公开(公告)号：US10766919B2

公开(公告)日：2020-09-08

申请号：US15886578

申请日：2018-02-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Brian Andresen ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Andrew Marc Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Rui Liang ,  Jongwon Lim ,  Hong Liu ,  Min Lu ,  Alan B. Northrup ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong ,  Shawn P. Walsh ,  Kake Zhao

IPC: A01N43/04 ,  A61K31/70 ,  C07H21/04 ,  C07H21/02 ,  A61K39/39 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  A61P35/00 ,  A61K31/7064 ,  A61K31/7084 ,  A61K31/708 ,  A61K31/706 ,  A61K31/7076

Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

公开(公告)号：US10047098B2

公开(公告)日：2018-08-14

申请号：US15527975

申请日：2015-11-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Xing Dai ,  Jared N. Cumming ,  Hong Liu ,  Jack D. Scott

IPC: A61K31/519 ,  C07D491/048 ,  C07D491/052

Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

公开(公告)号：US20170362248A1

公开(公告)日：2017-12-21

申请号：US15527975

申请日：2015-11-20

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Xing Dai ,  Jared N. Cumming ,  Hong Liu ,  Jack D. Scott

IPC: C07D491/052

CPC classification number: C07D491/052 ,  A61P25/16 ,  A61P25/28

Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

公开(公告)号：US20170044206A1

公开(公告)日：2017-02-16

申请号：US15234182

申请日：2016-08-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael D. Altman ,  Brian Michael Andresen ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Andrew Marc Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Rui Liang ,  Jongwon Lim ,  Hong Liu ,  Min Lu ,  Alan B. Northrup ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong ,  Shawn P. Walsh ,  Kake Zhao

IPC: C07H21/04 ,  C07H19/23 ,  C07H19/20 ,  C07H21/02 ,  A61K39/39

CPC classification number: C07H21/04 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7084 ,  A61K39/39 ,  A61P35/00 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  C07H21/02

Abstract: A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

Abstract translation: 一类通式（I），通式（I'）或通式（I“）的多环化合物，其中基团1，碱基2，Y，亚氨基，Xa，Xa1，Xb，Xb1，Xc，Xc1， Xd，Xd1，R1，R1a，R2，R2a，R3，R4，R4a，R5，R6，R6a，R7，R7a，R8和R8a在本文中定义，其可用作I型干扰素生产的电感器， 提供了STING活性剂，还提供了合成和使用化合物的方法。

公开(公告)号：US20160289207A1

公开(公告)日：2016-10-06

申请号：US15035255

申请日：2014-11-10

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Duane DeMong ,  Michael Miller ,  Hong Liu ,  Xing Dai ,  Thomas Greshock ,  Andrew Stamford ,  Ravi Nargund

IPC: C07D401/04 ,  C07D401/14

CPC classification number: C07D401/04 ,  C07D231/56 ,  C07D401/14

Abstract: The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. 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 LRRK-2 kinase is involved.

Abstract translation: 本发明涉及取代的吲唑化合物，其是LRRK2激酶的有效抑制剂并且可用于治疗或预防涉及LRRK2激酶的疾病，例如帕金森病。 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LRRK-2激酶的疾病中的用途。

公开(公告)号：US20150368246A1

公开(公告)日：2015-12-24

申请号：US14766487

申请日：2014-02-03

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Xing Dai ,  Hong Liu ,  Anandan Palani ,  Shuwen He ,  Zhong Lai ,  Ravi Nargund ,  Karen Marcantonio ,  Dong Xiao ,  Linda L. Brockunier ,  Nicolas Zorn ,  Qun Dang ,  Xuanjia Peng ,  Peng Li

IPC: C07D471/14 ,  C07D519/00 ,  C07D471/04 ,  A61K45/06 ,  A61K31/675 ,  C07D471/20 ,  A61K31/5377 ,  A61K31/519 ,  C07F9/6512

CPC classification number: C07D471/14 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/675 ,  A61K45/06 ,  C07D471/04 ,  C07D471/20 ,  C07D487/14 ,  C07D519/00 ,  C07F9/65128 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. I

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的用途的式I化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。 一世

公开(公告)号：US20140213571A1

公开(公告)日：2014-07-31

申请号：US14343450

申请日：2012-08-20

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Nigel J. Liverton ,  Casey Cameron McComas ,  Joerg Habermann ,  Uwe Koch ,  Frank Narjes ,  Peng Li ,  Xuanjia Peng ,  Richard Soll ,  Hao Wu ,  Anandan Palani ,  Shuwen He ,  Xing Dai ,  Hong Liu ,  Zhong Lai ,  Clare London ,  Dong Xiao ,  Nicolas Zorn ,  Ravi Nargund

IPC: A61K31/553 ,  A61K31/519 ,  A61K31/437 ,  A61K31/407 ,  C07D498/22 ,  C07D498/14 ,  C07D491/147 ,  C07D491/052 ,  A61K45/06 ,  A61K31/5365 ,  C07D498/04

CPC classification number: A61K31/553 ,  A61K31/407 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5365 ,  A61K45/06 ,  C07D491/052 ,  C07D491/147 ,  C07D498/04 ,  C07D498/14 ,  C07D498/22 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/395 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的式（I）化合物 并用于在基于细胞的系统中抑制HCV病毒复制和/或病毒生产。