公开(公告)号：WO2021026047A1

公开(公告)日：2021-02-11

申请号：PCT/US2020/044691

申请日：2020-08-03

Applicant: MERCK SHARP & DOHME CORP. ,  BOGEN, Stephane, L. ,  CHEN, Ping ,  CLAUSEN, Dane James ,  HAO, Jinsong ,  KALYANI, Dippanita ,  RUDD, Michael, T. ,  WALSH, Shawn, P. ,  WEI, Lan ,  YANG, Dexi

Inventor： BOGEN, Stephane, L. ,  CHEN, Ping ,  CLAUSEN, Dane James ,  HAO, Jinsong ,  KALYANI, Dippanita ,  RUDD, Michael, T. ,  WALSH, Shawn, P. ,  WEI, Lan ,  YANG, Dexi

IPC: C07D207/16 ,  C07D401/04 ,  C07D403/04

Abstract: The present invention is directed to heteroaryl pyrrolidine and piperidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

公开(公告)号：WO2012142085A1

公开(公告)日：2012-10-18

申请号：PCT/US2012/033017

申请日：2012-04-11

Applicant: MERCK SHARP & DOHME CORP. ,  GIRIJAVALLABHAN, Vinay ,  NJOROGE, F. George ,  BOGEN, Stephane ,  VERMA, Vishal ,  BENNETT, Frank ,  KEREKES, Angela ,  ARASAPPAN, Ashok ,  PISSARNITSKI, Dmitri ,  DANG, Qun ,  DAVIES, Ian ,  OLSEN, David, B. ,  STAMFORD, Andrew ,  VACCA, Joseph, P.

Inventor： GIRIJAVALLABHAN, Vinay ,  NJOROGE, F. George ,  BOGEN, Stephane ,  VERMA, Vishal ,  BENNETT, Frank ,  KEREKES, Angela ,  ARASAPPAN, Ashok ,  PISSARNITSKI, Dmitri ,  DANG, Qun ,  DAVIES, Ian ,  OLSEN, David, B. ,  STAMFORD, Andrew ,  VACCA, Joseph, P.

IPC: A01N43/08 ,  A61K31/34

CPC classification number: A61K31/7072 ,  A01N47/36 ,  A61K31/7042 ,  A61K31/7068 ,  A61K45/06 ,  A61P31/14 ,  C07H17/02 ,  C07H19/10 ,  C07H19/11 ,  C07H19/207 ,  C07H19/213 ,  A01N2300/00 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/76 ,  A01N43/82 ,  A01N43/84 ,  A01N43/90

Abstract: The present invention relates to 2'-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Substituted Nucleoside Derivative, and methods of using the 2'-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Abstract translation: 本发明涉及式（I）的2'-取代的核苷衍生物及其药学上可接受的盐，其中A，B，X，R 1，R 2和R 3如本文所定义。 本发明还涉及包含至少一种2'-取代的核苷衍生物的组合物，以及使用2'-取代的核苷衍生物治疗或预防患者HCV感染的方法。

公开(公告)号：WO2012142075A1

公开(公告)日：2012-10-18

申请号：PCT/US2012/032991

申请日：2012-04-11

Applicant: MERCK SHARP & DOHME CORP. ,  GIRIJAVALLABHAN, Vinay ,  NJOROGE, F. George ,  BOGEN, Stephane ,  BENNETT, Frank ,  VERMA, Vishal ,  ARASAPPAN, Ashok ,  CHEN, Kevin ,  HUANG, Ying ,  KEREKES, Angela ,  NAIR, Latha ,  PISSARNITSKI, Dmitri ,  DANG, Qun ,  DAVIES, Ian ,  OLSEN, David, B. ,  STAMFORD, Andrew ,  VACCA, Joseph, P.

Inventor： GIRIJAVALLABHAN, Vinay ,  NJOROGE, F. George ,  BOGEN, Stephane ,  BENNETT, Frank ,  VERMA, Vishal ,  ARASAPPAN, Ashok ,  CHEN, Kevin ,  HUANG, Ying ,  KEREKES, Angela ,  NAIR, Latha ,  PISSARNITSKI, Dmitri ,  DANG, Qun ,  DAVIES, Ian ,  OLSEN, David, B. ,  STAMFORD, Andrew ,  VACCA, Joseph, P.

IPC: C07H21/02

CPC classification number: C07H19/06 ,  A61K31/7056 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/708 ,  A61K45/06 ,  A61P31/14 ,  C07H19/10 ,  C07H19/11 ,  C07H19/12 ,  C07H19/16 ,  C07H19/20 ,  C07H19/207 ,  C07H19/213

Abstract: The present invention relates to 2'-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Azido Substituted Nucleoside Derivative, and methods of using the 2'-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Abstract translation: 本发明涉及式（I）的2'-叠氮基取代的核苷衍生物及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义。 本发明还涉及包含至少一种2'-叠氮基取代的核苷衍生物的组合物，以及使用2'-叠氮基取代的核苷衍生物治疗或预防患者HCV感染的方法。

公开(公告)号：WO2011046771A1

公开(公告)日：2011-04-21

申请号：PCT/US2010/051403

申请日：2010-10-05

Applicant: SCHERING CORPORATION ,  BOGEN, Stephane, L. ,  MA, Yao ,  WANG, Yaolin ,  LAHUE, Brian Robert ,  NAIR, Latha, G. ,  SHIZUKA, Manami ,  VOSS, Matthew Ernst ,  KIROVA-SNOVER, Margarita ,  PAN, Weidong ,  TIAN, Yuan ,  KULKARNI, Bheemashankar, A. ,  GIBEAU, Craig, R. ,  LIU, Yuan ,  SCAPIN, Giovanna ,  RINDGEN, Diane ,  DOLL, Ronald, J. ,  GUZI, Timothy, J. ,  HICKLIN, Danny, J. ,  NOMEIR, Amin ,  SEIDEL-DUGAN, Cynthia ,  SHIPPS, Gerald, W., Jr. ,  MACCOSS, Malcolm

Inventor： BOGEN, Stephane, L. ,  MA, Yao ,  WANG, Yaolin ,  LAHUE, Brian Robert ,  NAIR, Latha, G. ,  SHIZUKA, Manami ,  VOSS, Matthew Ernst ,  KIROVA-SNOVER, Margarita ,  PAN, Weidong ,  TIAN, Yuan ,  KULKARNI, Bheemashankar, A. ,  GIBEAU, Craig, R. ,  LIU, Yuan ,  SCAPIN, Giovanna ,  RINDGEN, Diane ,  DOLL, Ronald, J. ,  GUZI, Timothy, J. ,  HICKLIN, Danny, J. ,  NOMEIR, Amin ,  SEIDEL-DUGAN, Cynthia ,  SHIPPS, Gerald, W., Jr. ,  MACCOSS, Malcolm

IPC: A01N43/40 ,  A61K31/445

CPC classification number: C07D401/14 ,  C07D409/14

Abstract: The present invention provides a compound of Formula (1) as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

Abstract translation: 本发明提供本文所述的式（1）化合物或其药学上可接受的盐，溶剂合物或酯。 该化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

公开(公告)号：WO2008124148A3

公开(公告)日：2009-05-07

申请号：PCT/US2008004549

申请日：2008-04-08

Applicant: SCHERING CORP ,  VELAZQUEZ FRANCISCO ,  BOGEN STEPHANE L ,  ARASAPPAN ASHOK ,  VENKATRAMAN SRIKANTH ,  NJOROGE F GEORGE ,  SHIH NENG-YANG

Inventor： VELAZQUEZ FRANCISCO ,  BOGEN STEPHANE L ,  ARASAPPAN ASHOK ,  VENKATRAMAN SRIKANTH ,  NJOROGE F GEORGE ,  SHIH NENG-YANG

IPC: C07K5/08

CPC classification number: C07K5/0202 ,  A61K38/05 ,  C07D209/52 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07K5/06008 ,  C07K5/0804 ,  A61K2300/00

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract translation: 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。

公开(公告)号：WO2020167706A1

公开(公告)日：2020-08-20

申请号：PCT/US2020/017579

申请日：2020-02-11

Applicant: MERCK SHARP & DOHME CORP. ,  BOGEN, Stephane, L. ,  CLAUSEN, Dane James ,  GUIADEEN, Deodial Guy ,  RUDD, Michael, T. ,  YANG, Dexi

Inventor： BOGEN, Stephane, L. ,  CLAUSEN, Dane James ,  GUIADEEN, Deodial Guy ,  RUDD, Michael, T. ,  YANG, Dexi

IPC: A61P43/00 ,  A61K31/40 ,  A61K31/403 ,  C07D207/16 ,  C07D209/54

Abstract: The present invention is directed to 5-alkyl pyrrolidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

公开(公告)号：WO2017074914A1

公开(公告)日：2017-05-04

申请号：PCT/US2016/058614

申请日：2016-10-25

Applicant: MERCK SHARP & DOHME CORP. ,  WITTER, David, J. ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  BOGEN, Stephane, L. ,  HONG, Qingmei ,  HUANG, Chunhui ,  HUANG, Xianhai ,  LI, Bing ,  PARK, Min, K. ,  SLOMAN, David, L.

Inventor： WITTER, David, J. ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  BOGEN, Stephane, L. ,  HONG, Qingmei ,  HUANG, Chunhui ,  HUANG, Xianhai ,  LI, Bing ,  PARK, Min, K. ,  SLOMAN, David, L.

IPC: C07D487/04 ,  C07D487/12

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

Abstract translation: 本发明涉及作为一种或多种突变IDH酶抑制剂的式（I），（Ia）或（Ib）的三环化合物。 本发明还涉及这些三环化合物在潜在治疗或预防其中涉及一种或多种突变IDH酶的癌症中的用途。 本发明还涉及包含这些化合物的组合物。 本发明还涉及这些组合物在潜在预防或治疗这些癌症中的用途。

公开(公告)号：WO2014204831A1

公开(公告)日：2014-12-24

申请号：PCT/US2014/042463

申请日：2014-06-16

Applicant: MERCK SHARP & DOHME CORP. ,  BOGEN, Stephane ,  GIRIJAVALLABHAN, Vinay ,  TRUONG, Quang ,  CHEN, Ping ,  BENNETT, Frank ,  KEREKES, Angela ,  DANG, Qun ,  OLSEN, David, B. ,  DAVIES, Ian

Inventor： BOGEN, Stephane ,  GIRIJAVALLABHAN, Vinay ,  TRUONG, Quang ,  CHEN, Ping ,  BENNETT, Frank ,  KEREKES, Angela ,  DANG, Qun ,  OLSEN, David, B. ,  DAVIES, Ian

IPC: A61K31/66 ,  A61K31/712 ,  A61K31/7105

CPC classification number: C07H19/10 ,  A61K31/661 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06 ,  C07F9/65586 ,  C07F9/65744 ,  C07H19/11 ,  A61K2300/00

Abstract: The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

Abstract translation: 本发明涉及式（I）的环磷酸酯取代的核苷衍生物：（结构）及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义，以及使用 用于治疗或预防患者HCV感染的环磷酸酯取代的核苷衍生物。

公开(公告)号：WO2014100071A2

公开(公告)日：2014-06-26

申请号：PCT/US2013075917

申请日：2013-12-18

Applicant: MERCK SHARP & DOHME ,  DINSMORE CHRISTOPHER ,  FRADERA LLINAS FRANCESC XAVIER ,  KUDALE AMIT ASHOKRAO ,  MACHACEK MICHELLE ,  REUTERSHAN MICHAEL HALE ,  THOMPSON CHRISTOPHER FRANCIS ,  TROTTER B WESLEY ,  YANG LIPING ,  ALTMAN MICHAEL D ,  BOGEN STEPHANE L ,  DOLL RONALD J ,  VOSS MATTHEW E

Inventor： DINSMORE CHRISTOPHER ,  FRADERA LLINAS FRANCESC XAVIER ,  KUDALE AMIT ASHOKRAO ,  REUTERSHAN MICHAEL HALE ,  THOMPSON CHRISTOPHER FRANCIS ,  YANG LIPING ,  ALTMAN MICHAEL D ,  BOGEN STEPHANE L ,  DOLL RONALD J ,  VOSS MATTHEW E

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

Abstract translation: 本发明提供如本文所述的取代吡咯并嘧啶或其药学上可接受的盐或溶剂化物。 代表性化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

公开(公告)号：WO2013096150A1

公开(公告)日：2013-06-27

申请号：PCT/US2012/069996

申请日：2012-12-17

Applicant: MERCK SHARP & DOHME CORP. ,  MA, Yao ,  SHIZUKA, Manami ,  GUZI, Timothy, J. ,  LIU, Yuan ,  TIAN, Yuan ,  LAHUE, Brian, R. ,  GIBEAU, Craig, R. ,  SHIPPS, Gerald, W., Jr. ,  WANG, Yaolin ,  BOGEN, Stephane, L. ,  NAIR, Latha, G. ,  PAN, Weidong ,  VOSS, Matthew, E. ,  KIROVA-SNOVER, Margarita ,  CLAYTON, W. Brent ,  MCCOY, Mark, A.

Inventor： MA, Yao ,  SHIZUKA, Manami ,  GUZI, Timothy, J. ,  LIU, Yuan ,  TIAN, Yuan ,  LAHUE, Brian, R. ,  GIBEAU, Craig, R. ,  SHIPPS, Gerald, W., Jr. ,  WANG, Yaolin ,  BOGEN, Stephane, L. ,  NAIR, Latha, G. ,  PAN, Weidong ,  VOSS, Matthew, E. ,  KIROVA-SNOVER, Margarita ,  CLAYTON, W. Brent ,  MCCOY, Mark, A.

IPC: A61K31/497

CPC classification number: C07D495/04 ,  C07D409/14

Abstract: The present invention provides a compound of Formula I(The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

Abstract translation: 本发明提供如本文所述的式I化合物（该式应该在此插入）或其药学上可接受的盐或溶剂化物。 代表性化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。