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1. 发明申请

WO2015089809A1 ANTIDIABETIC SUBSTITUTED HETEROARYL COMPOUNDS 审中-公开
标题翻译：抗生素替代异氟醚化合物
公开(公告)号：WO2015089809A1
公开(公告)日：2015-06-25
申请号：PCT/CN2013/090014
申请日：2013-12-19
申请人： MERCK SHARP & DOHME CORP. , HAGMANN, William K. , LI, Bing , SZEWCZYK, Jason W. , WANG, Bowei , PARKER, Dann , BLIZZARD, Timothy , JOSIEN, Hubert , BIJU, Purakkattle , CHOBANIAN, Harry , GUDE, Candido , NARGUND, Ravi P. , PIO, Barbara , DANG, Qun , LIN, Linus S. , HU, Bin , CUI, Mingxiang , CHEN, Zhengxia , DAI, Meibi , ZHANG, Zaihong , LV, Ying , TIAN, Lili
发明人： HAGMANN, William K. , LI, Bing , SZEWCZYK, Jason W. , WANG, Bowei , PARKER, Dann , BLIZZARD, Timothy , JOSIEN, Hubert , BIJU, Purakkattle , CHOBANIAN, Harry , GUDE, Candido , NARGUND, Ravi P. , PIO, Barbara , DANG, Qun , LIN, Linus S. , HU, Bin , CUI, Mingxiang , CHEN, Zhengxia , DAI, Meibi , ZHANG, Zaihong , LV, Ying , TIAN, Lili
IPC分类号： C07D213/30 , C07D401/04 , C07D409/04 , C07D487/04 , C07D405/12 , C07D405/14 , C07D401/12 , C07D401/14 , C07D493/04 , C07D451/02 , A61P3/04 , A61P3/06 , A61P3/10 , A61K31/435 , A61K31/4353 , A61K31/4427 , A61K31/44
CPC分类号： C07D493/04 , A61K31/437 , A61K31/438 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/4545 , A61K31/46 , A61K31/505 , A61K31/506 , A61K45/06 , C07D213/64 , C07D213/74 , C07D221/20 , C07D239/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D451/06 , C07D471/04
摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译：本发明涉及由式I表示的化合物及其药学上可接受的盐。式I化合物是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制由G蛋白偶联受体40介导的疾病。本发明的化合物可能是有用的在治疗2型糖尿病以及通常与该疾病有关的病症，包括肥胖症和脂质疾病，例如混合型或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。

2. 发明申请

WO2005123757A1 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2005123757A1
公开(公告)日：2005-12-29
申请号：PCT/US2005/019870
申请日：2005-06-07
申请人： MERCK & CO., INC. , BLIZZARD, Timothy, A. , GUDE, Candido
发明人： BLIZZARD, Timothy, A. , GUDE, Candido
IPC分类号： C07J1/00
CPC分类号： C07J1/00
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：本发明涉及化合物及其衍生物，它们的合成，以及它们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：骨丢失，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，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，炎症，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。

3. 发明申请

WO2015095256A1 ANTIDIABETIC SUBSTITUTED HETEROARYL COMPOUNDS 审中-公开
标题翻译：抗生素替代异氟醚化合物
公开(公告)号：WO2015095256A1
公开(公告)日：2015-06-25
申请号：PCT/US2014/070706
申请日：2014-12-17
申请人： MERCK SHARP & DOHME CORP. , HAGMANN, William, K. , LI, Bing , SZEWCZYK, Jason, W. , WANG, Bowei , PARKER, Dann , BLIZZARD, Timothy , JOSIEN, Hubert , BIJU, Purakkattle , CHOBANIAN, Harry , GUDE, Candido , NARGUND, Ravi, P. , PIO, Barbara , DANG, Qun , LIN, Linus, S. , HU, Bin , CUI, Mingxiang , CHEN, Zhengxia , DAI, Meibi , ZHANG, Zaihong , LV, Ying , TIAN, Lili
发明人： HAGMANN, William, K. , LI, Bing , SZEWCZYK, Jason, W. , WANG, Bowei , PARKER, Dann , BLIZZARD, Timothy , JOSIEN, Hubert , BIJU, Purakkattle , CHOBANIAN, Harry , GUDE, Candido , NARGUND, Ravi, P. , PIO, Barbara , DANG, Qun , LIN, Linus, S. , HU, Bin , CUI, Mingxiang , CHEN, Zhengxia , DAI, Meibi , ZHANG, Zaihong , LV, Ying , TIAN, Lili
IPC分类号： A61K31/192 , A61K31/381
CPC分类号： C07D493/04 , A61K31/437 , A61K31/438 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/4545 , A61K31/46 , A61K31/505 , A61K31/506 , A61K45/06 , C07D213/64 , C07D213/74 , C07D221/20 , C07D239/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D451/06 , C07D471/04
摘要： The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译：本发明涉及由式（I）表示的化合物及其药学上可接受的盐。式I化合物是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制由G蛋白偶联受体40介导的疾病。本发明的化合物可能是有用的在治疗2型糖尿病以及通常与该疾病有关的病症，包括肥胖症和脂质疾病，例如混合型或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。

4. 发明申请

WO2006081152A3 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2006081152A3
公开(公告)日：2007-02-08
申请号：PCT/US2006002148
申请日：2006-01-20
申请人： MERCK & CO INC , BLIZZARD TIMOTHY A , GUDE CANDIDO
发明人： BLIZZARD TIMOTHY A , GUDE CANDIDO
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/00
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 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，男子母性发育，血管平滑肌细胞增殖，肥胖，失禁，炎症，炎性肠病和癌症，特别是乳腺癌，子宫癌和前列腺癌。

5. 发明申请

WO2006012333A1 ESTROGEN RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2006012333A1
公开(公告)日：2006-02-02
申请号：PCT/US2005/022564
申请日：2005-06-24
申请人： MERCK & CO., INC. , BLIZZARD, Timothy, A. , GUDE, Candido
发明人： BLIZZARD, Timothy, A. , GUDE, Candido
IPC分类号： C07J1/00
CPC分类号： C07J1/00
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.

6. 发明申请

WO2005051972A1 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2005051972A1
公开(公告)日：2005-06-09
申请号：PCT/US2004/038860
申请日：2004-11-19
申请人： MERCK & CO., INC. , BLIZZARD, Timothy, A. , GUDE, Candido , MORGAN, Jerry, D., II
发明人： BLIZZARD, Timothy, A. , GUDE, Candido , MORGAN, Jerry, D., II
IPC分类号： C07J1/00
CPC分类号： C07J41/0094 , C07J1/00 , C07J1/0022
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。

7. 发明申请

WO2015112465A1 ISOQUINOLINE DERIVATIVES AS MGAT2 INHIBITORS 审中-公开
标题翻译：异喹啉衍生物作为MGAT2抑制剂
公开(公告)号：WO2015112465A1
公开(公告)日：2015-07-30
申请号：PCT/US2015/011939
申请日：2015-01-20
申请人： MERCK SHARP & DOHME CORP. , BERGER, Richard , BLIZZARD, Timothy, A. , CAMPBELL, Brian, T. , CHEN, Helen, Y. , DEBENHAM, John, S. , DEWNANI, Sunita, V. , DUBOIS, Byron , GUDE, Candido , GUO, Zhiqiang , HARPER, Bart , HU, Zhiyong , LIN, Songnian , LIU, Ping , WANG, Ming , UJJAINWALLA, Feroze , XU, Jiayi , XU, Libo , ZHANG, Rui
发明人： BERGER, Richard , BLIZZARD, Timothy, A. , CAMPBELL, Brian, T. , CHEN, Helen, Y. , DEBENHAM, John, S. , DEWNANI, Sunita, V. , DUBOIS, Byron , GUDE, Candido , GUO, Zhiqiang , HARPER, Bart , HU, Zhiyong , LIN, Songnian , LIU, Ping , WANG, Ming , UJJAINWALLA, Feroze , XU, Jiayi , XU, Libo , ZHANG, Rui
IPC分类号： C07D471/04
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/14 , C07D471/04
摘要： The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
摘要翻译：式I化合物作为MGAT2抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

8. 发明申请

WO2015073342A1 ANTIDIABETIC TRICYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2015073342A1
公开(公告)日：2015-05-21
申请号：PCT/US2014/064722
申请日：2014-11-10
申请人： MERCK SHARP & DOHME CORP. , BIFTU, Tesfaye , BIJU, Purakkattle , COLLETTI, Steven, L. , DANG, Qun , DHONDI, Pawan, K. , GUDE, Candido , JOSIEN, Hubert , KAR, Nam Fung , NAIR, Anilkumar, G. , NARGUND, Ravi, P. , YANG, De-Yi , XIAO, Dong , ZHU, Cheng
发明人： BIFTU, Tesfaye , BIJU, Purakkattle , COLLETTI, Steven, L. , DANG, Qun , DHONDI, Pawan, K. , GUDE, Candido , JOSIEN, Hubert , KAR, Nam Fung , NAIR, Anilkumar, G. , NARGUND, Ravi, P. , YANG, De-Yi , XIAO, Dong , ZHU, Cheng
IPC分类号： C07D221/16
CPC分类号： C07D221/16 , A61K9/20 , A61K31/435 , A61K31/444 , A61K31/4545 , A61K45/06 , C07D401/12 , C07D487/04 , C07D487/10
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

9. 发明申请

WO2013028474A1 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL 审中-公开
标题翻译：肾脏外部药物通道的抑制剂
公开(公告)号：WO2013028474A1
公开(公告)日：2013-02-28
申请号：PCT/US2012/051195
申请日：2012-08-16
申请人： MERCK SHARP & DOHME CORP. , PASTERNAK, Alexander , BLIZZARD, Timothy , CHOBANIAN, Harry , DE JESUS, Reynalda , DING, Fa-Xiang , DONG, Shuzhi , GUDE, Candido , KIM, Dooseop , TANG, Haifeng , WALSH, Shawn , PIO, Barbara , JIANG, Jinlong
发明人： PASTERNAK, Alexander , BLIZZARD, Timothy , CHOBANIAN, Harry , DE JESUS, Reynalda , DING, Fa-Xiang , DONG, Shuzhi , GUDE, Candido , KIM, Dooseop , TANG, Haifeng , WALSH, Shawn , PIO, Barbara , JIANG, Jinlong
IPC分类号： A61K31/497
CPC分类号： C07D498/04 , A61K31/4985 , A61K31/5383 , A61K31/542 , A61K31/553 , A61K45/06 , C07D487/04 , C07D513/04
摘要： The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
摘要翻译：本发明提供式Ia化合物及其药学上可接受的盐，它们是ROMK（Kir1.1）通道的抑制剂。该化合物可以用作利尿剂和/或利尿钠剂，并且用于治疗和预防包括心血管疾病如高血压，心力衰竭以及与过量盐和保水有关的病症的医学病症。

10. 发明申请

WO2009091856A3 BETA-LACTAMASE INHIBITORS 审中-公开
标题翻译： BETA-LACTAMASE抑制剂
公开(公告)号：WO2009091856A3
公开(公告)日：2009-12-03
申请号：PCT/US2009031047
申请日：2009-01-15
申请人： MERCK & CO INC , BLIZZARD TIMOTHY A , CHEN HELEN , GUDE CANDIDO , HERMES JEFFREY D , IMBRIGLIO JASON E , KIM SEONGKON , WU JANE Y , HA SOOKHEE , MORTKO CHRISTOPHER J , MANGION IAN , RIVERA NELO , RUCK REBECCA T , SHEVLIN MICHAEL
发明人： BLIZZARD TIMOTHY A , CHEN HELEN , GUDE CANDIDO , HERMES JEFFREY D , IMBRIGLIO JASON E , KIM SEONGKON , WU JANE Y , HA SOOKHEE , MORTKO CHRISTOPHER J , MANGION IAN , RIVERA NELO , RUCK REBECCA T , SHEVLIN MICHAEL
IPC分类号： C07D471/08 , A61K31/529 , A61K31/535 , A61P31/04 , C07D487/08 , C07D519/00
CPC分类号： C07D471/08 , C07D211/58 , C07D211/60 , C07D211/78 , C07D487/08 , C07D519/00
摘要： Substituted bicyclic beta-lactams of Formula I: (I), are ß-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ß-lactam antibiotics. In particular, the compounds can be employed with a ß-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ß-lactam antibiotics due to the presence of the ß-lactamases.
摘要翻译：式I的取代的双环β-内酰胺：（I）是β-内酰胺酶抑制剂，其中a，X，R 1和R 2在本文中定义。化合物及其药学上可接受的盐可用于治疗细菌感染与β-内酰胺抗生素的组合。特别地，由于β-内酰胺酶的存在，这些化合物可以与β-内酰胺抗生素（例如亚胺培南，哌拉西林或头孢他啶）一起用于抗β-内酰胺抗生素的微生物。

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