-
1.发明申请SUBSTITUTED AMINOTETRAHYDROTHIOPYRANS AND DERIVATIVES THEREOF AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES 审中-公开作为用于治疗糖尿病的DIPIPTIDYP PEPTIDASE-IV抑制剂的替代氨苄西泮糖苷衍生物及其衍生物
公开(公告)号：WO2011103256A1
公开(公告)日：2011-08-25
申请号：PCT/US2011/025182
申请日：2011-02-17
Applicant: MERCK SHARP & DOHME CORP. , WILKENING, Robert, R. , APGAR, James, M. , BIFTU, Tesfaye , FENG, Danqing , QIAN, Xiaoxia , WEI, Lan
Inventor： WILKENING, Robert, R. , APGAR, James, M. , BIFTU, Tesfaye , FENG, Danqing , QIAN, Xiaoxia , WEI, Lan
CPC classification number: C07D487/04 , C07D335/02 , C07D498/04 , C07B2200/07
Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof 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.
Abstract translation: 本发明涉及作为二肽基肽酶-IV酶的抑制剂的结构式（I）的新型取代的氨基四氢硫代吡喃及其衍生物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 如糖尿病，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。
-
公开(公告)号：WO2018140368A1
公开(公告)日：2018-08-02
申请号：PCT/US2018/014761
申请日：2018-01-23
Applicant: MERCK SHARP & DOHME CORP. , YU, Tao , MCCAULEY, John, A. , WHITEHEAD, Alan , APGAR, James, M. , RAHEEM, Izzat, T. , DONG, Guizhen , WADDELL, Sherman, T. , LI, Hong
Inventor： YU, Tao , MCCAULEY, John, A. , WHITEHEAD, Alan , APGAR, James, M. , RAHEEM, Izzat, T. , DONG, Guizhen , WADDELL, Sherman, T. , LI, Hong
IPC: C07D455/00 , A61K31/4375 , C07D491/147
Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
-
公开(公告)号：WO2019209667A1
公开(公告)日：2019-10-31
申请号：PCT/US2019/028432
申请日：2019-04-22
Applicant: MERCK SHARP & DOHME CORP. , YU, Tao , APGAR, James, M. , WHITEHEAD, Alan , ZHANG, Yonglian , HU, Zhiyong , SHURTLEFF, Valerie, W. , MCCAULEY, John, A. , RAHEEM, Izzat, T.
Inventor： YU, Tao , APGAR, James, M. , WHITEHEAD, Alan , ZHANG, Yonglian , HU, Zhiyong , SHURTLEFF, Valerie, W. , MCCAULEY, John, A. , RAHEEM, Izzat, T.
IPC: A61K31/4985 , C07D487/16
Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
-
公开(公告)号：WO2014031468A1
公开(公告)日：2014-02-27
申请号：PCT/US2013/055246
申请日：2013-08-16
Applicant: MERCK SHARP & DOHME CORP. , APGAR, James, M. , ARASAPPAN, Ashok , BIFTU, Tesfaye , CHEN, Ping , FENG, Danqing , GUIDRY, Erin , HICKS, Jacqueline, D. , KEKEC, Ahmet , LEAVITT, Kenneth, J. , LI, Bing , SEBHAT, Iyassu , QIAN, Xiaoxia , WEI, Lan , WILKENING, Robert, R. , WU, Zhicai
Inventor： APGAR, James, M. , ARASAPPAN, Ashok , BIFTU, Tesfaye , CHEN, Ping , FENG, Danqing , GUIDRY, Erin , HICKS, Jacqueline, D. , KEKEC, Ahmet , LEAVITT, Kenneth, J. , LI, Bing , SEBHAT, Iyassu , QIAN, Xiaoxia , WEI, Lan , WILKENING, Robert, R. , WU, Zhicai
IPC: A01N43/50 , A61K31/4184
CPC classification number: C07D493/04 , A61K31/366 , A61K31/397 , A61K31/4184 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/454 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K45/06 , A61K2300/00
Abstract: The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention 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.
Abstract translation: 本发明的新型苯并咪唑六氢呋喃并[3,2-B]呋喃衍生物是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。
-
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
Applicant: 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
Inventor： 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: A61P3/10 , A61K31/4184 , A61K31/415 , A61K31/454
CPC classification number: C07D519/00 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/438 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
Abstract: 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.
Abstract translation: 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。
-
Patent Agency Ranking
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
Applicant: 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
Inventor： 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: A61P3/10 , A61K31/4184 , A61K31/415 , A61K31/454
CPC classification number: 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
Abstract: 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.
Abstract translation: 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。
-
7.发明申请NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS 审中-公开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
Applicant: 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
Inventor： 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: A01N43/58
CPC classification number: 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
Abstract: 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.
Abstract translation: 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。
-
公开(公告)号：WO2016064982A1
公开(公告)日：2016-04-28
申请号：PCT/US2015/056627
申请日：2015-10-21
Applicant: MERCK SHARP & DOHME CORP. , YOUNG, Katherine , OLSEN, David, B. , SINGH, Sheo, B. , SU, Jing , WILKENING, Robert, R. , APGAR, James, M. , MENG, Dongfang , PARKER, Dann , MANDAL, Mihir , YANG, Lihu , PAINTER, Ronald, E. , DANG, Qun , SUZUKI, Takao
Inventor： YOUNG, Katherine , OLSEN, David, B. , SINGH, Sheo, B. , SU, Jing , WILKENING, Robert, R. , APGAR, James, M. , MENG, Dongfang , PARKER, Dann , MANDAL, Mihir , YANG, Lihu , PAINTER, Ronald, E. , DANG, Qun , SUZUKI, Takao
IPC: C07D493/10
CPC classification number: C07D493/08 , C07C53/18 , C07C309/06 , C07D493/18 , C07D519/00 , C07F7/1856
Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis . The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
Abstract translation: 本发明涉及能够抑制DnaE并对结核分枝杆菌具有抗菌性，特别是抗分支杆菌活性的新型的nargenicin相关化合物。 本发明还涉及抑制分枝杆菌细胞生长的方法，以及通过施用抗分泌杆菌有效量的高泛度蛋白酶或与其相关的化合物和/或其药学上可接受的盐来治疗结核分枝杆菌的分枝杆菌感染的方法。
-
公开(公告)号：WO2016061772A1
公开(公告)日：2016-04-28
申请号：PCT/CN2014/089204
申请日：2014-10-22
Applicant: MERCK SHARP & DOHME CORP. , YOUNG, Katherine , OLSEN, David B. , SINGH, Sheo B. , SU, Jing , WILKENING, Robert R. , APGAR, James M. , MENG, Dongfang , PARKER, Dann , MANDAL, Mihir , YANG, Lihu , PAINTER, Ronald E. , DANG, Qun , SUZUKI, Takao
Inventor： YOUNG, Katherine , OLSEN, David B. , SINGH, Sheo B. , SU, Jing , WILKENING, Robert R. , APGAR, James M. , MENG, Dongfang , PARKER, Dann , MANDAL, Mihir , YANG, Lihu , PAINTER, Ronald E. , DANG, Qun , SUZUKI, Takao
IPC: C07D493/04 , A61K31/343 , A61P31/04
CPC classification number: C07D493/08 , C07C53/18 , C07C309/06 , C07D493/18 , C07D519/00 , C07F7/1856
Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterialactivity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
Abstract translation: 本发明涉及能够抑制DnaE并对结核分枝杆菌具有抗菌性，特别是抗分枝杆菌活性的新型的与腺苷酸相关的化合物。 本发明还涉及抑制分枝杆菌细胞生长的方法，以及通过施用抗分泌杆菌有效量的高泛度蛋白酶或与其相关的化合物和/或其药学上可接受的盐来治疗结核分枝杆菌的分枝杆菌感染的方法。
-
公开(公告)号：WO2014031517A1
公开(公告)日：2014-02-27
申请号：PCT/US2013/055531
申请日：2013-08-19
Applicant: 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 , ARASAPPAN, Ashok
Inventor： 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 , ARASAPPAN, Ashok
IPC: A61P3/10 , A61K31/4184 , A61K31/415 , A61K31/454
CPC classification number: C07D471/04 , A61K31/19 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/4985 , A61K31/5377 , C07C53/18 , C07D519/00 , A61K2300/00
Abstract: 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.
Abstract translation: 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。
-
-
-
-
-
-
-
-
-
Search Results
12
records
(took 0.023 seconds)
