公开(公告)号：US20150266897A1

公开(公告)日：2015-09-24

申请号：US14638733

申请日：2015-04-03

Applicant: Merck Sharp & Dohme Corp. ,  MSD Italia S.R.L.

Inventor： Nigel J. Liverton ,  Vincenzo Summa ,  Maria Emilia Di Francesco ,  Marco Ferrara ,  Kevin F. Gilbert ,  Steven Harper ,  John A. McCauley ,  Charles J. McIntyre ,  Alessia Petrocchi ,  Marco Pompei ,  Joseph J. Romano ,  Michael T. Rudd ,  John W. Butcher ,  M. Katharine Holloway

IPC: C07D498/22 ,  A61K31/437 ,  A61K31/439 ,  C07D498/08 ,  A61K31/407 ,  A61K31/4192 ,  C07D498/18 ,  A61K45/06

CPC classification number: C07D498/22 ,  A61K31/407 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/439 ,  A61K38/00 ,  A61K45/06 ,  C07D498/08 ,  C07D498/18 ,  C07K5/0804 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。

公开(公告)号：US09487504B2

公开(公告)日：2016-11-08

申请号：US14409147

申请日：2013-06-18

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： Jongwon Lim ,  Michael H. Reutershan ,  John Michael Ellis ,  Kaleen Konrad Childers ,  Anthony Donofrio ,  Michael D. Altman ,  Andrew M. Haidle ,  Anna Zabierek ,  Matthew Christopher ,  Jonathan Grimm ,  Jason Burch ,  Maria Emilia Di Francesco ,  Alessia Petrocchi ,  Christian Beaulieu ,  Vouy Linh Truong ,  Alan B. Northrup ,  Marc Blouin

IPC: C07D403/12 ,  C07D403/14 ,  C07D401/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14

Abstract: The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract translation: 本发明提供了式I的新型咪唑类似物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。

公开(公告)号：US20150175575A1

公开(公告)日：2015-06-25

申请号：US14409147

申请日：2013-06-18

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： Jongwon Lim ,  Michael H. Reutershan ,  John Michael Ellis ,  Kaleen Konrad Childers ,  Anthony Donofrio ,  Michael D. Altman ,  Andrew M. Haidle ,  Anna Zabierek ,  Matthew Christopher ,  Jonathan Grimm ,  Jason Burch ,  Maria Emilia Di Francesco ,  Alessia Petrocchi ,  Christian Beaulieu ,  Vouy Linh Truong ,  Alan B. Northrup ,  Marc Blouin

IPC: C07D403/12 ,  C07D401/14

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D403/14

Abstract: The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract translation: 本发明提供了式I的新型咪唑类似物，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。

公开(公告)号：US20140296203A1

公开(公告)日：2014-10-02

申请号：US14353381

申请日：2012-10-25

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Jongwon Lim ,  Elizabeth Helen Kelley ,  Joey L. Methot ,  Hua Zhou ,  Alessia Petrocchi ,  Faruk Mansoor ,  Christian Fischer ,  Brendan O'Boyle ,  David Joseph Guerin ,  Corey E. Bienstock ,  Christopher W. Boyce ,  Matthew H. Daniels ,  Danielle Falcone ,  Ronald D. Ferguson ,  Salem Fevrier ,  Xianhai Huang ,  Kathryn Ann Lipford ,  David L. Sloman ,  Kevin Wilson ,  Wei Zhou ,  David Witter ,  Milana M. Maletic ,  Phieng Siliphaivanh

IPC: C07D471/04 ,  A61K31/444 ,  A61K31/437 ,  A61K45/06 ,  A61K31/501 ,  A61K31/4709 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).

Abstract translation: 公开了式（1）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1）的化合物治疗癌症的方法。

公开(公告)号：US09670196B2

公开(公告)日：2017-06-06

申请号：US15105316

申请日：2014-12-18

Applicant: Merck Sharp & Dohme Corp.

Inventor： Thomas A. Miller ,  Alessia Petrocchi ,  Eric T. Romeo ,  Dilrukshi Vitharana ,  Solomon D. Kattar ,  Alan B. Northrup ,  Michael D. Altman ,  Neville J. Anthony

IPC: C07D417/12 ,  C07D417/14 ,  C07D413/12 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/517 ,  A61K31/519

CPC classification number: C07D417/12 ,  A61K31/437 ,  A61K31/444 ,  A61K31/517 ,  A61K31/519 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

公开(公告)号：US20160326156A1

公开(公告)日：2016-11-10

申请号：US15105316

申请日：2014-12-18

Applicant: Thomas A. MILLER ,  Alessia PETROCCHI ,  Eric T. ROMEO ,  Dilrukshi VITHARANA ,  Solomon D. KATTAR ,  Alan B. NORTHRUP ,  Michael D. ALTMAN ,  Neville J. ANTHONY ,  MERCK SHARP & DOHME CORP.

Inventor： Thomas A. Miller ,  Alessia Petrocchi ,  Eric T. Romeo ,  Dilrukshi Vitharana ,  Solomon D. Kattar ,  Alan B. Northrup ,  Michael D. Altman ,  Neville J. Anthony

IPC: C07D417/12 ,  C07D495/04 ,  A61K31/437 ,  C07D471/04 ,  A61K31/444 ,  C07D491/048 ,  A61K31/517 ,  A61K31/519

CPC classification number: C07D417/12 ,  A61K31/437 ,  A61K31/444 ,  A61K31/517 ,  A61K31/519 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04

Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

Abstract translation: 本发明提供了式（I）（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，环A和下标n 1，n 2和r如上定义 这里。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。