRoy, Jr. , RATCLIFFE, Ronald, W. , WILKENING, Robert, R.
发明人： MENG, Dongfang , PARKER, Dann, LeRoy, Jr. , RATCLIFFE, Ronald, W. , WILKENING, Robert, R.
IPC分类号： A61K31/135
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，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。

10. 发明申请

WO1998010761A1 CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴因抗菌化合物，含有这些化合物的组合物和处理方法
公开(公告)号：WO1998010761A1
公开(公告)日：1998-03-19
申请号：PCT/US1997016786
申请日：1997-09-09
申请人： MERCK & CO., INC. , CAMA, Lovji, D. , WILKENING, Robert, R. , RATCLIFFE, Ronald, W. , BLIZZARD, Timothy, A.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/425
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , 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 CH2 group. The naphthosultam 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：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯核在2-位被用CH2链连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式（I）表示。还包括药物组合物和使用方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式