公开(公告)号：US20180230178A1

公开(公告)日：2018-08-16

申请号：US15752144

申请日：2016-08-11

Applicant: Michael D. ALTMAN ,  Brian ANDRESEN ,  Wonsuk CHANG ,  Matthew Lloyd CHILDERS ,  Jared N. CUMMING ,  Andrew Marc HAIDLE ,  Timothy J. HENDERSON ,  James P. JEWELL ,  Min LU ,  Alan B. NORTHRUP ,  Ryan D. OTTE ,  Tony SIU ,  Benjamin Wesley TROTTER ,  Quang T TRUONG ,  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 ,  Min Lu ,  Alan B. Northrup ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Quang T. Truong

IPC: C07H21/04 ,  C07H21/02 ,  C07H19/23 ,  C07H19/20 ,  A61P35/00

Abstract: A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, 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：US20210206796A1

公开(公告)日：2021-07-08

申请号：US16771814

申请日：2018-12-17

Applicant: Brian M. ANDRESEN ,  Frank BENNETT ,  Wonsuk CHANG ,  Matthew Lloyd CHILDERS ,  Jared N. CUMMING ,  Jongwon LIM ,  Min LU ,  Benjamin Wesley TROTTER ,  Wen-Lian WU ,  Merck Sharp & Dohme Corp.

Inventor： Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

IPC: C07H21/00 ,  A61P37/04

Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a and R9 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：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：US20190337918A1

公开(公告)日：2019-11-07

申请号：US16513417

申请日：2019-07-16

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael D. Altman ,  Brandon D. Cash ,  Wonsuk Chang ,  Jared N. Cumming ,  Andrew M. Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Matthew A. Larsen ,  Rui Liang ,  Jongwon Lim ,  Min Lu ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Sriram Tyagarajan

IPC: C07D333/60 ,  C07D498/04 ,  C07D333/62 ,  C07D409/12

Abstract: Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 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 of the disclosure.

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：US11685761B2

公开(公告)日：2023-06-27

申请号：US16771814

申请日：2018-12-17

Applicant: Merck Sharp & Dohme Corp. ,  Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

Inventor： Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

IPC: C07H21/00 ,  A61P37/04 ,  C07H21/02 ,  A61K31/7084 ,  C07H21/04

CPC classification number: C07H21/00 ,  A61K31/7084 ,  A61P37/04 ,  C07H21/02 ,  C07H21/04 ,  C07B2200/07

Abstract: A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 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：US20200369657A1

公开(公告)日：2020-11-26

申请号：US16334605

申请日：2017-09-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： Jason Eugene Imbriglio ,  Whitney Lane Petrilli ,  Yusheng Xiong ,  Zhe Feng ,  Hyewon Youm ,  Wonsuk Chang ,  Rui Liang ,  Zhijian Lu ,  Jerry Andrew Taylor ,  Scott B. Hoyt

IPC: C07D417/12 ,  G01N33/58

Abstract: The present invention relates to PCSK9 allosteric binding compounds of Formula I: (Formula (I)) and pharmaceutically acceptable salts thereof wherein X1, X2, Y, R1, R2, RA, RB and n are as defined herein. The present invention also relates to compositions which comprise an allosteric binding compound of the invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The invention further relates, inter alia, to methods for inducing PCSK9 protein degradation in a subject, and methods for treating atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions, comprising administering to a subject an effective amount of a compound or a pharmaceutically acceptable salt of the invention. The invention also provides a means for the in vitro labeling, detection and/or quantification of PCSK9 in biological samples.

公开(公告)号：US20180244712A1

公开(公告)日：2018-08-30

申请号：US15886568

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

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：US20180093964A1

公开(公告)日：2018-04-05

申请号：US15722093

申请日：2017-10-02

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael D. Altman ,  Brandon D. Cash ,  Wonsuk Chang ,  Jared N. Cumming ,  Andrew M. Haidle ,  Timothy J. Henderson ,  James P. Jewell ,  Matthew A. Larsen ,  Rui Liang ,  Jongwon Lim ,  Min Lu ,  Ryan D. Otte ,  Tony Siu ,  Benjamin Wesley Trotter ,  Sriram Tyagarajan

IPC: C07D333/60 ,  C07D333/62 ,  C07D409/12 ,  C07D498/04

CPC classification number: C07D333/60 ,  C07D333/62 ,  C07D409/12 ,  C07D498/04

Abstract: Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 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 of the disclosure.

公开(公告)号：US11542505B1

公开(公告)日：2023-01-03

申请号：US17047271

申请日：2019-04-15

Applicant: Merck Sharp & Dohme Corp. ,  Craig A. Parish ,  Hongwu Wang ,  Wonsuk Chang ,  Quang T. Truong ,  Tony Siu ,  Anne Mai Wassermann

Inventor： Craig A. Parish ,  Hongwu Wang ,  Wonsuk Chang ,  Quang T. Truong ,  Tony Siu ,  Anne Mai Wassermann

IPC: C12N15/113 ,  C07H21/02

Abstract: This invention provides compositions, compounds, and uses thereof, wherein said compounds comprise a single strand oligonucleotide that may form a short oligonucleotide hairpin or stem loop molecule with self complementary base pairing of less than 12 base pairs that bind to RIG-I and activate the RIG-I pathway.