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

WO2018063955A1 CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：色氨酸，异色烯和二氢异苯并呋喃衍生物作为mGluR2-阴离子调节剂，组合物和它们的用途
公开(公告)号：WO2018063955A1
公开(公告)日：2018-04-05
申请号：PCT/US2017/053155
申请日：2017-09-25
申请人： MERCK SHARP & DOHME CORP. , SEBHAT, Iyassu, K. , ARASAPPAN, Ashok , HOYT, Scott, B. , WILKENING, Robert, R. , DEMONG, Duane
发明人： SEBHAT, Iyassu, K. , ARASAPPAN, Ashok , HOYT, Scott, B. , WILKENING, Robert, R. , DEMONG, Duane
IPC分类号： C07D491/04 , C07D491/18 , A61K31/436 , A61P25/00
摘要： The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from (II), (III), (IV), and (V), and ring B, n, R 1 , R 2 , R 2A , R 3 , and R 3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
摘要翻译：本发明提供了式（I）的某些取代的苯并二氢吡喃，异苯并二氢吡喃和二氢异苯并呋喃化合物或其药学上可接受的盐，其中环A是选自（II），（III），（ IV）和（V）中，并且环B，n，R 1，R 2，R 2A，R 3，和R 3A如本文所定义。本发明化合物可用作mGluR2抑制剂或mGluR2阴变构调节剂（NAM），并且可用于治疗患者涉及其中涉及mGluR2-NAM受体的疾病或病症如阿尔茨海默病，认知通过给患者施用治疗有效量的本发明化合物或其药学上可接受的盐，减轻，轻度认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍。本发明还涉及包含本发明化合物或其药学上可接受的盐（任选与一种或多种另外的活性成分组合）和药学上可接受的载体的药物组合物，以及所述化合物和药物组合物本发明在治疗这些疾病中的应用。

2. 发明申请

WO2016029454A1 TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：作为mGluR2负离子调节剂，组合物及其使用的四氢萘啶衍生物
公开(公告)号：WO2016029454A1
公开(公告)日：2016-03-03
申请号：PCT/CN2014/085582
申请日：2014-08-29
申请人： MERCK SHARP & DOHME CORP. , ARASAPPAN, Ashok , BUNGARD, Christopher James , FRIE, Jessica L. , HAN, Yongxin , HOYT, Scott B. , MANLEY, Peter J. , MEISSNER, Robert S. , PERKINS, James , SEBHAT, Iyassu K. , WILKENING, Robert R.
发明人： ARASAPPAN, Ashok , BUNGARD, Christopher James , FRIE, Jessica L. , HAN, Yongxin , HOYT, Scott B. , MANLEY, Peter J. , MEISSNER, Robert S. , PERKINS, James , SEBHAT, Iyassu K. , WILKENING, Robert R.
IPC分类号： C07D471/04 , A61K31/4375 , A61P25/28 , A61P25/20 , A61P25/18
CPC分类号： C07D471/04 , A61K31/4375
摘要： Provided are quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , L, X 1 , X 2 , and X 3 , are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
摘要翻译：提供式（I）的喹啉羧酰胺和喹啉腈化合物或其药学上可接受的盐，其中R 1，R 2，L，X 1，X 2和X 3如本文所定义。本发明的化合物及其药学上可接受的盐和包含它们的药物组合物可用作非竞争性mGluR2拮抗剂或mGluR2负变构调节剂（NAM），并且可用于治疗有需要的人的方法其中mGluR2-NAM受体起作用的疾病或障碍，例如阿尔茨海默病，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍。

3. 发明申请

WO2011146358A1 SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：作为用于治疗糖尿病的DIPEPTIDYDEPDDIV-IV抑制剂的取代的七分子杂环化合物
公开(公告)号：WO2011146358A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/036589
申请日：2011-05-16
申请人： MERCK SHARP & DOHME CORP. , HICKS, Jacqueline, D. , BIFTU, Tesfaye , CHEN, Ping , QIAN, Xiaoxia , WILKENING, Robert, R.
发明人： HICKS, Jacqueline, D. , BIFTU, Tesfaye , CHEN, Ping , QIAN, Xiaoxia , WILKENING, Robert, R.
IPC分类号： C07D471/00
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06 , C07D471/04
摘要： The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式（I）的新型氨基取代的七元杂环化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防其中二肽基肽酶-IV酶涉及糖尿病，特别是2型糖尿病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

4. 发明申请

WO2010019203A8 ANTIFUNGAL AGENTS 审中-公开
标题翻译：反真菌药
公开(公告)号：WO2010019203A8
公开(公告)日：2011-03-17
申请号：PCT/US2009004557
申请日：2009-08-07
申请人： MERCK SHARP & DOHME , GREENLEE MARK L , WILKENING ROBERT , APGAR JAMES , WILDONGER KENNETH JAMES , MENG DONGFANG , PARKER DANN L JR
发明人： GREENLEE MARK L , WILKENING ROBERT , APGAR JAMES , WILDONGER KENNETH JAMES , MENG DONGFANG , PARKER DANN L JR
IPC分类号： A01N37/18
CPC分类号： A01N43/653 , A61K31/4196 , C07J71/0005
摘要： 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)-ß-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.
摘要翻译：本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这种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。所公开的化合物，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。

5. 发明申请

WO2010019204A1 ANTIFUNGAL AGENTS 审中-公开
标题翻译：反真菌药
公开(公告)号：WO2010019204A1
公开(公告)日：2010-02-18
申请号：PCT/US2009/004560
申请日：2009-08-07
申请人： MERCK SHARP & DOHME CORP. , SCYNEXIS, INC. , GREENLEE, Mark, L. , WILKENING, Robert , APGAR, James , SPERBECK, Donald , WILDONGER, Kenneth, James , MENG, Dongfang , PARKER, Dann, L. , PACOFSKY, Gregory, James , HEASLEY, Brian, Haid , MAMAI, Ahmed , NELSON, Kingsley
发明人： GREENLEE, Mark, L. , WILKENING, Robert , APGAR, James , SPERBECK, Donald , WILDONGER, Kenneth, James , MENG, Dongfang , PARKER, Dann, L. , PACOFSKY, Gregory, James , HEASLEY, Brian, Haid , MAMAI, Ahmed , NELSON, Kingsley
IPC分类号： A01N43/64 , A61K31/21 , A61K31/41
CPC分类号： A61K31/343 , A01N43/653 , A61K31/21 , A61K31/41 , C07D493/08 , C07D519/00
摘要： 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.
摘要翻译：本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这种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。所公开的化合物，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。

6. 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。

7. 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。

8. 发明申请

WO2014031515A1 NOVEL AZABENZIMIDAZOLE HEXAHYDROFURO[3,2-B]FURAN DERIVATIVES 审中-公开
标题翻译：新亚氨基二咪唑十氢呋喃[3,2-B]呋喃衍生物
公开(公告)号：WO2014031515A1
公开(公告)日：2014-02-27
申请号：PCT/US2013/055528
申请日：2013-08-19
申请人： MERCK SHARP & DOHME CORP. , APGAR, James, M. , ARASAPPAN, Ashok , BIFTU, Tesfaye , CHEN, Ping , FENG, Danqing , GUIDRY, Erin , HICKS, Jacqueline , KEKEC, Ahmet , LEAVITT, Kenneth , LI, Bing , MCCRACKEN, Troy , SEBHAT, Iyassu , QIAN, Xiaoxia , WEI, Lan , WILKENING, Robert , WU, Zhicai
发明人： APGAR, James, M. , ARASAPPAN, Ashok , BIFTU, Tesfaye , CHEN, Ping , FENG, Danqing , GUIDRY, Erin , HICKS, Jacqueline , KEKEC, Ahmet , LEAVITT, Kenneth , LI, Bing , MCCRACKEN, Troy , SEBHAT, Iyassu , QIAN, Xiaoxia , WEI, Lan , WILKENING, Robert , WU, Zhicai
IPC分类号： A61P3/10 , A61K31/4184 , A61K31/415 , A61K31/454
CPC分类号： C07D519/00 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/438 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

9. 发明申请

WO2014031441A1 NOVEL BENZIMIDAZOLE TETRAHYDROFURAN DERIVATIVES 审中-公开
标题翻译：新型苯并咪唑四氢呋喃衍生物
公开(公告)号：WO2014031441A1
公开(公告)日：2014-02-27
申请号：PCT/US2013/055166
申请日：2013-08-15
申请人： MERCK SHARP & DOHME CORP. , APGAR, James, M. , BIFTU, Tesfaye , CHEN, Ping , FENG, Danqing , HICKS, Jacqueline, D. , KEKEC, Ahmet , LEAVITT, Kenneth, J. , LI, Bing , SEBHAT, Iyassu , QIAN, Xiaoxia , WEI, Lan , WILKENING, Robert, R. , WU, Zhicai
发明人： APGAR, James, M. , BIFTU, Tesfaye , CHEN, Ping , FENG, Danqing , HICKS, Jacqueline, D. , KEKEC, Ahmet , LEAVITT, Kenneth, J. , LI, Bing , SEBHAT, Iyassu , QIAN, Xiaoxia , WEI, Lan , WILKENING, Robert, R. , WU, Zhicai
IPC分类号： A61P3/10 , A61K31/4184 , A61K31/415 , A61K31/454
CPC分类号： C07D417/14 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/427 , A61K31/4985 , A61K31/506 , A61K31/5377 , C07D405/12 , C07D405/14 , C07D413/14
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

10. 发明申请

WO2012116145A1 NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS 审中-公开
标题翻译：用作抗糖尿病药物的新型CYABAZABENZIMIDAZOLE衍生物
公开(公告)号：WO2012116145A1
公开(公告)日：2012-08-30
申请号：PCT/US2012/026261
申请日：2012-02-23
申请人： MERCK SHARP & DOHME CORP. , ANAND, Rajan , APGAR, James, M. , BIFTU, Tesfaye , CHEN, Ping , CHU, Lin , COLANDREA, Vincent, J. , DONG, Guizhen , DROPINSKI, James, F. , FENG, Danqing , HICKS, Jacqueline, D. , JIANG, Jinlong , KIM, Alexander, J. , LEAVITT, Kenneth, J. , LI, Bing , QIAN, Xiaoxia , SEBHAT, Iyassu , WEI, Lan , WILKENING, Robert, R. , WU, Zhicai
发明人： ANAND, Rajan , APGAR, James, M. , BIFTU, Tesfaye , CHEN, Ping , CHU, Lin , COLANDREA, Vincent, J. , DONG, Guizhen , DROPINSKI, James, F. , FENG, Danqing , HICKS, Jacqueline, D. , JIANG, Jinlong , KIM, Alexander, J. , LEAVITT, Kenneth, J. , LI, Bing , QIAN, Xiaoxia , SEBHAT, Iyassu , WEI, Lan , WILKENING, Robert, R. , WU, Zhicai
IPC分类号： A01N43/58
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译：结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。

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