公开(公告)号：WO2022056051A1

公开(公告)日：2022-03-17

申请号：PCT/US2021/049545

申请日：2021-09-09

Applicant: MERCK SHARP & DOHME CORP. ,  OGAWA, Anthony Ken ,  SINZ, Christopher, J. ,  HICKS, Jacqueline, D. ,  CHENG, Alan, C. ,  YANG, Song ,  BAO, Jianming ,  HAYES, Donna, A. A. W. ,  LANG, Simon, B. ,  TIAN, Maoqun ,  JABRI, Salman ,  SHEARN-NANCE, Galen Paul ,  KUANG, Rongze ,  ZHAO, Zhiqiang ,  WU, Zhicai

Inventor： OGAWA, Anthony Ken ,  SINZ, Christopher, J. ,  HICKS, Jacqueline, D. ,  CHENG, Alan, C. ,  YANG, Song ,  BAO, Jianming ,  HAYES, Donna, A. A. W. ,  LANG, Simon, B. ,  TIAN, Maoqun ,  JABRI, Salman ,  SHEARN-NANCE, Galen Paul ,  KUANG, Rongze ,  ZHAO, Zhiqiang ,  WU, Zhicai

IPC: A61K31/4155 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：WO2022055877A2

公开(公告)日：2022-03-17

申请号：PCT/US2021/049277

申请日：2021-09-07

Applicant: MERCK SHARP & DOHME CORP. ,  PISSARNITSKI, Dmitri, A. ,  FENG, Danqing ,  HUO, Pei ,  KEKEC, Ahmet ,  LIN, Songnian ,  NARGUND, Ravi ,  SHI, Zhicai ,  WU, Zhicai ,  YAN, Lin ,  ZHU, Yuping

Inventor： PISSARNITSKI, Dmitri, A. ,  FENG, Danqing ,  HUO, Pei ,  KEKEC, Ahmet ,  LIN, Songnian ,  NARGUND, Ravi ,  SHI, Zhicai ,  WU, Zhicai ,  YAN, Lin ,  ZHU, Yuping

IPC: A61K38/28 ,  C07K14/62 ,  A61P3/10 ,  A61K47/60 ,  A61K38/00 ,  A61K47/55

Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

公开(公告)号：WO2022046739A1

公开(公告)日：2022-03-03

申请号：PCT/US2021/047304

申请日：2021-08-24

Applicant: MERCK SHARP & DOHME CORP. ,  MADSEN-DUGGAN, Christina, B. ,  FENG, Danqing ,  HUO, Pei ,  KEKEC, Ahmet ,  LIN, Songnian ,  NARGUND, Ravi ,  MOYES, Christopher, R. ,  PISSARNITSKI, Dmitri, A. ,  SHI, Zhicai ,  WU, Zhicai ,  YAN, Lin ,  ZHU, Yuping

Inventor： MADSEN-DUGGAN, Christina, B. ,  FENG, Danqing ,  HUO, Pei ,  KEKEC, Ahmet ,  LIN, Songnian ,  NARGUND, Ravi ,  MOYES, Christopher, R. ,  PISSARNITSKI, Dmitri, A. ,  SHI, Zhicai ,  WU, Zhicai ,  YAN, Lin ,  ZHU, Yuping

IPC: C07K14/62 ,  A61P3/10

Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

公开(公告)号：WO2018093716A1

公开(公告)日：2018-05-24

申请号：PCT/US2017/061281

申请日：2017-11-13

Applicant: MERCK SHARP & DOHME CORP. ,  HICKS, Jacqueline, D. ,  MCKITTRICK, Brian Alexander ,  WHITEHEAD, Brent, R. ,  LOMBARDO, Matthew ,  HAN, Xiaoqing ,  TAYLOR, Jerry ,  CHU, Hong Dong ,  SO, Sung-Sau ,  ORTH, Peter ,  WU, Zhicai

Inventor： HICKS, Jacqueline, D. ,  MCKITTRICK, Brian Alexander ,  WHITEHEAD, Brent, R. ,  LOMBARDO, Matthew ,  HAN, Xiaoqing ,  TAYLOR, Jerry ,  CHU, Hong Dong ,  SO, Sung-Sau ,  ORTH, Peter ,  WU, Zhicai

IPC: A61K31/4184 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61P7/02

Abstract: The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.

公开(公告)号：WO2014081618A1

公开(公告)日：2014-05-30

申请号：PCT/US2013/070212

申请日：2013-11-15

Applicant: MERCK SHARP & DOHME CORP. ,  CHOBANIAN, Harry ,  BIFTU, Tesfaye ,  PIO, Barbara ,  WU, Zhicai

Inventor： CHOBANIAN, Harry ,  BIFTU, Tesfaye ,  PIO, Barbara ,  WU, Zhicai

IPC: A61K31/165 ,  A61K31/401 ,  A61P7/02

CPC classification number: C07D207/16 ,  C07D207/34 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06

Abstract: The invention includes substituted azetidinyl and pyrrolidinyl compounds, as thrombin inhibitors, for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal. The compounds can be added to blood, blood products, or mammalian organs in order to effect the desired inhibitions.

Abstract translation: 本发明包括取代的氮杂环丁烷基和吡咯烷基化合物作为凝血酶抑制剂，用于抑制血小板的损失，抑制血小板聚集体的形成，抑制纤维蛋白的形成，抑制血栓的形成和抑制哺乳动物的栓塞形成。 可以将化合物加入到血液，血液制品或哺乳动物器官中以实现所需的抑制作用。

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：WO2009151800A1

公开(公告)日：2009-12-17

申请号：PCT/US2009/041766

申请日：2009-04-27

Applicant: MERCK & CO., INC. ,  YANG, Cangming ,  WU, Zhicai ,  LIANG, Rui ,  COLLETTI, Steven, L.

Inventor： YANG, Cangming ,  WU, Zhicai ,  LIANG, Rui ,  COLLETTI, Steven, L.

IPC: A01N43/40

CPC classification number: C07D213/74 ,  C07D237/20 ,  C07D241/20 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12

Abstract: Compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof is disclosed. The compounds are useful for treating diabetes, inflammation, atherosclerosis, hypertension, pain and the like. Pharmaceutical compositions and methods of use are also included.

Abstract translation: 公开了式（I）化合物或其药学上可接受的盐或溶剂合物。 该化合物可用于治疗糖尿病，炎症，动脉粥样硬化，高血压，疼痛等。 还包括药物组合物和使用方法。

公开(公告)号：WO2006036395A3

公开(公告)日：2007-12-21

申请号：PCT/US2005029941

申请日：2005-08-19

Applicant: MERCK & CO INC ,  BILODEAU MARK T ,  COSFORD NICHOLAS D P ,  HARTNETT JOHN C ,  LIANG JUN ,  MANLEY PETER J ,  NEILSON LOU ANNE ,  SIU TONY ,  WU ZHICAI ,  LI YIWEI

Inventor： BILODEAU MARK T ,  COSFORD NICHOLAS D P ,  HARTNETT JOHN C ,  LIANG JUN ,  MANLEY PETER J ,  NEILSON LOU ANNE ,  SIU TONY ,  WU ZHICAI ,  LI YIWEI

IPC: A61K31/519 ,  A61K31/397 ,  C07D225/04 ,  C07D403/14 ,  C07D471/14 ,  C07D487/14

CPC classification number: C07D471/04

Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract translation: 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代的5-去氮萘啶部分的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

公开(公告)号：WO03092595A2

公开(公告)日：2003-11-13

申请号：PCT/US0313353

申请日：2003-04-28

Applicant: MERCK & CO INC ,  BILODEAU MARK T ,  FRALEY MARK E ,  WU ZHICAI

Inventor： BILODEAU MARK T ,  FRALEY MARK E ,  WU ZHICAI

IPC: A61K31/09 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/551 ,  A61K31/575 ,  A61K31/737 ,  A61K38/00 ,  A61K38/21 ,  A61P17/00 ,  A61P19/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  C07D471/04 ,  A61K

CPC classification number: C07D471/04

Abstract: The present invention relates to imidazopyridine compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

Abstract translation: 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的咪唑并吡啶化合物，其含有这些化合物的组合物，及其用于治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长， 动脉粥样硬化，年龄相关性黄斑变性，糖尿病性视网膜病变，炎症性疾病等。

公开(公告)号：WO2021257353A1

公开(公告)日：2021-12-23

申请号：PCT/US2021/036706

申请日：2021-06-10

Applicant: MERCK SHARP & DOHME CORP. ,  JABRI, Salman ,  OGAWA, Anthony, Ken ,  SINZ, Christopher, J. ,  HICKS, Jacqueline, D. ,  CHENG, Alan, C. ,  GAO, Ying-Duo ,  YANG, Song ,  BAO, Jianming ,  HAYES, Donna, A., A., W. ,  LANG, Simon, B. ,  TAOKA, Brandon, M. ,  TIAN, Maoqun ,  SHEARN-NANCE, Galen, Paul ,  KUANG, Rongze ,  LOMBARDO, Matthew, J. ,  WU, Zhicai ,  ZHAO, Zhiqiang

Inventor： JABRI, Salman ,  OGAWA, Anthony, Ken ,  SINZ, Christopher, J. ,  HICKS, Jacqueline, D. ,  CHENG, Alan, C. ,  GAO, Ying-Duo ,  YANG, Song ,  BAO, Jianming ,  HAYES, Donna, A., A., W. ,  LANG, Simon, B. ,  TAOKA, Brandon, M. ,  TIAN, Maoqun ,  SHEARN-NANCE, Galen, Paul ,  KUANG, Rongze ,  LOMBARDO, Matthew, J. ,  WU, Zhicai ,  ZHAO, Zhiqiang

IPC: A61K31/4155 ,  C07D401/14 ,  A61P7/02

Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.