公开(公告)号：US20170037056A1

公开(公告)日：2017-02-09

申请号：US15104257

申请日：2014-12-16

Applicant: Xing DAI ,  Jared N. CUMMING ,  Jack D. SCOTT ,  Hong LIU ,  Anandan PALANI ,  MERCK SHARP & DOHME CORP.

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

IPC: C07D513/04 ,  C07D471/04 ,  C07D285/36 ,  C07D417/12

CPC classification number: C07D513/04 ,  C07D285/36 ,  C07D417/12 ,  C07D471/04

Abstract: In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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.

Abstract translation: 或其互变异构体和所述化合物和所述互变异构体的药学上可接受的盐，其中RN，R1A，R1B，R2，R3，R4，环A，RA，m，-L1-和RL如本文所定义。 本发明的新化合物可用作BACE抑制剂，并且可用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

公开(公告)号：US09440952B2

公开(公告)日：2016-09-13

申请号：US14772589

申请日：2014-02-27

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael Miller ,  Kallol Basu ,  Duane DeMong ,  Jack Scott ,  Hong Liu ,  Xing Dai ,  Joel M. Harris ,  Bernard Neustadt ,  Andrew Stamford ,  Marc Poirier ,  John A. McCauley ,  Thomas Greshock ,  Heather Stevenson ,  John Sanders ,  Jonathan Kern

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D451/02 ,  C07D487/10 ,  C07D491/04 ,  C07D491/08 ,  C07D491/056 ,  C07D498/04 ,  C07D498/08 ,  C07D403/04 ,  C07D491/10 ,  C07D487/04 ,  C07D491/107 ,  C07D491/113

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/056 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04 ,  C07D498/08

Abstract: The present invention is directed to 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.

公开(公告)号：US09364482B2

公开(公告)日：2016-06-14

申请号：US14898768

申请日：2014-06-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： Xing Dai ,  Hong Liu ,  Anandan Palani ,  Shuwen He ,  Ravi Nargund ,  Dong Xiao ,  Nicolas Zorn ,  Qun Dang ,  Casey C. McComas ,  Xuanjia Peng ,  Peng Li ,  Richard Soll

IPC: A61K31/65 ,  A61K31/519 ,  A61K31/517 ,  A61K31/437 ,  A61K31/4725 ,  A61K31/06 ,  C07D498/04 ,  C07D471/04 ,  C07D405/04 ,  C07D475/02 ,  C07D405/14 ,  A61K31/5365 ,  A61K31/53 ,  A61K45/06

CPC classification number: A61K31/5365 ,  A61K31/437 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D475/02 ,  C07D498/04

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：US20160009681A1

公开(公告)日：2016-01-14

申请号：US14772525

申请日：2014-02-27

Applicant: Michael MILLER ,  Kallol BASU ,  Duane MONG ,  Jack SCOTT ,  Hong LIU ,  Xing DAI ,  Andrew STAMFORD ,  Marc POIRIER ,  Paul TEMPEST ,  MERCK SHARP & DOHME CORP.

Inventor： Michael Miller ,  Kallol Basu ,  Duane DeMong ,  Jack Scott ,  Hong Liu ,  Xing Dai ,  Andrew Stamford ,  Marc Poirier ,  Paul Tempest

IPC: C07D401/04 ,  C07D498/08 ,  C07D401/14 ,  C07D495/08 ,  C07D498/04 ,  C07D487/04 ,  C07D413/14 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D495/08 ,  C07D498/04 ,  C07D498/08

Abstract: The present invention is directed to 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 LRRK2 kinase is involved.

Abstract translation: 本发明涉及作为LRRK2激酶的有效抑制剂的吲唑化合物，可用于治疗或预防其中涉及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LRRK2激酶的疾病中的用途。

公开(公告)号：US11377438B2

公开(公告)日：2022-07-05

申请号：US16669598

申请日：2019-10-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ashok Arasappan ,  Ian M. Bell ,  Michael J. Breslin ,  Christopher James Bungard ,  Christopher S. Burgey ,  Harry R. Chobanian ,  Jason M. Cox ,  Anthony T. Ginnetti ,  Deodial Guy Guiadeen ,  Kristen L. G. Jones ,  Mark E. Layton ,  Hong Liu ,  Jian Liu ,  James J. Perkins ,  Shawn J. Stachel ,  Linda M. Suen-Lai ,  Zhe Wu

IPC: C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

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：US09745324B2

公开(公告)日：2017-08-29

申请号：US15104257

申请日：2014-12-16

Applicant: Merck Sharp & Dohme Corp.

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

IPC: C07D513/04 ,  C07D417/12 ,  C07D471/04 ,  C07D285/36

CPC classification number: C07D513/04 ,  C07D285/36 ,  C07D417/12 ,  C07D471/04

Abstract: In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful 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：US09718818B2

公开(公告)日：2017-08-01

申请号：US14912761

申请日：2014-08-18

Applicant: MERCK SHARP & DOHME CORP. ,  Duane DeMong ,  Thomas J. Greshock ,  Ronald K. Chang ,  Xing Dai ,  Hong Liu ,  John A. McCauley ,  Wei Li ,  Kallol Basu ,  Jack D. Scott ,  Michael Miller

Inventor： Duane DeMong ,  Thomas J. Greshock ,  Ronald K. Chang ,  Xing Dai ,  Hong Liu ,  John A. McCauley ,  Wei Li ,  Kallol Basu ,  Jack D. Scott ,  Michael Miller

IPC: A61K31/44 ,  C07D471/04 ,  C07D498/04 ,  C07D519/00 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00

Abstract: The present invention is directed to azaindazole 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.

公开(公告)号：US09688654B2

公开(公告)日：2017-06-27

申请号：US14772525

申请日：2014-02-27

Applicant: Merck Sharp & Dohme Corp.

Inventor： Michael Miller ,  Kallol Basu ,  Duane DeMong ,  Jack Scott ,  Hong Liu ,  Xing Dai ,  Andrew Stamford ,  Marc Poirier ,  Paul Tempest

IPC: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D495/08 ,  C07D498/04 ,  C07D498/08

CPC classification number: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D495/08 ,  C07D498/04 ,  C07D498/08

Abstract: The present invention is directed to 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 LRRK2 kinase is involved.

公开(公告)号：US09493461B2

公开(公告)日：2016-11-15

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 ,  C07D471/04 ,  C07F9/6512 ,  A61K31/5377 ,  A61K31/675 ,  C07D471/20 ,  A61K31/519 ,  A61K45/06 ,  C07D519/00 ,  C07D487/14

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.